DESCRIPTION TRICYCLIC HETEROCYCLIC COMPOUNDS AND JAK INHIBITORS TECHNICAL FIELD The present invention relates to novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities. BACKGROUND ART The JAK (Janus kinase) family is a tyrosine kinase family consisting of four members, JAK1 , JAK2, JAK3 and Tyk2 (Tyrosine kinase 2) and plays an important role in cytokine signaling. While the kinases of this family, except for JAK3, are widely expressed in tissues, expression of JAK3 is restricted to immune cells. This is consistent with the fact that JAK3 plays an important role in various receptor-mediated signaling pathways such as IL (interleukin)-2, IL-4, IL-7, IL-9, IL-1 5 and IL-21 signaling by noncovalently associating with the common chain (Non-Patent Documents 1 and 2). Lowered JAK3 protein levels or defects in the common chain gene observed in patients with an immunodeficiency called X-linked Severe Combined Immuno Defficiency (XSCID) suggest that blocking of the JAK3 signaling pathway leads to immunosuppression (Non-Patent Documents 3 and 4). Animal experiments indicate the importance of JAK3 not only in maturation of B- and T-lymphocytes but also in maintenance of T-lymphocyte functions. Therefore, regulation of immune responses via this mechanism is a promising therapy for T-cell lymph oproliferative diseases such as organ transplant rejection and autoimmune diseases. Analyses of JAK1 knockout mice and JAK1 -deficient cells suggest involvement of JAK1 in various receptor-mediated signaling pathways such as IFN (Interferon)a, IFNp, IFNy, IL-2, IL-4, IL-6, IL-7 and IL-1 5 signaling (Non-Patent Document 5). Therefore, regulation of inflammatory responses via these signaling pathways is therapeutically promising for treatment of diseases involving macrophage and lymphocyte activation such as autoimmune diseases and acute and chronic organ transplant rejection. Analyses of JAK2 knockout mice and JAK2-deficient cells suggest involvement of JAK2 in various receptor-mediated signaling pathways such as EPO (Erythropoietin) a, thrombopoietin, IFNy, IL-3 and GM-CSF signaling (Non-Patent Documents 6, 7 and 8). These signaling pathways are supposed to mediate differentiation of erythrocyte or thrombocyte progenitor cells in bone marrow. Meanwhile, it is suggested that a substitution of phenylalanine-617 with valine in JAK2 is associated with myeloproliferative diseases (Non-Patent Document 6). Therefore, regulation of differentiation of myeloid progenitor cells via these signaling pathways is therapeutically promising for treatment of myeloproliferative diseases. The JAK inhibitor CP-690,550 is reported to have improved the pathology of rheumatoid arthritis and psoriasis in clinical tests (Non-Patent Documents 9 and 10) and suppressed rejection in a monkey model of kidney transplantation and airway inflammation in a murine asthma model (Non-Patent Documents 11 and 12). From these findings, immunosuppression by JAK inhibitors is considered to be useful for prevention or treatment of organ transplant rejection and post-transplant graft-versushost reaction, autoimmune diseases and allergic diseases. Although other compounds having JAK inhibitory action than CP-690,550 have been reported (Patent Documents 1 t o11), development of more of such compounds is demanded. PRIOR ART DOCUMENT Patent Document 1 WO01/42246 Patent Document 2 WO2008/084861 Patent Document 3 WO201 0/1 19875 Patent Document 4 WO201 1/045702 Patent Document 5 WO201 1/068881 Patent Document 6 WO201 1/075334 Patent Document 7 WO2007/00791 9 Patent Document 8 WO2007/077949 Patent Document 9 WO2009/152133 Patent Document 10 WO201 1/086053 Patent Document 11: WO20 11/068899 Non-Patent Document 1 Cell, 2002, 109, pp. S121-131 Non-Patent Document 2 Science, 2002, 298, pp., 1630-1 634 Non-Patent Document 3 Nature, 1995, 377, pp. 65-68 Non-Patent Document 4 Science, 1995, 270, pp. 797-800 Non-Patent Document 5 J. Immunol., 2007, 178, pp. 2623-2629 Non-Patent Document 6 Pathol. Biol., 2007, 55, pp. 88-91 Non-Patent Document 7 Cancer Genet. Cytogenet., 2009, 189, pp. 43-47 Non-Patent Document 8 Semin. Cell. Dev. Biol., 2008, 19, pp. 385-393 Non-Patent Document 9 Arthritis Rheum., 2009, 60, pp. 1895-1 905 Non-Patent Document 0 J. Invest. Dermatol., 2009, 129, pp. 2299-2302 Non-Patent Document 11: Science, 2003, 302, pp. 875-878 Non-Patent Document 12 Eur. J. Pharmacol., 2008, 582, pp. 154-1 6 1 DISCLOSURE OF THE INVENTION TECHNICAL PROBLEM The object of the present invention is to provide novel drug compounds having excellent JAK inhibitory activities useful for prevention or treatment of autoimmune diseases, inflammatory diseases and allergic diseases. SOLUTION TO PROBLEMS As a result of their extensive research in search of new low-molecular-weight compounds having JAK inhibitory activities, the present inventors found that the compounds of the present invention have high inhibitory action and accomplished the present invention. Namely, the present invention provide: ( 1) A compound represented by the formula (la): [wherein the ring Aa is represented by the following formula (lla-1) or the formula (lla-2): ( IIa-l ) ( -2 ) (wherein T a is a nitrogen atom or C R a , U1a is a nitrogen atom or C R 5a , T a is a single bond or C R aR 8a , and E2a is an oxygen atom or a sulfur atom), Xa is a nitrogen atom or C R 9a , Ya is C R 0a , R a is a hydrogen atom, a halogen atom, a C -6 alkyl group or a C -6 haloalkyl group, the ring Ba is a C 3 .n cycloalkane, a C 3- cycloalkene (a ring-constituting methylene group of the C3- cycloalkane and the C 3 cycloalkene may be replaced by a carbonyl group), a 3 to 14-membered non-aromatic heterocycle, a C 6- aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L a is a single bond, a C -6 alkylene group, a C 2-6 alkenylene group or a C2 -6 alkynylene group (the C -6 alkylene group, the C 2.6 alkenylene group and the C-2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L2a is a single bond, a C i -6 alkylene group, a C 2 -6 alkenylene group, a C-2-6 alkynylene group (the C -6 alkylene group, the C 2 -6 alkenylene group and the C 2 6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), =C(R 15a ) - (wherein R 5a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L2a is a double bond) or =C(R 5a)-CH 2- (wherein R 15a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L2a is a double bond), L3a is a single bond or represented by any of the following formulae (lll a-1) to (lll a-20) and the formula (Xlll a) : ( IIIa- ) ( IIIa-9 ) ( IIIa-10 ( IIIa-ll ) ( IIIa-17 ) ( IIIa-18 ) ( IIIa-19 ) ( IIIa-20 ) (wherein E1 is an oxygen atom, a sulfur atom or NR11a) , when L3a is a single bond, R a is a hydrogen atom, a halogen atom, an azido group, a C3-11 cycloalkyl group, a 3 to 14-membered non-aromatic heterocyclyl group, a C6 - 14 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 14-membered partially saturated aromatic cyclic group or a 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3- cycloalkyl group, the 3 to 14-membered nonaromatic heterocyclyl group, the C6 - 14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 14-membered partially saturated aromatic cyclic group and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of the substituent set V4a, substituent set V9a and C -6 alkyl groups (the C1-6 alkyl groups are substituted with a C -6 alkoxycarbonylamino group (the C1-6 alkoxycarbonylamino group is unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms))), when L3a is not a single bond, R a is a hydrogen atom, a Ci-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group (the C -6 alkyl group the C2-6 alkenyl group and the C2 -6 alkynyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V6a and the substituent set V9a) , a C 3. cycloalkyl group, a 3 to 14-membered non-aromatic heterocyclyl group, a C 6 -14 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 14-membered partially saturated aromatic cyclic group or a 8 to 14-membered aromatic ringcondensed alicydic hydrocarbon group (the C3.11 cycloalkyl group, the 3 to 14- membered non-aromatic heterocyclyl group, the C e-14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 14-membered partially saturated aromatic cyclic group and the 8 to 14-membered aromatic ring-condensed alicydic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) , na is 0, 1 or 2, R3a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a sulfamoyl group, a phosphono group, a phosphonooxy group, a sulfo group, a sulfoxy group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C 1-6 alkyl group, a C 1-6 haloalkyl group, a C 3-11 cycloalkyl group, a C 2 -6 alkenyl group, a C 2 -6 haloalkenyl group, a Ci-6 alkoxy group, a Ci-6 haloalkoxy group, a -6alkylthio group, a C -6 haloalkylthio group, a C -6 alkylcarbonyl group, a C i-6 haloalkylcarbonyl group, a C - 6 alkylsulfonyl group, a C -6 haloalkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-Ci -6 alkylamino group, a di-Ci -6 alkylamino group, a mono-Ci-6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group or a C -6 alkylcarbonylamino group (when na is 2, R3a's may be identical or different), each of R4a, R5a, R a and R a is independently a hydrogen atom, a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a C -6 alkyl group, a C 2 -6 alkenyl group, a C -6 alkoxy group, a C i-6 alkylthio group, a C 1-6 alkylcarbonyl group, a C 1-6 alkylsulfonyl group, a mono-Ci -6 alkylamino group, a di-Ci -6 alkylamino group (the C -6 alkyl group, the C 2-6 alkenyl group, the C 1-6 alkoxy group, the C -6 alkylthio group, the C -6 alkylcarbonyl group, the C i-6 alkylsulfonyl group, the mono-Ci -6 alkylamino group and the di-Ci -6 alkylamino group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , a C i-6 alkoxycarbonyl group, a C 3 - 11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C 6- 4 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3 -n cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C 6 - 4 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , R6a is a hydrogen atom, a C -6 alkyl group, a C 2-6 alkenyl group, a C 1-6 alkylcarbonyl group, a C 6 alkylsulfonyl group, a C i-6 alkoxycarbonyl group, a mono-Ci -6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group (the C 1-6 alkyl group, the C 2-6 alkenyl group, the C 1-6 alkylcarbonyl group, the C -6 alkylsulfonyl group, the C 6 alkoxycarbonyl group, the mono-Ci -6 alkylaminocarbonyl group and the di-Ci -6 alkylaminocarbonyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , a C 3 1 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C -14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3.11 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C e-14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , each of R 9 a and R 0 a is independently a hydrogen atom, a halogen atom, a cyano group, a carbamoyl group, a -6alkyl group, a C -6 haloalkyl group, a C 3 - cycloalkyl group, a C -6 alkoxy group, a C -6 haloalkoxy group, a C -6 alkylthio group, a C -6 alkylcarbonyl group, a C-i-e alkylsulfonyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C 6 - aryl group or a 5 to 10-membered aromatic heterocyclyl group, R 11a is a hydrogen atom, a hydroxy group, a cyano group, a nitro group, a C -6 alkyl group or a C -6 alkoxy group, each of R a , R 3 a and R 14a is independently a hydrogen atom, a C -6 alkyl group, a C i -6 haloalkyl group (the C -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a, the substituent set V and the substituent set V a) , a C 3. cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a Ce-u aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 14-membered partially saturated aromatic cyclic group or a 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3-11 cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C e-14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 14-membered partially saturated aromatic cyclic group and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) , the substituent set V1a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C 1-6 alkyl groups, C -6 haloalkyl groups, C3-11 cycloalkyl groups, C 2 -6 alkenyl groups, C-2-6 haloalkenyl groups, C -6 alkoxy groups, C- -6 haloalkoxy groups, C 1 6 alkylthio groups, . 6 haloalkylthio groups, C -6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, C 6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, 3 to 1 1 - membered non-aromatic heterocyclyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci- 6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups and C i - alkylcarbonylamino groups, the substituent set V2a consists of the groups in the substituent set V1a and C 6 - 14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C e- aryl groups and 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , the substituent set V3a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkoxy groups, C -6 haloalkoxy groups, C -6 alkylthio groups, C -6 haloalkylthio groups, C -6 alkylcarbonyl groups, Ci- 6 haloalkylcarbonyl groups, C 1-6 alkylsulfonyl groups, C 1-6 haloalkylsulfonyl groups, C i -6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups, C 3 - n cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C e- aryl groups and 5 to 10- membered aromatic heterocyclyl groups (the C 3 - cycloalkyl groups, the 3 to 11- membered non-aromatic heterocyclyl groups, the C 6 - u aryl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , the substituent set V4 consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkyl groups, C 2-6 alkenyl groups, -6 alkoxy groups, C 1-6 alkylthio groups, C -6 alkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci-6 alkylamino groups, di- -6alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di- -6alkylaminocarbonyl groups, C - alkylcarbonylamino groups (the C -6 alkyl groups, the C-2-6 alkenyl groups, the d -6 alkoxy groups, the C -6 alkylthio groups, the C -6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-d -6 alkylaminocarbonyl groups and the C -6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3a) , C 3 - cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C6-14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 3- cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C 6 - aryl group and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , the substituent set V a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, d-6 alkoxy groups, C -6 alkylthio groups, C -6 alkylcarbonyl groups, d-6 alkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-d-6 alkylamino groups, di-Ci-6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups, C3-11 cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C6-14 aryl group and 5 to 10-membered aromatic heterocyclyl groups (the Ci- 6 alkoxy groups, the Ci- 6 alkylthio groups, the Ci- 6 alkylcarbonyl groups, the C 1-6 alkylsulfonyl groups, the Ci- 6 alkoxycarbonyl groups, the mono-Ci-6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di- C -6 alkylaminocarbonyl groups, the C -6 alkylcarbonylamino groups, the C3-11 cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C e-14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3a) , the substituent set V a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkoxy groups, C -6 alkylthio groups, Ci- 6 alkylcarbonyl groups, Ci- 6 alkylsulfonyl groups, C 1-6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci-6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups (the C -6 alkoxy groups, the C -6 alkylthio groups, the C 6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the d .6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the d -6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C e-14 aryl groups, 5 to 10-membered aromatic heterocyclyl groups, 8 to 14-membered partially saturated aromatic cyclic groups and 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups (the C3.11 cycloalkyl groups, the 3 to 1 1-membered nonaromatic heterocyclyl groups, the C e-1 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups, the 8 to 14-membered partially saturated aromatic cyclic groups and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) , the substituent set V a consists of C 3 - cycloalkyl groups, 3 to 11-membered nonaromatic heterocyclyl groups (the C 3 -n cycloalkyl groups and 3 to 11-membered nonaromatic heterocyclyl groups are substituted with one or more identical or different substituent independently selected from the substituent set V a) , 8 to 14-membered partially saturated aromatic cyclic groups and 8 to 14-membered aromatic ringcondensed alicyclic hydrocarbon groups (the 8 to 14-membered partially saturated aromatic cyclic groups and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , and the substituent set V9a consists of mono-d -6 alkylaminosulfonyl groups, di-Ci -6 alkylaminosulfonyl groups, C i -6 alkylsulfonylamino groups, C 1-6 alkoxycarbonylamino groups (the mono-Ci-6 alkylaminosulfonyl groups, the di-Ci -6 alkylaminosulfonyl groups the C -6 alkylsulfonylamino groups and the C -6 alkoxycarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3a) , C 3-6 cycloalkoxy groups, C 3 .6 cycloalkylamino groups, C 3-6 cycloalkylthio groups, C 3-6 cycloalkylcarbonyl groups and C 3 6 cycloalkylsulfonyl groups (the C 3-6 cycloalkoxy groups, the C 3-6 cycloalkylamino groups, the C 3 -6 cycloalkylthio groups, the C 3 6 cycloalkylcarbonyl groups and the C 3-6 cycloalkylsulfonyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a)], a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. , which is represented by the formula (la) : [wherein the ring A is represented by the following formula (lla-1) or the formula (lla-2): ( I I a-l ) ( I I a-2 ) (wherein T a is a nitrogen atom or CR4a, U a is a nitrogen atom or a CR5a, T2a is a single bond or CR7aR8a , E2a is an oxygen atom or a sulfur atom), Xa is a nitrogen atom or CR9a, Ya is CR 0a, R a is a hydrogen atom, a halogen atom, a C -6 alkyl group or a -- haloalkyl group, the ring Ba is a C3- cycloalkane, a C3-n cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a Ce-14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L a is a single bond, a C -6 alkylene group, a C2-6 alkenylene group or a C2 -6 alkynylene group (the C i -6 alkylene group, the C 2-6 alkenylene group and the C 2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L a is a single bond, a C 1-6 alkylene group, a C 2 -6 alkenylene group or a C 2 -6 alkynylene group (the C -6 alkylene group, the C 2 -6 alkenylene group and the C2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L3a is a single bond or represented by any of the following formulae (lll a-1) to (lll a-20) ( III a-3 ) ( I I I ) ( III a-5 ) ( III a-6 ) ( III a-7 ) ( III a-8 ) ( III a-12 ) ( III a-13 ) ( III a-14 ) ( XXIa-15 ) ( III a-16 ) ( III a-17 ) ( I I I 8 ) ( III a-19 ) ( III a-20 ) (wherein E1a is an oxygen atom, a sulfur atom or NR1 a) , when L a is a single bond, R2a is a hydrogen atom, a halogen atom, a C3.11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C6 - 14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3-11 cycloalkyl group, the 3 to 1 1 - membered non-aromatic heterocyclyl group, the C6 -14 aryl group and the 5 to 10- membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a) , when L3a is not a single bond, R2a is a hydrogen atom, a C -6 alkyl group, a C2 -6 alkenyl group (the C -6 alkyl group and the C2 -6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5a) , a C3.11 cycloalkyl group, a 3 to 1 -membered non-aromatic heterocyclyl group, a C6-14 y group or a 5 to 10-membered aromatic heterocyclyl group (the C3.11 cycloalkyl group, the 3 to 1 -membered non-aromatic heterocyclyl group, the C6-14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a), na is 0 , 1 or 2 , R3a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a sulfamoyl group, a phosphono group, a phosphonooxy group, a sulfo group, a sulfoxy group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C 1-6 alkyl group, a Ci-6 haloalkyl group, a C3-11 cycloalkyl group, a C2-6 alkenyl group, a C2 -e haloalkenyl group, a Ci.6 alkoxy group, a C1-6 haloalkoxy group, a C 1-6 alkylthio group, a C-1-6 haloalkylthio group, a -6 alkylcarbonyl group, a C -6 haloalkylcarbonyl group, a C - 6 alkylsulfonyl group, a C -6 haloalkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-Ci-6 alkylamino group, a di-Ci-e alkylamino group, a mono-Ci-6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group or a C -6 alkylcarbonylamino group (when na is 2 , R a's may be identical or different), each of R a, R5a, R a and R8a is independently a hydrogen atom, a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a C -6 alkyl group, a C 2 -6 alkenyl group, a C -6 alkoxy group, a C -6 alkylthio group, a Ci-6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a mono-Ci -6 alkylamino group, a di-Ci -6 alkylamino group (the C -6 alkyl group, the C2-6 alkenyl group, the C1-6 alkoxy group, the C i -6 alkylthio group, the C -6 alkylcarbonyl group, the C i -6 alkylsulfonyl group, the mono-Ci -6 alkylamino group and the di-Ci -6 alkylamino group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , a C - alkoxycarbonyl group, a C 3 - cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a C e- aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3.11 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C 6 -14 aryl group and the 5 to 1Q-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , R6a is a hydrogen atom, a C -6 alkyl group, a C2-6 alkenyl group, a C 1-6 alkylcarbonyl group, a Ci-6 alkylsulfonyl group, a C1-6 alkoxycarbonyl group, a mono-Ci-6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group (the Ci-6 alkyl group, the C 2 -6 alkenyl group, the C1-6 alkylcarbonyl group, the C 1-6 alkylsulfonyl group, the C - alkoxycarbonyl group, the mono-Ci-6 alkylaminocarbonyl group and the di-Ci -6 alkylaminocarbonyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3a) , a C3-11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a Ce-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3 - cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C 6 - 14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , each of R9a and R 0a is independently a hydrogen atom, a halogen atom, a cyano group, a carbamoyl group, a Ci-6 alkyl group, a C -6 haloalkyl group, a C 3 -n cycloalkyl group, a C -6 alkoxy group, a C -6 haloalkoxy group, a C -6 alkylthio group, a C i -6 alkylcarbonyl group, a Ci-6 alkylsulfonyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a Ce-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group, R a is a hydrogen atom, a hydroxy group, a cyano group, a nitro group, a C 1-6 alkyl group or a C i -6 alkoxy group, each of R 2a, R13a and R14a is independently a hydrogen atom, a C 6 alkyl group or a Ci- 6 haloalkyl group (the C 1-6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , the substituent set V a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkyl groups, C -6 haloalkyl groups, C3.11 cycloalkyl groups, C 2 -6 alkenyl groups, C2-6 haloalkenyl groups, C -6 alkoxy groups, C i -6 haloalkoxy groups, C -6 alkylthio groups, C - 6 haloalkylthio groups, C -6 alkylcarbonyl groups, C i -6 haloalkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, 3 to 11- membered non-aromatic heterocyclyl groups, mono-Ci-6 alkylamino groups, di-C-i -6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups and C -6 alkylcarbonylamino groups, the substituent set V2a consists of the groups in the substituent set V a , Ce-14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the Ce-14 aryl group and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) the substituent set V3a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, Ci-6 alkoxy groups, C i -6 haloalkoxy groups, C -6 alkylthio groups, C -6 haloalkylthio groups, C - alkylcarbonyl groups, Ci-6 haloalkylcarbonyl groups, Ci- 6 alkylsulfonyl groups, Ci-6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci-6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci-6 alkylaminocarbonyl groups, Ci-6 alkylcarbonylamino groups, C 3-n cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6 -14 aryl groups and 5 to 10- membered aromatic heterocyclyl groups (the C3.1 cycloalkyl groups, the 3 to 11- membered non-aromatic heterocyclyl groups, the C 6 -14 aryl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , the substituent set V4a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C1-6 alkyl groups, C 2 -6 alkenyl groups, C 1-6 alkoxy groups, C1-6 alkylthio groups, C1-6 alkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci-6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di- C 1-6 alkylaminocarbonyl groups, Ci-6 alkylcarbonylamino groups (the C 1-6 alkyl groups, the C2-6 alkenyl groups, the C 1-6 alkoxy groups, the C -6 alkylthio groups, the C i -6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the Ci-6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the C i -6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , C3.11 cycloalkyl groups, 3 to 1 1-membered non-aromatic heterocyclyl groups, Ce-14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C3-11 cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6-i 4 aryl groups and 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , and the substituent set V5a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, Ci-6 alkoxy groups, C1-6 alkylthio groups, C -6 alkylcarbonyl groups, C1-6 alkylsulfonyl groups, -6 alkoxycarbonyl groups, mono-Ci-6 alkylamino groups, di- -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-C1-6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups, C3.11 cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6 - 1 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the Ci-6 alkoxy groups, the C -6 alkylthio groups, the Ci-6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the C 1-6 alkoxycarbonyl groups, the mono-Ci-6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di- -6 alkylaminocarbonyl groups, the C1-6 alkylcarbonylamino groups, the C3.11 cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C -14 aryl groups and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a)], a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (3) The compound according to (2), wherein R a is a hydrogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (4) The compound according to (2) or (3), wherein Ya is C R 10a (wherein R 0a is a hydrogen atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (5) The compound according to any one of (2) to (4), wherein Xa is a nitrogen atom or C R 9 a (wherein R 9a is a hydrogen atom, a halogen atom, a cyano group, a C 1-3 alkyl group, a C -3 haloalkyl group or a C3.6 cycloalkyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (6) The compound according to any one of (2) to (5), wherein the ring Aa is represented by any of the following formulae (IVa- 1) to (IVa-3): ( I V ) ( I Va-2 ) ( rVa-3 ) (wherein E2a is an oxygen atom or a sulfur atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (7) The compound according to any one of (2) to (6), wherein L a is a single bond, L a is a single bond, a C 1-6 alkylene group or a C 2 -6 alkenylene group (the d -6 alkylene group and the C 2 -6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), the ring Ba is a C3.11 cycloalkane, a C3-11 cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a C e-1 aromatic carbocycle or a 5 to 10-membered an aromatic heterocycle, na is 0 or 1, R a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C 1-3 alkyl group, a C -3 haloalkyl group, a C3-6 cycloalkyl group, a C1.3 alkoxy group, a C -3 haloalkoxy group or a C 1-3 alkylsulfonyl group, L3a is a single bond, and R2a is a hydrogen atom, a halogen atom, a C 3. cycloalkyl group, a 3 to 1-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 10- membered aromatic heterocyclyl group (the C 3-n cycloalkyl group, the 3 to 11- membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (8) The compound according to any one of (2) to (6), wherein L a is a single bond or a Ci-3 alkylene group, L a is a single bond or a C -3 alkylene group (the C -3 alkylene group is unsubstituted or substituted with a cyano group or a C i -3 haloalkyl group), the ring Ba is a C 3-n cycloalkane, a C 3-n cycloalkene, a 3 to 11-membered non-aromatic heterocycle, benzene or a 5 to 6-membered aromatic heterocycle, na is 0 or 1, R3a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C-1-3 alkyl group, a C1-3 haloalkyl group, a C 3-6 cycloalkyl group, a C -3 alkoxy group, a C-1.3 haloalkoxy group or a C -3 alkylsulfonyl group, L3a is a single bond, and R2a is a hydrogen atom, a halogen atom, a C 3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C 3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (9) The compound according to (7), wherein the ring Ba is a C 3 -n cycloalkane, a 4 to 7-membered non-aromatic heterocycle or benzene, na is, 0 or 1, and R3a is a hydroxy group, a halogen atom, a cyano group or a C -3 alkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (10) The compound according to (7) or (9), wherein L2a is a single bond, a C -6 alkylene group, a C2-6 alkenylene group or a C i -6 haloalkylene group (the Ci-6 alkylene group, the C2-6 alkenylene group and the C -6 haloalkylene group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups and cyano groups), the ring Ba is a C 3-n cycloalkane or a 4 to 7-membered non-aromatic heterocycle, and R a is a hydrogen atom, a halogen atom, a C3-6 cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, nitro groups, carboxy groups, carbamoyl groups, sulfamoyl groups, C -6 alkyl groups, C -6 alkoxy groups, mono-Ci -6 alkylamino groups, di-Ci-6 alkylamino groups, C -6 alkylthio groups, C -6 alkylcarbonyl groups, C -6 alkylsulfonyl groups, C1-6 alkoxycarbonyl groups, mono-Ci-6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups (the C -6 alkyl groups, the C -6 alkoxy groups, the mono-Ci-6 alkylamino groups, the di-Ci -6 alkylamino groups, the C -6 alkylthio groups, the C -6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the C - -6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and C1-3 alkoxy groups), C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -6 alkyl groups and C -6 haloalkyl groups)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (11) The compound according to (7) or (9), wherein L2a is a single bond, a C1-3 alkylene group, a C2-3 alkenylene group (the C -3 alkylene group and the C2-3 alkenylene group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups and cyano groups) or a C -3 haloalkylene group, and R a is a hydrogen atom or a halogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (12) The compound according to any one of (7), (9) and (10), wherein the ring Ba is a C4 -7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, and R a is a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, carbamoyl groups, C -3 alkyl groups, C -3 alkoxy groups, mono-C -3 alkylamino groups, di-C-1-3 alkylamino groups (the C -3 alkyl groups, the C-1-3 alkoxy groups, the mono-Ci -3 alkylamino groups and the di-C-1 -3 alkylamino groups are unsubstituted or substituted with a hydroxy group or a cyano group), C1-3 haloalkyl groups, C - -3 haloalkoxy groups, C -3 alkylthio groups, C1-3 haloalkylthio groups, C 1-3 alkylsulfonyl groups, C -3 haloalkylsulfonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a C -3 alkyl group and a C1-3 haloalkyl group)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (13) The compound according to any one of (7), (9) and (10), wherein the ring Ba is a C4 -7 cycloalkane, and R2a is a 4 to 7-membered non-aromatic heterocyclyl group (the 4 to 7-membered nonaromatic heterocyclyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, carboxy groups, C-1-3 a ky groups (the Ci-3 alkyl groups are unsubstituted or substituted with a hydroxy group or a cyano group), C1-3 haloalkyl groups, C -3 alkoxy groups, di-Ci -3 alkylamino groups, mono-Ci-3 alkylaminocarbonyl groups, C -3 alkylsulfonyl group, C -3 alkylcarbonylamino groups (the C -3 alkoxy groups, the di-Ci -3 alkylamino groups, the mono-C1-3 alkylaminocarbonyl groups, the C -3 alkylsulfonyl group and the C 1-3 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), 4 to 7-membered non-aromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, C i -3 alkyl groups and C -3 haloalkyl groups)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (14) The compound according to any one of (2) to (6), wherein L a is a single bond, L a is a single bond, a C -6 alkylene group or a C-2-6 alkenylene group (the C -6 alkylene group and the C-2-6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), the ring Ba is a C 3 - cycloalkane, a C 3 - cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a C-6-14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, na is 0 or 1, R3a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a halogen atom, a cyano group, a C -3 alkyl group, a C -3 haloalkyl group, a C 3 -6 cycloalkyl group, a Ci- 3 alkoxy group, a C 3 haloalkoxy group or a C -3 alkylsulfonyl group, a is represented by any of the following formulae (XIVa-1) to (XIVa-15): a-2 ) ( XIV a-3 ) ( XIVM ) ( XIV a-5 ) ( XIV a-6 ( XIV a-7 ) ( XIV a-8 ) ( XIV a-9 ) ( X IV O) ( XIV l ) ( X IV 2 ) ( XIV a-13 ) ( XIV a-14 ) ( X IV 5 ) (wherein E a is an oxygen atom, a sulfur atom or NR11a (wherein R11a is a hydroxy group or a C 1-3 alkoxy group), each of R a and R 3a is independently a hydrogen atom, a Ci-6 alkyl group or a C -6 haloalkyl group (the Ci-6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, cyano groups, C 3 - cycloalkyl groups, C 1-6 alkoxy groups, C -6 haloalkoxy groups, C -6 alkylthio groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di- C -6 alkylaminocarbonyl groups, C 1-6 alkylcarbonylamino groups, phenyl groups and 5 to 10-membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a))), and R a is a hydrogen atom, a -6alkyl group, a C 2-6 alkenyl group (the alkyl group and the C2 -6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5a) , a C3.11 cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 10-membered aromatic heterocyclyl group (the C3-11 cycloalkyl group, the 3 to 1 1-membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (15) The compound according to any one of (2) to (6), wherein L a is a single bond or a C -3 alkylene group, L a is a single bond or a C i -3 alkylene group (the C i -3 alkylene group is unsubstituted or substituted with a cyano group or a C -3 haloalkylene group), the ring Ba is a C 3.11 cycloalkane, a C 3.11 cycloalkene, a 3 to 11-membered non-aromatic heterocycle, benzene or a 5 to 6-membered aromatic heterocycle, na is 0 or 1 R3a is a hydroxy group, an amino group, a carbamoyl group, a halogen atom, a cyano group, a C 1-3 alkyl group, a C 1-3 haloalkyl group, a C3-6 cycloalkyl group, a C 1-3 alkoxy group, a C -3 haloalkoxy group or a C -3 alkylsulfonyl group, ( Va-7 ) ( Va-8 ) ( Va-9 ) ( Va-10 ) ( Va-ll ) (wherein E1a is an oxygen atom, each of R a and R13a is independently a hydrogen atom, a C -6 alkyl group or a C i -6 haloalkyl group), and R a is a hydrogen atom, a C- -6 alkyl group (the Ci- 6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5a) , a C 3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C 3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. ( 16) The compound according to (14), wherein L2a is a single bond, a C -3 alkylene group, a C2-3 alkenylene group (the C 1-3 alkylene group and the C2 -3 alkenylene group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups and cyano groups) or a Ci-3 haloalkylene group, the ring Ba is a C3-11 cycloalkane, a 4 to 7-membered non-aromatic heterocycle or benzene, na is 0 or 1, R3a is a halogen atom, a cyano group or a C -3 alkyl group, and a is represented by any of the following formulae (XVa-1) to (XVa-12): ( XVa-7 ) ( XV -8 ) ( XV a-9 ) ( XV O) ( XV a-ll ) ( XVa-12 ) (wherein E1a is an oxygen atom or NR11a (wherein R 1a is a hydroxy group), and R12a is a hydrogen atom, a C -6 alkyl group or a C -6 haloalkyl group (the C -6 alkyl group and the C -6 haloalkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C - .3 alkoxy group, a C3-6 cycloalkyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a cyano group, a C 1-3 alkyl group and a C -3 haloalkyl group))), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (17) The compound according to (14) or (16), wherein L a is a single bond or a C-1-3 alkylene group, the ring Ba is a C4-7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, and R2a is a hydrogen atom, a Ci-6 alkyl group, a Ci-6 haloalkyl group (the Ci-6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C -6 alkoxy groups, mono-Ci -6 alkylaminocarbonyl groups, di- C-1-6 alkylaminocarbonyl groups (the mono-Ci-6 alkylaminocarbonyl groups and the di- C -6 alkylaminocarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups or 5 to 10- membered aromatic heterocyclyl groups (the C3-6 cycloalkyl groups, the 4 to 7- membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstltuted or substituted with identical or different one , two or three substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, -6alkoxy groups, C -6 haloalkoxy groups, C - -6 alkylthio groups, C -6 haloalkylthio groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstltuted or substituted with a halogen atom))), a C 3-11 cycloalkyl group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3-11 cycloalkyl group, the 4 to 7- membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstltuted or substituted with one, two or three identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -6 alkyl groups (the C -6 alkyl groups are unsubstltuted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, hydroxy groups and C1-3 alkoxy groups), C -6 alkoxy groups, C -6 haloalkoxy groups, C -6 alkylthio groups, C -6 haloalkylthio groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups (the C -6 alkoxycarbonyl groups are unsubstltuted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), 4 to 7-membered nonaromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstltuted or substituted with a halogen atom)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (18) The compound according to any one of (14), (16) and (17), wherein L3a is represented by any of the following formulae (XXIIIa-1) to (XXIIIa-7): ( XXIII ) ( XXIIIa-5 ) ( XXIIIa-6 ) ( XXIIIa-7 ) (wherein E1a is an oxygen atom, and R a is a hydrogen atom, a C -3 alkyl group (the C - 3 alkyl group is unsubstltuted or substituted with a cyano group) or a C-1 .3 haloalkyl group), and R2a is a C -6 alkyl group (the C -6 alkyl group is unsubstltuted or substituted with a cyano group), a C -6 haloalkyl group, a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group or a phenyl group (the 4 to 7-membered non-aromatic heterocyclyl group and the phenyl group are unsubstltuted or substituted with a substituent selected from the group consisting of a halogen atom, a hydroxy group, a cyano group, a C1-3 alkyl group and a C -3 haloalkyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (19) The compound according to any one of ( 4) and (16) to (18), wherein L3a is represented by any of the following formulae (XXIVa-1) to (XXIVa-4): ( XXIVa-l ) ( XXIVa-2 ) ( XXIVa-3 ) ( XXIV ) (wherein E a is an oxygen atom, and R a is a hydrogen atom, a -3alkyl group (the C - 3 alkyl group is unsubstituted or substituted with a cyano group) or a C -3 haloalkyl group), and R a is a C -3 alkyl group (the C -3 alkyl group is unsubstituted or substituted with a cyano group), a C 1-3 haloalkyl group or a C3 -6 cycloalkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (20) The compound according to any one of (14), (16) and (17), wherein L3a is represented by the formula (XVIa) : (XVI ) (wherein R 2a is a hydrogen atom, a C -3 alkyl group (the C -3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C -3 alkoxy group, a C-3-6 cycloalkyl group and a phenyl group) or a C -3 haloalkyl group), and R a is a hydrogen atom, a C -6 alkyl group (the C1-6 alkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C1-3 alkoxy groups, mono- C 1-3 alkylaminocarbonyl groups (the mono-Ci-3 alkylaminocarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), C3-6 cycloalkyl groups, 4 to 7-membered nonaromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3 -6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -3 alkoxy groups, C -3 haloalkoxy groups, C1-3 alkylsulfonyl groups, C -6 alkoxy carbonyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with a halogen atom))), a C -6 haloalkyl group (the C i-6 haloalkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 6- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, C -3 alkoxy groups and C -3 alkylthio groups)), a C3-11 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10- membered aromatic heterocyclyl group (the C3-11 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -3 alkyl groups (the C1-3 alkyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group and a C1-3 alkoxy group), C -3 haloalkyl groups, -3 alkoxy groups, C -3 haloalkoxy groups, C1-3 alkylsulfonyl groups, C1-3 haloalkylsulfonyl groups, C1-6 alkoxycarbonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with a halogen atom)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (21) The compound according to any one of (2) to (12) and (14) to (19), wherein the ring Ba is cyclohexane or piperidine, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (22) The compound according to (13) or (20), wherein the ring Ba is cyclohexane, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (23) The compound according to any one of (5) to (22), wherein Xa is CR9a (wherein R9a is a hydrogen atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (24) The compound according to any one of (6) to (23), wherein the ring Aa is re resented by any of the following formulae (IVa-1) to (IVa-3): ( IVa-l ) ( IVa-2 ) ( I V -3 ) (wherein E2a is an oxygen atom or a sulfur atom, and each of R4a and R6a is independently a hydrogen atom or a C -3 alkyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (25) The compound according to any one of (8), (23) and (24), wherein L a is a single bond, L2a is a single bond or a C -3 alkylene group, the ring Ba is a C4-7 cycloalkane, benzene or a 4 to 7-membered non-aromatic heterocycle, na is 0 , L a is a single bond, and R2a is a hydrogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (26) The compound according to any one of ( 5), (23) and (24), wherein L a is a single bond, L a is a single bond, the ring Ba is a C4-7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, na is 0, L3a is represented by any of the following formulae (Vla-1) to (Vla-3): ( VIM ) ( VIa-2 ) ( VIa-3 ) and R a is a hydrogen atom or a Ci-3 a yl group (the C - -3 alkyl group is unsubstituted or substituted with a cyano group or a phenyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (27) The compound according to any one of (2) to (6), (8), (15), (25) and (26), wherein the ring Ba is cyclohexane, benzene or piperidine, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (28) The compound according to ( 1) , wherein R a is a hydrogen atom, Xa is C R 9 a (wherein R 9 a is a hydrogen atom or a halogen atom), Y a is C R a (wherein R 0 a is a hydrogen atom), he ring Aa is represented by any of the following formulae (IVa-1) to (IVa-3): ( IVa-l ) ( IVa- ) ( IVa-3 (wherein E is an oxygen atom or a sulfur atom, R is a hydrogen atom or a Ci-3 alkyl group, and R6a is a hydrogen atom), L a is a single bond, the ring Ba is a C3-11 cycloalkane, a C 3 - cycloalkene (a ring-constituting methylene group of the C 3 - cycloalkane and the C 3 - n cycloalkene may be replaced by a carbonyl group), a 3 to 11-membered non-aromatic heterocycle, a C-6-14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, na is 0, 1 or 2 , R3a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a halogen atom, a cyano group, a C 1-3 alkyl group, a C -3 haloalkyl group or a C 1-3 alkoxy group (when na is 2, R3a's may be identical or different), L a is a single bond, a Ci-6 alkylene group, a C2-6 alkenylene group (the C 1-6 alkylene group and the C2-6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), =C(R15a)- (wherein R15a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L a is a double bond) or =C(R15a)-CH2- (wherein R15a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L a is a double bond), L3a is a single bond or represented by any of the following formulae (XIVa-1) to (XIVa- 15) and (Xlll a) ( XIVa-6 ) ( XIVa-7 ) ( XIV -8 ) ( XIVa-9 ) ( XIV O) ( XIV l ) ( XIV 2 ) ( XIV 3 ) ( X V 4 ) ( XIV 5 ) (wherein E a is a n oxygen atom), when L a is a single bond, R a is a hydrogen atom, a halogen atom, a n azido group, a C-3- cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C-6-14 aryl group, a 5 t o 10-membered aromatic heterocyclyl group, a 8 t o 11-membered partially saturated aromatic cyclic group o r a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3- cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C6-i 4 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 11-membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon groupg are unsubstituted o r substituted with one o r more identical o r different substituents independently selected from the group consisting of the substituent set V a, the substituent set V a and C -6 alkyl groups (the C -6 alkyl groups are substituted with a -6 alkoxycarbonylamino group (the C -6 alkoxycarbonylamino group is unsubstituted o r substituted with one o r more identical o r different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms))), when L a is not a single bond, R a is a hydrogen atom, a C 1-6 alkyl group, a C2. alkenyl group, a C-2-6 alkynyl group (the C1-6 alkyl group, the C2 -6 alkenyl group and the C2-6 alkynyl group are unsubstituted o r substituted with one o r more identical o r different substituents independently selected from the substituent set V6a and the substituent set V 9a) , a C3-11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a Ce- 4 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 1 -membered partially saturated aromatic cyclic group o r a 8 to 11-membered aromatic ringcondensed alicyclic hydrocarbon group (the C3- cycloalkyl group, the 3 to 11- membered non-aromatic heterocyclyl group, the C6- aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to -membered partially saturated aromatic cyclic group and the 8 to 1 1-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V a) , and each of R 2a and R 3a is independently a hydrogen atom, a C -6 alkyl group, a -e haloalkyl group (the C -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V2a, the substituent set V8a and the substituent set V9a) , a C3- cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a C 6 -14 aryl group, a 5 to 10-membered aromatic heterocyclyl group or a 8 to -membered partially saturated aromatic cyclic group (the C 3- cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C 6 -14 aryl group, the 5 to 10-membered aromatic heterocyclyl group and the 8 to 11-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (29) The compound according to (1) or (28), wherein L a is a single bond, a C-i - alkylene group, a C 2-6 alkenylene group (the C -6 alkylene group and the C2 -6 alkenylene group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups and cyano groups) or a C-i -6 haloalkylene group, the ring Ba is a C4-7 cycloalkane (a ring-constituting methylene group of the C -7 cycloalkane may be replaced by a carbonyl group) or a 4 to 7-membered non-aromatic heterocycle, na is 0 , 1 or 2 , R3a is a cyano group, a C 1-3 alkyl group or a halogen atom (when na is 2, R a's may be identical or different), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (30) The compound according to any one of ( 1) , (28) and (29), wherein L3a is a single bond, R a is a hydrogen atom, a halogen atom, an azido group, a C 3. cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a 5 to 10-membered aromatic heterocyclyl group or a 8 to 1 1-membered partially saturated aromatic cyclic group (the C 3- cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group, the 5 to 10-membered aromatic heterocyclyl group and the 8 to 11-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of the substituent set V4a, the substituent set V9a and C -6 alkyl groups (the C -6 alkyl groups are substituted with a C- -6 alkoxycarbonylamino group (the C -6 alkoxycarbonylamino group is unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms))), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (31) The compound according to (30), wherein L2a is a C -3 alkylene group, the ring Ba is a 4 to 7-membered non-aromatic heterocycle, L a is a single bond, R a is a phenyl group or a 5 to 10-membered aromatic heterocyclyl group or a 8 to 11- membered partially saturated aromatic cyclic group (the phenyl group, the 5 to 10- membered aromatic heterocyclyl group and the 8 to 11-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, carbamoyl groups, C i-6 alkyl groups, C -6 haloalkyl groups, C -6 alkoxy groups, C -6 haloalkoxy groups, di-C-i -6 alkylamino groups, C -6 alkylthio groups, C -6 haloalkylthio groups, C --6 alkylsulfonyl groups, 4 to 7- membered non-aromatic heterocyclyl groups and 5 to 6-membered aromatic heterocyclyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (32) The compound according to any one of (28) to (30), wherein the ring Ba is a C4-7 cycloalkane, L3a is a single bond, R2a is a 3 to 11-membered non-aromatic heterocyclyl group (the 3 to 11-membered nonaromatic heterocyclyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, carbamoyl groups, carboxy groups, C 1-6 alkyl groups (the C -6 alkyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms or with a substituent selected from the group consisting of a hydroxy group, a cyano group and a C -6 alkoxycarbonylamino group), C -3 alkoxy groups, mono-C - alkylaminocarbonyl groups, C -3 alkylcarbonylamino groups (the C 1-3 alkoxy groups, the mono-Ci -3 alkylaminocarbonyl groups, the C 1-3 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), di-C-1-3 alkylamino groups, C 3 alkylsulfonyl groups, di-C-1-3 alkylaminosulfonyl groups, C -6 alkoxycarbonylamino groups, 4 to 7-membered non-aromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with a halogen atom)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. ( XVa-7 ) ( XVa-8 ) ( XVa-9 ) ( X V ) ) (wherein E a is an oxygen atom, and R a is a hydrogen atom, a C -6 alkyl group (the - 6 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C -3 alkoxy group, a C 3 -6 cycloalkyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a cyano group, a C -3 alkyl group and a C -3 haloalkyl group)), a C -6 haloalkyl group, a C 3 6 cycloalkyl group or a phenyl group (the phenyl group is unsubstituted or substituted with a halogen atom or a cyano group)), R2a is a hydrogen atom, a C -6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V 6 a and the substituent set V 9 a ) , a C-2-6 alkynyl group, a C 3 - cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 1 1-membered partially saturated aromatic cyclic group or a 8 to -membered aromatic ring-condensed alicyclic hydrocarbon group (the C3 - cycloalkyl group, the 3 to 1 1-membered nonaromatic heterocyclyl group, the phenyl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 1-membered partially saturated aromatic cyclic group and the 8 to 1 -membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (34) The compound according to (33), wherein the ring Ba is a C4-7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, L a is represented by the following formulae (XXVa- 1) or (XXVa-2): ( XXV ) ( XXV a-2 ) (wherein R a is a hydrogen atom, a C -3 alkyl group (the C-1 -3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C -3 alkoxy group, a C 3 -6 cycloalkyl group and a phenyl group), a C -3 haloalkyl group, a C 3 -6 cycloalkyl group or a phenyl group (the phenyl group is unsubstituted or substituted with a halogen atom or a cyano group)), R a is a hydrogen atom, a C -6 alkyl group, a C-i -6 haloalkyl group (the C -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, C -3 alkoxy groups, C -3 alkylthio groups, C -3 alkylsulfonyl groups, mono-C-1 -3 alkylaminocarbonyl groups, di-Ci -3 alkylaminocarbonyl groups (the mono-Ci -3 alkylaminocarbonyl groups and the di-C -3 alkylaminocarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), C3 -6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3 -6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, C -3 alkyl groups, C -3 haloalkyl groups, -3 alkoxy groups, C -3 haloalkoxy groups, C -3 alkylthio groups, C -3 haloalkylthio groups, C -3 alkylsulfonyl groups, Ci-3 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci -3 alkylamino groups, di- C- -3 alkylamino groups, mono-Ci-3 alkylaminocarbonyl groups, di-Ci-3 alkylaminocarbonyl groups, C 3 alkylcarbonylamino group (the C - alkoxycarbonyl groups, the mono-Ci- 3 alkylamino groups, the di-C 1-3 alkylamino groups, the mono-Ci -3 alkylaminocarbonyl groups, the di-Ci -3 alkylaminocarbonyl groups and the C -3 alkylcarbonylamino group are unsubstltuted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), 4 to 7-membered nonaromatic heterocyclyl groups, phenyl groups (the phenyl groups are unsubstltuted or substituted with a halogen atom) and 5 to 6-membered aromatic heterocyclyl groups)), a C2 -6 alkynyl group, a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group, a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3 -6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group, the 8 to 11-membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstltuted or substituted with one, two or three identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, C -3 alkyl groups (the Ci-3 alkyl groups are unsubstltuted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group and a C1-3 alkoxy group), C -3 haloalkyl groups, C -3 alkoxy groups, C1-3 haloalkoxy groups, C1-3 alkylthio groups, C1-3 haloalkylthio groups, C -3 alkylsulfonyl groups, Ci -3 haloalkylsulfonyl groups, C1-6 alkoxycarbonyl groups, mono-Ci -3 alkylamino groups, di-Ci -3 alkylamino groups, mono-C-1 -3 alkylaminocarbonyl groups, di-Ci -3 alkylaminocarbonyl groups, C -3 alkylcarbonylamino groups (the C -6 alkoxycarbonyl groups, the mono-Ci -3 alkylamino groups, the di-Ci -3 alkylamino groups, the mono-C-1 -3 alkylaminocarbonyl groups, the di-Ci -3 alkylaminocarbonyl groups and the C1-3 alkylcarbonylamino group are unsubstltuted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), 4 to 7-membered nonaromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstltuted or substituted with a halogen atom)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (35) The compound according to (33), wherein the ring Ba is a C -7 cycloalkane, ( XXVIM ) ( XXVIa-2 ) ( XXVF-3 ) ( XXVIM ) ( XXVIa-5 ) (wherein E a is an oxygen atom, and R 2a is a hydrogen atom, a C -3 alkyl group (the C . 3 alkyl group is unsubstltuted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C -3 alkoxy group, a C3.6 cycloalkyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the 5 to 6- membered aromatic heterocyclyl group is unsubstituted or substituted with a Ci-3 alkyl group)), a C1-3 haloalkyl group, a C3-6 cycloalkyl group or a phenyl group (the phenyl group is unsubstituted or substituted with a halogen atom or a cyano group)), and R a is a Ci-3 alkyl group (the C -3 alkyl group is unsubstituted or substituted with a cyano group), a C1-3 haloalkyl group or a C3-6 cycloalkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (36) The compound according to (34) or (35), wherein L3a is represented by the formula (XVIa) : NA ( XVI a ) R 12a (wherein R1 a is a hydrogen atom, a C -3 alkyl group (the C -3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C1-3 alkoxy group, a C3-6 cycloalkyl group and a phenyl group), a C1-3 haloalkyl group, a C3-6 cycloalkyl group or a phenyl group (the phenyl group is unsubstituted or substituted with a halogen atom or a cyano group)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (37) The compound according to (33), wherein L3a is represented by the formula (Xlll a) : (wherein E1a is an oxygen atom), R a is a C1-3 alkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (38) The compound according to any one of (1) to (24), (28) to (30) and (32) to (37), wherein L a is a single bond or a C -3 alkylene group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (39) The compound according to ( 1) or (28), wherein L a is a single bond, the ring Ba is a C4-7 cycloalkane, L a is =C(R15a)- (wherein R 5a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L2a is a double bond) or =C(R15a)-CH2- (wherein R 5a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L2a is a double bond), and R a is a hydrogen atom, and a-2): R is a C1-3 alkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (40) The compound according to any one of ( ) to (39), wherein na is 0, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (41 ) A compound represented by the formula (lb) : wherein the ring A is represented by the formula (llb) : (wherein T b is CR4bR5 , C(=0), C(=S), C(=NR ) , a sulfur atom, S(=0) or S(=0) 2, U b R6b, and W b is a nitrogen atom or CR b) , the formula (lll ) : (wherein is CR , is a nitrogen atom or CR , and is CR R , C(=0), C(=S), C(=NR 7 ) , NR10b, an oxygen atom, a sulfur atom, S(=O) or S(=0) 2 (provided that when 2 is CR6b,W2 is not C(=0))) or the formula (IVb) : (wherein T is CR4 R5b, C(=0), C(=S), C(=NR 7b), a sulfur atom, S(=0) or S(=0) 2 > U3b is CR6 R , C(=0), C(=S), C(=NR 7b) , NR10b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2, and W is CR bR9b, C(=0), C(=S), C(=NR 7 ) , NR , an oxygen atom, a sulfur atom, S(=0) or S(=0) 2 (provided that when T b is CR4bR5b and U3b is CR6bR b,W3b is not CR R9b)), X is a nitrogen atom or CR 5b, Yb is CR 6b R is a hydrogen atom, a halogen atom, a C1-6 alkyl group or a C -6 haloalkyl group, the ring Bb is a C3.11 cycloalkane, a C3-n cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a Ce-14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L b is a single bond, a C -6 alkylene group, a C2 -6 alkenylene group or a C2- alkynylene group (the C -6 alkylene group, the C2 -6 alkenylene group and the C2 -6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L2b is a single bond, a C 1-6 alkylene group, a C2 - 6 alkenylene group or a C2.6 alkynylene group (the C -6 alkylene group, the C2-6 alkenylene group and the C2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L3b is a sin le bond or represented by any of the following formulae (Vb-1) to (Vb-20): ( V b-12 ) ( Vb-13 ) ( V -14 ) ( Vb-15 ) ( V -16 ) ( V b-17 ) ( Vb-18 ) ( V b-19 ) ( V b-20 ) (wherein E is an oxygen atom, a sulfur atom or NR ) , when L is a single bond, R2b is a hydrogen atom, a halogen atom, a C3-11 cycloalkyl group, a 3 to 14-membered non-aromatic heterocyclyl group, a C e- aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 14-membered partially saturated aromatic cyclic group or a 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group (the C 3. cycloalkyl group, the 3 to 14-membered non-aromatic heterocyclyl group, the C e- aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 14-membered partially saturated aromatic cyclic group and the 8 to 14- membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b and the substituent set V9b) , when L3b is not a single bond, R b is a hydrogen atom, a C -6 alkyl group, a C 2 -6 alkenyl group (the C -6 alkyl group and the C2 -6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b and the substituent set V9b) , a C3- i cycloalkyl group, a 3 to 14- membered non-aromatic heterocyclyl group, a Ce-u aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 14-membered partially saturated aromatic cyclic group or a 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3.11 cycloalkyl group, the 3 to 14-membered non-aromatic heterocyclyl group, the C earyl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 14-membered partially saturated aromatic cyclic group and the 8 to 14-membered aromatic ringcondensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4 and substituent set V b) , nb is 0, 1 or 2 , R3 is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a sulfamoyl group, a phosphono group, a phosphonooxy group, a sulfo group, a sulfoxy group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C 1-6 alkyl group, a -6 haloalkyl group, a C3-11 cycloalkyl group, a C 2-6 alkenyl group, a C 2-6 haloalkenyl group, a C - alkoxy group, a C -6 haloalkoxy group, a -6 alkylthio group, a C -6 haloalkylthio group, a C -6 alkylcarbonyl group, a C -6 haloalkylcarbonyl group, a C i - 6 alkylsulfonyl group, a C 1-6 haloalkylsulfonyl group, a Ci- 6 alkoxycarbonyl group, a mono-Ci -6 alkylamino group, a di-Ci - alkylamino group, a mono-d -e alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group or a Ci- 6 alkylcarbonylamino group (when n is 2, R 's may be identical or different), each of R4b, R5b, R6b, R7 , R8b and R9b is independently a hydrogen atom, a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a Ci- 6 alkyl group, a C 2 -6 alkenyl group, a C -6 alkoxy group, a C -6 alkylthio group, a C 1-6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a mono-Ci -6 alkylamino group, a di-Ci-6 alkylamino group (the C 1-6 alkyl group, the C 2-6 alkenyl group, the C 1-6 alkoxy group, the C 1-6 alkylthio group, the C i -6 alkylcarbonyl group, the C i -6 alkylsulfonyl group, the mono-Ci -6 alkylamino group and the di-Ci -6 alkylamino group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , a C i -6 alkoxycarbonyl group, a C3.11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C e-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3.11 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C e-1 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V ) , each of R 0 and R11b is independently a hydrogen atom, a d -6 alkyl group, a C 2-6 alkenyl group, a d -6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-Ci -6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group (the C 1-6 alkyl group, the C 2-6 alkenyl group, the C -6 alkylcarbonyl group, the C -6 alkylsulfonyl group, the C -6 alkoxycarbonyl group, the mono-Ci -6 alkylaminocarbonyl group and the di-Ci -6 alkylaminocarbonyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V ) , a C 3 -n cycloalkyl group, a 3 to 1 1 - membered non-aromatic heterocyclyl group, a C e-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3 -n cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C e-14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V ) , each of R12 , R b and R1 b is independently a hydrogen atom, a d -6 alkyl group or a C _ 6 haloalkyl group (the C 1- alkyl group and the Ci- 6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b, the substituent set V b and the substituent set V9b) , each of R15 and R 6b is independently a hydrogen atom, a halogen atom, a cyano group, a carbamoyl group, a C -6 alkyl group, a C -6 haloalkyl group, a C 3 - cycloalkyl group, a C -6 alkoxy group, a C -6 haloalkoxy group, a C 1-6 alkylthio group, a C -6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a Ce-14 y oup or a 5 to 10-membered aromatic heterocyclyl group, each of R17b and R18b is independently a hydrogen atom, a hydroxy group, a cyano group, a nitro group, a C -6 alkyl group or a Ci- 6 alkoxy group, the substituent set V1b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, Ci-6 alkyl groups, Ci-6 haloalkyl groups, C 3-11 cycloalkyl groups, C -6 alkenyl groups, C-2-6 haloalkenyl groups, C -6 alkoxy groups, C -6 haloalkoxy groups, C - alkylthio groups, C-i . 6 haloalkylthio groups, Ci-6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, C -6 alkylsulfonyl groups, 1-6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, 3 to 11- membered non-aromatic heterocyclyl groups, mono-C -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di-Ci-6 alkylaminocarbonyl groups and C -6 alkylcarbonylamino groups, the substituent set V b consists of the groups in the substituent set V b, and C 6 - aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 6 -14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V ) , the substituent set V3b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C1-6 alkoxy groups, Ci-6 haloalkoxy groups, C1-6 alkylthio groups, C-i -6 haloalkylthio groups, C -6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, C1-6 alkylsulfonyl groups, C - -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci-6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, Ci-6 alkylcarbonylamino groups, C 3 -n cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6 - 14 aryl group and 5 to 10-membered aromatic heterocyclyl groups (the C3.11 cycloalkyl groups, the 3 to 1 1-membered nonaromatic heterocyclyl groups, the Ce-14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , the substituent set V4b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C1-6 alkyl groups, C 2 -e alkenyl groups, Ci- 6 alkoxy groups, C i -6 alkylthio groups, C i -6 alkylcarbonyl groups, C - alkylsulfonyl groups, C 1-6 alkoxycarbonyl groups, mono-Ci-6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di- C 1-6 alkylaminocarbonyl groups, Ci-6 alkylcarbonylamino groups (the Ci-6 alkyl groups, the C2-6 alkenyl groups, the C -6 alkoxy groups, the C i -6 alkylthio groups, the C -6 alkylcarbonyl groups, the C1-6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci-6 alkylamino groups, the di-Ci-6 alkylamino groups, the mono-Ci-6 alkylaminocarbonyl groups, the di-Ci-6 alkylaminocarbonyl groups and the C -6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , C3.11 cycloalkyl groups, 3 to 1-membered non-aromatic heterocyclyl groups, C 6 - 14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C3.11 cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C e-14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b), the substituent set V5b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C 1-6 alkoxy groups, C 1-6 alkylthio groups, Ci- 6 alkylcarbonyl groups, Ci- 6 alkylsulfonyl groups, C 1-6 alkoxycarbonyl groups, mono-Ci - 6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C .6 alkylcarbonylamino groups, C 3 -n cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6 -i 4 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C - alkoxy groups, the C -6 alkylthio groups, the C 1-6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci- alkylaminocarbonyl groups, the di- C -6 alkylaminocarbonyl groups, the C -6 alkylcarbonylamino groups, the C 3 -n cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C -i 4 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , the substituent set V6 consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkoxy groups, C -6 alkylthio groups, C -6 alkylcarbonyl groups, C i -6 alkylsulfonyl groups, C 1-6 alkoxycarbonyl groups, mono-Ci. 6 alkylamino groups, di-Ci- 6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C 1-6 alkylcarbonylamino groups (the C -6 alkoxy groups, the C 1-6 alkylthio groups, the C -6 alkylcarbonyl groups, the C 1-6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci - 6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the d -6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , C3-11 cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6- aryl groups, 5 to 10-membered aromatic heterocyclyl groups, 8 to 14-membered partially saturated aromatic cyclic groups and 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups (the C3.11 cycloalkyl groups, the 3 to 11-membered nonaromatic heterocyclyl groups, the C 6 -i 4 aryl groups, the 5 to 10-membered aromatic heterocyclyl groups, the 8 to 14-membered partially saturated aromatic cyclic groups and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b and the substituent set V9b) , and the substituent set V8 consists of 8 to 14-membered partially saturated aromatic cyclic groups and 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups (the 8 to 14-membered partially saturated aromatic cyclic groups and the 8 to 14- membered aromatic ring-condensed alicyclic hydrocarbon groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V2b), the substituent set V9b consists of, mono-C 1-6 alkylaminosulfonyl groups, di-C 1-6 alkylaminosulfonyl groups, C -6 alkylsulfonylamino groups (the mono -Ci -6 alkylaminosulfonyl groups, di-Ci -6 alkylaminosulfonyl groups and Ci-e alkylsulfonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V ) , C-3-6 cycloalkoxy groups, C3 -6 cycloalkylamino groups, C3 - 6 cycloalkylthio groups, C- - cycloalkylcarbonyl groups and C3-6 cycloalkylsulfonyl groups (the C 3-6 cycloalkoxy groups, the C3-6 cycloalkylamino groups, the C 3-6 cycloalkylthio groups, the C3-6 cycloalkylcarbonyl groups and the C3-6 cycloalkylsulfonyl groups unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b)], a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 1) , which is represented by the formula (lb) : [wherein the ring Ab is represented by the formula (ll b) : (wherein T is C R4bR5b, C(=0), C(=S), C(=NR 7b) , a sulfur atom, S(=0) or S(=0) 2, U1b R6 , and W b is a nitrogen atom or C R8b) , the formula (lll b) : (wherein T2b is CR4 , T is a nitrogen atom or CR , and V is C R R , C(=0), C(=S), C(=NR 7b) , NR 0b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2 (provided that when U2b is CR6b, W b is not C(=0))), or the formula (IV b) : (wherein T3b is CR bR5b, C(=0), C(=S), C(=NR b) , a sulfur atom, S(=0) or S(=0) 2, U3 is CR6 R , C(=0), C(=S), C(=NR1 b) , NR 0b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2, and W3b is CR8 R9b, C(=0), C(=S), C(=NR 7b), NR11b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2 (provided that when T3b is CR4bR5 and U3b is CR bR ,W3b is not CR bR9b)), Xb is a nitrogen atom or CR 5b, Yb is CR 6b, R is a hydrogen atom, a halogen atom, a -6 alkyl group or a C -6 haloalkyl group, the ring Bb is a C3- cycloalkane, a C 3-11 cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a C - aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L1b is a single bond, a C -6 alkylene group, a C2-6 alkenylene group or a C2 -6 alkynylene group (the C1-6 alkylene group, the C2 -6 alkenylene group and the C2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L2b is a single bond, a C -6 alkylene group, a C-2-6 alkenylene group or a C2-6 alkynylene group (the C -6 alkylene group, the C2-6 alkenylene group and the C2-6 alkynylene group are unsubstituted or substituted with one o r more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L3b a single bond or represented by any of the following formulae (Vb-1) to (Vb-20): V - 2 - -1 V - V -1 - V - - V - (wherein E1b is an oxygen atom, a sulfur atom or NR18b) , when L b is a single bond, R is a hydrogen atom, a halogen atom, a C 3.1 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C e-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3 - cycloalkyl group, the 3 to 11- membered non-aromatic heterocyclyl group, the C 6- aryl group and the 5 to 10- membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b) , when L b is not a single bond, R b is a hydrogen atom, a -6 alkyl group, a C 2 -6 alkenyl group (the C -6 alkyl group and the C 2 -6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5b) , a C 3 -n cycloalkyl group, a 3 to -membered non-aromatic heterocyclyl group, a C-6-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3-n cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C 6-i 4 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b) , nb is 0 , 1 or 2 , R3 is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a sulfamoyl group, a phosphono group, a phosphonooxy group, a sulfo group, a sulfoxy group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C - alkyl group, a -6 haloalkyl group, a C 3 -n cycloalkyl group, a C-2-6 alkenyl group, a C 2 -6 haloalkenyl group, a C -6 alkoxy group, a C -6 haloalkoxy group, a C i-6 alkylthio group, a C -6 haloalkylthio group, a C -6 alkylcarbonyl group, a Ci -6 haloalkylcarbonyl group, a d - 6 alkylsulfonyl group, a C -6 haloalkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-C -6 alkylamino group, a di-Ci -6 alkylamino group, a mono-d- 6 alkylaminocarbonyl group, a di-d -6 alkylaminocarbonyl group or a C 1-6 alkylcarbonylamino group (when nb is 2, R3b's may be identical or different), each of R4b, R5b, R6b, R7b, R8b and R9b is independently a hydrogen atom, a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a d -6 alkyl group, a C -2-6 alkenyl group, a C -6 alkoxy group, a C 1 -6 alkylthio group, a C -6 alkylcarbonyl group, a d - alkylsulfonyl group, a mono-Ci -6 alkylamino group, a di-Ci-6 alkylamino group (the C -6 alkyl group, the C 2 -6 alkenyl group, the d-6 alkoxy group, the C -6 alkylthio group, the d-6 alkylcarbonyl group, the d-6 alkylsulfonyl group, the mono-Ci-6 alkylamino group and the di-Ci- 6 alkylamino group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , a C -6 alkoxycarbonyl group, a C 3- cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a C6-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3-11 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C-6-14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1b) , each of R10b and R b is independently a hydrogen atom, a Ci-6 alkyl group, a C 2-e alkenyl group, a C -6 alkylcarbonyl group, a d - alkylsulfonyl group, a d-6 alkoxycarbonyl group, a mono-Ci-6 alkylaminocarbonyl group, a di-Ci-6 alkylaminocarbonyl group (the d-6 alkyl group, the C 2-6 alkenyl group, the d -6 alkylcarbonyl group, the C 1-6 alkylsulfonyl group, the d-6 alkoxycarbonyl group, the mono-Ci -6 alkylaminocarbonyl group and the di-Ci-6 alkylaminocarbonyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , a C3.11 cycloalkyl group, a 3 to 11- membered non-aromatic heterocyclyl group, a C6- aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3-n cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C e-14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1 ) , each of R b, R13b and R 4b is independently a hydrogen atom, a C -6 alkyl group or a Cihaloalkyl group (the C -6 alkyl group and the C1-6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , each of R 5b and R16 is independently a hydrogen atom, a halogen atom, a cyano group, a carbamoyl group, a C 1-6 alkyl group, a C -6 haloalkyl group, a C3-11 cycloalkyl group, a Ci-6 alkoxy group, a Ci-6 haloalkoxy group, a C -6 alkylthio group, a Ci-6 alkylcarbonyl group, a C - alkylsulfonyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C 6-i 4 aryl group or a 5 to 10-membered aromatic heterocyclyl group, each of R b and R 8 is independently a hydrogen atom, a hydroxy group, a cyano group, a nitro group, a C i -6 alkyl group or a C -6 alkoxy group, the substituent set V1 consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C 1-6 alkyl groups, C -6 haloalkyl groups, C3-11 cycloalkyl groups, C 2 -6 alkenyl groups, C 2 -6 haloalkenyl groups, C 1-6 alkoxy groups, C i -6 haloalkoxy groups, C - alkylthio groups, - 6 haloalkylthio groups, C -6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, C 6 alkylsulfonyl groups, C 1-6 haloalkylsulfonyl groups, C 1-6 alkoxycarbonyl groups, 3 to 11- membered non-aromatic heterocyclyl groups, mono-Ci-6 alkylamino groups, di-C -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci-6 alkylaminocarbonyl groups and C - alkylcarbonylamino groups, the substituent set V2 consists of the groups in the substituent set V1b and C 6-14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 6-14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1 ) , the substituent set V consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkoxy groups, C -6 haloalkoxy groups, C i -6 alkylthio groups, C -6 haloalkylthio groups, C 1-6 alkylcarbonyl groups, Ci-e haloalkylcarbonyl groups, C1-6 alkylsulfonyl groups, C - haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di-Ci-6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups, C 3-n cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6- 14 aryl groups and 5 to 10- membered aromatic heterocyclyl groups (the C 3-n cycloalkyl groups, the 3 to 11- membered non-aromatic heterocyclyl groups, the C 6-14 aryl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1b) , the substituent set V4 consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C- -6 alkyl groups, C 2-e alkenyl groups, C -6 alkoxy groups, C -6 alkylthio groups, C -6 alkylcarbonyl groups, C -6 alkylsulfonyl groups, C - -6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-Ci-6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di- C -6 alkylaminocarbonyl groups, C 1-6 alkylcarbonylamino groups (the C -6 alkyl groups, the C 2 -6 alkenyl groups, the C-i -6 alkoxy groups, the Ci-6 alkylthio groups, the Ci-6 alkylcarbonyl groups, the C i -6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci-6 alkylamino groups, the di-Ci-6 alkylamino groups, the mono-Ci-6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the C -6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , C3-11 cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6 - 14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C3-11 cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the Ce-14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V ) , and the substituent set V b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkoxy groups, C i -6 alkylthio groups, C -6 alkylcarbonyl groups, C -6 alkylsulfonyl groups, C 1-6 alkoxycarbonyl groups, mono-Ci-6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di-Ci-6 alkylaminocarbonyl groups, Ci- 6 alkylcarbonylamino groups, C3-11 cycloalkyl groups, 3 to 1 1-membered non-aromatic heterocyclyl groups, C 6- aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 1-6 alkoxy groups, the C -6 alkylthio groups, the C 1-6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the Ci- 6 alkoxycarbonyl groups, the mono-Ci.6 alkylamino groups, the di-d -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di- C 1-6 alkylaminocarbonyl groups, the C -6 alkylcarbonylamino groups, the C 3 -n cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C-6-i 4 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3 )], a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (43) The compound according to (42), wherein R b is a hydrogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (44) The compound according to (42) or (43), wherein Xb is a nitrogen atom or C R 5 b (wherein R 5 b is a hydrogen atom, a halogen atom, a cyano group, a C 1-3 alkyl group, a C 1-3 haloalkyl group or a C 3-6 cycloalkyl group), and Yb is C R (wherein R 16b is a hydrogen atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (45) The compound according to (44), wherein X is a nitrogen atom or C R 5 b (wherein R 15b is a hydrogen atom or a halogen atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (46) The compound according to any one of (42) to (45), wherein the ring A is represented by the formula (llb): (wherein T b is CR bR b, C(=0), C(=S) or S(=0) 2, U1b is a nitrogen atom or CR6b, and 1b is CR ) , the formula (lll ) : (wherein T b is CR4 b , U¾2b is a nitrogen atom, and W2b is C(=0) or C(=S)) or the formula (IVb) : (wherein T3 is CR bR5 , U b is NR10b or an oxygen atom, and W3b is CR bR9 , C(=0) or C(=S)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. A is ( XVIII" ) ( XVIII b-5 ) ( XVIII b-6 ) ( XVIII -7 ) ( XVIII -8 ) (wherein each of E2b and E3b is independently an oxygen atom or a sulfur atom, each of R4 , R b, R b, R and R9b is independently a hydrogen atom, a halogen atom or a -3 alkyl group, and R 0b is a hydrogen atom or a Ci-3 alkyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (48) The compound according to any one of (42) to (47), wherein L b is a single bond, L2b is a single bond, a C-|.6 alkylene group or a C2 - 6 alkenylene group (the C1-6 alkylene group and the C2-6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of a halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), the ring Bb is a C3-11 cycloalkane, a C3-11 cycloalkene, a 3 to 1-membered non-aromatic heterocycle, a C 6- 4 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, nb is, 0 or 1, R3b is a hydroxy group, an amino group, a halogen atom, a cyano group, a C-1-3 alkyl group, a C-i-3 haloalkyl group, a C 3 -6 cycloalkyl group, a C1-3 alkoxy group, a C 1-3 haloalkoxy group or a C 1-3 alkylsulfonyl group, L3 is a single bond, and R b is a hydrogen atom, a halogen atom, a C 3. 1 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 10- membered aromatic heterocyclyl group (the C3-11 cycloalkyl group, the 3 to 11- membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (49) The compound according to any one of (42) to (47), wherein L1b is a single bond or a C i -3 alkylene group, L2b is a single bond or a Ci-3 alkylene group (the -3 alkylene group is unsubstituted or substituted with a cyano group or a C1-3 haloalkyl group), the ring B is a C 3.11 cycloalkane, a C 3-11 cycloalkene, a 3 to 11-membered non-aromatic heterocycle, benzene or a 5 to 6-membered aromatic heterocycle, n is, 0 or 1, R3 is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C1-3 alkyl group, a C -3 haloalkyl group, a C3-6 cycloalkyl group, a -3 alkoxy group, a C 1 3 haloalkoxy group or a C1-3 alkylsulfonyl group, L3b is a single bond, and R b is a hydrogen atom, a halogen atom, a C 3 -6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3.6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (50) The compound according to (48), wherein the ring Bb is a C 3. cycloalkane or a 4 to 7-membered non-aromatic heterocycle, nb is 0 or 1, and R3b is a hydroxy group, a C1-3 alkyl group or a C1.3 alkoxy group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (51) The compound according to (48) or (50), wherein L2b is a single bond, a C1-6 alkylene group, a C2-6 alkenylene group or a C1-6 haloalkylene group (the Ci- 6 alkylene group, the C 2 -6 alkenylene group and the Ci- 6 haloalkylene group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups and cyano groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (52) The compound according to any one of (48), (50) and (51), wherein R b is a hydrogen atom, a C3.6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 0-membered aromatic heterocyclyl group (the 4 to 7- membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10- membered aromatic heterocyclyl group are unsubstituted o r substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, carbamoyl groups, sulfamoyl groups, halogen atoms, cyano groups, nitro groups, C1-6 alkyl groups, C -6 alkoxy groups, C -6 alkylthio groups, Ci-6 alkylsulfonyl groups, mono -Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, C -6 alkoxycarbonyl groups, mono -Ci -6 alkylaminocarbonyl groups, di-Ci- 6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups (the Ci-6 alkyl groups, the C -6 alkoxy groups, the C -6 alkylthio groups, the C1-6 alkylsulfonyl groups, the mono-Cialkylamino groups, the di-Ci -6 alkylamino groups, the C -6 alkoxycarbonyl groups, the mono -Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the C - 6 alkylcarbonylamino groups are unsubstituted o r substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms or with a hydroxy group or a cyano group), C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (53) The compound according to (52), wherein R b is a hydrogen atom, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, nitro groups, C-1-3 alkyl groups (the C1-3 alkyl groups are unsubstituted o r substituted with a cyano group), C -3 haloalkyl groups and C -6 alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (54) The compound according to any one of (48) and (50) to (53), wherein L b is a C-i -6 alkylene group, a C2-3 alkenylene group (the C -6 alkylene group and the C2 -3 alkenylene group are unsubstituted or substituted with a cyano group) or C -6 haloalkylene group, and R2b is, a hydrogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (55) The compound according to any one of (42) to (47), wherein L1 is a single bond, L2 is a single bond, a C -6 alkylene group or a C2-6 alkenylene group (the C -6 alkylene group and the C2-6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), the ring B is a C 3-11 cycloalkane, a C3 -n cycloalkene, a 3 to 1 1-membered non-aromatic heterocyclyl group, a C-6-14 y group or a 5 to 10-membered aromatic heterocycle, nb is 0 or 1, R3b is a hydroxy group, an amino group, a halogen atom, a cyano group, a C -3 alkyl group, a C1-3 haloalkyl group, a C3-6 cycloalkyl group, a C -3 alkoxy group o r a C -3 haloalkoxy group, L3b is represented by any of the following formulae (Vl b-1) to (Vl b-11): ( Ib-l ) ( Ib-2 ) ( I -3 ) ( Ib-4 ) ( VI -5 ) ( Ib- ) (wherein E b is an oxygen atom or a sulfur atom, each of R1 b and R 3b is independently a hydrogen atom, a C -6 alkyl group or a -6 haloalkyl group (the C -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, hydroxy group, C -6 alkoxy groups, Ci-6 alkylthio groups, C -6 alkylsulfonyl groups, C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a cyano group, a C 1-3 alkyl group and a C 1-3 haloalkyl group))), and R b is a hydrogen atom, a C -6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5b) , a C 3- cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3- cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (56) The compound according to any one of (42) to (47), wherein L b is a single bond or a C-1-3 alkylene group, L2b is a single bond or a C -3 alkylene group (the C 1-3 alkylene group is unsubstituted or substituted with a cyano group or a C -3 haloalkyl group), the ring Bb is a C 3- cycloalkane, a C3--11 cycloalkene, a 3 to 11-membered non-aromatic heterocycle, benzene or a 5 to 6-membered aromatic heterocycle, n is 0 or 1, R3b is a hydroxy group, an amino group, a carbamoyl group, a halogen atom, a cyano group, a C -3 alkyl group, a C -3 haloalkyl group, a C 3 -6 cycloalkyl group, a C 1-3 alkoxy group, a C 1-3 haloalkoxy group or a C-i -3 alkylsulfonyl group, L3b is represented by any of the following formulae (Vlb-1) to (Vlb-11): ( VIb-7 ) ( VIb-8 ) ( VIb-9 ) ( VIb-10 ) ( VI -ll ) (wherein E1b is an oxygen atom, each of R b and R13b is independently a hydrogen atom, a -6 alkyl group or a C 6 haloalkyl group), and R2 is a hydrogen atom, a C -6 alkyl group (the C i -6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5 ) , a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (57) The compound according to (55), wherein the ring Bb is a C3- cycloalkane or a 4 to 7-membered non-aromatic heterocycle, L3b is represented by any of the following formulae (XIXb- 1) to (XIX -7): R 12b ( XIX - ) ( XIXb-7 ) (wherein E b is an oxygen atom, and R 2b is a hydrogen atom, a C 1-6 alkyl group (the - 6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C -3 alkoxy groups, C3 -6 cycloalkyl groups and phenyl groups) or a C i -6 haloalkyl group), and R2 is a hydrogen atom, a Ci-6 alkyl group, a C-i-6 haloalkyl group (the C-i-6 alkyl group and the Ci-6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, Ci- 3 alkoxy groups, C -3 alkylthio groups, C -3 alkylsulfonyl groups, C3 -6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, cyano groups, C -6 alkoxy groups, C -6 haloalkoxy groups and C-i-6 alkoxycarbonyl groups)), a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3 - 6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, cyano groups, Ci-6 alkyl groups, 1-6 haloalkyl groups, -6 alkoxy groups, Ci-6 haloalkoxy groups and C -6 alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (58) The compound according to (55) or (57), wherein L b is represented by any of the following formulae (XX - 1) to (XXb-4): (XX -l) (XX -2) (XX -3) (XX -4) (wherein E b is an oxygen atom, and R1 b is a hydrogen atom, a -3 alkyl group (the Ci- 3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group, a C -3 alkoxy group, a C3-6 cycloalkyl group and a phenyl group) or C -3 haloalkyl group)), and R2b is a hydrogen atom, a Ci-3 alkyl group, a Ci -3 haloalkyl group (the C -3 alkyl group and the C1-3 haloalkyl group are unsubstituted or substituted with one or two identical or different substituent selected from the group consisting of hydroxy groups, cyano groups, Ci-3 alkoxy groups, C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a hydroxy group or a halogen atom)), a C 3- 6 cycloalkyl group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered nonaromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -6 alkyl groups, C -3 haloalkyl groups and C -6 alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (59) The compound according to any one of (48) to (53) or (55) to (58), wherein L b is a single bond or a C -3 alkylene group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (60) The compound according to any one of (44) to (59), wherein Xb is a nitrogen atom or CR15b (wherein R15b is a hydrogen atom), and Yb is CR 6b (wherein R16b is a hydrogen atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. g Ab is ( VII b-5 ) ( I I b- ) ( VII - ) (wherein E b is an oxygen atom, and each of R4 , R , R6 , R b, R9b and R10b is independently a hydrogen atom or a C-1 -3 alkyl group), a tautomer or a pharmace acceptable salt of the compound or a solvate thereof. 0), wherein the ring Ab is ) to (XXXIII -3): ( XXXIII" ) ( XXXIII b-l ) ( XXXIII -2) ( XXXIII -3 ) (wherein E2b is an oxygen atom, and each of R4b, R5b, R8b, R9b and R10b are hydrogen atoms, and R6b is a hydrogen atom, a halogen atom or a -3 alkyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (63) The compound according to any one of (49), (60) and (61), wherein L is a single bond, L b is a C-i-3 alkylene group, the ring B is a C4-7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, nb is 0 or 1, R3 is a C-1-3 alkyl group, L3b is a single bond, and R2b is a hydrogen atom or a phenyl group (the phenyl group is unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (64) The compound according to any one of (49), (60) and (61), wherein L b is a single bond, L b is a single bond, the ring Bb is a C4-7 cycloalkane or a 4 to 7-membered non-aromatic heterocycley nb is 0, L3b is a single bond, and R2b is a hydrogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (65) The compound according to any one of (56), (60) and (61), wherein L1b is a single bond, e or a 4 to 7-membered non-aromatic heterocycle, e following formula (Vlll b-1) or (Vlll b-2): b ) ( VIII b-2 ) and R¾ is a Ci-6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with a cyano group or a C3 -6 cycloalkyl group) or a C -3 haloalkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (66) The compound according to any one of (42) to (65), wherein the ring Bb is cyclohexane or piperidine, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (67) The compound according to any one of (42) to (62), wherein the ring Bb is a 4 to 7-membered non-aromatic heterocycle, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 15b (wherein Ib-8): ( XVIII b-l ) ( XVIII b-2 ) ( XVIII b-3 ) ( XVIII b-4 ) ( XVIII b ) ( XVIII b-5 ) ( XVIII -6 ) ( XVIII b-7 ) ( XVIII -8 ) (wherein each of E2b and E b is independently an oxygen atom or a sulfur atom, each of R , R , R , R and R is independently a hydrogen atom, a halogen atom or a C1-3 alkyl group, and R10b is a hydrogen atom, a -6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , a C3-n cycloalkyl group, a 3 to 11- membered non-aromatic heterocyclyl group, a Ce-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3.11 cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C6-i4 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b)), the ring Bb is a C3-11 cycloalkane, a 3 to 11-membered non-aromatic heterocycle, a Ce-14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L1b is single bond or a C -3 alkylene group, L2b is a single bond, a C -6 alkylene group or a C2-6 alkenylene group (the C i -6 alkylene group and the C2-6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), n is 0 or 1, R3b is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C1-3 alkyl group, a Ci-3 haloalkyl group, a C3-6 cycloalkyl group, a C -3 alkoxy group, a C -3 haloalkoxy group or a C1-3 alkylsulfonyl group, L3b is a single bond or represented by any of the following formulae (XXIIb-1) to (XXIIb- 15): b-l ) ( XXII b-2 ) ( XXII -3 ) ( XXII b-4 ) ( XXII b-5 ) XXII ) ( XXII -6 ) ( XXII b-7 ) ( XXII b-8 ) ( XXII -9 ) ( XXII b-10 ) (wherein E is an oxygen atom or a sulfur atom, and each of R 2 and R 3 is independently a hydrogen atom, a C i -6 alkyl group or a C 1-6 haloalkyl group (the C i -6 alkyl group and the C i -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, hydroxy groups, Ci-6 alkoxy groups, C 1-6 alkylthio groups, C1-6 alkylsulfonyl groups, C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the phenyl groups and 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a cyano group, a C 1 3 alkyl group and a C i -3 haloalkyl group))), when L3b is a single bond, R b is a hydrogen atom, a halogen atom, a C3- cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 1 1-membered partially saturated aromatic cyclic group or a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C 3- cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the phenyl group, the naphthyl group, the 5 to 10- membered aromatic heterocyclyl group, the 8 to -membered partially saturated aromatic cyclic group and the 8 to 1 1-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b and the substituent set V9 ) , when L3b is not a single bond, R2b is a hydrogen atom, a C -6 alkyl group, a C 2 -6 alkenyl group (the C -6 alkyl group and the C 2 -6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V6b and the substituent set V9b) , a C3-n cycloalkyl group, a 3 to 11- membered non-aromatic heterocyclyl group, a Ce-14 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3-11 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C 6 - 14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 1 1-membered partially saturated aromatic cyclic group or the 8 to 11-membered aromatic ringcondensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b and the substituent set V b) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. ny ( XXI b-l ) ( XXI b-2) ( XXI b-3 ) ( XXI -4 ) (wherein each of E b and E 3 b is independently an oxygen atom or a sulfur atom, R 4 b , R 5 b , R and R 9 are hydrogen atoms, R 6 b is a hydrogen atom, a halogen atom or a C -3 alkyl group, and R 10b is a hydrogen atom, a C -6 alkyl group (the -6 alkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C -3 alkoxy groups, C i -3 alkylthio groups, mono-Ci .3 alkylamino groups, di-Ci -3 alkylamino groups, mono-Ci-3 alkylaminocarbonyl groups, di-C1-3 alkylaminocarbonyl groups, C 3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 6- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, C -3 alkyl groups and C i-3 haloalkyl groups)), a C -6 haloalkyl group, a C3-6 cycloalkyl group or a 4 to 7-membered non-aromatic heterocyclyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 1), (68) and (69), wherein the ring Ab is or (XXIXb-2): ( X K b-l ) ( X K b-2 ) (wherein E and E are oxygen atoms, R is a hydrogen atom, a halogen atom or a C1-3 alkyl group, R8b is a hydrogen atom, and R10b is a hydrogen atom, a C -6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C 1-3 alkoxy groups, C -3 alkylthio groups, di-C- -3 alkylamino groups, C3-6 cycloalkyl groups and 4 to 7-membered non-aromatic heterocyclyl groups), a C - -6 haloalkyl group, a C3-6 cycloalkyl group or a 4 to 7-membered non-aromatic heterocyclyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (71) The compound according to any one of (41) and (68) to (71), wherein L b is a single bond, L b is a single bond, a C -6 alkylene group, a C2-6 alkenylene group or a C -6 haloalkylene group (the C -6 alkylene group, the C2-6 alkenylene group and the C1-6 haloalkylene group are unsubstituted or substituted with a hydroxy group or a cyano group), the ring Bb is a C 3. cycloalkane or a 4 to 7-membered non-aromatic heterocycle, n is 0 or 1, and R3b is a hydroxy group, a C -3 alkyl group or a C1-3 alkoxy group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (72) The compound according to any one of (41) and (68) to (70), wherein L3b is a single bond, and R2b is a hydrogen atom, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group, a 5 to 10-membered aromatic heterocyclyl group or a 8 to 1 1-membered partially saturated aromatic cyclic group (the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group, the 5 to 10-membered aromatic heterocyclyl group and the 8 to 1 1 - membered partially saturated aromatic cyclic group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, carbamoyl groups, sulfamoyl groups, halogen atoms, cyano groups, nitro groups, C 1-6 alkyl groups (the C -6 alkyl groups are unsubstituted or substituted with a cyano group), C 6 haloalkyl groups, C3-11 cycloalkyl groups, C -6 alkoxy groups, Ci -6 haloalkoxy groups, C1-6 alkylthio groups, C -6 haloalkylthio groups, C -6 alkylsulfonyl groups, Ci -6 haloalkylsulfonyl groups, Ci -6 alkoxycarbonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, mono-Ci-6 alkylamino groups, di-Ci -6 alkylamino groups, phenyl groups, 5 to 6-membered aromatic heterocyclyl groups, mono-Ci -6 alkylaminosulfonyl groups and di-Ci -6 alkylaminosulfonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound o r a solvate thereof. (73) The compound according to (72), wherein R2b is a hydrogen atom, a phenyl group, a 5 to 10-membered aromatic heterocyclyl group or a 8 to 11-membered partially saturated aromatic cyclic group (the phenyl group, the 5 to 10-membered aromatic heterocyclyl group and the 8 to 11-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, nitro groups, Ci-3 alkyl groups, Ci-3 haloalkyl groups and -6 alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound o r a solvate thereof. (74) The compound according to (72), wherein R b is a 4 to 7-membered non-aromatic heterocyclyl group (the 4 to 7-membered non-aromatic heterocyclyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -3 alkyl groups (the C 3 alkyl groups are unsubstituted o r substituted with a cyano group) and C -3 haloalkyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (75) The compound according to any one of (41 ) and (68) to (71 ), wherein L3b is represented by any of the following formulae (XIX b-1) to (XIX b-7): ( X I X ) (wherein E1b is an oxygen atom, and R12b is a hydrogen atom or a C1-6 alkyl group (the C1-6 alkyl group is unsubstituted or substituted with one or more identical o r different substituents independently selected from the group consisting of halogen atoms, cyano groups, hydroxy groups, C1-3 allkoxy groups, C-3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups)), and R2 is a hydrogen atom, a C 6 alkyl group, a C -6 haloalkyl group (the C -6 alkyl group and the Ci- 6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C1-6 alkoxy groups, Ci-6 alkylthio groups, Ci-6 alkylsulfonyl groups, C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3 -6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6- membered aromatic heterocyclyl groups are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of the substituent set V2b, mono-C-1-6 alkylaminosulfonyl groups and di-Ci -6 alkylaminosulfonyl groups)), a C3 6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group, a 5 to 6-membered aromatic heterocyclyl group or a 8 to -membered partially saturated aromatic cyclic group (the C3 -6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group, the 5 to 6- membered aromatic heterocyclyl group and the 8 to 11-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of the substituent set V b, mono-Ci -6 alkylaminosulfonyl groups and di-C-i -6 alkylaminosulfonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. of the (wherein E b is an oxygen atom, and R12b is a hydrogen atom, a C -3 alkyl group (the C - 3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group, a C -3 allkoxy group, a C3 -6 cycloalkyl group and a phenyl group) or C1-3 haloalkyl group), and R b is a hydrogen atom, a -6 alkyl group, a C-1-6 haloalkyl group (the C-1 -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituent selected from the group consisting of hydroxy groups, cyano groups, C1-3 alkoxy groups, C3 -6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a hydroxy group or a halogen atom)), a C3 -6 cycloalkyl group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered nonaromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -3 alkyl groups, C -3 haloalkyl groups and -6 alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (77) The compound according to (75), wherein L3b is represented by the formula b) : ( XXXII b ) (wherein R1 b is a hydrogen atom, a C1-3 alkyl group (the C -3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group, a Ci-3 allkoxy group, a C3-6 cycloalkyl group and a phenyl group) or a C -3 haloalkyl group), and R2b is a hydrogen atom, a C -3 alkyl group, a C1-3 haloalkyl group (the C1-3 alkyl group and the C-1 -3 haloalkyl group are unsubstituted or substituted with one or two identical or different substituent selected from the group consisting of hydroxy groups, cyano groups, C-1-3 alkoxy groups, C3-6 cycloalkyl groups (the C3 - 6 cycloalkyl groups are unsubstituted o r substituted with a hydroxy groups), 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups), a C3 -6 cycloalkyl group or a 4 to 7-membered non-aromatic heterocyclyl group (the C3-6 cycloalkyl group and the 4 to 7-membered non-aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of C 1-3 alkyl groups, C-1-3 haloalkyl groups and C -6 alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (78) The compound according to any one of (41) or (68) to (77), wherein L2b is a single bond or a C 1-3 alkylene group, and the ring B is cyclohexane or piperidine, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. (79) The compound according to any one of (41) to (78), wherein nb is 0 or 1, and R3 is a C 1-3 alkyl group, a tautomer or a pharmaceutically acceptable salt of the compound o r a solvate thereof. (80) A JAK inhibitor containing the compound as defined in any one of ( 1) to (79), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof, as an active ingredient. (81) A preventive, therapeutic or improving agent for diseases against which inhibition of JAK is effective, which contains the JAK inhibitor as defined in (80). (82) A therapeutic agent for articular rheumatism, which contains the JAK inhibitor as defined in (80). (83) Medicament containing the compound as defined in any one of ( 1) to (79), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof, as an active ingredient. The present invention has made it possible to provide novel tricyclic pyrimidine compounds and tricyclic pyridine compounds which have excellent JAK inhibitory action and are especially useful for prevention and treatment of autoimmune diseases, inflammatory diseases and allergic diseases. Now, the present invention will be described in further detail. In the present invention, "n-" denotes normal, "i-" denotes iso, "s-" or "sec" denotes secondary, "t-" or "tert-" denotes tertiary, "c-" denotes cyclo, "0-" denotes ortho, "m-" denotes meta, "p-" denotes para, "cis-" denotes a cis isomer, "trans-" denotes a trans isomer, "(E)-" denotes a E isomer, "(Z)-" denotes a Z isomer, "rac" and "racemate" denotes racemate, "diastereomixture" denotes a mixture of diastereomers, "Ph" denotes phenyl, "Py" denotes pyridyl, "Me" denotes methyl, "Et" denotes ethyl, "Pr" denotes propyl, "Bu" denotes butyl, "Boc" denotes tertiary-butoxycarbonyl, "Cbz" denotes benzyloxycarbonyl, "Ms" denotes methanesulfonyl, "Tf" denotes trifluoromethanesulfonyl, "Ts" denotes p-toluenesulfonyl, "SEM" denotes [2- (trimethylsilyl)ethoxy]methyl, "TIPS" denotes triisopropylsilyl, "TBDPS" denotes tertiarybutyldiphenylsilyl, and "TBS" denotes tertiary-butyldimethylsilyl. First, the terms used herein for description of chemical structures will be explained. A "halogen atom" is a fluorine atom, a chlorine atom, a bromine atom o r an iodine atom. A "Ci-3 alkyl group" is a methyl group, an ethyl group, a propyl group or an isopropyl group. A "C-i -6 alkyl group" is a linear or branched alkyl group containing one to six carbon atoms and may, for example, be a methyl group, an ethyl group, a n-propyl group, an isopropyl group, a n-butyl group, an isobutyl group, a t-butyl group, a n-pentyl group, nhexyl group or the like. A "C1 -3 haloalkyl group" is a group derived from the above-mentioned -3 alkyl group by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "C1 -6 haloalkyl group" is a group derived from the above-mentioned C -6 alkyl group by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "C3-11 cycloalkane" is a monocyclic, fused, bridged or spiro aliphatic hydrocarbon ring having 3 to 1 1 ring-constituting carbon atoms and may, for example, be cyclopropane, cyclobutane, cyclopentane, cyclohexane, cycloheptane, cyclooctane, adamantane, bicyclo[3. 1.OJoctane, bicyclo[2.2. 1Jheptane, spiro[5.5]undecane or the like. A "C-3-11 cycloalkyl group" is a monovalent group derived from the abovementioned "C3.11 cycloalkane" by removing a hydrogen atom at an arbitrary position. A "C3-6 cycloalkane" is a ring having 3 to 6 ring-constituting carbon atoms among the above-mentioned "C 3 -n cycloalkane" and may, for example, be cyclopropane, cyclobutane, cyclopentane, cyclohexane or the like. A "C3-6 cycloalkyl group" is a group having 3 to 6 ring-constituting carbon atoms among the above-mentioned "C 3 -n cycloalkyl group", and may, for example, be a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohexyl group or the like. A "C4 -7 cycloalkane" is a ring having 4 to 7 ring-constituting carbon atoms among the above-mentioned "C 3 -n cycloalkane" and may, for example, be cyclobutane, cyclopentane, cyclohexane, cycloheptane or the like. A "C3.11 cycloalkene" is a non-aromatic ring derived from replacing one or more bonds in the above-mentioned "C3.11 cycloalkane" are replaced by double bond(s) and may, for example, be cyclopropene, cyclobutene, cyclopentene, cyclohexene, cyclohexa-1 ,3-diene, cyclohexa-1 ,4-diene, bicyclo[2.2.1]hepta-2,5-diene, spiro[2.5]oct- 4-ene, 1,2,5,6-tetrahydronaphthalene or the like. A "C2 -6 alkenyl group" is a linear or branched alkenyl group having at least one double bond and 2 to 6 carbon atoms and may, for example be an ethenyl(vinyl) group, a 1-propenyl group, a 2-propenyl(allyl) group, an isopropenyl group, a 1-butenyl group, a 2-butenyl group, a 3-butenyl(homoallyl) group, a 4-pentenyl group, a 5-hexenyl group or the like. A "C2 -3 alkenyl group" is an ethenyl(vinyl) group, a 1-propenyl group, a 2- propenyl(allyl) group or an isopropenyl group. A "C 2 -6 haloalkenyl group" is a group derived from the above-mentioned "C 2 -6 alkenyl group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "C2 -6 alkynyl group" is a linear or branched alkynyl group having at least one triple bond and 2 to 6 carbon atoms and may, for example be an ethynyl group, a 1- propynyl group, a 3-propynyl group, a 1-butynyl group, a 2-butynyl group, a 3-butynyl group, a 4-pentynyl group, a 5-hexynyl group, a 1,5-hexandiynyl group or the like. A "C1 -6 alkoxy group" is a linear or branched alkoxy group having 1 to 6 carbon atoms and may, for example, be a methoxy group, an ethoxy group, a n-propoxy group, an isopropoxy group, a n-butoxy group, an isobutoxy group, a t-butoxy group, a npentyloxy group, a n-hexyloxy group or the like. A "C 1-3 alkoxy group" is a methoxy group, an ethoxy group, a n-propoxy group or an i-propoxy group. A "C -6 haloalkoxy group" is a group derived from the above-mentioned "Ci -6 alkoxy group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "C1-3 haloalkoxy group" is a group derived from the above-mentioned "C 1-3 alkoxy group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "C -6 alkylene group" is a bivalent group derived from the above-mentioned "Ci -6 alkyl group" by removing a hydrogen atom at an arbitrary position and may, for example, be a methylene group, an ethylene group, a propane-1 ,3-diyl group, a propane-1 ,2-diyl group, a 2,2-dimethyl-propane-1 ,3-diyl group, a hexane-1 ,6-diyl group, or a 3- methylbutane-1 ,2-diyl group or the like. A "C1-3 alkylene group" is a methylene group, an ethylene group, a propane-1 ,3- diyl group or a propane-1 ,2-diyl group. A "C -6 haloalkylene group" is a group derived from the above-mentioned "C -6 alkylene group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "C- -3 haloalkylene group" is a group derived from the above-mentioned "C -3 alkylene group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "C2-6 alkenylene group" is a bivalent group derived from the abovementioned "C2 -6 alkenyl group" by removing a hydrogen atom at an arbitrary position and may, for example, be an ethenylene group, an ethene-1 , -diyl group, an ethane- ,2-diyl group, a propene-1 ,1-diyl group, a propene-1 ,2-diyl group, a propene-1 ,3-diyl group, a but-1-ene-1 ,4-diyl group, a but-1 -ene-1 ,3-diyl group, a but-2-ene-1 ,4-diyl group, a but-1 ,3-diene-1 ,4-diyl group, a pent-2-ene-1 ,5-diyl group, a hex-3-ene-1 ,6-diyl group, a hexa-2,4-diene-1 ,6-diyl group or the like. A "C2-3 alkenylene group" is an ethene-1 ,1-diyl group, an ethane-1 ,2-diyl group, a propene-1 ,1-diyl group, a propene-1 ,2-diyl group, a propene-1 ,3-diyl group. A "C-2-6 alkynylene group" is a linear or branched alkynylene group having at least one triple bond and 2 to 6 carbon atoms and may, for example, be an ethyn-1 ,2-diyl group, a propyn-1 ,2-diyl group, a but-1 -yn-1 ,4-diyl group, a but-1 -yn-1 ,3-diyl group, a but-2-yn-1 ,4-diyl group, a pent-2-yn-1 ,5-diyl group, a pent-2-yn-1 ,4-diyl group, a hex-3- yn-1 ,6-diyl group or the like. A "C6- aromatic carbocycle" is a monocyclic, bicyclic or tricyclic aromatic carbocycle having 6 to 14 carbon atoms as the sole ring-constituting atoms and may, for example, be benzene, pentalene, naphthalene, azulene, anthracene, phenanthrene or the like. A "C -14 aryl group" is a monovalent group derived from the above-mentioned "C6- 4 aromatic carbocycle " by removing a hydrogen atom and may have the free valence at any position without particular restriction. A "5 to 0-membered aromatic heterocycle" is a monocyclic or fused aromatic heterocyclyl group having 5 to 10 ring-constituting atoms including 1 to 5 hetero atoms (such as nitrogen atoms, oxygen atoms and sulfur atoms) and may, for example, be furan, thiophene, pyrrole, imidazole, triazole, tetrazole, thiazole, pyrazole, oxazole, isoxazole, isothiazole, thiadiazole, oxadiazole, pyridine, pyrazine, pyridazine, pyrimidine, triazine, purine, pteridine, quinoline, isoquinoline, naphthylidine, quinoxaline, cinnoline, quinazoline, phthalazine, imidazopyridine, imidazothiazole, imidazooxazole, benzothiazole, benzoxazole, benzimidazole, indole, isoindole, indazole, pyrrolopyridine, thienopyridine, furopyridine, benzothiadiazole, benzoxadiazole, pyridopyrimidine, benzofuran, benzothiophene, thienofuran or the like. In the case of a "5 to 10-membered aromatic heterocycle" having a C=N double bond, it may be in the form of an N-oxide. A "5 to 10-membered aromatic heterocyclyl group" is a monovalent group derived from the above-mentioned "5 to 10-membered aromatic heterocycle" by removing a hydrogen atom at an arbitrary position and may have the free valence at any position without particular restrictions. A "5 to 6-membered aromatic heterocycle" is a monocyclic group having 5 to 6 ring-constituting atoms among the above-mentioned "5 to 10-membered aromatic heterocycles" and may, for example, be pyrrole, pyrazole, imidazole, triazole, tetrazole, pyridine, pyridazine, pyrimidine, pyrazine, triazine, furan, thiophene, thiazole, isothiazole, oxazole, isoxazole, oxadiazole, thiadiazole or the like. A "5 to 6-membered aromatic heterocyclyl group" is a monovalent group derived from the above-mentioned "5 to 6-membered aromatic heterocycle" by removing a hydrogen atom at an arbitrary position and may have the free valence at any position without particular restrictions. A "3 to 14-membered non-aromatic heterocycle" is a non-aromatic heterocycle: 1) which has 3 to 14 ring-constituting atoms, 2) the ring-constituting atoms of which contains 1 to 7 hetero atoms selected from nitrogen atoms, oxygen atoms or sulfur atoms, 3) which may have one or more carbonyl groups, one or more double or triple bonds in the ring system, 4) which may contain one or more sulfur atoms in the form of sulfinyl or sulfonyl groups as ring-constituting atoms, and 5) which may be a monocyclic ring, a fused ring (in the fused ring, a non-aromatic ring may be fused to non-aromatic ring(s) or to aromatic-ring(s)), a bridged ring or a spiro ring. It may, for example, be azetidine, pyrrolidine, piperidine, azepane, azocane, tetrahydrofuran, tetrahydropyran, morpholine, thiomorpholine, piperazine, thiazolidine, 1,4-dioxane, imidazoline, thiazoline, benzopyran, isochroman, chroman, indoline, isoindoline, azaindane, tetrahydroazanaphthalene, azachroman, tetrahydrobenzofuran, tetrahydrobenzothiophene, 2,3,4,5-tetrahydro-benzo[b]thiophene, ,3,4-dihydro-2Hbenzo[ b][1 ,4]dioxepane, 6,7-dihydro-5H-cyclopenta[b]pyrazine, 5,6-dihydro-4Hcyclopenta[ b]thiophene, 4,5,6, 7-tetrahydrobenz[b]thiophene, 2,3-dihydroisoindol-1 -one, 3,4-dihydro-2H-isoquinolin-1 -one, 3,4-dihydro-2H-benzo[b]oxepin-5-one, 2,3,4,4a,9,9ahexahydro- 1 H-carbazole, 1'H-spiro[cyclopropane-1 ,2-quinoxalin]-3'(4'H)-one, 10Hphenoxazine, [ 1 ,3]dioxolo[4,5-f]quinoline or the like. A "3 to 14-membered non-aromatic heterocyclyl group" is a monovalent group derived from the above-mentioned "3 to 14-membered non-aromatic heterocycle" by removing a hydrogen atom at an arbitrary position. It may have the free valence at any position without particular restrictions, but in the case of an fused ring system consisting of a non-aromatic ring fused to an aromatic ring, it has the free valence in the nonaromatic ring. A "3 to 11-membereed non-aromatic heterocycle" is non-aromatic heterocycle: ) which has 3 to ring-constituting atoms 2) the ring-constituting atoms of which contains 1 to 5 hetero atoms selected from nitrogen atoms, oxygen atoms or sulfur atoms, 3) which may have one or more carbonyl groups, one or more double or triple bonds in the ring system, 4) which may contain one or more sulfur atoms in the form of sulfinyl or sulfonyl groups as ring-constituting atoms, and 5) which may be a monocyclic ring, a fused ring (in the fused ring, a non-aromatic ring may be fused to non-aromatic ring(s) or to aromatic-ring(s)), a bridged ring or a spiro ring. It may, for example, be azetidine, pyrrolidine, piperidine, azepane, azocane, tetrahydrofuran, tetrahydropyran, morpholine, thiomorpholine, piperazine, thiazolidine, 1,4-dioxane, imidazoline, thiazoline, benzopyran, isochroman, chroman, indoline, isoindoline, azaindane, tetrahydroazanaphthalene, azachroman, tetrahydrobenzofuran, tetrahydrobenzothiophene, 2,3,4,5-tetrahydro-benzo[b]thiophene, 3,4-dihydro-2Hbenzo[ b][1 ,4]oxepine, 6,7-dihydro-5H-cyclopenta[b]pyrazine, 5,6-dihydro-4Hcyclopenta[ b]thiophene, 4,5,6,7-tetrahydrobenzo[b]thiophene, 2,3-dihydroisoindol-1 -one, 3,4-dihydro2H-isoquinolin-1-one, 3,4-dihydro2H-benzo[b]oxepin-5-one or the like. A 3 to 1 1-membered non-aromatic heterocyclyl group" is a monovalent group derived from the above-mentioned "3 to 11-membered non-aromatic heterocycle" by removing a hydrogen atom at an arbitrary position. It may have the free valence at any position without particular restrictions, but in the case of an fused ring system consisting of a non-aromatic ring fused to an aromatic ring, it has the free valence in the nonaromatic ring. A "4 to 7-membered non-aromatic heterocycle" is a monocyclic non-aromatic heterocycle: 1) which has 4 to 7 ring-constituting atoms 2) the ring-constituting atoms of which contains 1 to 3 hetero atoms selected from nitrogen atoms, oxygen atoms and sulfur atoms, 3) which may have one or more carbonyl groups, one or more double or triple bonds in the ring system, and 4) which may contain one or more sulfur atoms in the form of sulfinyl or sulfonyl groups as ring-constituting atoms. It may, for example, be azetidine, pyrrolidine, pyrrolidinone, oxazolidine, isoxazolidine, thiazolidine, isothiazolidine, piperazine, piperazinone, piperidine, piperidinone, morpholine, thiomorpholine, azepine, diazepine, oxetane, tetrahydrofuran, 1,3-dioxorane, tetrahydropyran, 1,4-dioxane, oxepane, homomorpholine or the like. A "4 to 7-membered non-aromatic heterocyclyl group" is a monovalent group derived from the above-mentioned "4 to 7-membered non-aromatic heterocycle" by removing a hydrogen atom at an arbitrary position and may have the free valence at any position without particular restrictions. A "C-1-6 alkylthio group" is a group consisting of the above-mentioned " C - 6 alkyl group" attached to a sulfur atom and may, for example, be a methylthio group, an ethylthio group, a n-propylthio group, an isopropylthio group, a n-butylthio group, an isobutylthio group, a t-butylthio group, a n-pentylthio group, a n-hexylthio group or the like. A "Ci-3 alkylthio group" is a group consisting of the above-mentioned "C-i -3 alkyl group" attached to a sulfur atom and may, for example, be a methylthio group, an ethylthio group, a n-propylthio group or an isopropylthio group. A "Ci-6 haloalkylthio group" is a group derived from the above-mentioned " -6 alkylthio group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "C -3 haloalkylthio group" is a group derived from the above-mentioned "C-i-3 alkylthio group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "Ci-6 alkylsulfonyl group" is a group consisting of the above-mentioned "C -6 alkyl group" attached to a sulfonyl group and may, for example, be a methylsulfonyl group, an ethylsulfonyl group, a n-propylsulfonyl group, an isopropylsulfonyl group, a nbutylsulfonyl group, an isobutylsulfonyl group, a t-butylsulfonyl group, a n-pentylsulfonyl group, a n-hexylsulfonyl group or the like. A "C-i -3 alkylsulfonyl group" is a group consisting of the above-mentioned "Ci-3 alkyl group" attached to a sulfonyl group and may, for example, be a methylsulfonyl group, an ethylsulfonyl group, a n-propylsulfonyl group or an isopropylsulfonyl group. A "C - haloalkylsulfonyl group" is a group derived from the above-mentioned "C1-6 alkylsulfonyl group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "Ci-3 haloalkylsulfonyl group" is a group derived from the above-mentioned "Ci -3 alkylsulfonyl group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "C-i -6 alkoxycarbonyl group" is a group consisting of the above-mentioned "C -6 alkoxy group" attached to a carbonyl group and may, for example, be a methoxycarbonyl group, an ethoxycarbonyl group, a n-propoxycarbonyl group, an isopropoxycarbonyl group, a n-butoxycarbonyl group, an isobutoxycarbonyl group, a tbutoxycarbonyl group, a n-pentyloxycarbonyl group, a n-hexyloxycarbonyl group or the like. A "Ci-3 alkoxycarbonyl group" is a methoxycarbonyl group, an ethoxycarbonyl group, a n-propoxycarbonyl group or an isopropoxycarbonyl group. A "mono-Ci -6 alkylamino group" is a group consisting of the above-mentioned "Ci -6 alkyl group" attached to an amino group and may, for example, be a methylamino group, an ethylamino group, a n-propylamino group, an isopropylamino group, a n-butylamino group, an isobutylamino group, a t-butylamino group, a n-pentylamino group, a nhexylamino group or the like. A "mono-Ci -3 alkylamino group" is a methylamino group, an ethylamino group, a npropylamino group or an isopropylamino group. A "di-C- -6 alkylamino group" is a group consisting of an amino group attached to two identical or different "C -6 alkyl groups" such as those mentioned above and may, for example, be a dimethylamino group, a diethylamino group, a di-n-propylamino group, a diisopropylamino group, a di-n-butylamino group, a diisobutylamino group, a di-tbutylamino group, a di-n-pentylamino group, a di-n-hexylamino group, an N-ethyl-Nmethylamino group, an N-methyl-N-n-propylamino group, an N-isopropyl-Nmethylamino group, an N-n-butyl-N-methylamino group, an N-isobutyl-N-methylamino group, an N-t-butyl-N-methylamino group, an N-methyl-N-n-pentylamino group, N-nhexyl- N-methylamino group, an N-ethyl-N-n-propylamino group, an N-ethyl-Nisopropylamino group, an N-n-butyl-N-ethylamino group, an N-ethyl-N-isobutylamino group, an N-t-butyl-N-ethylamino group, an N-ethyl-N-n-pentylamino group, an N-ethyl- N-n-hexylamino group or the like. A "di-Ci -3 alkylamino group" is a dimethylamino group, a diethylamino group, a din- propylamino group, a diisopropylamino group, an N-ethyl-N-methylamino group, an Nmethyl- N-n-propylamino group, an N-isopropyl-N-methylamino group, an N-ethyl-N-npropylamino group or an N-ethyl-N-isopropylamino group. A "Ci-6 alkylcarbonyl group" is a group consisting of the above-mentioned "Ci -6 alkyl group" attached to a carbonyl group and may, for example, be an acetyl group, a propionyl group, a butyryl group, an isobutyryl group, a pentanoyl group, a 3- methylbutanoyl group, a pivaloyl group, a hexanoyl group or a heptanoyl group. A "C -3 alkylcarbonyl group" is an acetyl group, a propionyl group, a butyryl group or an isobutyryl group. A "Ci-6 haloalkylcarbonyl group" is a group derived from the above-mentioned " - 6 alkylcarbonyl group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "Ci-3 haloalkylcarbonyl group" is a group derived from the above-mentioned "Ci- 3 alkylcarbonyl group" by replacing one or more hydrogen atom(s) at arbitrary position(s) by one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms. A "mono-Ci -6 alkylaminocarbonyl group" is a group consisting of the abovementioned "mono-Ci-6 alkylamino group" attached to a carbonyl group and may, for example, be a methylaminocarbonyl group, an ethylaminocarbonyl group, a npropylaminocarbonyl group, an isopropylaminocarbonyl group, a n-butylaminocarbonyl group, an isobutylaminocarbonyl group, a t-butylaminocarbonyl group, a npentylaminocarbonyl group, a n-hexylaminocarbonyl group or the like. A "mono-Ci-3 alkylaminocarbonyl group" is a methylaminocarbonyl group, an ethylaminocarbonyl group, a n-propylaminocarbonyl group or an isopropylaminocarbonyl group. A "di-Ci -6 alkylaminocarbonyl group" is a group consisting of the above-mentioned "di-Ci-6 alkylamino group" attached to a carbonyl group and may, for example, be a dimethylaminocarbonyl group, a diethylaminocarbonyl group, a di-npropylaminocarbonyl group, a diisopropylaminocarbonyl group, a di-nbutylaminocarbonyl group, a diisobutylaminocarbonyl group, a di-t-butylaminocarbonyl group, a di-n-pentylaminocarbonyl group, a di-n-hexylaminocarbonyl group, an N-ethyl- N-methylaminocarbonyl group, an N-methyl-N-n-propylaminocarbonyl group, an Nisopropyl- N-methylaminocarbonyl group, an N-n-butyl-N-methylaminocarbonyl group, an N-isobutyl-N-methylaminocarbonyl group, an N-t-butyl-N-methylaminocarbonyl group, an N-methyl-N-n-pentylaminocarbonyl group, an N-n-hexyl-N-methylaminocarbonyl group, an N-ethyl-N-n-propylaminocarbonyl group, an N-ethyl-Nisopropylaminocarbonyl group, an N-n-butyl-N-ethylaminocarbonyl group, an N-ethyl-Nisobutylaminocarbonyl group, an N-t-butyl-N-ethylaminocarbonyl group, an N-ethyl-N-npentylaminocarbonyl group, an N-ethyl-N-n-hexylaminocarbonyl group or the like. A "di-C -3 alkylaminocarbonyl group" is a dimethylaminocarbonyl group, a diethylaminocarbonyl group, a di-n-propylaminocarbonyl group, a diisopropylaminocarbonyl group, an N-ethyl-N-methylaminocarbonyl group, an Nmethyl- N-n-propylaminocarbonyl group, an N-isopropyl-N-methylaminocarbonyl group, N-ethyl-N-n-propylaminocarbonyl group, or an N-ethyl-N-isopropylaminocarbonyl group. A "C-1-6 alkylcarbonylamino group" is a group consisting of the above-mentioned "C -6 alkylcarbonyl group" attached to an amino group and may, for example, be a methylcarbonylamino group, an ethylcarbonylamino group, a n-propylcarbonylamino group, an isopropylcarbonylamino group, a n-butylcarbonylamino group, an isobutylcarbonylamino group, a t-butylcarbonylamino group, a n-pentylcarbonylamino group, a n-hexylcarbonylamino group or the like. A "Ci -3 alkylcarbonylamino group" is a methylcarbonylamino group, an ethylcarbonylamino group, a n-propylcarbonylamino group or an isopropylcarbonylamino group. A "mono-Ci -6 alkylaminosulfonyl group" is a group consisting of the abovementioned "mono-Ci -6 alkylamino group" attached to a sulfonyl group and may, for example, be a methylaminosulfonyl group, an ethylaminosulfonyl group, a npropylaminosulfonyl group, an isopropylaminosulfonyl group, a n-butylaminosulfonyl group, an isobutylaminosulfonyl group, a t-butylaminosulfonyl group, a npentylaminosulfonyl group, a n-hexylaminosulfonyl group or the like. A "mono-C -3 alkylaminosulfonyl group" is a methylaminosulfonyl group, an ethylaminosulfonyl group, a n-propylaminosulfonyl group or an isopropylaminosulfonyl group. A "di-Ci -6 alkylaminosulfonyl group" is a group consisting of the above-mentioned "di-Ci -6 alkylamino group" attached to a sulfonyl group and may, for example, be a dimethylaminosulfonyl group, a diethylaminosulfonyl group, a di-n-propylaminosulfonyl group, a diisopropylaminosulfonyl group, a di-n-butylaminosulfonyl group, a diisobutylaminosulfonyl group, a di-t-butylaminosulfonyl group, a di-npentylaminosulfonyl group, a di-n-hexylaminosulfonyl group, an N-ethyl-Nmethylaminosulfonyl group, an N-methyl-N-n-propylaminosulfonyl group, an Nisopropyl- N-methylaminosulfonyl group, an N-n-butyl-N-methylaminosulfonyl group, an N-isobutyl-N-methylaminosulfonyl group, an N-t-butyl-N-methylaminosulfonyl group, an N-methyl-N-n-pentylaminosulfonyl group, N-n-hexyl-N-methylaminosulfonyl group, an N-ethyl-N-n-propylaminosulfonyl group, an N-ethyl-N-isopropylaminosulfonyl group, an N-n-butyl-N-ethylaminosulfonyl group, an N-ethyl-N-isobutylaminosulfonyl group, an N-tbutyl- N-ethylaminosulfonyl group, an N-ethyl-N-n-pentylaminosulfonyl group, an Nethyl- N-n-hexylaminosulfonyl group or the like. A "di-Ci -3 alkylaminosulfonyl group" is a dimethylaminosulfonyl group, a diethylaminosulfonyl group, a di-n-propylaminosulfonyl group, a diisopropylaminosulfonyl group, an N-ethyl-N-methylaminosulfonyl group, an N-methyl- N-n-propylaminosulfonyl group, an N-isopropyl-N-methylaminosulfonyl group, an Nethyl- N-n-propylaminosulfonyl group, or an N-ethyl-N-isopropylaminosulfonyl group or an N-isopropyl-N-n-propylaminosulfonyl group. A "Ci -6 alkylsulfonylamino group" is a group consisting of the abovementioned "C - alkylsulfonyl group" attached to an amino group and may, for example, be a methylsulfonylamino group, an ethylsulfonylamino group, a n-propylsulfonylamino group, an isopropylsulfonylamino group, a n-butylsulfonylamino group, an isobutylsulfonylamino group, a t-butylsulfonylamino group, a n-pentylsulfonylamino group, a n-hexylsulfonylamino group or the like. A "C -6 alkoxycarbonylamino group" is a group consisting of the abovementioned "C1 -6 alkoxycarbonyl group" attached to an amino group and may, for example, be a methoxycarbonylamino group, an ethoxycarbonylamino group, a npropoxycarbonylamino group, an isopropoxycarbonylamino group, a nbutoxycarbonylamino group, an isobutoxycarbonylamino group, a t - butoxycarbonylamino group, a n-pentyloxycarbonylamino group, a nhexyloxycarbonylamino group or the like. A "C-3-6 cycloalkoxy group" is a group consisting of the above-mentioned "C3 -6 cycloalkyi group" attached to an oxygen atom and may, for example, be a cyclopropoxy group, a cyclobutoxy group, a cyclopentyloxy group, a cyclohexyloxy group or the like. A "C-3-6 cycloalkylamino group" is a group consisting of the above-mentioned "C3-6 cycloalkyi group" attached to an amino group and may, for example, be a cyclopropylamino group, a cyclobutylamino group, a cyclopentylamino group, a cyclohexylamino group or the like. A "di-C-3-6 cycloalkylamino group" is a group consisting of an amino group attached to two identical or different "C3 -6 cycloalkyi groups" such as those mentioned above and may, for example, be a dicyclopropylamino group, a dicyclobutylamino group, a dicylopentylamino group, a dicyclohexylamino group or the like. A "C-3-6 cycloalkylthio group" is a group consisting of the "C3 -6 cycloalkyi group" attached to -S- and may, for example, be a cyclopropylthio group, a cyclobutylthio group, a cyclopentylthio group, a cyclohexylthio group or the like. A "C3 -6 cycloalkylcarbonyl group" is a group consisting of the above-mentioned "C3 -6 cycloalkyi group" attached to a carbonyl group and may, for example, be a cyclopropylcarbonyl group, a cyclobutylcarbonyl group, a cyclopentylcarbonyl group, a cyclohexylcarbonyl group or the like. A "C3 -6 cycloalkylsulfonyl group" is a group consisting of the above-mentioned "C3- cycloalkyi group" attached to a sulfonyl group and may, for example, be a cyclopropylsulfonyl group, a cyclobutylsulfonyl group, a cyclopentylsulfonyl group, a cyclohexylsulfonyl group or the like. A "8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon" is a fused ring system: 1) which has 8 to 14 ring-constituting atoms, 2) all the ring-constituting atoms of which are carbon atoms, 3) which may have one or more carbonyl groups, one o r more double or triple bonds in the ring system, and 4) which consists of non-aromatic ring(s) fused to aromatic-ring(s). It may, for example, be 1H-indene, 2,3-dihydroindene, 1H-inden-1-on, 1,2-dihydronaphthalene, 1,2,3,4- tetrahydronaphthalene, 3,4-dihydronaphthalen-1 (2H)-on, 1,2,3,4-tetrahydro-1 ,4- methanonaphthalene, 1,2,3,4-tetrahydrophenanthrene, 2,3-dihydro-I H-phenalene, 9Hfluorene or the like. A "8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group" is a monovalent group derived from the above-mentioned "8 to 14-membered aromatic ringcondensed alicyclic hydrocarbon" by removing a hydrogen atom at an arbitrary position. It may have the free valence at any position in the alicyclic carbocycle without particular restrictions. It may, for example, be a 1H-inden-1 -yl group, a 1H-inden-2-yl group, a 1H-inden3- yl group, a 1,2,3,4-tetrahydronaphthalen-1-yl group, a 1,2,3,4-tetrahydronaphthalen-2- yl group, a 1,2,3,4-tetrahydronaphthalen-3-yl group, a 1,2,3,4-tetrahydronaphthalen-4-yl group, a 4-OXO-1,2,3,4-tetrahydronaphthalen-l -yl group, a 9H-fluoren-9-yl group or the like. A "8 to 14-membered partially saturated aromatic cyclic group" is a group derived from 1) a bicyclic or tricyclic ring having 8 to 14 ring-constituting atoms and consisting of a non-aromatic ring fused to aromatic rings among the above-mentioned "3 to 14- menbered non-aromatic heterocycle " or 2) the above-mentioned "8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon" by removing a hydrogen atom at an arbitrary position. It may have the free valence at any position in the aromatic ring without particular restrictions. It may, for example, be a 1H-inden-4-yl group, a 1H-inden-5-yl group, a 1H-inden- 6-yl group, a 1H-inden-7-yl group, a 5,6,7,8-tetrahydronaphthalen-1-yl group, a 5,6,7,8- tetrahydronaphthalen-2-yl group, a 5,6,7,8-tetrahydronaphthalen-3-yl group, a 5,6,7,8- tetrahydronaphthaleh-4-yl group, a 9H-fluorene2-yl group, an indolin-4-yl group, an indolin-5-yl group, an indolin-6-yl group, an indolin-7-yl group, a chroman-5-yl group, a chroman-6-yl group, a chroman-7-yl group, a chroman-8-yl group, a 4,5,6,7- tetrahydrobenzo[b]thiophen-3-yl group, a 2,3,4,4a, 9,9a-hexahydro-1 H-carbazol-5-yl group or the like. A "8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon" is a fused ring system: 1) which has 8 to 11 ring-constituting atoms, 2) all the ring-constituting atoms of which are carbon atoms, 3) which may have one or more carbonyl groups, one or more double or triple bonds in the ring system, and 4) which consists of an alicyclic hydrocarbon fused to a benzene ring, and it may, for example, be 1H-indene, 2,3-dihydroindene, H-inden-1-on, 1,2-dihydronaphthalene, 1,2,3,4-tetrahydronaphthalene, 3,4-dihydronaphthalen-1 (2H)-one or the like. A "8 to 1 -membered aromatic ring-condensed alicyclic hydrocarbon group" is a group derived from the above-mentioned "8 to 1 1-membered aromatic ring-condensed alicyclic hydrocarbon" by removing a hydrogen atom at an arbitrary position, and may have the free valence at any position in the alicyclic carbocycle without particular restrictions. It may, for example, be a 1H-inden-4-yl group, a 1H-inden-5-yl group, a 1H-inden- 6-yl group, a 1H-inden-7-yl group, a 5,6,7,8-tetrahydronaphthalen-1 -yl group, a 5,6,7,8- tetrahydronaphthalen-2-yl group, a 5,6,7,8-tetrahydronaphthalen-3-yl group, a 5,6,7,8- tetrahydronaphthalen-4-yl group or the like. A "8 to 1 -membered partially saturated aromatic cyclic group" is a group derived from 1) a partially saturated aromatic ring having 8 to 1 1 ring-constituting atoms and consisting of an aromatic ring fused to a non-aromatic ring or 2) the above-mentioned "8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group" by removing a hydrogen atom at an arbitrary position and may have the free valence at any position in the aromatic ring without particular restrictions. It may, for example, be a 1H-inden-4-yl group, a 1H-inden-5-yl group, a 1H-inden- 6-yl group, a 1H-inden-7-yl group, a 5,6,7,8-tetrahydronaphthalen-1-yl group, a 5,6,7,8- tetrahydronaphthalen-2-yl group, a 5,6,7,8-tetrahydronaphthalen-3-yl group, a 5,6,7,8- tetrahydronaphthalen-4-yl group, an indolin-4-yl group, an indolin-5-yl group, an indolin- 6-yl group, an indolin-7-yl group, a chroman-5-yl group, a chroman-6-yl group, a chroman-7-yl group, a chroman-8-yl group, 4,5,6,7-tetrahydrobenzo [b]thiophen-3-yl group or the like. Now, the tricyclic pyrimidine compounds of the present invention represented by the formula (la) will be described. First, how the ring Aa is fused in the tricyclic pyrimidine compounds of the present invention will be described. As is indicated in the formula (la) , the ring Aa is fused to the pyrimidine ring so as to have a carbon atom and a nitrogen atom in common and attached to L a via a carbon atom in the ring Aa in the formula (la) . ented by the formula (lla-1), ed by the formula (la)-2: and when the ring Aa is represented by the formula (lla-2) the molecule as a whole is represented by the formula (la)-3. In the present invention, the formulae representing L a indicate that the left ends of the formulae are bonded to L2a, and the right ends of the formulae are bonded to R a. In the present invention, L a , L2a and R3a may be bounded to the ring Ba in the formula (la) at any positions of the ring Ba without any particular restrictions. Next, preferred structures of the respective substituents will be mentioned. A preferred embodiment of the substltuent R a is a hydrogen atom or a halogen atom. A more preferred embodiment of the substltuent R a is a hydrogen atom. A preferred embodiment of the substltuent Ya is CR10a (wherein R 0a is a hydrogen atom, a halogen atom, a cyano group, a C -6 alkyl group, a -6 haloalkyl group or a C-3-6 cycloalkyl group). A more preferred embodiment of the substltuent Ya is CR 0a (wherein R10a is a hydrogen atom). A preferred embodiment of the substltuent Xa is CR9a (wherein R9a is a hydrogen atom, a halogen atom, a cyano group, a C -6 alkyl group, a C -6 haloalkyl group or a C3-6 cycloalkyl group) or a nitrogen atom. A more preferred embodiment of the substltuent Xa is CR9a (wherein R9a is a hydrogen atom). Another more preferred embodiment of the substltuent Xa is CR9a (wherein R9a is a halogen atom). A preferred embodiment of the ring Aa is represented by any of the following formulae (Vll a-1) to (Vll a-4) ( VIIM ) ( VIIa-2 ) ( VIIa-3 ) ( VIIM ) (wherein E a is an oxygen atom or a sulfur atom, each of R4a, R a and R a is independently a hydrogen atom, an amino group, a carbamoyl group, a halogen atom, a cyano group, a C -6 alkyl group, a C -6 alkoxy group, a C -6 alkylthio group, a C-1 -6 alkylsulfonyl group (the C -6 alkyl group, the C -6 alkoxy group, the Ci-6 alkylthio group and the C1-6 alkylsulfonyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substltuent set V3a) , a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3 -6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6- membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substltuent set V a) , and R6a is a hydrogen atom, a C -6 alkyl group (the Ci-6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substltuent set V3a) , a C3-6 cycloalkyl group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered nonaromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or ifferent substituents independently selected from the substituent set V a)). ny of the following ( IVa-l ) ( IVa-2 ( I Va-3 (wherein E is an oxygen atom or a sulfur atom, R is a hydrogen atom, a halogen atom, a C1-3 alkyl group, a C1-3 alkoxy group, a Ci-3 alkylthio group or a -3alkylsulfonyl group, and R6a is a hydrogen atom or a C1-3 alkyl group). A further preferred embodiment of the ring Aa is represented by any of the following formulae (Vlll a- 1) to (Vlll a-5). ( VIIIM ) ( VIII -2 ) ( VIII a-3 ) ( VIIIM ) ( VIII a-5 ) A particularly preferred embodiment of the ring Aa is represented by the formula A preferred embodiment of he substituent L a is a single bond or a C- -3 alkylene group. A more preferred embodiment of the substituent L1a is a single bond or a methylene group. A further preferred embodiment of the substituent L a is a single bond. A preferred embodiment of the ring Ba is a C3- cycloalkane, a 3 to 11-membered non-aromatic heterocycle, a C-6- 4 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle. Another preferred embodiment of the ring Ba is a C3. cycloalkane (a ringconstituting methylene group of the C3-n cycloalkane and the C3- cycloalkene is replaced by a carbonyl group). A more preferred embodiment of the ring Ba is a C4 -7 cycloalkane, a 4 to 7- membered non-aromatic heterocycle, benzene or a 5 to 6-membered aromatic heterocycle. Another more preferred embodiment of the ring Ba is a C4-7 cycloalkane (a ringconstituting methylene group of the C4-7 cycloalkane is replaced by a carbonyl group). Another more preferred embodiment of the ring Ba is spiro[2,5]octane or adamantane. A further preferred embodiment of the ring Ba is azetidine, pyrrolidine, piperidine, azepane, cyclobutane, cyclopentane, cyclohexane, bicyclo[2.2.1]heptane, cycloheptane or benzene. Another further preferred embodiment of the ring Ba is cyclohexanone. A particularly preferred embodiment of the ring Ba is cyclohexane or piperidine. A preferred embodiment of the substituent L2a is a single bond, a C -3 alkylene group or a C -3 haloalkylene group (the Ci-3 alkylene group and the C -3 haloalkylene group are substituted with a cyano group). Another preferred embodiment of the substituent L2a is a C -3 alkylene group or a C1-3 haloalkylene group (the Ci -3 alkylene group and the C -3 haloalkylene group are unsubstituted or substituted with a hydroxy group). Another preferred embodiment of the substituent L2a is a C-2-3 alkenylene group (the C2-3 alkenylene group is unsubstituted or substituted with a hydroxy group or a cyano group). Another preferred embodiment of the substituent L a is a C -3 alkylene group or a C2-3 alkenylene group (the C -3 alkylene group and the C2-3 alkenylene group are substituted with two cyano groups). Another preferred embodiment of the substituent L a is a C1-6 alkylene group or a C2-6 alkenylene group (the C -6 alkylene group and the C2-6 alkenylene group are unsubstituted or substituted with one or two cyano groups) or a Ci-6 haloalkylene. Another preferred embodiment of the substituent L2a is =C(R15a)- (wherein R 5a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L2a is a double bond) or =C(R15a)-CH 2- (wherein R15a is a cyano group, and the bond connecting the ring Ba and L2a is a double bond). A more preferred embodiment of the substituent L2a is a single bond or a methylene group (the methylene group is unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms or with a hydroxy group). Another more preferred embodiment of the substituent L a is an ethylene group (the ethylene group is unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms or with a hydroxy group) or a propylene group. Another more preferred embodiment of the substituent L a is a Ci -3 alkylene group (the Ci-3 alkylene group is substituted with a cyano group). Another more preferred embodiment of the substituent L a is a C -3 alkylene group (the Ci-3 alkylene group is substituted with two cyano groups). Another more preferred embodiment of the substituent L2a is a C2-3 alkenylene group (the C-2-3 alkenylene group is substituted with a cyano group). Another more preferred embodiment of the substituent L a is a C2-3 alkenylene group (the C2-3 alkenylene group is substituted with two cyano groups). A further preferred embodiment of the substituent L a is a single bond or a methylene group. Another further preferred embodiment of the substituent L a is a C -3 alkylene group (the C1-3 alkylene group is substituted with one or two cyano groups). A preferred embodiment of the substituent L3a and the substituent R a is such that L3a is a single bond, and R a is a hydrogen atom, a halogen atom, a C3.6 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the C-3-6 cycloalkyl group, the 3 to 11 - membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10- membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) . Another preferred embodiment of the substituent L3a and the substituent R a is such that L3a is a single bond, and R2a is a hydrogen atom, a halogen atom, an azido group, a C3-6 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the C3.6 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of the substituent set V a, the substituent set V9a and C -6 alkyl groups (the C-1-6 alkyl groups are substituted with a Ci-6 alkoxycarbonylamino group (the Ci-6 alkoxycarbonylamino group is unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms))). Another preferred embodiment of the substituent L a and the substituent R a is such that L3a is a single bond, and R2a is a 8 to 11-membered partially saturated aromatic cyclic group (the 8 to 11-membered partially saturated aromatic cyclic group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) . Another preferred embodiment of the substituent L3a and the substituent R a is such that L3a is represented by any of the foll win f rmula Va-1 to Va- 1 : ( V ) ( Va-2 ) ( Va-3 ) ( Va-4 ) ( Va-5 ) ( Va-6 ) ( Va-7 ) (Va-8 ) ( Va-9 ) ( Va-10 ) ( Va-ll ) (wherein E a is an oxygen atom or a sulfur atom, and each of R12a and R13a is independently a hydrogen atom , a Ci-6 alkyl group or a C- -6 haloalkyl group), and R a is a hydrogen atom, a C -6 alkyl group (the C 1-6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5a), a C 2-6 alkenyl group, a C 3-6 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the C 2 - 6 alkenyl group, the C 3 - 6 cycloalkyl group, the 3 to 11- membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10- membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a) . Another preferred embodiment of the substituent L3a and the substituent R2a is such that L3a is represented by any of the following formulae (XIVa-1) to (XIVa-15) and (Xlll a) : ( XIVM ) ( XIVa-2 ) ( XIV -3 ) ( XIVM ) ( XIVa-5 ) ( a-6 ) ( XIVa-7 ) ( XIVa-8 ) ( XIVa-9 ) ( X V O) ( XIV l ) ( XIVa-12 ) ( XIV 3 ) ( XIVa-14 ) ( XIVa-15 ) ( XIIIa ) an oxygen atom, a sulfur atom or NR11a (wherein R>11aa is a hydroxy group), and each of R 2a and R 3a is independently a hydrogen atom, a C -6 alkyl group or a C -6 haloalkyl group), and R2a is a hydrogen atom, a C -6 alkyl group, a C2 -6 alkenyl group, a C2 -6 alkynyl group (the C -6 alkyl group, the C2 -6 alkenyl group and the C2-6 alkynyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V6a and the substituent set V9a) , a C3-11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3.11 cycloalkyl group, the 3 to 11- membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 11-membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) . bodiment of the substituent L3a and the substituent R a is by the formula (Xa-9): R2a is a hydrogen atom. Another preferred embodiment of the substituent L3a and the substituent R a is such that L3a is represented by any of the following formulae (XXVI a- 1) to (XXVI a-5): ( XXVI ) ( XXVIa-2 ) ( XXVI -3 ) ( XXVI ) ( XXVIa-5 ) (wherein E a is an oxygen atom or a sulfur atom, and R1 a is a Ci-6 alkyl group or a -6 haloalkyl group (the Ci-6 alkyl group and the C -6 haloalkyl group is substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, halogen atoms, cyano groups, nitro groups, C1-6 alkoxy groups, -6 haloalkoxy groups, C -6 alkylthio groups, Ci-6 haloalkylthio groups, Ci-6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-C-i-6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-C - alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups, C3-11 cycloalkyi groups, 3 to 1 -membered non-aromatic heterocyclyl groups, C6- aryl groups and 5 to 0-membered aromatic heterocyclyl groups (the C3 -n cycloalkyi groups, the 3 to 1 1-membered non-aromatic heterocyclyl groups, the C 6 - aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a)), a C-3- cycloalkyi group, a 3 to 11- membered non-aromatic heterocyclyl group, a C-6-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3-11 cycloalkyi group, the 3 to 1 1-membered nonaromatic heterocyclyl group, the C-6-14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted and substituted with one or more identical or different substituents independently selected from the substituent set V a)), and R2a is a -6 alkyl group, a C2 -6 alkenyl group, a C2-6 alkynyl group (the Ci-6 alkyl group, the C 2-6 alkenyl group and the C 2 -6 alkynyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V6a and the substituent set V9a) , a C3-6 cycloalkyi group, a 3 to 1 1 - membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 10-membered aromatic heterocyclyl group (the C-3-6 cycloalkyi group, the 3 to 1 1 - membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V a) . A more preferred embodiment of the substituent L3a and the substituent R2a is such that L3a is a single bond, and R a is a hydrogen atom, a halogen atom, a C3-6 cycloalkyi group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyi group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) . Another more preferred embodiment of the substituent L3a and the substituent R2a is such that L3a is a single bond, and R2a is a 3 to 1-membered non-aromatic heterocyclyl group (the 3 to 1 1-membered non-aromatic heterocyclyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) . Another more preferred embodiment of the substituent L3a and the substituent R2a is such that L3a is a single bond, and R a is a C 3-6 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3 -6 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are substituted with identical or different one ,two or three substituents independently selected from the group consisting of C i -6 alkyl groups, C 1-6 alkoxy groups, C -6 alkylthio groups, C -6 alkylsulfonyl groups, C -6 alkylcarbonyl groups (the - 6 alkyl groups, the C -6 alkoxy groups, the C -6 alkylthio groups, the C -6 alkylsulfonyl groups and the Ci- 6 alkylcarbonyl groups are substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C 1-6 alkoxy group and a C 1-6 alkoxycarbonylamino group), C - -6 alkoxycarbonyl groups, mono-Ci- 6 alkylamino groups, di-Ci- 6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C - alkylcarbonylamino groups, (the C-1-6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-C 1-6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the d-6 alkylcarbonylamino groups are substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms or with a hydroxy group or a cyano group), mono-alkylaminosulfonyl groups, di-C- -6 alkylaminosulfonyl groups, C -6 alkylsulfonylamino groups, C -6 alkoxycarbonylamino groups (the mono-C-1-6 alkylaminosulfonyl groups, the di-Ci -6 alkylaminosulfonyl groups, the C -6 alkylsulfonylamino groups and the C -6 alkoxycarbonylamino groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the substituent set V a)). Another more preferred embodiment of the substituent L3a and the substituent R a is such that L3a is a single bond, and R a is a C3-6 cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are substituted with a substituent selected from the group consisting of a C 6 alkyl group, a C -6 alkoxy group (the C i -6 alkyl group and the C 1-6 alkoxy group are substituted with a hydroxy group or a cyano group), a mono-d-6 alkylamino group, a did- 6 alkylamino group, a mono-d-6 alkylaminocarbonyl group, a C -6 alkylcarbonylamino group (the mono-Ci -6 alkylamino group, the di-Ci -6 alkylamino group, the mono-d- 6 alkylaminocarbonyl group and the C -6 alkylcarbonylamino group are substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups and cyano groups), a phenyl group, a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, C -6 alkyl groups and d-6 haloalkyl groups), a mono-d-6 alkylaminosulfonyl group, a di-Ci- 6 alkylaminosulfonyl group, a d -6 alkylsulfonylamino group and a C - alkoxycarbonylamino group (the mono-Ci -6 alkylaminosulfonyl group, the di-C-1-6 alkylaminosulfonyl group, the C -6 alkylsulfonylamino group and the C - alkoxycarbonylamino group are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms) and with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -6 alkyl groups, C - 6 haloalkyl groups, C 6 alkoxy groups, C -6 haloalkoxy groups, Ci-6 alkylsulfonyl groups and Ci-6 haloalkylsulfonyl groups). Another more preferred embodiment of the substituent L3a and the substituent R2a is such that L3a is a single bond, and R a is an azido group. Another more preferred embodiment of the substituent L a and the substituent R a is such that L a is a single bond, and R2a is a 8 to 1 1-membered partially saturated aromatic cyclic group (the 8 to 11-membered partially saturated aromatic cyclic group is unsubstituted or substituted with one or two identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms). Another more preferred embodiment of the substituent L3a and the substituent R2a is such that L3a is re resented by any of the following formulae (IXa-1) to (IXa-9): ( IXa-6 ) ( IXa-7 ) ( IXa-8 ) ( IXa-9 ) (wherein R a is a hydrogen atom or a C i -3 alkyl group), and R a is a hydrogen atom, a C -6 alkyl group or a Ci-6 haloalkyl group (the Ci-6 alkyl group and the Ci-6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, carbamoyl groups, sulfamoyl groups, tetrazolyl groups, cyano groups, nitro groups, C 3 -6 cycloalkyl groups, Ci-3 alkoxy groups, C -6 haloalkoxy groups, C -3 alkylsulfonyl groups, Ci-3 haloalkylsulfonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups). Another more preferred embodiment of the substituent L3a and the substituent R a is such that L3a is represented by any of the following formulae (IXa-1) to (IXa-9): (IXa-l) ( a-2) (K a-3) (IXa-4) (IXa-5) (IX a-6 ) (IX a-7 ) (I -8) (IX -9) (wherein R a is a hydrogen atom, a C -3 alkyl group or a C -3 haloalkyl group), and R2a is a hydrogen atom, a -6 alkyl group, a C -6 haloalkyl group (the C -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, carbamoyl groups, sulfamoyi groups, cyano groups, nitro groups, C -6 alkoxy groups, C 1-6 haloalkoxy groups, C 6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, mono -Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-C-1 -6 alkylaminocarbonyl groups, di-Ci - alkylaminocarbonyl groups (the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups and the di-Ci-e alkylaminocarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), C3-6 cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 3-6 cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with identical or different one or more substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, carbamoyl groups, C -6 alkoxy groups, C -6 haloalkoxy groups, C- -6 alkylthio groups, C -6 haloalkylthio groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, mono -C-1-6 alkylamino groups, di- C -6 alkylamino groups, mono-C-1-6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups,Ci - alkoxycarbonyl groups (the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono -Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups, the C -6 alkylcarbonylamino groups and the -6 alkoxycarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6- membered aromatic heterocyclyl groups)), a C3-6 cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the C-3-6 cycloalkyl group, the 3 to 1 1-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with identical or different one or more substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, carbamoyl groups, C -6 alkyl groups (the C- -6 alkyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group and a Ci-3 alkoxy group), C1-6 haloalkyl groups, alkoxy groups, C -6 haloalkoxy groups, - alkylthio groups, C -6 haloalkylthio groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, mono-Ci -6 alkylamino groups, di-C- -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di- Ci -6 alkylaminocarbonyl groups, C - alkylcarbonylamino groups, C -6 alkoxycarbonyl groups (the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-C-1-6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups, the C -6 alkylcarbonylamino groups and the - alkoxycarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6- membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups and C -3 haloalkyl groups)). Another more preferred embodiment of the substituent L a and the substituent R2a is such that L a is represented by any of the following formulae (XVIIa- 1) to (XVIIa-3): O O A S s ( XVII ) ( XVII ) ( XVIIa-2 ) ( XVIIa-3 ) and R a is a hydrogen atom or a C -6 alkyl group. Another more preferred embodiment of the substituent L3a and the substituent R a is such that L3a is represented by the formula (XVIIIa) : (wherein R a is a hydrogen atom), and R a is a C -6 alkyl group (the C-1-6 alkyl group is, unsubstituted or substituted with a phenyl group). Another more preferred embodiment of the substituent L a and the substituent R2a is such that L3a is represented by any of the following formulae (IXa-1) to (IXa-9): ( IX ) (wherein R12a is a hydrogen atom, a C -3 alkyl group or a C 1-3 haloalkyl group), and R a is a C -6 alkyl group, a C 1-6 haloalkyl group (the -6alkyl group and the C -6 haloalkyl group are substituted with a substituent selected from the group consisting of a C3-6 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group and a 5 to 10-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 3 to 1 -membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10- membered aromatic heterocyclyl group are substituted with one or two identical or different substituents independently selected from the group consisting of C1-6 alkyl groups (the C 1-6 alkyl groups are unsubstituted or substituted with a hydroxy group or a cyano group) and C1-6 haloalkyl groups)) or a C 2 -6 alkynyl group. Another more preferred embodiment of the substituent L a and the substituent R2a is such that L3a is represented by any of the following formulae (IXa-1) to (IXa-9): ( IXa- ) ( I -2 ) ( x -3 ) ( IXa-4 ) ( IXa- ) ( IXa-6 ) ( IXa-7 ) ( IXa-8 ) ( IXa-9 ) (wherein R12a is a hydrogen atom, a C -3 alkyl group or a C1-3 haloalkyl group), and R a is a C-i-6 alkyl group or a C - haloalkyl group (the Ci-6 alkyl group and the -6 haloalkyl group are substituted with a substituent selected from the group consisting of a C3-6 cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a phenyl group and a 5 to 10-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10- membered aromatic heterocyclyl group are substituted with one or two identical or different substituents independently selected from the group consisting of C1-6 alkyl groups and C -6 haloalkyl groups and with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, C- -6 alkoxy groups, C - 6 haloalkoxy groups, mono-Ci- 6 alkylamino groups, di-Ci -6 alkylamino groups, C - 6 alkylthio groups, C -6 haloalkylthio groups, C - alkylsulfonyl groups, C-1-6 haloalkylsulfonyl groups, C 3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups)). Another more preferred embodiment of the substituent L3a and the substituent R2a resented by the formula (XVIa) : (wherein R a is a hydrogen atom), and R is a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the 8 to 1-membered partially saturated aromatic cyclic group and the 8 to 1 1-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms and hydroxy groups). Another more preferred embodiment of the substituent L3a and the substituent R2a resented by the formula (Xa-10): (wherein E a is NR a (wherein R a is a hydroxy group)), and R2a is a hydrogen atom. Another more preferred embodiment of the substituent L3a and the substituent R a is such that L3a is represented by any of the following formulae (XXVIa-1) to (XXVIa-5): x ( XXVIM ) ( XXVI -2 ) ( XXVIa-3 ) ( XXVIM ) ( XXVI -5 ) (wherein E a is an oxygen atom, and R a is a C1-6 alkyl group (the C1-6 alkyl group is substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a Ci-3 alkoxy group, a C3-6 cycloalkyl group, a 4 to 7-membered nonaromatic heterocyclyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a halogen atom, a cyano group, a C- -3 alkyl group, a C -3 haloalkyl group and a C -3 alkoxy group)), a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C 3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -3 alkyl groups, C1-3 haloalkyl groups and C - -3 alkoxy groups)), and R2a is a C -6 alkyl group, a C -6 haloalkyl group (the C -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, C -3 alkoxy groups, mono-C -6 alkylaminocarbonyl groups, (the mono-C-1.6 alkylaminocarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), C3 -6 cycloalkyl groups, 4 to 7- membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3 -6 cycloalkyl groups, the 4 to 7-membered nonaromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with identical or different one or two substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, carbamoyl groups, C -6 alkyl groups, C -6 haloalkyl groups, C- - alkoxy groups, C -6 haloalkoxy groups, mono-Ci -6 alkylamino groups and di-C-1-6 alkylamino groups)), a C -6 alkynyl group, a C3 - cycloalkyi group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyi group, the 4 to 7-membered nonaromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, carbamoyl groups, C -6 alkyl groups, C -6 haloalkyl groups, C alkoxy groups, C -6 halo alkoxy groups, mono-C-i-6 alkylamino groups, di-Ci-6 alkylamino groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl group). A further preferred embodiment of the substituent L a and the substituent R a is such that L3a is a single bond, and R2a is a hydrogen atom, a halogen atom, a C3 -6 cycloalkyi group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C 3-6 cycloalkyi group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with identical or different one, two or thee substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, nitro groups, carbamoyl groups, sulfamoyl groups, C -6 alkyl groups, C 1-6 haloalkyl groups, C -6 alkoxy groups, C -6 haloalkoxy groups, mono-Ci -6 alkylamino groups, di-Ci-6 alkylamino groups, Ci- 6 alkylthio groups, C -6 haloalkylthio groups, C -6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, carboxy groups, C -6 alkoxycarbonyl groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C - -6 alkylcarbonylamino groups, C3-6 cycloalkyi groups and 4 to 7-membered non-aromatic heterocyclyl groups). Another further preferred embodiment of the substituent L3a and the substituent R2a is such that L a is a single bond, and R a is a 3 to 11-membered non-aromatic heterocyclyl group (the 3 to 11-membered non-aromatic heterocyclyl group is unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, nitro groups, carbamoyl groups, sulfamoyl groups, C -6 alkyl groups, C -6 haloalkyl groups, C -6 alkoxy groups, C -6 haloalkoxy groups, mono- C -6 alkylamino groups, di-Ci -6 alkylamino groups, C -6 alkylthio groups, C -6 haloalkylthio groups, C -6 alkylcarbonyl groups, C 1-6 haloalkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, carboxy groups, Ci- 6 alkoxycarbonyl groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci- 6 alkylaminocarbonyl groups, C 6 alkylcarbonylamino groups, C 3-6 cycloalkyi groups and 4 to 7-membered non-aromatic heterocyclyl groups). Another further preferred embodiment of the substituent L3a and the substituent R a is such that L3a is a single bond, and R2a is a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6- membered aromatic heterocyclyl group are substituted with a C 1-6 alkyl group, a Ci- 6 alkoxy group (the C 1-6 alkyl group and the Ci- 6 alkoxy group are substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group and a C -6 alkoxycarbonylamino group), a mono-Ci- 6 alkylamino group, a di-Ci-6 alkylamino group, a mono-Ci -6 alkylaminocarbonyl group, a C -6 alkylcarbonylamino group (the mono-Ci -6 alkylamino group, the di-Ci -6 alkylamino group, the mono-Ci- 6 alkylaminocarbonyl group and the - alkylcarbonylamino group are substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms or with a hydroxy group or a cyano group), a C -6 alkoxycarbonyamino group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6- membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, C -3 alkyl groups and C 1-3 haloalkyl groups)). Another further preferred embodiment of the substituent L3a and the substituent R2a is such that L a is a single bond, R a is a 3 to 1 1-membered non-aromatic heterocyclyl group (the 3 to 1 1-membered non-aromatic heterocyclyl group is substituted with a di-Ci-3 alkylaminosulfonyl group). Another further preferred embodiment of the substituent L3a and the substituent R a is such that L a is a single bond, R2a is a 4 to 7-membered non-aromatic heterocyclyl group (the 4 to 7-membered non-aromatic heterocyclyl group is substituted with a phenyl group (the phenyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, C-1 .3 alkyl groups and C-1-3 haloalkyl groups) and with a substituent selected from the group consisting of a hydroxy group, a halogen atom, a cyano group, a C-i-3 alkyl group and a C -3 haloalkyl group). uent L3a and the substituent formulae (XXa-1) to (XXa-3): ( X X ) ( X X a- 2 ) ( X X a-3 ) (wherein R 2a is a hydrogen atom or a C -3 alkyl group), and R a is a hydrogen atom, a Ci-6 alkyl group or a -6 haloalkyl group (the C 1-6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, Ci-3 alkoxy groups, C 3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups). Another further preferred embodiment of the substituent L3a and the substituent 2a is such that L3a is represented by any of the following formulae (XXIa- 1) to (XXIa-3): and R is a hydrogen atom or a C -6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with a phenyl groups). Another further preferred embodiment of the substituent L3a and the substituent R a is such that L is represented by the formula (Xa-4): R a is a Ci-3 haloalkyl group. Another further preferred embodiment of the substituent L a and the substituent the following formulae (XXVIII a-1) to ( XXVIII ) ( XXV IIP- 1 ) ( XXVIIP-2 ) ( XXVffl a-3 ) (wherein E a is an oxgen atom, and R1 a is a hydrogen atom or a C-1-3 alkyl group), and R2a is a C-1-6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with a cyano group) or a C -6 haloalkyl group. Another further preferred embodiment of the substituent L3a and the substituent R2a is such that L a is represented by any of the following formulae (XX a-1) to (XX a-3): ( X X ) ( X X a-2 ) ( X X a-3 ) (wherein R a is a hydrogen atom or a C-1-3 alkyl group), and R a is a Ci-6 alkyl group or a Ci-6 haloalkyl group (the Ci-6 alkyl group and the C -6 haloalkyl group are substituted with a substituent selected from the group consisting of a mono-Ci-6 alkylaminocarbonyl group (the mono-Ci-6 alkylaminocarbonyl group is unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), a C3 -6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the C 3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6- membered aromatic heterocyclyl group are substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, carbamoyl groups, Ci-6 alkoxy groups, C -6 haloalkoxy groups, mono-Ci -6 alkylamino groups, di-Ci-6 alkylamino groups, C -6 alkylthio groups, C -6 haloalkylthio groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms and C -3 haloalkyl groups))). Another further preferred embodiment of the substituent L3a and the substituent R2a is such that L3a is represented by any of the following formulae (XX a- 1) to (XX a-3): ( XXa-l ) ( XXa-2 ) ( XXa-3 ) (wherein R 2a is a hydrogen atom or a C -| 3 alkyl group), and R2a is a C -6 alkyl group or a Ci-6 haloalkyl group (the Ci-6 alkyl group and the Ci-6 haloalkyl group are substituted with a substituent selected from the group consisting of a C3-6 cycloalkyl group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered nonaromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, carbamoyl groups, C -6 alkoxy groups, C -6 haloalkoxy groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, C -6 alkylthio groups, C -6 haloalkylthio groups, C1-6 alkylsulfonyl groups, Ci-6 haloalkylsulfonyl groups and 4 to 7-membered non-aromatic heterocyclyl groups) and with a substituent selected from the group consisting of a hydroxy group and a cyano group). Another further preferred embodiment of the substituent L3a and the substituent R a is such that L a is represented by any of the following formulae (XXVI la-1) to 2b is a hydrogen atom, a C1-6 alkyl group or a C i -6 haloalkyl group (the C-t-6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, C i -3 alkoxy groups, C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups). the r further preferred embodiment of the substituent L3b and the R b is such represented by the formula (XXXII b) : ( XXXII b ) (wherein R b is a C i -3 haloalkyl group), and R b is a hydrogen atom, a C -6 alkyl group or a Ci-6 haloalkyl group (the C 1-6 alkyl group and the Ci-6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, C -3 alkoxy groups, C3 -6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups). Another further preferred embodiment of the substituent L3b and the R2b is such that L3b is represented by the formula (XXXI lb) : NA ( XXXII b ) R 12b (wherein R b is a hydrogen atom or a -3 alkyl group), and R2b is a C -6 alkyl group (the Ci-6 alkyl group is substituted with a C3-6 cycloalkyl group (the C3-6 cycloalkyl group is substituted with a hydroxy group)), a C3-6 cycloalkyl group, a 4 to 7-membered nonaromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C-3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of -3 alkyl groups, C1-3 haloalkyl groups and C -6 alkoxycarbonyl groups). ther further preferred embodiment of the substituent L3b and the R b is such represented by the formula (XXXIIb) : ( xxxn b ) (wherein R b is a C 1 3 alkyl group (the -3 alkyl group is substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group and a phenyl group)), and R is a Ci-6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group and a phenyl group) or a C -6 haloalkyl group. A particularly preferred embodiment of the substituent L3b and the R2b is such that L3b is a single bond, and R2b is a hydrogrn atom or a phenyl group (the phenyl group is unsubstituted or substituted with one or more identical or different halogen atoms selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms). Another particularly preferred embodiment of the substituent L3b and the R b is such that L is a single bond, and R2 is a phenyl group (the phenyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups and Ci-3 haloalkyl groups). Another particularly preferred embodiment of the substituent L b and the R2 is such that L3b is a single bond, and R2b is a 5 to 6-membered aromatic heterocyclyl group (the 5 to 6-membered aromatic heterocyclyl group is unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a cyano group, a nitro group, a Ci-3 alkyl group, a Ci-3 haloalkyl group and a C -3 alkoxycarbonyl group). Another particularly preferred embodiment of the substituent L3b and the R b is such that L3b is a single bond, and R2b is a C3 - 6 cycloalkyl group. Another particularly preferred embodiment of the substituent L3b and the R b is such that L3b is a single bond, and R b is a 4 to 7-membered non-aromatic heterocyclyl group (the 4 to 7-membered non-aromatic heterocyclyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C1-3 alkyl groups and -3 haloalkyl groups). Another particularly preferred embodiment of the substituent L3b and the R b is following formula (Vlll b-1) or (Vlll b-2): ( VIII -l ) ( VIII b-2 ) and R b is a methyl group (the methyl group is unsubstituted or substituted with a cyano group, a cyclopropyl group or a trifluoromethyl group) or an isobutyl group. Another particularly preferred embodiment of the substituent L3b and the R b is such that L3b is represented by the following formula (Vlll b-1) or (Vlll b-2): ) ( VIII b - ) ( VIII b-2 ) and R b is a phenyl group (the phenyl group is unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a cyano group and a Ci-3 haloalkyl group) or a 5 to 6-membered aromatic heterocyclyl group (the 5 to 6- membered aromatic heterocyclyl group is unsubstituted or substituted with a halogen atom). Another particularly preferred embodiment of the substituent L b and the R2b is such that L3b is represented by the formula (XXXII b) : ( XXX I ) R 12b (wherein R 2b is a hydrogen atom), and R2b is a C3-6 cycloalkyl group or a 4 to 7- membered non-aromatic heterocyclyl group (the C3.6 cycloalkyl group and the 4 to 7- membered non-aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of C1-3 alkyl groups, C -3 haloalkyl groups and C-i-6 alkoxycarbonyl groups). A preferred embodiment of nb and the substituent R3b is such that nb is 0 , 1 or 2 , and R3b is a hydroxy group, an amino group, a halogen atom, a cyano group, a C -3 alkyl group, a C -3 haloalkyl group, a C -3 alkoxy group or a C -3 haloalkoxy group (when nb is 2, R3b's may be identical or different). A more preferred embodiment of nb and the substituent R b is such that nb is 0 or 1, and R3b is a C -3 alkyl group. As favorable tricyclic pyridine compounds of the present invention for use as JAK inhibitors and as preventive, therapeutic and/or improving agent for diseases against which inhibition of JAK is effective, the following compound may be mentioned. 1b) Compounds represented by the formula (l ) : [wherein R1b is a hydrogen atom o r a halogen atom, Xb is a nitrogen atom o r CR 5b (wherein R is a hydrogen atom, a halogen atom, a cyano group, a C-i-6 alkyl group, a C -6 haloalkyl group o r a C3-6 cycloalkyl group), hydrogen atom), he formula (ll ) : (wherein T is C R4bR5b, C(=0), C(=S), C(=NR b) , a sulfur atom, S (=0) o r S(=0) 2, U b R b, and W b is a nitrogen atom o r C R b) , the formula (lll b) : (wherein T is C R4 , is a nitrogen atom o r C R , and W is C R R , C(=0), C(=S), C(=NR 17b) , NR10b, an oxygen atom, a sulfur atom, S(=0) o r S (=0) 2 (provided that when 2b is CR6b, W2b is not C(=0))) o r the formula (IV b) : (wherein T3b is CR4 R5b, C(=0), C(=S), C(=NR 7b) , a sulfur atom, S(=0) o r S(=0) 2, U b is C R6bR b, C(=0), C(=S), C(=NR b) , NR 0 , an oxygen atom, a sulfur atom, S(=0) o r S(=0) 2, and W3b is CR8bR9b, C(=0), C(=S), C(=NR 1 b) , NR11b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2 (provided that when T b is C R4bR5b, and U3 is C R6bR7b, W b is not CR bR9b)), L b is a single bond o r a C-1.3 alkylene group, L b is a single bond, a C -6 alkylene group, a C2-6 alkenylene group or a C2 6 alkynylene group (the C1-6 alkylene group, the C2 -6 alkenylene group and the C-2-6 alkynylene group are unsubstituted or substituted with one o r more identical o r different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), the ring B is a C3-11 cycloalkane, a C3-11 cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a Ce-14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, nb is 0 or 1, R b is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C 3 alkyl group, a C -3 haloalkyl group, a C3-6 cycloalkyl group, a C 1-3 alkoxy group, a Ci-3 haloalkoxy group or a C-i -3 alkylsulfonyl group, and L3b is a single bond or represented by any of the following formulae (XXIIb- 1) to (XXIIb- 15): ( XXIIb-6 ) ( XXIIb-7 ) ( XXIIb-8 ) ( XXIIb-9 ) ( XXIIb-10 ) ( XXIIb-ll ) ( XXIIb-12 ) ( XXIIb-13 ) ( XXIIb-14 ) ( XXIIb-15 ) (wherein E1b is an oxygen atom or a sulfur atom), when L3b is a single bond, R2b is a hydrogen atom, a halogen atom, a C3-11 cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a C 6- 14 aryl group , a 5 to 10-membered aromatic heterocyclyl group, a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 1-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3-11 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the Ce-14 aryl group , the 5 to 10-membered aromatic heterocyclyl group, the 8 to 1 1-membered partially saturated aromatic cyclic group and the 8 to 1 1 - membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b and the substituent set V9b) , when L3b is not a single bond, R2b is a hydrogen atom, a C-|.6 alkyl group, a C2-6 alkenyl group (the C1-6 alkyl group and the C2-6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V6b and the substituent set V9b) , a C3-1 1 cycloalkyl group, a 3 to 11- membered non-aromatic heterocyclyl group, a C6- 4 aryl group , a 5 to 10-membered aromatic heterocyclyl group, a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 1 1-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3.11 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C 6-14 aryl group , the 5 to 10-membered aromatic heterocyclyl group, the 8 to 1 1-membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ringcondensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4 and the substituent set V9b) , nb is 0, 1 or 2, R is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a sulfamoyl group, a phosphono group, a phosphonooxy group, a sulfo group, a sulfoxy group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C -6 alkyl group, a C -6 haloalkyl group, a C3-11 cycloalkyl group, a C 2-6 alkenyl group, a C 2-6 haloalkenyl group, a C - alkoxy group, a C -6 haloalkoxy group, a C -6 alkylthio group, a C -6 haloalkylthio group, a C -6 alkylcarbonyl group, a C -6 haloalkylcarbonyl group, a C - . 6 alkylsulfonyl group, a C -6 haloalkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-Ci -6 alkylamino group, a di-Ci -6 alkylamino group, a mono-d-6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group or a C -6 alkylcarbonylamino group (when n is 2, R 's may be identical or different), each of R4b, R5b, R6 , R b, R b and R9b is independently a hydrogen atom, a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a C -6 alkyl group, a C 2 -6 alkenyl group, a C -6 alkoxy group, a C-i -6 alkylthio group, a C --alkylcarbonyl group, a C 1-6 alkylsulfonyl group, a mono-Ci -6 alkylamino group, a di-Ci -6 alkylamino group (the C- 6 alkyl group, the C -6 alkenyl group, the C 1-6 alkoxy group, the C i -6 alkylthio group, the C -6 alkylcarbonyl group, the C -6 alkylsulfonyl group, the mono-Ci -6 alkylamino group and the di-Ci -6 alkylamino group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3 ) , a C 1-6 alkoxycarbonyl group, a C 3- cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C-6-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3-11 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C 6 - 14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , each of R 0 and R b is independently a hydrogen atom, a C i - alkyl group, a C 2 -6 alkenyl group, a C -6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-C-i -6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group (the C -6 alkyl group, the C 2-6 alkenyl group, the C -6 alkylcarbonyl group, the C -6 alkylsulfonyl group, the C 1-6 alkoxycarbonyl group, the mono-Ci -6 alkylaminocarbonyl group and the di-Ci -6 alkylaminocarbonyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3 ) , a C3-11 cycloalkyl group, a 3 to 11- membered non-aromatic heterocyclyl group, a C 6 - 4 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3-11 cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the - aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1 ) , each of R and R b is independently a hydrogen atom, a C -6 alkyl group or a C -6 haloalkyl group (the C -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b, the substituent set V8b and the substituent set V9b) , and R1 is a hydrogen atom, a hydroxy group, a cyano group, a nitro group, a C -6 alkyl group or a C -6 alkoxy group], tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 2b) The compounds according to 1b) , wherein R1b is a hydrogen atom or a halogen atom, Xb is a nitrogen atom or CR b (wherein R 5b is a hydrogen atom, a halogen atom, a p, a -6 haloalkyl group or a C3-6 cycloalkyl group), hydrogen atom), he formula (llb) : (wherein T is CR4bR b, C(=0), C(=S), C(=NR b), a sulfur atom, S(=0) or S(=0) 2 U b R6b, and W1b is a nitrogen atom or CR b) , the formula (lll b) : (wherein is CR , T is a nitrogen atom or CR , and is CR R , C(=0), C(=S), C(=NR17b) , NR10b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2 (provided that when 2b is CR b,W2 is not C(=0))) or the formula (IVb) : (wherein T3b is CR4bR5 , C(=0), C(=S), C(=NR 7 ) , a sulfur atom, S(=0) or S(=0) 2, U is CR6bR7b, C(=0), C(=S), C(=NR b) , NR10b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2, and W3b is CR8 R9b, C(=0), C(=S), C(=NR17b) , NR b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2 (provided that when T3b is CR4bR5b, and U3b is CR6bR7b,W3b is not CR8 R9 )), L b is a single bond or a C 1-3 alkylene group, L2 is a single bond, a C -6 alkylene group or a -6 haloalkylene group (the C - alkylene group and the -6 haloalkylene group are unsubstituted or substituted with one or more hydroxy groups or one or more cyano groups), the ring B is a C3-11 cycloalkane, a C3-11 cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a C6-i 4 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, nb is 0 or 1, R3b is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C -3 alkyl group, a C-1.3 haloalkyl group, a C3-6 cycloalkyl group, a C -3 alkoxy group, a C -3 haloalkoxy group or a Ci-3 alkylsulfonyl group, L3b is a single bond, and R b is a hydrogen atom, a halogen atom, a C3-6 cycloalkyl group, a 3 to 1 -membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6- membered aromatic heterocyclyl group (the C3 -6 cycloalkyl group, the 3 to 1 1-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4 ) , or L b is represented by any of the following formulae (Vlb-1) to (Vlb-11): -l ) (V I -2 ) (V I -3 ) ( I -4 ) (V I -S ) ( I -6 ) (VIb-7) (VIb-8) (VI -9) (VI -10) (VIb-ll) (wherein E b is an oxygen atom, and each of R 12b and R is independently a hydrogen atom or a C -6 alkyl group), and R b is a hydrogen atom, a C 1-6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5b) , a C 3 -6 cycloalkyl group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered nonaromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b) , each of R4b, R5b, R6b, R , R b and R b is independently a hydrogen atom, an amino group, a carbamoyl group, a halogen atom, a cyano group, a -6 alkyl group, a C1-6 haloalkyl group, a C -6 alkoxy group, a Ci-6 haloalkoxy group, a C1-6 alkylsulfonyl group, a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1b) , each of R 10b and R 11b is independently a hydrogen atom, a C1-6 alkyl group, a C -6 haloalkyl group, a C3-6 cycloalkyl group, a C i -6 alkoxy group, a C i -6 haloalkoxy group, a C-i-6 alkylsulfonyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V ) , and R 7b is a hydrogen atom, a hydroxy group, a cyano group, a nitro group, a C 6 alkyl group or a -6 alkoxy group, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 3b) The compounds according to 1b) or 2b) , wherein R b is a hydrogen atom, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 4b) The compounds according to any one of b) to 3b) , wherein Xb is a nitrogen atom or a C R b (wherein R b is a hydrogen atom, a halogen atom or a cyano group) or a nitrogen atom, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 5b) The compounds according to any one of 1b) to 4b) , wherein Xb is a nitrogen atom o r C R15b (wherein R15b is a hydrogen atom), tautomers o r pharmaceutically acceptable salts of the compounds o r solvates thereof. 6 ) The compounds according to any one of 1b) to 5b) , wherein Yb is CR16b (wherein R16 is a hydrogen atom), tautomers or pharmaceutically acceptable salts of the compounds o r solvates thereof. 7b) The compounds according to any one of 1b) to 6 ) , wherein the ring Ab is VII -l ) ( VIIb-2 ) ( VIIb-3 ) ( VII -4 ) ( VII -5 ) ( VII -6 ) ( VIIb-7 ) (wherein E2b is an oxygen atom or a sulfur atom, each of each of R4 , R5b, R b, R b and R9b is independently a hydrogen atom, a n amino group, a carbamoyl group, a halogen atom, a cyano group, a Ci- 6 alkyl group, a C -6 haloalkyl group, a C3 6 cycloalkyl group, a C- -6 alkoxy group, a C1-6 haloalkoxy group, a C -6 alkylsulfonyl group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group o r a 5 to 6-membered aromatic heterocyclyl group, and R10b is a hydrogen atom, a Ci-6 alkyl group, a C -6 haloalkyl group, a C-3-6 cycloalkyl group, a C-i-6 alkoxy group, a C-i-6 haloalkoxy group, a Ci-6 alkylsulfonyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group o r a 5 to 6-membered aromatic heterocyclyl group), tautomers o r pharmaceutically acceptable salts of the compounds o r solvates thereof. 8b) The compounds according to any one of 1b) to 6b) , wherein the ring A is represented by the formula (XXVIII ) : ( XXVIIIb ) (wherein each of E2b and E3b is independently, an oxygen atom o r a sulfur atom, and R is a hydrogen atom, a - alkyl group (the Ci-6 alkyl group is unsubstituted o r substituted with one o r two identical o r different substituents independently selected from the group consisting of cyano groups, hydroxy groups, Ci_3 alkoxy groups, C -3 alkylthio groups, di-Ci -3 alkylamino groups, di-Ci -3 alkylaminocarbonyl groups, C3-6 cycloalkyl groups and 4 to 7-membered non-aromatic heterocyclyl groups), a Ci-6 haloalkyl group, a C3 -6 cycloalkyl group or a 4 to 7-membered non-aromatic heterocyclyl group), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 9b) The compounds according to any one of 1b) to 7b) , wherein the ring Ab is ( XVI -5 ) ( VI - ) ( XVI (wherein R is a hydrogen atom or a methyl group), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 10b) The compounds according to any one of 1 ) to 6b), wherein the ring Ab is g formula (XXIX -1) or (XXIXb-2) ( XXIX ) ( XXIXb-l ) ( XXIXb-2 ) (wherein E and E are oxygen atoms, R is a hydrogen atom, a halogen atom or a Ci-3 alkyl group, and R and R10b are hydrogen atoms), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 1 1b) The compounds according to any one of 1b) to 10b) , wherein L b is a single bond, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 12b) The compounds according to any one of 1b) to 11 ) , wherein L b is a single bond or a Ci-6 alkylene group, a -6 alkenylene group (the C -6 alkylene group and the C -6 alkenylene group are unsubstituted or substituted with a cyano group) or a haloalkylene group, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 13b) The compounds according to any one of b) to 1 b) , wherein L2b is a single bond or a Ci-3 alkylene group, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 14 ) The compounds according to any one of ) to 1 1b) , wherein L2b is a single bond or a methylene group, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 15b) The compounds according to any one of 1b) to 14b) , wherein the ring B is a C4-7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, tautomers or pharmaceutically acceptable salts of the compounds o r solvates thereof. 6b) The compounds according to any one of 1b) to 14b) , wherein the ring Bb is cyclohexane o r piperidine, tautomers o r pharmaceutically acceptable salts of the compounds or solvates thereof. 17b) The compounds according to any one of 1b) to 16b) , wherein nb is, 0 o r , and R b is a methyl group, tautomers o r pharmaceutically acceptable salts of the compounds o r solvates thereof. 18b) The compounds according to any one of 1 ) to 17b) , wherein L3 is a single bond, and R2b is a hydrogen atom, a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the C-3-11 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted o r substituted with one o r more identical o r different substituents independently selected from the substituent set V 1b) , tautomers o r pharmaceutically acceptable salts of the compounds o r solvates thereof. 19b) The compounds according to any one of b) to 17 ) , wherein L3b is a single bond, and R2b is a hydrogen atom, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group o r a 5 to 6-membered aromatic heterocyclyl group (the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted o r substituted with one o r two identical o r different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, nitro groups, C i-6 alkyl groups, C-i-6 alkoxy groups and Ci-6 alkoxycarbonyl groups (the C -6 alkyl groups, the C -6 alkoxy groups and the C -6 alkoxycarbonyl groups are unsubstituted or substituted with one o r more identical o r different substituents independently selected from the group consisting of halogen atoms and cyano groups)), tautomers o r pharmaceutically acceptable salts of the compounds or solvates thereof. 20b) The compounds according to any one of b) to 17 ) , wherein L3b is a single bond, and R is a hydrogen atom o r a phenyl group (the phenyl group is unsubstituted o r substituted with one o r two halogen atoms), tautomers o r pharmaceutically acceptable salts of the compounds o r solvates thereof. 2 1b) The compounds according to any one of 1b) to 7b) , wherein L3b is a single bond, and R2b is a C3-6 cycloalkyl group, tautomers o r pharmaceutically acceptable salts of the compounds o r solvates thereof. 22 ) The compounds according to any one of 1b) to 17b) , wherein L3b is a single bond, and R b is a 4 to 7-membered non-aromatic heterocyclyl group (the 4 to 7-membered non-aromatic heterocyclyl group is unsubstituted o r substituted with one o r more identical o r different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -6 alkyl groups (the Ci-6 alkyl groups are unsubstituted o r substituted with a cyano group), Ci-6 haloalkyl groups, C 1-6 alkoxy groups, Ci-6 haloalkoxy groups and Ci-6 alkoxycarbonyl groups), tautomers o r pharmaceutically acceptable salts of the compounds o r solvates thereof. 23b) The compounds according to any one of 1b) to 7b) , wherein L3b is represented by any of the following formulae (XIX b-1) to (XIX -7): ( XIX -l ) ( XIX -2 ) ( XIX -3 ) ( XIX- ) ( XIXb-5 ) ( XIX ) ( XIX -6 ) ( XIXb-7) (wherein E b is an oxygen atom, and R1 b is a hydrogen atom or a -3 alkyl group), and R b is a hydrogen atom, a Ci-6 alkyl group, a C1-6 haloalkyl group (the C1-6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group, a C3-6 cycloalkyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the C3.6 cycloalkyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, C -3 alkoxy groups, Ci -3 haloalkoxy groups, C -3 alkylsulfonyl groups and C -3 haloalkylsulfonyl groups)), a C3 cycloalkyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the phenyl group and the 5 to 6- membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, C -6 alkyl groups, Ci-3 haloalkyl groups, C -3 alkoxy groups, C -3 haloalkoxy groups, C -3 alkylsulfonyl groups and C -3 haloalkylsulfonyl groups), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. ny one of 1b) to 17b) , wherein L3b is represented by lb-2): (viiib-i ) (vmb-2) and R is a C -6 alkyl group (the Ci -6 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a C3 -6 cycloalkyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the phenyl group, the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms and cyano groups)) or a Ci -3 haloalkyl group, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 25 ) The compounds according to any one of 1b) to 17b) , wherein L b is represented by the following formula (Vlll - 1) or (Vlll b-2): ( VIII b ) ( VIII b-l ) ( Vffl b-2 ) and R2b is a methyl group (the methyl group is unsubstituted or substituted with a cyano groups, a cyclopropyl groups or a trifluoromethyl groups) or an isobutyl group, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof . ing to any one of ) to 17 ) , wherein L3b is represented by and R is a C -6 alkyl group (the Ci-6 alkyl group is unsubstituted or substituted with a cyano group or a phenyl group), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. to any one of ) to 17 ) , wherein L3b is represented by (wherein R 2 is a hydrogen atom), and R2b is a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with a C1-3 alkyl group or a Ci-3 haloalkyi group), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 28b) The compounds according to any one of 1b) to 17b) , wherein L3b is represented by the formula (XXVIIb) : 0 ( x viib ) and R2b is a hydrogen atom or a C1-3 alkyl group, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 29b) The compounds according to any one of 1b) to 17b) , wherein L b is represented by the formula (XXXIIb) / —N \ ( ) R 12b (wherein R b is a hydrogen atom, a C -3 alkyl group (the Ci-3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group, a C1-3 alkoxy group, a C3-6 cycloalkyl group and a phenyl group) or a C -3 haloalkyi group), and R b is a hydrogen atom, a C -3 alkyl group, a C -3 haloalkyi group (the C1-3 alkyl group and the C -3 haloalkyi group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, C -3 alkoxy groups, C3 -6 cycloalkyl groups, 4 to 7-membered nonaromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3 -6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a halogen atom and a cyano group)), a C 3-6 cycloalkyl group or a 4 to 7-membered non-aromatic heterocyclyl group (the C 3-6 cycloalkyl group and the 4 to 7-membered non-aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, C -3 alkyl groups, C -3 haloalkyl groups and C1-6 alkoxycarbonyl groups), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 30b) The compounds according to any one of 1b) to 17b) , wherein L3b is represented by the formula (XXXVb) : (wherein R b is a hydrogen atom, a C -3 alkyl group or a Ci-3 haloalkyl group), and R b is a C -6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with a cyano group) or a C -6 haloalkyl group, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. R15b (wherein VIIIb-8): ( XVIII ) ( XVIII b-5 ) ( XVIII -6 ) ( XVIII b-7 ) ( XVIII b-8 ) (wherein each of E and E3 is independently an oxygen atom or a sulfur atom, and each of R b, R5b, R6b, R8b and R9b is independently a hydrogen atom or a C1-3 alkyl group, and R10b is a hydrogen atom, a Ci-6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C1-3 alkoxy groups, di- -3 alkylamino groups, C3.6 cycloalkyl groups, 4 to 7-membered nonaromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the phenyl group and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, Ci-3 alkyl groups and Ci-3 haloalkyl groups)), a C 1-6 haloalkyl group, a C-3-6 cycloalkyl group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group), the ring Bb is a C3- cycloalkane, a 3 to 11-membered non-aromatic heterocycle, a C6- aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L is a single bond or a C-i-3 alkylene group, L b is a single bond, a C 1-6 alkylene group or a C-2-6 alkenylene group (the C -6 alkylene group and the C2-6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), nb is 0 or 1, R3b is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C -3 alkyl group, a Ci-3 haloalkyl group, a C3-6 cycloalkyl group, a Ci-3 alkoxy group, a C1-3 haloalkoxy group or a C -3 alkylsulfonyl group, L3b is a single bond or is represented by any of the following formulae (Vlb-1) to (Vlb-11) (VI -l) (VI -2) (VI"-3) (VI -4) (V Ib- ) (VI"-6) (VI b-7) (VI b-8) (VI b-9) (VI b-10) (VI b-ll) (wherein E1b is an oxygen atom or a sulfur atom, and each of R12b and R13b is independently a hydrogen atom, a C -6 alkyl group or a C 1-6 haloalkyl group (the -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C -6 alkoxy groups, C3-6 cycloalkyl groups, 4 to 7- membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups)), and when L3b is a single bond, R2b is a hydrogen atom, a halogen atom, a C3-11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3.11 cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the phenyl group, the naphthyl group, the 5 to 10- membered aromatic heterocyclyl group, the 8 to 11-membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b and the substituent set V9b) , and when L3b is not a single bond, R2b is a hydrogen atom, a C-i-e alkyl group, a C2 -6 alkenyl group (the C -6 alkyl group and the C -6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V6 and the substituent set V9b) , a C 3 cycloalkyl group, a 3 to 11- membered non-aromatic heterocyclyl group, a C6-i4 aryl group , a 5 to 10-membered aromatic heterocyclyl group, a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3.11 cycloalkyl group, the 3 to 1 1-membered non-aromatic heterocyclyl group, the C 6- aryl group , the 5 to 10-membered aromatic heterocyclyl group, the 8 to 11-membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ringcondensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b and the substituent set V9b) , tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. y ( XXI b- l ) ( XXI b-2) ( XXI b-3 ) ( XXI - ) (wherein and E are oxygen atoms, R , R , R and R are hydrogen atoms, and R6 is a hydrogen atom, a halogen atom or a C 1-3 alkyl group, and R 0b is a hydrogen atom, a C1-6 alkyl group (the C1-6 alkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C -3 alkoxy groups, C 1-3 alkylthio groups, di-Ci -3 alkylamino groups, di-Ci -3 alkylaminocarbonyl groups, C3-6 cycloalkyl groups and 4 to 7- membered non-aromatic heterocyclyl groups), a -6 haloalkyl group, a C3-6 cycloalkyl group or a 4 to 7-membered non-aromatic heterocyclyl group), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 33 ) The compounds according to 1 ) , 3 1 ) or 32 ) , wherein L b is a single bond, L b is a single bond , a C -6 alkylene group (the C -6 alkylene group is unsubstituted or substituted with a hydroxy group or a cyano group) or a C -6 haloalkylene group, the ring B is a C4 -7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, n is 0 or 1, and R3b is a C i -3 alkyl group, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 34b) The compounds according to any one of 1 ) and 3 1 ) to 33b) , wherein L3b is a single bond, and R2b is a hydrogen atom, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group, a 5 to 10-membered aromatic heterocyclyl group or a 8 to 11-membered partially saturated aromatic cyclic group (the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group, the 5 to 10-membered aromatic heterocyclyl group and the 8 to 11- membered partially saturated aromatic cyclic group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, carbamoyl groups, sulfamoyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkyl groups (the -6 alkyl groups are unsubstituted or substituted with a cyano group), C -6 haloalkyl groups, C3- cycloalkyl group, Ci-6 alkoxy groups, C e haloalkoxy groups, Ci-6 alkylthio groups, C -6 haloalkylthio groups, Ci-6 alkylsulfonyl groups, -6 haloalkylsulfonyl groups, Ci-6 alkoxycarbonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, mono-C 1-6 alkylamino groups, di-Ci -6 alkylamino groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 35b) The compounds according to any one of 1b) and 3 1b) to 33b) , wherein L3b is a single bond, and R2 is a 8 to 11-membered partially saturated aromatic cyclic group (the 8 to - membered partially saturated aromatic cyclic group is unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 36b) The compounds according to 34 ) or 35 ) , wherein L2b is a C -3 alkylene group, and the ring Bb is cyclohexane or piperidine, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 37 ) The compounds according to any one of 1 ) and 3 1 ) to 33 ) , wherein L3 is represented by any of the following formulae (XIXb-1) to (XIXb-7): (XIXb-l) (XIX -2) (XIX -3) (XIX- 4 ) (XIX -5) v v ( XIX b ) (XIX -6) (XIX -7) (wherein E b is an oxygen atom, and R 2 is a hydrogen atom, a C -6 alkyl group (the C - 6 alkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C -3 alkoxy groups, C3 -6 cycloalkyl groups and phenyl groups) or a C -6 haloalkyl groups), and R2b is a hydrogen atom, a C -6 alkyl group, a C-i -6 haloalkyl group (the C -6 alkyl group and the C - -6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C3 -6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups, 5 to 6-membered aromatic heterocyclyl groups and 8 to 11- membered partially saturated aromatic cyclic groups (the C3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups, the 5 to 6- membered aromatic heterocyclyl groups and the 8 to 1 1-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, C - alkyl groups, C1-3 haloalkyl groups, C- -3 alkoxy groups, C -3 haloalkoxy groups, C -3 alkylsulfonyl groups, C -3 haloalkylsulfonyl groups, 4 to 7-membered non-aromatic heterocyclyl group, phenyl groups, 5 to 6-membered aromatic heterocyclyl groups (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the substituent set V1b) , mono-C-i-6 alkylaminosulfonyl groups, di-C 1-6 alkylaminosulfonyl groups and C1-6 alkylsulfonylamino groups)), a C3 -6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group, a 5 to 6-membered aromatic heterocyclyl group or a 8 to 11-membered partially saturated aromatic cyclic group (the C3 -6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group, the 5 to 6- membered aromatic heterocyclyl group and the 8 to 1 1-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, C -6 alkyl groups, C -3 haloalkyl groups, C1-3 alkoxy groups, C -3 haloalkoxy groups, C -3 alkylsulfonyl groups, C1-3 haloalkylsulfonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups, 5 to 6-membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V ) , mono-C-i-6 alkylaminosulfonyl groups, di-C 1-6 alkylaminosulfonyl groups and Ci-6 alkylsulfonylamino groups), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 38 ) The compounds according to any one of 1b) , 3 1b) to 33 ) and 37 ) , wherein L3 is represented by any of the following formulae (XXXb- 1) to (XXXb-3): ( XXXb-l ) ( XXXb-2 ) ( XXb-3 ) (wherein E is an oxygen atom, and R b is a hydrogen atom), and R2 is a C -6 alkyl group (the C - alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a C 3-6 cycloalkyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, Ci-6 alkyl groups and C1-3 haloalkyl groups)), a Ci -3 haloalkyl group, a C3-6 cycloalkyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, C -3 alkyl groups and C -3 haloalkyl groups), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 39 ) The compounds according to any one of 1 ) and 3 1b) to 33 ) , wherein L3 is represented by the formula (XXXIIb) : (XXXIIb ) (wherein R 2b is a hydrogen atom, a C 1-3 alkyl group (the C1-3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group, a C-1 -3 alkoxy group, a C 3-6 cycloalkyl group and a phenyl group) or a C -3 haloalkyl group), and R2b is a hydrogen atom, a C -3 alkyl group, a C -3 haloalkyl group (the C i -3 alkyl group and the C1-3 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, C -3 alkoxy groups, C 3 6 cycloalkyl groups, 4 to 7-membered nonaromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C 3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a halogen atom, a cyano group and a C -3 haloalkyl group)), a C 3-6 cycloalkyl group or a 4 to 7-membered non-aromatic heterocyclyl group (the C 3 -6 cycloalkyl group and the 4 to 7-membered non-aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, C -3 alkyl groups, C -3 haloalkyl groups and -6 alkoxycarbonyl groups), tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 40 ) The compounds according to any one of 1b) and 3 b) to 33b) , wherein L3b is represented by the following formula (XXXVI b-1) or (XXXVI -2): ( XXXVIb-l) ( XXXVI -2) (wherein R 1 b is a hydrogen atom, a C1-3 alkyl group (the C -3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group, a C -3 alkoxy group, a C 3-6 cycloalkyl group and a phenyl group) or a C -3 haloalkyl group), and R2b is a hydrogen atom, a C -3 alkyl group, a C -3 haloalkyl group (the C-1-3 alkyl group and the C1-3 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, C -3 alkoxy groups, C 3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups), a C3.6 cycloalkyl group or a 4 to 7- membered non-aromatic heterocyclyl group, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 4 1 ) The compounds according to 37b) or 40b) , wherein L b is a single bond or a C1-3 alkylene group, and the ring Bb is a cyclohexane or piperidine, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. 42b) Compounds represented by the formula (XVII b) : ( XVII ) . TABLE 1 A b B 1 b A b B 1 b A b B b A B b A 1 B 1 A 1 B 3 A 1 B 5 A 1 B 1 7 A 2 B 1 1 A 2 B 1 3 A 2 B 1 5 A 2 B 7 A 3 B 1 1 A 3 B 3 A 3 B 5 A 3 B 7 A 4 B 1 A 4 B 3 A 4 B 5 A 4 B 1 7 A 5 B 1 A 5 B 3 A 5 B 5 A 5 B 7 A 6 B 1 A 6 B 1 3 A 6 B 1 5 A 6 B 7 A 7 B 1 A 7 B 1 3 A 7 B 5 A 7 B 7 A 8 B 1 1 A 8 B 1 3 A 8 B 5 A 8 B 1 7 A 1 B 1 2 A 1 B 4 A 1 B 1 6 A 1 B 8 A 2 B 2 A 2 B ' 4 A 2 B 6 A 2 B 1 8 A 3 B 2 A 3 B 4 A 3 B 6 A 3 B 8 A 4 B 2 A 4 B 1 4 A 4 B 1 6 A 4 B 1 8 A 5 B 1 2 A 5 B 4 A 5 B 6 A 5 B 8 A 6 B 1 2 A 6 B 4 A 6 B 6 A 6 B 8 A 7 B 2 A 7 B 4 A 7 B 1 6 A 7 B 1 8 A 8 B 2 A 8 B 1 4 A 8 B 1 6 A 8 B 8 43b) Compounds represented by the formula (XVIIb-1): TABLE13 2 A b B 2 b A b B 2 b A B 2 b A B 2 b A 1 B 1 A 1 B 2 3 A 1 B 2 5 A 1 B 2 7 A 2 B 2 1 A 2 B 2 3 A 2 B 2 5 A 2 B 2 7 A 3 B 1 A 3 B 2 3 A 3 B 2 5 A 3 B 2 7 A 4 B 2 1 A 4 B 2 3 A 4 B 2 5 A 4 B 2 7 A 5 B 1 A 5 B 2 3 A 5 B 2 5 A 5 B 2 7 A 6 B 2 1 A 6 B 2 3 A 6 B 2 5 A 6 B 2 7 A 7 B 2 1 A 7 B 2 3 A 7 B 2 5 A 7 B 2 7 A 9 B 2 1 A 9 B 2 3 A 9 B 2 5 A 9 B 2 7 A 1 B 2 2 A 1 B 2 4 A 1 B 2 6 A 1 B 2 8 A 2 B 2 A 2 B 2 4 A 2 B 2 6 A 2 B 2 8 A 3 B 2 2 A 3 B 2 4 A 3 B 2 6 A 3 B 2 8 A 4 B 2 2 A 4 B 2 4 A 4 B 2 6 A 4 B 2 8 A 5 B 2 2 A 5 B 2 4 A 5 B 2 6 A 5 B 2 8 A 6 B 2 2 A 6 B 2 4 A 6 B 2 6 A 6 B 2 8 A 7 B 2 2 A 7 B 2 4 A 7 B 2 6 A 7 B 2 8 A 9 B 2 A 9 B 2 4 A 9 B 2 6 A 9 B 2 8 44b) The compounds with the combinations of substituents as defined in 42b) or 43b) , wherein Xb is converted to a nitrogen atom, tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof. The compounds of the present invention can be synthesized by the processes mentioned later, but the production of the compounds of the present invention is not restricted to these general examples. The compounds of the present invention can usually be purified by column chromatography, thin layer chromatography, high performance liquid chromatography (HPLC) or high performance liquid chromatography-mass spectrometry (LC-MS) and, if necessary, they may be obtained with high purity by recrystallization or washing with solvents. In general, in the production of the compounds of the present invention, any solvents that are stable and inert under the reaction conditions and do not hinder the reactions may be used without any particular restrictions, and for example, sulfoxide solvents (such as dimethyl sulfoxide), amide solvents (such as N,N-dimethylformamide or ,-dimethylacetamide), ether solvents (such as diethyl ether, 1,2-dimethoxyethane, tetrahydrofuran, 1,4-dioxane or cyclopentyl methyl ether), halogenated solvents (such as dichloromethane, chloroform or 1,2-dichloroethane), nitrile solvents (such as acetonitrile or propionitrile), aromatic hydrocarbon solvents (such as benzene or toluene), aliphatic hydrocarbon solvents (such as hexane or heptane), ester solvents (such as ethyl acetate), alcohol solvents (such as methanol, ethanol, 1-propanol, 2- propanol or ethylene glycol) and water may be mentioned. The reactions may be carried out in an arbitrary mixture of solvents mentioned above or in the absence of a solvent. In general, in the production of the compounds of the present invention, the reaction temperature is chosen appropriately within the range of from -78°C to the boiling point of the solvent used for the reaction, and the production of the compounds of the present invention may be carried out at ordinary pressure or under pressure or with microwave irradiation. As acids generally used in the production of the compounds of the present invention, for example, organic acids (such as acetic acid, trifluoroacetic acid or ptoluenesulfonic acid) and inorganic acids (such as sulfuric acid or hydrochloric acid) may be mentioned. As bases generally used in the production of the compounds of the present invention, for example, organic metal compounds (such as n-butyllithium, s-butyllithium, lithiumdiisopropylamide or isopropylmagnesium bromide), organic bases (such as triethylamine, ,-diisopropylethylamine or ,-dimethylaminopyridine) and inorganic bases (such as sodium carbonate, potassium carbonate, cesium carbonate, sodium hydroxide, potassium hydroxide or sodium hydride) may be mentioned. General processes for production of the compounds of the present invention are shown below, and the formulae of the intermediate and the end product in each step therein conceptually cover their protected derivatives, too. Herein, protected derivatives are defined as compounds which can be converted to the desired product, if necessary, through hydrolysis, reduction, oxidation, alkylation or the like and include compounds protected with chemically acceptable protective groups. Protection and deprotection may be carried out by generally known protection and deprotection reactions (for example, by referring to Protective Groups in Organic Synthesis, Fourth edition, T.W. Greene, John Wiley & Sons Inc. (2006)). Hydrolysis, reduction and oxidation may be carried out by generally known functional group conversions (for example, by referring to Comprehensive Organic Transformations, Second Edition, R.C.Larock, Wiley-VCH (1999)). First, processes for producing the tricyclic pyrimidine compounds represented by the formula (la) will be described. Among the tricyclic pyrimidine compounds represented by the formula (la) , the compounds (1a)-3 can be produced, for example, through the following scheme (1a) (wherein R R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (la)-l (la)-2 a .3 A compound ( 1a)-1 can be converted to a compound ( 1a)-2 by using an equivalent or excessive amount of hydrazine or its equivalent in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. A compound (1a)-2 can be converted to a compound ( 1a)-3 by using an equivalent or excessive amount of an oxidizing agent such as manganese dioxide or iodobenzenediacetate in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. The presence of an acid or a base is sometimes effective for smooth progress of the reaction. A compound (1a)-3 can also be obtained by using a compound (1a)-1 and an equivalent or excessive amount of tosylhydrazine or its equivalent in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. The presence of a base is sometimes effective for smooth progress of the reaction. A compound (1a)-3 having a protective group as RPR can be converted to a compound (1a)-3 having a hydrogen atom as R by deprotection. Among the compounds represented by the formula (la) , the compounds (2a)-2, (2a)-3 and (2a)-4 can be produced, for example, through the following scheme (2a) (wherein E a is an oxygen atom or a sulfur atom, R R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (2a)-3 (2a)-4 A compound (2a)-1 can be converted to a compound (2a)-2 by using an equivalent or excessive amount of R4aCHO, R4aC0 2RQ, R4aC(ORQ)3, R4aCONRQ 2 or R aC(ORQ)2NRQ (wherein RQ is a hydrogen atom or a C -6 alkyl group) in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. Microwave irradiation or the presence of an acid or a base is sometimes effective for smooth progress of the reaction. A compound (2a)-1 can be converted to a compound (2a)-3 by using an equivalent or excessive amount of phosgene, phosgene dimer, phosgene trimer, 1, 1 '- carbonyldiimidazole, dimethyl carbonate, carbon disulfide or 1, 1 '- thiocarbonyldiimidazole in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. The presence of an acid or a base is sometimes effective for smooth progress of the reaction. A compound (2a)-3 can be converted to a compound (2a)-4 by using equivalent or excessive amounts of R6a-R (wherein R is a leaving group such as a halogen atom, a methanesulfonyloxy group or a p-toluenesulfonyloxy group) and a base such as potassium carbonate or sodium hydride in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. A compound (2a)-3 or (2a)-4 having an oxygen atom as E a can be converted to a compound (2a)-3 or (2a)-4 having a sulfur atom as E a by using an equivalent or excessive amount of a thiocarbonylation reagent such as phosphorus pentasulfide or Lawesson's reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. Compounds (2a)-2, (2a)-3 and (2a)-4 having a protective group as RPR can be converted to compounds (2a)-2, (2a)-3 and (2a)-4 having a hydrogen atom as R R by deprotection. (Synthesis of starting materials 1a) The compounds (3a)-3 and (3a)-6 can be produced, for example, through the following scheme (3a) (wherein X is a chlorine atom, a bromine atom or an iodine atom, each of Rx and RY is independently a C -6 alkyl group, and RP is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (3a)-5 (3a)-6 A compound (3a)-1 can be converted to a compound (3a)-3 by a metal-halogen exchange reaction using an equivalent or excessive amount of an organic metal reagent such as isopropylmagnesium chloride, 2,6-dimethylphenylmagnesium bromide or nbutyllithium in an appropriate solvent at -78°C to room temperature followed by treatment with an equivalent or excessive amount of a compound (3a)-2 in an appropriate solvent at -78°C to room temperature. A compound (3a)-1 can be converted to a compound (3a)-5 by a metal-halogen exchange reaction using an equivalent or excessive amount of an organic metal reagent such as isopropylmagnesium chloride, 2,6-dimethylphenylmagnesium bromide or nbutyllithium in an appropriate solvent at -78°C to room temperature followed by treatment with an equivalent or excessive amount of a compound (3a)-4 in an appropriate solvent at -78°C to room temperature. A compound (3a)-5 can be converted to a compound (3a)-3 by using an equivalent or excessive amount of an oxidizing agent such as manganese dioxide or 1, 1 ,1-triacetoxy-1 ,1-dihydro-1 ,2-benziodoxol-3(1 H)-one (Dess-Martin reagent) in an appropriate solvent at -78°C to a refluxing temperature. A compound (3a)-3 can be converted to a compound (3a)-6 by using equivalent or excessive amounts of an amine reagent such as ammonium acetate or hydroxylamine and a reducing agent such as sodium triacetoxyborohydride or zinc in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (3a)-5 can be converted to a compound (3a)-6 by carrying out a reaction using equivalent or excessive amounts of phthalimide, a Mitsunobu reagent and a phosphine reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature, followed by deprotection. As a Mitsunobu reagent, diethyl azodicarboxylate, diisopropyl azodicarboxylate or the like may be mentioned, and as a phosphine reagent, triphenylphosphine, tributylphosphine or the like may be mentioned. A compound (3a)-1 having a chlorine atom as X can be converted to a compound (3a)-1 having a bromine or iodine atom as X by using an equivalent or excessive amount of hydrobromic acid or hydroiodic acid in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. Compounds (3a)-3 and (3a)-6 having a protective group as RPR can be converted to compounds (3a)-3 and (3a)-6 having a hydrogen atom as R R by deprotection. (Synthesis of starting materials 2a) The compounds (4a)-2 can be produced, for example, through the following scheme (4a) (wherein each of Rx and RY is independently a C -6 alkyl group, and the other symbols are the same as defined above). (4a)-l (4a)-2 A compound (4a)-1 can be converted to a compound (4a)-2 by using equivalent or excessive amounts of RYNH(ORx) and a condensation agent such as dicyclohexycarbodiimide or 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. The presence of an acid or a base is sometimes effective for smooth progress of the reaction. Among the compounds represented by the formula (la) , the compounds (5a)-3, (5a)-4, (5a)-5 and (5a)-6 can be produced , for example, through the following scheme (5a) (wherein m is 0,1 ,2 or 3, R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, R is a protective group such as a Boc group or a Cbz group, E3a is an oxygen atom or a sulfur atom, and the other symbols are the same as defined above). A compound (5a)-1 among the compounds (1a)-3 can be converted to a compound (5a)-2 by deprotection. A compound (5a)-2 can be converted to a compound (5a)-3 by using equivalent or excessive amounts of an electrophilic reagent represented by R aL3aL2a-R (wherein R is a leaving group such as a halogen atom, a methanesulfonyloxy group, a ptoluenesulfonyloxy group) such as an alkyl halide, a methanesulfonate ester, an acid halide, a sulfonyl chloride, a chloroformate and a base such as triethylamine in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (5a)-2 can be converted to a compound (5a)-3 by using equivalent or excessive amounts of R a-CHO and a reducing agent such as 2-picoline borane or sodium triacetoxyborohydride in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. A compound (5a)-2 can be converted to a compound (5a)-4 by using equivalent or excessive amounts of a compound (5a)-7 and a base such as potassium carbonate or triethylamine in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (5a)-2 can be converted to a compound (5a)-5 or / and (5a)-6 by using equivalent or excessive amounts of a compound (5a)-8, a base such as triethylamine and an acid catalyst such as ytterbium (III) trifluoromethanesulfonate in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. Compounds (5a)-3, (5a)-4, (5a)-5 and (5a)-6 having a protective group as R can be converted to compounds (5a)-3, (5a)-4, (5a)-5 and (5a)-6 having a hydrogen atom as R by deprotection. Among the compounds represented by the formula (la) , the compounds (6a)-3, (6a)-4 and (6a)-5 can be produced, for example, through the following scheme (6a) (wherein m is 0,1 ,2 or 3, R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, RP 3 is a protective group such as a benzyl group or an acetyl group, and the other symbols are the same as defined above). A compound (6a)-1 among the compounds (1a)-3 is converted to a compound (6a)-2 by deprotection. A compound (6a)-2 can be converted to a compound (6a)-3 by using an equivalent or excessive amount of an oxidizing agent such as 2-iodoxybenzoic acid or pyridinium chlorochromate in an appropriate solvent or in the absence of solvent at - 78°C to a refluxing temperature. A compound (6a)-3 can be converted to a compound (6a)-4 by using equivalent or excessive amounts of a compound (6a)-6 and a reducing agent such as 2-picoline borane or sodium triacetoxyborohydride in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. A compound (6a)-2 can be converted to a compound (6a)-5 by using equivalent or excessive amounts of an acidic alcohol represented by R a-OH such as phenol, a Mitsunobu reagent and a phosphine reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. As a Mitsunobu reagent, diethyl azodicarboxylate, diisopropyl azodicarboxylate or the like may be mentioned, and as a phosphine reagent, triphenylphosphine, tributylphosphine or the like may be mentioned. Compounds (6a)-3, (6a)-4 and (6a)-5 having a protective group as R can be converted to compounds (6a)-3, (6a)-4 and (6a)-5 having a hydrogen atom as R R by deprotection. Among the compounds represented by the formula (la) , the compounds (7a)-3, A compound (7a)-1 among the compounds (1a)-3 can be converted to a compound (7a)-2 by deprotection. A compound (7a)-2 can be converted to a compound (7a)-3 by using an equivalent or excessive amount of an oxidizing agent such as 2-iodoxybenzoic acid or pyridinium chlorochromate in an appropriate solvent or in the absence of solvent at - 78°C to a refluxing temperature. A compound (7a)-3 can be converted to a compound (7a)-4 by using equivalent or excessive amounts of a compound (7a)-10 and a reducing agent such as 2-picoline borane or sodium triacetoxyborohydride in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. A compound (7a)-5 can be converted to a compound (7a)-4 by using an equivalent or excessive amount of a compound (7a)-10 in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. The presence of a base is sometimes effective for smooth progress of the reaction. A compound (7a)-2 can be converted to a compound (7a)-5 by using equivalent or excessive amounts of a halogenating agent and a phosphine reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. As a halogenating agent, N-bromosuccinimide, ,-diethylaminosulfur trifluoride or the like may be mentioned, and as a phosphine reagent, triphenylphosphine, tributylphosphine or the like may be mentioned. A compound (7a)-5 can be converted to a compound (7a)-6 by using an equivalent or excessive amount of a compound (7a)-11 in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. The presence of an acid or a base is sometimes effective for smooth progress of the reaction. A compound (7a)-2 can be converted to a compound (7a)-7 by using equivalent or excessive amounts of an electrophilic reagent represented by R2a-R (R is a leaving group such as a halogen atom, a methanesulfonyloxy group or a p-toluenesulfonyloxy group) such as an alkyl halide, a methanesulfonyl ester or an acid halide and a base such as potassium carbonate or sodium hydroxide in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (7a)-2 can be converted to a compound (7a)-7 by using equivalent or excessive amounts of an acidic alcohol represented by R2a-OH such as phenol, a Mitsunobu reagent and a phosphine reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. As a Mitsunobu reagent, diethyl azodicarboxylate, diisopropyl azodicarboxylate or the like may be mentioned, and as a phosphine reagent, triphenylphosphine, tributylphosphine or the like may be mentioned. A compound (7a)-2 can be converted to a compound (7a)-8 or (7a)-9 by using equivalent or excessive amounts of R2aC(=0)OH or R a(C=0)SH, a Mitsunobu reagent and a phosphine reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. As R2aC(=0)OH, acetic acid or the like may be mentioned, as R a(C=0)SH, thioacetic acid or the like may be mentioned. As a Mitsunobu reagent, diethyl azodicarboxylate, diisopropyl azodicarboxylate or the like may be mentioned, and as a phosphine reagent, triphenylphosphine, tributylphosphine or the like may be mentioned. Compounds (7a)-3, (7a)-4, (7a)-5, (7a)-6, (7a)-7, (7a)-8 and (7a)-9 having a protective group as R R can be converted to compounds (7a)-3, (7a)-4, (7a)-5, (7a)-6, (7a)-7, (7a)-8 and (7a)-9 having a hydrogen atom as R by deprotection. Among the compounds represented by the formula (la) , the compounds (8a)-2 and (8a)-3 can be produced, for example, through the following scheme (8a) (wherein m is 0, 1, 2 or 3, R R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). A compound (8a)-1 among the compounds (7a)-2 can be converted to a compound (8a)-2 by using an equivalent or excessive amount of an oxidizing agent such as Jones reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (8a)-2 can be converted to a compound (8a)-3 by using equivalent or excessive amounts of a compound (8a)-4 and a condensation agent such as ,'- dicyclohexylcarbodiimide or 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. The presence of an acid or a base is sometimes effective for smooth progress of the reaction. Compounds (8a)-2 and (8a)-3 having a protective group as RPR can be converted to compounds (8a)-2 and (8a)-3 having a hydrogen atom as R by deprotection. Among the compounds represented by the formula (la) , the compounds (9a)-2 and (9a)-3 can be produced, for example, through the following scheme (9a) (wherein m is 0 , 1, 2 or 3 , R is a hydrogen atom or a protective group such as a Ts group, a TIPS roup, Rz is a hydrogen atom or a -6 alkyl group, and the other ame as d fined above). A compound (9a)-1 among the compounds (7a)-9 can be converted to a compound (9a)-2 by using an equivalent or excessive amount of an oxidizing agent such as hydrogen peroxide in an appropriate solvent or in the absence of solvent at - 78°C to a refluxing temperature. The presence of an acid catalyst such as ammonium molybdate tetrahydrate is sometimes effective for smooth progress of the reaction. A compound (9a)-2 can be converted to a compound (9a)-3 by using equivalent or excessive amounts of a compound (9a)-4 and a halogenating agent such as thionyl chloride or phosphorus oxychloride in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. The presence of a base such as triethylamine is sometimes effective for smooth progress of the reaction. Compounds (9a)-2 and (9a)-3 having a protective group as R can be converted to compounds (9a)-2 and (9a)-3 having a hydrogen atom as RPR by deprotection. Among the compounds represented by the formula (la) , the compounds (10a)-2 and (10a)-3 can be produced, for example, through the following scheme ( 10a) (wherein m is 0 , 1, 2 or 3, R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, Rz is a hydrogen atom or a C - alkyl group, and the other mbols are the same as defined above). A compound (10a)-1 among the compounds (7a)-4 can be converted to a compound (10a)-2 by using an equivalent or excessive amount of an acid halide in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. The presence of a base is sometimes effective for smooth progress of the reaction. A compound (10a)-1 among the compounds (7a)-4 can be converted to a compound (10a)-3 by using an equivalent or excessive amount of a sulfonyl halide in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. The presence of a base is sometimes effective for smooth progress of the reaction. Compounds (10a)-2 and (10a)-3 having a protective group as R can be converted to compounds (10a)-2 and ( 10a)-3 having a hydrogen atom as R by deprotection. Among the compounds represented by the formula (la) , the compounds (11a)-2, (11 a)-3, (11a)-4, (11a)-5, (11a)-6, (11a)-7, (11a)-8 and (11a)-9 can be produced, for example, through the following scheme ( a) (wherein m is 0, 1, 2 or 3, RP is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, Rz is a hydrogen atom or a C -6 alkyl group, R 1 is a C -6 alkyl group, and the other symbols are the same as defined above). A compound (11 a)-1 can be converted to a compound ( 11a)-2, (11 a)-3 or ( 11a)-4 by using an equivalent or excessive amounts of a phosphonium ylide such as a Horner- Wadsworth-Emmons reagent and a base such as sodium hydride in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (11a)-2, (11a)-4 or (11a)-3 can be converted to a compound (11 a)-5, ( 11a)-6 or (11a)-7 respectively by using an equivalent or excessive amount of a metal catalyst such as palladium-carbon catalyst under a hydrogen atmosphere in an appropriate solvent at -78°C to a refluxing temperature. A compounds (11a)-7 can be converted to a compounds ( 11a)-8 by deprotection. A compound (11a)-8 can be converted to a compound (11a)-9 by using equivalent or excessive amounts of a compound (11 a)-10 and a condensation agent such as ,'- dicyclohexylcarbodiimide or 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. The presence of an acid or a base is sometimes effective for smooth progress of the reaction. Compounds ( 11a)-2, (11a)-3, (11a)-4, (11a)-5, (11a)-6, (11a)-7, (11a)-8 and (11 a)-9 having a protective group as R can be converted to compounds (11 a)-2, (11a)-3, (11a)-4, (11a)-5, (11a)-6, (11a)-7, ( 11a)-8 and (11a)-9 having a hydrogen atom as RP by deprotection. Among the compounds represented by the formula (la) , the compounds (12a)-2, (12a)-3, (12a)-4 and (12a)-5 can be produced, for example, through the following scheme ( a) (wherein m is 0, 1, 2 or 3, RP is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, Rz is a hydrogen atom or a C -6 alkyl A compound (12a)-1 among the compounds (7a)-3 can be converted to a compound (12a)-2 by using equivalent or excessive amounts of a phosphonium ylide such as a Horner-Wadsworth-Emmons reagent and a base such as sodium hydride in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (12a)-2 can be converted to a compound (12a)-3 by using an equivalent or excessive amount of a metal catalyst such as palladium-carbon catalyst under a hydrogen atmosphere in an appropriate solvent at -78°C to a refluxing temperature. A compound (12a)-1 can be converted to a compound (12a)-4 by using equivalent or excessive amounts of malononitrile and a base such as piperidine in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (12a)-4 can be converted to a compound (12a)-5 by using an equivalent or excessive amount of a metal catalyst such as palladium-carbon catalyst under a hydrogen atmosphere in an appropriate solvent at -78°C to a refluxing temperature. Compounds (12a)-2, (12a)-3, (12a)-4 and (12a)-5 having a protective group as R can be converted to compounds (12a)-2, (12a)-3, (12a)-4 and (12a)-5 having a hydrogen atom as R by deprotection. Next, processes for producing the tricyclic pyridine compounds represented by the formula (lb) will be described. Among the tricyclic pyridine compounds represented by the formula (lb) , the compounds ( 1b)-2 can be produced, for example, through the following scheme ( 1b) (wherein R R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (lb)-l (lb)-2 A compound ( 1b)-2 can be obtained by cyclization of a compound ( 1b)-1 . A compound (1b)-1 can be converted to a compound ( 1b)-2 by using an equivalent or excessive amount of R C(=0)R 9b or R8bC(ORQ)2R9 (wherein RQ is a hydrogen atom or a Ci-6 alkyl group) in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. Microwave irradiation or the presence of an acid catalyst such as acetic acid, trifluoroacetic acid, hydrochloric acid, sulfuric acid or p-toluenesulfonic acid is sometimes effective for smooth progress of the reaction. A compound (1b)-2 having a protective group as R R can be converted to a compound having a hydrogen atom as R by deprotection. Among the compounds represented by the formula (lb) , the compounds (2b)-2 and (3b)-2 can be produced, for example, through the following schemes (2b) and (3b) (wherein Y is an oxygen atom or a sulfur atom, RPR is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the (2b)-l (2b)-2 (3b)-l (3b)-2 A compound (2b)-2 can be obtained by cyclization of a compound (2b)-1 . A compound (2b)-1 can be converted to a compound (2b)-2 by using an equivalent or excessive amount of R CHO, R bC0 2RQ, R C(OR Q)3, R bCONR Q 2 or R bC(ORQ)2NRQ 2 (wherein RQ is a hydrogen atom or a C -6 alkyl group) in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. Microwave irradiation or the presence of an acid or a base is sometimes effective for smooth progress of the reaction. A compound (2b)-2 having an oxygen atom as Y can be converted to a compound (2b)-2 having a sulfur atom as Y by using an equivalent or excessive amount of a thiocarbonylation agent such as phosphorus pentasulfide or Lawesson's reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (2b)-2 having a protective group as R can be converted to a compound having a hydrogen atom as R by deprotection. A compound (3b)-2 can be obtained by cyclization of a compound (3b)- 1 like the synthesis of a compound (2b)-2. A compound (3b)-2 having a protective group as R can be converted to a compound having a hydrogen atom as R R by deprotection. Among the compounds represented by the formula (lb) , the compounds (4b)-2, (4b)-3 and (4b)-4 can be produced, for example, through the following scheme (4b) (wherein Y is an oxygen atom or a sulfur atom, R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the (RlOb = H ) ( 4b ) A compound (4b)-2 can be obtained by cyclization of a compound (4b)-1 . A compound (4b)-1 can be converted to a compound (4b)-2 by using an equivalent or excessive amount of phosgene, phosgene dimmer, phosgene trimer, 1, 1 '- carbonyldiimidazole, dimethyl carbonate, 1, 1 '-thiocarbonyldiimidazole, carbon disulfide or the like in an appropriate solvent at room temperature to a refluxing temperature. The presence of an acid or a base is sometimes effective for smooth progress of the reaction. A compound (4b)-2 having hydrogen atoms as R5b and R10b can be converted to a compound (4b)-3 by using a catalyst such as palladium-carbon or manganese dioxide in an appropriate solvent at room temperature to a refluxing temperature. A compound (4b)-2 or (4b)-3 having an oxygen atom as Y can be converted to a compound (4b)-2 or (4b)-3 having a sulfur atom as Y by using a thiocarbonylation agent such as phosphorus pentasulfide or Lawesson's reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (4b)-2 or (4b)-3 having a protective group as R can be converted to a compound having a hydrogen atom as RP by deprotection. A compound (4b)-1 having a hydrogen atom as R10b can be converted to a compound (4b)-4 by cyclization. A compound (4b)-1 can be converted to a compound (4b)-4 by using an equivalent or excessive amount of R8bCHO, R8bC0 2RQ, R bC(ORQ)3, R bCONRQ 2 or R8bC(ORQ)2NRQ 2 (wherein RQ is a hydrogen atom or C1-6 alkyl group) in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. Microwave irradiation or the presence of an acid or a base is sometimes effective for smooth progress of the reaction. A compound (4b)-4 having a protective group as R can be converted to a compound having a hydrogen atom as R by deprotection. Among the compounds represented by the formula (lb) , the compounds (5b)-2 can be produced, for example, through the following scheme (5b) (wherein Y is an oxygen atom or a sulfur atom, R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (5b)-l (5b)-2 A compound (5b)-2 can be obtained by cyclization of a compound (5b)-1 . A compound (5b)-1 can be converted to a compound (5b)-2 by using an equivalent or excessive amount of R bCHO, R bC0 2RQ, R8 C(ORQ)3, R8 CONRQ 2 or R8bC(ORQ)2NRQ 2 (wherein RQ is a hydrogen atom or a C1-6 alkyl group) in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. Microwave irradiation or the presence of an acid or a base is sometimes effective for smooth progress of the reaction. A compound (5b)-2 having an oxygen atom as Y can be converted to a compound having a sulfur atom as Y by using an equivalent or excessive amount of a thiocarbonylation agent such as phosphorus pentasulfide or Lawesson's reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (5b)-2 having a protective group as R can be converted to a compound having a hydrogen atom as R R by deprotection. Among the compounds represented by the formula the compounds (6b)-2 and (6b)-3 can be produced, for example, through the following scheme (6b) (wherein XB is a bromine atom or an iodine atom, R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (6b)-l (6b)-2 (6b)-3 A compound (6b)-3 can be obtained by bromination or iodination of a compound (6b)-1 followed by cyanization of the resulting compound (6b)-2. A compound (6b)-1 can be converted to a compound (6b)-2 by using an equivalent or excessive amount of a halogenating agent such as bromine, iodine, Nbromosuccinimide or N-iodosuccinimide in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (6b)-2 can be converted to a compound (6b)-3 by using an equivalent or excessive amount of a metal cyanide such as copper cyanide or zinc cyanide in the presence of a palladium catalyst such as tetrakis(triphenylphosphine)palladium(0) or bis(triphenylphosphine)palladium(ll) dichloride in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. A compound (6b)-2 or (6b)-3 having a protective group as R can be converted to a compound having a hydrogen atom as R by deprotection. (Synthesis of starting materials 1b) The compounds (7b)-2 can be produced, for example, through the following rogen atom or a the other (7b)-3 A compound (7b)-2 can be obtained by a Mitsunobu reaction of a compound (7b)- 1 with R1 R NH (wherein R is a protective group suited for a Mitsunobu reaction such as a methanesulfonyl group or a p-toluenesulfonyl group) following by deprotection. A compound (7b)-1 can be converted to a compound (7b)-2 by using equivalent or excessive amounts of R 0bR 1NH, a Mitsunobu reagent and a phosphine reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature, followed by deprotection. As a Mitsunobu reagent, diethyl azodicarboxylate, diisopropyl azodicarboxylate or the like may be mentioned, and as a phosphine reagent, triphenylphosphine, tributylphosphine or the like may be mentioned. A compound (7b)- 2 having a hydrogen atom as R10b can be obtained by a similar reaction using phthalimide instead of R 0 R 1NH followed by deprotection. A compound (7b)-2 can be obtained by conversion of a compound (7b)-1 to a compound (7b)-3 having a leaving group R followed by a substitution reaction using R10bNH2. A compound (7b)-1 can be converted to a compound (7b)-3 by using an equivalent or excessive amount of phosphorus oxychloride, thionyl chloride, methanesulfonyl chloride, p-toluenesulfonyl chloride or the like in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. The presence of a base is sometimes effective for smooth progress of the reaction. A compound (7b)-3 can be converted to a compound (7b)-2 by using an equivalent or excessive amount of R10bNH2 in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. Microwave irradiation or the presence of a base is sometimes effective for smooth progress of the reaction. (Synthesis of starting materials 2b) The compounds (8b)-3 can be produced, for example, through the following scheme (8b) (wherein R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (8b)-l (8b)-2 (8b)-3 A compound (8b)-3 can be obtained by oxidation of a compound (8b)-1 followed by condensation of the resulting compound (8b)-2. A compound (8b)-1 can be converted to a compound (8b)-2 by using an equivalent or excessive amount of a oxidizing agent such as potassium permanganate or sodium chlorite in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. A compound (8b)-2 can be converted to a compound (8b)-3 by using equivalent or excessive amounts of ammonia-methanol or its equivalent and a condensation agent such as ,'-dicyclohexylcarbodiimide or 1-ethyl-3-(3- dimethylaminopropyl)carbodiimide hydrochloride in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. The presence of a catalyst such as N-hydroxybenzotriazole or a base is sometimes effective for smooth progress of the reaction. (Synthesis of staring materials 3b) The compounds (9b)-2 and (9b)-3 can be produced, for example, through the following scheme (9b) (wherein R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (9b)-3 A compound (9b)-2 can be obtained by an addition reaction of a compound (9b)-1 . A compound (9b)-1 can be converted to a compound (9b)-2 by using an equivalent or excessive amount of an addition reaction reagent in a solvent inert to the reaction at -78°C to a refluxing temperature. As an addition reaction reagent, a hydride reducing agent such as sodium borohydride or diiisobutylaluminum hydride or a metal reagent such as methyllithium or phenylmagnesium bromide may be mentioned. A compound (9b)-3 can be obtained by reductive N-alkylation of a compound (9b)- 1 through formation of an imine. A compound (9b)-1 can be converted to a compound (9b)-3 by using equivalent or excessive amounts of R10bNH2 and a hydride reducing agent such as sodium cyanoborohydride or sodium tnacetoxyborohydride in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. Microwave irradiation or the presence of an acid is sometimes effective for smooth progress of the reaction. A compound having a hydrogen atom as R10b can be obtained by using hydroxylamine or its equivalent instead of R10bNH2 and lithium aluminum hydride, zinc or a hydrogen atmosphere containing palladium-carbon as a reducing agent. (Synthesis of starting materials 4b) The compounds (10b)-3, (11 b)-3 and (12b)-3 can be produced, for example, through the following schemes (10b), ( ) and (12b) (wherein R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (llb)-l (llb)-2 (llb)-3 (12b)-l (12b)-2 (12b)-3 A compound (10b)-1 can be converted to a compound (10b)-3 by using an equivalent or excessive amount of an amine derivative (10b)-2 in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. The substituent reaction is preferred to be carried out under microwave irradiation or sometimes in the presence of a base or may be carried out under the reaction conditions used for the Buchwald-Hartwig reaction (for example, by referring to Advanced Synthesis & Catalysis, 2004, 346, pp. 1599-1626). It is possible to appropriately combine tris(dibenzylideneacetone)dipalladium (0), tetrakis(triphenylphosphine)palladium(0), palladium (II) acetate or the like with 4,5- bis(diphenylphosphino)-9,9-dimethylxanthene (Xantphos), 2-dicyclohexylphosphino- 2',6'-dimethoxybiphenyl (SPhos), 2-dicyclohexylphosphino-2 ,,4',6'-triisopropylbiphenyl (XPhos) or the like, without particular restrictions. Compounds (11 b)-3 and (12b)-3 can be obtained by using a compound ( b)-1 and an amine derivative (11b)-2 or a compound (12b)-1 and an amine derivative (12b)-2, like a compound (10b)-3. (Synthesis of starting materials 5b) The compounds (13b)-4 can be produced, for example, through the following scheme (13b) (wherein R R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, RQ is a hydrogen atom or a -6alkyl group, and the other symbols are the same as defined above). i3b (13b)-l (13b)-2 (13b)-4 A compound (13b)-4 can be obtained by the Stille reaction of compounds (13b)-2 and (13b)-3 (for example, by referring Bulletin of the Chemical Society of Japan, 1987,60,pp.767-768). A compound (13b)-2 can be converted to a compound (13b)-4 by using an equivalent or excessive amount of a compound ( 13b)-3 in the presence of a palladium catalyst such as tetrakis(triphenylphosphine)palladium (0), bis(triphenylphosphine)palladium (II) dichloride or bis(acetonitrile)palladium (II) dichloride in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. The presence of an acid or a base is sometimes effective for smooth progress of the reaction. A compound (13b)-2 can be obtained by oxidization of a compound (13b)-1 followed by a reaction of the resulting N-oxide derivative with a chlorination agent. A compound (13b)-1 can be converted to a compound (13b)-2 by oxidation with an equivalent or excessive amount of an oxidizing agent such as m-chloroperbenzoic acid, peracetic acid or aqueous hydrogen peroxide in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature, followed by a reaction of the resulting N-oxide derivative with an equivalent or excessive amount of a chlorination agent such as phosphorus oxychloride or methanesulfonyl chloride in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. (Synthesis of starting materials 6b) The compounds (14b)-3 and (14b)-5 can be produced, for example, through the following scheme (14b) (wherein R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (14b)-l (14b)-2 (14b)-3 ( 14b ) (14b)-4 (14b)-5 Compounds (14b)-3 and (14b)-4 can be obtained by coupling of an anion formed from a compound (14b)-2. A compound (14b)-2 can be converted to a compound (14b)-3 by lithiation using an equivalent or excessive amount of an organic metal reagent such as n-butyllithium or s-butyllithium in an appropriate solvent or in the absence of solvent at -78°C to room temperature followed by coupling with an electrophilic reagent such as N,Ndimethylformamide, R bC0 2RQ, R4bCONRQ 2 or R bC(0)N(OR Q)RQ (wherein RQ is a hydrogen atom or a C - alkyl group). A compound (14b)-2 can be converted to a compound (14b)-4 by lithiation using an equivalent or excessive amount of an organic metal reagent such as n-butyllithium or s-butyllithium in an appropriate solvent or in the absence of solvent at -78°C to room temperature followed by coupling with an electrophilic reagent such as (R bCH2S)2. A compound (14b)-4 can be converted to a compound (14b)-5 by using an equivalent or excessive amount of an oxidizing agent such as m-chloroperbenzoic acid, peracetic acid or aqueous hydrogen peroxide in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. A compound (14b)-1 can be converted to a compound (14b)-2 by oxidation with an equivalent or excessive amount of an oxidizing agent such as m-chloroperbenzoic acid, peracetic acid or aqueous hydrogen peroxide in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature, followed by a reaction of the resulting N-oxide derivative with an equivalent or excessive amount of a chlorination agent such as phosphorus oxychloride or methanesulfonyl chloride in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. (Synthesis of starting materials 7b) The compounds (15b)-4 can be produced, for example, through the following scheme (15b) (wherein R is a hydrogen atom or a protective group such as a Ts (15b)-l (15b)-2 (15b)-3 (15b)-4 A compound (15b)-4 can be obtained by bromination or iodination of a compound (15b)-2 followed by dehydrogenation of the resulting compound (15b)-3. A compound (15b)-3 can be converted to a compound (15b)-4 by using a catalyst such as palladium-carbon or manganese dioxide in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. A compound (15b)-2 can be converted to a compound (15b)-3 by using an equivalent or excessive amount of a halogenating agent such as bromine, Nbromosuccinimide, iodine or N-iodosuccinimide in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. A compound (15b)-1 can be converted to a compound (15b)-2 in the presence of a palladium-carbon catalyst under a hydrogen atmosphere in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. (Synthesis of starting materials 8b) The compounds (16b)-2 can be produced, for example, through the following scheme (16b). A compound (16b)-1 can be converted to a compound (16b)-2 by using an equivalent or excessive amount of R16bC0 2RQ or R16bC(ORQ)3 (wherein RQ is a hydrogen atom or a C -6 alkyl group) in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. For synthesis of 7-azaindole or 1-deazapurine, the following general methods may be referred to. As general methods for synthesis of 7-azaindole, those disclosed in Current Organic Chemistry,2001 ,5,pp.471 -506 are known. As general methods for synthesis of 1-deazapurine, those disclosed in Shin-pen Hetero-kan Kagoubutsu Ouyou-hen (Kodansha, 2004) pp.233-251 are known. (Synthesis of starting materials 9b) (17b)-l The amine compounds (17b)-1 can be produced from the corresponding nitrile compounds, acid amide compounds, oxime compounds, halogen compounds, ketone compounds, aldehyde compounds, alcohol compounds, boron compounds, epoxide compounds, acid imide compounds and carbamate compounds (for example, by referring to Jikken Kagaku Koza vol. 20 Yuki Gosei II, edited by the Chemical Society of Japan, published by MARUZEN Co., Ltd., 1992; Bioorganic & Medicinal Chemistry, 13, 4022, 2005, Kuramochi T. et al.; Journal of Medicinal Chemistry, 50, 49, 2007; Journal of Organic Chemistry, 46, 4296, 1981 ; Journal of Organic Chemistry, 44, 2081 , 1979; Acta Chemica Scandinavica, 19, 1741 , 1965; and Organic Letters, 5, 4497, 2003). Among the compounds represented by the formula (l ) , the compounds ( 8b)-2 and (18b)-3 can be produced, for example, through the following scheme ( 18b) (wherein R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, and the other symbols are the same as defined above). (18b)-l (18b)-2 (18b)-3 A compound (18b)-3 can be obtained by cyclization of a compound ( 1 8b)-1 followed by a substitution reaction of the resulting compound (18b)-2. A compound (18b)-1 can be converted to a compound (18b)-2 by using an equivalent or excessive amount of phosgene, phosgene dimer, phosgene trimer, 1, 1 '- carbonyldiimidazole, dimethyl carbonate, 1, 1 '-thiocarbonyldiimidazole , carbon disulfide or the like in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. The presence of an acid or a base or microwave irradiation is sometimes effective for smooth progress of the reaction. A compound (18b)-2 can be converted to a compound (18b)-3 by using an equivalent or excessive amount of an electrophilic reagent represented by R 0b-R (wherein R is a leaving group such as a chlorine atom, a methanesulfonyloxy group or a p-toluenesulfonyloxy group) such as an alkyl halide, an alkyl mesylate or an aryl halide in the presence of a base such as triethylamine in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. Microwave irradiation is sometimes effective for smooth progress of the reaction. A compound (18b)-2 can also be converted to a compound ( 8b)-3 by using equivalent or excessive amounts of a primary or secondary alcohol, a Mitsunobu reagent and a phosphine reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. As a Mitsunobu reagent, diethyl azodicarboxylate, diisopropyl azodicarboxylate or the like may be mentioned, and as a phosphine reagent, triphenylphosphine, tributylphosphine or the like may be mentioned. A compound (18b)-2 or (18b)-3 having an oxygen atom as Y can be converted to a compound ( 8b)-2 or ( 18b)-3 having a sulfur atom as Y by using an equivalent or excessive amount of a thiocarbonylation agent such as phosphorus pentasulfide or Lawesson's reagent in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (18b)-2 or (18)-3 having a protective group as RP can be converted to a compound having a hydrogen atom as RP by deprotection. Among the compounds represented by the formula (lb) , the compounds (19b)-2 and (19b)-3 can be produced, for example, through the following scheme (19b) (wherein RPR is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, R 2 is a benzyl type protective group such as a benzyl group or a benzyloxycarbonyl group, m is 0-3, and the other symbols are the same as defined (19b)-l (19b)-2 (19b)-3 A compound (19b)-3 can be obtained by deprotection of the R in a compound ( 19b)-1 among the compounds (2b)-2 followed by a substitution reaction of the resulting compound (19b)-2. A compound (19b)-1 having a benzyl type protective group as R R2 can be converted to a compound (19b)-2 by using a catalytic amount of palladium-carbon under a hydrogen atmosphere in an appropriate solvent at room temperature to a refluxing temperature. The presence of an acid is sometimes effective for smooth progress of the reaction. A compound (19b)-2 can be converted to a compound (19b)-3 by using equivalent or excessive amounts of an electrophilic reagent represented by R2bL3bL2b-R (wherein R is a leaving group such as a halogen atom, a methanesulfonyloxy group or a ptoluenesulfonyloxy group) such as an alkyl halide, an acid chloride, a sulfonyl chloride, a chloroformate ester, an isocyanate or an isothiocyanate and a base such as triethylamine in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (19b)-2 can also be converted to a compound (19b)-3 by using an equivalent or excessive amount of an aldehyde or a ketone in the presence of a hydride reducing agent such as sodium cyanoborohydride or 2-picoline borane in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. Microwave irradiation or the presence of an acid is sometimes effective for smooth progress of the reaction. A compound ( 9b)-3 having a protective group as R can be converted to a compound having a hydrogen atom as R by deprotection. Among the compounds represented by the formula (lb) , the compounds (20b)-2 and (20b)-3 can be produced, for example, through the following scheme (20b) (wherein R R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, R 2 is a benzyl type protective group such as a benzyl group or a benzyloxycarbonyl group, m is 0, , 2 or 3 and the other symbols are the same as defined above). (20b)-l (20b)-2 (20b)-3 A compound (20b)-3 can be obtained by deprotection of the R in a compound (20b)-1 among the compounds ( 18b)-3 followed by a substitution reaction of the resulting compound (20b)-2. A compound (20b)- having a benzyl type protective group as R 2 can be converted to a compound (20b)-2 by using a catalytic amount of palladium-carbon under a hydrogen atmosphere in an appropriate solvent at room temperature to a refluxing temperature. The presence of an acid is sometimes effective for smooth progress of the reaction. A compound (20b)-2 can be converted to a compound (20b)-3 by using equivalent or excessive amounts of an electrophilic reagent represented by R L3bL b-R (wherein R is a leaving group such as a halogen atom, a methanesulfonyloxy group or a ptoluenesulfonyloxy group) such as an alkyl halide, an acid chloride, sulfonyl chloride, a chloroformate, an isocyanate or an isothiocyanate and a base such as triethylamine in an appropriate solvent or in the absence of solvent at -78°C to a refluxing temperature. A compound (20b)-2 can also be converted to a compound (20b)-3 by using an equivalent or excessive amount of an aldehyde or a ketone in the presence of a reducing agent such as sodium cyanoborohydride or 2-picoline borane in an appropriate solvent or in the absence of solvent at 0°C to a refluxing temperature. Microwave irradiation or the presence of an acid is sometimes effective for smooth progress of the reaction. A compound (20b)-3 having a protective group as R can be converted to a compound having a hydrogen atom as R by deprotection. Among the compounds represented by the formula (l ) , the compounds (21 b)-2, (21 b)-3 and (21b)-4 can be produced, for example, through the following scheme (21b) (wherein R is a hydrogen atom or a protective group such as a Ts group, a TIPS group or a SEM group, R 5 is a protective group such as a benzyl group or an acetyl group, Rz is a hydrogen atom or a C - alkyl group, m is 0, 1, 2 or 3 , and the other symbols are the same as defined above). A compound (21 b)-1 among the compounds (18b)-3 is converted to a compound (21 b)-2 by deprotection. A compound (21 b)-2 can be converted to a compound (21 b)-3 by oxidation with an equivalent or excessive amount of an oxidizing agent such as 2-iodoxybenzoic acid or pyridinium chlorochromate in an appropriate solvent or in the absence of solvent at - 78°C to a refluxing temperature. A compound (21 b)-3 can be converted to a compound (21 b)-4 by using equivalent or excessive amounts of a compound (21 b)-5 and a reducing agent such as 2-picoline borane or sodium triacetoxyborohydride in an appropriate solvent or in the absence of solvent at room temperature to a refluxing temperature. Compounds (21 b)-3 and (21 b)-4 having a protective group as R can be converted to compounds (21 b)-3 and (21 b)-4 having a hydrogen atom as R by deprotection. In the present invention, the tricyclic pyrimidine compounds of the present invention represented by the formula (la) and the tricyclic pyridine compounds of the present invention represented by the formula (lb) may be present in the form of tautomers or geometrical isomers which undergo endocyclic or exocyclic isomerization, mixtures of tautomers or geometric isomers or mixtures of thereof. When the compounds of the present invention have an asymmetric center, whether or not resulting from an isomerization, the compounds of the present invention may be in the form of resolved optical isomers or in the form of mixtures containing them in certain ratios. Further, when the compounds of the present invention have two or more asymmetric centers, the compounds of the present invention can be in the form of diastereomers due to optical isomerism about them. The compounds of the present invention may be in the form of a mixture of all these isomers in certain ratios. For example, diastereomer can be separated by techniques well known to those skilled in the art such as fractional crystallization, and optical isomers can be obtained by techniques well known in the field of organic chemistry for this purpose. The tricyclic pyrimidine compounds of the present invention represented by the formula (la) and the tricyclic pyridine compounds of the present invention represented by the formula (lb) or pharmaceutically acceptable salts thereof may be in the form of arbitrary crystals or arbitrary hydrates, depending on the production conditions. The present invention covers these crystals, hydrates and mixtures. They may be in the form of solvates with organic solvents such as acetone, ethanol, 1-propanol and 2- propanol, and the present invention covers any of these forms. The present invention covers pharmaceutically acceptable salts of the compounds of the present invention represented by the formulae (l ) and (lb) . The compounds of the present invention represented by the formulae (la) and (lb) may be converted to pharmaceutically acceptable salts or may be liberated from the resulting salts, if necessary. The pharmaceutically acceptable salts of the present invention may be, for example, salts with alkali metals (such as lithium, sodium and potassium), alkaline earth metals (such as magnesium and calcium), ammonium, organic bases, amino acids, inorganic acids (such as hydrochloric acid, hydrobromic acid, phosphoric acid and sulfuric acid) and organic acids (such as acetic acid, citric acid, maleic acid, fumaric acid, tartaric acid, benzenesuifonic acid, methanesulfonic acid and p-toluenesulfonic acid). The present invention covers prodrugs of the compounds of the present invention represented by the formulae (la) and (lb) . Prodrugs are derivatives of medicinal compounds having chemically or metabolically degradable groups and give pharmacologically active medicinal compounds upon solvolysis or under physiological conditions in vivo. Methods for selecting or producing appropriate prodrugs are disclosed in, for example, Design of Prodrugs (Elsevier, Amsterdam 1985). In the present invention, in the case of a compound having a hydroxy group, prodrugs like acyloxy derivatives obtained by reacting the compound with appropriate acyl halides, appropriate acid anhydrides or appropriate haloalkoxycarbonyl compounds may, for example, be mentioned. Structures particularly preferred as prodrugs include -OCOC2H5, -OCO(t-Bu), - OCOC15H3 1, -OCO(m-C0 2Na-Ph), -OCOCH2CH2C0 2Na, -OCOCH(NH2)CH3, - OCOCH2N(CH3)2 -0-CH 2OC(=0)CH 3 or the like. In the case of a compound having an amino group, prodrugs obtained by reacting the compound having an amino group with appropriate acid halides, appropriate mixed acid anhydrides or haloalkoxycarbonyl compounds may, for example, be mentioned. Structures particularly preferred as prodrugs include -NHCO(CH2)20OCH3, -NHCOCH(NH 2)CH3, -NH-CH20(C=0)CH 3 or the like. The JAK inhibitors and the preventive, therapeutic and/or improving agents for diseases against which inhibition of JAK is effective are those mentioned below among the tricyclic pyrimidine compounds and the tricyclic pyridine compounds of the present invention. 1) JAK inhibitors containing the compounds as defined in any one of 1a) to 62a) and 1b) to 44 ) , tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof, as an active ingredient. 2) Preventive, therapeutic or improving agents for diseases against which inhibition of JAK is effective, which contains the JAK inhibitors as defined in 1) as an active ingredient. 3) Therapeutic agents for rheumatoid arthristis, which contain the JAK inhibitors as defined in 1) as an active ingredient. 4) Medicaments containing the compound as defined in any one of 1a) to 62a) and 1b) to 44b) , tautomers or pharmaceutically acceptable salts of the compounds or solvates thereof, as an active ingredient. The preventive, therapeutic and improving agents for diseases against which inhibition of JAK is effective which contain the JAK inhibitors of the present invention, as an active ingredient may usually be administered as oral medicines such as tablets, capsules, powder, granules, pills and syrup, as rectal medicines, percutaneous medicines or injections. The agents of the present invention may be administered as a single therapeutic agent or as a mixture with other therapeutic agents. Though they may be administered as they are, they are usually administered in the form of medical compositions. These pharmaceutical preparations can be obtained by adding pharmacologically and pharmaceutically acceptable additives by conventional methods. Namely, for oral medicines, ordinary additives such as excipients, lubricants, binders, disintegrants, humectants, plasticizers and coating agents may be used. Oral liquid preparations may be in the form of aqueous or oily suspensions, solutions, emulsions, syrups or elixirs or may be supplied as dry syrups to be mixed with water or other appropriate solvents before use. Such liquid preparations may contain ordinary additives such as suspending agents, perfumes, diluents and emulsifiers. In the case of rectal administration, they may be administered as suppositories. Suppositories may use an appropriate substance such as cacao butter, laurin tallow, Macrogol, glycerogelatin, Witepsol, sodium stearate and mixtures thereof as the base and may, if necessary, contain an emulsifier, a suspending agent, a preservative and the like. For injections, pharmaceutical ingredients such as distilled water for injection, physiological saline, 5% glucose solution, propylene glycol and other solvents or solubilizing agents, a pH regulator, an isotonizing agent and a stabilizer may be used to form aqueous dosage forms or dosage forms which need dissolution before use. The dose of the agents of the present invention for administration to human is usually about from 0.1 to 1000 mg/body/day in the case of oral drugs or rectal administration and about from 0.05 mg to 500 mg/body/day in the case of injections, though it depends on the age and conditions of the patient. The above-mentioned ranges are mere examples, and the dose should be determined from the conditions of the patient. The present invention is used when it is expected to improve pathology of diseases associated with JAK1 , JAK2 and JAK3 separately or in combination. Among these diseases, JAK3-associated diseases are, in addition to rheumatoid arthristis, inflammatory or proliferative dermatoses such as psoriasis, atopic dermatitis, contact dermatitis, eczematoid dermatitis, seborrheic dermatitis, lichen planus, pemphigus, pemphigoid, epidermolysis bullosa, hives, angioedema, angiitis, erythema, dermal eosinophilia, lupus erythematosus, acne, alopecia areata, immune dermatoses, reversible airway obstruction, mucitis and angitis. Among these diseases, JAK3- and JAK1 -associated diseases are, in addition to rheumatoid arthristis, asthma, atopic dermatitis, Alzheimer disease, atherosclerosis, cancer, leukemia, rejection of organ or tissue grafts (such as heart, kidney, liver, bone marrow, skin, horn, lung, pancreas, islet, small intestine, extremities, muscles, nerves, intervertebral disks, trachea, myoblasts and cartilage), graft-versus-host reaction after bone marrow transplantation and autoimmune diseases such as rheumatic disease, systemic lupus erythematosus (SLE), Hashimoto's disease, multiple sclerosis, myasthenia gravis, type I diabetes and diabetic complications. Among these diseases, JAK2-associated diseases include, for example, myeloproliferative disorders. As an application of the present invention, treatment and prevention of the abovementioned diseases may be mentioned, but there is no restriction. Compounds of the present invention are administered either alone or in combination with one or more additional agents such as immunomodulators, antiinflammatory agents or antirheumatic drugs. The additional agents may be cyclosporin A, tacrolimus, leflunomide, deoxyspergualin, mycophenolate, azathioprine, etanercept (e.g. Enbrel®) , infliximab (e.g. Remicade®) , adalimumab (e.g. Humira®) , certolizumab pegol (e.g. Cimzia®) , Golimumab (e.g. Simponi®) , Anakinra (e.g. Kineret®) , rituximab (e.g. Rituxan®) , Tocilizumab (e.g. Actemra ®) , methotrexate, aspirin, acetaminophen, ibuprofen, naproxen, piroxicam, and antiinflmmatory steroids (e.g. prednisolone or dexamethasone), but are not restricted thereto. Now, the present invention will be described in further detail with reference to Reference Synthetic Examples, Synthetic Examples, Assay Examples and Formulation Examples. However, it should be understood that the present invention is by no means restricted by these specific Examples. In the Examples, "NMR" denotes nuclear magnetic resonance, "LC/MS" denotes high performance liquid chromatography-mass spectrometry, "v/v" means volume ratio. In the tables, "Rf" denotes Reference Synthetic Example, "Ex" denotes Synthetic Example, "Structure" denotes chemical structural formula, "diastereomixture" denotes a diastereomeric mixture, "racemate" denotes a racemic mixture, "cis/trans mixture" denotes a cis- and trans-isomeric mixture, and "E/Z mixture" denotes a E- and Z-isomeric mixture, and "Data" denotes physical property data, "condition" denotes measurement condition, "retention time" denotes retention time in LC/MS, "Compound Name" denotes compound name of the synthesized compound, "Morphology" denotes morphology of a synthesized compound, "Yield" denotes yield of a synthesized compound, "quant" denotes quantitative, "min" denotes minute. In the Examples herein, "rac-" or "racemate" used in texts or tables for a compound having more than one asymmetric center means that the compound is in the form of a racemic mixture of the specified absolute configuration and its enantiomer. The 1H-NMR data show chemical shifts (unit : ppm) (splitting pattern, value of integral) measured at 300 MHz (with JNM-ECP300, manufactured by JEOL Ltd or JNMECX300, manufactured by JEOL Ltd) using tetramethylsilane as an internal standard. "s" denotes "singlet", "d" denotes "doublet", "t" denotes "triplet", "q" denotes "quartet " , "quint" denotes quintet, "sextet" denotes sextet, "septet" denotes septet, "dd" denotes doublet of doublets, "dt" denotes doublet of triplets, "td" denotes triplet of doublets, "dq" denotes doublet of quartets, "qd" denotes quartet of doublets, "tt" denotes triplet of triplets, "ddd" denotes doublet of doublet of doublets, "m" denotes multiplet, "br" denotes broad, "J" denotes coupling constant, "CDCI3" denotes deuterated chloroform, "CD3OD" denotes deuterated methanol, and "DMSO-d6" denotes deuterated dimethyl sulfoxide. For purification by silica gel column chromatography, Hi Flash column manufactured by Yamazen Corporation, a silica gel 60 manufactured by Merck & Co., Inc. or PSQ60B manufactured by Fuji Silysia Chemical Ltd. was used unless otherwise noted. For purification by silica gel thin layer chromatography, PLC plate manufactured by Merck & Co., Inc. was used unless otherwise noted. As a microwave reactor, Initiator sixty manufactured by Biotage was used. LC/MS spectra were measured by using ESI (electrospray ionization). "ESI+" denotes ESI-positive mode, and "ESI " denotes ESI-negative mode. LC/MS condition 1 Instrument: Waters Alliance-ZQ Column: Waters SunFire C18(3.5pm, 2.1 x20mm) Column Temp.: 40°C Eluents: Liquid A: 0.1% aqueous formic acid Liquid B: 0.1 % formic acid in acetonitrile Elution: A mixture of Liquids A and B was flown at 0.4 mL/min while the mixing ratio was linearly changed from 90/10 (v/v) to 15/85 (v/v) over the first 3 minutes, and then the flow rate was linearly changed to 0.5 mUmin for 2 minutes at a constant mixing ratio of 15/85 (v/v). Then, the mixing ratio was linearly changed to 90/10 (v/v) over 0.5 minute and maintained at 90/10 (v/v) for 2.5 minutes. LC/MS condition 2 Instrument: Waters Alliance-ZQ Column: Waters SunFire C18(3.5pm, 2.1x20mm) Column Temp.: 40°C Eluents: Liquid A: 0.2% aqueous formic acid Liquid B: acetonitrile Elution: A mixture of Liquids A and B was flown at 0.4 mlJ min while the mixing ratio was linearly changed from 90/1 0 (v/v) to 15/85 (v/v) over the first 3 minutes, and then the flow rate was linearly changed to 0.5 mUmin over 2 minutes at a constant mixing ratio of 15/85 (v/v). Then, the mixing ratio was linearly changed to 95/5 (v/v) over 0.5 minute and maintained at 95/5 (v/v) for 1.5 minutes. LC/MS condition 3 Instrument:: Thermo LTQ XL Column: Waters AQUITY UPLC BEH 018(1 .7, 2.1x50mm) Column Temp.: 40°C Eluents: Liquid A: 0.1 % aqueous formic acid Liquid B: 0.1% formic acid in acetonitrile Elution: A mixture of Liquids A and B was flown at 0.6 mUmin at a mixing ratio of 90/10 (v/v) for the first 0.5 minutes, and then the mixing ratio was linearly changed to 10/90 (v/v) over 2.5 minutes and then maintained at 10/90 (v/v) for 0.7 minute. The mixing ratio and the flow rate were linearly changed to 90/10 (v/v) and 0.8 mL/min, respectively, over 0.1 minute, maintained constant for 1 minute and linearly changed to 90/ 0 (v/v) and 0.6 mL/min, respectively, over 0.1 minute. REFERENCE SYNTHETIC EXAMPLE 1 4-lodo-7H-pyrrolor2,3-cnpyrimicline Hydroiodic acid (55 wt%, 100g) was mixed with 4-chloro-7H-pyrrolo[2,3- d]pyrimidine (manufactured by Tokyo Chemical Industry Co., Ltd., 10.6 g, 69.0 mmol) under cooling with ice and stirred at 0°C for 1 hour and then at room temperature for one day. The precipitated solid was collected by filtration and washed with water. The residue was suspended in water, neutralized with 1 M aqueous sodium hydroxide and filtered. The yellow solid was washed with water and dried under reduced pressure to give the title compound as a yellow solid (16.2 g, yield 96%, including 10% 4-chloro-7H-pyrrolo[2,3-d]pyrimidine as the starting compound). REFERENCE SYNTHETIC EXAMPLE 2 4-lodo-7-(triisopropylsilyl)-7H-pyrrolo[2,3-dlpyrimidine 4-lodo-7H-pyrrolo[2,3-d]pyrimidine (352 mg, 1.44 mmol) in tetrahydrofuran (15 mL) cooled to 0°C was mixed with sodium hydride (55 wt% dispersion in mineral oil, 75.5 mg, 1.73 mmol) and chlorotriisopropylsilane (0.37 mL, 1.7 mmol) and stirred at room temperature for 45 minutes. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate =100/1 (v/v)) to give the title compound as a pale yellow oil (431 mg, yield 74%). REFERENCE SYNTHETIC EXAMPLE 3 Cvclohexyl[7-(triisopropylsilyl)-7H-pyrrolo[2,3-dlpyrimidin-4-vnmethanol n-Butyllithium ( 1 .6 M solution in hexane, 0.23 mL, 0.380 mmol) was gradually added dropwise to 4-iodo-7-(triisopropylsilyl)-7H-pyrrolo[2,3-d]pyrimidine (126 mg, 0.3 0 mmol) in tetrahydrofuran ( .5 mL) cooled to -78°C, and the reaction mixture was stirred at -78°C for 30 minutes. After addition of cyclohexanecarbaldehyde (42 L, 0.35 mmol) in tetrahydrofuran ( 1 .5 mL), the reaction mixture was gradually warmed from -78°C to room temperature and stirred for one day. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: hexane / ethyl acetate = 10/1 7/1 4/1 (v/v)) to give the title compound as a colorless oil (65.5 mg, yield 55%). REFERENCE SYNTHETIC EXAMPLE 4 Cvclohexyl[7-(triisopropylsilyl)-7H-pyrrolof2,3-dlpyrimidin-4-vnmethanone Cyclohexyl[7-(triisopropylsilyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]methanol (21 mg, 0.540 mmol) in dichloromethane (7 mL) was stirred with 1, 1 , 1 -triacetoxy-1 ,1-dihydro- 1,2-benziodoxol-3(1 H)-one (347 mg, 0.820 mmol) at room temperature for 2.5 hours. After addition of a mixture (1/1 (v/v)) of saturated aqueous sodium hydrogen carbonate and saturated aqueous sodium thiosulfate, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ ethyl acetate = 30/1 (v/v)) to give the title compound as a colorless solid (117 mg, yield 55%). REFERENCE SYNTHETIC EXAMPLE 5 Cvclohexyl(7H-pyrrolor2.3-d1pyrimidin-4-yl)methanone Cyclohexyl[7-(triisopropylsilyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]methanone (22.4 mg, 58.0 mol) was stirred with hydrogen chloride - methanol solution (10 wt%, 2.0 mL) at room temperature for 15 minutes. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 10/1 (v/v)) to give the title compound as a pale yellow oil (9.2 mg, yield 69%). REFERENCE SYNTHETIC EXAMPLE 6 Cvclohexyl(7 -(f2-(trimethylsilyl)ethoxylmethyl)-7H-pyrrolor2,3-d1pyrimidin-4- vQmethanone Cyclohexyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)methanone (50.0 mg, 0.21 8 mmol) in N,N-dimethylformamide ( 1 mL) was mixed with sodium hydride (60 wt% dispersion in mineral oil, 9.6 mg, 0.24 mmol) and [2-(chloromethoxy)ethyl]trimethylsilane (42.5 L, 0.240 mmol) under cooling with ice and stirred for 30 minutes while the temperature was gradually raised to room temperature. Separately, cyclohexyl(7H-pyrrolo[2,3- d]pyrimidin-4-yl)methanone (500 mg, 2.18 mmol) in N,N-dimethylformamide (5 mL) was mixed with sodium hydride (60 wt% dispersion in mineral oil, 96 mg, 2.4 mmol) and (chloromethoxy)ethyl]trimethylsilane (425 L, 2.40 mmol) under cooling with ice and stirred for 30 minutes while the temperature was gradually raised to room temperature. After addition of water, the reaction solution and the previously obtained reaction solution were extracted with ethyl acetate, respectively, and the organic layers were washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residues were combined and purified by silica gel column chromatography (hexane/ ethyl acetate =5/1 (v/v)) to give the title compound as a pale yellow oil (850 mg, yield 99%). REFERENCE SYNTHETIC EXAMPLE 7 Cvclohexyl(7 - 2-(trimethylsilyl)ethoxy1methyl)-7H-pyrrolor2,3-dlpyrimidin-4- vDmethanamine Cyclohexyl(7-{[2-(trimethylsilyl)ethoxy]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4- yl)methanone (406 mg, 1.13 mmol) in methanol (10 ml) was stirred with hydroxylamine hydrochloride (395 mg, 5.66 mmol) for 4 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in ethanol (3.0 mL), mixed with ammonium acetate (105 mg, 1.36 mmol), water (3 mL) and aqueous ammonia (5 mL) and refluxed with zinc powder (600 mg, 9.17 mmol) for 4 hours. The reaction mixture was allowed to cool to room temperature and filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 20/1 (v/v)) to give the title compound as a yellow oil (390 mg, yield 79%). REFERENCE SYNTHETIC EXAMPLE 3 8 1-Cvclohexyl-7 -(r2-(trimethylsilyl)ethoxylmethyl)-7H-imidazon ,5-clpyrroloi3,2- elpyrimidine Cyclohexyl(7-{[2-(trimethylsilyl)ehoxy]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4- yl)methanamine (10 mg. 0.028 mmol) in ,-dimethylformamide dimethyl acetal (0.7 mL) was stirred at 170°C for 30 minutes under microwave irradiation. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure, and the resulting residue was dissolved in 1,3-dimethylimidazolidin-2-one ( 1 .0 mL) and stirred at 230°C for 1.5 hours under microwave irradiation. Separately, cyclohexyl(7-{[2-(trimethylsilyl)ethoxy]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4- ylmethanamine (89 mg, 0.25 mmol) in ,-dimethylformamide dimethyl acetal ( 1 mL) was stirred at 170°C for 30 minutes under microwave irradiation. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure, and the resulting residue was dissolved in 1,3-dimethylimidazolidin-2-one (4.5 mL) and stirred at 230°C for 1.5 hours under microwave irradiation. The reaction mixture and the previously obtained reaction mixture were combined, diluted with ethyl acetate, acidified with 1 M hydrochloric acid and washed with saturated aqueous ammonium chloride and saturated aqueous sodium chloride, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (hexane / ethyl acetate = 2/1 1/1 1/2 (v/v)) to give the title compound as a pale yellow oil (31 .4 mg, yield 30%). REFERENCE SYNTHETIC EXAMPLE 9 N-Methoxy-N,2-dimethylbenzamide 2-Methylbenzoic acid ( 1 .00 g, 7.34 mmol) and 1-(3-dimethylaminopropyl)-3- ethylcarbodiimide hydrochloride ( 1 .69 g, 8.81 mmol) in chloroform (10 mL) stirred with N,N-diisopropylethylamine ( 1 .50 mL, 8.81 mmol) for 10 minutes under cooling with ice and then stirred with ,-dimethylhydroxylamine hydrochloride (860 mg, 8.81 mmol) and N,N-diisopropylethylamine ( 1 .50 mL, 8.81 mmol) for one day while the temperature was gradually raised to room temperature. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a pale yellow oil (658 mg, yield 50%). REFERENCE SYNTHETIC EXAMPLE3 10 (7H-Pyrrolof2,3-dlpyrimidin-4-yl)(o-tolyl)methanone Isopropylmagnesium chloride (2.0 M solution in tetrahydrofuran, 1.05 mL, 2.10 mmol) was gradually added dropwise to 4-iodo-7H-pyrrolo[2,3-d]pyrimidine (245 mg, 1.00 mmol) obtained in Reference Synthetic Example 1 in tetrahydrofuran (5 mL) cooled to -78°C, and the resulting reaction mixture was stirred at -78°C for 15 minutes. The reaction mixture was warmed to room temperature and stirred with (2,6- dimethylphenyl)magnesium bromide ( 1 .0 M solution in tetrahydrofuran, 1. 1 mL, 1. 1 mmol) and N-methoxy-N,2-dimethylbenzamide ( 180 mg, 1.00 mmol) in tetrahydrofuran (4 mL) at room temperature for one day. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ ethyl acetate = 2/1 1/1 (v/v)) to give the title compound as a pale yellow solid ( 162 mg, yield 68%). REFERENCE SYNTHETIC EXAMPLE3 11 N-Methoxy-N-methylcvclohexanecarboxamide The reactions in Reference Synthetic Example3 9 were carried out in substantially the same manners except that cyclohexanecarboxylic acid was used instead of 2- methylbenzoic acid to give the title compound as a colorless oil (2.14 g, yield 46%). REFERENCE SYNTHETIC EXAMPLE 12 Cvclohexyl(7H-pyrrolo[2,3-d1pyrimidin-4-yl)methanone The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that N-methoxy-Nmethylcyclohexanecarboxamide was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as a pale yellow solid ( 1 .26 g , yield 67%). REFERENCE SYNTHETIC EXAMPLE 13 N-Methoxy-N.2-dimethylcvclohexanecarboxamide The reactions in Reference Synthetic Example 9 were carried out in substantially the same manners except that 2-methylcyclohexanecarboxylic acid was used instead of 2-methylbenzoic acid to give the title compound as a colorless oil (623 mg, yield 48%). REFERENCE SYNTHETIC EXAMPLE 14 (2-Methylcvclohexyl)(7H-pyrrolof2,3-dlpyrimidin-4-yl)methanone The reactions in Reference Synthetic Example3 0 were carried out in substantially the same manners except that N-methoxy-N,2- dimethylcyclohexanecarboxamide was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as a colorless solid (165 mg, yield 68%). REFERENCE SYNTHETIC EXAMPLE 15 4-lodo-7-{[2-(trimethylsilyl)ethoxy1methyl)-7H-pyrrolor2,3-d1pyrimidine 4-lodo-7H-pyrrolo[2,3-d]pyrimidine (90 mg, 0.037 mmol) obtained in Reference Synthetic Example 1 in N,N-dimethylformamide (4 mL) was stirred with sodium hydride (55 wt% dispersion in mineral oil, 19.2 mg, 0.0440 mmol) and [2- (chloromethoxy)ethyl]trimethylsilane (77.9 i , 0.0440 mmol) at room temperature for one day. After addition of saturated aqueous sodium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 10/1 4/1 (v/v)) to give the title compound as a colorless oil (115 mg, yield 83%). REFERENCE SYNTHETIC EXAMPLE3 16 Benzyl 3-(hydroxymethyl)piperidine-1 -carboxylate 3-Piperidinemethanol (3.59 g, 3 1.2 mmol) in 1,4-dioxane (8 mL) was mixed with potassium carbonate (4.55 g, 33.0 mmol), 1 M aqueous sodium hydroxide (2 mL) and benzyl chloroformate (5.20 mL, 36.4 mmol) under cooling with ice and stirred at room temperature for one day. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous potassium hydrogen sulfate and saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a colorless oil (6.41 g , yield 83%). REFERENCE SYNTHETIC EXAMPLE3 17 Benzyl 3-fmethoxy(methvDcarbamovnpiperidine-1 -carboxylate Benzyl 3-(hydroxymethyl)piperidine-1-carboxylate (2.0 g, 8.0 mmol) in dichloromethane (50 mL) was stirred with 1, 1 ,1-triacetoxy-1 , 1 -dihydro-1 ,2-benziodoxol- 3(1 H)-one (5.1 g, 12 mmol) at room temperature for 2.5 hours. After addition of a mixture (1/1 (v/v)) of saturated aqueous sodium hydrogen carbonate and saturated aqueous sodium thiosulfate, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in t-butanol (25 mL), mixed with sodium dihydrogen phosphate (2.89 g, 24.1 mmol), water (25 mL) and 2-methyl-2- butene (25 mL, 241 mmol), then stirred with sodium chlorite (3.62 g, 40.1 mmol) at 0°C for 1 hour and then stirred at room temperature for 1 hour. After addition of saturated aqueous sodium thiosulfate, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in N,N-dimethylformamide (60 mL) and mixed with ,-dimethylhydroxylamine hydrochloride ( 1 .02 g, 10.4 mmol) and 0-(7-azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate (4.0 g, 10.4 mmol) and then stirred with triethylamine ( 1 .5 mL, 10 mmol) at room temperature for 2.5 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/1 1/1 (v/v)) to give the title compound as a pale yellow oil ( .44 mg, yield 59% (three steps)). REFERENCE SYNTHETIC EXAMPLE 8 Benzyl 3-(7-{r2-(trimethylsilyl)ethoxy1methyl)-7H-pyrrolof2,3-dlpyrimidine-4- carbonyQpiperidine-1 -carboxylate Isopropylmagnesium chloride (2.0 M solution in tetrahydrofuran, 0.4 mL, 0.80mmol) was gradually added dropwise to 4-iodo-7-{[2-(trimethylsilyl)ethoxy]methyl}- 7H-pyrrolo[2,3-d]pyrimidine (200 mg, 0.530 mmol) obtained in Reference Synthetic Example 15 in tetrahydrofuran (3 mL) cooled to -78°C, and the resulting reaction mixture was stirred at -78°C for 15 minutes. The reaction mixture was warmed to room temperature and stirred with (2,6-dimethylphenyl)magnesium bromide ( 1 .0 M solution in tetrahydrofuran, 0.8 mL, 0.80 mmol) and benzyl 3- [methoxy(methyl)carbamoyl]piperidine-1 -carboxylate (245 mg, 0.800 mmol) in tetrahydrofuran (3.0 mL) at room temperature for 2.5 hours. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 4/1 2/1 1/1 (v/v)) to give the title compound as a yellow oil ( 107 mg, yield 41%). REFERENCE SYNTHETIC EXAMPLE3 19 Benzyl 3-[amino(7-(r2-(trimethylsilyl)ethoxy1methyl)-7H-pyrrolof2,3-d1pyrimidin-4- yl)methyllpiperidine-1-carboxylate The reactions in Reference Synthetic Example3 7 were carried out in substantially the same manners except that 3-(7-{[2-(trimethylsilyl)ehoxy]methyl}-7H-pyrrolo[2,3- d]pyrimidine-4-carbonyl)piperidine-1-carboxylate (253 mg, 0.510 mmol) was used instead of cyclohexyl(7-{[2-(trimethylsilyl)ethoxy]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4- yl)methanone to give the title compound as a pale blue oil (183 mg, yield 72%). REFERENCE SYNTHETIC EXAMPLE3 20 Benzyl 3-(7-(r2-(trimethylsilvnethoxylmethyl)-7H-imidazof 1.5-c1pyrrolor3,2-elpyrimidin-1 - yl)piperidine-1 -carboxylate Benzyl 3-[amino(7-{[2-(trimethylsilyl)ethoxy]methy}-7H-pyrrolo[2,3-d]pyrimidin-4- yl)methyl]piperidine-1 -carboxylate (63 mg, 0.13 mmol) in N,N-dimethylformamide dimethyl acetal ( 1 mL) was stirred at 170°C for 30 minutes under microwave irradiation. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure, and the resulting residue was dissolved in 1,3-dimethylimidazolidin- 2-one ( 1 mL) and stirred at 230°C for 1.5 hours under microwave irradiation. The reaction mixture was allowed to cool to room temperature, diluted with ethyl acetate and washed with saturated aqueous ammonium chloride and saturated aqueous sodium chloride, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The concentrate was purified by silica gel thin layer chromatography (hexane / ethyl acetate = 1/1 1/2 (v/v)) to give a brown oil containing the title compound (45.2 mg). The resulting mixture was used for the next step. REFERENCE SYNTHETIC EXAMPLE3 2 1 trans-4-(Hvdroxymethvn-N-methoxy-N-methylcvclohexanecarboxamide The reactions in Reference Synthetic Example 9 were carried out in substantially the same manners except that trans-4-(hydroxylmethyl)cyclohexanecarboxylic acid (manufactured by Tokyo Chemical Industry Co., Ltd.) was used instead of 2- methylbenzoic acid to give the title compound as a colorless oil (515 mg, yield 41%). REFERENCE SYNTHETIC EXAMPLE 22 trans-4-[(tert-Butyldiphenylsilyloxy)methyl1-N-methoxy-Nmethylcvclohexanecarboxamide trans-4-(Hydroxymethyl)-N-methoxy-N-methylcyclohexanecarboxamide (403 mg, 2.00 mmol) in N,N-dimethylformamide (4 mL) was mixed with tertbutylchlorodiphenylsilane (514 L, 2.00 mmol) and H-imidazole (136 mg, 2.00 mmol) under cooling with ice and stirred for one day while the temperature was gradually raised to room temperature. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 8/1 (v/v)) to give the title compound as a colorless oil (536 mg, yield 61%). REFERENCE SYNTHETIC EXAMPLE3 23 (trans-4-[(tert-Butyldiphenylsilyloxy)methvncvclohexyl)(7H-pyrrolor2,3-dlpyrimidin-4- ypmethanone The reactions in Reference Synthetic Example3 10 were carried out in substantially the same manners except that trans-4-[(tert-butyldiphenylsilyloxy)methyl]- N-methoxy-N-methylcyclohexanecarboxamide was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as a yellow oil (11 1 mg, yield 59%). REFERENCE SYNTHETIC EXAMPLE3 24 1-(trans-4-f(tert-Butyldiphenylsilyloxy)methyllcvclohexyl)-7H-pyrrolof3,2- elf1 ,2,31triazolo[1 ,5-clpyrimidine The reactions in Synthetic Example 5 were carried out in substantially the same manners except that {trans-4-[(tert-butyldiphenylsilyloxy)methyl]cyclohexyl}(7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)methanone obtained in Reference Synthetic Example 23 was used instead of (7H-pyrrolo[2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a pale yellow solid (50.6 mg, yield 46%). REFERENCE SYNTHETIC EXAMPLE3 25 3-Methyl 1-tert-butyl 4-methylpiperidine-1 ,3-dicarboxylate 4-Methylpyridine-3-carboxylic acid ( 1 .13 g, 6.48 mmol) in methanol (20 mL) was refluxed with concentrated sulfuric acid (4.0 mL) for 2 days under heating. The reaction mixture was concentrated under reduced pressure, gradually adjusted to pH 8 or above with saturated aqueous sodium hydrogen carbonate and extracted with ethyl acetate twice. The resulting organic layer was washed with water and saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give a red oil (0.89 g). The reactions were carried out with 4-methylpyridine-3-carboxylic acid ( 1 .77 g, 10.2 mmol) to give a red oil ( 1 .37 g). The red oil (2.26 g) obtained above was dissolved in ethyl acetate (35 mL) was stirred with active carbon (400 mg) at room temperature for 30 minutes. The mixture was filtered, and the filtrate was concentrated under reduced pressure. The resulting residue was dissolved in acetic acid (35 mL) and stirred with platinum(IV) oxide ( 162 mg) under a hydrogen atmosphere at 0.5 MPa for 3 days. The reaction mixture was filetered, and the filtrate was concentrated under reduced pressure. The resulting residue was dissolved in acetonitrile (50 mL) and water (40 mL) and stirred with sodium hydrogen carbonate (5.00 g, 59.5 mmol) and tert-butyl bicarbonate (5.1 0 g, 23.4 mmol) for one day. The reaction mixture was extracted with diethyl ether twice, and the organic layer was washed with 1 M hydrochloric acid and saturated aqueous magnesium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a colorless oil (4.33 g, yield 90% (three steps)). REFERENCE SYNTHETIC EXAMPLE 26 tert-Butyl 3-[methoxy(methyl)carbamoyll-4-methylpiperidine-1 -carboxylate Diisobutylaluminum hydride ( 1 .0 M solution in toluene, 23.4 mL, 23.7 mmol) was added dropwise to 3-methyl 1-tert-butyl 4-methylpiperidine-1 ,3-dicarboxylate (2.43 g , 9.46 mmol) in tetrahydrofuran (60 mL) cooled to -78°C, and the resulting reaction mixture was stirred at -78°C for 1 hour and at room temperature for 2 hours, then stirred with methanol and Celite at room temperature for 30 minutes and filtered. The filtrate was concentrated under reduced pressure. The resulting residue was roughly purified by silica gel column chromatography (hexane / ethyl acetate = 4/1 2/1 1/1 (v/v)) to give a colorless oil ( .62 g). The crude product ( 1 .02 g) was dissolved in dichloromethane (30 mL) and stirred with 1, 1 , 1 -triacetoxy-1 ,1-dihydro-1 ,2-benziodoxol- 3(1 H)-one (2.83 g, 6.67 mmol) at room temperature for 1.5 hours. After addition of a mixture (1/1 (v/v)) of saturated aqueous sodium hydrogen carbonate and saturated aqueous sodium thiosulfate, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in t-butanol (12 mL), mixed with sodium dihydrogen phosphate ( 1 .33 g, 1 1 . 1 mmol), water (12 mL) and 2-methyl-2- butene (12 mL, 111 mmol) and stirred with sodium chlorite ( 1 .68 g, 18.6 mmol) under cooling with ice for 30 minutes and then at room temperature 1 hour. After addition of saturated aqueous sodium thiosulfate, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in N,Ndimethylformamide (30 mL), mixed with ,-dimethylhydroxylamine hydrochloride (396 mg, 4.06 mmol) and 0-(7-azabenzotriazol-1 -yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate (2.00 g, 5.41 mmol) and stirred with N,N-diisopropylethylamine ( 1 .50 mL, 8.45 mmol) at room temperature for one day. After addition of water, the reaction solution was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 4/1 2/1 (v/v)) to give the title compound as a pale yellow oil (644 mg, yield 38% (four steps)). REFERENCE SYNTHETIC EXAMPLE 27 tert-Butyl 4-methyl-3-(7H-pyrrolof2,3-dlpyrimidine-4-carbonyl)piperidine-1 -carboxylate The reactions in Reference Synthetic Example3 10 were carried out in substantially the same manners except that tert-butyl 3-[methoxy(methyl)carbamoyl]-4- methylpiperidine-1-carboxylate was used instead of N-methoxy-N,2-dimethylbenzamide to give the title compound as a pale yellow solid (53.8 mg, yield 73%). REFERENCE SYNTHETIC EXAMPLE 28 tert-Butyl 3-imethoxy(methyl)carbamoyllpiperidine-1 -carboxylate The reactions in Reference Synthetic Example 9 were carried out in substantially the same manners except that 1-(tert-butoxycarbonyl)piperidine-3-carboxylate was used instead of 2-methylbenzoic acid to give the title compound as a colorless oil ( 1 .68 g , yield 57%). REFERENCE SYNTHETIC EXAMPLE3 29 tert-Butyl 3-(7H-pyrrolor2,3-dlpyrimidine-4-carbonyl) piperidine - 1-carboxylate The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that tert-butyl 3- [methoxy(methyl)carbamoyl]piperidine-1-carboxylate was used instead of N-methoxy- N,2-dimethylbenzamide to give the title compound as a pale yellow solid ( 1 .19 g, yield 68%). REFERENCE SYNTHETIC EXAMPLE3 30 1- (Benzyloxy)carbonyl1piperidine-3-carboxylic acid Nipecotic acid (3.93 g, 30.4 mmol) and sodium carbonate (5.1 0 g, 48.1 mmol) in water (40 mL) was mixed with benzyl chloroformate (5.20 mL, 36.4 mmol) under cooling with ice and stirred at room temperature for one day. After addition of water and 1 M aqueous sodium hydroxide, the reaction mixture was allowed to separate by adding diethyl ether. The aqueous layer was adjusted to pH 1 with concentrated hydrochloric acid and extracted with ethyl acetate. The resulting organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give the title compound as a pale yellow oil (5.86 g, yield 73%). REFERENCE SYNTHETIC EXAMPLE3 3 1 Benzyl 3-[methoxy(methyl)carbamovnpiperidine-1 -carboxylate 1-[(Benzyloxy)carbonyl]piperidine-3-carboxylic acid (5.86 g , 22.3 mmol) and ,- dimethylhydroxylamine hydrochloride (3.55 g, 36.4 mmol) in tetrahydrofuran (60 mL) was stirred with triethylamine (5.50 mL, 39.5 mmol), 1-hydroxybenzotriazole ( 1 . 17 g, 8.66 mmol) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (7.18 g , 37.4 mmol) at room temperature for one day. After addition of water, the reaction solution was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a colorless oil (5.95 g, yield 87%). REFERENCE SYNTHETIC EXAMPLE 32 Benzyl 3-(7H-pyrrolof2,3-d1pyrimidine-4-carbonyl)piperidine-1 -carboxylate The reactions in Reference Synthetic Example3 10 were carried out in substantially the same manners except that benzyl 3- [methoxy(methyl)carbamoyl]piperidine-1-carboxylate was used instead of N-methoxy- N,2-dimethylbenzamide to give the title compound as a pale yellow solid (3.56 g, yield 53%). REFERENCE SYNTHETIC EXAMPLE3 33 1-Benzylpiperidine-3-carboxylic acid Nipecotic acid ( 1 .31 g, 10.2 mmol), benzaldehyde ( 1 .12 g, 10.6 mmol) and 5% palladium-carbon (0.18 g) in methanol ( 10 mL) was stirred at room temperature for one day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The resulting residue was dissolved in methanol (50 mL) was stirred with benzaldehyde (4.40 g, 4 .5 mmol) and 5% palladium-carbon (0.118 g) at room temperature for one day. The reaction mixture was filtered, and the filtrated was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (chloroform / methanol = 10/1 5/1 (v/v)) to give the title compound as a colorless oil ( 1 .41 g, yield 63%). REFERENCE SYNTHETIC EXAMPLE 34 1-Benzyl-N-methoxy-N-methylpiperidine-3-carboxamide 1-Benzylpiperidine-3-carboxylic acid (31 8 mg, 1.45 mmol) and ,- dimethylhydroxylamine hydrochloride (287 mg, 2.94 mmol) in tetrahydrofuran (5 mL) was stirred with triethylamine (283 , 2.03 mmol) , -hydroxybenzotriazole (101 mg, 0.747 mmol) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (560 mg, 2.92 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residues was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a colorless oil (272 mg, yield 71%). REFERENCE SYNTHETIC EXAMPLE 35 (1-Benzylpiperidin-3-yl)(7H-pyrrolo[2,3-dlpyrimidin-4-y0methanone The reactions in Reference Synthetic Example 3 10 were carried out in substantially the same manners except that 1-benzyl-N-methoxy-N-methylpiperidine-3- carboxamide was used instead of N-methoxy-N,2-dimethylbenzamide to give the title compound as a yellow amorphous (121 mg, yield 91%). REFERENCE SYNTHETIC EXAMPLE 3 36 Phenyl 1,3,4-thiadiazol-2-ylcarbamate 1,3,4-Thiadiazol-2-amine (253 mg, 2.50 mmol) in dimethylacetamide (3 mL) was stirred with phenyl chloroformate (392 , 3.13. mmol) at room temperature for one day. After addition of water, the precipitated solid was collected by filtration, washed with water and hexane and dried under reduced pressure to give the title compound as a colorless solid (418 mg, yield 76%). REFERENCE SYNTHETIC EXAMPLE 37 Phenyl (3-methylisothiazol-5-yl)carbamate 3-Methythiazol-5-amine (156 mg, 1.04 mmol) in pyridine ( 1 .2 mL) was mixed with phenyl chloroformate (260 , 2.07 mmol) under cooling with ice and stirred at room temperature for 3 hours. The reaction mixture was concentrated under reduced pressure, and after addition of water, extracted with chloroform twice, and the organic layer was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a pale yellow solid (173 mg, yield 7 1%). REFERENCE SYNTHETIC EXAMPLE 38 tert-Butyl 4-[methoxy(methyl)carbamovHpiperidine-1 -carboxylate The reactions in Reference Synthetic Example 3 9 were carried out in substantially the same manners except that 1-(tert-butoxycarbonyl)piperidine-carboxylic acid was used instead of 2-methylbenzoic acid to give the title compound as a colorless oil (763 mg, yield 64%). REFERENCE SYNTHETIC EXAMPLE 39 tert-Butyl 4-(7H-pyrroloi2,3-d1pyrimidine-4-carbonyl)piperidine-1 -carboxylate The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that tert-butyl 4- [methoxy(methyl)carbamoyl]piperidine-1 -carboxylate was used instead of N-methoxy- N,2-dimethylbenzamide to give the title compound as a pale yellow amorphous (486 mg, yield 74%). REFERENCE SYNTHETIC EXAMPLE 40 N-Methoxy-N-methylpiperidine-4-carboxamide hydrochloride tert-Butyl 4-[methoxy(methyl)carbamoyl]piperidine-1 -carboxylate ( 1 .00 g, 3,67 mmol) obtained in Reference Synthetic Example 3 38 in 1,4-dioxane ( 10 mL) was stirred with 4 M hydrogen chloride - 1,4-dioxane solution (8 mL) at room temperature for one day. The solid precipitated in the reaction mixture was collected by filtration to give the title compound as a colorless solid (650 mg, yield 85%). REFERENCE SYNTHETIC EXAMPLE 4 1 N-Methoxy-N-methyl-1 -(2,2,2-trifluoroethyl)pipehdine-4-carboxamide N-Methoxy-N-methylpiperidine-4-carboxamide hydrochloride (600 mg, 2.88 mmol) in water (5 mL) was adjusted to pH 10 with 1 M aqueous sodium hydroxide and extracted with 1-butanol. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give a colorless solid. The resulting solid (200 mg, 1.16 mmol) was dissolved in N,N-dimethylformamide (4 mL) and stirred with potassium carbonate (481 mg, 3.48 mmol) and 2,2,2-trifluoroethyl trifluoromethanesulfonate (335 L, 2.32 mmol) at room temperature for one day. After addition of water and saturated aqueous sodium chloride, the reaction mixture was extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (methanol / chloroform = 1/19 1/9 (v/v)) to give the title compound as a colorless oil ( 190 mg, yield 26%). REFERENCE SYNTHETIC EXAMPLE 42 (7H-Pyrrolor2,3-dlpyrimidin-4-yl)[1-(2,2,2-trifluoroethyl)piperidin-4-yl1methanone The reactions in Reference Synthetic Example 3 10 were carried out in substantially the same manners except that N-methoxy-N-methyl-1 -(2,2,2- trifluoroethyl)piperidine-4-carboxamide was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as a colorless solid (100 mg, yield 43%). REFERENCE SYNTHETIC EXAMPLE 43 Benzyl 4-fmethoxy(methyl)carbamoyl1piperidine-1 -carboxylate Benzyl chloroformate ( 1 .64 mL, 11 .6 mmol) was gradually added dropwise to piperidine-4-carboxylic acid ( 1 .00 g, 7.74 mmol) and sodium carbonate ( 1 .64 g, 15.5 mmol) in water (20 mL) under cooling with ice, and the resulting reaction mixture was stirred for 2 hours. After addition of 1 M aqueous sodium hydroxide, the reaction mixture was allowed to separate by adding ethyl acetate. The resulting aqueous layer was adjusted to pH 4 with 1 M hydrochloric acid and extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give a colorless oil. The oil was dissolved in chloroform (30 mL) and stirred with ,-dimethylhydroxylamine hydrochloride ( 1 .50 g, 15.4 mmol), 1-(3- dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (3.00 g, 15.4 mmol), 1- hydroxybenzotriazole (2.00 g, 15.4 mmol) and triethylamine (3.2 mL, 23.1 mmol) at room temperature for 3 days. After addition of water and saturated aqueous ammonium chloride, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a colorless oil ( 1 .57 g, yield 66%). REFERENCE SYNTHETIC EXAMPLE 44 Benzyl 4-(7H-pyrrolof2,3-dlpyrimidine-4-carbonyl)piperidine-1-carboxylate The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that benzyl 4- [methoxy(methyl)carbamoyl]piperidine-1-carboxylate was used instead of N-methoxy- N,2-dimethylbenzamide to give the title compound as a yellow oil ( 1.40 g, yield 78%). REFERENCE SYNTHETIC EXAMPLE 3 45 tert-Butyl (trans-4-rmethoxy(methyl)carbamovncyclohexyl)carbamate trans-4-Aminocyclohexanecarboxylic acid (500 mg, 3.49 mmol) in water ( 10 mL) was stirred with di-tert-butyl bicarbonate ( .50 g , 6.98 mmol) and sodium hydroxide (280 mg, 6.98 mmol) at room temperature for 2 hours. The reaction mixture was washed with ethyl acetate, and the aqueous layer was adjusted to pH 3 with 1 M hydrochloric acid and extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give a colorless oil. The oil was dissolved in chloroform (10 mL) and stirred with ,-dimethylhydroxylamine hydrochloride (683 mg, 7.00 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride ( 1.34 g, 7.00 mmol), 1-hydroxybenzotriazole (946 mg, 7.00 mmol) and triethylamine ( 1.50 mL, 0.5 mmol) at room temperature for one day. After addition of water and saturated aqueous sodium chloride, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 2/1 1/1 (v/v)) to give the title compound as a colorless solid (513 mg, yield 5 1%). REFERENCE SYNTHETIC EXAMPLE 46 tert-Butyl [trans-4-(7H-pyrrolo[2,3-dlpyrimidine-4-carbonyl)cvclohexyllcarbamate The reactions in Reference Synthetic Example3 10 were carried out in substantially the same manners except that tert-butyl {trans-4- [methoxy(methyl)carbamoyl]cyclohexyl}carbamate was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as a colorless solid (52.0 mg, yield 8.4%). REFERENCE SYNTHETIC EXAMPLE 47 Benzyl (trans-4-fmethoxy(methyl)carbamoyllcvclohexyl)carbamate Benzyl chloroformate (885 L, 6.30 mmol) was gradually added dropwise to trans- 4-aminocyclohexanecarboxylic acid (600 mg, 4.20 mmol) and sodium carbonate (891 mg, 8.40 mmol) in water (12 mL) under cooling with ice, and the reaction mixture was stirred for one day. After addition of 1 M aqueous sodium hydroxide and ethyl acetate, the insoluble solid was collected by filtration to give a colorless solid. The solid was dissolved in chloroform (10 mL) and stirred with N,0-dimethylhydroxylamine hydrochloride (416 mg, 4.27 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (819 mg, 4.27 mmol), 1-hydroxybenzotriazole (577 mg, 4.27 mmol) and triethylamine (892 L, 6.40 mmol) at room temperature for one day. After addition of water and saturated aqueous sodium chloride, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (hexane / ethyl acetate = 2/1 (v/v)) to give the title compound as a colorless solid (350 mg, yield 26%). REFERENCE SYNTHETIC EXAMPLE 48 Benzyl [trans-4-(7H-pyrrolor2,3-dlpyrimidine-4-carbonyl)cvclohexyl1carbamate The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that benzyl {trans-4- [methoxy(methyl)carbamoyl]cyclohexyl}carbamate was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as a colorless solid (33.0 mg, yield 9.0%). REFERENCE SYNTHETIC EXAMPLE3 49 trans-N-Methoxy-4-(methoxymethyl)-N-methylcvclohexanecarboxamide trans-4-(Hydroxymethyl)-N-methoxy-N-methylcyclohexanecarboxamide (200 mg, 0.994 mmol) obtained in Reference Synthetic Example 3 2 1 in N,N-dimethylformamide (2 mL) was mixed with sodium hydride (55 wt% dispersion in mineral oil, 52.0 mg, 1. 9 mmol) and methyl iodide (74.0 L, 1.19 mmol) under cooling with ice and stirred for 1 hour while the temperature was gradually raised to room temperature. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 1/2 1/1 (v/v)) to give the title compound as a colorless oil (197 mg, yield 92%). REFERENCE SYNTHETIC EXAMPLE 50 [trans-4-(Methoxymethyl)cvclohexyn(7H-pyrrolor2,3-dlpyrimidin-4-yl)methanone The reactions in Reference Synthetic Example3 10 were carried out in substantially the same manners except that trans-N-methoxy-4-(methoxymethyl)-Nmethylcyclohexanecarboxamide was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as an ivory solid (153 mg, yield 70%). REFERENCE SYNTHETIC EXAMPLE3 5 1 trans-4-Hvdroxy-N-methoxy-N-methylcvclohexanecarboxamide The reactions in Reference Synthetic Example3 9 were carried out in substantially the same manners except that trans-4-hydroxycyclohexanecarboxylic acid was used instead of 2-methylbenzoic acid to give the title compound as a colorless oil ( 1 .89 g, yield 48%). REFERENCE SYNTHETIC EXAMPLE 52 trans-N,4-Dimethoxy-N-methylcvclohexanecarboxamide trans-4-Hydroxy-N-methoxy-N-methylcyclohexanecarboxamide (536 mg, 2.86 mmol) in N,N-dimethylformamide (5 mL) was mixed with sodium hydride (55 wt% dispersion in mineral oil, 150 mg, 3.44 mmol) and methyl iodide (214 L, 3.44 mmol) under cooling with ice and stirred for 3 hours while the temperature was gradually raised to room temperature. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 1/2 1/1 (v/v)) to give the title compound as a colorless oil (556 mg, yield 97%). REFERENCE SYNTHETIC EXAMPLE3 53 (trans-4-Methoxycvclohexyl)(7H-pyrrolo[2,3-d1pyrimidin-4-yl)methanone The reactions in Reference Synthetic Example3 10 were carried out in substantially the same manners except that trans-N,4-dimethoxy-Nmethylcyclohexanecarboxamide was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as an ivory solid (178 mg, yield 69%). REFERENCE SYNTHETIC EXAMPLES 54 To 60 The reactions in Reference Synthetic Example 9 were carried out in substantially the same manners except that 4,4-difluoroxyclohexanecarboxylic acid, bicycle[2.2.1]heptane-2-carboxylic acid, cycloheptanecarboxylic acid, cyclobutanecarboxylic acid, cyclopentanecarboxylic acid, trans-4- (trifluoromethyl)cyclohexanecarboxylic acid or cis-4- (trifluoromethyl)cyclohexanecarboxylic acid was used instead of 2-methylbenzoic acid to give the compounds of Reference Synthetic Examples 54 to 60. The names, morphologies and yields of the compounds synthesized are shown in Table3 5. TABLE 5 REFERENCE SYNTHETIC EXAMPLES3 6 1 TO 67 The reactions in Reference Synthetic Example3 0 were carried out in substantially the same manners except that the compounds obtained in Reference Synthetic Examples3 54 to 60 were used instead of N-methoxy-N,2-dimethylbenzamide to give the compounds of Reference Synthetic Examples 6 1 to 67. The names, morphologies and yields of the compounds synthesized are shown in Table3 6. TABLE3 6 REFERENCE SYNTHETIC EXAMPLE 68 ftrans-4-(tert-Butyldiphenylsilyl)oxy1-N-methoxyl-N-methylcvclohexanecarboxamide trans-4-Hydroxy-N-methoxy-N-methylcyclohexanecarboxamide ( 1 .35 g, 7.21 mmol) obtained in Reference Synthetic Example 5 1 in N,N-dimethylformamide (48 ml_) was stirred with imidazole (598 mg, 8.65 mmol) and tert-butylchlorodiphenylsilane (2.07 ml_, 7.93 mmol) for 4 hours under cooling with ice. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 15/1 7/1 3/1 (v/v)) to give the title compound as a colorless oil ( 1 .52 g, yield 50%). REFERENCE SYNTHETIC EXAMPLE 69 (trans-4-[(tert-Butyldiphenylsilyl)oxy1cvclohexyl)(7H-pyrroloi2,3-d1pyrimidin-4- vQmethanone The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that trans-4-[(tert-butyldiphenylsilyl)oxy]-Nmethoxy- N-methylcyclohexanecarboxamide was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as a yellow amorphous ( 1 .34 g, yield 78%). REFERENCE SYNTHETIC EXAMPLE 70 1-(4-i(tert-Butyldiphenylsilyl)oxylcvclohexyl)-7H-pyrrolor3,2-e1f 1,2,31triazoloM ,5- clpyrimidine The reactions in Synthetic Example 5 were carried out in substantially the same manners except that {trans-4-[(tert-butyldiphenylsilyl)oxy]cyclohexyl}(7H-pyrrolo[2,3- d]pyrimidin-4-yl)methanone was used instead of (7H-pyrrolo[2,3-d]pyrimidin-4-yl)(otolyl) methanone to give the title compound as a pale yellow solid (838 mg, yield 61%). REFERENCE SYNTHETIC EXAMPLE 3 7 1 4-Hvdroxy-N-methoxy-N-methylcvclohexanecarboxamide 4-Hydroxycyclohexanecarboxylic acid (10.0 g, 69.4 mmol) and ,- dimethylhydroxylamine hydrochloride (8.80 g, 90.2 mmol) in dichloromethane (500 mL) was stirred with 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (17.3 g , 90.2 mmol), 1-hydroxybenzotriazole (12.2 g, 90.2 mmol) and N,N-diisopropylethylamine (24.2 mL, 139 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v) ethyl acetate) to give the title compound as a yellow oil (9.07 g, yield 70%). REFERENCE SYNTHETIC EXAMPLE 3 72 4-[(tert-Butyldimethylsilyl)oxy1-N-methoxy-N-methylcvclohexanecarboxamide 4-Hydroxy-N-methoxy-N-methylcyclohexanecarboxamide (7.34 g, 39.2 mmol) in N,N-dimethylformamide (200 mL) was stirred with imidazole (4.80 g, 70.6 mmol) and tert-butylchlorodimethylsilane (7.70 g, 5 1.0 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 25/1 4/1 (v/v)) to give the title compound as a colorless oil (8.68 g, yield 73%). REFERENCE SYNTHETIC EXAMPLE 3 73 l4- (tert-Butyldimethylsilyl)oxy1cvclohexyl)(7H-pyrrolor2.3-d1pyrimidin-4-vnmethanone The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that 4-[(tert-butyldimethylsilyl)oxy]-N-methoxy- N-methylcyclohexanecarboxamide was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as a pale yellow solid (7.14 g, yield 69%). REFERENCE SYNTHETIC EXAMPLE 74 1-(4-r(tert-Butyldimethylsilyl)oxy1cvclohexyl)-7H-pyrrolor3,2-ein .2.31triazoloM ,5- clpyrimidine The reactions in Synthetic Example3 5 were carried out in substantially the same manners except that {4-[(tert-butyldiphenylsilyl)oxy]cyclohexyl}(7H-pyrrolo[2,3- d]pyrimidin-4-yl)methanone was used instead of (7H-pyrrolo[2,3-d]pyrimidin-4-yl)(otolyl) methanone to give the title compound as a pale yellow solid (5.20 g , yield 70%). REFERENCE SYNTHETIC EXAMPLE3 75 4-(7H-Pyrrolof3,2-e1M ,2,31triazoloH ,5-c1pyrimidin-1 -vQcvclohexanol 1-{4-[(tert-Butyldimethylsilyl)oxy]cyclohexyl}-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidine (500 mg, 1.35 mmol) in a mixture of dichloromethane (5 mL) and methanol (5 mL) was stirred with pyridinium p-toluenesulfonate (338 mg, 1.35 mmol) at 60°C for 3 hours. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (hexane / ethyl acetate = 4/1 1/1 (v/v) ethyl acetate) to give the title compound as a colorless solid (259 mg, yield 75%). REFERENCE SYNTHETIC EXAMPLE 76 Benzyl 4-(7-(r2-(trimethylsilyl)ethoxy1methyl)-7H-pyrrolor2,3-dlpyrimidine-4- carbonyl)piperidine-1-carboxylate The reactions in Reference Synthetic Example3 18 were carried out in substantially the same manners except that benzyl 4- [methoxy(methyl)carbamoyl]piperidine-1-carboxylate obtained in Reference Synthetic Example 43 was used instead of benzyl 3-[methoxy(methyl)carbamoyl]piperidine-1 - carboxylate to give the title compound as a yellow oil (49.6 mg, yield 71%). REFERENCE SYNTHETIC EXAMPLE 77 Benzyl 4-[amino(7-([2-(trimethylsilyl)ethoxy1methyl)-7H-pyrrolor2,3-d1pyrimidin-4- vDmethyllpiperidine-l -carboxylate The reactions in Reference Synthetic Example3 7 were carried out in substantially the same manners except that benzyl 4-(7-{[2-(trimethylsilyl)ethoxy]methyl}-7Hpyrrolo[ 2,3-d]pyrimidine-4-carbonyl)piperidine-1-carboxylate was used instead of cyclohexyl(7-{[2-(trimethylsilyl)ethoxy]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4- yl)methanone to give the title compound as a colorless oil (33.2 mg, yield 67%). REFERENCE SYNTHETIC EXAMPLE3 78 Benzyl 4-(7-(r2-(trimethylsilyl)ethoxy1methyl|-7H-imidazori ,5-c1pyrrolo[3,2-elpyrimidin-1 - yl)piperidine-1 -carboxylate The reactions in Reference Synthetic Example 20 were carried out in substantially the same manners except that benzyl 4-[amino(7-{[2- (trimethylsilyl)ethoxy]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)methyl]piperidine-1 - caryoxylate was used instead of benzyl 3-[amino(7-{[2-(trimethylsilyl)ethoxy]methy}-7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)methyl]piperidine-1 -carboxylate to give a brown oily mixture containing the title compound (16.0 mg). The resulting mixture was used for the next step without purification. REFERENCE SYNTHETIC EXAMPLE3 79 Benzyl 4-ramino(7H-pyrrolor2,3-dlpyrimidin-4-yl)methyllpiperidine-1 -carboxylate Benzyl 4-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)piperidine-1 -carboxylate (50.0 mg, 0.137 mmol) obtained in Reference Synthetic Example 44 in methanol ( 1 ml_) was stirred with aqueous hydroxylamine (300 _) at 75°C for 4 hours and allowed to cool to room temperature. After addition of water and saturated aqueous ammonium chloride, the reaction mixture was extracted with chloroform. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give a colorless oil. The oil was dissolved in methanol (3 ml_), stirred with zinc powder (45.0 mg, 0.685 mmol) and acetic acid (24.0 , 0.411 mmol) at 75°C for 3 hours and allowed to cool to room temperature. After addition of water and saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with chloroform. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give the title compound as a yellow oil (50.0 mg, yield 99%). REFERENCE SYNTHETIC EXAMPLE 80 Piperidin-4-yl(7H-pyrrolof2,3-dlpyrimidin-4-yl)methanone hydrochloride tert-Butyl 4-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)piperidine-1 -carboxylate (840 mg, 2.54 mmol) obtained in Reference Synthetic Example 39 in 1,4-dioxane (3 ml_) was stirred with 4 M hydrogen chloride-1 ,4-dioxane (3 mL) at room temperature for one day. The resulting solid was collected by filtration to give the title compound as a brown solid (677 mg, yield 99%). REFERENCE SYNTHETIC EXAMPLE3 8 1 (7H-Pyrrolof2,3-d1pyrimidin-4-yl){1-[4-(trifluoromethv0benzvnpiperidin-4-yllmethanone Piperidin-4-yl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)methanone hydrochloride (60.0 mg, 0.224 mmol) in acetonitrile (3 mL) was stirred with 4-(trifluoromethyl)benzyl bromide (70.0 mg, 0.292 mmol) and N,N-diisopropylethylamine (144 , 0.784 mmol) at 60°C for 2 hours and allowed to cool to room temperature. After addition of water and saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a pale yellow solid (65.0 mg, yield 75%). REFERENCE SYNTHETIC EXAMPLE 82 (7H-Pyrrolo[2,3-dlpyrimidin-4-yl)(1-[4-(trifluoromethyl)benzyl1piperidin-4-yl)methanamine The reactions in Reference Synthetic Example 3 79 were carried out in substantially the same manners except that (7H-pyrrolo[2,3-d]pyrimidin-4-yl){1-[4- (trifluoromethyl)benzyl]piperidin-4-yl}methanone was used instead of benzyl 4-(7Hpyrrolo[ 2,3-d]pyrimidine-4-carbonyl)piperidine-1 -carboxylate to give the title compound as a colorless solid (65.0 mg, yield 99%). REFERENCE SYNTHETIC EXAMPLE 83 Benzyl 3-rmethoxy(methyl)carbamovnazetidine-1 -carboxylate The reactions in Reference Synthetic Example 43 were carried out in substantially the same manners except that azetidine-3-carboxylic acid was used instead of piperidine-4-carboxylic acid to give the title compound as a colorless oil ( 1 .18 g, yield 21%). REFERENCE SYNTHETIC EXAMPLE 84 Benzyl 3-(7H-pyrrolor2,3-dlpyrimidine-4-carbonyl)azetidine-1 -carboxylate The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that benzyl 3- [methoxy(methyl)carbamoyl]azetidine-1 -carboxylate was used instead of N-methoxyN, 2-dimethylbenzamide to give the title compound as a yellow solid (656 mg, yield 46%). REFERENCE SYNTHETIC EXAMPLE 85 4-(Hvdroxymethyl)-N-methoxy-N-methylbenzamide 4-(Hydroxymethyl)benzoic acid (3.00 g, 19.7 mmol) and N,0- dimethylhydroxylamine hydrochloride (2.31 g, 23.7 mmol) in chloroform (30 ml_) was stirred with 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (4.54 g, 23.7 mmol), 1-hydroxybenzotriazole (3.20 g, 23.7 mmol) and N,N-diisopropylethylamine (8.04 ml_, 47.3 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure to give a mixture containing the title compound as a colorless oil (4.20 g). The resulting mixture was used for the next step. REFERENCE SYNTHETIC EXAMPLE 86 4-(r(tert-Butyldimethylsilyl)oxylmethyl)-N-methoxy-N-methylbenzamide 4-(Hydroxymethyl)-N-methoxy-N-methylbenzamide (4.20 g) obtained in Reference Synthetic Example 85 in N,N-dimethylformamide ( 10 mL) was stirred with imidazole (4.00 g, 59.2 mmol) and tert-butylchlorodimethylsilane (3.60 g , 23.7 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate =5/1 3/1 (v/v)) to give the title compound as a colorless oil (5.45 g, yield 89% (two steps)). REFERENCE SYNTHETIC EXAMPLE 87 (4-([(tert-Butyldimethylsilyl)oxy1methyl)phenyl)(7H-pyrrolof2,3-dlpyrimidin-4- vQmethanone The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that 4-{[(tert-butyldimethylsilyl)oxy]methyl}-Nmethoxy- N-methylbenzamide was used instead of N-methoxy-N,2-dimethylbenzamide to give the title compound as a pale yellow solid (4.40 g , yield 68%). REFERENCE SYNTHETIC EXAMPLE3 88 1-(4-{r(tert-Butyldimethylsilyl)oxy1methyl)phenyl)-7H-pyrrolor3.2-eiri ,2,31triazolof1,5- clpyrimidine The reactions in Synthetic Example 5 were carried out in substantially the same manners except that (4-{[(tert-butyldimethylsilyl)oxy]methyl}phenyl)(7H-pyrrolo[2,3- d]pyrimidin-4-yl)methanone was used instead of (7H-pyrrolo[2,3-d]pyrimidin-4-yl)(otolyl) methanone to give the title compound as a colorless solid (3.58 g, yield 79%). REFERENCE SYNTHETIC EXAMPLE 89 cis-4-(Hvdroxymethyl)-N-methoxy-N-methylcvclohexanecarboxamide The reactions in Reference Synthetic Example 85 were carried out in substantially the same manners except that cis-4- (hydroxymethyl)cyclohexanecarboxylic acid was used instead of 4- (hydroxymethyl)benzoic acid to give a mixture containing the title compound as a colorless oil (3.17 g). The resulting mixture was used for the next step. REFERENCE SYNTHETIC EXAMPLE3 90 cis-4-(f(tert-Butyldimethylsilyl)oxy1methylj-N-methoxy-Nmethylcyclohexanecarboxamide The reactions in Reference Synthetic Example3 86 were carried out in substantially the same manners except that cis-4-(hydroxymethyl)-N-methoxy-Nmethylcyclohexanecarboxamide obtained in Reference Synthetic Example 89 was used instead of 4-(hydroxymethyl)-N-methoxy-N-methylbenzamide to give the title compound as a colorless oil (5.3 g, yield 89% (two steps)). REFERENCE SYNTHETIC EXAMPLE 9 1 (cis-4-(r(tert-Butyldimethylsilyl)oxylmethyl|cvclohexyl)(7H-pyrroloi2,3-d1pyrimidin-4- vQmethanone The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that cis-4-{[(tert-butyldimethylsilyl)oxy]methyl}- N-methoxy-N-methylcyclohexanecarboxamide was used instead of N-methoxy-N,2- dimethylbenzamide to give the title compound as a pale yellow solid (4.50 g , yield 72%). REFERENCE SYNTHETIC EXAMPLE 92 1-(trans-4-([(tert-Butyldimethylsilyl)oxylmethyl)cvclohexyn-7H-pyrrolo[3,2- e ,2,31triazolof1 ,5-clpyrimidine The reactions in Synthetic Example 5 were carried out in substantially the same manners except that (cis-4-{[(tert-Butyldimethylsilyl)oxy]methyl}cyclohexyl)(7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)methanone was used instead of (7H-pyrrolo[2,3-d]pyrimidin- 4-yl)(o-tolyl)methanone to give the title compound as a pale yellow solid (3.49 g, yield 75%). (although the cis-isomer was used as the starting material, only the transisomer of the title compound was obtained.) REFERENCE SYNTHETIC EXAMPLE3 93 5-(Bromomethyl)thiophene-2-carbonitrile 5-Methylthiophene-2-carbonitrile (500 mg, 4.06 mmol) in carbon tetrachloride (10 mL) was stirred with N-bromosuccinimide (867 mg, 4.87 mmol) and 2,2'- azobis(isobutyronitrile) (133 mg, 0.810 mmol) at 60°C for 4.5 hours and allowed to cool to room temperature. After addition of saturated aqueous sodium thiosulfate, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 2/1 1/1 (v/v)) to give the title compound as a yellow oil (186 mg, yield 23%). REFERENCE SYNTHETIC EXAMPLE 94 4-([4-(7H-pyrroloi2,3-d1pyrimidine-4-carbonyl)piperidin-1-vnmethyl)benzonitrile The reactions in Reference Synthetic Example3 8 1 were carried out in substantially the same manners except that 4-(bromomethyl)benzonitrile was used instead of 4-(trifluoromethyl)benzyl bromide to give the title compound as a pale yellow solid ( 150.9 mg, yield 65%). REFERENCE SYNTHETIC EXAMPLE3 95 4-([4-(7-{[2-(Trimethylsilyl)ethoxy1methyl)-7H-pyrrolor2.3-dlpyrimidine-4- carbonyl)piperidin-1 -yllmethyl)benzonitrile The reactions in Reference Synthetic Example3 15 were carried out in substantially the same manners except that 4-{[4-(7H-pyrrolo[2,3-d]pyrimidine-4- carbonyl)piperidin-1-yl]methyl}benzonitrile was used instead of 4-iodo-7H-pyrrolo[2,3- d]pyrimidine to give the title compound as a yellow oil (124.1 mg, yield 75%). REFERENCE SYNTHETIC EXAMPLE3 96 4-((4-rAmino(7-([2-(trimethylsilvnethoxy1methyl)-7H-pyrrolo[2.3-d1pyrimidin-4- yl)methyl1piperidin-1-yl)methyl)benzonitrile The reactions in Reference Synthetic Example3 7 were carried out in substantially the same manners except that 4-({4-[amino(7-{[2-(trimethylsilyl)ethoxy]methyl}-7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)m was used instead of cyclohexyl(7-{[2-(trimethylsilyl)ethoxy]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4- yl)methanone to give the title compound as a yellow oil (42.9 mg, yield 34%). REFERENCE SYNTHETIC EXAMPLE 97 4-(r4-(7-(r2-(trimethylsilyl)ethoxy1methyl)-7H-imidazori ,5-c1pyrrolof3.2-e1pyrimidin-1- yl)piperidin-1-yl1methyl)benzonitrile The reactions in Reference Synthetic Example 20 were carried out in substantially the same manners except that 4-({4-[amino(7-{[2- (trimethylsilyl)ethoxy]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)methyl]piperidin-1 - yl}methyl)benzonitrile was used instead of benzyl 3-[amino(7-{[2- (trimethylsilyl)ethoxy]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)methyl]piperidine-1 - carboxylate to give a brown oil containing the title compound (37.4 mg). The resulting mixture was used for the next step. REFERENCE SYNTHETIC EXAMPLE 98 Benzyl 3-[methoxy(methyl)carbamoyl1pyrrolidine-1 -carboxylate Triethylamine ( 1 .68 mL, 12.0 mmol) was added dropwise to 1- [(benzyloxy)carbonyl]pyrrolidine-3-carboxylic acid ( 1 .00 g , 4.01 mmol), ,- dimethylhydroxylamine hydrochloride (782 mg, 8.02 mmol), 1-(3-dimethylaminopropyl)- 3-ethylcarbodiimide hydrochloride ( 1 .54 g, 8.02 mmol) and 1-hydroxybenzotriazole ( 1 .08 g, 8.02 mmol) in chloroform (20 mL), and the reaction mixture was stirred at room temperature for 16 hours. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 3/7 (v/v)) to give the title compound as a yellow oil ( 1 .11 g, yield 95%). REFERENCE SYNTHETIC EXAMPLE 99 Benzyl 3-(7H-pyrrolor2,3-d1pyrimidine-4-carbonyl)pyrrolidine-1 -carboxylate The reactions in Reference Synthetic Example 10 were carried out in substantially the same manners except that benzyl 3- [methoxy(methyl)carbamoyl]pyrrolidine-1-carboxylate was used instead of N-methoxy- N,2-dimethylbenzamide to give a pale yellow solid containing the title compound (216 mg). The resulting mixture was used for the next step. REFERENCE SYNTHETIC EXAMPLE3 100 3-Amino-2-(4-chlorophenyl)-1 , 1 ,1-trifluoropropan-2-ol 1-(4-Chlorophenyl)-2,2,2-trifluoroethanone (2.00 g, 9.59 mmol) in nitromethane (10 mL) was stirred with potassium carbonate ( 1 .32 g, 9.59 mmol) at room temperature for 1 hour. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue (pale yellow amorphous, 3.3 g) was dissolved in ethanol (52 mL), then 6 M hydrochloric acid was added dropwise under cooling with ice, and zinc powder (3.13 g, 48.0 mmol) was gradually added. The reaction mixture was stirred for one day while the temperature was gradually raised to room temperature, and filtered through Celite. The filtrate was concentrated under reduced pressure. The residue was mixed with 28 wt% aqueous ammonia and extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/1 1/1 (v/v)) to give the title compound as a colorless solid (609 mg, yield 26%). REFERENCE SYNTHETIC EXAMPLE 101 3-Amino-1 . 1 , 1 -trifluoro-2-phenylpropan-2-ol The reactions in Reference Synthetic Example 100 were carried out in substantially the same manners except that 2,2,2-trifluoro-1-phenylethanone was used instead of 1-(4-chlorophenyl)-2,2,2-trifluoroethanone to give the title compound as a colorless solid (54 mg, yield 46%). REFERENCE SYNTHETIC EXAMPLE 102 3-Amino-1 . ,1-trifluoro-2-(4-fluorophenyl)propan-2-ol n-Butyllithium (2.66 M solution in hexane, 12.4 mL, 33.0 mmol) was added dropwise to 1-bromo-4-f luorobenzene (5.25 g, 30.0 mmol) in tetrahydrofuran (50 mL) cooled to -78°C, and the reaction mixture was stirred at -78°C for 30 minutes, mixed with ethyl 2,2,2-trifluoroacetate (4.64 mL, 45 mmol) at -78°C and then stirred for another 30 minutes while the temperature was gradually raised to room temperature. The reaction mixture was stirred with nitromethane (3.25 mL, 60 mmol) at room temperature for 30 minutes. The resulting reaction mixture was added to 1 M hydrochloric acid (50 mL) and extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 5/1 (v/v/)) to give a colorless oil. The colorless oil was dissolved in ethanol (25 mL) and stirred with 10% palladiumcarbon ( 1 g) at room temperature for one day under a hydrogen atmosphere. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give the title compound as a colorless solid (4.52 g , yield 68% (three steps)). REFERENCE SYNTHETIC EXAMPLE 103 2-f4-(Trifluoromethyl)phenvnoxirane Trimethylsulfonium iodide (4.08 g, 20.0 mmol) in dimethyl sulfoxide (15 mL) was stirred with sodium hydride (55 wt% dispersion in mineral oil, 873 mg, 20.0 mmol) at room temperature for 1 hour and then with 4-(trifluoromethyl)styrene (2.96 g, 7.0 mmol) in dimethyl sulfoxide ( 10 mL) at room temperature for 2 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 9/1 (v/v)) to give the title compound as a colorless oil (2.59 g, yield 81%). REFERENCE SYNTHETIC EXAMPLE 104 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e1f1 .2.3ltriazolof1 ,5-ctoyrimidine acetate 5% Palladium-carbon (0.87 g) was added to benzyl 4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)piperidine-1 -carboxylate (4.88 g , 13.0 mmol) obtained in Synthetic Example3 26 in a mixture of acetic acid (60 mL), water (6 mL) and ethanol (10 mL), and after then the reaction system was flushed with hydrogen, the reaction mixture was stirred at room temperature for one day and then filtered. The filtrate was concentrated, and the resulting yellow solid was washed with ethanol to give the title compound as a colorless solid ( 3.30 g, yield 84%). REFERENCE SYNTHETIC EXAMPLE3 105 2-(4-Formylphenoxy)acetonitrile 4-Hydroxybenzaldehyde (244 mg, 2.00 mmol) in N,N-dimethylformamide (5 mL) was mixed with sodium hydride (60 wt% dispersion in liquid paraffin, 120 mg, 3.00 mmol) and chloroacetonitrile (189 L, 3.00 mmol) under cooling with ice and then stirred at 50°C for 3 hours. The reaction mixture was allowed to cool to room temperature and mixed with saturated aqueous ammonium chloride and extracted with ethyl acetate. The organic layer was washed with 1M aqueous sodium hydroxide, dried over anhydrous sodium sulfate and concentrated under reduced pressure to give the title compound as a brown oil (128 mg, yield 40%). REFERENCE SYNTHETIC EXAMPLE 106 4-(BromomethvQbenzamide 4-(Bromomethyl)benzoic acid (300 mg, 1.40 mmol) in ethyl acetate (5 mL) was stirred with thionyl chloride (249 L, 3.50 mmol) at 75°C for 9 hours. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure. The residue was dissolved in dichloromethane (5 mL) and stirred with 28% ammonia aqueous solution (380 L, 5.60 mmol) under cooling with ice for 80 minutes. The reaction mixture was mixed with water, and the precipitate was collected by filtration, washed with dichloromethane to give the title compound as a colorless solid (274 mg, yield 9 1%). REFERENCE SYNTHETIC EXAMPLE 107 5-(Bromomethyl)-2-(trifluoromethyl)benzonitrile 5-Methyl-2-(trifluoromethyl)benzonitrile (200 mg, .08 mmol) in 1,2-dichloroethane (3 mL) was stirred with N-bromosuccinimide ( 192 mg, 1.08 mmol) and azobisisobutyronitrile (36.1 mg, 0.22 mmol) at 80°C for 2 hours. The reaction mixture allowed to cool to room temperature and was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane ethyl acetate / hexane = 1/3 (v/v)) to give the title compound as a colorless solid (140 mg, yield 49%). REFERENCE SYNTHETIC EXAMPLE 108 4-(Bromomethyl)phthalonitrile The reactions in Reference Synthetic Example 3 107 were carried out in substantially the same manners except that 4-methylphthalonitrile was used instead of 5-methyl-2-(trifluoromethyl)benzonitrile to give the title compound as a colorless solid (163 mg, yield 52%). REFERENCE SYNTHETIC EXAMPLE 3 109 4-(Bromomethyl)-2-(trifluoromethyl)benzonitrile The reactions in Reference Synthetic Example 3 107 were carried out in substantially the same manners except that 4-methyl-2-(trifluoromethyl)benzonitrile was used instead of 5-methyl-2-(trifluoromethyl)benzonitrile to give the title compound as a colorless solid (177 mg, yield 62%). REFERENCE SYNTHETIC EXAMPLE 110 tert-Butyl 4-cvanophenethylcarbamate 2-(4-Bromophenyl)ethylamine (2.00 g, 10.0 mmol) in tetrahydrofuran (5 mL) was mixed with Di-tert-butyl dicarbonate (2.20 g, 10.0 mmol) under cooling with ice and then stirred at room temperature for one day. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue (900 mg) was dissolved in N,N-dimethylformamide (30 mL) and mixed with zinc cyanide (705 mg, 60.0 mmol) and tetrakis(triphenylphosphine)palladium(0) (347 mg, 0.300 mmol), and the reaction mixture was stirred at 150°C for 20 minutes under microwave irradiation. The resulting reaction mixture was allowed to cool to room temperature, mixed with saturated aqueous ammonium chloride and extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 0/1 4/1 (v/v)) to give the title compound as a pale yellow solid (305 mg, yield 41%). REFERENCE SYNTHETIC EXAMPLE 1 11 4-(2-Aminoethyl)benzonitrile tert-Butyl 4-cyanophenethylcarbamate (305 mg, 1.24 mmol) in dichloromethane (4 mL) was mixed with trifluoroacetic acid (3.50 mL, 47.1 mmol) under cooling with ice and then stirred at room temperature for 30 minutes. The reaction mixture was concentrated under reduced pressure, mixed with saturated aqueous potassium carbonate and extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure to give the title compound as a pale orange solid (72.5 mg, yield 40%). REFERENCE SYNTHETIC EXAMPLE 112 tert-Butyl 3-oxoazetidine-1 -carboxylate tert-Butyl 3-hydroxyazetidine-1 -carboxylate (4.02 g, 23.2 mmol) in dichloromethane (305 mL) was mixed with Dess-Martin Periodinane (9.55 g , 22.5 mmol) under cooling with ice and then stirred at room temperature for 3 hours. After addition of 10% aqueous sodium thiosulfate and saturated aqueous sodium hydrogen carbonate under cooling with ice, the reaction mixture was extracted with chloroform, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 2/1 (v/v)) to give the title compound as a colorless solid (3.39 g, yield 85%). REFERENCE SYNTHETIC EXAMPLE 113 tert-Butyl 3-hydroxy-3-methylazetidine-1 -carboxylate Methylmagnesium bromide - tetrahydrofuran solution ( 1 .12 M, 3.90 mL, 4.38 mmol) was added dropwise to tert-butyl 3-oxoazetidine-1 -carboxylate (500 mg, 2.92 mmol) in tetrahydrofuran (5 mL) under cooling with ice and stirred for 90 minutes. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 2/1 1/1 (v/v)) to give the title compound as a colorless solid (224 mg, yield 41%). REFERENCE SYNTHETIC EXAMPLE3 114 3-Methylazetidin-3-ol hydrochloride tert-Butyl 3-hydroxy-3-methylazetidine-1 -carboxylate (224 mg, 1.20 mmol) in ethyl acetate ( 1 mL) was mixed with 4 M hydrogen chloride - 1,4-dioxane solution (3.0 mL) under cooling with ice and then stirred at room temperature for 1 hour. The reaction mixture was concentrated under reduced pressure to give a mixture containing the title compound (colorless oil, 62 mg). The mixture was used for the next step without further purification. REFERENCE SYNTHETIC EXAMPLE3 115 3-(Trifluoromethyl)azetidin-3-ol hydrochloride tert-Butyl 3-oxoazetidine-1 -carboxylate (500 mg, 2.92 mmol) obtained in Reference Synthetic Example 112 and (trifluoromethyl)trimethysilane (0.648 mL, 4.38 mmol) in tetrahydrofuran (10 mL) were mixed with tetrabutylammonium fluoride - tetrahydrofuran solution ( 1 M, 0.291 mL, 0.291 mmol) under cooling with ice and then stirred at room temperature for 1 hour. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with diethyl ether, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was mixed with ethyl acetate (5 mL) and 1M aqueous citric acid (5 mL) and stirred at room temperature for 1 hour. After addition of water, the reaction mixture was extracted with diethyl ether. The organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in ethyl acetate ( 1 .0 mL), mixed with 4 M hydrogen chloride - 1,4-dioxane solution (4 mL) under cooling with ice and then stirred at room temperature for 22 hours. The reaction mixture was concentrated under reduced pressure, and the precipitate was washed with ethyl acetate to give the title compound as a white solid (340 mg, yield 66% (2 steps)). REFERENCE SYNTHETIC EXAMPLE 116 tert-Butyl 3-(2,2,2-trifluoroethoxy)azetidine-1 -carboxylate Sodium hydride (55 wt% dispersion in liquid paraffin, 151 mg, 3.46 mmol) in N,Ndimethylformamide (5 mL) was mixed with tert-butyl 3-hydroxyazetidine-1-carboxylate (500 mg, 2.89 mmol) in N,N-dimethylformamide (3 mL) under cooling with ice and stirred for 30 minutes, and the resulting reaction mixture was mixed with 2,2,2- trifluoroethyl trifluoromethanesulfonate (0.499 mL, 3.46 mmol) under cooling with ice and then stirred at room temperature for 5 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/1 1/1 (v/v)) to give the title compound as a colorless solid (350 mg, yield 48%). REFERENCE SYNTHETIC EXAMPLE 117 3-(2 2,2-Trifluoroethoxy)azetidine hydrochloride tert-Butyl 3-(2,2,2-trifluoroethoxy)azetidine-1 -carboxylate (350 mg, 1.37 mmol) in ethyl acetate ( 1 .0 mL) was mixed with 4 M hydrogen chloride - 1,4-dioxane solution (3.0 mL) under cooling with ice and then stirred at room temperature for 2 hours. The reaction mixture was concentrated to give a mixture containing the title compound as a colorless oil (224 mg). The mixture was used for next step without further purification. REFERENCE SYNTHETIC EXAMPLE3 118 3-Amino-1 , 1 , 1-trifluoro-2-(pyridin-3-yl)propan-2-ol Isopropylmagnesium chloride-lithium chloride complex - tetrahydrofuran solution ( 1 .3 M, 20.7 mL, 27.0 mmol) was added dropwise to 5-bromo-2-chloropyridine (5.20 g, 27.0 mmol) in tetrahydrofuran (40 mL) under cooling with ice, and the reaction mixture was stirred for 30 minutes and then mixed with ethyl 2,2,2-trifluoroacetate (11 .5 g , 8 1.0 mmol) under cooling with ice and stirred at room temperature for 10 minutes. After addition of 1M hydrochloric acid, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give a yellow oil. The yellow oil was dissolved in nitromethane (30 mL) and stirred with potassium carbonate (3.73 g, 27.0 mmol) at room temperature for 30 minutes. The reaction mixture was added to M hydrochloric acid and extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/1 (v/v)) to give a yellow oil. The yellow oil was dissolved in tetrahydrofuran (20 mL), mixed with 10% palladium-carbon (600 mg) and triethylamine (2.60 mL, 18.7 mmol) and then stirred at room temperature for one day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate ethyl acetate / methanol / triethylamine = 9/1/1 (v/v/v)) to give the title compound as a colorless solid (913 mg, yield 31%(4 steps)). REFERENCE SYNTHETIC EXAMPLE 119 3-Amino-1 , 1 ,1-trifluoro-2-r4-(methylthio)phenyl1propan-2-ol The reactions in Reference Synthetic Example 102 were carried out in substantially the same manners except that (4-bromomethyl)(methyl)sulfane was used instead of 1-bromo-4-fluorobenzene to give the title compound as a colorless solid (2.61 g, yield 64%). REFERENCE SYNTHETIC EXAMPLE 3 120 3-Amino-1 , 1 1 -trifluoro-2-(6-methoxypyridin-3-yl)propan-2-ol The reactions in Reference Synthetic Example 3 102 were carried out in substantially the same manners except that 5-bromo-2-methoxypyridine was used instead of 1-bromo-4-fluorobenzene to give the title compound as a colorless solid ( 1 .52 g, yield 76%). REFERENCE SYNTHETIC EXAMPLE 121 3-Amino-1 , 1 , 1 -trifluoro-2-(4-methoxyphenyl)propan-2-ol The reactions in Reference Synthetic Example 3 00 were carried out in substantially the same manners except that 2,2,2-trifluoro-1-(4-methoxyphenyl)etanone was used instead of 1-(4-Chlorophenyl)-2,2,2-trifluoroethanone to give the title compound as a colorless solid (823 mg, yield 36%). REFERENCE SYNTHETIC EXAMPLE 122 3-Amino-2-(3,4-dimethoxyphenyl)-1 , 1 , 1 -trifluoropropan-2-ol The reactions in Synthetic Example 100 were carried out in substantially the same manners except that 1-(3,4-dimethoxyphenyl)-2,2,2-trifluoroetanone was used instead of 1-(4-Chlorophenyl)-2,2,2-trifluoroethanone to give the title compound as a colorless solid (532 mg, yield 39%). REFERENCE SYNTHETIC EXAMPLE 3 123 Ethyl (E)-3-(4-fluorophenyl)acrylate 4-Fluorobenzaldehyde (9.61 g, 80.0 mmol) in tetrahydrofuran (120 mL) was mixed with ethyl 2-(diethoxyphosphoryl)acetate (17.9 g, 80.0 mmol) under cooling with ice, and then sodium ethoxide - ethanol solution (21 wt%, 44.8 mL, 120 mmol) was added dropwise to the reaction mixture under cooling with ice, and the resulting reaction mixture was stirred at room temperature for 2 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 20/1 10/1 (v/v)) to give the title compound as a colorless oil (14.1 g, yield 91%). REFERENCE SYNTHETIC EXAMPLE 3 124 trans-Ethyl 2-(4-fluorophenyl)cvclopropanecarboxylate Trimethylsulfoxonium iodide (7.92 g, 36.0 mmol) in dimethyl sulfoxide (40 mL) was mixed with sodium hydride (55 wt% dispersion in mineral oil, 1.57 g, 36.0 mmol) under cooling with ice, stirred at room temperature for 1 hour and then stirred with (E)-ethyl 3- (4-fluorophenyl)acrylate (5.83 g, 30.0 mmol) for 18 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 10/1) to give the title compound as a colorless oil (793 mg, yield 13%). REFERENCE SYNTHETIC EXAMPLE 125 2-(rtrans-2-(4-Fluorophenvncvclopropynmethyl)isoindoline-1 ,3-dione trans-Ethyl 2-(4-Fluorophenyl)cycloprpane-1-carboxylate (793 mg, 4.57 mmol) in tetrahydrofuran (7 mL) was stirred with lithium aluminium hydride (173 mg, 4.57 mmol) under cooling with ice for 10 minutes. After addition of 1 M aqueous sodium hydroxide, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in tetrahydrofuran (10 mL), mixed with triphenylphosphine (999 mg, 3.81 mmol), isoindoline-1 ,3-dione (560 mg, 3.81 mmol) and azodicarboxylic acid diisopropyl ester - toluene solution ( 1 .9 M, 2.00 mL, 3.81 mmol) under cooling with ice, and the reaction mixture was stirred at room temperature for 1 hour and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 5/1 (v/v)) to give the title compound as a colorless solid (975 mg, yield 87%(2 steps)). REFERENCE SYNTHETIC EXAMPLE 126 ftrans-2-(4-Fluorophenyl)cvclopropyl1methanamine 2-{[trans-2-(4-Fluorophenyl)cyclopropyl]methyl}isoindoline-1 ,3-dione (974 mg, 3.30 mmol) in ethanol (50 mL) was stirred with hydrazine monohydrate (825 mg, 16.5 mmol) at 100°C for 30 minutes. The reaction mixture was concentrated to give the title compound as a colorless oil (360 mg, yield 66%). REFERENCE SYNTHETIC EXAMPLE 3 127 4-Aminoadamantan-1 -ol Concentrated sulfuric acid (35 mL) was mixed with concentrated nitric acid (4.5 mL) and 2-adamanthylamine (5.10 g, 4.57 mmol) under cooling with ice, and the reaction mixture was stirred at room temperature for 2 hours. The reaction mixture was added to ice water and adjusted to pH 0 with 7.5 M aqueous sodium hydroxide. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give the title compound as a yellow solid (2.79 g, yield 61%). REFERENCE SYNTHETIC EXAMPLE 3 128 128a: Benzyl ( 1 R,2s,3S,5s,7s)-5-hvdroxyadamantan-2-vHcarbamate 128b: Benzyl [(1 R,2r,3S,5s,7s)-5-hydroxyadamantan-2-vncarbamate 4-Aminoadamantan-1 -ol (2.57 g, 15.4 mmol) in tetrahydrofuran (25 mL) was mixed with benzyl chloroformate (2.30 mL, 16.1 mmol) and 1 M aqueous sodium hydroxide (16.0 mL, 16.0 mmol) under cooling with ice and then stirred at room temperature for one day. After addition of 10% aqueous potassium hydrogen sulfate, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/2 (v/v)) to give benzyl [(1 R,2S3S,5S,7S)-5- hydroxyadamantan-2-yl]carbamate (Reference Synthetic Example 128a; yellow oil, 1.72 g, yield 37%) in a more polar fraction and benzyl [(1 R,2R,3S,5S,7S)-5- hydroxyadamantan-2-yl]carbamate (Reference Synthetic Example 128b; yellow oil, 2.24 g, yield 48%) in a less polar fraction. REFERENCE SYNTHETIC EXAMPLE 3 129 ( 1s.3R,4s.5S,7s)-4-Aminoadamantan-1 -ol Benzyl [(1 R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl]carbamate (318 mg, 1.05 mmol) obtained in Reference Synthetic Example 128a and 5% palladium-carbon (63 mg) in methanol (2 mL) were stirred at room temperature for one day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give the title compound as a colorless solid (144 mg, yield 82%). REFERENCE SYNTHETIC EXAMPLE3 130 (1s,3R,4r,5S,7s)-4-Aminoadamantan-1-ol Benzyl [(1 R,2r,3S,5s,7s)-5-hydroxyadamantan-2-yl]carbamate (2.24 g , 7.46 mmol) obtained in Reference Synthetic Example 28b and 5% palladium-carbon (700 mg) in methanol (30 mL) were stirred at room temperature for one day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give the title compound as a colorless solid ( 1 .29 g, quantitative yield). REFERENCE SYNTHETIC EXAMPLE 131 2-Bromo-2,2-difluoroethanamine hydrochloride Borane tetrahydrofuran complex - tetrahydrofuran solution ( 1 .06 M, 12.0 mL, 12.6 mmol) was added dropwise to 2-bromo-2,2-difluoroacetamide (2.00 g, 1 1 .5 mmol) in tetrahydrofuran (20 mL) under cooling with ice, and the resulting reaction mixture was stirred at room temperature for 5 hours. After addition of ethanol ( 10 mL) and concentrated hydrochloric acid (7 mL), the reaction mixture was concentrated under reduced pressure. The precipitate was collected by filtration to give the title compound as a colorless solid ( 1 .60 g, yield 71%). REFERENCE SYNTHETIC EXAMPLE 132 4-Cyanophenethyl 4-methylbenzenesulfonate 4-(2-Hydroxyethyl)benzonitrile (200 mg, 1.35 mmol) in tetrahydrofuran (4 mL) was mixed with 4-methylbenzene-1-sulfonyl chloride (389 mg, 2.04 mmol) and triethylamine (569 i , 4.08 mmol) and stirred at room temperature for 1 day. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 9/1 3/1 1/1 (v/v)) to give the title compound as a colorless solid ( 174 mg, yield 43%). REFERENCE SYNTHETIC EXAMPLE 133 4-(r(tert-Butyldimethylsilv0oxy1methyl)-N-methoxy-N-methylcvclohexanecarboxamide 4-(Hydroxymethyl)cyclohexanecarboxic acid (25.0 g, 158 mmol) and ,- dimethylhydroxylamine hydrochloride (23.1 g, 237 mmol) in chloroform (100 mL) were mixed with 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (36.4 g, 190 mmol), -hydroxybenzotriazole (5.00 g, 37.0 mmol) and N,N-diisopropylethylamine (41 .3 mL, 237 mmol) and stirred at room temperature for 1 day. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was dissolved in N,N-dimethylformamide (100 mL) and mixed with imidazole (21 .5 g , 316 mmol) and tert-butylchlorodimethylsilane (26.2 g, 174 mmol). The reaction mixture was stirred at room temperature for 1 day. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 5/1 3/1 (v/v)) to give the title compound as a colorless oil (32.4 g, yield 65%). REFERENCE SYNTHETIC EXAMPLE 134 (4-(f(tert-Butyldimethylsilv0oxy1m vDmethanone Isopropylmagnesium chloride-lithium chloride complex - tetrahydrofuran solution ( 1 .3 M, 39.2 mL, 5 1.0 mmol) was added dropwise to 4-iodo-7H-pyrrolo[2,3-d]pyrimidine (5.00 g, 20.4 mmol) obtained in Reference Synthetic Example3 1 in tetrahydrofuran (50 mL) at -50°C, and stirred at -50°C for 1 hour. The reaction mixture was mixed with 4- {[(tert-butyldimethylsilyl)oxy]methyl}-N-methoxy-N-methylcyclohexanecarboxamide (6.44 g, 20.4 mmol) in tetrahydrofuran (30 mL) at -50°C and then stirred at room temperature for 23 hours. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/1 (v/v)) to give the title compound as a colorless oil (5.14 g , yield 67%). REFERENCE SYNTHETIC EXAMPLE 135 135a: 1-(cis-4-(f(tert-Butyldimethylsilyl)oxy1methyl)cvclohexyl)-7H-pyrrolof3,2- elf 1,2,3ltriazolo[1 ,5-clpyrimidine 135b: 1-(trans-4-([(tert-Butyldimethylsilyl)oxy1methyl)cvclohexyl)-7H-pyrrolo[3.2- e ,2,31triazolof ,5-clpyrimidine (4-{[(tert-Butyldimethylsilyl)oxy]methyl}cyclohexyl)(7H-pyrrolo[2,3-d]pyrimidin-4- yl)methanone (9.23 g, 24.7 mmol) in methanol (200 mL) was mixed with hydrazine monohydrate (38.0 mL, 618 mmol) and then stirred at 80°C for 3 hours. The reaction mixture was allowed to cool to room temperature and mixed with ethyl acetate, washed with water and saturated sodium chloride. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was dissolved in chloroform (240 mL) and mixed with manganese(IV) oxide ( 10.7 g, 124 mmol). The reaction mixture was stirred at 70°C for 1 day. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel chromatography (hexane / ethyl acetate = 3/1 (v/v)) to give 1-(cis-4-{[(tertbutyldimethylsilyl) oxy]methyl)}cyclohexyl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidine (Reference Synthetic Example 135a; pale yellow solid, 670 mg, yield 7%) in a less polar fraction and 1-(trans-4-{[(tert-butyldimethylsilyl)oxy]methyl)}cyclohexyl)- 7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (Reference Synthetic Example 135b; pale yellow solid, 5.02 g, yield 52%) in a more polar fraction. REFERENCE SYNTHETIC EXAMPLE3 136 Cvclopropylamine hydrochloride Cyclopropylamine (0.600 mL, 8.76 mmol) was mixed with 1 M hydrogen chloride - diethylether solution (10 mL) under cooling with ice and stirred for 2 hours. The reaction mixture was concentrated under reduced pressure, and the precipitate was washed with diethyl ether to give the title compound as a colorless solid (686 mg, yield 84%). REFERENCE SYNTHETIC EXAMPLE3 137 tert-Butyl 3-(dimethylamino)azetidine-1 -carboxylate tert-Butyl 3-oxoazetidine-1-carboxylate (300 mg, 1.75 mmol) obtained in Reference Synthetic Example 112 in methanol ( 5 mL) was mixed with acetic acid ( 1 .0 mL), dimethylamine - tetrahydrofuran solution (2.0M, 1.31 mL, 2.63 mmol) and 2- picoline borane (280 mg, 2.63 mmol). The reaction mixture was stirred at room temperature for 1 day. After addition of 1M aqueous hydrogen chloride, the reaction mixture was extracted with ethyl acetate. The aqueous layer was adjusted to pH 0 with 1 M aqueous sodium hydroxide and extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give the title compound as a colorless solid (134 mg, yield 90%). REFERENCE SYNTHETIC EXAMPLE 138 tert-Butyl 3-iethyl(methyl)aminolazetidine-1 -carboxylate The reactions in Reference Synthetic Example 137 were carried out in substantially the same manners except that N-methylethanamine hydrochloride was used instead of dimethylamine - tetrahydrofuran solution to give the title compound as a colorless solid ( 2 1 mg, yield 46%). REFERENCE SYNTHETIC EXAMPLE 139 tert-Butyl 3-(cvanomethylene)azetidine-1 -carboxylate Potassium tert-butoxide (2.03 g, 2 1. 1 mmol) in tetrahydrofuran (20 mL) was mixed with diethyl cyanomethylphosphonate (3.54 g, 20.0 mmol) in tetrahydrofuran (20 mL) under cooling with ice and stirred for 30 minutes. The reaction mixture was mixed with tert-butyl 3-oxoazetidine-1 -carboxylate (2.96 g, 17.3 mmol) obtained in Reference Synthetic Example3 112 in tetrahydrofuran (20 mL) under cooling with ice and then stirred at room temperature for 1 day. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/1 (v/v)) to give the title compound as a colorless solid ( 1 .93 g, yield 58%). REFERENCE SYNTHETIC EXAMPLE 140 3-Hvdroxy-N-methoxy-N-methyladamantane-1-carboxamide 3-Hydroxyadamantane-1 -carboxylic acid (500 mg, 2.55 mmol) in dichloromethane (15 mL) was mixed with 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (587 mg, 3.06 mmol), 1-hydroxybenzotriazole (103 mg, 0.765 mmol), ,- dimethylhydroxylamine hydrochloride (298 mg, 3.06 mmol) and N,Ndiisopropylethylamine ( 1.06 mL, 6.12 mmol) and then stirred at 40°C for 1 hours. The reaction mixture was stirred with 4-dimethylaminopyridine (779 mg, 6.38 mmol) at 40°C for 1 hours. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with chloroform. The organic layer was washed with 1M hydrochloric acid and saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure to give the title compound as a yellow oil (248 mg, yield 41%). REFERENCE SYNTHETIC EXAMPLE 141 3-Hvdroxyadamantan-1 -yl)(7H-pyrrolor2,3-dlpyrimidin-4-yl)methanone Isopropylmagnesium chloride - tetrahydrofuran solution (2.0 M, 0.518 mL, 1.035 mmol) was gradually added dropwise to 4-iodo-7H-pyrrolo[2,3-d]pyrimidine (56.4 mg, 0.230 mmol) in tetrahydrofuran ( 1 mL) cooled to -78°C, and the resulting reaction mixture was stirred at -78°C for 15 minutes. The reaction mixture was mixed with (2,6- dimethylphenyl)magnesium bromide - tetrahydrofuran solution ( 1 .0 M, 0.575 mL, 0.575 mmol) and 3-hydroxy-N-methoxy-N-methyladamantane-1-carboxamide (55.1 mg, 0.23 mmol) in tetrahydrofuran ( 1 mL) and then stirred at room temperature for 1 day. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with water and saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate) to give the title compound as a pale yellow solid (22.5 mg, yield 33%). SYNTHETIC EXAMPLE 1 1-Cvclohexyl-3-methyl-7H-imidazon ,5-clpyrrolof3,2-elpyrimidine Cyclohexyl[7-(triisopropylsilyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]methanone (48.2 mg, 0.120 mmol) obtained in Reference Synthetic Example 4 in acetic acid ( 1 .2 mL) was stirred with ammonium acetate (46.2 mg, 0.600 mmol) and acetaldehyde (purity 90%, 15 , 0.24 mmol) at 110°C for 2.5 hours, and the reaction mixture was allowed to cool to room temperature, basified with saturated aqueous sodium hydrogen carbonate and extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (NH-PLC05 plate manufactured by Fuji Silysia Chemical Ltd.: ethyl acetate) and further purified under the same conditions to give the title compound as a brown solid (12.4 mg, yield 41%). SYNTHETIC EXAMPLE 2 1-Cvclohexyl-7H-imidazof 1,5-clpyrrolo[3,2-elpyrimidine Cyclohexyl[7-(triisopropylsilyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]methanone (52.5 mg, 0.136 mmol) obtained in Reference Synthetic Example 4 in formamide (2 mL) was stirred with formic acid (0.4 mL) at 170°C for 2 hours. The reaction mixture was allowed to cool to room temperature, and after dropwise addition of water, basified with 10 M aqueous sodium hydroxide and extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was stirred with phosphorus oxychloride (2 mL) at 110°C for 4 hours. The reaction mixture was allowed to cool to room temperature, and after dropwise addition of water, basified with 10 M aqueous sodium hydroxide and extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 7/1 (v/v)) and further purified by silica gel thin layer chromatography (NHPLC05 plate manufactured by Fuji Silysia Chemical Ltd.: ethyl acetate) to give the title compound as a brown solid (2.29 mg. yield 7%). SYNTHETIC EXAMPLE 3 3 Benzyl 3-(7H-imidazoH ,5-c1pyrrolof3,2-elpyrimidin-1 -yl)piperidine-1 -carboxylate Benzyl 3-(7-{[2-(trimethylsilyl)ethoxy]methyl}-7H-imidazo[1 ,5-c]pyrrolo[3,2- e]pyrimidin-1-yl)piperidine-1 -carboxylate obtained in Reference Synthetic Example 20 in dichloromethane ( 1 mL) was stirred with trifluoroacetic acid (0.5 mL) at room temperature for .5 hours. The reaction mixture was concentrated under reduced pressure and azeotropically distilled with toluene. The resulting residue was dissolved in a mixture of dichloromethane ( 1 mL) and methanol (0.5 mL) and stirred with ethylenediamine (50 L, 0.75 mmol) and 1 M aqueous sodium hydroxide (0.5 mL, 0.5 mmol) at room temperature for one day. The reaction mixture was diluted with ethyl acetate and washed with saturated aqueous ammonium chloride and saturated aqueous sodium chloride, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 10/1 5/1 (v/v)) to give the title compound as a pale yellow oil ( 17.3 mg, yield 52%). SYNTHETIC EXAMPLE 4 3-r3-(7H-lmidazof 1,5-clpyrrolof3,2-elpyrimidin-1 -yl)piperidin-1 -yll-3-oxopropanenithle Benzyl 3-(7H-imidazo[1 ,5-c]pyrrolo[3,2-e]pyrimidin-1 -yl)piperidine-1 -carboxylate (13.3 mg, 0.0354 mmol) and 10% palladium hydroxide-carbon (small amount) in ethanol ( 1 .5 mL) was stirred at room temperature for 2.5 hours under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The resulting residue was dissolved in N,N-dimethylformamide ( 1 mL) and stirred with 2-cyanoacetic acid (5.0 mg, 0.054 mmol), 0-(7-azabenzotriazol-1-yl)- ,,' ,'-tetramethyluronium hexafluorophosphate (27.5 mg, 0.0722 mmol) and N,Ndiisopropylethylamine (19.0 , 0.11 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (NH-PLC05 plate manufactured by Fuji Silysia Chemical Ltd.: chloroform / methanol =15/1 (v/v)) to give the title compound as a pale yellow oil ( .02 mg, yield 11%). SYNTHETIC EXAMPLE 5 1-o-Tolyl-7H-pyrrolo[3,2-e1f1 ,2,3ltriazolof1 ,5-clpyrimidine (7H-Pyrrolo[2,3-d]pyrimidin-4-yl)(o-tolyl)methanone (50.0 mg, 0.211 mmol) obtained in Reference Synthetic Example 10 in methanol ( 1 ml) was stirred with hydrazine monohydrate (295 ί , 9.48 mmol) at 75°C for 7 hours. After addition of water and 1 M aqueous sodium hydroxide, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue (pale yellow amorphous, 60.3 mg) was dissolved in chloroform (4 mL) and stirred with manganese dioxide (91 .6 mg, 1.05 mmol) at 75°C for 6 hours. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 4/1 1/1 (v/v)) to give the title compound as a white solid (21 .5 mg, yield 41%). SYNTHETIC EXAMPLE 6 1-Cvclohexyl-7H-pyrrolo[3,2-e1f1 ,2,31triazolof1,5-clpyrimidine The reactions in Synthetic Example 5 were carried out in substantially the same manners except that cyclohexyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)methanone obtained in Reference Synthetic Example 1 was used instead of (7H-pyrrolo[2,3-d]pyrimidin-4- yl)(o-tolyl)methanone to give the title compound as a pale yellow solid (76.6 mg, yield 73%). SYNTHETIC EXAMPLE 3 7 1-(2-Methylcvclohexyl)-7H-pyrrolor3,2 -ei ,2,31triazolon ,5-clpyrimidine The reactions in Synthetic Example 5 were carried out in substantially the same manners except that (2-methylcyclohexyl)(7H-pyrrolo[2,3-d]pyrimidin-4-yl)methanone obtained in Reference Synthetic Example 3 14 was used instead of (7H-pyrrolo[2,3- d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a pale yellow amorphous (16.9 mg, yield 32%). SYNTHETIC EXAMPLE 3 8 1-Cvclohexyl-2H-imidazof1 ,5-c1pyrrolof3,2-elpyrimidine-3(7H)-thione Cyclohexyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)methanone (50 mg, 0.22 mmol) obtained in Reference Synthetic Example 3 12 in methanol ( 1 mL) was stirred with hydroxylamine (50 wt% aq., 735 , 12.0 mmol) at 75°C for 6 hours. After addition of water and 1 M aqueous sodium hydroxide, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue (colorless oil, 53.0 mg) was dissolved in methanol (3 mL) and stirred with zinc (128 mg, 1.96 mmol) and acetic acid (37.5 _, 0.654 mmol) at 75°C for 7 hours, and the reaction mixture was filtered. Chloroform and saturated aqueous sodium hydrogen carbonate were added to the filtrate, and the precipitate was separated by filtration. The filtrate was extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue (pale yellow oil, 23.7 mg) was dissolved in methanol ( 1 mL) and stirred with carbon disulfide (62.0 L, .03 mmol) and triethylamine (43.0 L, 0.309 mmol) at 75°C for 2 hours. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 10/1 (v/v)) to give the title compound as a yellow solid (22.6 mg, yield 38%). SYNTHETIC EXAMPLE 9 1-Cvclohexyl-2H-imidazof1 ,5-clpyrrolof3,2-elpyrimidin-3(7H)-one Cyclohexyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)methanone ( 100 mg, 0.436 mmol) obtained in Reference Synthetic Example 12 in methanol (2 mL) was stirred with hydroxylamine (50 wt% aq., 1.34 mL, 2 1.8 mmol) at 75°C for 5 hours. After addition of water and 1 M aqueous sodium hydroxide, the reaction mixture was extracted with chloroform. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue (colorless oil, 110 mg) was dissolved in methanol (3 mL) and stirred with zinc (258 mg, 3.93 mmol) and acetic acid (75.0 pL, 1.31 mmol) at 70°C for 7.5 hours, and the reaction mixture was filtered. Chloroform and saturated aqueous sodium hydrogen carbonate were added to the filtrate, and the precipitate was separated by filtration. The filtrate was extracted with dichloromethane, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue (pale yellow amorphous, 57.5 mg) was dissolved in chloroform ( 1 mL) and stirred with triphosgene (29.6 mg, 0.0999 mmol) at room temperature for 3 hours. After addition of methanol, the reaction mixture was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 10/1 (v/v)) to give the title compound as a yellow solid (6.0 mg, yield 5.4%). SYNTHETIC EXAMPLE 10 ftrans-4-(7H-Pyrrolof3,2-e1f 1,2,31triazoloH ,5-clpyrimidin-1 -vDcvclohexynmethanol 1-{trans-4-[(tert-Butyldiphenylsilyloxy)methyl]cyclohexyl}-7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (48.0 mg, 0.0942 mmol) obtained in Reference Synthetic Example 24 in tetrahydrofuran (3 mL) was cooled with ice and stirred with tetrabutylammonium fluoride ( 1 .0 M solution in tetrahydrofuran, 104 pL, 0.104 mmol) for 4 hours while the temperature was gradually raised to room temperature. After addition of water, the reaction solution was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 10/1 (v/v)) to give the title compound as a pale yellow solid (25.3 mg, yield 99%). SYNTHETIC EXAMPLE 11 tert-Butyl 4-methyl-3-(7H-pyrrolo[3.2-e1M ,2.31triazolo[1 ,5-c1pyrimidin-1 -yl)piperidine-1 - carboxylate The reactions in Synthetic Example 5 were carried out in substantially the same manners except that tert-butyl 4-methyl-3-(7H-pyrrolo[2,3-d]pyrimidine-4- carbonyl)piperidine-1 -carboxylate obtained in Reference Synthetic Example 27 was used instead of (7H- pyrrolo[2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a pale yellow solid ( .0 mg, yield 1.3%). SYNTHETIC EXAMPLE 12 3-r4-Methyl-3-(7H-pyrrolor3,2-e1f 1,2,31triazoloM .5-clpyrimidin-1 -vhpiperidin-1 -yl1-3- oxopropanenitrile tert-Butyl 4-methyl-3-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)piperidine-1 -carboxylate (5.6 mg, 0.016 mmol) in 4 M hydrogen chloride - 1,4-dioxane solution ( 1 .0 mL) was stirred under cooling with ice for 1 hour and concentrated under reduced pressure. The residue was dissolved in N,N-dimethylformamide ( 1 mL) and mixed with 2-cyanoacetic acid (2.7 mg, 0.0314 mmol) and 0-(7-azabenzotriazol-1 -yl)- ,,' ,'-tetramethyluronium hexafluorophosphate (11 .9 mg, 0.0314 mmol) and then with N,N-diisopylethylamine (0.0082 mL, 0.0471 mmol) and stirred at room temperature for 2 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (NH-PLC05 plate manufactured by Fuji Silysia Chemical Ltd.: chloroform / methanol =15/1 (v/v)) and further purified by silica gel thin layer chromatography (ethyl acetate) to give the title compound as a pale yellow solid (0.62 mg, yield 12%). SYNTHETIC EXAMPLE 3 13 tert-Butyl 3-(7H-pyrrolo[3,2-elf1 ,2,31triazoloH ,5-c1pyrimidin-1-yl)piperidine-1 -carboxylate The reactions in Synthetic Example 5 were carried out in substantially the same manners except that tert-butyl 3-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)piperidine-1 - carboxylate obtained in Reference Synthetic Example 29 was used instead of (7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a pale yellow oil (48.2 mg, yield 47%). SYNTHETIC EXAMPLE 3 14 Benzyl 3-(7H-pyrrolof3.2-ein ,2.31triazolori ,5-c1pyrimidin-1 -yl)piperidine-1 -carboxylate The reactions in Synthetic Example 5 were carried out in substantially the same manners except that benzyl 3-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)piperidine-1- carboxylate obtained in Reference Synthetic Example 3 32 was used instead of (7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a pale yellow solid (185 mg, yield 85%). SYNTHETIC EXAMPLE 3 5 1-(Piperidin-3-yl)-7H-pyrroloi3.2-ein ,2,31triazoloH ,5-clpyrimidine Benzyl 3-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)piperidine-1 - carboxylate (25.0 mg, 0.0664 mmol) in ethanol was stirred with 5% palladium-carbon (10 mg) under a hydrogen atmosphere at 50°C for 2.5 hours. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give the title compound as a light brown solid (16.1 mg, yield quantitative). SYNTHETIC EXAMPLE 16 1-(1 -Benzylpiperidin-3-yl)-7H-pyrrolof3,2-e1[1 ,2,31triazolori ,5-clpyrimidine The reactions in Synthetic Example 5 were carried out in substantially the same manners except that (1-benzylpiperidin-3-yl)(7H-pyrrolo[2,3-d]pyrimidin-4-yl)methanone obtained in Reference Synthetic Example 35 was used instead of (7H-pyrrolo[2,3- d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a pale yellow solid (2.6 mg, yield 2.5%). SYNTHETIC EXAMPLE 17 1- 3-(7H-Pyrrolo 3 2-e r1,2,31triazolori ,5-c1pyrimidin-1 -yl)piperidin-1 -yll-3,3,3- trifluoropropan-1 -one 1-(Piperidin-3-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (20.0 mg., 0.0825 mmol) obtained in Synthetic Example 15 in N,N-dimethylformamide ( 1 .5 ml_) was mixed with 3,3,3-trifluoropropanoic acid (8.6 _, 0.099 mmol) and 0-(7- azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate (62.7 mg, 0.1 65 mmol) and then with N,N-diisopropylethylamine (0.0431 ml, 0.248 mmol) and stirred at room temperature for one day. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 1/2 (v/v) ethyl acetate) to give the title compound as a colorless solid (7.3 mg, yield 25%). SYNTHETIC EXAMPLE 18 1- 1-(Pyridin-S-ylmethvDpiperidin-S-yll^H-pyrrolofS -ei i ,2,31triazolo[1 ,5-clpyrimidine 1-(Piperidin-3-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (21 .9 mg, 0.0903 mmol) obtained in Synthetic Example 3 15 in methanol ( 1 .5 mL) was stirred with 3- pyridinecarboxyaldehyde (12.7 , 0.135 mmol) at 50°C for 1.5 hours, then with a small amount of acetic acid at room temperature for 2 hours and with sodium triacetoxyborohydride (28.6 mg, 0.135 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 15/1 (v/v)) and then by silica gel thin layer chromatography (NH-PLC05 plate manufactured by Fuji Silysia Chemical Ltd.: ethyl acetate) to give the title compound as a colorless solid (5.8 mg, yield 19%). SYNTHETIC EXAMPLE 3 19 5-(f3-(7H-Pyrrolor3,2 -ei ,2,31triazolof 1,5-c1pyrimidin-1 -yl)-piperidin-1 -yllmethvPthiazole The reactions in Synthetic Example 18 were carried out in substantially the same manners except that thiazole-5-carbaldehyde was used instead of 3- pyridinecarboxyaldehyde to give the title compound as a colorless solid (3.4 mg, yield 12%). SYNTHETIC EXAMPLE 20 3-(7H-Pyrrolor3,2 -eiri ,2.31triazoloM ,5-clpyrimidin-1 -y l -N- 1,3.4-thiadiazol-2- yl)piperidine-1 -carboxamide 1-(Piperidin-3-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (22.1 mg, 0.0912 mmol) obtained in Synthetic Example 15 in tetrahydrofuran ( 1 .5 mL) was stirred with phenyl 1,3,4-thiadiazol-2-ylcarbamate (24.1 mg, 0.109 mmol) obtained in Reference Synthetic Example 3 36 and triethylamine (0.0191 mg, 0.137 mmol) at 60°C for 1.5 hours and then stirred at room temperature for one day. The precipitate in the reaction mixture was washed with ethyl acetate, methanol and tetrahydrofuran, and the solid was dried under reduced pressure to give the title compound as a light brown solid (2.4 mg, yield 7%). SYNTHETIC EXAMPLE 3 2 1 N-(3-Methylisothiazol-5 -vn-3-(7H-pyrrolor3,2-eiri ,2.31triazoloM ,5-c1pyrimidin-1 - yl)piperidine-1 -carboxamide 1-(Piperidin-3-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (23.2 mg., 0.0957 mmol) obtained in Synthetic Example 15 in tetrahydrofuran ( 1 .5 mL) was stirred with phenyl (3-methylisothiazol-5-yl)carbamate (26.9 mg, 0.115 mmol) obtained in Reference Synthetic Example 37 and triethylamine (0.0201 mL, 0.144 mmol) at 60°C for 1.5 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 7/1 (v/v)), and the resulting solid was washed with ethyl acetate, methanol and tetrahydrofuran to give the title compound as a light brown solid (3.0 mg, yield 8.3%). SYNTHETIC EXAMPLE 3 22 4-(i3-(7H-Pyrrolor3,2-e1M ,2,31triazoloM ,5-clpyrimidin-1 -yl)piperidin-1 - yllmethvPbenzonitrile 1-(Piperidin-3-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (29.4 mg., 0.121 mmol) obtained in Synthetic Example 3 15 in acetonitrile ( 1 .5 mL) was stirred with 4- (bromomethyl)benzonitrile (31 .0 mg, 0.168 mmol) and N,N-diisopropylethylamine (0.0317 mL, 0.182 mmol) at 60°C for 2 hours. The reaction mixture was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: hexane / ethyl acetate = 1/1 (v/v) ethyl acetate) to give the title compound as a colorless solid (24.9 mg, yield 58%). SYNTHETIC EXAMPLE 23 1-(1 - 4 -(Trifluoromethyl)benzyl1piperidin-3-yl)-7H-pyrrolo[3,2-e1[1 ,2,31triazoloH .5- clpyrimidine The reactions in Synthetic Example 22 were carried out in substantially the same manners except that 1-(bromomethyl)-4-(trifluoromethyl)benzene was used instead of 4- (bromomethyl)benzonitrile to give the title compound as a light brown solid (30.9 mg, yield 68%). SYNTHETIC EXAMPLE 24 tert-Butyl 4-(7H-pyrrolo[3,2-e1[1 ,2,31triazolori ,5-c1pyrimidin-1-yl)piperidine-1 -carboxylate The reactions in Synthetic Example 3 5 were carried out in substantially the same manners except that tert-butyl 4-(7H-pyrrolo[2,3-d]pyrimidin-4-carbonyl)piperidine-1- carboxylate obtained in Reference Synthetic Example 3 39 was used instead of (7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a pale yellow solid ( 157 mg, yield 69%). SYNTHETIC EXAMPLE 3 25 1- -(2,2,2-Trifluoroethyl)piperidin-4-yl1-7H-pyrrolor3,2 -eiri ,2,31triazoloi1 ,5-clpyrimidine The reactions in Synthetic Example 3 5 were carried out in substantially the same manners except that (7H-pyrrolo[2,3-d]pyrimidin-4-yl)[1 -(2,2,2-trifluoroethyl)piperidin-4- yljmethanone obtained in Reference Synthetic Example 42 was used instead of (7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a pale yellow solid (6.6 mg, yield 12%). SYNTHETIC EXAMPLE 26 Benzyl 4-(7H-pyrrolof3.2-e1H ,2,31triazoloM ,5-c1pyrimidin-1 -yl)piperidine-1 -carboxylate The reactions in Synthetic Example 5 were carried out in substantially the same manners except that benzyl 4-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)piperidine-1- carboxylate obtained in Reference Synthetic Example 44 was used instead of (7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a colorless solid (49.6 mg, yield 34%). SYNTHETIC EXAMPLE 27 1-(Piperidin-4-yl)-7H-pyrrolof3,2-e1f 1,2,31triazolof1,5-clpyrimidine 5% Palladium-carbon ( 10.0 mg) was added to benzyl 4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)piperidine-1 -carboxylate (30.0 mg, 0.0800 mmol) in methanol (2 mL) under an argon atmosphere, and after the reaction system was flushed with hydrogen, the reaction mixture was stirred at room temperature for 6 hours and then filtered. The filtrate was concentrated under reduced pressure. The resulting yellow solid was washed with methanol and collected by filtration to give the title compound as a pale yellow solid (5.0 mg, yield 26%). SYNTHETIC EXAMPLE 28 1- -(Pyridin-3-ylmethyl)piperidin-4-yll-7H-pyrrolo[3.2-e1f 1,2,3ltriazoloi1 ,5-clpyrimidine 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (11 .0 mg, 0.0450 mmol) in a mixture of methanol ( 1 mL) and tetrahydrofuran ( 1 mL) was stirred with 3- pyridinecarboxyaldehyde (5.0 pL, 0.054 mmol), acetic acid (33 pL) and sodium cyanoborohydride (4.3 mg, 0.068 mmol) at room temperature for one day. The reaction mixture was stirred with sodium triacetoxyborohydride (10.0 mg, 0.047 mmol) for another 2 hours. The resulting reaction mixture was purified by silica gel thin layer chromatography (methanol / chloroform = 1/9 (v/v)) twice to give the title compound as a colorless solid ( 1 .4 mg, yield 9.3%). SYNTHETIC EXAMPLE 29 1-4-(7->3,2- 11,2,31triazoloi1 ,5-clpyrimidin-1 -yl)piperidin-1 -yll-3.3.3- trifluoropropan-1 -one 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine acetate (30.0 mg, 0.0992 mmol) obtained in Reference Synthetic Example3 104 in N,N-dimethylformamide ( 1 mL) was stirred with 3,3,3-trifluoropropionic acid (14.0 pL, 0.1 6 1 mmol), 1-(3- dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (48.0 mg, 0.248 mmol), 1- hydroxybenzotriazole (34.0 mg, 0.248 mmol) and triethylamine (43.0 L, 0.310 mmol) at room temperature for 3 hours and then with water ( 1 mL) for another 1 day. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 2/1 (v/v)) to give the title compound as a colorless solid (11 .7 mg, yield 34%). SYNTHETIC EXAMPLE 30 4-(7H-Pyrrolor3,2 -ei .2.31triazolori .5-clpyrimidin-1 -yl)-N-(1 .3,4-thiadiazol-2- yl)piperidine-1 -carboxamide 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine acetate (25.0 mg, 0.0827 mmol) obtained in Reference Synthetic Example3 104 in tetrahydrofuran ( 1 mL) was stirred with phenyl 1,3,4-thiadiazol-2-ylcarbamate (27.0 mg, 0.124 mmol) obtained in Reference Synthetic Example3 36 and triethylamine (22.0 pL, 0.155 mmol) at room temperature for 2 hours. Water and ethyl acetate were added to the reaction mixture, and the insolubles were collected by filtration. The resulting solid was washed with methanol, chloroform, acetonitrile and ethanol to give the title compound as a colorless solid (19.3 mg, yield 63%). SYNTHETIC EXAMPLE3 3 1 N-(3-Methylisothiazol-5 -vn-4-(7H-pyrrolo[3.2-ein ,2.31triazolof1 ,5-clPyrimidin-1 - yl)piperidine-1 -carboxamide The reactions Synthetic Example 30 were carried out in substantially the same manners except that phenyl (3-methylisothiazol-5-yl)carbamate obtained in Reference Synthetic Example 37 was used instead of phenyl 1,3,4-thiadiazol-2-ylcarbamate to give the title compound as a pale yellow solid (17.6 mg, yield 56%). SYNTHETIC EXAMPLE 32 1-(1 -Benzylpiperidin-4-yl)-7H-pyrroloi3,2 -e i .2,31triazolof 1,5-clpyrimidine 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine acetate (20.0 mg, 0.0662 mmol) obtained in Reference Synthetic Example 3 104 in acetonitrile ( 1 mL) was stirred with benzyl bromide ( 15.0 L, 0.124 mmol) and ,-diisopropylethylamine (28.0 L, 0.166 mmol) at 60°C for 2 hours. The reaction mixture was purified by silica gel column chromatography (methanol / chloroform = 1/30 1/25 (v/v)), and the resulting solid was washed with isopropyl ether to give the title compound as a colorless solid (2.92 mg, yield 13%). SYNTHETIC EXAMPLES 33 TO 43 The reactions in Synthetic Example 32 were carried out in substantially the same manners except that 4-(trifluoromethyl)benzyl bromide, 4-cyanobenzyl bromide, 3- cyanobenzyl bromide, 4-(chloromethyl)-3,5-dimethylisoxazole, 4- (trifluoromethoxy)benzyl bromide, 4-(trifluoromethylthio)benzyl bromide, 3- (trifluoromethyl)benzyl bromide, 4-(bromomethyl)-3-fluorobenzonitrile, 1-bromo-4- (bromomethyl)benzene, 1-(2-bromoethyl)-4-(trifluoromethyl)benzene or 4-fluorobenzyl bromide was used instead of benzyl bromide to give the compounds of Synthetic Examples a 33 to 43. The names, morphologies and yields of the synthesized compounds are shown in Table3 7 . TABLE 7 SYNTHETIC EXAMPLE 44 5-if4-(7H-Pyrrolor3,2-e1f 1,2,31triazolo[1 ,5-clpyrimidin-1 -yl)piperidin-1 -vnmethvDthiazole 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2 3]triazolo[1 ,5-c]pyrimidine acetate (20.0 mg, 0.0662 mmol) obtained in Reference Synthetic Example3 104 in methanol ( 1 mL) was stirred with thiazole-5-carbaldehyde (11 .0 , 0.124 mmol), acetic acid (100 ) and 2- picoline borane (13.0 mg, 0.124 mmol) at room temperature for one day. The reaction mixture was purified by silica gel column chromatography (methanol / chloroform = 1/30 1/25 1/20 (v/v)). The resulting solid was washed with isopropyl ether to give the title compound as a colorless solid (9.05 mg, yield 40%). SYNTHETIC EXAMPLES 45 TO 55 The reactions in Synthetic Example 44 were carried out in substantially the same manners except that 3-phenylpropionaldehyde, 3-fluoro-4-methoxybenzaldehyde, 3,5- bis(trifluoromethyl)benzaldehyde, 2-formylthiazole, 5-chlorothiophene-2-carboxaldehyde, cyclohexanecarboxaldehyde, cyclopentanone, 6-(trifluoromethyl)-3- pyridinecarboxaldehyde, 3,5-difluoro-4-formylbenzonitrile, 4-chlorobenzaldehyde or 3- fluorobenzaldehyde was used instead of thiazole-5-carbaldehyde to give the compounds of Synthetic Examples 45 to 55. The names, morphologies and yields of the compounds synthesized are shown in Table 8. TABLE3 8 SYNTHETIC EXAMPLE3 56 1-(1 -r4 -(Trifluoromethyl)cvclohexyllpiperidin-4-yl)-7H-pyrrolo[3,2-el[1 ,2.31triazolo[1 ,5- clpyrimidine The reactions in Synthetic Example 44 were carried out in substantially the same manners except that 4-(trifluoromethyl)cyclohexanone was used instead of thiazole-5- carbaldehyde to give an isomer mixture as a pale yellow solid. The isomer mixture was purified by silica gel thin layer chromatography (methanol / chloroform = 1/9 (v/v)) to give the two isomers of the title compound in a less polar fraction (Synthetic Example 56a; pale yellow solid, 5.6 mg, yield 22%) and in a more polar fraction (Synthetic Example3 56b; pale yellow solid, 4.9 mg, yield 19%). SYNTHETIC EXAMPLE3 57 4-(7H-Pyrrolor3,2-e1f1,2,31triazolon .5-clpyrimidin-1 ---3- (trifluoromethyl)phenyllpiperidine-l -carboxamide 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine acetate (20.0 mg, 0.0662 mmol) obtained in Reference Synthetic Example 104 in tetrahydrofuran ( 1 ml_) was stirred with 3-(trifluoromethyl)phenyl isocyanate (14.0 _, 0.0990 mmol) and triethylamine (14.0 , 0.0990 mmol) at room temperature for 3 days. The reaction mixture was purified by silica gel thin layer chromatography (methanol / chloroform = 1/9 (v/v)) to give the title compound as a light gray solid (7.5 mg, yield 27%). SYNTHETIC EXAMPLE 58 i4-(7H-Pyrrolo[3,2-e1[1 ,2,31triazolori ,5-c1pyrimidin-1 -yl)piperidin-1 -yll[4- (trifluoromethyl)phenvnmethanone 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine acetate (20.0 mg, 0.0662 mmol) obtained in Reference Synthetic Example 104 in N,N-dimethylformamide ( 1 ml_) was stirred with 4-(trifluoromethyl)benzoyl chloride (14.8 L, 0.100 mmol) and triethylamine (13.9 _, 0.100 mmol) under cooling with ice for 80 minutes. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (methanol / chloroform = 1/19 (v/v)) to give the title compound as a colorless oil (16.3 mg, yield 59%). SYNTHETIC EXAMPLE 59 tert-Butyl ftrans-4-(7H-pyrrolor3,2-e1f1 .2,31triazolof1 ,5-c1pyrimidin-1- vDcyclohexyllcarbamate The reactions in Synthetic Example 5 were carried out in substantially the same manners except that tert-butyl [trans-4-(7H-pyrrolo[2,3-d]pyrimidine-4- carbonyl)cyclohexyl]carbamate obtained in Reference Synthetic Example3 46 was used instead of (7H-pyrrolo[2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a colorless solid (4.7 mg, yield 15%). SYNTHETIC EXAMPLE3 60 Benzyl [trans-4-(7H-pyrrolo[3,2-eiri ,2,3ltriazolo[1 ,5-clpyrimidin-1- vPcvclohexyHcarbamate The reactions in Synthetic Example3 5 were carried out in substantially the same manners except that benzyl [trans-4-(7H-pyrrolo[2,3-d]pyrimidine-4- carbonyl)cyclohexyl]carbamate obtained in Reference Synthetic Example 48 was used instead of (7H-pyrrolo[2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a colorless solid ( 10.0 mg, yield 29%). SYNTHETIC EXAMPLE 6 1 trans-4-(7H-Pyrrolof3,2-e1[1 ,2,31triazolof1,5-clpyrimidin-1 -ypcyclohexanamine 5% Palladium-carbon (5.00 mg) was added to benzyl [trans-4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexyl]carbamate (7.00 mg, 0.0180 mmol) in a mixture of ethanol ( 1 mL) and chloroform ( 1 mL) under an argon atmosphere, and after the reaction system was flushed with hydrogen, the reaction mixture was stirred at room temperature for one day and then filtered. The filtrate was concentrated under reduced pressure. The resulting residue was purified by silica gel thin layer chromatography (NH-PLC05 plate manufactured by Fuji Silysia Chemical Ltd.:methanol /chloroform = 1/19 (v/v)) to give the title compound as a colorless solid (0.35 mg, yield 8.0%). SYNTHETIC EXAMPLE 62 1-ftrans-4-(Methoxymethyl)cvclohexyll-7H-pyrrolof3,2-e1f 1,2,31triazolof1,5-clpyrimidine The reactions in Synthetic Example3 5 were carried out in substantially the same manners except that [trans-4-(methoxymethyl)cyclohexyl](7H-pyrrolo[2,3-d]pyrimidin-4- yl)methanone obtained in Reference Synthetic Example 50 was used instead of (7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a colorless solid (52.4 mg, yield 63%). SYNTHETIC EXAMPLE 63 1-[trans-4-Methoxycvclohexyn-7H-pyrrolo[3,2-e1[1 ,2.31triazoloM ,5-clpyrimidine The reactions in Synthetic Example 5 were carried out in substantially the same manners except that (trans-4-methoxycyclohexyl)(7H-pyrrolo[2,3-d]pyrimidin-4- yl)methanone obtained in Reference Synthetic Example 3 53 was used instead of (7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a pale yellow solid (7.80 mg, yield 7.6%). SYNTHETIC EXAMPLES 3 64 TO 69 The reactions in Synthetic Example 5 were carried out in substantially the same manners except that the compounds obtained in Reference Synthetic Examples 6 1 to 66 were used instead of (7H-pyrrolo[2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compounds of Synthetic Examples 3 64 to 69. The names, morphologies and yields of the compounds synthesized are shown in Table 9 . TABLE 9 SYNTHETIC EXAMPLE 3 70 1-ftrans-4-(Trifluoromethyl)cyclohexyn-7H-pyrrolor3,2-e1f ,2,31triazolof1,5-clpyrimidine The reactions in Synthetic Example 3 5 were carried out in substantially the same manners except that (7H-pyrrolo[2,3-d]pyrimidin-4-yl)[cis-4- (trifluoromethyl)cyclohexyl]methanone obtained in Reference Synthetic Example 3 67 was used instead of (7H-pyrrolo[2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a colorless solid (12.0 mg, yield 23%). (although the cis-isomer was used as the starting material, only the trans-isomer of the title compound was obtained.) SYNTHETIC EXAMPLE 7 1 S-(rtrans-4-(7H-Pyrrolof3,2 -eiri .2.3¾riazoloH ,5-clpyrimidin-1 -vOcvclohexyllmethyl) ethanethioate Triphenylphosphine (58.0 mg, 0.221 mmol) in tetrahydrofuran ( 1 mL) was mixed with diisopropyl azodicarboxylate (116 pL, 0.428 mmol) and [trans-4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexyl]methanol (30.0 mg, 0.111 mmol) obtained in Synthetic Example 10 and thioacetic acid (16.0 pL, 0.225 mmol) under cooling with ice, and stirred for 30 minutes while the temperature was gradually raised to room temperature. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 1/10 1/3 (v/v)) to give the title compound as a colorless solid (22.4 mg, yield 62%). SYNTHETIC EXAMPLE 72 ftrans-4-(7H-Pyrrolor3.2 -ei ,2,31triazoloi1 ,5-c1pyrimidin-1 -vQcvclohexynmethyl acetate The reactions in Synthetic Example 7 1 were carried out in substantially the same manners except that acetic acid was used instead of thioacetic acid to give the title compound as a colorless solid (18.3 mg, yield 53%). SYNTHETIC EXAMPLE 3 73 1-rtrans-4-(Fluoromethyl)cvclohexyn-7H-pyrrolor3,2-elf 1,2,31triazolof 1,5-clpyrimidine [trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]methanol (30.0 mg, 0.111 mmol) obtained in Synthetic Example 10 suspended in dichloromethane (3 mL) was mixed with ,-diethylaminosulfur trifluoride (16.1 L, 0.122 mmol) under cooling with ice and stirred for 30 minutes while the temperature was gradually raised to room temperature. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate /hexane =1/5 1/3 (v/v)) to give the title compound as a colorless solid (6.7 mg, yield 22%). SYNTHETIC EXAMPLE 3 74 1-rtrans-4-(Bromomethyl)cvclohexyn-7H-pyrrolor3,2 -ei ,2,31triazoloH ,5-clpyrimidine [trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]methanol (50.0 mg, 0.1 84 mmol) obtained in Synthetic Example 3 10 in dichloromethane (3 mL) was mixed with triphenylphosphine (58.0 mg, 0.221 mmol) and N-bromosuccinimide (39.0 mg, 0.221 mmol) under cooling with ice and stirred for 19 hours while the temperature was gradually raised to room temperature. The reaction mixture was purified by silica gel column chromatography (ethyl acetate/ hexane = 1/1 (v/v)) to give the title compound as a colorless solid (27.4 mg, yield 44%). SYNTHETIC EXAMPLE 75 1-ftrans-4-(Chloromethyl)cvclohexyl1-7H-pyrrolor3,2-elf 1,2,31triazolof1 ,5-clpyrimidine The reactions in Synthetic Example 3 74 were carried out in substantially the same manners except that N-chlorosuccinimide was used instead of N-bromosuccinimide to give the title compound as a colorless solid ( 1 .25 mg, yield 2%). SYNTHETIC EXAMPLE 76 itrans-4-(7H-Pyrroloi3.2-eiri .2,31triazoloH ,5-clpyrimidin-1 -vDcvclohexyllmethanethiol S-{[trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]methyl} ethanethioate (30.0 mg, 0.0911 mmol) obtained in Synthetic Example 3 7 1 in methanol (2 mL) was stirred with sodium methoxide (28 wt% solution in methanol, 0 pL) at room temperature for 30 minutes. The solid precipitated in the reaction solution was removed by filtration and washed with methanol. The filtrate and the washings were mixed with water, and the precipitated solid was collected by filtration and dried under reduced pressure to give the title compound as a colorless solid (12.9 mg, yield 49%). SYNTHETIC EXAMPLE 77 1-arans-4 -r(Methylsulfonvnmethvncvclohexyl)-7H-pyrrolor3,2-elf ,2,31triazolof ,5- clpyrimidine 1-[trans-4-(Bromomethyl)cyclohexyl]-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidine (27.3 mg, 0.0817 mmol) obtained in Synthetic Example 74 in N,Ndimethylformamide (2 mL) was stirred with sodium methanesulfinate ( 10.8 mg, 0.106 mmol) at room temperature for 30 minutes and then at 65°C for 1.5 hours. The reaction mixture was allowed to cool to room temperature and stirred with sodium methanesulfinate (21 .7 mg, 0.21 2 mmol) at 65°C for 7.5 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residues was purified by silica gel column chromatography (ethyl acetate / hexane = 1/1 (v/v)) to give the title compound as a colorless solid (5.3 mg, yield 25%). SYNTHETIC EXAMPLE 78 trans-4-(7H-Pyrrolor3,2 -eiri ,2,31triazoloi1 ,5-clpyrimidin-1 -vQcvclohexanecarbaldehvde [trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]methanol (50.0 mg, 0.184 mmol) obtained in Synthetic Example 10 in a mixture of toluene ( 1 mL) and dimethyl sulfoxide (200 L) was stirred with 2-iodoxybenzoic acid (62.0 mg, 0.221 mmol) at room temperature for 30 minutes and at 50°C for 3 hours. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residues was purified by silica gel column chromatography (ethyl acetate / hexane = 1/1 (v/v)) to give the title compound as a colorless solid (38.0 mg, yield 77%). SYNTHETIC EXAMPLE 79 1-rtrans-4-(Difluoromethyl)cvclohexyl1-7H-pyrrolo[3,2-elf 1,2,31triazoloH ,5-clpyrimidine The reactions in Synthetic Example 73 were carried out in substantially the same manners except that trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexanecarbaldehyde was used instead of [trans-4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexyl]methanol to give the title compound as a colorless solid (21 . 1 mg, yield 65%). SYNTHETIC EXAMPLE3 80 trans-4-(7H-Pyrroloi3,2-e1[1 ,2,31triazolof1 ,5-clpyrimidin-1-yl)cvclohexanecarboxylic acid trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexanecarbaldehyde (25.8 mg, 0.0958 mmol) obtained in Synthetic Example 78 in t-butanol (0.31 mL) was mixed with sodium dihydrogen phosphate (34.4 mg, 0.287 mmol), water (0.31 mL) and 2-methyl-2-butene (0.31 mL, 2.87 mmol) and then with sodium chlorite (43.3 mg, 0.479 mmol) and stirred at room temperature for 2 hours. After addition of saturated aqueous sodium thiosulfate, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 10/1 4/1 2/1 (v/v)) to give the title compound as a colorless solid (14.7 mg, yield 54%). SYNTHETIC EXAMPLE3 8 1 trans-4-(7H-Pyrroloi3,2-e1f 1,2,31triazoloM .5-clpyrimidin-1 -vPcvclohexanol 1-{4-[(tert-Butyldiphenylsilyl)oxy]cyclohexyl}-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidine (400 mg, 0.807 mmol) obtained in Reference Synthetic Example 3 70 in tetrahydrofuran (8 mL) was mixed with tetrabutylammonium fluoride ( 1 M solution in tetrahydrofuran, 0.97 mL, 0.986 mmol) under cooling with ice and stirred at room temperature for 2 hours and then at 40°C for 1.5 hours. The reaction solution was stirred with tetrabutylammonium fluoride ( 1 M solution in tetrahydrofuran, 0.458 ml_, 0.484 mmol) at 40°C for 1 hour. After addition of water, the reaction solution was extracted with chloroform, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate chloroform / methanol = 10/1 (v/v)) to give the title compound as a colorless solid (78.1 mg, yield 37%). SYNTHETIC EXAMPLE 82 4-(7H-Pyrroloi3,2-e1f ,2,31triazolo[1 ,5-c1pyrimidin-1 -vDcvclohexanone The reactions in Synthetic Example 78 were carried out in substantially the same manners except that trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexanol was used instead of [trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidin-1-yl)cyclohexyl]methanol to give the title compound as a pale yellow solid (27.1 mg, yield 35%). SYNTHETIC EXAMPLE 83 cis-4-(7H-Pyrrolo[3,2-eli1 ,2,31triazolof ,5-clpyrimidin-1 -vQcvclohexanol 1-{4-[(tert-Butyldimethylsilyl)oxy]cyclohexyl}-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidine ( 1 . 8 g, 3. 6 mmol) obtained in Reference Synthetic Example 74 in tetrahydrofuran (10 mL) was stirred with tetrabutylammonium fluoride ( 1 M solution in tetrahydrofuran, 3.8 mL, 3.79 mmol) at room temperature for 15 hours and then with tetrabutylammonium fluoride ( 1 M solution in tetrahydrofuran, 7.6 mL, 7.58 mmol) at 60°C for 8 hours and then allowed to cool to room temperature. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 1/1 (v/v) ethyl acetate) to give a less polar fraction (colorless solid, 237 mg) and a more polar fraction (colorless solid, 438 mg). The less polar fraction was stirred with tetrabutylammonium fluoride ( 1 M solution in tetrahydrofuran, 440 L) at room temperature for 4 days. After addition of water, the reaction solution was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The concentrate was purified by silica gel column chromatography (hexane/ ethyl acetate = 1/1 (v/v) ethyl acetate) to give the title compound as a colorless solid (66.4 mg, yield 14%). SYNTHETIC EXAMPLE 84 Benzyl 4-(7H-imidazof ,5-c1pyrrolof3,2-elpyrimidin-1 -yl)piperidine-1 -carboxylate The reactions in Synthetic Example 3 3 were carried out in substantially the same manners except that benzyl 4-(7-{[2-(trimethylsilyl)ethoxy]methyl}-7H-imidazo[1 ,5- c]pyrrolo[3,2-e]pyrimidin-1-yl)piperidine-1-carboxylate obtained in Reference Synthetic Example 78 was used instead of benzyl 3-(7-{[2-(trimethylsilyl)ethoxy]methyl}-7Himidazo[ 1 ,5-c]pyrrolo[3,2-e]pyrimidin-1-yl)piperidine-1-carboxylate to give the title compound as a yellow solid (4.6 mg, yield 2%). SYNTHETIC EXAMPLE 85 Benzyl 4-(3-thioxo-3,7-dihydro-2H-imidazof 1,5-clpyrrolof3,2-e1pyrimidin-1 -yQpiperidine- 1-carboxylate Benzyl 4-[amino(7H-pyrrolo[2,3-d]pyrimidin-4-yl)methyl]piperidine-1-carboxylate (50.0 mg, 0.137 mmol) obtained in Reference Synthetic Example 3 79 in methanol ( 1 mL) was stirred with carbon disulfide (81 .0 , 1.35 mmol) and triethylamine (56.0 , 0.405 mmol) at 75°C for .5 hours. The reaction mixture was allowed to cool to room temperature, and the precipitated solid was collected by filtration and washed with methanol to give the title compound as a yellow solid (28.0 mg, yield 5 1%). SYNTHETIC EXAMPLE 86 1- 1 -f4-(Trifluoromethyl)benzyl1piperidin-4-yl)-2H-imidazori ,5-c1pyrrolol3,2-e1pyrimidine- 3-(7H)-thione The reactions in Synthetic Example 85 were carried out in substantially the same manners except that (7H-pyrrolo[2,3-d]pyrimidin-4-yl){1 -[4- (trifluoromethyl)benzyl]piperidin-4-yl}methanamine obtained in Reference Synthetic Example 82 was used instead of benzyl 4-[amino(7H-pyrrolo[2,3-d]pyrimidin-4- yl)methyl]piperidine-1 -carboxylate to give the title compound as a yellow solid (2.6 mg, yield 4%). SYNTHETIC EXAMPLE 3 87 Benzyl 3-(7H-pyrrolor3,2-elH ,2,31triazolof ,5-clpyrimidin-1 -yl)azetidine-1 -carboxylate The reactions in Synthetic Example 5 were carried out in substantially the same manners except that benzyl 3-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)azetidine-1- carboxylate obtained in Reference Synthetic Example 84 was used instead of (7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a yellow solid (186 mg, yield 60%). SYNTHETIC EXAMPLE 3 88 4-(rtrans-4-(7H-Pyrrolor3,2 -e ,2,31triazoloM ,5-c1pyrimidin-1 - vOcvclohexyllmethyllthiomorpholine , -dioxide trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexanecarbaldehyde (30.0 mg, 0.11 1 mmol) obtained in Synthetic Example 78 in a mixture of methanol (2 mL) and acetic acid (200 L) was stirred with thiomorpholine ,1 -dioxide (22.6 mg, 0. 67 mmol) at room temperature for 1 hour, and then with 2- picoline borane (17.9 mg, 0.167 mmol) at room temperature for another 3 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. A mixture of ethyl acetate ( 1 mL), hexane ( 1 mL) and chloroform ( 100 pL) was added to the residue, and the precipitated solid was collected by filtration to give the title compound as a colorless solid (28.3 mg, yield 65%). SYNTHETIC EXAMPLES 89 TO 120 The reactions in Synthetic Example 88 were carried out in substantially the same manners except that piperidin-4-carbonitrile, 3-aminopropanenitrile, morpholine, 4- aminobenzonitrile, 4-(aminomethyl)benzonitrile hydrochloride, (S)-3-fluoropyrrolidine, (R)-3-fluoropyrrolidine, 3,3-dimethylazetidine hydrochloride, 4,4-difluoropiperidine hydrochloride, [4-(trifluoromethyl)phenyl]methanamine, 4-(trifluoromethyl)aniline, 4- fluoroaniline, (4-fluorophenyl)methanamine, 4-fluoro-N-methylaniline, 4-amino-3- methylbenzonitrile, 2-methyl-4-(trifluoromethoxy)aniline, 4-amino-2- (trifluoromethyl)benzonitrile, (5-methylthiophen-2-yl)methanamine hydrochloride, 2- fluoroethanamine hydrochloride, 4-(methylamino)benzonitrile, 1-(3,4- difluorophenyl)ethanamine, [4-(trifluoromethoxy)phenyl]methanamine, 2-(4- fluorophenyl)ethanamine, [4-fluoro-3-(trifluoromethyl)phenyl]methanamine, [4- (methylsulfonyl)phenyl]methanamine, 4-(trifluoromethoxy)aniline, 2-chloro-4- (triluforomethoxy)aniline, 2-amino-5-fluorobenzonitrile, 4-fluoro-2-(trifluoromethyl)aniline, 4-morpholinoaniline, (S)-pyrrolidin-3-ol hydrochloride or (S)-(tetrahydrofuran-2- yl)methanamine was used instead of thiomorpholine ,1 -dioxide to give the compounds of Synthetic Examples 89 to 120. The names, morphologies and yields of the compounds synthesized are shown in Tables 10 to 12. TABLE 10 Ex Compound Name Morphology Yield 1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] t 89 riazolo [1,5-c]pyrimidin-l-yl)cyclohexy colorless solid 83 l]methyl}piperidine-4-carbonitrile 3-({[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 ] 90 triazolo[l, 5-c]pyrimidin-l-yl)cyclohex colorless solid 74% yl]methyl}amino)propanenitrile 4-{[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3]t 9 1 riazolo[l, 5-c]pyrimidin-l-yl)cyclohexy colorless solid 73% l]methyl}morpholine 4-({[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 ] 92 triazolo[l, 5~c]pyrimidin-l-yl) cyclohex colorless solid 57% yl]methyl}amino)benzonitrile 4-[({ [trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 93 ]triazolo[l, 5-c]pyrimidin-l-yl)cyclohe colorless solid 64% xyl]methyl}amino)methyl]benzonitrile l-(trans-4-{ [(S)-3-fluoropyrrolidin-l- 94 yl]methyl}cyclohexyl)-7H-pyrrolo[3, 2-e colorless solid 80% ] [1, 2 ,3]triazolo[l, 5-c]pyrimidine l-(trans-4-{ [(R)-3-fluoropyrrolidin-l- 95 yl]methyl} cyclohex yl)-7H-pyrrolo[3, 2 e colorless solid 63% ] [l, 2,3]triazolo[l, 5-c]pyrimidine l-{trans-4-[ (3, 3-dimethylazetidin-l-yl 96 )methyl]cyclohexyl} -7H-pyrrolo[3, 2-e] [ colorless solid 37% 1 , , 3]triazo 1o [1,5~ c]pyrimidine 1- {trans-4- [(4, 4-difluoropiperidin-l-y 97 l)methyl]cyclohexyl}-7H-pyrrolo[3, -e] colorless solid 64% [1,2 , 3 ] triazolo[l, 5-c]pyrimidine 1- [trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] r iazo1o [1,5-c]pyrimidin-l-yl) cyclohexyl 98 colorless solid 59% ]-N-[4-(trifluoromethyl)benzyl]methana mine N-{[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3]t 99 riazolo [l, 5-c]pyrimidin-l-yl)cyclohexy colorless solid 63% l]methyl}-4-(trifluoromethyl) aniline N - ί [trans-4- (7H-pyrrolo [3, 2-e] [l, 2 , 3 ] 100 riazolo [ ,5-c]pyrimidin-l-yl)cyclohexy colorless solid 31% l]methyl}-4-fluoroaniline 1- [trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] tr 101 iazo1o[1,5~ c]pyrimidin-l-yl) cyclohexyl colorless solid 67% ]- - (4-fluorobenzyl)methan amine N - {[trans-4- (7H-pyrrolo [3, 2-e] [1 , 2 , 3 ] t 102 riazolo [1,5-c]pyrimidin - l_ yl)cyclohexy colorless solid 78% l]methyl}-4-fluoro-N-methyl aniline 4 - ( ί [trans - 4 - (7H-pyrrolo [3, 2-e] [l, 2 , 3 ] 103 triazolo [1, 5-c]pyrimidin-l-yl) cyclohex colorless solid 82% yl]methyl) amino) -3-methylbenzonitrile TABLE 11 Ex Compound Name Morphology Yield N-{[trans-4- (7H-pyrrolo[3 2-e] [l, 2 , 3]t ia o [1,5-c]pyrimidin-l-yl) cyclohexy 104 colorless solid 66% l]methyl}-2-methyl-4-(trifluoromethoxy )a il ne 4-({[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl) ycloh 105 colorless solid 61% yl]methyl}amino)-2-(trifluoromethyl)be 1 z itrile 1- [trans -4- (7H-pyrrolo [3, 2-e] [l, 2 , 3]tr iazo 1o [1,5~ c]pyrimidin-l-yl) cyclohexyl 106 colorless solid 49% ]- - [ (5- methylthiophen-2-yl) methyl] e hanamine N-{[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3]t 107 riazolo [1,5-c]pyrimidin-l-yl) cyclohexy colorless solid 19% l]methyl}-2-fluoroethan am i 4- ({[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] 108 triazolo [1,5-c]pyrimidin-l-yl) cyclohex colorless solid 36% yljmethyl} (methyl) amino) benzonitri le N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] t riazolo [1,5-c]pyrimidin-l-yl) cyclohexy 109 colorless solid 8 . 1% l]methyl}-l - (3, 4-difluorophenyl) ethana m i e l-[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3]tr iazo1o [1,5-c]pyriraidin-l-yl) cyclohexyl 110 colorless solid 16% ]- - [4- (trifluoromethoxy) benzyl]methan m e N- {[trans-4- (7H-pyrrolo [3, 2-e] [ 1 ,2,3 ] t pale purple 111 riazolo [1,5-c]pyrimidin-l-yl) cyclohexy 12% solid l]methyl}-2- (4-fluorophenyl) ethanamine 1- [trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] tr iazo 1o [1,5-c]pyrimidin-l-yl) cyclohexyl 112 colorless solid 5 . 1% ]-N- [4-fluoro-3- (trifluoromethyl)benzy 1]metha nami ne 1- [trans-4- (7H-pyrrolo [3, 2-e] [l, 2 , 3]tr iazolo[l, 5-c]pyrimidin-l-yl) cyclohexyl 113 colorless solid 5 . 0% ]-N ~ [4- (methylsulfonyl)benzyl]methanam ine N- {[trans-4 - (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] t 114 riazolo [1,5-c]pyrimidin-l-yl) cyclohexy colorless solid 69% l]methyl}-4-(trifluoromethoxy)aniline N-{[trans-4- (7H-pyrrolo[3, 2-e] [l, 2 , 3]t riazolo [1,5-c]pyrimidin-l-yl) cyclohexy 115 colorless solid 77% l]methyl}-2-chloro-4-(trifluoromethoxy )an i ne 2-({[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 ] 116 triazolo[l, 5-c]pyrimidin-l-yl)cyclohex colorless solid 59% yl]methyl}amino)-5-fluorobenzonitrile TABLE 12 SYNTHETIC EXAMPLE 121 4-([4-(7 -3.2-.2,31triazolori ,5-clpyrimidin-1 -vhcvclohexyllaminolbenzonitrile 4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexanone (21 .5 mg, 0.0842 mmol) obtained in Synthetic Example 3 82 in a mixture of methanol ( 1 mL) and acetic acid (0.1 mL) was stirred with 4-aminobenzonitrile (15.0 mg, 0.126 mmol) and 2- picoline borane (13.5 mg, 0.126 mmol) at room temperature for one day. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel thin layer chromatography (NH-PLC05 plate manufactured by Fuji Silysia Chemical Ltd.: ethyl acetate) to give cis/trans mixture of the title compound as a pale yellow solid (17.1 mg, yield 57%). SYNTHETIC EXAMPLES 3 122 TO 133 The reactions in Synthetic Example3 121 were carried out in substantially the same manners except that 2-(pyridin-4-yl)ethanamine, 2-phenylethanamine, morpholine, 2-[3-(trifluoromethyl)phenyl]ethanamine, 2-morpholinoethanamine, piperidine-4- carbonitrile, 4-(trifluoromethyl)aniline, 4-amino-3-fluorobenzonitrile, 4-fluoro-Nmethylaniline, 4-fluoroaniline, 4-amino-3-methylbenzonitrile or 2-methyl-4- (trifluoromethoxy)aniline was used instead of 4-aminobenzonitrile to give the compounds of Synthetic Examples 122 to 133. The names, morphologies and yields of the compounds synthesized are shown in Table 13. TABLE 13 SYNTHETIC EXAMPLE 134 134a: 4-(rcis-4-(7H-Pyrrolo[3,2 -ei .2.3¾riazoloM .5-clpyrimiclin-1 - yDcyclohexynaminojbenzonitrile 134b: 4-(rtrans-4-(7H-Pyrrolor3,2-elf1 ,2,31triazoloi1 ,5-c1pyrimidin-1- vDcyclohexynaminolbenzonitrile 4-{[4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexyl]amino}benzonitrile (16.5 mg, 0.462 mmol) obtained in Synthetic Example 121 was resolved by silica gel thin layer chromatography (hexane / ethyl acetate =1/2 (v/v)) into 4-{[cis-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexyl]amino}benzonitrile (Synthetic Example 134a; pale yellow solid, 7.3 mg, yield 44%) in a less polar fraction and into 4-{[trans-4-(7H-Pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexyl]amino}benzonitrile (Synthetic Example 134b; pale yellow solid, 3.0 mg, yield 18%) in a more polar fraction. SYNTHETIC EXAMPLE 135 35a: cis-N-Phenethyl-4-(7H-pyrrolo[3,2 -e .2.31triazoloM .5-c1pyrimidin-1 - vDcyclohexanamine 35b: trans-N-Phenethyl-4-(7H-pyrrolof3,2 -eiri .2.3ltriazolof1 ,5-c1pyrimidin-1- vDcyclohexanamine The reactions in Synthetic Example 134 were carried out in substantially the same manners except that N-phenethyl-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidin-1-yl)cyclohexanamine obtained in Synthetic Example 123 was used instead of 4-{[4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexyl]amino}benzonitrile to give cis-N-phenethyl-4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexanamine (Synthetic Example 135a; colorless solid, 3.22 mg, yield 16%) in a less polar fraction and trans-N-phenethyl-4- (7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexanamine (Synthetic Example 135b; colorless solid, 2.52 mg, yield 1 1%) in a more polar fraction. SYNTHETIC EXAMPLE 136 136a: cis-N-(3-Phenylpropyl)-4-(7H-pyrrolo[3,2 -ei ,2,31triazoloM ,5-clpyrimidin-1- vPcyclohexanamine 136b: trans-N-(3-Phenylpropyl)-4-(7H-pyrrolo[3.2 -e r ,2,31triazoloM .5-clpyrimidin-1 - vDcyclohexanamine 4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexanone (30.0 mg, 0.11 8 mmol) obtained in Synthetic Example 82 in a mixture of methanol ( 1 .5 ml) and acetic acid (0.15 mL) was mixed with 3-phenylpropan-1 -amine (25.0 L, 0.176 mmol) at room temperature and stirred at 40°C for 30 minutes. The reaction mixture was allowed to cool to room temperature and stirred with 2-picoline borane ( 19.0 mg, 0.1 76 mmol) at room temperature for one day. After addition of 1 M hydrochloric acid and ethyl acetate, the aqueous layer was separated, and after addition of 1 M aqueous sodium hydroxide, extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure, and the residue was purified by silica gel chromatography (Hi Flash amino silica gel column manufactured by Yamazen Corporation: ethyl acetate / hexane = 1/1 (v/v) ethyl acetate) to give cis-N-(3-phenylpropyl)-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidin-1 -yl)cyclohexanamine (Synthetic Example 136a; colorless oil, 6.00 mg, yield 13%) in a less polar fraction and trans-N-(3-phenylpropyl)-4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexanamine (Synthetic Example 3 136b; colorless solid, 2.52 mg, yield 5.7%) in a more polar fraction. SYNTHETIC EXAMPLES 3 37 TO 39 The reactions in Synthetic Example 3 136 were carried out in substantially the same manners except that 4-(aminomethyl)benzonitrile, [4- (trifluoromethyl)phenyl]methanamine or morpholin-4-amine was used instead of 3- phenylpropan-1 -amine to give the compounds of Synthetic Examples 137a to 139a in less polar fractions and the compounds of Synthetic Examples 3 137b to 139b in more polar fractions. The names, morphologies and yields of the compounds synthesized are shown in Table 14. TABLE 14 SYNTHETIC EXAMPLE 3 140 4-(7-ί3,2-1 ,2,31triazoloM ,5-c1pyrimidin-1 -vDphenyllmethanol 1-(4-{[(tert-Butyldimethylsilyl)oxy]methyl}phenyl)-7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (3.58 g, 9.43 mmol) obtained in Reference Synthetic Example 3 88 in a mixture of dichloromethane (20 mL) and methanol (50 mL) was stirred with pyridinium p-toluenesulfonate ( 1 .1 8 g, 4.72 mmol) at 60°C for 8 hours. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v) ethyl acetate ethyl acetate / methanol = 1/1 (v/v)) to give the title compound as an ivory solid (831 mg, yield 33%). SYNTHETIC EXAMPLE 141 rtrans-4-(7H-Pyrrolo[3,2-e1[1 ,2,31triazolon ,5-ctoyrimidin-1 -vDcvclohexynmethanol The reactions in Synthetic Example 140 were carried out in substantially the same manners except that 1-(trans-4-{[(tert-butyldimethylsilyl)oxy]methyl}cyclohexyl)- 7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine obtained in Reference Synthetic Example 92 was used instead of 1-(4-{[(tert-butyldimethylsilyl)oxy]methyl}phenyl)-7Hpyrrolo[ 3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine to give the title compound as a pale yellow solid (2.05 g , yield 78%). (alternative to Synthetic Example 3 10). SYNTHETIC EXAMPLES 3 142 TO 144 The reactions in Synthetic Example 32 were carried out in substantially the same manners except that 1-(bromomethyl)-2-fluorobenzene, 2-(bromomethyl)-5- (trifluoromethyl)furan or 5-(bromomethyl)thiophene-2-carbonitrile (Reference Synthetic Example 93) was used instead of benzyl bromide to give the compounds of Synthetic Examples 142 to 144. The names, morphologies and yields of the compounds synthesized are shown in Table 15. TABLE 15 SYNTHETIC EXAMPLES 145 TO 171 The reactions in Synthetic Example 44 were carried out in substantially the same manners except that 6-fluoronicotinaldehyde, furan-2-carbaldehyde, 5-iodofuran-2- carbaldehyde, thiophene-2-carbaldehyde, 5-bromofuran-2-carbaldehyde, 2- chlorothiazole-5-carbaldehyde, 1H-pyrazole-5-carbaldehyde, 1,2,3-thiadiazole-4- carbaldehyde, 2-bromothiazole-5-carbaldehyde, 4-fluoro-3- (trifluoromethyl)benzaldehyde, 4-chloro-3-(trifluoromethyl)benzaldehyde, 4- (methylsulfonyl)benzaldehyde, 2-fluoro-4-(trifluoromethyl)benzaldehyde, 4-chloro-2- fluorobenzaldehyde, 4-chloro-3-fluorobenzaldehyde, 2-chloroisonicotinaldehyde, 3- fluoroisonicotinaldehyde, 5-fluoropyridine-2-carbaldehyde, 3-chloroisonicotinaldehyde, 2,4-difluorobenzaldehyde, 2-chloro-4-fluorobenzaldehyde, 3,4-difluorobenzaldehyde, 3- fluoro-4-(trifluoromethyl)benzaldehyde, 4-(2-hydroxyethoxy)benzaldehyde, 4-(1 , 1 ,2,2- tetrafluoroethoxy)benzaldehyde, 6-methoxynicotinaldehyde or tert-butyl (2- oxoethyl)carbamate was used instead of thiazole-5-carbaldehyde to give the compounds of Synthetic Examples3 145 to 171 . The names, morphologies and yields of the compounds synthesized are shown in Tables3 16 and 17. TABLE 16 Ex Compound Name r holo y Yield l-{l-[(6-fluoropyridin-3-yl) methyl]pip 145 eridin-4-yl}-7H-pyrrolo[3, 2-e] [l, 2 , 3]t colorless solid 66% riazolo[l, 5-c]pyrimidine l-[l-(furan-2-ylmethyl)piperidin-4-yl] 146 -7H-pyrrolo[3, 2-e ] [1,2 , 3]triazolo[l, 5- colorless solid 7 . 0% clpyrimidine l-{l-[(5-iodofuran-2-yl)methyl]piperid 147 in-4-yl}-7H-pyrrolo[3, 2-e] [ l 2 , 3]triaz colorless solid 66% 1 [1,5-c]pyrimidine l-[l-(thiophen-2-ylmethyl)piperidin-4- 148 yl]-7H-pyrrolo[3, 2-e] [1, 2 , 3 ] triazolo[l colorless solid 49 ,5-c]pyrimidine l-{l-[(5-bromofuran-2-yl)methyl]piperi 149 din-4-yl}-7H-pyrrolo[3, 2-e] [l, 2 , 3 ] tria colorless solid 6 z 1 [1,5-c]p im 5-{ [4-(7H-pyrrolo[3, 2-e] [l, 2 , 3]triazol 150 o [1, 5-c]pyrimidin-l-yl)piperidin-l-yl] colorless solid 62% methyl} -2-chlorothiazole l-{l-[(lH-pyrazol-5-yl)methyl]piperidi 151 n-4-yl} -7H-pyrrolo[3, 2-e] [l, 2 , 3]triazo colorless solid 17% 1 [ ,5-c]pyrimidine 4-i [4-(7H-pyrrolo[3, 2-e] [l, 2 , 3]triazol 152 [1,5-c]pyrimidin-l-yl)piperidin-l-yl] colorless solid 45% methyl} -1, 2 , 3-thiadiazole 5-{[4-(7H-pyrrolo [3, 2-e] [l, 2 , 3]triazol 153 o [1, 5-c]pyrimidin-l-yl)piperidin-l-yl] colorless solid 58% methyl} -2-bromothiazole l-{l-[4-fluoro-3 - (trifluoromethyl)benz 154 yl]piperidin-4-yl)-7H-pyrrolo[3, 2-e] [ 1 colorless solid 27% , , 3 ] triazolo[l, 5-c]pyrimidine 1-{1- [4-chloro-3 - (trifluoromethyl) benz 155 yl]piperidin-4-yl}-7H-pyrrolo[3, 2-e] [ l colorless solid 9 . 0% ,2 , 3 ] triazolo[l, 5-c]pyrimidine 1- {1- [4 - (methylsulfonyl) benzyllpiperid 156 in-4-yl}-7H-pyrrolo[3, 2-e] [l, 2 , 3]triaz colorless solid 21% 1o [ ,5-c]pyrimidine l-{l-[2-fluoro-4 _ (trifluoromethyl)benz 157 yl]piperidin-4-yl}-7H-pyrrolo[3, -e] [ l colorless solid 8 . 0% ,2 , 3]triazolo[l, 5-c]py imidi l-[l- (4-chloro-2 ~ fluorobenzyl)piperidi 158 n-4-yl]-7H-pyrrolo[3, 2-e] [ l 2 , 3]triazo colorless solid 50% 1o [1,5-c]pyrimidine l-[l-(4-chloro-3 _ fluorobenzyl)piperidi 159 ii-4-yl]-7H-pyrrolo[3, 2-e] [l, 2 , 3]triazo colorless solid 44% 1o [1,5-c]pyrimidine l-{l-[(2-chloropyridin-4-yl) methyl]pip 160 e d n-4-y -7H-p yrro 1o [3, 2-e] [l, 2 , 3]t colorless solid 39% riazolo[l, 5-c]pyrimidine TABLE 17 Ex Compound Name Morphology Yield 1- {1- [(3-fluoropyridin-4-yl) methyllpip 161 eridin-4-yl} -7H-pyrrolo [3,2-e] [ l ,2 , 3]t colorless solid 22% riazolo [1,5-c]pyrimidine 1- {1- [(5-fluoropyridin-2-yl) methyllpip 162 eridin-4-y l}-7H- rrolo[3,2- e] [ l ,2 , 3]t colorless solid 39% riazolo [1, 5-c]pyrimidine 1- {1- (3-chloropyridin-4-yl) methyllpip 163 erid -4-y l}-7H-pyrrolo [3,2-e] [ l ,2,3]t col less solid 33% riazolo [1,5-c]pyrimidine 1-[1- (2, 4-difluorobenzyl)piperidin-4-y 164 l]- 7H-pyrrolo [3,2-e] [ l ,2 3]triazolo [ l , pink solid 1 % 5-c]pyrimidine l - [ l -(2-chloro-4-fluorobenzyl)piperidi 165 n-4-y l]-7H-pyrrolo [3,2-e] [ l ,2 , 3]triazo colorless solid 18% 1o [ ,5-c]pyrimidine 1— [1- (3, 4-difluorobenzyl) pipe ridin-4-y 166 l]-7H-pyrrolo[3, 2-e] [1, 2 , 3]triazolo l , colorless solid 30% 5-c]pyrimidine l - { l -[3-fluoro-4- (trifluoromethyl) benz 167 yl]piperidin-4-yl}-7H-pyrrolo[3, 2-e] [ l colorless solid 15% ,2 , 3 ] triazolo [ l , 5-c]pyrimidine 2- ( 4 - { [ 4 -(7H-pyrrolo[3, 2-e] [1, 2 , 3]tria 168 zoloil, 5-c]pyrimidin - l -yl)piperidin - l - colorless solid 7 . 0% yl]methyl}phenoxy)ethanol 1- 1- [4 - ( 1 ,1 , 2 , 2-tetrafluoroethoxy)ben 169 zyl]piperidin - 4 -yl}-7H-pyrrolo[3, 2-e] [ colorless solid 11% 1 , 2 , 3]triazolo[l, 5-c]pyrimidine l - { l -[(6-methoxypyridin-3-yl)methyl]pi 170 peridin -4-y l }- 7H-pyrrolo [3,2-e] [ l ,2 , 3 ] colorless solid 15% triazolofl, 5-c]pyrimidine tert-butyl {2-[4-(7H-pyrrolo [3, 2-e ] [ l ,2 , 3]triazol pale yellow 171 75% o [1,5-c]pyrimidin _ l -yl)piperidin - l -yl] amorphous ethyl} carbamate SYNTHETIC EXAMPLES 72 TO 193 The reactions in Synthetic Example 88 were carried out in substantially the same manners except that 3-amino-1 , 1 ,1-trifluoro-2-phenylpropan-2-ol (Reference Synthetic Example 101), 4-[(trifluoromethyl)sulfonyl]aniline, 2-phenylethanamine, 2- (trifluoromethyl)-l H-benzo[d]imidazol-6-amine, 4-chloroaniline, (4- chlorophenyl)methanamine, 2-(4-chlorophenyl)ethanamine, 5-fluoroindoline, 3,3'- azanediyldipropanenitrile, (S)-N,N-dimethylpyrrolidin-3-amine, (5-methylfuran-2- yl)methanamine, (5-methylpyrazin-2-yl)methanamine, (S)-1-aminopropan-2-ol, (R)-1- aminopropan-2-ol, 2-amino-1-phenylethanol, (S)-pyrrolidine-3-carbonitrile hydrochloride, 2,2,2-trifluoroethanamine, 5-(methylsulfonyl)indoline, N,N-dimethylindoline-5- sulfonamide, 1-(2-aminoethyl)imidazolidin-2-on, 2-(1 H-imidazol-4-yl)ethanamine dihydrochloride or phenylmethanamine was used instead of thiomorpholine 1, 1-dioxide to give the compounds of Synthetic Examples 172 to 193. The names, morphologies and yields of the compounds synthesized are shown in Tables 8 and 19. TABLE 8 Ex Compound Name Morphology Yield 3-( {[trans-4-(7H-pyrrolo[3, 2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl) cyelohex 172 colorless solid % yl]methyl} amino) - 1,1 , l-trifluoro-2-phe 1 y1prop an-2- o1 N-{[trans-4- (7H-pyrrolo[3, 2-e] [l, 2 , 3]t riazolo [1,5-c]pyrimidin _ l-yl)cyclohexy 173 colorless solid 10% l]methyl}-4-[(trifluoromethyl)sulfonyl ]aniline N-{[trans-4- (7H- rrolo [3,2-e] [l, 2 , 3]t 174 riazolo[l, 5-c]pyrimidin-l-yl)cyclohexy colorless solid 97% 1]methy )-2-pheny 1ethana ine N-{[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3]t riazolo [1,5-c]pyrimidin-l-yl) cyclohexy 175 colorless solid 15% l]methyl}-2- (trifluoromethyl)-lH-benzo [d] imidazol-5-amine - {[trans-4- (7H-pyrrolo [3, 2-e] [l, 2 , 3]t 176 riazolo [1,5-c]pyrimidin-l-yl) cyclohexy colorless solid 52% l]methyl}-4-chloro aniline l- [tran s 4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] tr 177 iazo1o [1,5-c]pyrimidin-l-yl) cyclohexyl colorless solid 37% ]-N-(4-chlorobenzyl)methanamine N-{ [trans-4- (7H-pyrro 1o [3, 2-e] [l, 2 , 3]t pale purple 178 riazolo [1,5-c]pyrimidin-l-yl) c lohe 86% solid l]methyl} -2- (4-chlorophenyl) ethan amine l-[trans-4- ((5-fluoroindolin-l-yl) meth 179 yl)cyclohexyl]-7H-pyrrolo[3, 2-e] [l, 2 , 3 colo ess solid 83% ] triazolo[l, 5-c]pyrimidine 3 , 3 ' -({ [trans-4-(7H-pyrrolo[3, 2-e] [i, 2 ,3]triazolo[l, 5-c]pyrimidin-l-yl)cyclo 180 colorless solid 74% hexyl]methyl}azanediyl)dipropanenitril e (S)-l-{ [trans-4-(7H-pyrrolo[3, 2-e] [l, 2 ,3]triazolo[l, 5-c]pyrimidiri-l-yl)cyclo 181 colorless solid 71% hexyl]methyl}-N, N-diraethylpyrrolidin-3 - a e l-[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] tr iaz o [1,5-c ]pyrimidin-l-yl) cyclohexyl pale yellow 182 44% ]- - [(5-methylfuran-2-yl)methyl]methan solid amine l-[trans-4-(7H-pyrrolo [3, 2-e] [l, 2 , 3]tr iazo1o [1,5-c]py imidi l-yl)cyclohexyl 183 colorless solid 55% ]- - [(5-methylpyrazin-2-yl) methyl] meth anam ine (S) -l-( {[trans-4- (7H-pyrrolo [3, 2-e] [1, 184 2 , 3]triazolo [1,5-c]pyrimidin-l-yl) cycl colorless solid 21% ohexyl]methyl}amino)propan-2 _ o l (R)-l-( {[trans-4- (7H-p yrrolo [3, 2-e] [1, 185 2 ,3]triazolo [1, 5-c]pyrimidin-l-yl) cycl colorless solid 20% ohexyl]methyl}amino)propan-2-ol TABLE 19 SYNTHETIC EXAMPLES 194 TO 197 The reactions in Synthetic Example 136 were carried out in substantially the same manners except that phenylmethanamine, (4-fluorophenyl)methanamine, 3- amino-1 , 1 ,1-trifluoro-2-phenylpropan-2-ol (Reference Synthetic Example3 101) or (4- chlorophenyl)methanamine was used instead of 3-phenylpropan-1 -amine to give the compounds of Synthetic Examples3 194a to 197a in less polar fractions and the compounds of Synthetic Examples 194b to 197b in more polar fractions. The names, morphologies and yields of the compounds synthesized are shown in Table3 20. TABLE 20 SYNTHETIC EXAMPLES 198 TO 204 The reactions in Synthetic Example3 136 were carried out in substantially the same manners except that 2-(4-chlorophenyl)ethanamine, 3-amino-2-(4-chlorophenyl)- 1, 1 ,1-trifluoropropan-2-ol (Reference Synthetic Example 100), 3-amino-1 , 1 ,1-trifluoro- 2-(4-fluorophenyl)propan-2-ol (Reference Synthetic Example3 102), 2-(4- fluorophenyl)ethanamine, 2-amino-1-phenylethanol, (S)-2-amino-1 -phenylethanol or (R)-2-amino-1-phenylethanol was used instead of 3-phenylpropan-1 -amine to give the compounds of Synthetic Examples 98b to 204b in more polar fractions. The names, morphologies and yields of the compounds synthesized are shown in Table3 2 1. TABLE 2 1 SYNTHETIC EXAMPLE 205 -4-(7-ΐΊΌΐ 3,2-1 ,2,3ltriazoloi1 ,5-c1pyrimidin-1 -yl)cyclohexyl1-4-chloroaniline The reactions in Synthetic Example3 121 were carried out in substantially the same manners except that 4-chloroaniline was used instead of 4-aminobenzonitrile to give the title compound as a colorless solid ( 10.2 mg, yield 28%). SYNTHETIC EXAMPLE 206 trans-N-(4-Fluorophenyl)-4-(7H-pyrrolor3,2-e1H ,2,31triazolori ,5-ctoyrimidin-1 - vDcyclohexanecarboxamide trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexanecarboxylic acid (19.5 mg, 0.0683 mmol) obtained in Synthetic Example3 80 in N,Ndimethylformamide ( 1 .5 mL) was mixed with 4-fluoroaniline (0.0977 mL, 0.102 mmol) and 0-(7-azabenzotriazol-1 -yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate (38.8 mg, 0.102 mmol) and then with N,N-diisopropylethylamine (0.0238 mL, 0.137 mmol) and stirred at room temperature for 3 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (NH-PLC05 plate manufactured by Fuji Silysia Chemical Ltd.: ethyl acetate). The resulting solid was washed with methanol to give the title compound as a colorless solid (6.45 mg, yield 25%). SYNTHETIC EXAMPLES 207 TO 209 The reactions in Synthetic Example3 206 were carried out in substantially the same manners except that (4-fluorophenyl)methanamine, 2-(4-fluorophenyl)ethanamine or (S)-3-fluoropyrrolidine was used instead of 4-fluoroaniline to give the compounds of Synthetic Examples3 207 to 209. The names, morphologies and yields of the compounds synthesized are shown in Table 22. TABLE 22 SYNTHETIC EXAMPLE 210 4-{f4-(7H-lmidazori ,5-clpyrrolo[3,2-e1pyrimidin-1 -yl)piperidin-1 -yllmethvDbenzonitrile The reactions in Synthetic Example3 3 were carried out in substantially the same manners except that 4-{[4-(7-{[2-(trimethylsilyl)ethoxy]methyl}-7H-imidazo[1 ,5- c]pyrrolo[3,2-e]pyrimidin-1-yl)piperidin-1-yl]methyl}benzonitrile obtained in Reference Synthetic Example 97 was used instead of benzyl 3-(7-{[2- (trimethylsilyl)ethoxy]methyl}-7H-imidazo[1 ,5-c]pyrrolo[3,2-e]pyrimidin-1 -yl)piperidine-1 - carboxylate to give the title compound as a brown solid ( 1 .3 mg, yield 4%). SYNTHETIC EXAMPLE 3 2 11 Benzyl 3-(7H-pyrrolo[3,2-e1f ,2,3]triazoloH ,5-clpyrimidin-1 -yl)pyrrolidine-1 -carboxylate The reactions in Synthetic Example 5 were carried out in substantially the same manners except that benzyl 3-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)pyrrolidine-1 - carboxylate obtained in Reference Synthetic Example 3 99 was used instead of (7Hpyrrolo[ 2,3-d]pyrimidin-4-yl)(o-tolyl)methanone to give the title compound as a colorless solid (27.4 mg, yield 2%). SYNTHETIC EXAMPLE 212 2-f4-(7H-Pyrrolor3,2-e1f 1,2,31triazolo[1 ,5-clpyrimidin-1 -yl)piperidin-1 -yll-1 -4- (trifluoromethyl)phenyllethanol 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine acetate (33.1 mg, 0.110 mmol) obtained in Reference Synthetic Example 104 in ethanol (3 mL) was stirred with water (0.5 mL), triethylamine (0.1 mL), ytterbium (III) trifluoromethanesulfonate (12.7 mg, 0.0237 mmol) and 2-[4- (trifluoromethyl)phenyl]oxirane (47.0 mg, 0.250 mmol) obtained in Reference Synthetic Example3 103 at 80°C for 3 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (methanol / chloroform, = 1/20 (v/v)). The resulting solid was washed with hexane / ethyl acetate to give the title compound as a red solid ( 19.7 mg, yield 42%). SYNTHETIC EXAMPLES 213 TO 226 The reactions in Synthetic Example3 44 were carried out in substantially the same manners except that 2-(4-formylphenoxy)acetonitrile (Reference Synthetic Example 3 105), 6-chloronicotinaldehyde, (E)-3-(furan-2-yl)acrylaldehyde, 1-methyl- 1H-pyrrole-2- carbaldehyde, 3-chloro-1 H-indazole-5-carbaldehyde, quinoxaline-6-carbaldehyde, oxazole-4-carbaldehyde, 4-(difluoromethoxy) benzaldehyde, 4-(1 H-imidazole-1-yl) benzaldehyde, 2-fluoro-4-formylbenzonitrile, 2-fluoro-5-formylbenzonitrile, 2,6-difluoro- 4-(trifluoromethyl)benzaldehyde, 3-oxo-3,4-dihydro-2H-benzo[b][1 ,4]oxazine-6- carbaldehyde or 4-[(2-cyanoethyl)methylamino]benzaldehyde was used instead of thiazole-5-carbaldehyde to give the compounds of Synthetic Examples 213 to 226. The names, morphologies and yields of the synthesized compounds are shown in Table 23. TABLE 23 SYNTHETIC EXAMPLE 227 1-(1 -r(2,2-Difluorobenzordiri .31dioxol-5-yl)methvnpiperidin-4-yl)-7H-pyrrolof3.2- e .2,31triazolof ,5-clpyrimidine 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine acetate (20.0 mg, 0.0660 mmol) obtained in Reference Synthetic Example 04 in methanol ( 1 mL) was mixed with 2,2-difluorobenzo[d][1 ,3]dioxole-5-carbaldehyde (20.0 l_, 0.0990 mmol), nicotinic acid (12.3 mg, 0.0990 mmol), and 2-picoline borane (10.7 mg, 0.0990 mmol) and stirred at room temperature for 1 day. After addition of 1M aqueous sodium hydroxide, the reaction mixture was extracted with chloroform. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (methanol / chloroform = 1/10 (v/v)) to give the title compound as a colorless solid (13.1 mg, yield 48%). SYNTHETIC EXAMPLES 228 TO 239 The reactions in Synthetic Example 227 were carried out in substantially the same manners except that 5-chlorofuran-2-carbaldehyde, 2,2- difluorobenzo[d][1 ,3]dioxol-4-carbaldehyde, 3-oxo-2-phenylpropanenitrile, 2,6- dichloronicotinaldehyde, benzo[d]thiazole-2-carbaldehyde, 4,5-dibromothiophene-2- carbaldehyde, 2-morpholinothiazole-5-carbaldehyde, 2-(4-chlorophenyl)-3- oxopropanenitrile, 5-methylthiophene-2-carbaldehyde, 4-bromothiophene-2- carbaldehyde, 5-bromothiophene-2-carbaldehyde or isonicotinaldehyde was used instead of 2,2-difluorobenzo[d][1 ,3]dioxole-5-carbaldehyde to give the compounds of Synthetic Examples 228 to 239. The names, morphologies and yields of the synthesized compounds are shown in Table 24. TABLE 24 SYNTHETIC EXAMPLES 240 TO 246 The reactions in Synthetic Example 32 were carried out in substantially the same manners except that 4-(chloromethyl)thiazole hydrochloride, 4- (bromomethyl)benzamide (Reference Synthetic Example 106), 4- (bromomethyl)phthalonitrile (Reference Synthetic Example 108), 5-(bromomethyl)-2- (trifluoromethyl)benzonitrile (Reference Synthetic Example 107), 4-(bromomethyl)-2- (trifluoromethyl)benzonitrile (Reference Synthetic Example3 109), (1- bromoethyl)benzene or 2-chloroacetonitrile was used instead of benzylbromide to give the compounds of Synthetic Examples3 240 to 246. The names, morphologies and yields of the synthesized compounds are shown in Table3 25. TABLE 25 SYNTHETIC EXAMPLES 247 TO 345 The reactions in Synthetic Example3 88 were carried out in substantially the same manners except that 4-amino-2-chlorobenzonitrile, 4-amino-1 -naphthonitrile, 3,4- difluoroaniline, 3,4,5-trifluoroaniline, 4-fluoro-3-(trifluoromethyl)aniline, 5-amino-2- fluorobenzonitrile, 3-aminodihydrothiophen-2(3H)-one hydrochloride, thiazolidine, 2,2- difluoroethaneamine, 3,3,3-trifluoropropane-1-amine, 3-hydroxyazetidine hydrochloride, 4-(trifluoromethyl)piperidine hydrochloride, 2-aminoacetonitrile hydrochloride, piperazin- 2-one, piperidine-4-carboxamide, 4-aminophthalonitrile, 5-amino-2-chlorobenzonitrile, 2- (4-aminophenyl)acetonitrile, (R)-pyrrolidine-2-yl methanol, (S)-pyrrolidine-2-yl methanol, (R)-pyrrolidin-3-ol, 2-(benzylamino)ethanol, 2-bromo-2,2-difluoroethaneamine hydrochloride (Reference Synthetic Example 131), (4-methoxyphenyl)methanamine, piperidin-4-ol, 2-aminoethanol, 7-amino-2H-benzo[b][1 ,4]oxazine-3(4H)-one, 6-amino- 2H-benzo[b][1 ,4]oxazine-3(4H)-one, 2,2-difluorobenzo[d][1 ,3]dioxol-5-amine, (R)-2- amino-1-phenylethanol, (S)-2-amino-1 -phenylethanol, azetidine-3-carboxylic acid, 3- aminodihydrofuran-2(3H)-one hydrobromide, cyclopropylamine, azetidine-3-carbonitrile hydrochloride, 4-(2-aminoethyl)benzonitrile (Reference Synthetic Example 111), cyclobutanamine, cyclopentanamine, cyclopropylmethanamine, azetidine hydrochloride, pyrrolidine, (R)- 4-aminoisoxazolidin-3-one, (R)-(tetrahydrofuran-2-yl)methanamine, 2,2- dimethylcyclopropanamine hydrochloride, 2-methylcyclopropanamine, 1- (trifluoromethyl)cyclopropanamine, 1-(methoxymethyl)cyclopropanamine hydrochloride, oxetan-3-amine, 1-methylcyclopropanamine hydrochloride, dimethylamine hydrochloride, 2-(methylamino)ethanoi, 2,2'-azanediyl diethanol, (R)-tert-butyl pyrrolidin- 3-ylcarbamate, 3-(phenylamino)propanenitrile, (R)-pyrrolidine-3-carbonitrile hydrochloride, 3-(methylamino)propanenitrile, ( 1s,3R,4r,5S,7s)-4-aminoadamantan-1 -ol (Reference Synthetic Example3 129), (1s,3R,4s,5S,7s)-4-aminoadamantan-1-ol (Reference Synthetic Example 130), trans-4-aminocyclohexanol, 2- (cyclohexylamino)ethanol, tert-butyl (S)-pyrrolidin-3-ylcarbamate, 3-(4- chlorophenyl)oxetan-3-amine hydrochloride, 4-[4-chloro-3- (trifluoromethyl)phenyl]piperidin-4-ol, 4-phenylpiperidine-4-carbonitrile hydrochloride, 2- (piperidin-4-yl)propan-2-ol, cis-2-(aminomethyl)cyclohexanol hydrochloride, 1- (aminomethyl)cyclohexanol hydrochloride, 3-(piperazin-1 -yl)propanenitrile, 2-(piperazin- 1-yl)ethanol, bicyclo[1 . 1 .1]pentan-1 -amine hydrochloride, 1, 1 ,1,3,3,3-hexafluoropropan- 2-amine, (R)-N-(pyrrolidin-3-yl)acetamide, (S)-N-(pyrrolidin-3-yl)acetamide, (R)-2,2,2- trifluoro-N-(pyrrolidin-3-yl)acetamide hydrochloride, (S)-2,2,2-trifluoro-N-(pyrrolidin-3- yl)acetamide hydrochloride, 3-(4-fluorophenyl)oxetan-3-amine hydrochloride, 1-(4- fluorophenyl)cyclopropanamine hydrochloride, 1-(4-fluorophenyl)cyclobutanamine hydrochloride, 2-methoxy-N-methylethanamine, bis(2-methoxyethyl)amine, ( 1- aminocyclopropyl)methanol hydrochloride, 3,3-difluoropyrrolidine hydrochloride, methanamine hydrochloride, ethanamine hydrochloride, propan-2-amine, 2- methylpropan-2-amine, prop-2-yn-1 -amine, 4-(piperidin-4-yl)morpholine, tert-butyl 4- (aminomethyl)piperidine-l-carboxylate, tert-butyl (piperidin-4-ylmethyl)carbamate, tertbutyl (S)-3-aminopyrrolidine-1 -carboxylate, 3-fluoroazetidine hydrochloride, 3,3- difluoroazetidine hydrochloride, (R)-N,N-dimethylpyrrolidin-3-amine, 2-amino-N-(2,2,2- trifluoroethyl)acetamide hydrochloride, 2,2, 3,3,3-pentafluoropropan-1 -amine, 3-amino- 1, 1 ,1-trifluoropropan-2-ol, thietan-3-amine hydrobromide or 1-(ethylsulfonyl)piperazine was used instead of thiomorpholine 1, 1-dioxide to give the compounds of Synthetic Examples 247 to 345. The names, morphologies and yields of the synthesized compounds are shown in Tables 26 to 33. TABLE3 26 Ex Compound Name Morphology Yield 4-({[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 ]triazolo [ l ,5-c]pyrimidin - l -yl)cycloh 247 colorless solid 79% exyl]methyl}amino)-2-chlorobenzonitri le 4 - ({[trans - 4 - (7H-pyrrolo [3, 2 - e ] [1, 2 , 3 248 ]triazolotl, 5-c]pyrimidin-l-yl) cycloh pale pink solid 56% exyl] methyl} amino) -1-naphthonitrile N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] 249 triazolotl, 5-c]pyrimidin-l-yl) cyclohe colorless solid 47% xyl]methyl}-3, 4-difluoroaniline N- {ttrans-4- (7H-pyrrolo [ 3 , 2-e] [1, 2 , 3 ] 250 triazolo [l, 5-c]pyrimidin-l-yl) cyclohe colorless solid 65% xyl]methyl}-3, 4 , 5-trifluoroaniline N- {[trans-4- ( H-py ro o [3,2-e] [1, 2 , 3 ] triazolotl, 5-c]pyrimidin-l-yl) cyclohe 251 colorless solid 47% xyl]methyl}-4-fluoro-3-(trifluorometh yl)aniline 5-({ttrans-4- (7H-pyrr o1o [3,2-e] [1, 2 , 3 ]triazolo [ l ,5-c]pyrimidin - l -yl)cycloh 252 colorless solid 69% exyl]methyl} amino) -2-fluorobenzonitri le 3-({[trans-4-(7H-pyrrolot3, 2-e] tl, 2 , 3 ]triazolo 11,5-c] pyrimidin _ l-yl) cycloh 253 colorless solid 73% exyl]methyl} amino) dihydrothiophen-2 (3 H ) -one 3- {ttrans-4- (7H-pyrrolo t3, 2-e] [1, 2 , 3 ] 254 triazolo [1,5 c]pyrimidin-l-yl) cyclohe pale pink solid 21% xyl]methyl} thiazolidine N- {[trans-4- (7H-pyr ro1o [3 ,2-e] [1, 2 , 3 ] pale purple 255 triazolotl, 5-c]pyrimidin-l-yl) cyclohe 62% solid xyl]methyl}-2, 2-difluoroethanamine N- {[trans - 4 - (7H-pyrrolo [3, 2- e ] [1, 2 , 3 ] triazolo [1, 5-c]pyrimidin-l-yl) cyclohe 256 colorless solid 66% xyl]methyl}-3, 3 , 3-trifluoropropan-l-a mine 1- {[trans-4- (7H-pyrrolo 3 , 2-e] [1, 2 , 3 ] 257 triazolo [1, 5-c]pyrimidin - l -yl) cyclohe colorless solid 37% xyl]methyl}azetidin-3-ol 1- (trans-4 - {[4 - (trifluoromethyl) piper idin - l -yl]methyl} cyclohexyl) -7H-pyrro 258 colorless solid 94% 1o [3,2-e] [1, 2 , 3 ] triazolotl, 5~ c]pyrimi dine 2- ({[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 259 ]triazolotl, 5-c]pyrimidin - l -yl)cycloh colorless solid 27% exy1] ethy1}amino)acetonitri1e 4- {[trans-4- (7H-pyrrolo t3, 2-e] [1, 2 , 3 ] 260 triazolo [1, 5-c]pyrimidin-l-yl) cyclohe colorless solid 52% xyl]methyl}piperazin-2-one TABLE 27 TABLE 28 Ex Compound Name Morphology Yield 6-({[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 ]triazolo[l, 5-c]pyrimidin-l-yl)cycloh 274 pale pink solid 98 exyl]methyl}amino)-2H-benzo[b] [1, 4]ox azin-3 (4H) -one N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolotl, 5-c]pyrimidin-l-yl) cyclohe 275 colorless solid 63% xyl]methyl}-2, 2-difluorobenzo[d] [l, 3 ] dioxo 1-5-ami ne (R) - 2 - ({[trans-4- (7H-py rro1o [3,2-e] [ l ,2 , 3]triazolo[l, 5-c]pyrimidin-l-yl)cy 276 colorless solid 50% clohexyllmethyl} amino) -1-phenylethano 1 (S) -2- ( { [trans-4- (7H-py r o1o [3 ,2-e] [ 1 ,2 , 3]triazolo[l, 5-c]pyrimidin-l-yl)cy 277 colorless solid 73% clohexyllmethyl} amino) -1-phenylethano 1 1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolotl, 5-c]pyrimidin-l-yl) cyclohe 278 colorless solid 90% xyl]methyl}azetidine-3-carboxylic acid 3-({[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 ]triazolo [1, 5-c ]pyrimidin-l-yl) cycloh 279 colorless solid quant . exyl]methyl} amino) dihydrofuran-2 (3H)- one N- {[trans-4- (7H-py o1o [3,2-e] [1, 2 , 3 ] 280 triazolo[l, 5-c]pyrimidin-l-yl)cyclohe colorless solid 34% xyl]methyl}cyclopropanamine 1- {[trans-4- (7H-pyrr o1o [3,2-e] [1, 2 , 3 ] 281 triazolotl, 5-c]pyrimidin-l-yl)cyclohe colorless solid 46% xyl]methyl}azetidine-3-carbonitrile 4- [2- ( { [trans-4- (7H-p rro1o [3,2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl)cyc 282 colorless solid 54% lohexyl]methyl}amino)ethyl]benzonitri le N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] 283 triazolotl, 5-c]pyrimidin-l-yl)cyclohe colorless solid 70% xyl]methyl} cyclobutanamine N- {[trans-4- (7H-pyr ro1o [3,2-e] [1, 2 , 3 ] 284 triazolotl, 5-c]pyrimidin-l-yl)cyclohe colorless solid 63% xyl]methyl} cyclopentanamine 1- [trans-4 - (7H-pyrrolo 3 , 2-e] [l, 2 , 3]t 285 riazolo[l, 5-c]pyrimidin-l-yl) cyclohex colorless solid 53% yl]-N-(cyclopropylmethyl)methanamine l-[trans-4-(azetidin-l-ylmethyl)cyclo 286 hexyl]-7H-pyrrolo[3, 2-e] [l, 2 , 3]triazo colorless solid 60% 1o [1,5-c]pyrimidine TABLE 29 Ex Compound Name Morphology Yield l-[trans-4-(pyrrolidin-l-ylmethyl)cyc 287 lohexyl]-7H-pyrrolo[3 2-e] [l, 2 , 3]tria colorless solid 64% zo1o [1,5-c]pyrimidine (R) -4- ({[trans -4- (7H-pyrr o1o [3 ,2-e ] [ 1 ,2 , 3]triazolo[l, 5-c]pyrimidin-l-yl)cy 288 colorless solid 78% clohexyl]methyl} amino) isoxazolidi-n-3- on e 1- [trans-4- (7H-pyrrolo [3, 2-e] [l, 2 , 3]t riazolo [1, 5-c]pyrimidin-l-yl) cyclohex 289 colorless solid 6% y ] -N- {[(R) - etrahydrof uran-2-y 1] eth 1}methanamine N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl)cyclohe 290 colorless solid 44% xyl]methyl}-2, 2-dimethylcyclopropanam ine N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] 291 triazolo[l, 5-c]pyrimidin-l-yl) cyclohe colorless solid 53% xyl]methyl}-2-methylcyclopropanamine N- {[trans-4- (7H ~ pyrro 1o [3, 2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl) cyclohe 292 colorless solid 60% xyl] methyl }-1- (trifluoromethyl) cyclop ropanamine N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, , 3 ] triazolo[l, 5-c]pyrimidin-l-yl)cyclohe 293 colorless solid 52% xyl]methyl} -1- (methoxymethyl) cyclopro panamine N-{[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 ] 294 triazolo[l, 5-c]pyrimidin-l-yl) cyclohe colorless solid 0% xyl]methyl} oxetan-3-amine N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] 295 triazolo[l, 5-c]pyrimidin-l-yl) cyclohe colorless solid 25% xyl]methyl}-l-methylcyclopropanamine l-[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3]t 296 riazolo [1, 5~ c ] pyrimidin-l-yl) cyclohex colorless solid 43% ]- ,N-dimethylmethanamine 2- ({[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 297 ]triazolo [1, 5 c ]pyrimidin-l-yl) cycloh colorless solid 57% exyl]methyl} (methyl) amino) ethanol 2 , 2 ' - ( { [trans-4- (7H-py r o1o [3,2-e] [1, 298 2 , 3]triazolo[l, 5-c]pyrimidin-l-yl)cyc colorless solid 43% lohexyl]methyl}azanediyl)diethanol tert-butyl ((R)-l-{ [trans-4- (7H-pyrrolo [3, 2-e] [ 1 299 ,2 , 3]triazolo[l, 5-c]pyrimidin-l-yl)cy colorless solid 64% clohexyl]methyl}pyrrolidin-3-yl)carba mate TABLE 30 Ex Compound Name Morphology Yield 3- ({[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ]triazolo [1, 5 c]pyrimidin-l-yl) cycloh 300 colorless solid 72% exyl]methyl} (phenyl) amino) propaneni tr ile (R) -1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3]triazolo[l, 5-c]pyrimidin-l-yl)cyc 301 colorless solid 58% lohexyl]methyl}pyrrolidine-3-carbonit rile 3-({[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 ]triazolo[l, 5-c]pyrimidin-l-yl)cycloh 302 colorless solid 42% exyl]methyl} (methyl)amino)propanenitr ile (IS, 3R, 4r, 5S, 7S) -4- ({[trans-4- (7H-pyr ro1o [3,2-e] [1, 2 , 3]triazolo[l, 5-c]pyri 303 colorless solid 61% midin-l-yl) cyclohexyl] methyl} amino) ad aman an- 1-o 1 (IS, 3R, 4s, 5S, 7S) -4- ({[trans-4- (7H-pyr ro1o [3,2-e] [1, 2 , 3]triazolo[l, 5-c]pyri 304 colorless solid 53% midin-l-yl) cyclohexyl] methyl} amino) ad amantan-l-ol trans-4 - ( { [trans-4- (7H-pyrrolo [3, 2-e] 305 [1, 2 , 3]triazolo[l, 5-c]pyrimidin-l-yl) colorless solid 35% cyclohexyl]methyl}amino)cyclohexanol 2- ( { [trans-4- (7H-py rro1o [3,2-e] [1, 2 , 3 306 ]triazolo[l, 5-c]pyrimidin-l-yl) cycloh colorless solid 40% exyl]methyl} (cyclohexyl) amino) ethanol tert-buty 1 ((S) -1- {[trans-4- (7H-pyrr o1o [3 ,2-e] [ 1 307 ,2 , 3]triazolo[l, 5-c]pyrimidin-l-yl)cy colorless solid 69% clohexyl]methyl} pyrrolidin-3-yl) carba mate N- {[trans-4- (7H-pyr ro o [3,2-e] [1, , 3 ] triazolo[l, 5-c]pyrimidin-l-yl) cyclohe 308 colorless solid 72% xyl]methyl}-3-(4-chlorophenyl)oxetan- 3-ami ne 1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolotl, 5-c]pyrimidin-l-yl) cyclohe 309 colorless solid 54% xyl] methyl} -4- [4-chloro-3 - (trifluorom ethyl)phenyl]piperidin-4-ol 1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl) cyclohe 310 colorless solid 56% xyl]methyl}-4-phenylpiperidine-4-carb onitrile 2- (1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 ,3]triazolo[l, 5-c]pyrimidin-l-yl)cycl 311 colorless solid 59% ohexyl]methyl}piperidin-4-yl)propan-2 -o TABLE 3 1. Ex Compound Name Morphology Yield cis-2- [({[trans-4- (7H-pyrrolo [3, 2-e] [ 1 , 2 , 3]triazolo[l, 5-c]pyrimidin-l-yl)c 312 colorless solid 14% yclohexyl]methyl}amino)methyl]cyclohe xano 1 1- [({ [trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3]triazolo[l,5-c]pyrimidin-l-yl)cyclo 313 colorless solid 47% hexyl]methyl}amino)methyl]cyclohexano 1 3- (4- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 ,3]triazolo[l, 5-c]pyrimidin-l-yl)cycl 314 colorless solid 35% ohexyl]methyl}piperazin-l-yl)propanen itri1e 2-(4-{[trans-4-(7H-pyrrolo[3,2-e] [l,2 315 ,3]triazolo[l, 5-c]pyrimidin-l-yl)cycl colorless solid 35% ohexyl]methyl}piperazin-l-yl)ethanol N- {[trans-4- (7 py ro1o [3,2-e] [1, 2 , 3 ] triazoloil, 5-c]pyrimidin-l-yl) cyclohe 316 colorless solid 44% xy1]m ethy1}b icyc1o [1.1 . 1]pentan-l-ami ne N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, , 3 ] triazolo[l, 5-c]pyrimidin-l-yl) cyclohe 317 colorless solid 77% xyl]methyl}-l, 1 , 1 , 3 , 3 , 3-hexafluoropro pan-2-amine N- ((R) -1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3]triazolo[l, 5-c]pyrimidin-l-yl) 318 colorless solid 48% cyclohexyl]methyl}pyrrolidin-3-yl)ace tami de N- ((S) -1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3]triazolo[l, 5-c]pyrimidin-l-yl) 319 colorless solid 29% cyclphexyl]methyl) pyrrolidin-3-yl) ace tami de N- ((R) -1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3]triazolo[l, 5-c]pyrimidin-l-yl) 320 colorless solid 49% cyclohexyl]methyl}pyrrolidin-3-yl)-2, 2 , 2- r if1uor oac etami de N- ((S) -1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3]triazolo[l, 5-c]pyrimidin-l-yl) 321 colorless solid 48% cyclohexyl]methyl}pyrrolidin-3-yl)-2, 2 , 2-trifluoroacetamide N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl) cyclohe 322 colorless solid 52% xyl]methyl} -3- (4-fluorophenyl) oxetan- 3-amine N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl) cyclohe 323 colorless solid 39 xyl]methyl}-l-(4-fluorophenyl)cyclopr opanami n e TABLEa3 . 2 Ex Compound Name Morphology Yield N- {[trans -4- (7H-pyr ro1o [3 ,2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl) cyclohe 324 colorless solid 39% xyl]methyl}-l-(4-fluorophenyl)cyclobu tanamine N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolo [1, 5-c]pyrimidin-l-yl) cyclohe 325 colorless solid 71 xyl]methyl}-2-methoxy-N-methylethanam ine N- {[trans-4- (7H-pyrrolo [3, 2-e] [l, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl)cyclohe 326 colorless solid 76% xyl] methyl }-2-methoxy-N-(2-methoxyeth yl) ethanamine [1- ( { [trans-4- (7H-py rro1o [3,2-e] [1, 2 , 3]triazolo[l, 5-c]pyrimidin-l-yl)cyclo 327 colorless solid 58% hexyl]methyl} amino) cyclopropyl]methan o l l-{trans-4-[(3, 3-difluoropyrrolidin-l 328 -yl)methyl]cyclohexyl}-7H-pyrrolo[3, 2 colorless solid 26% -e] [1, 2 , 3]triazolo[l, 5-c]pyrimidine 1- [trans-4- (7H-pyrrolo [3, 2-e] [l, 2 , 3]t 329 riazolo[l, 5-c]pyrimidin-l-yl)cyclohex colorless solid 26% yl]-N-methylmethanamine N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, , 3 ] 330 triazolo[l, 5-c]pyrimidin-l-yl) cyclohe colorless solid 58% xyl]methyl) ethanamine N- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] 331 triazolo[l, 5-c]pyrimidin-l-yl) cyclohe colorless solid 55% xyl]methyl}propan-2-amine N-{[trans-4-(7H-pyrrolo[3, 2-e] [l, 2 , 3 ] 332 triazolo [1, 5-c]pyrimidin-l-yl) cyclohe colorless solid 34% xyl] eth l}-2-methylpropan-2-amine N- {[trans-4- (7H-py ro1o [3,2-e] [1, 2 , 3 ] 333 triazolo[l, 5-c]pyrimidin-l-yl) cyclohe colorless solid 62% xyl]methyl}prop-2-yn-l-amine 4- (1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 ,3]triazolo[l, 5-c]pyrimidin-l-yl)cycl 334 colorless solid 44% ohexyl]methyl}piperidin-4-yl)morpholi ne tert-buty 1 4- [({[trans-4- (7H-pyrrolo [3, 2-e] [1, , 335 3 ] triazolo [1, 5-c]pyrimidin-l-yl) cyclo colorless solid 17% hexyl]methyl}amino)methyl]piperidine- 1-carboxylate tert-buty 1 [(1- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 336 3 ] triazolo [1, 5-c ]pyrimidin-l-yl) cyclo colorless solid 3 . 0% hexyl]methyl}piperidin-4-yl)methyl]ca rbamat e TABLE 33 SYNTHETIC EXAMPLE 346 trans-4-(7H-Pyrrolor3.2-e1f1,2.3¾riazolon ,5-ctoyrimidin-1 -yl)-N-(3.3,3-trif luoro-2- hvdroxy-2-phenylpropyl)cvclohexanecarboxamide trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexanecarboxylic acid (10.0 mg, 0.0350 mmol) obtained in Synthetic Example 80 in N,Ndimethylformamide ( 1 mL) was mixed with 1-(3-dimethylaminopropyl)-3- ethylcarbodiimide hydrochloride (8.10 mg, 0.0420 mmol), 1-hydroxybenzotriazole (4.70 mg, 0.0350 mmol) and 3-amino-1 , 1 ,1-trifluoro-2-phenylpropan-2-ol (7.20 mg, 0.0350 mmol) obtained in Reference Synthetic Example3 101 and stirred at room temperature for one day. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate, The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate / hexane = 1/1 (v/v)) to give the title compound as a colorless solid (5.80 mg, yield 35%). SYNTHETIC EXAMPLE3 347 trans-4-(7H-Pyrrolor3,2-e1M ,2.31triazolon ,5-c1pyrimidin-1 -yl)-N-r3.3.3-trifluoro-2-(4- fluorophenyl)-2-hvdroxypropyncvclohexanecarboxamide The reactions in Synthetic Example 346 were carried out in substantially the same manners except that 3-amino-1 , 1 ,1-trifluoro-2-(4-fluorophenyl)propan-2-ol obtained in Reference Synthetic Example 102 was used instead of 3-amino-1 , 1 ,1- trifluoro-2-phenylpropan-2-ol to give the title compound as a colorless solid (7.37 mg, yield 43%). SYNTHETIC EXAMPLE3 348 TO 363 The reactions in Synthetic Example 206 were carried out in substantially the same manners except that ammonium chloride, 5-methylfurfurylamine, 4- (aminomethyl)benzonitrile hydrochloride, 2-phenylglycinonitrile hydrochloride, 2-(4- chlorophenyl)ethylamine, (S)-2-amino-1 -phenylethanol, 2,2,2-trifluoroethylamine hydrochloride, 2-aminoacetonitrile hydrochloride, 3-aminopropionitrile, (S)-pyrrolidine-3- carbonitrile, (S)-pyrrolidine-3-ol, cyclopropylamine, 2-aminoethanol, 3-hydroxyazetidine hydrochloride, 4-(2-aminoethyl)benzonitrile or azetidine-3-carbonitrile hydrochloride was used instead of 4-fluoroaniline to give the compounds of Synthetic Examples 348 to 363. The names, morphologies and yields of the synthesized compounds are shown in Tables 34 to 35. TABLE 34 Ex Compound Name Morphology Yield trans-4- (7 H-py rro1o [3,2-e] [l, 2 , 3]tria 348 zolo [1, 5-c]pyrimidin-l-yl) cyclohexane colorless solid 87 % carboxami de trans-N-[(5-methylfuran-2-yl)methyl]- 4- ( 7 H-pyrrolo[3, 2-e] [l, 2 , 3]triazolo[l 349 colorless solid 69% ,5~ c ]pyrimidin-l-yl) cyclohexanecarbox amide trans -N- (4-cyanobenzyl) -4- ( 7 H-pyrrolo 350 [3, 2-e] [1, 2 , 3]triazolo[l, 5-c]pyrimidi colorless solid 57 % n-1-y1)cyclohexanecarboxamide trans -N- [cyano (phenyl )methyl ]-4- ( 7 H-p 351 yrrolo[3, 2-e] [1, 2 , 3]triazolo[l, 5-c]py colorless solid 58% rimidin-l-yl) cyclohexanecarboxamide trans-N- (4-chlorophenethyl) -4- ( 7 H-pyr pale yellow 352 ro1o [3,2-e] [1, 2 , 3]triazolo[l, 5-c]pyri 68% solid midin-l-yl)cyclohexanecarboxamide trans-N-[(S)-2-hydroxy-2-phenyl ethyl] -4- ( 7 H-pyrrolo[3, 2-e] [l, 2 , 3]triazolo[ 353 colorless solid 40% 1 , 5-c]pyrimidin-l-yl) cyclohexanecarbo xamide TABLE3 35 SYNTHETIC EXAMPLES3 364 TO 366 The reactions in Synthetic Example 77 were carried out in substantially the same manners except that sodium benzene sulfinate, sodium 4-fluorobenzenesulfinate or sodium cyclopropanesulfinate was used instead of sodium methanesulfinate to give the compounds of Synthetic Examples3 364 to 366. The names, morphologies and yields of the synthesized compounds are shown in Table3 36. TABLE 36 SYNTHETIC EXAMPLE 367 1-rtrans-4-(lodomethyl)cvclohexyl1-7H-pyrrolor3,2-e1[1 ,2,31triazoloH ,5-clpyrimidine 2,3-Dichloro-5,6-dicyano-p-benzoquinone (50.0 mg, 0.221 mmol) and triphenylphosphine (58.0 mg, 0.221 mmol) in dichloromethane (3 mL) were mixed with tetrabutylammonium iodide (81 .7 mg, 0.221 mmol) and [trans-4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyirimidin-1-yl)cyclohexyl]methanol (50.0 mg, 0.184 mmol) obtained in Synthetic Example 3 10 and then was stirred at 40°C for 8 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 3/2 (v/v)) to give the title compound as a colorless solid (51 .9 mg, yield 74%). SYNTHETIC EXAMPLE 368 1-(trans-4-{f(Trifluoromethyl)sulfonvnmethyl)cvclohexyl)-7H-pyrrolo[3,2- e ,2,31triazolof 1,5-clpyrimidine 1-[trans-4-(lodomethyl)cyclohexyl]-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (50.0 mg, 0.131 mmol) and sodium trif!uoromethylsulfinate (205 mg, 1.31 mmol) in N,Ndimethylformamide( 3 mL) were stirred at 100°C for 26 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer washed with saturated aqueous sodium hydrogen carbonate, saturated aqueous ammonium chloride and saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/2 1/1 (v/v)) and preparative HPLC (Waters XBridge Prep C18 m ODS, 9x 100mm, acetonitrile / 0.1% aqueous formic acid solution = 20/80 80/20(v/v)) to give the title compound as a colorless solid (6.30 mg, yield 12%). SYNTHETIC EXAMPLE 3 369 1-ftrans-4-(Azidomethyl)cvclohexyn-7H-pyrrolor3,2-e1[1 ,2,31triazolon ,5-clpyrimidine 1-[trans-4-(Bromomethyl)cyclohexyl]-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- cjpyrimidine (50.0 mg, 0.150 mmol) obtained in Synthetic Example 3 74 in tetrahydrofurane (2 mL) was mixed with trimethylsilylazide (39.0 L, 0.299 mmol) and tetrabutylammonium fluoride - tetrahydrofuran solution ( 1 M, 299 pL, 0.299 mmol) and then stirred at 50°C for 3 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was washed with ethyl acetate / hexane (1/5 (v/v)) to give the title compound as a colorless solid (30.6 mg, yield 69%). SYNTHETIC EXAMPLE 370 2-( 1-(rtrans-4-(7H-Pyrrolor3,2 -e ,2,31triazoloM ,5-c1pyrimidin-1 -vDcvclohexyllmethyl)- 1H-1 ,2,3-triazol-4-yl)propan-2-ol 1-[trans-4-(Azidomethyl)cyclohexyl]-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidine (30.0 mg, 0.1 0 1 mmol) and 2-methyl-3-butyn-2-ol (12.0 , 0.122 mmol) in dichloromethane (3 ml_) were mixed with copper(ll) sulfate (24.0 mg, 0.152 mmol) and sodium ascorbate (60.0 mg, 0.304 mmol) and then stirred at 80°C for 2 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium hydrogen carbonate, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 4/1 0/1 ethyl acetate / methanol=20/1 (v/v)) to give the title compound as a colorless solid (13.2 mg, yield 34%). SYNTHETIC EXAMPLE 371 rtrans-4-(7H-Pyrrolor3,2-elf1 ,2,31triazoloi1 ,5-clpyrimidin-1 -vDcyclohexyllmethanamine 1-[trans-4-(Azidomethyl)cyclohexyl]-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidine (127 mg, 0.427 mmol) obtained in Synthetic Example 369 and 5% palladium-carbon (12.7 mg) in methanol (3 mL) and dichloromethane (3 mL) were stirred at room temperature for 4 hours under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / methanol=1/0 10/1 (v/v/) to give the title compound as a colorless solid (95.0 mg, yield 82%). SYNTHETIC EXAMPLE 372 N-(itrans-4-(7H-Pyrrolo[3,2 -ei ,2,31triazolof1,5-c1pyrimidin-1 -yl)cvclohexyl1methyl)-2- cvanoacetamide [trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexyl]methanamine (40.0 mg, 0.148 mmol), 2-cyanoacetic acid (15.0 mg, 0.1 78 mmol) and 0-(7-azabenzotriazol-1-yl)-N,N >N',N'-tetramethyluronium hexafluorophosphate (68.0 mg, 0.1 78 mmol) in N,N-dimethylformamide (2 mL) were mixed with N,N-diisopropylethylamine (57.0 , 0.326 mmol) and stirred at room temperature for 16 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium hydrogen carbonate, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / acetone = 1/1 2/3 (v/v)) to give the title compound as a colorless solid ( .4 mg, yield 23%). SYNTHETIC EXAMPLE 3 373 N-(ftrans-4-(7H-Pyrrolo[3,2 -ei ,2,31triazoloM ,5-c1pyrimidin-1 -vPcvclohexyllmethyl)- 3,3,3-trifluoropropanamide The reactions in Synthetic Example 372 were carried out in substantially the same manners except that 3,3,3-trifluoropropanoic acid was used instead of 2- cyanoacetic acid to give the title compound as a colorless solid (5.00 mg, yield 12%). SYNTHETIC EXAMPLE 3 374 1-(1 -f(3-Chloro-5-methyl-1 -(2.2.2-trifluoroethyl)-1 H-pyrazol-4-yl)methvnpiperidin-4-yll- 7H-pyrrolor3 ,2-e1f1,2,31triazolori ,5-clPyrimidine 3-Chloro-5-methyl-1 H-pyrazole-4-carbaldehyde (100 mg, 0.692 mmol) in N,Ndimethylformamide (2 mL) was mixed with potassium carbonate (287 mg, 2.08 mmol) and 2,2,2-trifluoroethyl trifluoromethanesulfonate (200 L, 1.38 mmol) and stirred at room temperature for 1 day. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with chloroform. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue and 1-(piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine acetate (20.0 mg, 0.0660 mmol) obtained in Reference Synthetic Example 104 were dissolved in methanol ( 1 ml_) and mixed with nicotinic acid (12.3 mg, 0.0990 mmol) and 2-picoline borane ( 10.7 mg, 0.0990 mmol). The reaction mixture was stirred at room temperature for 1 day. After addition of 1 M aqueous sodium hydroxide, the reaction mixture was extracted with chloroform. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (methanol / chloroform = 1/1 0 (v/v)) to give the title compound as a colorless solid (2.35 mg, yield 8%). SYNTHETIC EXAMPLE 375 4-(2 -r4-(7H-Pyrrolor3,2-eiri ,2,31triazoloM ,5-c1pyrimidin-1 -yl)piperidin-1 - yllethyDbenzonitrile The reactions in Synthetic Example 32 were carried out in substantially the same manners except that 4-cyanophenethyl 4-methylbenzenesulfonate (Reference Synthetic Example 3 132) was used instead of benzyl bromide to give the title compound as a colorless solid (7.03mg, yield 29%). SYNTHETIC EXAMPLE 3 376 4-[4-(7H-Pyrrolo[3,2 -e ,2,31triazolof 1,5-c1pyrimidin-1 -yl)piperidin-1 -yllbenzonithle 1-(Piperidin-4-yl)-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine acetate (30.0 mg, 0.0992 mmol) obtained in Reference Synthetic Example 3 104 in N,N-dimethylformamide ( 1 mL) was mixed with 4-fluorobenzonitrile ( 18.0 mg, 0.149 mmol) and potassium carbonate (27.4 mg, 0.1 98 mmol) and then stirred at 80°C for 3 1 hours. After addition of water, the reaction mixture was extracted with chloroform. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (methanol / chloroform = 1/1 9 (v/v)) to give the title compound as a colorless solid (0.520mg, yield 2%). SYNTHETIC EXAMPLE 377 4-(f4-(9-Chloro-7H-pyrrolor3.2-eli1 .2,31triazolon ,5-clpyrimidin-1 -yl)piperidin-1 - yllmethyPbenzonitrile 4-{[4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)piperidin-1 - yl]methyl}benzonitrile (20.0 mg, 0.0660 mmol) obtained in Synthetic Example 34 in N,N-dimethylformamide ( 1 mL) was mixed with N-chlorosuccinimide ( 0.7 mg, 0.0990 mmol) and stirred at room temperature for 1 day. After addition of 1M aqueous sodium hydroxide, the reaction mixture was extracted with chloroform. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (methanol / chloroform = 1/10 (v/v)) to give the title compound as a colorless solid (13.1 mg, yield 48%). SYNTHETIC EXAMPLES 3 378 TO 380 The reactions in Synthetic Example 121 were carried out in substantially the same manners except that ( 1 R,2S)-1 -amino-2,3-dihydro-1 H-inden-2-ol, ( 1S,2R)-1- amino-2,3-dihydro-1 H-inden-2-ol or 3,3'-azanediyldipropanenitrile was used instead of 4-aminobenzonitrile to give cis/trans mixture of the compounds of Synthetic Examples 378 to 380. The names, morphologies and yields of the compounds synthesized are shown in Table 3 37. TABLE 37 SYNTHETIC EXAMPLES3 381 TO 384 The reactions in Synthetic Example 136 were carried out in substantially the same manners except that 4-fluoroaniline, 2-bromo-2,2-difluoroethanamine hydrochloride (Reference Synthetic Example 131), 2,2,3,3,3-pentafluoropropylamine or 2-amino-N-(2,2,2-trifluoroethyl)acetamide was used instead of 3-phenylpropan-1 -amine to give the compounds of Synthetic Examples 381a to 384a in less polar fractions and the compounds of Synthetic Examples3 381b to 384b in more polar fractions. The names, morphologies and yields of the compounds synthesized are shown in Table 38. TABLE 38 SYNTHETIC EXAMPLES 385 TO 400 The reactions in Synthetic Example 136 were carried out in substantially the same manners except that 3-amino-1 , ,1-trifluoro-2-(pyridin-3-yl)propan-2-ol, 3-amino- 1, 1 , 1 -trifluoro-2-[4-(methylthio)phenyl]propan-2-ol, 3-amino-1 , 1 ,1-trifluoro-2-(6- methoxypyridin-3-yl)propan-2-ol, 3-amino-1 , 1 ,1-trifluoro-2-(4-methoxyphenyl)propan-2- ol, [trans-2-(4-fluorophenyl)cyclopropyl]methanamine, 3-amino-2-(3,4- dimethoxyphenyl)-1 , 1 , 1 -trifluoropropan-2-ol, 4-(2-aminoethyl)benzonitrile, cyclopropylamine, 2-aminoacetonitrile hydrochloride, 3-aminopropanenitrile, 2,2,2- trifluoroethanamine hydrochloride, cyclopropylmethanamine, dimethylamine (2M solution in tetrahydrofuran), methanamine (2M solution in methanol), 2,2- difluoroethanamine or 1, 1 , 1 ,3,3,3,-hexafluoropropan-2-amine was used instead of 3- phenylpropan-1 -amine to give the compounds of Synthetic Examples 385b to 400b in more polar fractions. The names, morphologies and yields of the compounds synthesized are shown in Tables 39 to 40. TABLE 39 Ex Compound Name Morphology Yield 3- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl)cyclohe 385b colorless solid 30% xy1]ami no }- 1,1 , 1- rif1uor o 2- (p y i in - 3-y1)propan-2-ol 3- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolo [1, 5-c]pyrimidin-l-yl) cyclohe 386b colorless solid 3 xyl] amino} -1, 1 , 1-tr if1uor o-2- [4- (me th ylthio)phenyl]propan-2-ol 3- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolo [1, 5-c]pyrimidin-l-yl) cyclohe 387b colorless solid 26% x 1]am ino}-1,1 , 1-tr if1uor o 2- (6-me ho xypyridin-3-yl)propan~2-ol 3- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl) cyclohe 388b colorless solid 38% y1]ami no}-1,1 , 1-tr if1uor o 2- (4-me ho xyphenyl) propan-2-ol trans-N- {[trans-2 - (4-fluorophenyl) eye lopropyl]methyl}-4-(7H-pyrrolo[3, 2-e] 389b colorless solid 16% [1, 2 , 3]triazolo[l, 5-c]pyrimidin-l-yl) cyclohexanamine 3- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 , 3 ] triazolo[l, 5-c]pyrimidin-l-yl)cyclohe 390b colorless solid 12% xyl]amino}-2-(3, 4-dimethoxyphenyl)-l, 1 , 1-1rif1uor opr opan-2 -o 1 4- (2- {[trans-4- (7H-pyrrolo [3, 2-e] [1, 2 391b ,3]triazolo[l, 5-c]pyrimidin-l-yl)cycl colorless solid 12% ohexyl]amino} ethyl)benzonitrile tran s-N-c yc1opr o y1-4- (7H-py ro1o [3,2 392b -e] [1, 2 , 3]triazolo[l, 5-c]pyrimidin-l colorless solid 26% yl) cyclohexanamine 2- {[trans-4- (7H-p yr o1o [3,2-e] [1, 2 , 3 ] pale yellow 393b triazolo[l, 5-c]pyrimidin-l-yl)cyclohe 15% solid xyl] amino} acetonitrile 3- {[trans-4- ( H- yrro1o [3 ,2-e] [1, 2 , 3 ] pale yellow 394b triazolo[l, 5-c]pyrimidin-l-yl)cyclohe 8 . 0% solid xyl] amino} propanen itrile trans-4- (7H-pyrrolo [3, 2-e] [l, 2 , 3]tria 395b zolo [1, 5-c]pyrimidin-l-yl) -N- (2, 2 , 2-t colorless solid 15% rifluoroethyl) cyclohexanamine trans-N-(cyclopropylmethyl)-4-(7H-pyr 396b ro1 [3,2-e] [1, 2 , 3]triazolo[l, 5-c]pyri pale brown solid 40% midin-l-yl) cyclohexanamine trans-N, N-dimethyl -4- (7H-pyrrolo [3, 2- pale yellow 397b e ] [1, 2 , 3]triazolo[l, 5-c]pyrimidin-l-y 27% solid 1)cyc1ohexanami ne TABLE 40 SYNTHETIC EXAMPLE 401 rcis-4-(7H-Pyrrolof3,2-e1f1 ,2,31triazolo[1 ,5-c1pyrimidin-1 -vDcvclohexyllmethanol The reactions in Synthetic Example 3 141 were carried out in substantially the same manners except that 1-(cis-4-{[(tert-butyldimethylsilyl)oxy]methyl}cyclohexyl)-7Hpyrrolo[ 3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (Reference Synthetic Example 135a) was used instead of 1-(trans-4-{[(tert-butyldimethylsilyl)oxy]methyl}cyclohexyl)-7Hpyrrolo[ 3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine to give the title compound as a pale pink solid (297 mg, yield 57%). SYNTHETIC EXAMPLE 3 402 cis-4-(7H-Pyrrolor3,2-e1[1 ,2,31triazolof1,5-clpyrimidin-l -vQcvclohexanecarbaldehvde The reactions in Synthetic Example 78 were carried out in substantially the same manners except that [cis-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexyl]methanol was used instead of [trans-4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]methanol to give the title compound as a colorless solid ( 92 mg, yield 88%). SYNTHETIC EXAMPLE 403 1-{[cis-4-(7H-Pyrrolof3,2-e1[1 ,2,31triazoloi1 ,5-clpyrimidin-1 -vDcvclohexyllmethyllazetidin- 3zOl cis-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexanecarbaldehyde (30.0 mg, 0.111 mmol) in methanol (2 mL), tetrahydrofuran ( 1 mL) and acetic acid ( 100 L) was mixed with 3-hydroxyazetidine hydrochloride (41 .3 mg, 0.334 mmol) and stirred at room temperature for 1 hour. The reaction mixture was mixed with 2-picoline borane (23.8 mg, 0.334 mmol) and stirred at room temperature for 14 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The aqueous layer was adjusted to pH 10 with 1 M aqueous sodium hydroxide, and extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was washed with hexane / ethyl acetate (5/1 (v/v)) to give the title compound as a colorless solid (7.40 mg, yield 31%). SYNTHETIC EXAMPLES 3 404 TO 406 The reactions in Synthetic Example 403 were carried out in substantially the same manners except that (S)-pyrrolidin-3-ol hydrochloride, (R)-pyrrolidin-3-ol hydrochloride or cyclopropylamine hydrochloride (Reference Synthetic Example 3 136) was used instead of 3-hydroxyazetidine hydrochloride to give the compounds of Synthetic Examples 404 to 406. The names, morphologies and yields of the compounds synthesized are shown in Table 4 . TABLE 4 1 SYNTHETIC EXAMPLE 407 N-(ftrans-4-(7H-Pyrrolof3,2-e1f1 ,2.31triazolof1 ,5-c1pyrimidin-1-yl)cvclohexyl1methyl)-2- cvano-N-(2,2,2-trifluoroethyl)acetamide N-{[trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexyl]methyl}-2,2,2-trifluoroethanamine (20.0 mg, 0.0567 mmol) obtained in Synthetic Example 188 in N,N-dimethylformamide ( 1 mL) was mixed with 2- cyanoacetic acid (9.60 mg, 0.1 13 mmol) and O-(7-azabenzotriazol-1-yl)-N,N,N',N'- tetramethyluronium hexafluorophosphate (45.0 mg, 0.113 mmol) and stirred with N,Ndiisopropylethylamine (0.0346 mL, 0.198 mmol) at room temperature for 2 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 6/1 (v/v)) to give the title compound as a colorless solid (23.6 mg, yield 99%). SYNTHETIC EXAMPLES3 408 TO 4 10 The reactions in Synthetic Example3 407 were carried out in substantially the same manners except that 2-({[trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin- 1-yl)cyclohexyl]methyl}amino)acetonitrile (Synthetic Example 259), N-{[trans-4-(7Hpyrrolo[ 3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]methyl}cyclopropanamine (Synthetic Example3 280) or 1-[trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin- 1-yl)cyclohexyl]-N-[(5-methylfuran-2-yl)methyl]methanamine (Synthetic Example 182) was used instead of N-{[trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexyl]methyl}-2,2,2-trifluoroethanamine to give the compounds of Synthetic Examples 408 to 4 0. The names, morphologies and yields of the compounds synthesized are shown in Table3 42. TABLE 42 SYNTHETIC EXAMPLE 4 N-(itrans-4-(7H-Pyrrolor3,2-eiri .2.31triazoloM .5-clPyrimidin-l -vDcvclohexyllmethyl)- 3,3,3-trifluoro-N-(2,2,2-trifluoroethyl)propanamide The reactions in Synthetic Example 407 were carried out in substantially the same manners except that 3,3,3-trifluoropropionic acid was used instead of 2- cyanoacetic acid to give the title compound as a colorless solid (8.80 mg, yield 33%). SYNTHETIC EXAMPLE3 412 N-(rtrans-4-(7H-Pyrrolo[3,2-elf 1,2.31triazoloM .5-c1pyrimidin-1 -vOcvclohexyllmethyD-N- (cvanomethyl)-3,3,3-trifluoropropanamide The reactions in Synthetic Example 4 11 were carried out in substantially the same manners except that 2-({[trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin- 1-yl)cyclohexyl]methyl}amino)acetonitrile (Synthetic Example 259) was used instead of N-{[trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]methyl}- 2,2,2-trifluoroethanamine to give the title compound as a colorless solid (6.40 mg, yield 64%). SYNTHETIC EXAMPLE3 413 trans-N-(Cvclopropylmethyl)-4-(7H-pyrrolor3.2-e1f 1.2,31triazoloH ,5-c1pyrimidin-1 -yl)-N- (2,2,2-trifluoroethyl)cvclohexanamine trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)-N-(2,2,2- trifluoroethyl)cyclohexanamine (5.00 mg, 0.0148 mmol) obtained in Synthetic Example 3 395 in methanol ( 1 mL) and acetic acid (0.1 mL) was mixed with cyclopropanecarbaldehyde ( .60 L, 0.0222 mmol) and 2-picoline borane (2.30 mg, 0.0222 mmol) and stirred at room temperature for 1 day. After addition of 1 M aqueous sodium hydroxide, the reaction mixture was extracted with ethyl acetate. The orgnic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 1/3 1/1 (v/v)) to give the title compound as a colorless solid (4.00 mg, yield 70%). SYNTHETIC EXAMPLES 4 14 AND 4 15 The reactions in Synthetic Example3 413 were carried out in substantially the same manners except that 2-({[trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin- 1-yl)cyclohexyl]methyl}amino)acetonitrile (Synthetic Example3 259) or N-{[trans-4-(7Hpyrrolo[ 3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]methyl}-2,2,2- trifluoroethanamine (Synthetic Example 188) was used instead of trans-4-(7Hpyrrolo[ 3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)-N-(2,2,2-trifluoroethyl)cyclohexanamine to give the compounds of Synthetic Examples 414 and 415. The names, morphologies and yields of the compounds synthesized are shown in Table 43. TABLE3 43 SYNTHETIC EXAMPLE 416 [trans-4-(7H-Pyrrolof3,2-ein ,2,31triazolof ,5-clpyrimidin-l -vDcyclohexyllmethanesulfonic acid S-[trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]methyl ethanethioate (127 mg, 0.390 mmol) obtained in Synthetic Example 7 1 in methanol (4 mL) was mixed with ammonium molybdate tetrahydrate (145 mg, 0.117 mmol) and hydrogen peroxide solution (0.63 mL, 7.80 mmol) and stirred at room temperature for 1day. The reaction mixture was mixed with saturated aqueous sodium thiosulfate, concentrated under reduced pressure and purified by silica gel column chromatography (ethyl acetate / methanol = 4/1 1/1 (v/v)). The resulting solid was mixed with water and extracted with n-butanol. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give the title compound as a pale yellow solid (39.8 mg, yield 28%). SYNTHETIC EXAMPLE 417 1-rtrans-4-(7H-Pyrrolof3.2-e1i1 ,2.31triazolof1,5-clpyrimidin-1 -vPcyclohexyll-Ncyclopropylmethanesulfonamide [trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexyl]methanesulfonic acid (17.8 mg, 0.0530 mmol) in dichloromethane ( 1 .5 mL) and N,N-dimethylformamide ( 1 .8 mL) was stirred with thionyl chloride (0.00770 mL, 0.106 mmol) at room temperature for 1 hour. The reaction mixture was concentrated under reduced pressure. The residue was dissolved in dichloromethane ( .0 mL) and mixed with N,N-diisopropylethylamine (0.0923 mL, 0.530 mmol) and cyclopropylamine (0.0148 mL, 0.212 mmol) under cooling with ice and then stirred at room temperature for 1 day. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl hexane / acetate = 4/1 1/1 1/3 (v/v)) to give the title compound as a brown solid ( 1.50 mg, yield 7.5%). SYNTHETIC EXAMPLES 4 18 TO 420 The reactions in Synthetic Example3 417 were carried out in substantially the same manners except that dimethylamine hydrochloride, 2-aminoacetonitrile hydrochloride or 2,2,2-trifluoroethanamine hydrochloride was used instead of cyclopropylamine to give the compounds of Synthetic Examples3 4 18 to 420. The names, morphologies and yields of the compounds synthesized are shown in Table 44. TABLE 3 44 SYNTHETIC EXAMPLE 3 421 1-(trans-4-(r3-(2,2,2-Trifluoroethoxy)azetidin-1 -vnmethyl)cvclohexyl)-7H-pyrrolor3.2- e f 1 ,2,31triazolo[1 ,5-ctoyrimidine tert-Butyl 3-(2,2,2-trifluoroethoxy)azetidine-1-carboxylate (350 mg, 1.37 mmol) obtained in Reference Synthetic Example 116 in ethyl acetate ( 1 mL) was mixed with 4 M hydrogen chloride - 1,4-dioxane solution (3 mL) under cooling with ice and then stirred at room temperature for 2 hours. The reaction mixture was concentrated to give a colorless oil (224 mg). The resulting colorless oil (64.0 mg) was dissolved in methanol (2 mL), tetrahydrofuran ( 1 mL) and acetic acid (100 L) and stirred with trans- 4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexanecarbaldehyde (30.0 mg, 0.11 1 mmol) obtained in Synthetic Example 78 at room temperature for 1 hour. The reaction mixture was mixed with 2-picoline borane (23.8 mg, 0.334 mmol) and stirred at room temperature for 14 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The aqueous layer was adjusted to pH 0 with 1 M aqueous sodium hydroxide, and extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was washed with hexane / ethyl acetate (5/1 (v/v)) to give the title compound as a light purple solid (14.9 mg, yield 33%). SYNTHETIC EXAMPLES 422 TO 424 The reactions in Synthetic Example 421 were carried out in substantially the same manners except that tert-butyl 3-hydroxy-3-methylazetidine-1-carboxylate (Reference Synthetic Example 113), tert-butyl 3-(dimethylamino)azetidine-1- carboxylate (Reference Synthetic Example 3 137) or tert-butyl 3- [ethyl(methyl)amino]azetidine-1-carboxylate (Reference Synthetic Example 138) was used instead of tert-butyl 3-(2,2,2-trifluoroethoxy)azetidine-1-carboxylate to give the compounds of Synthetic Examples 3 422 to 424. The names, morphologies and yields of the compounds synthesized are shown in Table 45. TABLE 45 SYNTHETIC EXAMPLE 425 1-(ftrans-4-(7H-Pyrrolof3,2 -ei ,2,31triazoloH ,5-c1pyrimidin-1 -yl)cvclohexynmethyl)-3- (trifluoromethyl)azetidin-3-ol The reactions in Synthetic Example 88 were carried out in substantially the same manners except that 3-(trifluoromethyl)azetidin-3-ol hydrochloride (Reference Synthetic Example 5) was used instead of thiomorpholine 1, 1-dioxide to give the title compound as a colorless solid (11 .9 mg, yield 27%). SYNTHETIC EXAMPLE 426 1-(ftrans-4-(7H-Pyrrolor3,2-e1f 1,2,31triazoloM ,5-c1pyrimidin-1 -yl)cvclohexyllmethyll-N- (2,2,2-trifluoroethyl)azetidine-3-carboxamide 1-{[trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexyl]methyl}azetidine-3-carboxylic acid (40.0 mg, 0.1 3 mmol) obtained in Synthetic Example 3 278 and 2,2,2-trifluoroethanamine hydrochloride (19.9 mg, 0.147 mmol) in N,N-dimethylformamide (2 mL) were mixed with N,N-diisopropylethylamine (74.9 L, 0.440 mmol) and (1-cyano-2-ethoxy-2-oxoethylidenaminooxy)dimethylaminomorpholino- carbenium hexafluorophosphate (62.8 mg, 0.147 mmol) and stirred at room temperature for 1 day. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with ethyl acetate. The organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was washed with hexane / chloroform (3/1 (v/v)) to give the title compound as a pale yellow solid (5.40 mg, yield 11%). SYNTHETIC EXAMPLE 3 427 N-([trans-4-(7H-Pyrrolor3,2 -eiri ,2.31triazolof1.5-c1pyrimidin-1 - vOcvclohexynmethvUmethanesulfonamide [trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexyl]methanamine (20.0 mg, 0.0740 mmol) obtained in Synthetic Example 3 371 in dichloromethane (2 mL) was mixed with methanesulfonyl chloride (13.8 L, 0.0814 mmol) under cooling with ice and then stirred at room temperature for 65 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The aqueous layer was washed with 1 M hydrochloric acid and saturated aqueous ammonium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was washed with chloroform / hexane (1/5 (v/v)) to give the title compound as a colorless solid (6.00 mg, yield 23%). SYNTHETIC EXAMPLE 3 428 tert-Butyl 3-((rtrans-4-(7H-pyrrolor3,2-e1M ,2,31triazolon .5-clpyrimidin-1- yl)cvclohexyllmethyl)amino)-3-(cvanomethyl)azetidine-1-carboxylate [trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexyl]methanamine (11 .2 mg, 0.0414 mmol) obtained in Synthetic Example 371 and tert-butyl 3-(cyanomethylene)azetidine-1 -carboxylate ( 10.4 mg, 0.0535 mmol) obtained in Reference Synthetic Example 139 in acetonitrile (2 mL) were mixed with 1,8-diazabicyclo[5.4.0]undec-7-ene (12.0 _, 0.0535 mmol) and stirred at room temperature for 1 day. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (NH-silica gel manufactured by Fuji Silysia Chemical Ltd.; chloroform / methanol = 20/1 (v/v)) to give the title compound as a pale yellow solid (14.2 mg, yield 74%). SYNTHETIC EXAMPLE 429 4-(7H-Pyrrolor3,2-e1f1 ,2,31triazolon ,5-c1pyrimidin-1-yl)cvclohexanecarbaldehvde oxime [trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexylcarbaldehyde (60.0 mg, 0.223 mmol) obtained in Synthetic Example 78 in methanol ( 1 mL) and water ( 1 mL) was mixed with hydroxylamine hydrochloride (31 .0 mg, 0.446 mmol) and sodium hydrogen carbonate (37.4 mg, 0.446 mmol) and then stirred at 50°C for 5 hours. The reaction mixture was filtered, and the resulting solid washed with water, water / methanol (10/1 (v/v)) and hexane to give the title compound as a colorless solid (44.6 mg, yield 70%). SYNTHETIC EXAMPLE 430 trans-4-(7H-Pyrrolor3,2-e1f 1,2,3¾riazoloM ,5-clpyrimidin-1 -vDcvclohexanecarbonitrile trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexanecarbaldehyde oxime (37.4 mg, 0.132 mmol) in dichloromethane (3 mL) was mixed with trifluoromethanesulfonic anhydride (24.0 L, 0.145 mmol) and 1,8- diazabicyclo[5.4.0]undec-7-ene (43.0 pL, 0.289 mmol) and stirred at room temperature for 18 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium hydrogen carbonate, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/2 (v/v)) and washed with hexane / ethyl acetate (5/1 (v/v)) to give the title compound as a colorless solid (20.7 mg, yield 59%). SYNTHETIC EXAMPLE 431 2-(ftrans-4-(7H-Pyrrolof3,2-el[1 ,2,31triazolori ,5-clpyrimidin-1 - vDcvclohexyllmethylenelmalononitrile trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexylcarbaldehyde (50.0 mg, 0.1 86 mmol) obtained in Synthetic Example 78 and malononitrile (24.5 mg, 0.371 mmol) were mixed with acetic acid (3 mL), piperidine ( 18.3 pL, 0.186 mmol) and dichloromethane (2 mL) under cooling with ice and stirred for 1 hours. The reaction mixture was mixed anhydrous sodium sulfate and then stirred room temperature for 17 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium hydrogen carbonate, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / acetone = 2/1 3/2 (v/v)) to give the title compound as a colorless solid (36.3 mg, yield 62%). SYNTHETIC EXAMPLE 432 2-(ftrans-4-(7H-Pyrrolof3,2-e1f 1,2,31triazolof 1,5-c1pyrimidin-1 - vDcvclohexyllmethvDmalononitrile 2-{[trans-4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexyl]methylene}malononitrile (25.8 mg, 0.0812 mmol) in tetrahydrofuran (3 mL) was mixed with diethyl 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate (30.8 mg, 0.122 mmol) and stirred at room temperature for 1 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous ammonium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 1/2 0/1 (v/v)) to give the title compound as a colorless solid (14.2 mg, yield 55%). SYNTHETIC EXAMPLE 433 1-(4-Methylenecvclohexyl)-7H-pyrrolo[3,2 -eiri ,2,31triazolof 1,5-clpyrimidine 1-[trans-4-(lodomethyl)cyclohexyl]-7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidine (15.0 mg, 0.0393 mmol) obtained in Synthetic Example 367 in tetrahydrofuran ( 1 mL) was mixed with (trifluoromethyl)trimethysilane (7.60 L, 0.0512 mmol) and tetrabutylammonium fluoride - tetrahydrofuran solution ( 1 M, 5 1.2 L, 0.0512 mmol) under cooling with ice and then stirred at room temperature for 2 days. The reaction mixture was mixed with water, and the precipitate was collected by filtration. The resulting residue was purified by silica gel thin layer chromatography (ethyl acetate / hexane = 1/1 (v/v)) to give the title compound as a colorless solid (3.80 mg, yield 38%). SYNTHETIC EXAMPLE 3 434 2- 4-(7H-Pyrrolof3,2-e1f 1,2,31 ,5-clpyrimidin-l -vQcvclohexylidenelacetonitrile Diethyl (cyanomethyl)phosphonate (37.0 pL, 0.235 mmol) in tetrahydrofuran ( 1 mL) was mixed with sodium hydride (55 wt% dispersion in mineral oil, 10.0 mg, 0.235 mmol) under cooling with ice and then stirred for 30 minutes. The reaction mixture was mixed with 4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexanone (20.0 mg, 0.0783 mmol) obtained in Synthetic Example 82 and then stirred at room temperature for 30 minutes. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 1/2 1/1 1/0 (v/v)) to give the title compound as a colorless solid (20.0 mg, yield 92%). SYNTHETIC EXAMPLE 435 435a: 2-rcis-4-(7H-Pyrrolof3,2-e1M ,2.31triazolon ,5-clpyrimidin-1- vDcyclohexyllacetonitrile 435b: 2-rtrans-4-(7H-Pyrrolor3,2 -e r ,2,31triazolo[1 ,5-c1pyrimidin-1- vDcyclohexyllacetonitrile 2-[4-(7H-Pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexylidene]acetonitrile (20.0 g, 0.0720 mmol) in tetrahydrofuran (10 mL) were stirred with 5% palladium-carbon (10 mg) at room temperature for 4 hours under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give 2-[cis-4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexyl]acetonitrile (Synthetic Example 435a; colorless solid, .30 mg, yield 6%) in a less polar fraction and 2-[trans-4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimiclin-1-yl)cyclohexyl]acetonitrile (Synthetic Example 435b; colorless solid, 3.40 mg, yield 17%) in a more polar fraction. SYNTHETIC EXAMPLES 436 AND 437 The reactions in Synthetic Example 434 were carried out in substantially the same manners except that ethyl 2-(diethoxyphosphoryl)acetate or diethyl ( 1- cyanoethyl)phosphonate was used instead of diethyl (cyanomethyl)phosphonate to give the compounds of Synthetic Examples 3 436 and 437. The names, morphologies and yields of the compounds synthesized are shown in Table3 46. TABLE 46 SYNTHETIC EXAMPLE 438 Ethyl 2-f4-(7H-pyrrolo[3,2 -e ,2,31triazolof1,5-clpyrimidin-1 -vQcyclohexynacetate The reactions in Synthetic Example 435 were carried out in substantially the same manners except that ethyl 2-[4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexylidene]acetate obtained in Synthetic Example 3 436 was used instead of 2- [4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexylidene]acetonitrile to give the title compound as a colorless solid (cis / trans mixture ; 29.0 mg, yield 51%). SYNTHETIC EXAMPLE 439 439a: 2-[cis-4-(7H-Pyrrolo[3,2 -eiri ,2,31triazolo[1 ,5-c1pyrimidin-1 - vDcvclohexynpropanenitrile 439b: 2-rtrans-4-(7H-Pyrrolo[3,2 -eiri ,2,3¾riazolof1 ,5-clpyrimidin-1- vDcvclohexyllpropanenitrile The reactions in Synthetic Example 3 435 were carried out in substantially the same manners except that 2-[4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexylidene]propanenitrile obtained in Synthetic Example 437 was used instead of 2-[4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexylidene]acetonitrile to give 2-[cis-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexyl]propanenitrile (Synthetic Example 439a; colorless solid, 0.750 mg, yield 7%) in a less polar fraction and 2-[trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidin-1 -yl)cyclohexyl]propanenitrile (Synthetic Example 439b; colorless solid, 2.00 mg, yield 19%) in a more polar fraction. SYNTHETIC EXAMPLE 440 (E)-3-[trans-4-(7H-Pyrrolor3,2 -eiri ,2,3ltriazolof1 ,5-clpyrimidin-1 - vDcvclohexynacrylonitrile The reactions in Synthetic Example 434 were carried out in substantially the same manners except that trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexanecarbaldehyde (30.0 mg, 0.111 mmol) obtained in Synthetic Example 3 78 was used instead of 4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1- yl)cyclohexanone to give the title compound as a colorless solid (3.60 mg, yield 7%). SYNTHETIC EXAMPLE 3 441 3-ftrans-4-(7H-Pyrrolof3,2-e1H ,2.31triazoloi1 ,5-ctoyrimidin-1 -vhcvclohexyllpropanenitrile The reactions in Synthetic Example 438 were carried out in substantially the same manners except that (E)-3-[trans-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidin-1-yl)cyclohexyl]acrylonitrile obtained in Synthetic Example 440 was used instead of ethyl 2-[4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 - yl)cyclohexylidene]acetate to give the title compound as a colorless solid (7.30 mg, yield 72%). SYNTHETIC EXAMPLE3 442 442a: 2-rcis-4-(7H-Pyrroloi3,2-e1M ,2,31triazolori ,5-ctoyrimidin-1-yl)cvclohexyn-N-2,2.2- trifluoroethylacetamide 442b: 2-ftrans-4-(7H-Pyrrolo[3,2-ein ,2,31triazolof1 .5-ctoyrimidin-1-vncvclohexyn-N- 2,2,2-trifluoroethylacetamide Ethyl 2-[4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexyl]acetate (10.0 mg, 0.0305 mmol) obtained in Synthetic Example 438 in tetrahydrofuran ( 1 ml_) was mixed with ethanol (0.5 mL), water (0.25 mL) and 1 M aqueous lithium hydroxide (60 , 0.061 mmol) and stirred at room temperature for 4 hours. The reaction mixture was mixed with 1 M hydrochloric acid and concentrated under reduced pressure. The residue was dissolved in N,N-dimethylformamide (2 mL) and stirred with 0-(7- azabenzotriazol-1 -yl)-N,N,N\N'-tetramethyluronium hexafluorophosphate (23.2 mg, 0.0610 mmol), N,N-diisopropylethylamine (21 .0 , 0.122 mmol) and 2,2,2- trifluoroethanamine hydrochloride (8.30 mg, 0.0610 mmol) at room temperature for 13 hours. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate) to give 2-[cis-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidin-1 -yl)cyclohexyl]-N-(2,2,2-trifluoroethyl)acetamide (Synthetic Example 442a; colorless solid, 5.80 mg, yield 50%) in a less polar fraction and 2-[trans-4-(7HPyrrolo[ 3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]-N-(2,2,2- trifluoroethyl)acetamide (Synthetic Example 442b; colorless solid, 3.10 mg, yield 27%) in a more polar fraction. SYNTHETIC EXAMPLE 443 443a: 2-rcis-4-(7H-Pyrrolo[3,2-ein ,2,31triazolon ,5-clpyrimidin-1-yl)cvclohexyn-N- (cyanomethyl)acetamide 443b: 2-rtrans-4-(7H-Pyrrolof3,2-e1f1 ,2,31triazoloM ,5-c1pyrimidin-1-yl)cvclohexyl1-N- (cyanomethyl)acetamide The reactions in Synthetic Example 442 were carried out in substantially the same manners except that 2-aminoacetonitrile hydrochloride was used instead of 2,2,2- trifluoroethanamine hydrochloride to give 2-[cis-4-(7H-pyrrolo[3,2-e][1 ,2,3]triazolo[1 ,5- c]pyrimidin-1-yl)cyclohexyl]-N-(cyanomethyl)acetamide (Synthetic Example 443a; pale brown solid, 7.00 mg, yield 47%) in a less polar fraction and 2-[trans-4-(7H-pyrrolo[3,2- e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1 -yl)cyclohexyl]-N-(cyanomethyl)acetamide (Synthetic Example3 443b; pale brown solid, 3.80 mg, yield 25%) in a more polar fraction. SYNTHETIC EXAMPLE3 444 6-(7H-PyrroloF3,2-e1f1,2,31triazoloH ,5-c1pyrimidin-1 -yl)spiror2.5loctane-1 -carbonitrile Trimethylsulfonium iodide (59.0 , 0.269 mmol) in dimethyl sulfoxide ( 1 mL) was stirred with sodium hydride (55 wt% dispersion in mineral oil, 12.0 mg, 0.269 mmol) at room temperature for 30 minutes. The reaction mixture was mixed with 2-[4-(7Hpyrrolo[ 3,2-e][1 ,2,3]triazolo[1 ,5-c]pyrimidin-1-yl)cyclohexylidene]acetonitrile (15.0 mg, 0.0539 mmol) obtained in Synthetic Example 434 and then stirred at room temperature for 15 hours. After addition of water, the reaction mixture was extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 1/1 (v/v)) to give the title compound as a colorless solid (5.80 mg, yield 37%). SYNTHETIC EXAMPLE 445 3-(7H-Pyrrolor3,2-e1f1 .2,31triazolori ,5-clpyrimidin-1-yl)adamantan-1-ol (3-Hydroxyadamantan-1-yl)(7H-pyrrolo[2,3-d]pyrimid in-4-yl)methanone (22.5 mg, 0.0757 mmol) obtained in Reference Synthetic Example 141 in methanol ( 1 .5 mL) was mixed with hydrazine hydrate (0.141 mL, 2,27 mmol) and then stirred at 80°C for 2 hours. The reaction mixture was mixed with hydrazine hydrate (0.118 mL, 1.89 mmol) and acetic acid ( 1 drop) and stirred at 80°C for 2 hours. The reaction mixture was mixed with ethyl acetate, washed with water and saturated sodium chloride. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was dissolved in chloroform ( .5 mL) and mixed with manganese(IV) oxide (32.9 mg, 0.379 mmol). The reaction mixture was stirred at 70°C for 6 hours. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate) and further by silica gel thin layer chromatography (NH-PLC05 plate manufactured by Fuji Silysia Chemical Ltd.: ethyl acetate / hexane = 15/1) to give the title compound as a colorless solid (3.30 mg, yield 14%). The structural formulae of the compounds obtained the Reference Synthetic Examples and Synthetic Examples3 are shown below in Tables 47 to 80. The physical property data on the compounds obtained the Reference Synthetic Examples3 and Synthetic Examples are shown below in Tables 8 1 to 151 . TABLE 47 TABLEa 48 TABLE 49 TABLE 50 TABLE 5 1 TABLE 52 TABLE 53 TABLE 54 TABLE 55 TABLE3 56 TABLE 57 TABLE 58 TABLE 59 TABLE 60 TABLE 6 1 TABLE 62 TABLE3 63 TABLE 64 TABLE 65 TABLE 66 TABLE 67 TABLE3 68 TABLE 69 TABLE 70 TABLE 7 1 TABLE 72 „ TABLE3 73 TABLE 74 TABLE 75 TABLE 76 TABLE 77 TABLE 78 TABLE 79 TABLE 80 TABLE 8 1 Rf Data H-N MR (DMSO- ) : 6.63 (d , J = 2 .6 Hz, 1H), 7.67 (t, J = 2.6 Hz , 1H) , 8.44 (s, 1H). 1 LC/M S: con ditio n 1, retention t ime = 2.61 mi n LC/M S( ESI +) m/z; 246 [M+H] + LC/MS( ES I ) m/z; 244 [- H-N MR (C DCI 3) : 1.11 (d, J = 7.2 Hz, 18H) , 1.79- 1.89 (m, 3H) , 6.46 (d , J = 3.3 Hz , 1H) , 7.3 1 (d , J 2 = 3.6 Hz, 1H) , 8 .4 7 (s , 1H) . LC/M S: con ditio n 1, retention t ime = 5 .97 mi n LC/MS( ESI +) m/z; 402 [M+H] + 3 LC/MS: con ditio n 1, retention tim e = 4.91 mi n LC/M S(ES I+) m/z; 388 [M+H] + 4 LC/M S: con ditio n 1, retention tim e = 4.05 min LC/M S(ES I+) m/z; 230 [M-TI PS] + H-NMR (C D 3O D ) : 1.46 (dd, J = 18.8 9.5 Hz, 4H), 1.70-2. 00 (m, 6H) , 3.90-4.00 ( , 1H) , 7.08 (d, J = 3.6 Hz, 1H), 7 .63 (d, J = 3.6 Hz, 5 1H), 8 .88 (s, 1H). LC/M S: con ditio n 1, retention tim e = 4 .02 mi n LC/MS( ES I+) m/z; 230 [M+H] + LC/M S(ES I ) m/z; 228 [M-H] ~ Ή -NMR (C D C I 3) : -0.06 (s , 9H) , 0 .81-0. 97 (m, 2H) , 1.19-1 .60 (m, 5H) , 1.69-2 .07 (m, 5H) , 3 .45-3. 58 (m, 2H) , 3.86-4.03 ( , 1H), 5.68 (s, 6 2H), 7 . 18-7.26 (m, 1H) , 7 .51 (d, J = 3 .6 Hz, 1H) , 9.0 1 (s, 1H). LC/M S: condition 1, retention tim e = 5.59 min LC/M S(ES I+) m/z; 360 [M+H]+ 7 LC/M S: con ditio n 1, retention tim e = 3 .39 mi n LC/MS( ES I+) m/z; 36 1 [+ 8 LC/MS: con ditio n 1, retention t ime = 4 .54 min LC/M S(ES I+) m/z; 37 1 [M+1] + H-NMR (C D C I3) : 2.34 (s, 3H) , 3 .30 (s, 3H) , 3 .53 (br s , 3H) , 9 7 . 12-7.22 (m, 3H), 7.27-7. 39 (m, 1H). LC/M S: con ditio n 1, retention time = 2 .94 min LC/MS( ES I+) m/z; 180 [M+H]+ H-N MR (C D C I3) : 2.46 (s, 3H) , 7 .02-7. 10 (m, 1H), 7.2 1-7.39 (m, 2H) , 7.40-7.48 (m, 1H) , 7 .50-7. 58 (m, 2H) , 9 .01 (s, 1H) , 9.49 (br s , 1H). 10 LC/M S: con ditio n 1, retention tim e = 3 .59 min LC/MS( ES I+) m/z; 238 [M+H]+ LC/M S( ES I ) m/z; 236 [M-H] ' H-N MR ( C D C I 3) : 1.15-1 .58 (m, 5H) , 1.61 - 1.90 (m, 5H) , 2.58-2 .78 11 (m, 1H) , 3 . 17 (s, 3H) , 3.6 9 (s , 3H) . LC/MS: con ditio n 1, retention tim e = 3.47 mi n LC/M S( ES I+) m/z; 172 [M+H]+ -NMR ( C D C I3) : 1.19-1 .60 (m, 5H) , 1.68-2. 10 (m, 5H) , 3.85-4.07 (m, 1H), 7.1 9-7.2 5 (m, 1H) , 7.45-7. 58 ( , 1H) , 9.00 (s, 1H), 9.43 (br 12 s , 1H) . LC/M S: con ditio n 1, retention tim e = 4.05 mi n LC/MS( ES I+) m/z; 230 [M+H]+ LC/M S(ES I ) m/z; 228 [M-H] TABLE 82 Rf Data H-N MR (CDCI 3) : 0.91 (s, 1.5H), 0 .94 (s, 1.5H) , 1.2 1- 1 .9 1 (m, 8H) , 2 .00-2 . 19 ( , 1H), 2 .80-2 .94 13 ( , 1H), 3. 17 (s, 3H) , 3 .68 (s, 3H) . LC/M S: con ditio n 1, retention t ime = 3 .84 mi n LC/MS( ES I+) m/z; 186 [M+ H]+ H-N MR (CDCI 3) : 0 .77-0. 86 (m, 3H) , 1.20-2.00 (m, 8H) , 2 .3 1-2 .50 ( , 1H) , 4 .10-4.20 (m, 1H) , 7 .17 -7.22 ( , 1H) , 7.43-7. 52 (m, 1H) , 14 8.98 (s, 1H) , 9.18 (br s , 1H) . LC/M S: con ditio n 1, retention t ime = 4 .22 min LC/M S( ES I+) m/z; 244 [M+H] + LC/M S(ES I ) m/z; 242 [ M-H] 15 LC/MS: con ditio n 2, retention tim e = 4 . 17 min LC/M S( ES I+) m/z; 376 [M+H]+ 16 Ή -NMR ( C D C I3) : 1.10-1 .90 (m, 5H) , 2 .73-3.20 ( , 2H) , 3.5 0 (t, J = 6 .0 Hz, 2H) , 3.65-4. 15 (m, 2H), 5.13 (br s , 2H), 7.22-7. 4 1 (m, 5H) . 17 LC/M S: con ditio n 1, retention t ime = 3.89 mi n LC/M S(ES I+) m/z; 307 [M+H]+ 18 LC/MS: con ditio n 1, retention time = 5 .34 min LC/MS( ES I+) m/z; 495 [M+H]+ 19 LC/M S: con ditio n 2, retention t ime = 3 .77 mi n LC/MS( ES I+) m/z; 496 [M+H]+ 20 LC/M S: con ditio n 1, retention time = 4 .87 min LC/M S(ES I+) m/z; 506 [M+Hl+ H-N MR ( C D C I3) : 0.93-1 .13 (m, 2H) , 1.20- 1.32 ( , 1H) , 1.44- 1.65 (m, 2H) , 1.78-1 .9 3 ( , 4H) , 2 .56-2 .74 ( , 1H) , 3 .18 (s, 3H), 3.48 (t, J 2 1 = 6.0 Hz, 2H) , 3.6 9 (s, 3H) . LC/M S: con ditio n 1, retention t ime = 1.22 mi n LC/M S(ES I+) m/z; 202 [M+H]+ ' H-N MR (C D C I3) : 1.05 (s, 9H) , 1.40-1 .68 (m, 5H), 1.72- 1.95 (m, 4H), 2 .5 1-2. 73 (m, 1H) , 3 .18 (s, 3H) , 3 .47 (d, J = 6 .3 Hz, 2H), 3.69 22 (s , 3H) , 7.28-7.48 (m, 6H), 7 .53-7. 72 (m, 4H) . LC/M S: con ditio n 1, retention t ime = 5 .67 min LC/M S(ES I+) m/z; 440 [M+H]+ H-NMR (C D C I3) : 1.07 (s, 9H) , 1.42-1 .68 (m, 5H) , 1.87-2.00 (m, 3H), 2.0 1-2. 13 (m, 1H) , 3.53 (d , J = 6 .0 Hz, 2H) , 3 .8 1-4.00 (m, 1H) , 23 7.20-7.27 (m, 1H) , 7.30-7.43 (m, 6H) , 7.45-7. 53 (m, 1H) , 7.59-7.73 (m, 4H), 9 .0 1 (d , J = 4 .5 Hz, 1H) , 9.07 (br s , 1H) . LC/M S: con ditio n 1, retention tim e = 5 .94 min LC/M S(ES I+) m/z; 498 + H-N MR (C D C I3) : 1.09 (s, 9H) , 1. 17-1 .37 (m, 2H), 1.68- 1.82 ( , 1H) , 1.83-2. 2 1 (m, 6H) , 3.07-3.22 (m, 1H) , 3.58 (d, J = 6.3 Hz, 2H) , 6.75-6. 85 (m, 1H) , 7.25-7.32 ( , 1H) , 7 .33-7. 50 ( , 6H), 7 .62-7 .78 24 (m, 4H), 9.0 1 (br s, 1H), 9 .2 1 (s, 1H) . LC/M S: con ditio n 1, retention tim e = 5 .67 mi n LC/M S(ES I+) m/z; 510 [M+H]+ LC/MS( ES I ) m/z; 508 [M-Hl TABLE 83 TABLE 84 Rf Data Ή - MR (CDCIg) : 1. 16-1 .40 (m, 3H), 1.61 - 1.82 ( , 1H) , 1.85-2.09 (m, 4H) , 2 .10-2.26 ( , 2H) , 3 .09-3 .25 (m, 1H) , 3.58 (t , J = 6.0 Hz, 2H) , 6 .74-6. 85 ( , 1H), 7.20-7. 32 ( , 1H), 9 .04 (br s , 1H) , 9 .22 (s , 36 1H). LC/M S: condition 1, retention t ime = 2.99 min LC/M S(ESI +) m/z; 272 [M+H] + LC/M S(ESI ) m/z; 270 [M- H] H-NMR ( C D C I3) : 0 .93-1 . 13 (m, 2H) , 1.20- 1.32 (m, 1H) , 1.44- 1.65 ( , 2H), 1.78-1 .93 (m, 4H), 2.56-2 .74 (m, 1H) , 3 .18 (s , 3H) , 3 .48 (t , 37 J = 6.0 Hz, 2 H) , 3.69 (s , 3H) . LC/M S: condition 1, retention tim e = 1.22 min LC/M S(ESI +) m/z; 202 [M+H] + H-NMR (C D C I3) : 1.46 (s, 9H), 1.60-1 .8 1 (m, 4H), 2 .65-2. 90 ( , 3H) , 3 . 18 (s, 38 3H) , 3 .7 1 (s, 3H) , 4.00-4. 30 (m, 2H). LC/M S: condition 1, retention time = 3.66 min LC/M S(ESI +) m/z; 273 [M+H] + H- MR ( C D C I3) : 1.40-1 .53 (m, 9H) , 1.55- 1.82 ( , 2H) , 1.87-2. 10 (m, 2H) , 2.80-3. 10 (m, 2H) , 4 .00-4. 37 (m, 3H) , 7 .15-7. 30 (m, 1H) , 39 7 .46-7. 59 (m, 1H), 8 .90-9 .08 (m, 1H) , 9.53 (br s , 1H) . LC/M S: condition 1, retention time = 3.87 min LC/M S(ESI +) m/z; 33 1 [M+H] + LC/M S(ESI ) m/z; 329 [M- H] H-NMR (DMSO-d ) : 1.63-1 .89 ( , 4H) , 2.82-3.04 (m, 3H), 3 . 10 (s , 40 3H) , 3 . 18-3. 3 1 (m, 2H), 3 .69 (s, 3H), 8.73 (br s, 1H) , 9 .07 (br s , 1H) . LC/M S: condition 1, retention time = 0 .50 min LC/M S(ESI +) m/z; 173 [M+H 1+ H-NMR ( C D C I3) : 1.65-1 .92 (m, 4H) , 2 .38-2 .5 1 (m , 2H) , 2 .57-2 .72 4 1 ( , 1H) , 2 .92-3.06 ( , 4H) , 3 .18 (s, 3H) , 3 .70 (s, 3H). LC/M S: condition 1, re tention tim e = 0 .74 min LC/M S(ESI +) m/z; 255 [+ H-NMR ( C D C I3) : 1.78-2 .05 (m, 4H), 2.56-2 .68 (m, 2H) , 2.87-3. 12 (m, 4H) , 3 .87-4.00 ( , 1H) , 7 .22-7. 25 (m, 1H), 7.26 (s, 1H) , 42 7 .50-7 .56 (m, 1H), 8.99 (s, 1H) , 9.74 (br s, 1H) . LC/M S: condition 1, re tention tim e = 2 .75 min LC/M S(ESI +) m/z; 3 13 [M+H] + H-N MR (C D C I 3) : 1.64-1 .82 ( , 4H) , 2.76-2.95 (m, 3H) , 3 .18 (s , 3H) , 3 .7 1 (s, 3H), 4 . 12-4. 30 (m, 2H) , 5 ,13 (s, 2H) , 7.25-7.39 (m, 43 5H). LC/M S: condition 1, re tention t ime = 3 .65 min LC/M S(ESI +) m/z; 307 [M+H] + ' H-N MR ( C D C I3) : 1.60-1 .82 ( , 3H), 1.92-2.09 (m, 2H) , 2.95-3. 15 (m, 2H) , 4 .18-4. 38 (m, 2H) , 5. 15 (s, 2H) , 7 .20-7 .25 (m, 1H) , 44 7.25-7.40 (m, 5H) , 7.50-7.55 (m, 1H), 8.9 9 (s , 1H), 9.44-9. 7 1 ( , 1H) . LC/M S: condition 1, retention t ime = 3 .90 min LC/M S(ESI +) m/z; 365 [M+H 1+ TABLE 85 TABLE 86 TABLE 87 Rf Data Ή -NMR (C DCI 3) : 1.95 (m, 1H) , 2 .14 (m, 1H) , 2.38 (m, 4H) , 4.60 (qu in t , J = 8.4 Hz, 1H) , 7 .28 ( , 1H), 7 .52 ( , 1H) , 8.97 (s, 1H) . 64 LC/M S: condition 1, re tention t ime = 3.22 min LC/M S(ESI +) m/z; 202 [M+H] + LC/M S(ESI ) m/z; 200 [M- H] - ' H-NMR (CDCI 3) : 1.76 (m, 4H) , 1.91 (m, 2H) , 2 .03 (m, 2 H), 4.36 (m, 1H) , 7 .26 ( , 1H), 7 .55 (65 m, 1H) , 9.03 (s, 1H) , 10.43 (br s , 1H). LC/M S: condition 1, re tention t ime = 3 .64 min LC/M S(ESI +) m/z; 2 16 [M+H] + H-NMR (DMSO- ) : 1.30-1 .60 (m, 4H) , 1.90-2. 13 (m, 4H) , 2.20-2 .45 (m, 1H), 3.80-4. 00 (m, 1H), 6.91 -7.05 (m, 1H) , 7.75-7.90 66 (m, 1H) , 8.96 (s, 1H) , 12 .47 (br s , 1H) . LC/M S: condition 1, retention t ime = 4 .07 min LC/M S(ESI +) m/z; 298 [M+H] + LC/M S(ESI ) m/z; 296 [M- H] 'H-N MR (DMSO- ) : 1.50-1 .88 ( , 6H) , 1.95-2. 11 (m, 2H) , 2.30-2.45 (m, 1H), 4.05-4.20 (m, 1H) , 6.90-7.05 (m, 1H) , 7.75-7.90 67 (m, 1H) , 8 .93 (s , 1H), 12 .46 (br s , 1H). LC/M S: condition 1, re tention t ime = 4 .00 min LC/M S(ESI +) m/z; 298 [M+H] + LC/M S(ESI ) m/z; 296 [M- H] ' H-N MR (CDCI 3) : 1.05 (s, 9H) , 1.38 (dq , J = 10 .9, 3.0 Hz, 4H) , 1.65-1 .74 (m, 2H) , 1.86- 1.95 (m, 2H) , 2 .5 3-2.65 (m, 1H) , 3 . 13 (s, 68 3H) , 3 .56-3. 64 (m, 1H) , 3.67 (s, 3H) , 7 .32-7 .45 (m, 6H), 7 .64-7 .69 (m, 4H). LC/M S: condition 1, retention tim e = 5 .45 min LC/M S(ESI +) m/z; 426 [M+H] + H-N MR (CDC I3) : 1.07 (s, 9H), 1.30-1 .45 (m, 2H) , 1.52-1 .67 ( , 2H) , 1.89-2.00 (m, 4H) , 3.60-3 .7 1 ( , 1H) , 3.89 (tt , J = 12.2, 3 .0 Hz, 1H) , 7 .17 (dd , J = 3.6, 2 .0 Hz, 1H), 7.33-7.49 (m, 7H) , 7 .65-7. 72 ( , 69 4H) , 8 .99 (s, 1H) , 9 . 11 (br s , 1H) . LC/M S: condition 1, re tention t ime = 5 .64 min LC/M S(ESI +) m/z; 484 [M+H] + LC/M S(ESI ) m/z; 482 [M- H] ' H-N MR (CDCI 3) : 1.09 (s , 5H) , 1.15 (s , 4H) , 1.53-1 .97 (m, 5H) , 1.98-2. 08 (m, 2H) , 2.49 (dq , J = 1 .6, 3.0 Hz, 1H) , 3 . 11 (tt , J = 11.2, 3.3 Hz, 0 .6H) , 3.25 (tt , J = 12.2 , 3 .3 Hz, 0.4H ) , 3.75-3.85 (m, 0 .6H) , 4 .13-4. 18 (m, 0.4H) , 6.71 (dd, J = 3 .3 , 2 .0 Hz , 0.6H ) , 7 .01 (dd , J = 3.0, 2 .3 Hz, 0 .4H) , 7 . 16 (t, J = 3 .3 Hz, 0 .6H) , 7.2 1-7.28 ( , 0.4H) , 70 7.34-7.47 (m, 6H) , 7.69-7.75 (m, 4H) , 9.04 (br s , 1H) , 9.18 (s, 0 .6H) , 9.24 (s, 0.4H) . LC/M S: condition 1, retention tim e = 5 .32, 5.39 mi n (cis/trans mixture) LC/M S(ESI +) m/z; 496 [M+H] + LC/M S(ESI ) m/z; 494 [M- H] TABLE 88 TABLE3 89 Rf Data -NMR ( C D C I3) : -0. 07 (s, 9H) , 0.9 1 (t, J = 8.3 Hz, 2H), 1.27- 1.38 (m, 3H) , 1.97-2 .02 ( , 2H) , 2 .70-2 .74 (m, 2H) , 3 .53 (t , J = 8 .3 Hz, 2H) , 4.02-4.23 ( , 3H) , 5 .10 77 (s, 2H) , 5.64 (d, J = 2 .4Hz, 2 H) , 6.6 1 (d, J = 3 .3Hz, 1H) , 7.26-7.33 (m, 6H) , 8.85 (s , 1H) . LC/M S: condition 3 , retention t ime = 2 .26 min LC/M S(ESI +) m/z; 496 [M+H] + 78 LC/M S: condition 3 , re tention tim e = 3.05 min LC/M S(ESI +) m/z; 506 [M+H] + 79 LC/M S: condition 3 , re tention t ime = 1.55 min LC/M S(ESI +) m/z; 366 [M+H] + 80 LC/M S: condition 3 , retention tim e = 0.70 min LC/M S(ESI +) m/z; 231 [M+H] + LC/M S: condition 3 , re tention tim e = 1.63 min 8 1 LC/M S(ESI +) m/z; 389 [M+H] + LC/M S(ESI ) m/z; 387 [M- H 82 LC/M S: condition 3 , re tention t ime = 1.08 min LC/MS(ESI +) m/z; 390 [M+H] + H-NMR (C D C I3) : 3 .20 (s , 3H) , 3 .65 (s , 3H) , 3.68-3. 70 (m, 1H) , 4 . 14 (t , J = 8.7 Hz, 2H) , 4.22 (d, J = 6.0 Hz, 2H), 5 .09 (s, 2H) , 83 7 .30-7. 36 (m, 5H) . LC/M S: condition 3 , re tention tim e = 1.88 min LC/M S(ESI +) m/z; 279 [M+H] + H-NMR (C D C I3) : 4.3 1-4.4 1 (m, 4H), 4.62-4.69 (m, 2H) , 5.11 (s , 2H) , 7.27-7. 36 (m, 6H) , 7 .55 (dd , J = 3 .6 , 2.4 Hz, 1H) , 8.9 5 (s, 1H) , 84 9.18 (br s , 1H). LC/M S: condition 3 , retention t ime = 2 .09 min LC/M S(ESI +) m/z; 337 [M+H] + 1H-N MR (C D C I3) : 1.88 (br s , 1H) . 3.3 5 (s, 3H) , 3.55 (s, 3H) , 4.74 85 (s, 2H) , 7.39 (d , J = 8 . 1 Hz , 2H), 7 .67 (d, J = 8.1 Hz, 2H) . LC/M S: condition 1, retention t ime = 0 .84 min LC/M S(ESI +) m/z; 196 [M+H] + 1H-N MR (C D C I 3) : 0 .11 (s, 6H) , 0 .95 (s , 9H) , 3.35 (s, 3H), 3.55 (s , 86 3H), 4.77 (s, 2H) , 7 .35 (d, J = 8.1 Hz, 2H) , 7.65 (d , J = 8.1 Hz, 2H) . LC/M S: condition 1, retention t ime = 4 .73 min LC/M S(ESI +) m/z; 3 10 [M+H] + H-N MR (C D C I3) : 0 .12 (s, 6H) , 0 .96 (s, 9H) , 4 .83 (s, 2H) , 7 .00 (dd , J = 3.9, 2.1 Hz, 1H) , 7 .47 (d, J = 8.1 Hz, 2H) , 7.49 (m, 1H) , 8.14 (d , 87 J = 8.1 Hz, 2 H) , 9.04 (s , 1H) , 9.59 (br s , 1H) . LC/M S: condition 1, retention t ime = 4.80 min LC/M S(ESI +) m/z; 368 [M+H] + LC/M S(ESI ) m/z; 366 [M- Hl H-NMR (C D C I3) : 0 . 15 (s, 6H), 0 .98 (s, 9H) , 4 .84 (s, 2H) , 6 .97 (dd, J = 3 .3, 2 .1 Hz, 1H) , 7.27 (dd, J = 6 .0 , 3.3 Hz, 1H) , 7 .50 (d , J = 8 .4 88 Hz, 2H) , 7 .98 (d, J = 8.4 Hz, 2H) , 9.22 (br s , 1H) , 9 .30 (s, 1H) . LC/M S: condition 1, retention t ime = 4 .93 min LC/M S(ESI +) m/z; 380 [M+H] + TABLE 90 Rf Data Ή -MR (CDCI 3) : 1.58 (m, 4H) , 1.73 (m, 5H) , 2 .80 (tt, J = 8.4, 3.6 Hz, 1H), 3 . 89 17 (s, 3H) , 3.62 (m, 2H), 3 .69 (s, 3H) . LC/M S: condition 1, retention time = 1.42 min LC/M S(ESI +) m/z; 202 [M+H] + ' H-N MR (C D C I3) : 0 .04 (s, 6H) , 0.89 (s, 9H) , 1.55 (m, 4H) , 1.69 (m, 5H) , 2.80 (tt, J = 7.8 , 4.2 Hz, 1H) , 3 .17 (s , 3H) , 3 .58 (d , J = 90 10.5 Hz , 2H), 3 .68 (s, 3H) . LC/M S: condition 1, re tention t ime = 5.08 min LC/M S(ESI +) m/z; 3 16 [M+H] + ' H-N MR (C D C I3) : 0.06 (s, 6H), 0.90 (s, 9H) , 1.7 1 (m, 7H) , 1.90 (m, 2H) , 3.53 (d , J = 6.9 Hz, 2H), 4.07 (m, 1H) , 7.20 (d d, J = 3 .3 2 .1 Hz, 9 1 1H) , 7 .50 (t, J = 3 .3 Hz, 1H) , 8.98 (s, 1H) , 9.42 (br s, 1H) . LC/M S: condition 1, re tention t ime = 5.19 min LC/M S(ESI +) m/z; 374 [M+H] + LC/M S(ESI ) m/z; 372 [M- H] H-N MR (C D C I3) : 0.08 (s, 6H) , 0.93 (s, 9H) , 1.22 (m, 2H) , 1.70 (m, 1H), 1.90-2 .05 (m, 4H) , 2.15 ( , 2H) , 3 .16 (m, 1H), 3 .5 1 (d, J = 6 .6 92 Hz, 2H) , 6 .08 Hz (m, 1H) , 7 .27 ( , 1H) , 9 . 1 6 (br s , 1H) , 9 .22 (s, 1H) . LC/M S: condition 1, retention t ime = 5 .09 min LC/M S(ESI +) m/z; 428 [M+H] + LC/M S(ESI ) m/z; 426 [M- H] LC/M S: condition 1, retention t ime = 3 .62 min 93 LC/M S(ESI +) m/z; 202, 2 04 [M+H] + Ή -NMR (C D C I 3) : 1.83-2.04 (m, 4H) , 2 .25 (td, J = 11.6 , 2 .5 Hz, 2 H), 2 .93 (d , J = 11.7 Hz, 2H) , 3 .59 (s, 2H) , 3.92-3.99 (m, 1H) , 7.24 (dd , J = 3 .6, 2 .1 Hz , 1H) , 7.47 (d , J = 8.1 Hz, 2H) , 7 .50 (dd , J = 3 .6, 94 2.4 Hz , 1H), 7 .6 1 (d, J = 8 . 1 Hz, 2H), 8.98 (s, 1H) , 9.04 (br s , 1H). LC/M S: condition 3 , re tention t ime = 1.25 min LC/M S(ESI +) m/z; 346 [M+H] + -NMR ( C D C I3) : -0. 06 (s, 9H) , 0 .91 (t, J = 8.3 Hz, 2H), 1.78-2 .04 (m, 4H) , 2.25 (td , J = 11.6 , 2 .8 Hz, 2H) , 2 .93 (d , J = 11.7 Hz, 2H) , 3 .53 (t , J = 8 .3 Hz, 2H) , 3 .60 (s , 2H) , 3 .95 (tt, J = 11.4 , 3 .9 Hz, 1H) , 95 5.68 (s, 2H) , 7.23 (d, J = 3.3 Hz, 1H) , 7.47 (d , J = 8.1 Hz, 2H) , 7.53 (d, = 3.6 Hz , 1H) , 7.6 1 (d, J = 8.7 Hz, 2H) , 8 .99 (s, 1H) . LC/M S: condition 3 , retention time = 2 .19 min LC/M S(ESI +) m/z; 476 [M+H] + ' H-N MR (C D C I3) : -0.07 (s , 9H) , 0.90 (t, J = 8. 1 Hz, 2H) , 1.23 (d, J = 14 .4 Hz, 1H) , 1.3 1- 1 .53 (m, 2H) , 1.78-2. 0 1 ( , 6H), 2.73 (d , J = 10 .5 Hz, 1H) , 2.89 (d , J = 11.4 Hz, 1H) , 3.49 (s, 2H) , 3.54 (t, J = 8 .1 96 Hz, 2H) , 4 .05 (d, J = 7.5 Hz, 1H) , 5 .65 (d, J = 2 .1 Hz , 2H) , 6.63 (d, J = 3.6 Hz , 1H) , 7.32 (d, J = 3 .6 Hz, 1H) , 7 .4 1 (d , J = 8.1 Hz, 2H) , 7.57 (d, J = 8 . 1 Hz, 2H) , 8.86 (s, 1H) . LC/M S: condition 3 , re tention t ime = 1.64 min LC/M S(ESI +) m/z; 477 [M+H] + 97 LC/M S: condition 3 , retention time = 2.15 min LC/M S(ESI +) m/z; 487 [+ TABLE 9 1 Rf Data Ή -NMR (C D C I3) : 2 .05-2.20 (m, 2H), 3.20 (s, 3H) , 3 .39-3. 80 (m, 98 8H) , 5 . 14 (s, 2H) , 7 .28-7. 39 (m, 5H) . LC/M S: condition 3 , re tention t ime = 2.02 min LC/M S(ESI +) m/z; 293 [M+H] + LC/M S: condition 3 , retention tim e = 2 . 13 min 99 LC/M S(ESI +) m/z; 35 1 [M+H] + LC/M S(ESI ) m/z; 349 [M- H] 'H-N MR ( C D C I3) : 2.74 (br s , 2H) , 2 .96 (d, J = 12 .0 Hz , 1H) , 3.54 (d, J = 12 .0 Hz, 1H), 7.35 (d , J = 9.0 Hz, 2 H), 7.50 (d, J = 9.0 Hz, 100 2H). LC/M S: condition 1, re tention t ime = 0 .78 min LC/M S(ESI +) m/z; 240, 2 42 [M+H] + Ή -N R ( C D C I3) : 2.69 (br s , 1H), 3.02 (d, J = 13 .2 Hz, 1H) , 3.52 (d , J = 13 .2 Hz , 1H), 7 .38 ( , 3H) , 7.57 (m, 2H) . 10 1 LC/M S: condition 1, retention t ime = 0.55 min LC/M S(ESI +) m/z; 206 [M+H] + Ή -NMR (C D C I 3) : 2 .97 (d , J = 12 .9 Hz, 1H), 3.57 (d, J = 13 .2 Hz, 102 1H), 7.08 (m, 2H), 7 .55 (m, 2H) . LC/M S: condition 1, re tention time = 0 .56 min LC/M S(ESI +) m/z; 224 [M+H] + Ή -NMR (C D C I3) : 2 .77 (ddd , J = 5 .5, 2.5, 1.2 Hz, 1H) , 3 . 19 (ddd , J 103 = 5.5, 4.0, 1.1 Hz , 1H) , 3 .92 (dd , J = 4.0, 2 .5 Hz, 1H) , 7 .40 (d, J = 8.3 Hz, 2H), 7 .6 1 (d , J = 8 .3 Hz, 2H) . ' H-N MR (C D 3O D ) : 1.9 1 (s, 3H) , 2 .20-2 .33 ( , 4H), 3 .20-3. 30 (m, 2H) , 3.50-3 .69 (m, 3H) , 6 .95 (d , J = 3 .3 Hz, 1H) , 7 .43 (d , J = 3 .3 Hz , 104 1H) , 9 .34 (s, 1H) . LC/M S: condition 1, re tention time = 2 . 15 min LC/M S(ESI +) m/z; 243 [M+H] + LC/M S(ESI ) m/z; 24 1 [M- H] TABLE 92 TABLE 93 TABLE 94 Rf Data ' H-N R ( C D C I3) : -0. 06 (s , 6H) , 0 .83 (s, 9H) , 1.61 -2 .15 ( , 9H) , 3 .29-3 .37 (m, 1H) , 3 .56 (d , J = 6 .6 Hz, 2H) , 6 .72 (dd , J = 3 .3 2 .1 Hz, 1H) ,7.22 (t , J = 3 135 .3 Hz, 1H) , ) , 9 .04 (s, 2H) , 9 .17 a (b r s , 1H) . LC/M S: condition 3 , retention tim e = 3 .22 min LC/M S(ESI +) m/z; 386 [M+H] + LC/M S(ESI ) m/z; 384 [M-H] H-NMR (C D C I3) : 0 .08 (s, 6H) , 0 .93 (s , 9H) , 1.20 (qd , J = 12 .2 , 3 .6 Hz , 2H) , 1.7 6-1 .6 1 ( , 1H) , 2 .05- 1.84 (m, 4H), 2 .19-2. 09 (m, 2H) , 3 .16 (tt , J = 12 .2 , 3 .6 Hz, 1H) , 3.52 (d, J = 6.3 Hz, 2H) , 6.8 1 135 (dd , J = 3.3 , 2 .0 Hz, 1H) , 7.29 (t, J = 3 .3 Hz, 1H), 9 .2 1 (br s , 1H) , b 9.23 (s, 1H). LC/M S: condition 3, retention time = 3 .20 min LC/M S(ESI +) m/z; 386 [M+H] + LC/M S(ESI ) m/z; 384 [M- H] 137 LC/M S: condition 1, retention tim e = 0 .32 min LC/MS (ESI +) m/z; 20 1 + 138 LC/M S: condition 1, retention tim e = 0 .34 min LC/M S(ESI +) m/z; 2 15 [M+H] + H-N R (C D C I3) : 1.46 (s, 9H) , 4 .58-4. 65 (m, 2H), 4 .68-4. 74 (m, 139 2H), 5.36-5 .4 1 (m, 1H) . LC/M S: condition 1, retention tim e = 3.44 min LC/M S(ESI +) m/z; 195 [M+H] + H-NMR ( C D C I3) : 1.56- 1.75 ( , 6H) , 1.82-1 .96 ( , 6H) , 2 .22-2.28 140 ( , 2H) , 3 . 17 (s, 3H), 3 .68 (s, 3H) . LC/M S: condition 3 , retention tim e = 2.84 min LC/M S(ESI +) m/z; 240 [+ H-NMR ( C D C I3) : 1.50- 1.97 ( , 8H) , 2 .10-2 .27 (m, 6H) , 2 .33-2.38 (m, 2H) , 6.96-6.99 (m, 1H), 7.43-7.47 ( , 1H) , 8.93 (s , 1H) , 9.25 14 1 (br s , 1H) . LC/M S: condition 3 , retention tim e = 3 . 17 min LC/MS(ESI +) m/z; 298 [M+H] + LC/M S(ESI ) m/z; 296 [M- H] TABLE 95 TABLE 96 Ex Data H-N MR (CDCI 3) : 0 .86 (d , J = 6.5 Hz, 3H) , 1.48 (br s , 9H) , 1.87 (d, J = 12.3 Hz, 1H) , 2.04-2. 11 ( , 1H) , 2.23-2 .3 9 (m, 2H) , 2.92 (td , J = 1.0 , 4.5 Hz, 2H) , 3 . 17 (t, J = 11.0 Hz, 1H) , 3.48 (d, J = 7.0 Hz, 1H) , 11 7.24-7. 32 (m, 2H) , 9.18 (br s , 1H) , 9 .22 (s, 1H) . LC/M S: condition 1, retention t ime = 4 .05 min LC/M S(ESI +) m/z; 30 1 [M-'Bu] + LC/M S(ESI ) m/z; 355 [M- H] 12 LC/M S: condition 1, retention t ime = 3.09 min LC/M S(ESI +) m/z; 324 [M+H] + 1H-NMR (CDC I3) : 1. 18-1 .29 ( , 1H) , 1.49 (s, 9H) , 1.63-1 .77 ( , 1H) , 1.90 (dt, J = 13 .9 , 3 .0 Hz, 1H) , 2.09-2.33 (m, 2H) , 2.87 (t, J = 13.2 Hz, 1H) , 3.30 (tt, J = 11.6 , 4 .3 Hz, 1H) , 4 .23 (br s , 1H) , 4.44 13 (br s, 1H), 6.92 (br s , 1H), 7.3 1 (t , J = 3 .3 Hz, 1H), 9 .23 (s, 1H) , 9.27 (br s , 1H) . LC/M S: condition 1, retention t ime = 3.79 min LC/M S(ESI +) m/z; 287 [M- Bu ]+ LC/M S(ESI ) m/z; 341 [- H-NMR (CDCI 3) : 1.68-1 .80 (m, 1H) , 1.93 (d, J = 13 .5 Hz, 1H) , 2 . 14-2. 37 (m, 2H) , 2.95 (br s , 1H) , 3 .07-3. 22 (m, 1H) , 3.26-3.38 (m, 1H) , 4.33 (br s , 1H), 4 .55 (br s , 1H) , 5 .20 (d, J = 5 .9 Hz, 2H) , 14 6 .95-7. 17 (m, 1H) , 7.28-7. 43 (m, 6H), 9 .22 (s, 1H) , 9 .39 (br s , 1H) . LC/M S: condition 1, re tention t ime = 3 .84 min LC/M S(ESI +) m/z; 377 [M+H] + LC/M S(ESI ) m/z; 375 [M- H] H-N MR (CD 3OD) : 1.71- 1 .93 (m, 3H) , 2.0 1-2. 24 ( , 2H) , 2.70-2 .8 1 (m, 1H) , 2.94-3 .17 (m, 2H), 3 .37-3. 47 (m, 1H) , 6.9 1 (d , J = 3 .3 Hz, 15 1H), 7 .4 1 (d , J = 3 .0 Hz, 1H) , 9.32 (s, 1H) . LC/M S: condition 1, retention time = 0 .35 min LC/M S(ESI +) m/z; 243 [M+H] + LC/M S(ESI ) m/z; 24 1 [M- H] 16 LC/M S: condition 1, retention time = 0.40 min LC/M S(ESI +) m/z; 333 [M+H] + LC/M S: condition 1, re tention t ime = 3.25 min 17 LC/M S(ESI +) m/z; 353 [M+H] + LC/M S(ESI ) m/z; 35 1 [M- H] H-N MR (CDCI 3) : 1.23- 1.35 ( , 4H) , 1.85-1 .96 (m, 2H), 2.20 (m, 1H), 2.50 (t , J = 11.6 Hz, 1H), 3 .0 1 (d, J = 10 .9 Hz, 1H) , 3. 16 (d, J = 10 .9 Hz, 1H) , 3.41 -3. 53 (m, 1H), 6 .7 1 (dd, J = 3.3, 2 .0 Hz, 1H) , 18 7 .22-7. 31 (m, 2H) , 7.70 (d, J = 7.6 Hz, 1H) , 8.50 (dd , J = 4.6, 2.0 Hz, 1H) , 8.60 (d, J = 2.0 Hz, 1H) , 9 .21 (s, 1H), 9.32 (br s, 1H) . LC/M S: condition 1, retention time = 0 .35 min LC/M S(ESI +) m/z; 334 [M+H] + LC/M S(ESI ) m/z; 332 [M- H] TABLE 97 Ex Data ' H-NMR (CDCIg) : 1.23-1 .29 ( , 1H) , 1.85- 1.96 (m, 3H) , 2 .13-2.27 ( , 2H), 2.49 (t , J = 1 .2 Hz, H) , 3.0 5 (d , J = 0.2 Hz, 1H) , 3.20 (d, J = 10 .9 Hz , 1H) , 3.41 -3.53 (m, 1H) , 6.75 (dd , J = 3.3, 2.0 Hz, 1H) , 19 7.23-7.29 (m, 1H) , 8.74 (s, 1H) , 9.19 (br s , 1H) , 9.2 1 (s , 1H) . LC/M S: condition 1, retention t ime = 0 .35 min LC/M S(ESI +) m/z; 340 [M+H] + LC/M S(ESI ) m/z; 338 [M- H] H-NMR (DMSO-c ) : 1.62-1 .79 (t, J = 12.6 Hz, 1H) , 1.8 1- 1 .92 (m, 1H) , 1.95-2 .11 (m, 1H), 2 .12-2.24 (m, 1H) , 3.07 (t, J = 12.6 Hz , 1H) , 3.2 1 (m, 1H) , 4.37 (d, J = 12 .6 Hz, 1H) , 4.57 (d, J = 11.6 Hz, 1H) , 6 .99 (s, 1H) , 7 .53 (s , 1H) , 8.95 (br 20 s , 1H) , 9.56-9. 60 (m, 1H) , 12.59 (s, 1H) . LC/M S: condition 1, retention t ime = 2.94 min LC/M S(ESI +) m/z; 370 [M+H] + LC/M S(ESI ) m/z; 368 [M- H] H-NMR (DMSO- ) : 1.64-1 .79 (m, 1H) , 1.82-2 .06 (m, 2H) , 2 .13-2.22 ( , 1H) , 2 .25 (s, 3H) , 3 .07 (t, J = 12 .2 Hz, 1H), 4 .22 (d , J = 13 .2 Hz, 1H) , 4.43 (d , J = 12.9 Hz, 1H) , 6.59 (s, 1H), 6 .98 (d, J = 2 1 2.6 Hz, 1H) , 7 .53 (d , J = 3 .3 Hz, 1H), 9.57 (s, 1H) , 10.46 (br s , 1H) , 12 .58 (br s , 1H) . LC/M S: condition 1, retention t ime = 2.90 min LC/M S(ESI +) m/z; 383 [M+H] + LC/M S(ESI ) m/z; 381 [M- H] H-N MR ( C D C I3 ) : 1.26 (t, J = 7.3 Hz, 1H) , 1.86-2 .01 (m, 2H) , 2 . 15-2 .27 (m, 2H) , 2.47 (t , J = 11.2 Hz, 1H) , 2 .98 (d, J = 11.2 Hz, 1H), 3 . 11 (dt , J = 1 1.2, 1.7 Hz, 1H) , 3.40-3.5 1 (m, 1H), 3.57 (d, J = 13 .9 Hz, 1H) , 3 .69 (d , J = 13 .9 Hz, 1H) , 6 .66 ( dd, J = 3.3 , 2.0 Hz, 22 1H) , 7.25-7.28 (m, 1H) , 7.49 (d , J = 8 .3 Hz, 2H) , 7.60 (d , J = 7 .9 Hz , 2H) , 9 . 17 (br s, 1H) , 9.2 1 (s, 1H) . LC/M S: condition 1, retention t ime = 0 .59 min LC/M S(ESI +) m/z; 358 [M+H] + LC/MS(ESI ) m/z; 356 [M- H] H-N MR ( C D C I3) : 1.23-1 .32 (m, 1H) , 1.8 1- 1.98 (m, 2H) , 2 .15-2 .27 (m, 2H), 2.42 (t , J = 1 1.2 Hz, 1H) , 3.0 1 (d, J = 10.9 Hz, 1H) , 3 .15 (d, J = 10.6 Hz, 1H) , 3.45 (td , J = 11.6, 3 .0 Hz, 1H) , 3 .56 (d, J = 13.2 23 Hz, 1H) , 3.7 1 (d , J = 13.2 Hz, 1H) , 6 .58-6 .62 (m, 1H) , 7 .20-7.24 (m, 1H) , 7 .48 (d , J = 7 .9 Hz, 2 H) , 7.56 (d , J = 7 .9 Hz, 2H) , 9 .2 1 (s, 2H) . LC/M S: condition 1, retention t ime = 2.49 min LC/M S(ESI +) m/z; 40 1 [M+H] + LC/M S(ESI ) m/z; 399 M- HV H-N MR (C D C I3) : 1.51 (s, 9H) , 1.95-2 .20 (m, 4H) , 2 .85-3. 10 (m, 2H) , 3.2 9-3.48 (m, 1H) , 4 .15 -4.42 (m, 2H) , 6 .7 1-6 .80 ( , 1H) , 24 7 .27-7.35 (m, 1H) , 9.23 (s, 1H) , 9.27 (br s , 1H) . LC/M S: condition 1, re tention t ime = 3.94 min LC/M S(ESI +) m/z; 343 [M-fBu] + LC/M S(ESI ) m/z; 34 1 [M- H] TABLE3 98 Ex Data H-NMR (CDCI 3) : 1.99 -2. 10 (m, 2H) , 2 .39 (dq, J = 11.7, 3 .9 Hz, 2H) , 2.65 (dt, J = 11.7 , 2 .4 Hz, 2H) , 3.09 (q, J = 9 .6 Hz, 2H) , 3 .11-3.2 9 ( , 3H) , 6 .85 (dd, J = 2 .5, 0 .9 Hz, 1H) , 7.3 1 (dd , J = 3 .0, 25 0.9 Hz, 1H) , 9 .11 (br s , 1H) , 9 .23 (s , 1H) . LC/M S: co ndition 1, retenti on time = 2 .30 mi n LC/M S(ESI +) m/z; 325 [M+H]+ LC/M S(ES ) m/z ; 323 [M-H] Ή -NMR (CDCI 3) : 2 .00-2 .15 (m, 4H) , 3.0 1-3. 18 (m, 2H) , 3 .32-3 .45 (m, 1H) , 4.30-4.44 (m, 2H) , 5 .19 (s , 2H) , 6 .70-6 .76 (m, 1H) , 7.25-7.43 (m, 26 6H) , 9 .18 (br s , 1H) , 9.22 (s, 1H) . LC/M S: co ndition 1, retenti on time = 3.79 mi n LC/M S(ES I+) m/z; 377 [M+H]+ LC/M S(ESI ) m/z ; 375 [M-H] 'H-N MR (CD 3OD) : 2.05-2. 15 (m, 4H) , 2.90-3. 13 (m, 2 H) , 3 .38-3 .50 (m, 1H) , 6.93 (d , J = 3.3 Hz , 1H) , 7.40 (d, J = 3 .3 Hz, 1H) , 9 .3 1 (s , 27 1H) . LC/M S: co ndition 1, retention time = 0.44 mi n LC/M S(ESI +) m/z; 243 [M+H] + LC/M S(ES I ) m/z ; 24 1 [M-H] Ή -NMR (CDCI 3) : 1.95-2 .12 (m, 2H) , 2 .12-2.3 1 (m, 4H) , 2 .99-3 .12 (m, 2H) , 3 .17-3.3 1 (m, 1H) , 3 .61 (s , 2H) , 6 .85 (d, J = 2.4 Hz , 1H) , 7.23-7.35 (m, 2H) , 7 .74 (d , J = 7.8 Hz , 1H) , 8.52 (dd, J = 4 .5, 1.2 28 Hz, 1H), 8.62 (d, J = 2 .1 Hz, 1H) , 9.22 (s, 1H) , 9.3 9 (b r s , 1H) . LC/M S: co ndition 3 , retention time = 0.52 mi n LC/M S(ESI +) m/z; 334 [M+H]+ LC/M S(ES I ) m/z ; 332 [M-H] Ή -NMR (DMSO- ) : 1.64- 1.82 (m, 1H) , 1. 86-2 .04 (m, 3H) , 2.85-3.00 (m, 1H) , 3.30-3.3 9 (m, 1H) , 3.45 -3.60 (m, 1H) , 3 .6 1-3 .84 (m, 2H) , 3 . 92-4. 05 (m, 1H) , 4.43-4.55 (m, 1H) , 6 .82-6 .90 (m , 1H), 2 9 7.49-7.53 ( , 1H) , 9.53 (s , 1H) , 12.5 1 (br s , 1H) . LC/M S: co ndition 3 , retenti on time = 1.62 mi n LC/M S(ESI +) m/z; 353 [M+H]+ LC/M S(ES I ) m/z ; 35 1 [- 'H-NM (DMSO-c/ ) : 1.70-2 .10 (m, 4H) , 3 . 09-3 .26 (m, 2H) , 3.43-3.65 (m, 1H) , 4 .14-4 .50 (m, 2H) , 6.85 (s, 1H) , 7 .49 (s, 1H) , 30 9.00 (br s , 1H) , 9.53 (s, 1H) , 11.34 (b r s , 1H) , 12 .54 (b r s , 1H). LC/M S: co ndition 3 , retention time = 1.40 min LC/M S(ESI +) m/z; 370 [M+H]+ LC/M S(ESI ) m/z ; 368 - Ή -MR (DMSO-d ) : 1.70-2. 10 (m, 4H) , 2 .27 (s , 3H) , 3 . 10-3 .26 (m, 2H) , 3.43-3.64 (m, 1H) , 4 .15-4 .41 ( , 2 H) , 6 .63 (s , 1H) , 6 .83-6 .89 (m, 1H) , 7.45-7. 52 (m, 1H) , 9 .54 (s , 1H) , 10.48 (s, 1H) , 12 .55 (b r s , 3 1 1H) . LC/M S: co ndition 3 , retenti on time = 1.43 mi n LC/M S(ES I+) m/z; 383 [M+H]+ LC/M S(ESI ) m/z ; 38 1 [- TABLE 99 Ex Data 1H-N MR (DMSO- ) : 1.85-2. 08 (m, 4H) , 2.13-2. 30 ( , 2H) , 2 .90-3. 03 ( , 2H) , 3 .11-3. 25 (m, 1H) , 3.55 (s , 2H) , 6.8 1 (s, 1H) , 32 7.20-7.40 (m, 5H) , 7.49 (s, 1H) , 9.52 (s, 1H) , 12.53 (br s , 1H) . LC/M S: condition 3 , retention t ime = 1.3 1 in LC/MS(ESI +) m/z; 333 [+ H-NMR (DMSO- ) : 1.87-2. 11 ( , 4H) , 2.18-2. 31 (m, 2H) , 2.88-3.02 (m, 2H) , 3 .12-3. 26 ( , 1H) , 3.65 (s , 2H) , 6.83 (s, 1H) , 7 .49 (m, 1H) , 7 .60 (d, J = 8.3 Hz, 2H) 33 , 7 .71 (d , J = 8.3 Hz, 2H) , 9.52 (s, 1H) , 12.5 3 (b r s , 1H) . LC/M S: condition 3 , re tention t ime = 1.63 min LC/M S(ESI +) m/z; 401 [M+H] + H-NMR (DMSO- ) : 1.85-2 .10 (m, 4H) , 2.19-2. 33 (m, 2H) , 2.87-3 .00 (m, 2H), 3 .10-3.26 (m, 1H) , 3.65 (s, 2H) , 6.82 (d, J = 3 .0 Hz, 1H), 7.49 (d, J = 3.0 Hz, 1H) , 7 .58 (d, J = 8.2 Hz, 2H), 7.81 (d, J 34 = 8 .2 Hz, 2H) , 9.52 (s, 1H) , 12.53 (br s , 1H) . LC/M S: condition 3 , retention tim e = 1.23 min LC/M S(ESI +) m/z; 358 [M+H] + LC/M S(ESI ) m/z; 356 [M- H] H-NMR (DMSO- ) : 1.85-2 .10 (m, 4H) , 2.18-2. 31 ( , 2H) , 2.87-2 .99 ( , 2H) , 3 .13-3. 23 (m, 1H) , 3.62 (s , 2H) , 6.83 (s, 1H) , 7.49 (s, 1H), 7 .57 (t, J = 7.8 Hz , 1H) , 7.67-7.77 (m, 2H) , 7 .94 (s, 35 1H) , 9 .52 (s , 1H) , 12 .53 (br s, 1H) . LC/M S: condition 3 , retention tim e = 1.24 min LC/M S(ESI +) m/z; 358 [M+H] + LC/M S(ESI ) m/z; 356 - H-N MR (DMSO-de) : 1.85-2. 05 (m, 4H), 2.10-2 .30 ( , 2H) , 2 .24 (s , 3H), 2 .36 (s, 3H), 2.85-2 .99 ( , 2H) , 3 .10-3. 27 (m, 1H) , 6.79 (d, J = 3.2 Hz , 1H) , 7.49 (d, = 3.2 Hz, 1H), 9.52 (s, 1H) , 12.53 (br s , 1H) . 36 LC/M S: condition 3, re tention t ime = 1.07 min LC/M S(ESI +) m/z; 352 [M+H] + LC/M S(ESI ) m/z; 350 [M-H] H-N MR (DMSO- ) : 1.86-2. 08 (m, 4H) , 2 .16-2. 29 (m, 2H) , 2.88-3. 00 (m, 2H) , 3 .10-3.25 (m, 1H) , 3 .58 (s, 2H) , 6 .82 (d, J = 3.0 Hz, 1H) , 7 .34 (d , J = 8.4 Hz, 2H), 7.46-7. 55 (m, 3H) , 9.53 (s , 1H) , 37 12.54 (br s, 1H). LC/M S: condition 3 , re tention t ime = 1.69 min LC/M S(ESI +) m/z; 417 [M+H] + LC/M S(ESI ) m/z; 415 [M- H] H-NMR (DMSO- ) : 1.87-2. 06 (m, 4H) , 2 .16-2. 30 (m, 2H) , 2 .90-3 .03 (m, 2H) , 3 .12-3.25 (m, 1H) , 3.6 3 (s, 2H) , 6 .80-6. 85 (m, 1H) , 7.49-7.53 ( , 1H) , 7 .55 (d , J = 7 .8 Hz, 2H) , 7.70 (d , J = 7 .8 Hz , 38 2H) , 9.53 (s , 1H) , 12.54 (br s, 1H) . LC/M S: condition 3 , retention t ime = 1.78 min LC/M S(ESI +) m/z; 433 [M+H] + LC/M S(ESI ) m/z; 431 [M- H] TABLE 100 Ex Data -N R (DMSO- ) : 1 .85-2. 15 (m, 4H) , 2.20-2 .38 (m, 2H) , 2 .88-3. 08 (m, 2H) , 3 . 12-3.27 (m, 1H), 3.66 (s, 2H) , 6 .82 (d , J = 3.0 Hz, 1H), 7 .49 (s, 1H), 7 .52-7 .80 (m, 4H) , 9 .52 (s, 1H) , 12 .53 (br s , 39 1H). LC/M S: condition 3 , retention tim e = 1.60 in LC/M S(ESI +) m/z; 40 1 [M+H] + LC/M S(ESI ) m/z; 399 [M- H] -NMR ( D MSO - ) : 1.95-2 .09 (m, 4H) , 2.27-2. 33 (m, 2H) , 2.96 (d , J = 11.4 Hz, 2H) , 3 . 5-3.20 (m, 1H) , 3 .69 (s, 2H) , 6.82 (dd, J = 3 .2 , 1.4 Hz, 1H), 7 .50 (t , J = 2.9 Hz, 1H) , 7.72 (d, J = 4.2 Hz , 2H) , 40 7 .84 ( , J = 9 .9 Hz, 1H) , 9 .53 (s , 1H) , 12.54 (br s , 1H) . LC/M S: condition 3 , retention tim e = 1.28 min LC/M S(ESI +) m/z; 376 [M+H] + LC/M S(ESI ) m/z; 374 [M-H] -NMR (DMS O- ) : 1 .85-2.05 (m, 4H) , 2 .14-2 .30 (m, 2H) , 2 .86-3. 00 (m, 2H) , 3 .10-3.25 ( , 1H) , 3.53 (s, 2H), 6.79 -6.8 6 (m, 1H) , 7 .33 (d, J = 8 .3 4 1 Hz, 2H) , 7 .44-7.52 (m, 1H), 7 .53 (d , J = 8.3 Hz , 2H) , 9 .52 (s, 1H) , 12 .53 ( br s , 1H) . LC/M S: condition 3 , retention tim e = 1.58 min LC/M S(ESI +) m/z; 4 11, 4 13 [M+H -NMR (DMS O- ) : 2 .15-2 .37 (m, 4H) , 3 .16-3 .30 (m, 3H) , 3 .36-3. 50 (m, 3H) , 3.50-3.73 (m, 1H) , 3.79-3.82 (m, 2H) , 7 .07 (br s , 1H), 7 .53-7. 62 (m, 3H) , 7.70-7.79 (m, 2H) , 9 .57 (s, 1H) , 9 .75-9.98 42 (br s , 1H) , 12.6 1 (b r s , 1H) . LC/M S: condition 3, retention time = 1.79 min LC/M S(ESI +) m/z; 4 15 [M+H] + LC/M S(ESI ) m/z; 4 13 [M- H] H-N MR (DMSO- ) : 1.94-2.06 (m, 4H) , 2 .20 (td, J = 10 .8, 3 .3 Hz, 2H), 2.94 (d , J = 11.7 Hz, 2H) , 3 . 18 (septet , J = 5 .2 Hz, 1H), 3.54 (s, 2H) , 6 .82 (d , J = 3 .3 Hz, 1H), 7 .16 (tt, J = 9.2 , 2 .5 Hz, 2H) , 7.40 43 (dd , J = 8.4, 5.7 Hz , 2H) , 7 .50 (d , J = 3 .3 Hz, 1H) , 9 .52 ( s , 1H) , 12 .53 (br s , 1H) . LC/M S: condition 3 , retention tim e = 1.49 min LC/M S(ESI +) m/z; 35 1 [M+H] + LC/M S(ESI ) m/z; 349 [M- H] H-NMR (DM SO- ) : 1 .86-2 .08 (m, 4H) , 2.20-2.35 (m, 2H) , 2 .92-3. 06 (m, 2H) , 3 . 10-3.25 (m, 1H) , 3.84 (s, 2H) , 6 .82 (d , J = 3.3 Hz, 1H) , 7.49 (d , J = 3 .3 Hz, 1H) , 7 .80 (s, 1H) , 9.03 (s , 1H), 9 .52 44 (s, 1H) , 12.53 (br s , 1H) . LC/M S: condition 3 , retention time = 0 .62 min LC/M S(ESI +) m/z; 340 [+] + LC/M S(ESI ) m/z; 338 [M- H] H-NMR (DM SO- ) : 1 .73- 1.88 (m, 2H) , 1.88-2. 12 (m, 4H) , 2 . 14-2. 32 (m, 2H) , 2 .33-2. 50 (m, 2 H) , 2.59-2.71 (m, 2H) , 2.98-3. 13 (m, 2H) , 3.1 4-3.25 (m, 1H), 6.82 (s, 1H) , 7 . 1 0-7.36 (m, 5H) , 7.49 45 (s, 1H) , 9.52 (s , 1H) , 12.53 (br s , 1H) . LC/M S: condition 3 , retention time = 1.55 min LC/M S(ESI +) m/z; 361 [M+H] + LC/M S(ESI ) m/z; 359 [M- H] TABLE 101 Ex Data H- MR (DMSO- ) : 1.9 1-2.05 (m, 4H) , 2 . 16-2 .23 (m, 2H), 2.94 (d , = 11.4 Hz, 2H) , 3 . 14-3. 2 1 (m, 1H) , 3 .50 (s, 2H) , 3 .83 (s, 3H), 6.82 (t, J = 2.4 Hz, 1H) , 7 .12-7 46 .20 (m, 3H) , 7 .50 (t, J = 2 .7 Hz, 1H), 9.53 (s, 1H) , 12.54 (b r s , 1H) . LC/M S: condition 3 , retention t ime = 1.39 min LC/M S(ESI +) m/z; 38 1 [M+H] + H-N MR (DMSO- ) : 1.85-2.09 (m, 4H) , 2 .22-2 .39 (m, 2H) , 2 .88-3. 03 (m, 2H), 3 .12-3 .25 ( , 1H) , 3 .78 (s, 2H), 6 .84 (d, J = 2 .8 Hz, 1H) , 7.49 (d , J = 2 .8 Hz, 1H) , 8 .00 (s, 1H) , 8 .07 (s, 2H) , 9.52 (s, 4 7 1H) , 12 .55 (b r s , 1H). LC/M S: condition 3 , retention tim e = 1.84 min LC/M S(ESI +) m/z; 469 [M+H] + LC/M S(ESI ) m/z; 467 [M- HI H-N MR (DMSO- ) : 1.88-2. 13 (m, 4H) , 2.32-2. 46 (m, 2H) , 2 . 97-3. 10 (m, 2H), 3 .14-3.27 (m, 1H) , 3 .9 1 (s, 2H), 6 .85 (d , J = 3 .0 Hz, 1H) , 7 .5 (d , J = 3 .0 Hz, 1H) , 7 .67 (d, J = 3.3 Hz, 1H) , 7 .72 (d , J 48 = 3 .3 Hz, 1H), 9 .52 (s, 1H), 12 .55 (br s , 1H). LC/M S: condition 3 , retention tim e = 0 .9 1 min LC/M S(ESI +) m/z; 340 [M+H] + LC/M S(ESI ) m/z; 338 [M- H H-NMR (DMSO- ) : 1.87-2. 07 (m, 4H) , 2 . 18-2. 34 (m, 2H) , 2 .94-3. 08 (m, 2H), 3 .12-3.34 (m, 1H) , 3 .7 1 (s, 2H) , 6 .82 (d, J = 3 .3 Hz, 1H), 6 .87 (d , J = 3.3 Hz, 1H), 6 .96 (d , J = 3.6 Hz, 1H) , 7.50 (d , J 4 9 = 3 .6 Hz, 1H) , 9 .52 (s, 1H) , 12 .55 (br s , 1H) . LC/M S: condition 3 , re tention t ime = 1.4 9 min LC/M S(ESI +) m/z; 373, 3 75 [M+H] + LC/M S(ESI ) m/z; 37 1, 373 [M- H]- -NM (DMSO- ) : 0 . 78-0. 98 ( , 2H) , 1. 12-1 .32 (m, 3H) , 1.59-1 .72 (m, 2H), 1.72-1 .85 (m, 2H), 1.85-2.04 (m, 4 H) , 2 .04-2.23 (m, 3H) , 2 .67-2 .78 (m, 2H) , 2 .88-3. 05 (m, 3H) , 3 . 08-3. 2 1 (m, 1H), 50 6.79 (s, 1H) , 7 .4 9 ( s , 1H) , 9.5 2 (s , 1H) , 12.52 (br s , 1H) . LC/M S: condition 3 , retention time = 1.5 1 min LC/M S(ESI +) m/z; 339 [M+H] + LC/M S(ESI ) m/z; 337 [M- H] H-N MR (DMSO- ) : 1.32-1 .70 (m, 6H) , 1.77-2. 05 (m, 6H) , 2 .06-2. 30 (m, 2H) , 3 .04-3 .23 (m, 3H) , 6 .80 (d , J = 3 .0 Hz, 1H) , 7.49 5 1 (s, 1H) , 9 .52 (s , 1H) , 12.53 (br s , 1H) . LC/M S: condition 3 , retention t ime = 1.18 min LC/M S(ESI +) m/z; 3 1 1 [M+H] + H-N MR (DMSC- ) : 1.86-2. 10 (m, 4H) , 2.23-2. 35 (m, 2H) , 2 .90-3.03 ( , 2H) , 3 .14-3.27 (m, 1H) , 3.7 1 (s, 2H), 6 .8 3 (d, J = 3 .3 Hz, 1H), 7 .49 (d, J = 3.3 Hz, 1H) , 7 .8 9 (d , J = 8 .1 Hz , 1H), 8 .07 (d, J 52 = 9 .3 Hz, 1H) , 8 .75 (s, 1H) , 9 .52 (s, 1H) , 12 .53 (br s , 1H) . LC/M S: condition 3 , retention tim e = 1.40 min LC/M S(ESI +) m/z; 402 [M+H] + LC/M S(ESI ) m/z; 400 [M- H] TABLE 102 Ex Data H-NMR (DMSO- ) : 1.90-1 .97 (m, 4H) , 2.26-2. 34 (m, 2H) , 2.93-2. 97 (m, 2H) , 3. 13 (qui nt , J = 6.2 Hz, 1H) , 3.72 (s, 2H) , 6.80 (dd , J = 2.9 Hz, 1.7 Hz, 1H) , 7.47 53 (t , J = 2.9 Hz, 1H) , 7 .8 1 (s, 1H) , 7.84 (s, 1H) , 9 .51 (s, 1H) , 12.51 (br s , 1H) . LC/M S: condition 3 , retention t ime = 1.26 in LC/M S(ESI +) m/z; 394 [M+H] + H-N MR (DMSO-de) : 1.95-2 .02 (m, 4H) , 2.18-2 .24 (m, 2H) , 2.94 (d , J = 11.4 Hz, 2H) , 3.55 (s, 2H) , 6 .79 (d, J = 3.0 Hz, 1H) , 7.40 (s, 4H) , 54 7.48 (d, J = 3 .0 Hz, 1H) , 9.48 (s, 1H) . LC/M S: condition 3 , retention t ime = 1.75 min LC/M S(ESI +) m/z; 367, 369 [M+H] + LC/M S(ESI ) m/z; 365, 367 [M- H] H-N MR (DMSO-d ) : 1.95-2.03 (m, 4H) , 2 . 19-2. 27 (m, 2H), 2.95 (d, J = 12.0 Hz, 2H) , 3.58 (s, 2H) , 6.80 (d , J = 2.7 Hz, 1H) , 7 .05-7 .22 55 (m, 3H) , 7.35-7.42 (m, 1H), 7.48 (d, J = 3.3 Hz, 1H) , 9.49(s, 1H) . LC/M S: condition 3 , re tention tim e = 1.61 min LC/M S(ESI +) m/z; 35 1 + H-N MR (DMSO- de) : 1.20-1 .52 (m, 4H) , 1.86-2. 10 (m, 8H) , 2.16-2 .41 (m, 3H) , 2.63-2 .80 (m, 1H) , 2 .88-3.24 (m, 3H) , 6.84 (br s , 56a 1H) , 7 .46-7. 53 (m, 1H) , 9 .52 (s, 1H) , 12.53 (br s , 1H) . LC/M S: condition 3, re tention tim e = 1.57 min LC/M S(ESI +) m/z; 393 [M+H] + LC/M S(ESI ) m/z; 39 1 [M- H] H-N MR (DMSO- d ) : 1.40-1 .66 (m, 4H) , 1.66-1 .85 (m, 2H) , 1.92-2 .18 (m, 8H) , 2 .34-2 .40 (m, 1H), 2.65-2.77 ( , 1H) , 3.08-3.28 (m, 3H) , 6 .78-6. 84 (m, 1H) , 7 .45-7. 56 (m, 1H), 9.52 (s, 1H) , 12.53 56b (br s , 1H) . LC/M S: condition 3, re tention time = 1.53 min LC/M S(ESI +) m/z; 393 [M+H] + LC/M S(ESI ) m/z; 39 1 [M- H] 1H-N MR (DMSO- ) : 1.83-2 .10 (m, 4H) , 3 .06-3.22 (m, 2H) , 3.43-3. 60 (m, 1H) , 4.20-4. 35 (m, 2H) , 6 .86 (d, J = 3.3 Hz, 1H) , 7.26 (d, J = 8.1 Hz, 1H) , 7.42-7.53 (m, 2H) , 7.79 (d , J = 8.1 Hz, 1H), 7.97 57 (s, 1H) , 8.94 (s , 1H) , 9.54 (s, 1H) , 12.57 (br s, 1H) . LC/M S: condition 3 , re tention t ime = 2 . 14 min LC/M S(ESI +) m/z; 430 [M+H] + LC/M S(ESI ) m/z; 428 [- ' H-N MR (DMSO- ) : 1.93-2 .07 (m, 4H) , 3 . 17 (br s , 1H), 3.56-3.62 ( , 2H), 4.5 8 (br s , 1H) , 6 .86 (d, J = 3 .0 Hz, 1H) , 7.50 (d , J = 3.0 Hz, 1H) , 7 .68 (d, J = 8 . 1 Hz, 2H), 7.85 (d, J = 8.4 Hz, 2H) , 9.50 (s, 58 1H). LC/MS : condition 3, retention time = 2. 13 min LC/M S(ESI +) m/z; 4 15 [M+H] + LC/M S(ESI ) m/z; 413 [M- H] TABLE3 03 Ex Data -N R (CDCI 3) : 1.20- 1.42 (m, 4 H) , 1.4 8 (s , 9H) , 1.92-2.30 (m, 5H) , 3 .10-3 .25 (m , 1H) , 3 .63 (br s , 1H) , 4 .47 (b r s, 1H) , 6.7 9 (dd , J = 3.3 , 1.8 Hz, 1H) , 7.29 (dd , J = 59 3 .3 , 1.8 Hz, 1H) , 9.22 (s , 1H) . LC/M S: co ndition 1, retenti on time = 3.74 mi n LC/M S(ES I+) m/z; 357 [M+H] + LC/M S(ESI ) m/z; 355 [M-H] H-NMR (DMSO-d ) : 1.18 (d, J = 6.6 Hz, 1H) , 1.3 8- 1.57 (m, 2H) , 1.7 1- 1.9 0 (m, 2H) , 1.9 1-2. 10 (m, 4H) , 3.05 -3.20 (m, 1H) , 3 .37-3 .54 60 (m, 1H) , 5.03 (s , 2H) , 6 .8 1 (d , J = 3 .3 Hz, 1H) , 7 .26-7 .42 (m, 5H) , 7.48 (d, J = 3.3 Hz, 1H) , 9.5 1 (s , 1H) , 12.5 1 (br s , 1H) . LC/M S: co ndition 3 , retenti on time = 2 .10 mi n LC/M S(ES I+) m/z; 391 [M+H]+ 6 1 LC/M S: co ndition 3 , retenti on time = 0.50 mi n LC/M S(ES ) m/z; 257 [M+H]+ H-NMR ( C D C I 3) : 1.15- 1.35 (m, 2H) , 1.70- 1.85 (m, 1H) , 1.86-2 .07 (m, 4H) , 2 .08-2 .23 (m, 2 H), 3 .09-3 .25 (m, 1H) , 3 .30 (d , J = 6 .3 Hz, 2H) , 3.38 (s , 3H) , 6.73-6.83 (m, 1H) , 7 .21 -7 .33 ( , 1H), 9 .02 (br s , 62 1H) , 9 .2 1 (s , 1H) . LC/M S: co ndition 1, retenti on time = 3.57 mi n LC/M S(ESI +) m/z; 2 86 [M+H] + LC/M S(ESI ) m/z ; 284 [M-H] H- MR (C D C I3) : 1.46 , ( , 2H) , 1.95 (m , 2H) , 2 .24 (m, 4H) , 3 .18 (tt, J = 12 .0, 3 . 3Hz, 1H) , 3 .34 (tt , J = 10.8 , 3.9 Hz , 1H) , 3.43 (s, 63 3H) , 6 .79 (m, 1H) , , 7.30 (m, 1H) , 9.22 (s, 1H) , 9.3 1 (b r s , 1H) . LC/M S: co ndition 1, retenti on time = 3 .13 mi n LC/M S(ESI +) m/z; 272 [M+H] + LC/M S(ES I ) m/z ; 270 [M-H] H-N MR (C D C I3) : 1.83-2 .43 (m, 8H) , 3.27-3.45 (m, 1H), 6.8 1 (dd, J = 3.3, 2.1 Hz , 1H) , 7 .28-7.39 (m, 1H) , 9.24 (s, 1H) , 9.2 5 (br s , 1H) . 64 LC/M S: co ndition 1, retenti on time = 3.59 mi n LC/M S(ES I+) m/z; 278 [M+H]+ LC/M S(ESI ) m/z ; 276 [M-H] H-N MR ( C D C I 3) : 1.23- 1.87 (m, 7H) , 2 .46 (m, 2H) , 2.57 (s, 1H), 3.22 (m, 1H) , 6 .80 (m, 1H) , 7.2 9 (t, J = 3 .3 Hz, 1H) , 9 .17 (br s, 1H) , 65 9.22 (s , 1H) . LC/M S: co ndition 1, retention time = 3.89 mi n LC/M S(ES I+) m/z; 254 [M+H]+ LC/M S(ESI ) m/z ; 252 [M-H] - H-N MR ( C D C I3) : 1.67- 1.75 (m, 6H) , 1.92 (m, 2H) , 2.06-2. 14 (m, 4H) , 3 .40 (tt, J = 9 .6, 4.8 Hz , 1H) , 6.80 (m, 1H) , 7.27 (t, J = 2.7 Hz, 66 1H) , 9 .03 (b r s , 1H) , 9.2 1 (s, 1H) . LC/M S: co ndition 1, retention time = 3.94 mi n LC/M S(ES I+) m/z; 256 [M+H]+ LC/M S(ES I ) m/z ; 254 [M-H] TABLE3 104 TABLE 05 Ex Data H- R (CDCI 3) : 1.23-1 .44 ( , 2H), 1.76-2.27 ( , 7H) , 3.09-3 .25 (m, 1H) , 3.5 1 (d , J = 6.6 Hz, 2H), 6 .79 (dd , J = 3.3, 2 .1 Hz , 1H) , 75 7 .20-7 .33 (m, 1H), 9 .03 (br s , 1H), 9 .22 (s, 1H) . LC/M S: condition 2, retention t ime = 1.75 min LC/M S(ES m/z; 290, 2 92 [+ H-N MR (CDCI 3) : 1. 15-1 .3 1 ( , 2H) , 1.32- 1.42 ( , 1H) , 1.50- 1.73 (m, 1H) , 1.85-2 .03 (m, 2 H) , 2 .04-2.25 (m, 4H) , 2 .55 (dd, J = 8.3, 6.6 Hz, 2H) , 3.06-3.25 (m, 1H) , 6.72-6. 85 (m, 1H) , 7.20-7. 36 ( , 1H) , 76 9.00 (br s , 1H) , 9 .2 1 (s, 1H) . LC/M S: condition 1, retention time = 3 .84 min LC/M S(ESI +) m/z; 288 [M+H] + LC/M S(ESL) m/z; 286 [M- H] H-NMR (CDCI 3) : 1.32-1 .50 ( , 2H), 1.90-2.09 (m, 2H) , 2 .0 1-2 .36 (m, 5H) , 2.97 (s , 3H) , 3.04 (d , J = 5.4 Hz, 2H), 3 . 10-3. 29 (m, 1H) , 6 .78 (dd, J = 2 .1, 3 .3 Hz, 1H), 7 .29 (t, J = 3.0 Hz, 1H), 9.00 (br s , 77 1H) , 9 .2 1 (s, 1H). LC/M S: condition 1, retention time = 2 .87 min LC/M S(ESI +) m/z; 334 [M+H] + LC/M S(ESI ) m/z; 332 [M- H] 1H-N MR (CDCI 3) : 1.4 1- 1 .69 (m, 2H), 1.89-2 .10 (m, 2H) , 2 .16-2 .32 (m, 4H) , 2.36-2.54 ( , 1H) , 3 .09-3. 27 (m, 1H) , 6 .70-6. 80 (m, 1H) , 7 .27-7. 35 (m, 1H) , 9.03 (br s , 1H) , 9.22 (s, 1H) , 9 .74 (d , J = 1.2 Hz , 78 1H) . LC/M S: condition 1, re tention t ime = 3 . 13 min LC/M S(ESI +) m/z; 270 [M+H] + LC/M S(ESI ) m/z; 268 [M- H] H-N MR (CDCI 3) : 1.35-1 .60 (m, 2H), 1.80-2 .40 (m, 7H) , 3 .10-3.60 (m, 1H) , 5.40-5 .90 ( , 1H) , 6 .72-6. 85 (m, 1H) , 7.20-7. 40 (m, 1H) , 79 9.02 (br s , 1H) , 9.22 (s, 1H) . LC/M S: condition 1, retention time = 3 .74 min LC/M S(ESI +) m/z; 292 [M+H] + LC/M S(ESI ) m/z; 290 [M- H] H-NMR (DMSO- ) : 1.60 (dq, J = 12 .2, 2 .3 Hz, 2H), 1.78 (dq , J = 12 .6 , 2.3 Hz, 2H) , 1.97-2 . 10 (m, 4H) , 2.26-2.37 (m, 1H) , 2 .43-2 .47 (m, 1H) , 3 . 17 (tt , J = 11.6, 3.3 Hz, 1H) , 6.86 (d, J = 3 .3 Hz, 1H) , 80 7.49 (d, J = 3 .0 Hz, 1H) , 9.52 (s, 1H) , 12.53 (br s , 1H) . LC/M S: condition 1, retention t ime = 2.70 min LC/M S(ESI +) m/z; 286 [M+H] + LC/M S(ESI ) m/z; 284 [M- H] H-N MR (CD 3OD) : 1.54 (q, J = 11.2 Hz , 2 H) , 1.91 (dq , J = 12.2, 4.0 Hz, 2H) , 2 .05-2. 18 (m, 4H), 3 .17 (dt, J = 12.9, 3.3 Hz, 1H) , 3 .67-3. 78 ( , 1H) , 6 .82 (d, J = 3 .0 Hz , 1H) , 7 .40 (d, J = 3 .3 Hz, H) , 81 9 .30 (s, 1H). LC/M S: condition 1, retention t ime = 1.79 min LC/M S(ESI +) m/z; 258 [M+H] + LC/MS(ESI ) m/z; 256 [M- H] TABLE 106 Ex Data H-NMR (CDCI 3) : 2.38-2.47 ( , 4H) , 2.53-2.65 ( , 2H) , 2 .7 1 (dt, J = 14.5, 5.0 Hz, 2H) , 3 .65-3. 77 (m, 1H) , 6.80 (dd , J = 3.6, 2 .0 Hz, 1H) , 7 .33 82 (t, J = 3 .0 Hz, 1H) , 9 .26 (s, 2H) . LC/M S: condition 1, retention t ime = 2.55 min LC/M S(ESI +) m/z; 256 [M+H] + LC/M S(ESI ) m/z; 254 [M- H] Ή -NMR (CD 3OD) : 1.79 ( , 4 H) , 1.97 (m, 2H), 2.34 (m, 2H) , 3.26 (m, 1H) , 4 .10 (br s , 1H) , 6.96 (d, J = 3 .3Hz , 1H) , 7 .37 (d, J = 3.0 Hz , 83 1H) , 7.89 (s, 1H) , 9.28 (s, 1H) . LC/M S: condition 1, retention t ime = 2.67 min LC/M S(ESI +) m/z; 258 [M+H] + LC/M S(ESI ) m/z; 256 [M- H] H-N MR (CDCI 3) : 1.97-2.09 (m, 4H), 3.02 (br s , 2H), 3 .19-3. 26 (m, 1H) , 4 .37 (br s , 2H) , 5. 1 8 (s, 2H) , 6.61 (dd , J = 3.2, 2 .3 Hz , 1H) , 84 7 .09 (t, J = 3.0 Hz, 1H) , 7 .28-7. 4 1 (m, 5H) , 8 .11 (s , 1H) , 8.50 (s , 1H) , 8 .89 (br s , 1H) . LC/M S: condition 3 , re tention t ime = 2 .05 min LC/M S(ESI +) m/z; 376 [M+H] + H-NMR (DMSO-af ) : 1.64-1 .92 (m, 4H) , 3 .0 1 ( br s , 2H) , 3.20-3.30 (m, 1H) , 4.07-4.20 (m, 2H) , 5 .12 (s, 2H) , 6.63 (br s , 1H), 7 .14-7.20 ( , 1H) , 7.29-7.43 ( , 5H), 8.63 (s , 1H) , 12.05 (br s , 1H), 13 . 14 (br 85 s , 1H) . LC/M S: condition 3 , retention tim e = 2.20 min LC/M S(ESI +) m/z; 408 [M+H] + LC/M S(ESI ) m/z; 406 [-  H-N MR (DMSO- ) : 1.62-1 .76 (m, 2H) , 1.90-2. 09 (m, 2H) , 2 .13-2.28 (m, 2H) , 2 .85-3. 05 ( , 3H) , 3 .63 (s , 2H) , 6 .56 (br s , 1H) , 7 . 14-7.2 1 (m, 1H) , 7 .69 (d, J = 8 .3 Hz , 2H) , 7 .7 1 (d, J = 8 .3 Hz, 2H) , 86 8 .64 (s, 1H) , 12 .05 (br s , 1H) , 13 . 14 (br s , 1H) . LC/M S: condition 3 , retention t ime = 1.64 min LC/M S(ESI +) m/z; 432 [M+H] + LC/M S(ESI ) m/z; 430 [M- H] LC/M S: condition 3 , retention t ime = 2 .0 1 min 87 LC/MS (ESI +) m/z; 349 [M+H] + LC/M S(ESI ) m/z; 347 [M- H] ' H-N MR (CDCI 3) : 1.07-1 .33 (m, 2H), 1.45- 1.73 (m, 1H) , 1.80-2.28 (m, 6H) , 2.40 (d , J = 7 . 1 Hz, 2H) , 2.90-3. 28 (m, 9H) , 6.7 1-6.84 (m, 88 1H) , 7 .20-7. 40 ( , 1H) , 9 .02 (br s , 1H) , 9.22 (s, 1H) . LC/M S: condition 1, retention t ime = 1.84 min LC/M S(ESI +) m/z; 389 [M+H] + LC/M S(ESI ) m/z; 387 [M-H] H-N MR (CDCI 3) : 1.04-1 .24 (m, 2H) , 1.60-2.40 (m, 15H) , 2.55-2.77 (m, 3H) , 3 .05-3 .25 (m, 1H) , 6 .7 1-6 .84 (m, 1H) , 7 .20-7 .36 (m, 1H), 89 8 .99 (br s , 1H), 9.2 1 (s, 1H) . LC/M S: condition 1, retention tim e = 0 .39 min LC/M S(ESI +) m/z; 364 [M+H] + LC/M S(ESI ) m/z; 362 [M- H] TABLE 107 Ex Data H- MR ( C D C I3) : 1.2 1- 1 .32 (m, 2H) , 1.40-2.27 ( , 8H) , 2 .50-2.75 (m, 4H), 2 .97 (t, J = 6.3 Hz, 2H) , 3 . 10-3 .25 (m, 1H) , 6.7 1-6 .87 ( , 1H) , 7 .20-7 .35 (m, 90 1H), 9.00 (br s, 1H), 9 .2 1 (s, 1H). LC/M S: condition 1, re tention t ime = 0 .37 min LC/M S(ESI +) m/z; 324 [M+H] + LC/M S(ESI ) m/z; 322 [M- H] H-NMR ( C D C I3) : 1.05-1 .3 1 (m, 2H) , 1.6 1- 1.80 ( , 1H) , 1.8 1- 1.99 (m, 2H), 2.00-2 .20 (m, 4H) , 2 .24 (d, J = 7 .1 Hz, 2H) , 2.39-2.53 ( , 4H) , 3 .10-3.25 (m, 1H) , 3.65 -3.8 1 (m, 4H) , 6 .7 1-6. 85 (m, 1H) , 91 7.20-7. 35 (m, 1H) , 9.00 (br s , 1H), 9.2 1 (s, 1H) . LC/M S: condition 1, re tention t ime = 0 .37 min LC/M S(ESI +) m/z; 34 1 [M+H] + LC/M S(ESI ) m/z; 339 [-  H-N MR (DMSO- ) : 1.15-1 .40 (m, 2H) , 1.55-1 .90 (m, 3H) , 1.92-2. 12 (m, 4H) , 2.99-3.09 (m, 2H) , 3 .00-3.26 (m, 1H) , 6.69 (d , J = 8.9 Hz, 2H) , 6.8 1 (d , J = 3 .3 Hz, 2H) , 7 .45 (d, J = 8.6 Hz, 2H) , 7.50 92 (d, J = 3.3 Hz , 1H), 9 .52 (s, 1H) , 12 .54 (br s , 1H) . LC/M S: condition 1, retention t ime = 3 .95 min LC/M S(ESI +) m/z; 372 [M+H] + LC/M S(ESI ) m/z; 370 [-  -NMR ( C D C I3) : 1. 10-1 .3 1 (m, 2H) , 1.50- 1.77 ( , 1H) , 1.82-2.20 (m, 6H) , 2.56 (d , J = 6 .6 Hz, 2 H) , 3.07-3.23 (m, 1H) , 3 .89 (s, 2H) , 6 .78 (dd , J = 3.3, 2 . 1 Hz, 1H) , 7.2 1-7.32 (m, 1H) , 7.48 (d , J = 8 .6 93 Hz, 2H) , 7 .56-7. 68 (m, 2H) , 9 .02 (br s , 1H), 9 .2 1 (s, 1H). LC/M S: condition 1, retention t ime = 2 .27 min LC/M S(ESI +) m/z; 386 [M+H] + LC/M S(ESI ) m/z; 384 [M- H] H-N MR ( C D C I3) : 1.10-1 .30 (m, 2H), 1.50- 1.75 (m, 1H) , 1.82-2.30 (m, 8H) , 2.33-2 .60 (m, 3H) , 2 .63-2 .97 (m, 3H) , 3 .05-3.40 (m, 1H) , 5 .02-5 .33 (m, 1H) , 6.72-6.84 (m, 1H), 7 .20-7. 34 (m, 1H) , 9.15 (br s , 94 1H) , 9 .2 1 (s, 1H) . LC/M S: condition 1, re tention t ime = 0.44 min LC/M S(ESI +) m/z; 343 [M+H] + LC/M S(ESI ) m/z; 341 [M- H] H-N MR ( C D C I3) : 1.04-1 .32 (m, 2H) , 1.50- 1.77 (m, 1H) , 1.8 1-2 .29 (m, 8H) , 2.33-2.6 1 (m, 3H) , 2 .65-2. 98 (m, 3H) , 3.09-3 .40 (m, 1H) , 5.00-5. 35 (m, 1H), 6.73-6.85 (m, 1H) , 7 .2 1-7. 35 (m, 1H) , 9.12 (br s, 95 1H) , 9 .2 1 (s, 1H) . LC/M S: condition 1, retention t ime = 0.42 min LC/M S(ESI +) m/z; 343 [M+H] + LC/M S(ESI ) m/z; 341 [M- H] H-NMR (C D C I3) : 1.05-1 .2 1 (m, 2H), 1.23 (s, 6H) , 1.48-1 .66 (m, 1H), 1.79-2. 17 (m, 8H) , 2 .43 (d, J = 6 .8 Hz, 2H), 3 .00-3 .23 (m, 1H) , 3.05 (s, 2H), 6.72-6.82 (m, 1H), 7.20-7 .32 (m, 1H) , 9.2 1 (s, 1H) , 96 9 .41 (br s , 1H) . LC/M S: condition 1, re tention t ime = 0 .79 min LC/M S(ESI +) m/z; 339 [M+H] + LC/M S(ESI ) m/z; 337 [M-HV TABLE 108 Ex Data -NMR ( C D C I3) : 1.05-1 .33 (m, 2H) , 1.50- 1.80 (m, 1H) , 1.82-2 .20 (m, 10H) , 2 .28 (d, J = 7.4 Hz, 2H) , 2.4 9-2. 62 (m, 4H), 3.0 7-3. 44 (m, 1H) , 6.79 (dd , J = 3.3, 2. 1 Hz, 1H) , 7.20-7. 34 ( , 1H), 9 .15 (br s , 97 1H) , 9 .22 (s, 1H) . LC/M S: condition 1, retention t ime = 0 .62 min LC/M S(ESI +) m/z; 375 [M+H] + LC/M S(ESI ) m/z; 373 [M- H] H-N MR (DMSO- d ) : 1.06-1 .30 (m, 2H) , 1.50-1 .66 (m, 1H) , 1.68-1 .85 (m, 2H) , 1.90-2. 08 (m, 4H), 2.42 (d, J = 6.6 Hz, 1H) , 3 .03-3.20 (m, 1H) , 3.25-3.38 (m, 1H) , 3.8 1 (s, 2H) , 6 .70-6. 85 (m, 1H) , 7.40-7.5 1 (m, 1H) , 7 .58 (d , J = 8 98 .3 Hz, 2H) , 7 .67 (d, J = 8 .0 Hz , 2H), 9 .51 (s, 1H) , 12.51 (br s, 1H) . LC/M S: condition 1, re tention t ime = 2.95 min LC/M S(ESI +) m/z; 429 [M+H] + LC/M S(ESI ) m/z; 427 [M- H] H-N MR (DMSO- d ) : 1.19-1 .40 (m, 2H) , 1.65-1 .88 (m, 3H) , 1.95-2 .11 (m, 4H) , 2 .95-3. 07 (m, 2H) , 3 .10-3.25 (m, 1H) , 6.40-6.52 (m, 1H) , 6.69 (d, J = 8.6 Hz, 2H), 6 .76-6. 87 (m, 1H), 7.36 (d , J = 8.6 99 Hz, 2H) , 7.45-7. 55 (m, 1H), 9.51 (s, 1H) , 12 .52 (br s , 1H). LC/M S: condition 1, re tention time = 4 .49 min LC/M S(ESI +) m/z; 415 [M+H] + LC/M S(ESI ) m/z; 413 [M- H] ' H-N MR (DMSO- ) : 1.16-1 .40 (m, 2H) , 1.61- 1 .88 (m, 3H) , 1.94-2. 10 (m, 4H), 2.85-3.00 (m, 2H) , 3.10-3.25 (m, 1H) , 5.52-5 .65 100 (m, 1H) , 6.50-6.63 (m, 2H) , 6 .76-6. 82 (m, 1H) , 6 .85-6. 98 (m, 2H) , 7.49 (t, J = 3.0, 1H) , 9.5 1 (s, 1H) , 12.52 (br s , 1H) . LC/M S: condition 1, re tention tim e = 3 .63 min LC/M S(ESI + m/z; 365 [+ H-N MR (DMSO- ) : 1. 10-1 .30 (m, 2H) , 1.50-2. 10 (m, 9H) , 3 .08-3.2 1 (m, 1H), 3 .69-3. 90 (m, 2H) , 6.79 (d , J = 3.3 Hz, 1H) , 10 1 7.10-7 .25 (m, 2H), 7.38-7 .56 ( , 3H) , 9.51 (s, 1H), 12.52 (br s , 1H) . LC/M S: condition 1, retention time = 2 .67 min LC/M S(ESI +) m/z; 379 [M+H] + LC/M S(ESI ) m/z; 377 [M- H] ' H-N MR (DMSO- ) : 1. 18-1 .40 (m, 2H) , 1.60-2. 10 ( , 7H), 2.92 (s , 3H) , 3.05-3.25 (m, 3H) , 6.68 (dd , J = 9.5 , 4.2 Hz, 2H) , 6 .76-6. 83 (m, 1H), 6 .94-7. 08 (m, 2 H) , 7.41 -7. 54 (m, 1H), 9.50 (s , 1H), 12.52 (br s , 102 1H) . LC/M S: condition 1, retention t ime = 3 .80 min LC/M S(ESI +) m/z; 379 [M+H] + LC/M S(ESI ) m/z; 377 [M- H] Ή -NMR (DMSO- ) : 1. 15-1 .37 (m, 2H) , 1.65-1 .88 (m, 3H) , 1.91-2 .08 (m, 4H) , 2 .12 (s, 3H), 3.05-3.23 (m, 3H), 5 .89-6. 00 (m, 1H), 6 .65 (d, J = 8.6 Hz , 1H), 6 .75-6. 84 (m, 1H), 7 .26-7 .53 (m, 3H) , 103 9.5 1 (s , 1H) , 12.5 1 (br s, 1H) . LC/M S: condition 1, re tention t ime = 4 .07 min LC/M S(ESI +) m/z; 386 [M+H] + LC/M S(ESH m/z; 384 [- TABLE 109 Ex Data H-NMR (DMSO- ) : 1.15-1 .38 (m, 2H) , 1.66-1 .90 (m, 3H) , 1.95-2. 10 (m, 4H) , 2 .13 (s, 3H) , 2.95-3.08 ( , 2H) , 3 . 10-3. 25 ( , 1H), 6 .56 ( , J = 8.3 Hz, 1H) , 6.76-6. 85 ( , 1H) , 6 .9 1-7 .05 (m, 2H) , 104 7.41 -7. 54 (m, 1H) , 9.51 (s, 1H), 12.51 (br s, 1H). LC/M S: cond ition 1, retention t ime = 4 .67 min LC/M S(ESI +) m/z; 445 [M+H] + LC/M S(ESI ) m/z; 443 [M- H] H-N MR (D MSO- ) : 1. 15-1 .40 (m, 2H) , 1.65-1 .88 (m, 3H) , 1.95-2. 10 ( , 4H), 3 .01-3.25 (m, 3H), 6.75-6.95 ( , 2H) , 7.0 1-7. 12 (m, 1H) , 7.27-7.39 (m, 1H) , 7.43-7. 53 (m, 1H) , 7.66-7. 77 ( , 1H), 105 9.5 1 (s , 1H) , 12.52 (br s , 1H) . LC/M S: condition 1, re tention t ime = 4.22 min LC/M S(ESI +) m/z; 440 [M+H] + LC/M S(ESI ) m/z; 438 [M- H] H-N MR (DMSO- ) : 1.06-1 .29 ( , 2H) , 1.45-1 .63 (m, 1H) , 1.65-1 .85 (m, 2H) , 1.89-2.07 ( , 4H) , 2.32-2 .62 (m , 2 H) , 2.39 (s, 3H) , 3.05-3.20 (m, 1H), 3.74-3.89 (m, 2H), 6.55-6.67 (m, 1H) , 6.7 1 (d, J = 3.3 Hz, 1H), 6.80 106 (d, J = 2.7 Hz, 1H) , 7.42-7.54 (m, 1H) , 9.50 (s, 1H) , 12.5 1 (b r s , 1H) . LC/M S: condition 1, retention t ime = 2.75 min LC/M S(ESI +) m/z; 38 1 [M+H] + LC/M S(ESI ) m/z; 379 [M- H] ' H-N MR (DMSO- ) : 1.06-1 .30 (m, 2H) , 1.45-1 .63 (m, 1H) , 1.65-1 .87 (m, 2H) , 1.89-2. 08 ( , 4H) , 2.77 (t, J = 5.4 Hz, 1H) , 2.8 1-2 .91 (m, 1H) , 3 .05-3 .20 (m, 1H) , 4.39 (t, J = 5.1 Hz, 1H) , 107 4.49-4. 61 ( , 1H) , 6.72-6.85 ( , 1H) , 7.40-7. 53 (m, 1H) , 9 .51 (s, 1H) , 12 .51 (br s, 1H) . LC/M S: condition 1, re tention time = 0.39 min LC/M S(ESI +) m/z; 3 17 [M+H] + LC/M S(ESI ) m/z; 3 15 [M- H] - MR (DMSO-d ) : 1.19-1 .42 (m, 2H), 1.60-2 .10 (m, 7H) , 3.05 (s , 3H), 3.07-3. 22 (m, 1H) , 3.25 -3.4 1 ( , 2H) , 6 .70-6. 90 (m, 3H) , 108 7 .40-7.60 (m, 3H) , 9 .50 (s, 1H) , 12.51 (br s , 1H) . LC/M S: condition 1, retention t ime = 4 .10 min LC/M S(ESI +) m/z; 386 [M+H] + LC/M S(ESI ) m/z; 384 [- H-N MR (C D C I3) : 1.12-1 .28 (m, 2H) , 1.33 (d, J = 6 .6 Hz, 3H) , I .37-2. 16 (m, 7H) , 2 .30 (dd , J = 11.4, 6.9 Hz, 1H) , 2.48 (dd , J = I I .7 , 6.3 Hz, 1H) , 3 .15 (tt, J = 12.0, 3.3 Hz, 1H) , 3.74 (q, J = 6.3 109 Hz, 1H) , 6.77 (d , J = 2.4 Hz, 1H) , 7 .05-7. 7.28 (m, 4H) , 9 .23 (s, 1H) , 9 .52 (br s , 1H) . LC/M S: condition 1, re tention t ime = 2 .89 min LC/M S(ESI +) m/z; 411 [M+H] + LC/M S(ESI ) m/z; 409 - TABLE 1 10 Ex Data H-NMR (CDCI 3) : 1.22 (m, 2H) , 1.86-2 .17 ( , 7H) , 2.58 ( , J = 6.6 Hz, 2H) , 3 .18 (tt , J = 11.7 , 3 .6 Hz, 1H) , 3.83 (s, 2H), 6.77 (m, 1H) , 7 .16-7. 39 ( , 5H), 110 9 .22 (s, 1H) , 9 .43 (br s , 1H) . LC/M S: condition 1, retention t ime = 3 .03 min LC/M S(ESI +) m/z; 445 [M+H] + LC/M S(ESI ) m/z; 443 [M- H] Ή -NMR ( C D C I3) : 1.22 (m, 2H) , 1.85-2. 14 (m, 7H) , 2 .58 (d , J = 6 .6 Hz, 2H), 2 .72-2 .95 ( , 4H) , 3 . 16 (tt , J = 11.7 , 3.3 Hz, 1H) , 6 .78 (d, J 111 = 3 .9 Hz, 1H), 6 .95-7. 27 (m, 5H), 9.2 1 (s, 1H) . LC/M S: condition 1, retention t ime = 2.8 1 min LC/M S(ESI +) m/z; 393 [M+H] + LC/M S(ESI ) m/z; 39 1 [M- H] H-N MR ( C D C I3) : 1.25 (m, 2H) , 1.70 (m, 1H) , 1.86-2. 18 ( , 6H), 2 .57 (d , J = 6.6 Hz, 2H) , 3 . 7 (tt , J = 11.7 , 3.6 Hz, H) , 3.84 (s, 2H) , 6.78 (m, 1H) , 7 .15 (t , J = 9.9 Hz, 1H), 7 .29 (t, J = 2 .7 Hz, 1H) , 7.54 2 (m, 1H) , 7 .60 (dd , J = 6 .9, 1.5 Hz, 1H) , 9.25 (s, 1H), 9 .60 (br s , 1H) . LC/M S: condition 1, re tention t ime = 2.97 min LC/M S(ESI +) m/z; 447 [M+H] + LC/M S(ESI ) m/z; 445 [M- H] H-NMR ( C D C I 3) : 1.22 (m, 2H) , 1.87-2 .17 (m, 7H) , 2.57 (d, J = 6.6 Hz, 2H) , 3.06 (s, 3H), 3 . 16 (tt, J = 12 .0 , 3.3 Hz, 1H) , 3 .93 (s, 2H) , 1 3 6 .78 ( , 1H) , 7.27, (m, 1H) , 7.58 (d, J = 8.4 Hz, 2H) , 7 .90 (d, J = 8 .7 Hz , 2H), 9 .09 (br s , 1H), 9.2 1 (s, 1H) . LC/M S: condition 1, re tention t ime = 0.70 min LC/M S(ESI +) m/z; 439 [+ H-NMR (DMSO- ) : 1.27 (q, J = 11.4 Hz, 2H) , 1.68-1 .8 5 (m, 3H) , 1.96-2. 09 ( , 4H) , 2.94 (t, J = 5 .7 Hz , 1H) , 3. 17 (d , J = 5.3 Hz, 2H) , 5 .96 (t, J = 5.7 Hz, 1H) , 6.62 (d , J = 9 .0 Hz, 2H), 6.80 (d d, J = 3 .3 , 114 1.2 Hz, 1H) , 7 .04 (d , J = 8 .6 Hz, 2H) , 7 .48 (t, J = 2 .5 Hz, 1H) , 9 .5 1 (s, 1H) , 12.5 1 (b r s , 1H) . LC/M S: condition 1, retention time = 4.49 min LC/M S(ESI +) m/z; 431 [M+H] + LC/M S(ESI ) m/z; 429 [M-H] H-NMR (DMSO- ) : 1.26 (q, J = 11.4 Hz, 2H) , 1.76 (q , J = 12.3 Hz, 3H) , 1.92-2 .07 (m, 4H) , 3.10 (t, J = 6 .1 Hz, 2H) , 5 .61 (t, J = 6 . 1 Hz, 1H) , 6 .78-6.82 (m, 2H), 7 .17 (dd , = 8.6 , 2 .5 Hz, 1H) , 7.35 (dd, 115 J = 2 . 9 , 0.8 Hz, 1H) , 7.48 (t, J = 2 . 9 Hz, 1H) , 9.5 1 (s, 1H) , 12 .5 1 (br s , 1H). LC/M S: condition 1, retention time = 4 .77 min LC/M S(ESI +) m/z; 465 [M+H] + LC/M S(ESI ) m/z; 463 [M- H] TABLE 111 Ex Data H-N MR (DMSO- ) : 1.25 (q, J = 11.4 Hz, 2H) , 1.67-1 .83 ( , 3H) , 1.91-2. 07 (m, 4H) , 3 .08-3.22 (m, 3H) , 6 .08 (t, J = 5 .7 Hz, 1H) , 6 .79-6. 87 ( , 2H) , 7 .33 (td, J = 9 .0 , 3 .3 Hz, 1H) , 7.42 (dd , J = 8.6 , 116 2.9 Hz, 1H) , 7 .48 (d, J = 2.9 Hz, 1H) , 9.5 1 (s, 1H) , 12.5 1 (br s , 1H). LC/M S: condition 1, retention tim e = 4 .15 min LC/M S(ESI +) m/z; 390 [M+H] + LC/M S(ESI ) m/z; 388 [M- H] Ή -NMR (DMSO- ) : 1.25 (dq , J = 12.3, 2.5 Hz, 2H) , 1.67-1 .83 (m, 3H), 1.94-2 .03 (m, 4 H) , 3.07-3. 22 ( , 3H), 5.33 (t, J = 5 .7 Hz, 1H) , 6 .80 (d, J = 2 .9 Hz, 1H) , 6 .88 (dd , J = 9 .0 , 4.5 Hz, 1H) , 7 .28 (dd, J = 9.0 , 3.3 Hz, 1H) , 7.33 (dd , J = 9.0, 3 .3 7 Hz, 1H) , 7 .48 (br s , 1H) , 9 .50 (s, 1H) , 12 .51 (br s , 1H) . LC/M S: condition 1, retention tim e = 4.55 min LC/M S(ESI +) m/z; 433 [M+H] + LC/M S(ESI ) m/z; 431 [M- H] H-NMR (DMSO- c ) : 1.26 (q , J = 11.9 Hz, 2H) , 1.67-1 .84 ( , 3H) , 1.96-2. 08 (m, 4 H) , 2.90 (br s , 5H) , 3.17 (t , J = 12.3 Hz, 1H) , 3.3 1 (s, 2H), 3.71 (t, J = 3 .7 Hz, 4H) , 6.55 (d , J = 7 .8 Hz, 2H) , 6.77 (d , J = 118 7 .8 Hz, 2H) , 6 .80 (dd, J = 3 .3 , 2.0 Hz, 1H) , 7.48 (t, J = 2 .9 Hz, 1H) , 9 .51 (s, 1H) , 12 .52 (br s , 1H) . LC/M S: condition 1, retention time = 2 .80 min LC/MS (ESI +) m/z; 432 [M+H] + LC/M S(ESI ) m/z; 430 [M- H] Ή -NMR (CDCI 3) : 1.06- 1.37 (m, 2H), 1.57-2.37 (m, 11H) , 2.3 8-2 .47 (m, 2H) , 2.48-2 .59 (m, 1H) , 2.72-2 .87 (m, 1H) , 2.90-3 .04 (m, 1H) , 3 .09-3.25 (m, 1H) , 4 .25-4. 44 (m, 1H) , 6.71 -6.87 ( , 1H) , 7.22-7. 38 19 (m, 1H) , 9 . 10 (br s , 1H) , 9 .21 (s , 1H) . LC/M S: condition 1, retention tim e = 0 .39 min LC/MS (ESI +) m/z; 34 1 [M+H] + LC/M S(ESI ) m/z; 339 [M-H] H-NMR (CD CI3) : 1.11- 1 .33 (m, 2H), 1.42-1 .8 1 (m, 2H), 1.83-2 .23 (m, 10H) , 2.51 -2.83 ( , 4H) , 3.07-3 .25 (m, 1H), 3 .70-3. 94 ( , 2H), 3 .99-4. 14 ( , 1H) , 6.72-6.83 (m, 1H) , 7.2 1-7. 35 (m, 1H) , 9.05 (br s , 120 1H), 9.2 1 (s, 1H) . LC/M S: condition 1, retention tim e = 1. 19 min LC/MS (ESI +) m/z; 355 [M+H] + LC/M S(ESI ) m/z; 353 [M- H] LC/M S: condition 1, retention tim e = 3.74, 3 .87 min (cis/trans 121 mixture) LC/M S(ESI +) m/z; 358 [M+H] + LC/MS(ESI ) m/z; 356 [M- H] LC/M S: condition 1, retention time = 0 .36 min (cis/trans mixtu re) 122 LC/MS (ESI +) m/z; 362 [M+H] + LC/M S(ESI ) m/z; 360 [M- H] LC/M S: condition 1, retention time = 2 .6 1 min (cis/trans mixtu re) 123 LC/M S(ESI +) m/z; 36 1 [M+H] + LC/M S(ESI ) m/z; 359 [M- H] TABLE3 112 Ex Data LC/M S: condition 1, re tention tim e = 0.39 min (cis/trans mixtu re) 124 LC/M S(ESI +) m/z; 327 [M+H] + LC/M S(ESI ) m/z; 325 [M- H] LC/M S: condition 1, retention t ime = 3.04 min (cis/trans mixture) 125 LC/M S(ESI +) m/z; 429 [M+H] + LC/M S(ESI ) m/z; 427 - LC/M S: condition 1, re tention t ime = 0 .36 min (cis/trans mixtu re) 26 LC/M S(ESI +) m/z; 370 [M+H] + LC/M S(ESI ) m/z; 368 [M- H] LC/M S: condition 1, re tention t ime = 0 .37 min (cis/trans mixtu re) 127 LC/M S(ESI +) m/z; 350 [M+H] + LC/M S(ESI ) m/z; 348 [M- H] LC/M S: condition 1, retention tim e = 4.25 , 4 .39 min (cis/trans 128 mixtu re) LC/M S(ESI +) m/z; 40 1 [M+H] + LC/M S(ESI ) m/z; 399 [M- H] LC/M S: condition 1, retention t ime = 3 .95 min (cis/trans mixtu re) 129 LC/M S(ESI +) m/z; 376 [M+H] + LC/M S(ESI ) m/z; 374 [M- H] LC/M S: condition 1, re tention tim e = 2 .79 min (cis/trans mixtu re) 130 LC/M S(ESI +) m/z; 365 [M+H] + LC/M S(ESI ) m/z; 363 [M- H] LC/M S: condition 1, retention tim e = 2.84, 3 .24 min (cis/trans 131 mixtu re) LC/M S(ESI +) m/z; 35 1 [M+H] + LC/M S(ESI ) m/z; 349 [M- H] LC/M S: condition 1, retention tim e = 3.94, 4 .02 mi n (cis/trans 132 mixtu re) LC/M S(ESI +) m/z; 372 [M+H] + LC/M S(ESI ) m/z; 370 [M- H] LC/M S: condition 1, re tention t ime = 4.45 min (cis/trans mixtu re) 133 LC/M S(ESI +) m/z; 431 [M+H] + LC/M S(ESI ) m/z; 429 -  ' H-N MR (DMSO- ) : 1.82-1 .95 ( , 6H) , 2 .07-2 .23 (m, 2H) , 3 .35-3.43 (m, 1H), 3 .67 (br s , 1H) , 6 .77-6. 73 (m, 3H) , 6 .86 (dd , J = 134 2 .9, 1.2 Hz, 1H), 7.44 (d , J = 9.0 Hz, 2H) , 7 .50 (t , J = 2.9 Hz , 1H) , a 9.53 (s, 1H), 12.53 (br s , 1H). LC/M S: condition 1, re tention t ime = 3 .88 min LC/M S(ESI +) m/z; 358 [M+H] + LC/M S(ESI ) m/z; 356 [M- H] H-N MR (DMSO-d ) : 1.48 (dq , J = 11.9, 3.7 Hz, 2H) , 1.86-2. 18 ( , 6H), 3 . 15-3. 25 (m, 1H) , 3.50 (br s , 1H) , 6.64 (d , J = 8. 1, 1H) , 6.72 134 (d, J = 8.6 Hz, 2H), 6 .90 (dd , J = 3.3, 1.6 Hz, 1H) , 7 .44 (d, J = 8.6 b Hz, 2H), 7 .50 (t, J = 2 .9 Hz, 1H) , 9 .52 (s, 1H) , 12 .53 (br s , 1H) . LC/M S: condition 1, retention tim e = 3 .74 min LC/M S(ESI +) m/z; 358 [M+H] + LC/M S(ESI ) m/z; 356 [M- H] TABLE 113 Ex Data ' H-N MR (CDCI 3) : 1.91 (m, 6H) , 2 .29 ( , 2H) , 2.92 (m, 5H), 3.34 (tt , J = 9 .9, 3 .6Hz, 1H) , 7 . 1 0 ( , J = 3 .3 Hz, 1H) , 7 .18-7.33 (m, 6H) , 135 9.2 1 (s, 1H) , 9 .69 (br s , 1H) . a LC/M S: condition 1, retention tim e = 2.78 min LC/M S(ESI +) m/z; 36 1 [M+H] + LC/M S(ESI ) m/z; 359 [M- H] -NMR (C D C I3) : 1.30 (m, 2H) , 1.88 (m, 2H) , 2 .07 (m, 4H) , 2 .62 (tt , J = 11.4, 3.3 Hz, 1H) , 2.79 (t , J = 7.5 Hz, 2H) , 2.95 (t , J = 7.2 Hz, 2H), 3 .10 (tt, J = 12.3, 3.3H z , 1H) 135 , 6 .68 (d , J = 2 .7 Hz, 1H) , b 7 .12-7 .26 (m, 6H), 9.15 (s, 1H) , 9 .95 (br s , 1H) . LC/M S: condition 1, retention t ime = 2 .5 1 min LC/M S(ESI +) m/z; 361 [M+H] + LC/M S(ESI ) m/z; 359 [M- H H-N MR (C D C I3) : 1.31 - 1.94 (m, 10H) , 2.30 (m, 1H) , 2.72 ( , 4H) , 2 .92 (s, 1H) , 3 .30 (m, 1H), 7 . 14-7. 34 (m, 7H) , 9.2 1 (s, 1H), 9.48 (br 136 s , 1H) . a LC/M S: condition 1, retention time = 2.84 min LC/M S(ESI +) m/z; 375 [M+H] + LC/M S(ESI ) m/z; 373 [M- H] H-N MR (CDCI 3) : 1.37 (m, 2H), 1.80-2 .0 1 (m, 5H) , 2 . 13 ( , 4H) , 2 .63 (m, 1H) , 2 .70 (t , J = 7.5 Hz, 1H) , 2 .76 (t, J = 7 .5 Hz, 1H) , 3.26 136 (m, 1H) , 3 . 17 (m, 1H) , 6 .76 (d, J = 3.6Hz, 1H) , 7 .16-7.34 (m, 6H) , b 9.2 1 (br s , 1H) , 9.2 1(s, 1H). LC/M S: condition 1, retention t ime = 2 .76 min LC/M S(ESI +) m/z; 375 [M+H] + LC/M S(ESI ) m/z; 373 [M- H] H-N MR ( C D C I3) : 1.37 (m, 2H) , 1.80-2 .0 1 (m, 5H) , 2 . 13 (m, 4H) , 2.63 (m, 1H) , 2.70 (t, J = 7.5 Hz, 1H) , 2.76 (t, J = 7.5 Hz, 1H) , 3 .26 136 (m, 1H) , 3 . 17 (m, 1H) , 6 .76 (d , J = 3 .6Hz, 1H) , 7 .16-7.34 (m, 6H) , b 9.2 1 (br s , 1H) , 9.2 1(s, 1H) . LC/M S: condition 1, re tention tim e = 2 .76 min LC/M S(ESI +) m/z; 375 [M+H] + LC/M S(ESI ) m/z; 373 [M- H] H-N MR (DMSO- ) : 1.56-1 .7 1 (m, 4H) , 1.80-1 .90 (m, 2H) , 2 . 19-2. 35 (m, 2H) , 2 .84 (br s , 1H) , 3. 19-3. 26 (m, 1H) , 3 .84 (br s , 137 2H), 7.08 (d , J = 3.0 Hz, 1H), 7 .43 (t, J = 2 .6 Hz, 1H) , 7.63 (d , J = a 8 .3 Hz , 2H) , 7 .83 (d, J = 8 .3 Hz, 2H), 9.52 (s , 1H) , 12 .5 1 (br s, 1H) . LC/M S: condition 1, retention t ime = 1.03 min LC/M S(ESI +) m/z; 372 [M+H] + 1H-N MR (C D C I3 ) : 1.40 (dq , J = 12.6, 3 .3 Hz, 2H) , 1.96 (dq , J = 12 .9 , 4 .0 Hz, 2H) , 2 .12-2 .22 (m, 4H) , 2 .7 1 (tt, J = 11.2 , 3 .6 Hz, 1H) , 3 . 19 (tt, J = 12 .2, 3.3 Hz, 1H) , 3.96 (s, 2H) , 6 .77 (dd , J = 3 .6, 2 .3 137 Hz, 1H) , 7.30 (t, J = 3.0 Hz, 1H) , 7 .50 (d , J = 7.9 Hz, 2H) , 7.64 (d, J b = 8.3 Hz, 2H) , 9 . 14 (br s , 1H) , 9 .23 (s, 1H) . LC/M S: condition 1, re tention time = 0 .85 min LC/M S(ESI +) m/z; 372 [M+H] + LC/M S(ESI ) m/z; 370 [M- H] TABLE 114 Ex Data ' H-NMR (C D C I3) : 1.74 (t, J = 3.3 Hz, 1H) , 1.76-1 .8 7 (m, 4H) , 1.95 (br s , 2H) , 2.27-2 .42 (m, 2H) , 2.99-3. 05 (m, 1H) , 3.29-3. 4 1 (m, 1H) , 3 .91 (s , 2H) , 7 .10 (dd , J = 3 .3 , 2.0 Hz, 1H) , 7 . 19 (t, J = 2.6 Hz, 138 1H), 7 .53 (d , J = 8.3 Hz, 2H) , 7.6 1 (d , J = 8.3 Hz, 2H) , 9.23 (s , 1H) , a 9 .31 (br s , 1H). LC/M S: condition 1, retention tim e = 2 .87 min LC/M S(ESI +) m/z; 415 [M+H] + LC/M S(ESI ) m/z; 4 13 [M- H] ' H-NMR (DMSO-cY ) : 1.35 (q , J = 10.6 Hz, 2H) , 1.76 (q , J = 12.2 Hz, 2H) , 1.95-2. 14 (m, 4H), 2 .19-2 .32 (m, 1H) , 3 .15 (t, J = 12.2 Hz, 1H) , 3.89 (s, 2H) , 6.80 (d , J = 2 .6 Hz, 1H) , 7 .49 (br s , 1H) , 7.6 1 (d, 138 J = 8 .6 Hz, 2H) , 7 .69 (d , J = 8.3 Hz, 2H), 9.52 (d , J = 1.3 Hz , 1H) , b 12.53 (br s , 1H) . LC/M S: condition 1, retention time = 2 .72 min LC/M S(ESI +) m/z; 415 [M+H] + LC/M S(ESI ) m/z; 413 [- 1H-NMR (C D C I 3) : 1.64-1 .78 (m, 5H) , 1.90- 1.99 (m, 2H), 2.33 (dq , J = 13.2, 3.0 Hz, 2H), 2.74 (br s , 4H) , 3.2 1 (t, J = 3.3 Hz, 1H) , 139 3.27-3. 38 (m, 1H), 3.75 (t , J = 4.6 Hz, 4H) , 7 .23 (dd , J = 3 .6 , 2.0 a Hz, 1H) , 7.28 (t, J = 3 .0 Hz, 1H) , 9.21 (br s , 1H) , 9.22 (s , 1H). LC/M S: condition 1, retention time = 0 .79 min LC/M S(ESI +) m/z; 342 [M+H] + 'H-NMR (C D C I3) : 1.37 (dq, J = 12.9, 4.0 Hz, 2H) , 1.57 (br s , 1H) , 1.96 (dq , J = 12 .6, 3 .0 Hz, 2H) , 2.08-2 .19 (m, 4H) , 2 .69 (br s, 4H) , 2.94 (tt, J = 11.2 , 3.3 Hz, 1H) 139 , 3 . 18 (tt, J = 12.2, 4.0 Hz, 1H) , 3 .76 b (t, J = 4.6 Hz, 4H) , 6.78 (dd , J = 3.3, 2.3 Hz, 1H) , 7.29 (t, J = 2.6 Hz , 1H), 9 .09 (br s , 1H) , 9.22 (s, 1H) . LC/MS : condition 1, retention time = 0.57 min LC/M S(ESI +) m/z; 342 [M+H] + H-NMR (DMSO- ) : 4.59 (d , J = 5.4 Hz, 2H) , 5.27 (t , J = 6.0 Hz , 1H), 6.86 (m, 1H) , 7.54 ( , 3H), 7.92 (d , J = 8.1 Hz, 2H) , 9.65 (s, 140 1H) , 12 .68 (br s , 1H) . LC/M S: condition 1, retention time = 2.77 min LC/M S(ESI +) m/z; 266 [M+H] + LC/M S(ESI ) m/z; 264 [M- H] -N R (DMSO-d ) : 1.25 (m, 2H) , 1.66 (m, 1H) , 1.87 (m, 2H) , 2 .00-2. 15 (m, 4H) , 3 . 18 (tt , J = 12.3 Hz, 3.6 Hz , 1H) , 3 .47 (d , J = 6.6 Hz, 2 H) , 6.81 Hz (d, J = 3 .3 Hz, 1H) , 7 .38 (d , J = 3 .3 Hz, 1H) , 141 9 .28 (s, 1H) . LC/MS : condition 1, retention time = 2.80 min LC/M S(ESI +) m/z; 272 [M+H] + LC/MS(ESI ) m/z; 270 [M- H] - ' H-NMR (DMSO- c ) : 1.88-2 .06 (m, 4H) , 2 .19-2.32 (m, 2H) , 2.92-3. 02 (m, 2H) , 3.10-3. 14 ( , 1H) , 3 .62 (s, 2H) , 6.82 (br s , 1H) , 7.13-7 .25 (m, 2H) , 7 .27-7 .40 ( , 1H) , 7.45-7.53 (m, 2H), 9.52 (s , 142 1H), 12.52 (br s , 1H). LC/M S: condition 3 , retention time = 1.33 min LC/M S(ESI +) m/z; 351 [M+H] + LC/M S(ESI ) m/z; 349 [M- H] TABLE 1 15 Ex Data H-NMR (DMSO- ) : 1.88-2.05 (m, 4H) , 2.2 1-2.35 (m, 2H) , 2 .94-3. 03 ( , 2H) , 3. 10-3.24 (m, 1H) , 3.68 (s, 2H) , 6.58 (d, J = 3.3 Hz , 1H) , 6.8 1 (d, J = 3.3 Hz, 1H) , 7 .15-7.20 ( , 1H), 7.46 -7.52 ( , 143 1H) , 9.52 (s, 1H) , 12 .52 (br s , 1H). LC/M S: condition 3 , retention time = 1.52 in LC/M S(ESI +) m/z; 391 [M+H] + LC/M S(ESI ) m/z; 389 [M- H] LC/M S: condition 3, retention time = 1.22 min 144 LC/M S(ESI +) m/z; 364 [M+H] + LC/M S(ESI ) m/z; 362 [M- H] ' H-N MR (CDCI3) : 1.97-2 .11 (m, 2H), 2.12-2 .33 (m, 4H) , 2.97-3. 10 (m, 2H) , 3 .15-3.3 1 ( , 1H) , 3.59 (s, 2H), 6.80-6.87 (m, 1H) , 6.93 (dd , J = 8 .4 , 2.7 Hz, 1H) , 7 .3 145 1 (t , J = 3.0 Hz, 1H) , 7 .80-7. 90 ( , 1H) , 8.15-8.20 (m, 1H), 9 .15 (br s , 1H) , 9 .23 (s , 1H). LC/M S: condition 3 , retention tim e = 1.58 min LC/M S(ESI +) m/z; 411, 4 13 [M+H] + Ή -NMR (DMSO- d ) : 1.90-2.04 (m, 4H) , 2 .19-2 .3 1 (m, 2H) , 2 .92-3. 03 (m, 2H) , 3 .06-3.20 (m, 1H), 3.57 (s, 2H) , 6.30 -6.3 5 (m, 146 1H) , 6.40-6.45 (m, 1H) , 6.78-6 .84 (m, 1H) , 7.47-7.53 (m, 1H) , 7.60 (s, 1H) , 9.52 (s , 1H) , 12.52 (br s , 1H) . LC/M S: condition 3 , retention tim e = 1. 14 min LC/M S(ESI +) m/z; 323 [M+H] + H-N MR (DMSO- de) : 1.84-2 .06 (m, 4H) , 2 .15-2 .33 (m, 2H) , 2.87-3. 04 (m, 2H) , 3 .06-3. 22 (m, 1H), 3.58 (s, 2H) , 6.29 (d, J = 3.3 Hz , 1H) , 6 .63 (d, J = 3.3 Hz, 1H) , 6.8 1 (br s , 1H) , 7.44-7 .5 1 (m, 147 1H) , 9.51 (s , 1H) , 12.52 (br s , 1H). LC/M S: condition 3, retention time = 1.44 min LC/M S(ESI +) m/z; 449 [M+H] + LC/M S(ESI ) m/z; 447 [- H-NMR (DMSO- ) : 1.86-2. 10 (m, 4H) , 2 .18-2.33 ( , 2H) , 2 .94-3. 10 (m, 2H) , 3.1 1-3.26 (m, 1H) , 3.76 (s, 2H) , 6 .82 (br s, 1H) , 6 .91-7. 03 (m, 2H) , 7 .40-7.46 (m, 1H), 7.46-7.53 (m, 1H) , 9.52 (s , 148 1H) , 12.52 (br s , 1H) . LC/M S: condition 3 , retention time = 1.24 min LC/MS (ESI +) m/z; 339 [M+H] + LC/M S(ESI ) m/z; 337 [M- H] Ή -NMR (DMSO- ) : 1.84-2.06 (m, 4H) , 2.17-2.33 (m, 2H) , 2.88-3. 04 (m, 2H) , 3 .05-3.22 (m, 1H), 3.57 (s, 2H) , 6.40 (d, J = 3.3 149 Hz, 1H) , 6 .5 1 (d, J = 3 .3 Hz, 1H) , 6.8 1 (br s, 1H) , 7.43-7.52 (m, 1H) , 9.51 (s, 1H) , 12.52 (br s , 1H) . LC/M S: condition 3 , retention tim e = 1.39 min LC/M S(ESI +) m/z; 40 1, 403 [M+H] + -NMR (DMSO- ) : 1.85-2.08 (m, 4H) , 2.20-2.37 (m, 2H) , 2 .94-3. 05 (m, 2H), 3 .11-3.27 (m , 1H) , 3 .78 (s, 2H) , 6 .82 (br s, 1H) , 150 7.46-7 .53 ( , 1H), 7.58 (s, 1H) , 9 .52 (s, 1H), 12.52 (br s , 1H) . LC/M S: condition 3 , retention tim e = 1.2 1 min LC/M S(ESI +) m/z; 374 [M+H] + LC/M S(ESI ) m/z; 372 [M- H] TABLE 1 16 Ex Data H-N MR (DMSO- ) : 1.82-2. 08 (m, 4H) , 2 .12-2.28 (m, 2H) , 2 .86-3. 05 (m, 2H), 3 .05-3.20 ( , 1H), 3.46-3.65 (m, 2H), 6.09-6.23 (m, 1H), 6.8 1 (br s , 1H) , 7.48 (br s , 1H), 9 .52 (s, 1H) , 12 .52 (br s , 151 1H). LC/M S: condition 3 , re tention time = 0 .63 min LC/M S(ESI +) m/z; 323 [M+H] + LC/M S(ESr) m/z; 321 [M- H] -N R (DMSO- c ) : 1.87-2 .12 (m, 4H) , 2 .25-2. 42 ( , 2H) , 2 .97-3. 10 (m, 2H) , 3 . 10-3 .25 (m, 1H) , 4 . 13 (s , 2H) , 6 .82 (br s , 1H) , 7.45-7. 53 (m, 1H) , 9.10 (s, 1H) 152 , 9.52 (s, 1H), 1 .52 (br s , 1H) . LC/M S: condition 3, re tention t ime = 0 .8 1 min LC/M S(ESI +) m/z; 34 1 [M+H] + LC/M S(ESI m/z; 339 -  Ή -NMR (DMSO- d ) : 1.85-2. 06 (m, 4H) , 2 .20-2. 36 ( , 2H) , 2 .92-3. 05 (m, 2H) , 3.12-3 .27 (m, 1H) , 3 .80 (s , 2H) , 6 .82 (br s , 1H) , 153 7 .48-7 .53 (m, 1H) , 7 .59 (s, 1H) , 9.52 (s, H) , 2 .52 (br s , H) . LC/M S: condition 3 , re tention t ime = 1.58 min LC/M S(ESI +) m/z; 4 18, 4 20 [M+H] + LC/M S(ESI ) m/z; 4 16 , 4 18 [M- H] H-N MR (DMSO- ) : 1.96-2.03 (m, 4H) , 2 .23-2 .29 (m, 2H) , 2.94 (d, J = 11.4 Hz, 2H) , 3 . 16-3.2 1 (m, 1H), 3 .63 (s, 2H) , 6.82 (d, J = 2 .4 Hz, 1H) , 7 .46-7. 52 (m, 2H) , 7.74 (d , J = 7.5 Hz, 2H) , 9.52 (s , 1H), 154 12 .55 (br s , 1H) . LC/M S: condition 3 , re tention t ime = 1.68 min LC/M S(ESI +) m/z; 4 19 [M+H] + LC/M S(ESI ) m/z; 4 17 [M- H] H-N MR (DMSO-de) : 1.95-2 .06 (m, 4H) , 2 .23-2 .30 (m, 2H) , 2 .94 (d , J = 11.7 Hz, 2H) , 3 . 16-3. 19 (m, 1H), 3 .65 (s, 2H) , 6 .82 (d, J = 3.3 Hz, 1H) , 7.49 (d, J = 3.3 Hz, 1H) , 7.7 1 (s, 2H) , 7 .84 (s, 1H), 9.52 (s, 155 1H). LC/M S: condition 3 , retention t ime = 1.79 min LC/M S(ESI +) m/z; 435, 437 [M+H] + LC/M S(ESI ) m/z; 433, 435 [M- H] H-N MR (DMSO-de) : 1.96-2.04 (m, 4H) , 2 .23-2. 30 ( , 2H) , 2.96 (d , J = 10.2 Hz, 2H) , 3 .22 (s, 3H), 3 .67 (s, 2H) , 6 .8 1 (d, J = 3.0 Hz, H) , 7.49 (d , J = 3.3 Hz, 1H) , 7.65 (d, J = 8.4 Hz, 2H) , 7.9 1 (d, J = 8.7 156 Hz, 2H), 9.49 (s, 1H) . LC/M S: condition 3 , retention t ime = 1.12 min LC/M S(ESI +) m/z; 4 1 1 [M+H] + LC/M S(ESI ) m/z; 409 -Hl H-N MR (DMSO-d ) : 1.95-2.07 (m, 4H) , 2 .27-2 .33 (m , 2H) , 2.98 (d , J = 11.7 Hz, 2H) , 3 . 15-3. 18 (m, 1H), 3 .70 (s, 2H) , 6 .82 (d, J = 3.0 Hz, 1H) , 7 .49 (d , J = 3 .3 Hz, 1H) , 7 .6 1-7 .68 (m, 2H) , 7.7 6 (t, J = 7 .7 157 Hz, 1H) , 9.5 1 (s, 1H). LC/M S: condition 3 , retention t ime = 1.66 min LC/M S(ESI +) m/z; 4 19 [M+H] + LC/M S(ESI ) m/z; 4 17 [M- H] TABLE 1 7 Ex Data H-N MR (DMSO- ) : 1.94-2 .04 (m, 4H), 2 .26 (td , J = 10.8, 3.5 Hz, 2H), 2.95 (d , J = 11.7 Hz, 2H) , 4.12 (s , 2H) , 6.82 (d, J = 3.0 Hz, 1H), 7 .31 (dd , J = 8.4, 2 . 1 Hz, 158 1H) , 7.4 1 (dd , J = 9.9 , 2. 1 Hz, 1H) , 7.49-7. 54 (m, 2H) , 9.53 (s, 1H) , 12.54 (br s , 1H) . LC/M S: condition 3 , retention t ime = 1.54 min LC/M S(ESI +) m/z; 385, 387 [M+H] + H-N MR (DMSO-d ) : 1.95-2.06 (m, 4H) , 2.21 -2.27 ( , 2H) , 2.94 (d, J = 11.4 Hz, 2H) , 3 .15-3.22 ( , 1H) , 3.57 (s, 2H) , 6.83 (d, J = 3.3 Hz, 1H) , 7.25 (d , J = 7.8 Hz, 1H) , 7 .40 (d , J = 10 .8 Hz , 1H) , 7.50 (d , 159 J = 3.3 Hz, 1H) , 7.56 (t , J = 8 .1 Hz, 1H), 9.53 (s, 1H) , 12.54 (br s, 1H). LC/M S: condition 3 , retention t ime = 1.58 min LC/M S(ESI +) m/z; 385, 387 [M+H] + LC/M S(ESI ) m/z; 383, 385 [M- H] Ή -MR ( C D C I3) : 1.99-2 .13 (m, 2H) , 2 .17-2 .37 ( , 4H) , 2.94-3. 10 (m, 2H) , 3.16-3. 32 (m, 1H) , 3.59 (s, 2H) , 6 .80-6 .88 (m, 1H) , 7.2 1-7. 35 (m , 2H) , 7.4 1 (s, 1H) , 8.34 (d, J = 5.1 Hz, 1H), 9.18 (br s, 160 1H) , 9 .24 (s , 1H) . LC/M S: condition 3 , re tention t ime = 1.16 min LC/M S(ESI +) m/z; 368, 370 [M+H] + LC/M S(ESI ) m/z; 366, 368 [M- H] Ή -NMR ( C D C I3) : 2 .00-2 .16 (m, 2H), 2.16-2.42 (m, 4H) , 3.00-3. 15 (m, 2H) , 3 .15-3 .30 (m, 1H) , 3 .7 1 (s, 2H) , 6.80-6 .90 (m, 1H) , 7.28-7. 37 (m, 1H) , 7 .53 (t, J = 5 .4 Hz, 1H) , 8 .38-8 .50 (m, 2H) , 16 1 9.11-9 .30 (m, 2H). LC/M S: condition 3 , retention tim e = 0.86 min LC/M S(ESI +) m/z; 352 [M+H] + LC/M S(ESI ) m/z; 350 - H-N MR ( C D C I3) : 2.00-2. 10 (m, 2H), 2.16-2.42 ( , 4H) , 3.01 -3. 15 ( , 2H), 3 .16-3. 32 (m, 1H), 3.74 (s, 2H), 6 .80-6. 89 (m, 1H) , 7.29 (t, J = 3 .0 Hz, 1H), 7.40 (td , J = 8.7 , 3 .0 Hz, 1H) , 7.54 (dd, J = 8.4 , 4 .5 162 Hz, 1H) , 8 .42 (d , J = 2 .7 Hz , 1H), 9.08 (br s , 1H), 9 .22 (s, 1H) . LC/M S: condition 3 , retention t ime = 1.17 min LC/M S(ESI +) m/z; 352 [M+H] + LC/M S(ESI ) m/z; 350 [M- H] - 1H-N MR ( C D C I3) : 2.00-2 .15 ( , 2H) , 2 .19-2 .50 ( , 4H) , 3.02-3. 14 (m, 2H) , 3 .18-3 .33 (m, 1H) , 3 .70 (s, 2H) , 6.82-6 .9 1 (m, 1H) , 163 7.29-7.38 (m, 1H) , 7.59 (d , J = 4.8 Hz, 1H) , 8.48 (d, J = 4.8 Hz, 1H) , 8 .54 (s, 1H), 9.09 (br s , 1H) , 9.23 (s , 1H) . LC/M S: condition 3 , retention t ime = 1.13 min LC/M S(ESI +) m/z; 368, 370 [M+H]+ ' H-N MR (DMSO- ) : 1.93-2.00 (m, 4H) , 2 .21-2. 27 (m , 2H) , 2.95 (d , J = 10 .5 Hz, 2H), 3.59 (s, 2H) , 6 .81 (d, J = 2.4 Hz, 1H) , 7 .10 (t, J = 164 8.4 Hz, 1H), 7 .21 (t , J = 9.3 Hz, 1H), 7 .48-7. 56 (m, 2H) , 9.52 (s , 1H) . LC/M S: condition 3, retention tim e = 1.39 min LC/M S(ESI +) m/z; 369 [M+H] + TABLE 1 8 Ex Data H-N MR (DMSO- ) : 1.95-2 .07 (m, 4H) , 2 .23 (td , J = 11.3 , 3.0 Hz, 2H) , 2 .97 (d , J = 11. 1 Hz, 2H) , 3.62 (s , 2H) , 6.83 (d , J = 3.3 Hz, 1H) , 7 .25 (td, J = 8 .6, 2.6 Hz, 1H) 165 , 7.43 (dd , J = 8 .9, 2 .6 Hz, 1H) , 7 .50 (d , J = 3 .3 Hz, 1H) , 7.60 (dd , J = 8 .6, 6 .2 Hz, 1H) , 9 .52 (s, 1H) . LC/M S: condition 3 , re tention t ime = 1.50 min LC/M S(ESI +) m/z; 385, 387 [M+H] + H-N MR (DMSO- ) : 1.9 1-2 .06 ( , 4H) , 2 .23 (td, J = 11.2 , 3 .1 Hz, 2H) , 2 .94 (d , J = 11.7 Hz, 2H), 3 .55 (s , 2H) , 6.82 (d , J = 3 .3 Hz, 1H) , 7 . 19-7 .24 (m, 1H) , 7.35-7.45 (m, 2H) , 7 .50 (d , J = 3.3 Hz, 1H) , 166 9 .52 (s , 1H). LC/M S: condition 3 , retention t ime = 1.45 min LC/M S(ESI +) m/z; 369 [M+H] + LC/M S(ESI ) m/z; 367 - 1 -NMR (DMSO-d ) : 1.92-2.09 (m, 4H) , 2 .25-2 .3 1 (m, 2H) , 2 .96 (d , J = 12.0 Hz, 2H) , 3.67 (s, 2H) , 6.82 (d , J = 3.3 Hz, 1H) , 7.43-7.52 167 ( , 3H) , 7.77 (t, J = 8.0 Hz, 1H) , 9.5 1 (s, 1H) . LC/M S: condition 3 , re tention time = 1.71 min LC/M S(ESI +) m/z; 4 19 [M+H] + LC/M S(ESI ) m/z; 4 17 [M- H] -NMR (DMSO-d ) : 1.91-2. 23 (m, 8H) , 2.9 1 (t, J = 11.6 Hz, 1H) , 3.46 (s , 2H) , 3.69-3.7 1 ( , 2H) , 3.96 (br s , 2H) , 6.71 (s, H) , 6.90 168 (t, J = 6.8 Hz, 2H) , 7.2 5 (t , J = 8.3 Hz, 2H) , 7 .43 (s, 1H) , 9.37 (s , 1H). LC/M S: condition 3 , retention time = 1.15 min LC/M S(ESI +) m/z; 393 [+ H-NMR ( C D C I3) : 1.98-2 .13 (m, 2H), 2 .13-2.34 ( , 4H) , 2.98-3. 16 (m, 2H) , 3 . 16-3. 32 (m, 1H), 3.59 (s, 2H) , 5 .91 (tt, J = 56. 1, 3 .0 Hz , 1H) , 6 .81-6. 90 (m, 1H) , 7.18 (d, J = 8 .4 Hz, 2H) , 7 .27-7 .33 (m, 1H) , 169 7.4 1 (d, J = 8 .4 Hz, 2H) , 9.19 (br s , 1H), 9 .23 (s, 1H). LC/M S: condition 3 , retention time = 1.72 min LC/M S(ESI +) m/z; 449 [M+H] + LC/M S(ESI ) m/z; 447 [M- H] H-N MR ( C D C I3) : 1.96-2. 12 (m, 2H) , 2 .12-2 .35 (m, 4H) , 3.00-3. 16 (m, 2H), 3 .16-3 .31 ( , 1H) , 3.54 (s, 2H) , 3.95 (s, 3H) , 6 .75 (d , J = 170 8.1 Hz, 1H) , 6.8 1-6.90 (m, 1H) , 7 .27-7. 36 (m, 1H) , 7.64 (dd , = 8 .4 , 2.4 Hz , 1H) , 8.11 (d, J = 2.1 Hz, 1H) , 9.23 (s , 1H) , 9.5 1 (br s , 1H) . LC/M S: condition 3 , retention t ime = 1.22 min LC/M S(ESI +) m/z; 364 [M+H] + 17 1 LC/M S: condition 3 , retention t ime = 1.40 min LC/M S(ESI +) m/z; 386 [M+H] + TABLE3 119 Ex Data H-N MR (C D C I3 ) : 1.12- 1.28 (m, 2H) , 1.62 (m, 1H) , 1.84-2.02 (m, 4H) , 2 .15 ( , 2H) , 2 .52 (dd, J = 12 .0, 6 .9 Hz, 1H) , 2.66 (dd , J = 12 .0, 6.6 Hz, 1H) , 2 .98 (d , J = 12.9 Hz, 1H) , 3. 15 (tt, J = 12 .3, 3 .3 Hz, 1H) , 3.54 (d , J = 12 172 .9 Hz, 1H) , 6.78 (m, 1H) , 7.33 -7.40 ( , 4H) , 7.60 ( , 2H) , 9.22 (s , 1H) , 9 .45 (b r s , 1H) . LC/M S: co ndition 1, retention time = 2.81 i n LC/M S(ES I+) m/z; 459 [M+H]+ LC/M S(ESI ) m/z ; 45 7 [M-H] 'H-N MR (DMSO-de) : 1.23- 1.38 (m, 2H) , 1.7 1- 1.86 (m, 2H) , 1.95-2.09 (m , 4H) , 3 .08-3.23 (m, 3H) , 6.82 (dd, J = 1.7, 3.3 Hz, 1H) , 6.86 (d , J = 9.2 Hz, 2 H), 7.50 (t, J = 3 .0 Hz, H) , 7 .59 (t, J = 5.6 Hz, 173 1H) , 7 .68 (d , J = 8 .9 Hz , 2H) , 9 .52 (s , 1H) , 12.54 (br s , 1H) . LC/M S: co ndition 1, retention time = 4.30 mi n LC/M S(ESI +) m/z; 479 [M+H]+ LC/M S(ESI ) m/z ; 477 [M-H] 'H-N MR ( C D 3O D ) : 1.17- 1.33 (m, 2H) , 1.70- 1.78 (m, 1H) , 1.78-1 .90 (m, 2H) , 1.93-2 .01 (m, 2 H), 2 .06-2 .15 (m, 2H) , 2 .66 (d , J = 7 .0 Hz, 2H) , 2.79 -3.02 (m, 5H) , 3 .17 (tt, J = 12 .3, 3.3 Hz, 1H) , 6.79 (d, J = 174 3.3 Hz , 1H) , 7. 16-7 .32 (m, 6H) , 7 .38 (d , J = 3.3 Hz , 1H) , 9 .27 (b r s , 1H) . LC/M S: co ndition 1, retenti on time = 2.75 mi n LC/M S(ESI +) m/z; 375 [M+H]+ LC/M S(ESI ) m/z ; 373 [M-Hl 'H-N MR (DMSO-d ) : 1.24- 1.39 (m, 2H) , 1.71- 1.87 (m, 3H) , 2.0 1-2.09 ( , 5H) , 3.00 (d, J = 5.9 Hz , 2H) , 3 .13-3 .25 (m, 1H) , 5 .94 (bs , 1H) , 6 .57 (b r s , 1H) , 6.79-6.83 (m, 2H) , 7.44 (d, J = 8 .9 Hz, 175 1H) , 7 .50 (t , J = 3 .0 Hz, 1H) , 9.52 (s , 1H) , 12.53 (br s , 1H) . LC/M S: co ndition 1, retenti on time = 3.35 min LC/M S(ES I+) m/z; 455 [M+H]+ LC/M S(ESI ) m/z; 453 [- Ή -NMR (DMSO- ) : 1. 19- 1.34 (m, 2H) , 1.69- 1.84 (m, 3H) , 1.96-2.07 (m, 4 H), 2.9 3 (t, J = 5.6 Hz, 2H) , 3 .11-3 .25 (m, 1H) , 5 .89 (t, J = 5.6 Hz, 1H) , 6.5 6-6. 62 (m, 2H) , 6 .81 (dd, = 3 .0, 1.7 Hz , 1H) , 176 7.05-7. 11 (m, 2H) , 7.49 (t, J = 3 .0 Hz, 1H), 9.52 (s , 1H) , 12.53 (b r s , 1H) . LC/M S: co ndition 1, retenti on time = 4.32 mi n LC/M S(ES I+) m/z; 381 [M+H]+ LC/M S(ESI ) m/z ; 379 M-H Ή -NMR ( C D C I3) : 1.24 ( , 2H) , 1.76 (m, 1H) , 1.86-2 .17 ( , 6 H), 2.57 (d, J = 6 .6 Hz, 1H) , 3 .16 (tt, J = 12 .3 , 3 .6 Hz, 1H) , 3 . 81 (s , 2H) , 6.77 (d, J = 3.3 Hz, 1H) , 7.26-7.2 9 (m, 5H) , 9.22 (s, 1H) , 9.70 (br s , 177 1H) . LC/M S: co ndition 1, retention time = 2.84 mi n LC/M S(ESI +) m/z; 395 , 39 7 [M+H] + LC/M S(ESI ) m/z; 393, 395 I M-H] TABLE 120 Ex Data H-N MR (CDCI 3) : 1.19 (m, 2H), 1.66 ( , 1H), 1.90 (m, 4H), 2.12 (m, 2H) , 2 .57 (d , J = 6 .6 Hz, 2H) , 2.70-2 .97 ( , 4H) , 3.16 (tt , J = 12.6, 3.3 Hz , 1H) , 6.77 ( , J = 3 .3 Hz, 1H) , 7.15 ( , 3H) , 7.27 ( , 178 2H), 9 .2 1 (s, 1H), 9.33 (br s, 1H). LC/M S: condition 1, retention t ime = 2 .97 in LC/M S(ESI +) m/z; 409, 4 11 [M+H] + LC/M S(ESr) m/z; 407, 409 [M- H] ' H-NMR (CDCI 3) : 1. 17-1 .39 (m, 2H), 1.7 1-2.28 ( , 7H) , 2.86-3.06 (m, 4H) , 3.10-3.30 (m, 1H) , 3 .33-3. 55 ( , 2H) , 6 .30-6. 43 (m, 1H), 6.70-6. 88 (m, 3H), 7 .20-7 .39 (m, 179 1H), 9 .02 (br s, 1H), 9.22 (s , 1H) . LC/M S: condition 1, retention t ime = 4.40 min LC/M S(ESI +) m/z; 39 1 [M+H] + LC/M S(ESL) m/z; 389 -1 H-NMR (CDCI 3) : 1.04-1 .28 (m, 2H), 1.46- 1.73 (m, 1H) , 1.82-2.02 (m, 2H) , 2.04-2.23 (m, 4H) , 2 .39-2 .60 (m, 6H) , 2.84-3. 00 (m, 4H) , 3 .09-3.28 (m, 1H) , 6.72-6.83 (m, 1H) , 7 .27-7. 37 (m, 1H) , 8.99 (br s , 180 1H) , 9 .21 (s , 1H) . LC/M S: condition 1, retention time = 3 .38 min LC/M S(ESI +) m/z; 377 [M+H] + LC/M S(ESI ) m/z; 375 [- H-N MR (CDCI 3) : 1.00-1 .3 1 ( , 2H), 1.50- 1.80 ( , 1H) , 1.81 -2. 18 (m, 7H) , 2.24 (s , 6H), 2.26-2 .59 (m, 4H), 2.68-2 .92 (m, 3H) , 3.08-3.24 (m, 1H), 6 .71-6. 83 (m, 1H), 7 .17-7.33 ( , 1H) , 9.00-9.40 18 1 ( , 1H), 9.2 1 (s, 1H) . LC/M S: condition 1, retention t ime = 0 .34 min LC/M S(ESI +) m/z; 368 [M+H] + LC/M S(ESI ) m/z; 366 [M- H] H-NMR (CDCI 3) : 1.00-1 .32 (m, 2H) , 1.40- 1.80 ( , 1H) , 1.82-2 .2 1 (m, 7H), 2.29 (s , 3H) , 2.58 (d, J = 6.6 Hz, 2H) , 3.08-3. 25 (m, 1H) , 3.76 (s, 2H) , 5.89 (d , J = 2.1 Hz, H) , 6.06 (d , J = 3.0 Hz , 1H) , 6.78 182 (d , J = 3.0 Hz, 1H), 7. 17-7.32 (m, 1H) , 9 .00-9. 40 (m, 1H) , 9.2 1 (s , 1H) . LC/M S: condition 1, retention tim e = 2.49 min LC/M S(ESI +) m/z; 365 [M+H] + LC/M S(ESr) m/z; 363 [M- H] H-N MR (CDCI 3) : 1.11- 1 .35 (m, 2H), 1.40- 1.8 1 ( , 1H) , 1.83-2.25 (m, 7H), 2.57 (s , 3H) , 2.62 (d, J = 6.6 Hz, 2H), 3 .07-3. 27 (m, 1H) , 3 .96 (s , 2H) , 6 .70-6. 85 (m, 1H), 7 .10-7.37 (m, 1H) , 8 .35-8. 46 (m, 183 1H) , 8.49-8. 59 (m, 1H), 9.00-9 .40 (m, 1H) , 9.2 1 (s , 1H) . LC/M S: condition 1, retention t ime = 0 .77 min LC/M S(ESI +) m/z; 377 [M+H] + LC/M S(ESI ) m/z; 375 [M- H] H-N MR (CDCI 3) : 1. 11- 1 .38 (m, 5H), 1.55-2.35 ( , 9H) , 2.40-2.85 (m, 4H) , 3.09-3.27 (m, 1H) , 3 .72-3. 92 (m, 1H) , 6.80 (d , J = 3.3 Hz, 184 1H), 7 .30 (d, J = 3 .3 Hz, 1H) , 8.60- 10.00 ( , 1H) , 9.2 3 (s , 1H) . LC/M S: condition 1, retention time = 0.39 min LC/M S(ESI +) m/z; 329 [M+H] + LC/MS(ESI ) m/z; 327 [M- Hl TABLE 121 Ex Data ' H-NMR ( C D C I3) : 1. 10-1 .50 (m, 5H) , 1.5 5-2 .35 (m, 9H) , 2 .40-2 .90 (m, 4H), 3 .10-3.3 1 (m, 1H) , 3 .75-4. 00 (m, 1H) , 6.80 (d , J = 3 .3 Hz, 1H) , 7.30 (d, J = 3 .3 Hz, 1H) , 8 185 .80- 10 .00 (m, 1H) , 9 .23 (s, 1H) . LC/M S: condition 1, retention tim e = 0 .37 min LC/M S(ESI +) m/z; 329 [M+H] + LC/M S(ESI ) m/z; 327 [M- H] H-NMR (CD 3OD) : 1.30 ( , 2H) , 1.70 -2 .15 (m, 7H) , 2 .74 (t , J = 6.6 Hz, 2H) , 2 .92 (d, J = 6.6 Hz, 2H) , 3 .2 1 (tt , J = 12 .0 , 4 .2 Hz, 1H) , 186 4 .92 (m, 1H), 6.82 (d, J = 3 .3 Hz , 1H) , 6 .83-7 .43 (m, 6H) , 9.30 (s, 1H). LC/M S: condition 1, retention tim e = 2 .52 min LC/M S(ESI +) m/z; 39 1 [M+H] +, LC/M S(ES I ) m/z; 38 9 [M-H] H-NMR ( C D C I3) : 1.07- 1.3 1 (m, 2H), 1.4 7-1 .74 (m, 1H) , 1.80-2 .32 (m, 8H) , 2 .34-2.49 (m, 2H) , 2 .55-2 .80 (m, 3H) , 2 .88-3. 25 (m, 3H) , 187 6 .7 1-6. 86 (m, 1H) , 7 . 18-7. 39 (m, 1H), 9 .0 1 (br s , 1H), 9 .2 1 (s, 1H) . LC/M S: condition 3 , retention time = 1. 14 min LC/M S(ESI +) m/z; 350 [M+H] + LC/MS (ESI ) m/z; 348 [M- H] H-NMR ( C D C I3) : 1. 10-1 .40 (m, 3H) , 1.5 0- 1.80 (m, 1H), 1.83-2.24 (m, 6H), 2.68 (d , J = 6 .0 Hz , 2H) , 3.06-3 .50 (m, 3H) , 6.70-6. 85 ( , 188 1H) , 7 . 18-7. 35 (m, 1H), 9. 10 (br s , 1H) , 9 .22 (s, 1H) . LC/M S: condition 3 , retention tim e = 1.30 min LC/M S(ESI +) m/z; 353 [M+H] + H-NMR ( C D C I3) : 1. 11- 1 .45 (m, 3H), 1.7 8-2 .36 (m, 6H), 2.9 1-3.31 (m, 5H) , 3.00 (s , 3H) , 3 .52-3. 80 (m, 2H) , 6 .40 (d, J = 8 .6 Hz, 1H) , 189 6 .70-6. 90 ( , 1H) , 7.20-7.38 (m, 1H), 7 .50 (s, 1H), 7 .54-7 .73 ( , 1H) , 9 .22 (s, 1H) , 9.30 (br s , 1H) . LC/M S: condition 3 , retention tim e = 2 . 13 min LC/M S(ESI +) m/z; 45 1 +, LC/M S(ES I ) m/z; 44 9 [M-Hl H-N MR (C D C I3) : 1. 15-1 .40 (m, 3H), 1.80-2.30 (m, 6H) , 2.68 (s, 6H), 3 .00-3 .30 (m, 5H) , 3.55-3.74 (m, 2H) , 6 .40 (d , J = 8.6 Hz, 1H) , 190 6 .79 (t, J = 2 .4 Hz, 1H) , 7.29 (t, J = 3 .0 Hz, 1H) , 7 .34 (s , 1H) , 7.50 (dd , J = 8 .3, 1.2 Hz, 1H) , 9 .09 (br s , 1H) , 9.22 (s, 1H) . LC/M S: condition 3 , retention time =2.35 min LC/MS (ESI +) m/z; 480 [M+H] +, LC/MS( ES I ) m/z; 47 8 [M-H] -NMR ( C D C I3) : 1.00-1 .40 (m, 3H) , 1.5 0-2.40 (m, 7H) , 2.5 1-2.93 (m, 4H) , 3.00-3.23 (m, 1H) , 3 .25-3. 68 ( , 6H) , 4 .50-4. 89 ( , 1H), 19 1 6 .67-6. 84 (m, 1H) , 7.20-7. 42 (m, 1H) , 9 .20 (s, 1H) , 9 . 97 (br s , 1H) . LC/M S: condition 3 , retention tim e = 1. 13 min LC/M S(ESI +) m/z; 383 [M+H] + LC/M S(ESI ) m/z; 381 [M-H] 1H-NMR (DMSO- ) : 1. 13-1 .42 (m, 2H) , 1.64-2 . 15 (m, 6H) , 2 .78-3. 60 (m, 9H) , 6 .8 1 (s, 1H) , 7 .40-7. 62 (m, 2H) , 8 .99 (s, 1H) , 9 .08 (br s , 1H) , 9.52 (s, 1H) , 12 .56 (s, 1H) , 14.44 ( br s , 1H) . 192 LC/M S: condition 3 , retention tim e = 0 .68 min LC/MS(ESI +) m/z; 365 [M+H] + LC/M S(ESI ) m/z; 363 [M- H] TABLE 122 Ex Data H-N MR (DMSO- ) : 1. 10-1 .26 (m, 2H) , 1.5 1- 1.63 (m, 1H) , 1.75 (qd, J = 12.2, 3 .3 Hz, 2H) , 1.92-2.04 (m, 4H) , 2.42 (d, J = 6.6 Hz, 2H) , 3 . 13 (tt , J = 12 .6, 3.3 Hz , 1H) , 3 .72 (s, 2H), 6.80 (d, J = 3.6 Hz, 1H) , 7.22 (tt, J = 6 .9 , 2.0 Hz , 1H) 193 , 7.28-7.38 (m, 4H) , 7 .49 (d, J = 3 .3 Hz , 1H) , 9.5 1 (s, 1H), 12 .52 (br s , 1H). LC/M S: condition 1, retention t ime = 2 .67 min LC/M S(ESI +) m/z; 36 1 [M+H] + LC/M S(ESI ) m/z; 359 [M- H] H-N MR (DMSO- ) : 1.55-1 .70 (m, 4H) , 1.8 1- 1 .92 (m, 2H) , 1.99-2 .07 (m, 1H) , 2 .20-2 .35 ( , 2H), 2.84-2.89 (m, 1H) , 3 .16-3.29 194 ( , 1H) , 3.75 (s, 2H), 7.13 (d , J = 3 .3 Hz, 1H) , 7 .23 (tt , J = 6.9 , 1.7 a Hz, 1H) , 7.31-7. 43 (m, 5H) , 9.50 (s , 1H) , 12.49 (br s , 1H) . LC/M S: condition 1, retention t ime = 2 .22 min LC/M S(ESI +) m/z; 347 [M+H] + LC/M S(ESI ) m/z; 345 [M- H] H-NMR (DMSO-de) : 1.26- 1.42 (m, 2H) , 1.75 (qd , J = 12 .7 , 3 .3 Hz, 2H), 1.95-2. 14 (m, 5H) , 2.5 1-2.62 (m, 1H) , 3 .15 (tt , J = 12.3, 3 .7 Hz, 1H) , 3 .79 (s, 2H) , 6 .79 (d , J = 3 .3 Hz , 1H) , 7 .22 (tt, J = 7 .4 , 1.6 Hz, 194 1H), 7 .28-7. 39 (m, 4H) , 7.48 (d , J = 3.3 Hz, 1H) , 9.50 (s, 1H) , 12.5 1 b (br s , 1H) . LC/M S: condition 1, retention t ime = 1.47 min LC/M S(ESI +) m/z; 347 [M+H] + LC/M S(ESI ) m/z; 345 [M- H] H-N MR (DMSO- ) : 1.54- 1.69 (m, 4H) , 1.80-1 .90 (m, 2H) , 2. 18-2.33 (m, 2H), 2.8 1-2.88 (m, 1H) , 3.14-3. 17 ( , 1H) , 3.18-3 .30 195 (m, 1H), 3.73 (s, 2H) , 7.08-7.20 (m, 3H) , 7 .38-7. 46 (m, 3H) , 9.50 (s, a 1H), 12.49 (br s , 1H) . LC/M S: condition 1, retention time = 2.55 min LC/M S(ESI +) m/z; 365 [M+H] + LC/M S(ESI ) m/z; 363 [M- H] H-N MR (DMSO- ) : 1.25-1 .41 ( , 2H) , 1.67-1 .83 (m, 2H) , 1.95-2. 12 ( , 5H) , 2.5 1-2.60 (m, 1H) , 3.0 8-3.20 (m, 1H) , 3 .78 (s, 195 2H) , 6 .80 (d , J = 3.3 Hz, 1H) , 7. 10-7. 18 ( , 2H) , 7 .37-7 .44 (m, 2H) , b 7.49 (d, J = 3 .3 Hz, 1H) , 9.5 1 (s, 1H) , 12.53 (br s , 1H). LC/M S: condition 1, retention t ime = 1.03 min LC/M S(ESI +) m/z; 365 [M+H] + LC/M S(ESI ) m/z; 363 [M- H] Ή -NMR ( C D C I3) : 1.77- 1.92 (m, 6H), 2 .19 (m, 2 H) , 2 .81 (m, 1H) , 3 .00 (d, J = 13.2 Hz , 1H) , 3.35 (m, 1H) , 3 .55 (d , J = 13.2 Hz, 1H) , 196 6 .75 (d , J = 3 .3 Hz, 1H) , 7 .30 (m, 1H) , 7.37 (m, 3H) , 7 .60 (m, 2H) , a 9 .22 (s, 1H) , 9.44 (br s , 1H) . LC/M S: condition 1, retention time = 2.75 min LC/M S(ESI +) m/z; 445 [M+H] + LC/M S(ESI ) m/z; 443 -1 TABLE 23 Ex Data 1H-N MR (CDCI 3) : 1.26- 1.38 (m, 2H) , 1.92 (m, 2 H) , 2 . 15 (m, 4H), 2 .62 (tt , J = 11.4, 3.6 Hz, 1H) , 3 .02 (d , J = 13 .2 Hz, 1H) , 3 . 5 (tt , J = 12 .0, 3.3 Hz, 1H) , 3.6 0 (d, J = 13.2 Hz, 1H) , 6 .74 (d , J = 3 .3 Hz, 196 1H) , 7 .30 (d, J = 2.7 Hz, 1H) , 7 .39 (m, 3H) , 7 .61 (m, 2H) , 9.22 (s , b 1H) , 9 .63 (br s, 1H) . LC/M S: condition 1, retention t ime = 2 .57 min LC/M S(ESI +) m/z; 445 [M+H] + LC/M S(ESI ) m/z; 443 [M- H] 1H-N MR (DMSO- d ) : 1.56- 1.7 1 (m, 4H) , 1.80- 1.9 1 (m, 2H) , 2 . 13-2 .35 (m, 3H) , 2.82-2.88 (m, 1H), 3 .19-3. 30 (m , 1H) , 3 .75 (s, 2H) , 7 .10 (d , J = 3.3 Hz, 1H) 197 , 7 .39-7 .47 ( , 5H) , 9.52 (s, 1H) , 12 .51 a (br s , 1H) . LC/M S: condition 1, retention t ime = 2.75 min LC/M S(ESI +) m/z; 38 1 [M+H] + LC/M S(ESL) m/z; 379 [M- H] H-NMR (DMSO- ) : 1.26- 1.4 1 (m, 2H) , 1.75 (qd , J = 12 .6 , 2 .3 Hz, 2H) , 1.95-2. 12 (m, 5H) , 2.54 (tt, J = 10 .9 , 3 .3 Hz, 1H) , 3.14 (tt, J = 197 11.9 , 3 .3 Hz, 1H) , 3.78 (s , 2H) , 6 .80 (d, J = 3.3 Hz, 1H), 7.34-7.43 b (m, 4H) , 7.49 (d, J = 3 .0 Hz, 1H) , 9.5 1 (s, 1H) , 12.53 (br s , 1H) . LC/M S: condition 1, retention t ime = 2.62 min LC/M S(ESI +) m/z; 381 [M+H] + LC/M S(ESI ) m/z; 379 [M- H] ' H-N MR (CDCI 3) : 1.33 ( , 2H) , 1.94 ( , 2H) , 2 .14 (m, 4H) , 2 .69 (m, 1H) , 2.83 (t , J = 6 .9 Hz, 2H) , 2.99 (t, J = 6.9 Hz , 2H) , 3 .16 (tt , J 198 = 12.0, 3 .3 Hz, 1H), 7.75 (d , J = 3 .3 Hz, 1H) , 7 . 16 (m , 2H) , 7.29 (m, b 3H), 9.2 1 (s , 1H), 9 .46 (br s , 1H) . LC/M S: condition 1, retention tim e = 2 .87 min LC/M S(ESI +) m/z; 395, 397 [M+H] + LC/M S(ESI ) m/z; 393, 395 [M- H] -NMR (CDCI 3) : 1.26- 1.38 (m, 2H), 1.92 (m, 2 H) , 2. 15 (m, 4H) , 2.62 (tt , J = 1.1, 3 .3 Hz , H) , 2 .98 (d , J = 2.9 Hz, H) , 3 . 6 (tt , J = 12 .6, 3.3 Hz, 1H) , 3.6 0 (d, J = 13.2 Hz, 1H) , 6 .74 (d , J = 3.3 Hz, 199 1H), 7 .30-7. 39 ( , 3H), 7 .55 (m, 2H), 9.23 (s , 1H) , 9 .77 (br s , 1H) . b LC/M S: condition 1, retention t ime = 2 .97 min LC/M S(ESI +) m/z; 479, 4 8 1 [M+H] + LC/M S(ESI m/z; 477, 479 fM- HV H-N MR (CDCI 3) : 1.26- 1.43 ( , 2H), 1.92 (m, 2 H) , 2. 15 (m, 4H) , 2 .63 (tt, J = 11.4, 3.3 Hz, 1H) , 3.00 (d, J = 13.2 Hz, 1H) , 3 . 17 (tt , J = 12 .3, 3.3 Hz, 1H) , 3.6 0 (d, J = 13.2 Hz, 1H) , 6 .74 (d , J = 3 .3 Hz, 200 1H), 7.09 (t , J = 8.4 Hz , 2H) , 7 .32 (d, J = 3 .0 Hz, 1H) , 7.59(dd , J = b 8 .7 , 5.7 Hz, 2H) , 9.2 4 (s , 1H) , 10.00 (br s , 1H) . LC/M S: condition 1, retention t ime = 2 .79 min LC/M S(ESI +) m/z; 463 [M+H] + LC/M S(ESI ) m/z; 46 1 - 1 TABLE 124 Ex Data 1H-N MR (DMSO-of ) : 1.19- 1.35 (m, 2H) , 1.78 (qd , J = 12 .6, 4 .0 Hz, 2H), 1.92-2. 07 ( , 4H) , 2.5 1-2.6 1 (m, 1H) , 2 .68-2 .75 (m, 2H) , 2.78-2. 86 (m, 2H) , 3 .07-3. 19 ( , 2H), 6.80 (d , J = 3.6 Hz, 1H) , 20 1 7 .06-7. 14 (m, 2H) , 7.24-7. 3 1 (m, 2H) , 7.49 (d , J = 3 .6 Hz, 1H) , 9.5 1 b (s, 1H) , 12.52 (b r s , 1H) . LC/M S: condition 1, retention t ime = 2 .57 min LC/M S(ESI +) m/z; 379 [M+H] + LC/M S(ESI ) m/z; 377 [M- H] H-NMR (CD3OD) : 1.52 (m, 2H), 1.90 ( , 2H) , 2 . 18 (m, 4H) , 2 .80-3. 00 (m, 3H) , 3.23 (m, 1H), 4.92 (m, 1H) , 6 .82 (d , J = 3 .3 Hz , 202 1H), 6 .83-7. 43 (m, 6H), 9 .29 (s, 1H) . b LC/M S: condition 1, retention t ime = 0 .94 min LC/M S(ESI +) m/z; 377 [M+H] + LC/M S(ESI ) m/z; 375 [M- H] H-N MR (CD 3OD) : 1.43 (m, 2 H) , 1.90 ( , 2H) , 2 .12 (m, 4H) , 2 .7 1 (tt , J = 11.1, 3.9 Hz, 1H) , 2 .79-2 .9 1 (m, 2H) , 3.2 1 (tt, J = 12.3, 3.6 Hz, 1H) , 4 .79 (m, 1H), 203 6.8 1 (d, J = 3.3 Hz, 1H) , 7.25-7. 42 (m, 6H) , b 9.27 (s, 1H). LC/M S: condition 1, retention t ime = 1.29 min LC/M S(ESI +) m/z; 377 [M+H] + LC/M S(ESI ) m/z; 375 [M-H] H-N MR (CD3OD) : 1.57 (m, 2H) , 1.93 (m, 2H), 2.20 ( , 4H) , 2 .95-3.09 (m, 3H) , 3.24 (m, 1H) , 4.90 ( , 1H) , 6 .83 (d , J = 3 .3 Hz , 204 1H) , 7 .27-7. 44 ( , 6H), 9 .30 (s, 1H). b LC/M S: condition 1, retention t ime = 1.29 min LC/M S(ESI +) m/z; 377 [M+H] + LC/M S(ESI ) m/z; 375 [M- H] LC/M S: condition 1, retention tim e = 3.80, 4. 15 mi n (cis/t rans 205 mixtu re) LC/M S(ESI +) m/z; 367 [M+H] + LC/M S(ESI ) m/z; 365 [M- H] H-N MR (DMSO- ) : 1.72-1 .88 (m, 4H) , 1.96-2. 13 (m, 4H) , 3 . 19-3. 38 (m, 2H) , 6 .89 (d, J = 3 .3 Hz, 1H) , 7 . 10-7 .18 (m, 2H) , 7.5 1 (d, J = 3.0 Hz, 1H) , 7.63-7.70 (m, 2H) , 9 .54 (s , 1H) , 9.98 (s, 1H) , 206 12 .55 (br s , 1H). LC/M S: condition 1, retention t ime = 3 .63 min LC/M S(ESI +) m/z; 379 [M+H] + LC/M S(ESI ) m/z; 377 [M- H] H-NMR (DMSO- ds) : 1.66-1 .82 (m, 4H) , 1.89- 1.97 (m, 2H) , 2 .00-2. 09 (m, 2H) , 2.32-2.43 (m, 1H) , 3 . 14-3.25 (m, 1H) , 4.27 (d , J = 6.3 Hz, 2H) , 6.86 (dd , J = 3.0, 1.7 Hz, 1H) , 7 .12-7.20 ( , 2H) , 207 7.26-7. 32 (m, 2H) , 7 .50 (t, J = 3 .0 Hz , 1H), 8.3 1-8.37 (m, 1H), 9.52 (s, 1H) , 12.5 3 (b r s , 1H) . LC/M S: condition 1, retention tim e = 3.49 min LC/M S(ESI +) m/z; 393 [M+H] + LC/M S(ESI ) m/z; 391 [M- H] TABLE 125 Ex Data H-N MR (DMSO- c ) : 1.60-1 .88 (m, 6H) , 1.98-2. 06 (m, 2H) , 2 .20- 2 .3 1 (m, 1H) , 2 .72 (t, J = 6 .9 Hz, 2 H) , 3 . 11-3.22 (m, 1H) , 3.24-3.31 ( , 2H) , 6.84 ( d , J = 3 .0 , 1.7 Hz, 1H) , 7.07-7 .16 (m, 2H) , 7.2 1-7.28 (m , 2H) , 7.50 (t, J = 3.0 208 Hz, 1H) , 7 .85 (t, J = 5.6 Hz, 1H) , 9 .52 (s, 1H), 12 .53 (br s , 1H). LC/M S: condition 1, retention t ime = 3 .59 in LC/M S(ESI +) m/z; 407 [M+H] + LC/M S(ESI ) m/z; 405 [M- H] LC/M S: condition 1, retention t ime = 3 .00 min 209 LC/M S(ESI +) m/z; 357 [M+H] + LC/M S(ESI ) m/z; 355 [M- H] H-N MR (DM SO-d ) : 1.78-1 .98 (m, 3H) , 2 .2 1 (br s , 1H) , 2.9 1 (br s , 3H) , 3 .63 (s, 2H) , 6 .57 (s, 1H) , 7. 17 (s, 1H) , 7.57 (d, J = 7.5 Hz, 2 10 2H) , 7.82 (d , J = 7 .5 Hz, 2H) , 8.3 1 (s, 1H) , 8 .83 (s, 1H), 11.94 (br s , 1H). LC/M S: condition 3 , re tention t ime = 1.2 1 min LC/M S(ESI +) m/z; 357 [+ H-N MR (C D C I3) : 2 .46-2. 63 (m, 2H) , 3.58-4.09 (m , 5H) , 5.18 (s , 2H) , 6 .76 (s, 1H) , 7 .3 1-7. 40 (m, 6H) , 9.19 (br s , 1H), 9.24 (s, 1H) . 2 11 LC/M S: condition 3 , re tention tim e = 2 .05 min LC/M S(ESI +) m/z; 363 [M+H] + LC/M S(ESI ) m/z; 36 1 [M- H] H-N MR (C D C I 3) : 2.02-2 .41 (m, 5H) , 2 .45-2. 73 (m, 3H), 3.02 (d, J = 10.7 Hz, 1H) , 3.2 1-3.36 (m, 1H) , 3 .37 (d, J = 9.4 Hz, 1H) , 4.86 (dd , J = 10.7, 3.4 Hz, 1H) , 6 .82 (d , J = 3.0 Hz, 1H) , 7 .32 (br s, 1H) , 2 12 7.54 (d , J = 8 .3 Hz, 2H), 7 .63 (d , J = 8.3 Hz, 2H) , 9.14 (br s , 1H) , 9.25 (s, 1H) . LC/M S: condition 1, retention t ime = 2 .67 min LC/M S(ESI +) m/z; 43 1 [M+H] + LC/M S(ESI ) m/z; 429 [M- H] TABLE 126 Ex Data LC/M S: co ndition 3 , retention time = 1.35 i n 2 13 LC/M S(ESI +) m/z; 388 [M+H] + LC/M S(ESI ) m/z; 386 [M-H] -NMR (DMSO-cfe) : 1.86-2 .05 (m, 4H) , 2 .19-2.32 (m, 2H) , 2 .8 8-3.00 (m, 2H) , 3 .37 -3.50 (m, 1H) , 3 .60 (s , 2H) , 6 . 80-6. 85 (m, 1H) , 7 .47-7. 54 (m, 2H) , 7 .80-7 .8 9 ( , 1H) , 8 .38-8 .42 (m, 1H) , 2 14 9.53 (s , 1H) , 12 .54 (br s , 1H) . LC/M S: co ndition 3 , ret enti on time = 1.2 1 mi n LC/M S(ES I+) m/z; 368 [M+H]+ LC/M S(ES I ) m/z ; 366 [M-H] H-N MR (DM SO-d ) : 1.88-2.08 (m, 4 H) , 2 . 13-2. 29 (m , 2H) , 2.94-3.07 (m, 2H) , 3 .10-3.22 (m, 3H) , 6 .10-6 .22 (m, 1H) , 6.37-6. 53 (m, 3H) , 6.8 1 (d, J = 3 .2 Hz, 1H) 2 15 , 7.49 (d, J = 3 .2 Hz , 1H) , 7.60 (s , 1H) , 9 .52 (s , 1H) , 12.52 (br s , 1H) . LC/M S: co ndition 3 , ret enti on time = 1.40 mi n LC/M S(ESI +) m/z; 349 [M+H]+ H-N MR (DMSO-de) : 1.84-2.05 (m, 4H) , 2.05-2. 18 (m, 2H) , 2.24 (s, 3H) , 2.86-2.96 (m, 2H) , 3 .15-3. 18 (m, 1H) , 6.80 (d , J = 3 .2 Hz , 216 1H) , 7 .49 (d , J = 3 .2 Hz , 1H) , 9 .52 (s , 1H) , 12.53 (br s , 1H) . LC/M S: co ndition 3 , ret enti on time = 0.47 mi n LC/M S(ES I+) m/z; 257 [M+H]+ H-NMR (DMSO-de) : 1.85 -2.06 (m, 4 H) , 2 . 18-2. 32 (m , 2H) , 2.70-2.76 (m, 1H) , 2.9 0-3. 03 (m, 2 H) , 3 .68 (s, 2H) , 6 .82 (d, J = 3 .3 2 17 Hz, 1H), 7.45 -7.62 (m, 4H) , 9 .52 (s , 1H), 12.53 (br s, 1H) , 13.22 (br s , 1H) . LC/M S: co ndition 3 , retenti on time = 1.35 mi n LC/M S(ES I+) m/z; 407 , 40 9 [M+H] + H-N MR (DMSO-de) : 1.88-2. 15 (m, 4 H) , 2 .25-2. 40 (m , 2H) , 2.97-3. 10 (m, 2H) , 3.14-3. 30 ( , 1H) , 3. 83 (s, 2H) , 6 .84 (d, J = 3 .0 218 Hz, 1H) , 7 .50 (d , J = 3.0 Hz, 1H) , 7 .89-7.96 (m, 1H) , 8 .00-8 .15 (m, 2H) , 8 .89-9 .00 (m , 2H) , 9 .52 (s, 1H) , 12.5 3 (br s , 1H) . LC/M S: co ndition 3 , retention time = 1.15 mi n LC/M S(ESI +) m/z; 385 [M+H]+ H-N MR (DMSO-d ) : 1.82 -2.08 (m, 4 H) , 2 .20-2. 32 (m , 2H) , 2.94-3. 10 (m, 2H) , 3 .10-3. 23 (m, 1H) , 3 .50 (s, 2H) , 6 .80 (d, J = 3 .2 Hz, 1H) , 7.4 8 (d , J = 3 .2 Hz, 1H) , 8.01 (s, 1H) , 8.3 1 (s, 1H) , 9.52 2 1 9 (s, 1H) , 12 .53 (b r s, 1H) . LC/M S: co ndition 3 , retention time = 0.63 mi n LC/M S(ESI +) m/z; 324 [M+H]+ H-N MR (DMSO- fi ) : 1.93 -2.00 (m, 4H) , 2 . 16-2.22 (m, 2H) , 2 .93 (d, J = 11.4 Hz , 2H) , 3. 16 (s, 1H) , 3.53 (s , 2 H) , 6.78 (dd, J = 3.3 , 220 1.2 , 1H) , 7. 3 (d, J = 8.4 Hz, 2H) , 7 .20 (s, 1H) , 7.39 (d , J = 7 .8 Hz , 2H) , 7 .45-7 .47 (m , 1H) , 9 .48 (s, 1H) . LC/M S: co ndition 3 , retention time = 1.54 mi n LC/M S(ESI +) m/z; 399 [M+H]+ TABLE 127 Ex Data H-NMR (DMSO-d ) : 1.95-2 .06 (m, 4 H), 2 .23 (t, J = 9.8 Hz, 2H) , 2 .97 (d, J = 10 .8 Hz, 2 H), 3 .16 (s , 1H) , 3.5 9 (s, 2H) , 6 .80 (d , J = 3.3 Hz, 22 1 1H) , 7.08 (s, 1H), 7.47-7.49 (m, 3H), 7.61 (d, J = 8.4 Hz , 2H) , 7 .72 (s , 1H) , 8.22 (s, 1H) , 9.49 (s, 1H) . LC/M S: condition 3 , retention time = 0.48 mi n LC/M S(ES I+) m/z; 399 [M+H] + H-N MR (DMSO-ai 6) : 1.92-2 .09 ( , 4H) , 2 .25-2.32 (m, 2H) , 2 .9 4 (d , J = 11.1 Hz, 2H) , 3 .68 (s , 2H) , 6 .82 (d , J = 2.7 Hz , 1H) , 222 7 .43-7 .54 (m, 3H) , 7 .9 1 (t, J = 7.5 Hz, 1H) , 9 .50 (s, 1H) . LC/M S: co ndition 3, retenti on time = 1.35 mi n LC/M S(ES I+) m/z; 376 [M+H]+ LC/M S(ESI ) m/z; 374 [M- H] 'H- MR (DMSO- ) : 1.9 3-2.0 5 (m, 4 H) , 2.24 (td, J = 11. 1, 3 .3 Hz , 2H) , 2 .92 (d, J = 11.7 Hz, 2 H) , 3.58 (s , 2H) , 6 .81 (d , J = 2.7 Hz , 1H) , 7.47-7.5 3 (m, 2H) , 7.75-7.80 (m, 1H) , 7.86 (dd, J = 6 .3, 2 . 1 223 Hz, 1H), 9.5 1 (s, 1H) , 12 .5 1 (b r s , 1H) . LC/M S: co ndition 3 , retenti on time = 1.37 mi n LC/M S(ESI +) m/z; 376 [M+H] + LC/M S(ESI ) m/z; 374 [M-H] LC/M S: co ndition 3 , retenti on time = 1.63 mi n 224 LC/M S(ESI +) m/z; 437 [M+H]+ LC/M S(ES I ) m/z ; 435 [M-H] Ή -NMR (DM SO- ) : 1.89-2.08 (m, 4 H) , 2 . 11-2. 32 (m , 2H) , 2 .89-3.03 (m, 2H) , 3 .12-3.26 (m , 1H) , 3.40-3.52 ( , 2H) , 4.55 (s , 2H) , 6 .77-7 .00 (m, 4H) , 7.47-7.5 3 (m, 1H) , 9.52 (s, 1H) , 10.66 (br 225 s , 1H) , 12 .53 (b r s , 1H) . LC/M S: co ndition 3 , retenti on time = 1.23 mi n LC/M S(ESI +) m/z; 404 [M+H]+ LC/M S(ES I ) m/z ; 402 [M-H] -N R (DMSO-d ) : 1.90- 1.97 (m, 4H) , 2 . 13 (t, J = 10.7 Hz , 2H) , 2.69 (t, J = 6.6 Hz, 2H) , 2.9 1-2.96 (m, 5H) , 3.4 1 (s , 2H) , 3.64 (t, J 226 = 6.8 Hz, 2H) , 6.73 (d, J = 8 .4 Hz, 2 H) , 6 .79 (d , J = 3.3 Hz , 1H) , 7 .15 (d, J = 8 .1 Hz, 2H) , 7.48 (d , J = 3 .0 Hz, 1H) , 9.50 (s , 1H) . LC/M S: co ndition 3, ret enti on time = 1.48 mi n LC/M S(ESI +) m/z; 4 15 [M+H]+ Ή -NMR (DM SO-d ) : 1.87-2.08 (m, 4 H) , 2 . 15-2. 30 ( , 2H) , 2.90-3.00 (m, 2H) , 3.10-3. 26 (m, 1H) , 3 .57 (s, 2H) , 6 .82 (d, J = 3 .3 Hz, 1H) , 7 .19 (dd, J = 1.5 , 8.5 Hz , 1H) , 7 .36 (d, J = 8 .5 Hz, 1H) , 227 7.3 9 (d, J = 1.5 Hz, 1H) , 7 .49 (d , J = 3.3 Hz, 1H) , 9 .52 (s , 1H) , 12 .52 (b r s , 1H) . LC/M S: co ndition 3 , ret enti on time = 1.66 mi n LC/M S(ESI +) m/z; 4 13 [M+H]+ LC/M S(ES I ) m/z ; 4 1 1 [M-Hl TABLE 128 Ex Data H-NMR (DM SO-de) : 1.87-2.08 (m, 4 H) , 2 . 18-2. 32 ( , 2H) , 2 .90-3.03 (m, 2H) , 3.04-3.22 (m , 1H) , 3.55 (s , 2H) , 6.39 -6.48 ( , 2H) , 6.8 1 (d , J = 3.0 Hz , 1H) 22 8 , 7 .48 (d, J = 3.0 Hz, 1H), 9.5 1 (s , 1H) , 12 .52 (b r s , 1H) . LC/M S: co ndition 3 , retention time = 1.37 mi n LC/M S(ES I+) m/z; 357 , 359 [M+H] + H-NMR (DMSO- ) : 1.86-2 .06 (m, 4H) , 2 .20-2.34 ( , 2H) , 2 .9 2- 3.02 ( , 2H) , 3 . 10-3.24 (m, 1H) , 3 .67 (s , 2H) , 6 .80-6. 85 (m, 1H) , 7 .14-7 .33 (m, 3H) , 7 .44-7 .50 (m, 1H) , 9.52 (s , 1H) , 12 .52 229 (br s , 1H) . LC/M S: condition 3 , retenti on time = 1.60 mi n LC/M S(ES I+) m/z; 413 [M+H]+ LC/M S(ES I ) m/z; 4 1 1 [M-H] Ή -NMR (DM SO- ) : 1.94-2. 17 (m, 4H) , 3 .46-3. 65 (m , 3H) , 4.25-4.38 (m, 2H) , 6 .9 1 (d , J = 3 .3 Hz, 1H) , 7 .10 (t, J = 6. 9 Hz, 1H) , 7.31 (t, J = 6.9 Hz, 2H) , 7 .5 1 (d, J = 7.5 Hz, 2H) , 7 .52 (s, 2H) , 230 9.54 (s , 1H) , 12 .56 (br s , 1H) . LC/M S: co ndition 3 , ret enti on time = 2.23 mi n LC/M S(ES I+) m/z; 370 [M+H]+ LC/M S(ESI ) m/z ; 368 [M-Hl LC/M S: co ndition 3 , ret enti on time = 1.44 mi n 23 1 LC/M S(ES I+) m/z; 402 , 404 [M+H]+ LC/M S(ES I ) m/z ; 400, 403 [ M-H] LC/M S: co ndition 3 , retenti on time = 1.49 mi n 232 LC/M S(ESI +) m/z; 390 [M+H]+ LC/M S(ES I ) m/z ; 38 8 [M-H] LC/M S: co ndition 3 , ret enti on time = 1.77 mi n 233 LC/M S(ESI +) m/z; 495 , 497, 499 [M+H] + LC/M S(ESI ) m/z ; 493 , 495, 497 [M-H] - LC/M S: co ndition 3 , retenti on time = 1.20 mi n 234 LC/M S(ESI +) m/z; 425 [M+H] + LC/M S(ES I ) m/z ; 423 [M-H] LC/M S: co ndition 3 , retention time = 2.44 mi n 235 LC/M S(ES I+) m/z; 404 , 406 [M+H] + LC/M S(ESI ) m/z; 402, 404 [ M-H] LC/M S: co ndition 3, ret ention time = 1.46 mi n 236 LC/M S(ESI +) m/z; 353 [M+H]+ LC/M S(ES I ) m/z ; 35 1 [M-H] 237 LC/M S: co ndition 3 , retention time = 1.51 mi n LC/M S(ESI +) m/z; 4 17, 4 1 9 [M+H] + LC/M S: co ndition 3, retenti on time = 1.55 mi n 238 LC/M S(ESI +) m/z; 4 17 , 4 1 9 [M+H] + LC/M S(ESI ) m/z ; 4 15 , 4 17 [ M-H] LC/M S: co ndition 3 , retention time = 0.50 mi n 239 LC/M S(ESI +) m/z; 334 [M+H] + LC/M S(ES I ) m/z ; 332 [M-H] TABLE3 129 Ex Data 1H-N MR (D SO-d ) : 1.85-2.08 (m, 4H) , 2 .20-2. 34 (m , 2H) , 2.96-3.09 ( , 2H) , 3.09-3. 22 (m, 1H) , 3 .74 (s, 2H) , 6 .8 1 (d, J = 3 .2 Hz, 1H) , 7.4 8 (d , J = 3 240 .2 Hz, 1H) , 7.55 (s, 1H) , 9.06 (s, 1H) , 9.52 (s, 1H) , 12 .52 (b r s, 1H) . LC/M S: co ndition 3 , retenti on time = 0.88 min LC/M S(ESI +) m/z; 340 [M+H]+ H-N MR (DMSO- e) : 1.95-2 .08 (m, 4H) , 2.22 (t, J = 11.1Hz, 2 H) , 2 .9 5 (d , J = 9 .9 Hz , 2H) , 3 .2 8 (s , 1H) , 3.60 (s , 2H) , 6 .82 (br s , 1H) , 7.2 8 (b r s , 1H) , 7 .42 (d, J = 8 .1 Hz, 2H) , 7.49 (t , J = 2.7 Hz , 1H) , 7.84 (d, J = 8.1 Hz, 2H) , 7 .9 1 (b r s , 1H) , 9.5 1 24 1 (s , H) , 12 .52 (br s , 1H) . LC/M S: co ndition 3 , ret enti on time = 0.73 mi n LC/M S(ESI +) m/z; 376 [M+H]+ LC/M S(ESI ) m/z ; 374 [M-HV 'H-N MR (DMSO-d ) : 1.95 -2.04 ( , 4H) , 2 .28 (t, J = 10 .1 Hz , 2H) , 2.92 (d , J = 11.7 Hz, 2 H) , 3. 16-3. 19 (m, 1H) , 3.70 (s, 2H) , 6.82 (d d , J = 3 .3, 1.5 Hz, 1H) , 7 .49 (d , J = 3.3 Hz, 1H) , 7 .92 (d, J = 8.7 Hz, 242 1H) , 8 .11-8 .13 ( , 2H) , 9 .51 (s, 1H) . LC/M S: co ndition 3 , retenti on time = 1.34 mi n LC/M S(ESI +) m/z; 383 [M+H]+ LC/M S(ESI ) m/z ; 38 1 [M-H] 'H-N MR (DMSO-de) : 1.95 -2.07 (m, 4H) , 2 .28 (t, J = 10 .1 Hz , 2H) , 2.94 (d, J = 11.1 Hz, 2 H), 3 .71 (s , 2H) , 6 .83 (dd , J = 3 .3, 1.2 Hz , 1H) , 7.49 (d, J = 3.3 Hz, 1H) , 7 .97 (m, 2H) , 8 .13 (s , 1H) , 9.52 (s , 243 1H) . LC/M S: condition 3 , retenti on time = 1.65 mi n LC/M S(ESI +) m/z; 426 [M+H]+ LC/M S(ESI ) m/z ; 424 [M-HV Ή -NMR (DMSO- ) : 1.9 1-2.08 (m, 4H) , 2.30 (td, J = 11.3 , 2 .9 Hz , 2H) , 2 .93 (d, J = 11.7 Hz, 2H) , 3 .16-3 .23 ( , 1H) , 3 .74 (s, 2H) , 6.82 (d, J = 3 .3 Hz , 1H) , 7 .48 (d , J = 3.3 Hz, 1H), 7.8 9 (d, J = 7 .8 244 Hz, 1H), 7.98 (s, 1H) , 8 .14 (d , J = 7 .8 Hz, 1H) , 9.5 0 (s , 1H) . LC/M S: condition 3 , retenti on time = 1.60 mi n LC/M S(ES I+) m/z; 426 [M+H] + LC/M S(ESI ) m/z ; 424 fM-Hl Ή -NMR (DM SO- ) : 1.35 (d, J = 6.6 Hz, 3H) , 1.82-2 .05 (m, 4H) , 2.05-2.30 (m, 2H) , 2.83-2.95 (m, 1H) , 3 .02 -3. 19 (m , 1H) , 3 .55 (q , J = 6.6 Hz, 1H) , 6.79 (d , J = 8.3 Hz, 2H) , 7 . 18-7 .28 (m, 1H) , 245 7.28-7.40 (m, 4H), 7.48 (d, J = 3.3 Hz , 1H) , 9.5 1 (s, 1H) , 12.5 1 (br s , 1H) . LC/M S: co ndition 3 , retenti on time = 1.44 mi n LC/M S(ESI +) m/z; 347 [M+H]+ LC/M S(ES I ) m/z ; 345 - LC/M S: co ndition 3 , ret ention time = 1.16 mi n 246 LC/M S(EST) m/z; 282 [M+H] + LC/M S(ESI ) m/z ; 280 - TABLE 130 Ex Data LC/M S: condition 3 , retention tim e = 2 .38 min 247 LC/M S(ESI +) m/z; 406 [M+H] + LC/M S(ESI ) m/z; 404 [M-H] LC/M S: condition 3 , retention tim e = 2.48 min 248 LC/MS(ESI +) m/z; 422 [M+H] + LC/M S(ESI ) m/z; 420 [- LC/M S: condition 3 , retention tim e = 2.48 min 249 LC/M S(ESI +) m/z; 383 [M+H] + LC/M S(ESI ) m/z; 381 [M- H] LC/M S: condition 3 , retention tim e = 2.6 1 min 250 LC/M S(ESI +) m/z; 40 1 [M+H] + LC/M S(ESI ) m/z; 399 [M- H] LC/M S: condition 3 , retention tim e = 2 .67 min 25 1 LC/M S(ESI +) m/z; 433 [M+H] + LC/M S(ESI ) m/z; 43 1 [- LC/M S: condition 3 , retention time = 2 .36 min 252 LC/M S(ESI +) m/z; 390 [M+H] + LC/MS(ESI ) m/z; 388 [M- H] LC/MS : condition 3, retention time = 0.65 min 253 LC/M S(ESI +) m/z; 37 1 [M+H] + LC/M S(ESI ) m/z; 369 [M- H] 254 LC/M S: condition 3 , retention time = 1.24 min LC/M S(ESI +) m/z; 343 [M+H] + LC/M S: condition 3 , retention time = 1. 18 min 255 LC/MS(ESI +) m/z; 335 [M+H] + LC/M S(ESI ) m/z; 333 [- LC/M S: condition 3 , retention time = 1.40 min 256 LC/M S(ESI +) m/z; 367 [M+H] + LC/M S(ESI ) m/z; 365 [M- H] 257 LC/M S: condition 3 , retention tim e = 1.08 min LC/M S(ESI +) m/z; 327 [M+H] + LC/M S: condition 3 , retention time = 1.48 min 258 LC/MS (ESI +) m/z; 407 [M+H] + LC/MS(ESI ) m/z; 405 [M- H] LC/M S: condition 3 , retention tim e = 1. 16 min 259 LC/M S(ESI +) m/z; 3 10 [M+H] + LC/M S(ESI ) m/z; 308 [M- H] LC/M S: condition 3 , retention tim e = 0 .96 min 260 LC/M S(ESI +) m/z; 354 [M+H] + LC/M S(ESI ) m/z; 352 [M- Hl 261 LC/M S: condition 3 , retention time = 1.09 min LC/M S(ESI +) m/z; 382 [M+H] + LC/MS : condition 3 , retention tim e = 2.22 min 262 LC/M S(ESI +) m/z; 397 [M+H] + LC/MS(ESI ) m/z; 395 [M- H] TABLE 132 Ex Data LC/M S: condition 1, retention tim e = 0.37 in 278 LC/M S(ESI +) m/z; 355 [M+H] + LC/M S(ESI ) m/z; 353 [M- H] LC/M S: condition 1, retention time = 0 .39 min 279 LC/M S(ESI +) m/z; 355 [M+H] + LC/M S(ESI ) m/z; 353 [- LC/M S: condition 1, retention tim e = 0 .63 min 280 LC/M S(ESI +) m/z; 3 1 1 [M+H] + LC/M S(ESI ) m/z; 309 [M- H] LC/MS : condition 1, retention tim e = 0.39 min 281 LC/M S(ESI +) m/z; 336 [M+H] + LC/M S(ESI ) m/z; 334 [M- H] LC/M S: condition 1, retention time = 2.70 min 282 LC/M S(ESI +) m/z; 400 [M+H] + LC/M S(ESI ) m/z; 398 - 283 LC/M S: condition 3 , retention tim e = 1.36 min LC/M S(ESI +) m/z; 325 [M+H] + 284 LC/M S: condition 3 , retention t ime = 1.46 min LC/MS (ESI +) m/z; 339 [M+H] + 285 LC/M S: condition 3 , retention time = 1.36 min LC/M S(ESD m/z; 325 [M+H 286 LC/M S: condition 3 , retention time = 1.15 min LC/M S(ESI +) m/z; 3 1 1 [M+H] + 287 LC/M S: condition 3 , retention time = 1.22 min LC/M S(ESI +) m/z; 325 [M+H] + LC/M S: condition 3 , retention tim e = 1.07 min 288 LC/M S(ESI +) m/z; 356 [M+H] + LC/M S(ESI ) m/z; 354 [M- H] 289 LC/M S: condition 3, retention time = 1.33 min LC/M S(ESI +) m/z; 355 [M+H] + LC/M S: condition 3, retention time = 1.49 min 290 LC/M S(ESI +) m/z; 339 [M+H] + LC/MS (ESI ) m/z; 337 [M- H] LC/M S: condition 3 , retention tim e = 1.39 min 291 LC/M S(ESI +) m/z; 325 [M+H] + LC/M S(ESI ) m/z; 323 [M-H] LC/M S: condition 3 , retention time = 2.33 min 292 LC/M S(ESI +) m/z; 379 [M+H] + LC/M S(ESI ) m/z; 377 [M-H] LC/M S: condition 3 , retention tim e = 1.37 min 293 LC/M S(ESI +) m/z; 355 [M+H] + LC/M S(ESI ) m/z; 353 [M-H LC/M S: condition 3 , retention tim e = 1.09 min 294 LC/M S(ESI +) m/z; 327 [M+H] + LC/M S(ESI ) m/z; 325 [M- H] TABLE 133 Ex Data 295 LC/M S: condition 3, retention tim e = 1.36 min LC/M S(ESI +) m/z; 325 [M+H] + 296 LC/M S: condition 3, retention tim e = 1.10 min LC/M S(ESI +) m/z; 299 [M+H] + 297 LC/M S: condition 3, retention tim e = 1.07 min LC/M S(ESI +) m/z; 329 [M+H] + LC/M S: condition 3, retention tim e = 1.03 min 298 LC/M S(ESI +) m/z; 359 [M+H 1+ 299 LC/M S: condition 3 , retention tim e = 1.62 min LC/M S(ESI +) m/z; 440 [M+H] + LC/M S: condition 3 , retention tim e = 2.38 min 300 LC/M S(ESI +) m/z; 400 [M+H] + LC/M S(ESI ) m/z; 398 [M- H 30 1 LC/M S: condition 3 , retention tim e = 1.16 min LC/M S(ESI +) m/z; 350 [M+H] + LC/M S: condition 3 , retention tim e = 1.14 min 302 LC/M S(ESI +) m/z; 338 [M+H] + LC/M S(ESi ) m/z; 336 [M- Hl 303 LC/MS : condition 3, retention time = 1.3 1 min LC/M S(ESI +) m/z; 42 1 [M+H] + 304 LC/M S: condition 3 , retention tim e = 1.45 min LC/M S(ESI +) m/z; 42 1 [M+H] + 305 LC/M S: condition 3 , retention tim e = 1.20 min LC/M S(ESI +) m/z; 369 [+ 306 LC/M S: condition 3 , retention tim e = 1.54 min LC/M S(ESI +) m/z; 397 [M+H] + 307 LC/M S: condition 3 , retention tim e = 1.62 min LC/M S(ESI +) m/z; 440 [M+H] + LC/M S: condition 3 , retention tim e = 1.74 min 308 LC/M S(ESI +) m/z; 437 [M+H]+ LC/MS (ESI ) m/z; 435 [- LC/M S: condition 3 , retention tim e = 2.00 min 309 LC/M S(ESI +) m/z; 533 [M+H] + LC/M S(ESI ) m/z; 531 - 310 LC/M S: condition 3 , retention time = 1.71 min LC/M S(ESI +) m/z; 440 [M+H] + 311 LC/M S: condition 3 , retention time = 1.30 min LC/M S(ESI +) m/z; 397 [M+H] + LC/M S: condition 3 , retention time = 1.46 min 3 12 LC/M S(ESI +) m/z; 383 [M+H] + LC/M S(ESI ) m/z; 38 1 [M- H] LC/M S: condition 3 , retention tim e = 1.46 min 3 13 LC/M S(ESi +) m/z; 383 [M+H] + LC/MS : condition 3, retention tim e = 1.23 min 3 14 LC/M S(ESI +) m/z; 393 [+ TABLE 134 Ex Data 3 15 LC/M S: condition 3, retention tim e = 0.96 min LC/M S(ESI +) m/z; 384 [M+H] + 3 16 LC/M S: condition 3 , retention tim e = 1.4 1 min LC/M S(ESI +) m/z; 337 [M+H] + LC/M S: condition 3 , retention time = 2 .52 min 3 17 LC/M S(ESI +) m/z; 42 1 [M+H] + LC/M S(ESI ) m/z; 4 19 [- 318 LC/M S: condition 3 , retention tim e = 1.13 min LC/M S(ESI +) m/z; 382 [M+H] + 319 LC/M S: condition 3 , retention time = 1. 13 min LC/M S(ESI +) m/z; 382 [M+H] + LC/M S: condition 3 , retention tim e = 1.4 1 min 320 LC/M S(ESI +) m/z; 436 [M+H] + LC/M S(ESI ) m/z; 434 [M- H] LC/M S: condition 3 , retention time = 1.4 1 min 32 1 LC/M S(ESI +) m/z; 436 [M+H] + LC/M S(ESI ) m/z; 434 - LC/MS : condition 3 , retention time = 1.60 min 322 LC/M S(ESI +) m/z; 421 [M+H] + LC/M S(ESL) m/z; 4 19 [M- H] 323 LC/M S: condition 3 , retention time = 1.76 min LC/M S(ESI +) m/z; 405 [M+H 1+ 324 LC/M S: condition 3 , retention time = 1.83 min LC/M S(ESI +) m/z; 4 19 [M+H] + 325 LC/M S: condition 3 , retention tim e = 1.23 min LC/M S(ESI +) m/z; 343 [M+H] + 326 LC/MS : condition 3 , retention tim e = 1.38 min LC/M S(ESI +) m/z; 387 [M+H] + 327 LC/M S: condition 3 , retention tim e = 1. 19 min LC/M S(ESI +) m/z; 34 1 [M+H] + LC/M S: condition 3 , retention tim e = 1.26 min 328 LC/M S(ESI +) m/z; 36 1 [M+H] + LC/M S(ESI ) m/z; 359 - LC/M S: condition 3 , retention tim e = 1.08 min 329 LC/M S(ESI +) m/z; 285 [M+H] + LC/M S(ESI ) m/z; 283 [ M-H] 330 LC/M S: condition 3 , retention time = 1. 18 min LC/M S(ESI +) m/z; 299 [M+H] + 33 1 LC/M S: condition 3 , retention tim e = 1.28 min LC/MS (ESI +) m/z; 3 13 [M+H] + 332 LC/M S: condition 3 , retention tim e = 1.38 min LC/MS (ESI +) m/z; 327 [M+H] + 333 LC/M S: condition 3 , retention tim e = 1.2 1 min LC/MS (ESI +) m/z; 309 [M+H] + LC/M S: condition 1, retention time = 0 .34 min 334 LC/M S(ESI +) m/z; 424 [M+H] + LC/M S(ESI ) m/z; 422 [M-H] TABLE 135 Ex Data LC/M S: co ndition 1, retention time = 2.94 mi n 335 LC/M S(ESI +) m/z; 468 [M+H]+ LC/M S(ESI ) m/z ; 466 [M-H] LC/M S: co ndition 1, retention time = 2.75 mi n 336 LC/M S(ESI +) m/z; 468 [M+H]+ LC/M S(ES I ) m/z ; 466 [- LC/M S: condition 1, retention time = 2.77 mi n 337 LC/M S(ES I+) m/z; 440 [M+H] + LC/M S(ES I ) m/z ; 438 - LC/M S: co ndition 3 , retention time = 1.15 mi n 338 LC/M S(ES I+) m/z; 329 [M+H] + LC/M S(ES I ) m/z ; 327 [M-H LC/M S: co ndition 3 , retention time = 1.19 mi n 339 LC/M S(ESI +) m/z; 347 [M+H]+ LC/M S(ES I ) m/z ; 345 [- 340 LC/M S: co ndition 3 , retention time = 0 .8 1 mi n LC/M S(ES I+) m/z; 368 [M+H]+ LC/M S: co ndition 3, retention time = 1.39 mi n 34 1 LC/M S(ESI +) m/z; 4 10 [M+H]+ LC/M S(ES I ) m/z; 408 [M-H] LC/M S: co ndition 3 , retention time = 1.85 mi n 342 LC/M S(ESI +) m/z; 403 [M+H]+ LC/M S(ESI ) m/z ; 40 1 [M-H] LC/M S: co ndition 3 , retention time = 1.38 min 343 LC/M S(ESI +) m/z; 383 [M+H]+ LC/M S(ES I ) m/z ; 38 1 [M-H] LC/M S: co ndition 3 , retention time = 1.3 1 mi n 344 LC/M S(ES I+) m/z; 343 [M+H]+ LC/M S(ESI ) m/z ; 34 1 - LC/M S: condition 3 , retention time = 1.3 1 mi n 345 LC/M S(ES I+) m/z; 432 [M+H]+ LC/M S(ESI ) m/z ; 430 [M-HV Ή -NMR (CD 3OD) : 1.3 9- 1.74 (m, 6H) , 1.95 (m , 2H) , 2 .19 (tt, J = 11.7, 3.3, 1H) , 3.05 (tt, J = 12.6, 3.9 , 1H) , 3 .67 (d, J = 14 .4 Hz, 1H) , 4.02 (d, J = 14 .4 Hz, 1H) , 6 .70 (d , J = 3 .3 Hz, 1H) , 7 .28 (m, 346 4H) , 7 .50 ( , 2H) , 9 .17 (s, 1H). LC/M S: co ndition 1, retenti on time = 3.77 mi n LC/M S(ES I+) m/z; 473 [M+H]+ LC/M S(ESI ) m/z ; 389 [- Ή -NMR (CD3OD) : 1.4 1- 1.76 (m, 6H) , 1.96 ( , 2H) , 2 .20 (tt, J = 12 , 3 .3, H) , 3.06 (tt, J = 11.7 , 3.6, 1H), 3 .65 (d, J = 14 .4 Hz, 1H) , 4.02 (d, J = 14 .4 Hz, 1H) , 6.70 (d, J = 3 .3 Hz, 1H) , 7 .02 (t, J = 8 .7 347 Hz, 2H) , 7 .28 (d, J = 3 .3 Hz , 1H) , 7.53 (dd , J = 8.7, 5 .4 Hz, 2H) , 9 .17 (s , 1H) . LC/M S: co ndition 1, ret enti on time = 3.84 mi n LC/M S(ES I+) m/z; 491 [M+H]+ LC/M S(ESI ) m/z ; 489 [- TABLE 136 Ex Data H-NMR (DMSO- ) : 1.56-1 .85 (m, 4H) , 1.92 (dd , J = 12.7, 2.5 Hz, 2H) , 2.03 (dd, J = 13.1, 3 .3 Hz, 2H), 2.28 (tt, J = 11.4 , 3.3 Hz, 1H), 3 .16 (tt , J = 11.9, 3.7 Hz, 1H), 6 .69 (br s , 1H) , 6 .82-6. 85 (m, 1H) , 7 .24 (br s , 1H) , 7.49 (t, J = 348 2.9 Hz, 1H) , 9.5 1 (s, 1H) , 12 .52 (br s , 1H) . LC/MS : condition 1, retention tim e = 1.22 in LC/M S(ESI +) m/z; 285 [M+H] + LC/M S(ESI ) m/z; 283 [M-H] LC/M S: condition 1, retention tim e = 3 .42 min 349 LC/M S(ESI +) m/z; 379 [M+H] + LC/M S(ESI ) m/z; 377 [M- H] Ή -NMR (DMSO- ) : 1.67- 1.87 (m, 4H) , 1.9 1-2 .10 (m, 4H), 2.35-2. 43 (m, 1H), 3 . 14-3.25 (m, 1H) , 4 .37 (d , J = 5.7 Hz, 2H) , 6 .84-6 .87 (m, 1H), 7 .44 (d, J = 7 .8 Hz , 2 H) , 7 .49 (t , J = 2 .9 Hz, 350 1H) , 7 .80 (d, J = 7.8 Hz, 2H) , 8.45 (t, J = 5.7 Hz, 1H) , 9.5 1 (s, 1H) , 12 .52 (br s , 1H) . LC/M S: condition 1, retention time = 3 .34 min LC/MS (ESI +) m/z; 400 [M+H] + LC/M S(ESI ) m/z; 398 [M- H] H-NMR (DMSO- ) : 1.65- 1.83 ( , 4H) , 1.88-2. 11 (m, 5H) , 3 .14-3. 26 (m, 1H), 6 .19 (d, J = 7.8 Hz, 1H) , 6.84-6 .87 (m, 1H) , 7 .46-7. 51 (m, 6H) , 9.14 (d, J = 7.8 Hz, 1H) , 9.5 1 (s, 1H) , 12 .52 (br 35 1 s , 1H) . LC/M S: condition 1, retention tim e = 3 .34 min LC/M S(ESI +) m/z; 400 [M+H] + LC/MS (ESI ) m/z; 398 [M- H] H-NMR (DMSO- ) : 1.60- 1.88 ( , 6H) , 1.98-2.06 (m, 2H) , 2 . 19-2 .32 (m, 1H) , 2.69-2 .76 (m, 2 H) , 3 .12-3.22 (m, 1H) , 3.25-3.33 (m, 2H) , 6.83-6. 86 (m, 1H) , 7.24 (d, J = 8 .3 Hz, 2H) , 7 .35 (d , J = 352 8 .9 Hz , 2H) , 7.50 (t, J = 2 .6 Hz, 1H), 7 .85 (t , J = 5 .6 Hz, 1H) , 9.52 (s, 1H) , 12 .53 (br s , 1H) . LC/M S: condition 1, retention time = 3 .84 min LC/M S(ESI +) m/z; 423 [M+H] + LC/MS (ESI ) m/z; 42 1 [M- H] H-N MR (DMSO- ) : 1.55- 1.89 (m, 6H) , 1.97-2.05 (m, 2H) , 2 .26-2 .39 (m, 1H) , 3 . 11-3 .22 (m, 1H) , 3.26-3.34 (m , 2H) , 4.58-4.66 (m, 1H) , 5.4 5 (d , J = 4 .5 Hz, 1H) , 6.84 (d, J = 3 .3 Hz, 1H) , 353 7 .2 1-7. 28 ( , 1H) , 7 .33 (d, J = 4.1 Hz, 4H) , 7 .49 (d , J = 3 .3 Hz, 1H), 7 .8 1 (t, J = 5.3 Hz, 1H), 9 .5 1 (s, 1H), 12 .52 (br s , 1H). LC/M S: condition 1, retention tim e = 3 . 19 min LC/MS(ESI +) m/z; 405 [M+H] + LC/MS (ESI ) m/z; 403 [M- H] TABLE 137 Ex Data H-N MR (DMSO-d ) : 1.65 - 1.82 (m, 4 H) , 1.87- 1.95 (m , 2H) , 2.00-2.09 (m, 2H) , 2.36 -2.43 (m, 1H) , 3 .13-3 .24 (m, 1H) , 3.8 5-3. 98 (m, 2H) , 6 .84-6 .87 (m, 1H) , 7 .49 (t , J = 2.9 Hz, 1H) , 8 .47 (t, J = 6 .5 354 Hz, 1H), 9.5 1 (s, 1H) , 12 .52 (b r s, 1H) . LC/M S: co ndition 1, retenti on time = 3.27 mi n LC/M S(ES I+) m/z; 367 [M+H]+ LC/M S(ES I ) m/z ; 365 [M-H] 'H-N MR (DMSO-d ) : 1.64-1 .82 (m, 4 H) , 1.87- 1.96 ( , 2H) , 2.0 1-2.09 (m, 2 H) , 2.26-2.3 9 (m, 1H) , 3 .14-3.25 (m, 1H) , 4 .15 (d , J = 5.9 Hz, 2H) , 6.8 5-6. 88 (m , 1H) , 7.5 0 (t, J = 2 .6 Hz, 1H) , 8.55 (t, J 355 = 5.3 Hz , 1H) , 9 .52 (s, 1H) , 12 .53 (b r s, 1H) . LC/M S: co ndition 1, ret ention time = 2.65 mi n LC/M S(ES I+) m/z; 324 [M+H]+ LC/M S(ES I ) m/z; 322 [M-Hl Ή -NMR (DMSO-d ) : 1.64- 1.82 (m, 4 H) , 1.87-1 .95 (m, 2 H), 2.00-2.08 (m, 2H) , 2.26-2.37 (m, 1H) , 2 .66 (t , J = 6 .6 Hz, 2H) , 3 .13-3.24 (m, 1H) , 3.26-3.32 ( , 2H) , 6 .84-6 .87 ( , 1H) , 7 .50 (t , J = 3.3 Hz, 1H) , 8 .19 (t, J = 356 5.6 Hz , 1H) , 9 .52 (s, 1H), 12.53 (b r s , 1H) . LC/M S: co ndition 1, retention time = 2.65 mi n LC/M S(ES I+) m/z; 338 [M+H]+ LC/M S(ES I ) m/z; 336 [- LC/M S: co ndition 1, retention time = 2 .90 mi n 35 7 LC/M S(ES I+) m/z; 364 [M+H]+ LC/M S(ES I ) m/z ; 362 [M-H] LC/M S: co ndition 1, retenti on time = 2.47 mi n 358 LC/M S(ES I+) m/z; 355 [M+H]+ LC/M S(ES I ) m/z ; 35 3 [M-H] 'H-N MR (DMSO- ) : 0 .39 (d d , J = 4.3 , 2.6 Hz, 2 H) , 0.61 (dd , J = 6.9 , 2.3 Hz, 2H) , 1.6 1- 1.78 (m, 4H) , 1.8 0- 1.89 ( , 2H) , 1. 98-2.07 (m, 2H) , 2.16-2. 28 ( , 1H) , 2 .60-2 .68 ( , 1H) , 3 .11-3.22 ( , 1H) , 6.84 (dd , = 3 .3, 2 .0 Hz , 1H) , 7 .50 (t, J = 3 .0 Hz, 1H) , 7 .83 (d , J = 35 9 4.3 Hz, 1H) , 9.52 (s, 1H) , 12 .53 (b r s , 1H) . LC/M S: condition 1, retenti on time = 2.92 mi n LC/M S(ES I+) m/z; 325 [M+H]+ LC/M S(ES I ) m/z ; 323 [M-H] Ή -NMR (DMSO-cfe) : 1.62-1 .80 (m, 4 H) , 1.83-1 .92 (m, 2 H), 1.9 9-2.07 (m, 2H) , 2.26-2.37 (m, 1H) , 3 .10-3 .19 (m, 1H) , 3 .32-3 .44 (m, 4H) , 4.65 (t, J = 5.6 Hz, 1H) , 6.8 3-6.87 (m, 1H) , 7 .48-7 .52 ( , 360 1H) , 7 .76 (t , J = 5 .9 Hz, 1H) , 9.52 (s , 1H) , 12.53 (br s , 1H) . LC/M S: co ndition 1, retenti on time = 2.34 mi n LC/M S(ES I+) m/z; 329 [M+H]+ LC/M S(ES I ) m/z ; 327 [M-H] TABLE 138 Ex Data H-N MR (DMSO- ) : 1.55- 1.70 (m, 2H) , 1.76- 1.87 (m, 4H) , 1.97-2. 06 (m, 2H) , 2 .32-2 .46 (m, 1H) , 3 .12-3. 23 (m, 1H) , 3.58 ( d , J = 10.2 , 3 .6 Hz, 1H) , 3.89 -3.96 ( , 1H) , 3 .99-4 .07 (m, 1H) , 4.41 -4. 49 (m, 1H) , 5.68-5.73 ( , 36 1 1H) , 6.88 (dd , J = 3.3 , 2 .0 Hz, 2H), 7 .49 (t, J = 3 .0 Hz, 1H) , 9.51 (s, 1H) , 12 .52 (br s , 1H) . LC/MS : condition 1, retention time = 1.79 in LC/M S(ESI +) m/z; 34 1 [M-H] + LC/M S (ES ) m/z; 339 [M- H] ' H-NMR (DMSO- ) : 1.59- 1.86 ( , 6H) , 1.98-2.06 (m, 3H) , 2 .19-2 .30 (m , 2H), 2 .83 (t, J = 7 .3 Hz, 2H) , 3 .15-3.25 (m, 1H) , 6.83-6. 86 (m , 1H) , 7 .43 (d , J = 7.9 Hz , 2H) , 7 .50 (t, J = 3 .0 Hz, 362 1H), 7.78 (d, J = 7 .6 Hz, 2H) , 7.87 (t , J = 5 .6 Hz, 1H) , 9.52 (s, 1H) , 12 .53 (br s, 1H) . LC/M S: condition 1, retention tim e = 3.40 min LC/M S(ESI +) m/z; 4 14 [M+H] + LC/M S(ESI ) m/z; 4 12 [M- Hl H-NMR (DMSO- ) : 1.56- 1.70 (m, 2H) , 1.73- 1.9 1 (m, 4H) , 1.97-2. 06 (m, 2H), 2 .33-2 .44 (m, 1H), 3 .13-3.25 (m, 1H) , 3.74-3. 86 (m, 1H) , 3 .97-4.05 (m, 1H) , 4 .11-4.20 (m, 1H) , 4.4 1-4.56 (m, 2H) , 363 6 .89 (dd , J = 3 .3 , 2.0 Hz, 1H) , 7 .49 (t, J = 2 .6 Hz, 1H) , 9.5 1 (s, 1H) , 12.52 (br s , 1H). LC/M S: condition 1, retention time = 2.88 min LC/MS (ESI +) m/z; 350 [M+H] + LC/M S(ESI ) m/z; 348 [M- Hl 1H-NMR (CDCI 3) : 1.30- 1.40 (m, 2H) , 1.81-2. 02 (m, 2H) , 2.05-2 .25 (m, 5H) , 3 .10 (d, J = 6.0 Hz, 2H) , 3 .12-3.2 1 (m, 1H) , 6.76 (dd , J = 3 .6 , 2 . 1 Hz, 1H) , 7.29 (t, J = 3.0 Hz, 1H) , 7 .55-7. 73 (m, 3H) , 364 7.91-7. 99 (m, 2H) , 9 .00 (br s , 1H) , 9.2 1 (s, 1H) . LC/M S: condition 3, retention time = 2 .00 min LC/M S(ESI +) m/z; 396 [M+H] + LC/M S(ESI ) m/z; 394 [M- H] 1H-N MR ( C D C I3) : 1.3 1- 1.56 ( , 2H), 1.86-2. 02 (m, 2H) , 2 .06-2 .24 (m, 5H) , 3.09 (d, J = 6.0 Hz, 2H), 3.11-3.22 (m, 1H) , 6.76 (dd , J = 6 .0 , 2 .4 Hz, 1H) , 7.2 2-7. 3 1 (m, 3H) , 7 .93-8.00 (m, 2H) , 9. 13 (br s , 365 1H) , 9.2 1 (s, 1H) . LC/M S: condition 3, retention tim e = 2 .06 min LC/M S(ESI +) m/z; 4 14 [M+H] + LC/M S(ESI ) m/z; 4 12 [M-H] H-N MR (D MSO- ) : 0.96- 1.07 (m, 4H) , 1.3 1- 1.5 1 (m , 2H) , 1.70-1 .9 1 ( , 2H), 1.95-2 .18 ( , 4H) , 2 .69-2 .84 (m, 1H) , 3 .15 (d, J = 5 .7 Hz, 2H) , 3 .65 (s, 2H), 6 .8 1 (dd , = 3.3 , 1.8 Hz, 1H), 7 .49 (t, 366 J = 2 .7 Hz, 1H) , 9.5 1 (s , 1H) , 12.52 (br s , 1H) . LC/M S: condition 3, retention tim e = 1.5 1 min LC/M S(ESI +) m/z; 360 [M+H] + LC/M S(ESI ) m/z; 358 [M-H] TABLE 139 Ex Data H-NMR ( C D C I3) : 1.20- 1.38 ( , 2H), 1.58-1 .67 (m, 1H) , 1.87-2.05 ( , 2H) , 2 .06-2.2 1 (m, 4H) , 3.09-3. 19 (m, 1H) , 3 .22 (d , J = 6.0 Hz , 2H), 6.78 (dd , J = 3 .0 , 1.8 367 Hz, 1H), 7.29 (t, J = 3 .0 Hz, 1H) , 9 .11 (br s , 1H) , 9.22 (s , 1H). LC/M S: condition 3 , retention tim e = 2 .42 min LC/MS (ESI +) m/z; 382 [M+H] + H-NMR ( C D C I3) : 1.5 1- 1.56 (m, 2H), 1.92-2. 12 (m, 2H) , 2 .13-2 .32 (m, 4H), 2.33-2 .5 1 (m, 1H) , 3 . 11-3. 20 ( , 1H) , 3 .2 1 (d , J = 6.6 Hz , 2H) , 6 .77 (dd , J = 6.0 , 2 .1 Hz, 1H), 7 .30 (t, J = 6 .0 Hz, 1H) , 9 .11 368 (br s , 1H) , 9.22 (s , 1H) . LC/M S: condition 3 , retention time = 2 .16 min LC/M S(ESI +) m/z; 388 [M+H] + LC/MS (ESI ) m/z; 386 [M- Hl H-NMR ( C D C I 3) : 1.20- 1.38 (m , 2H) , 1.70-1 .85 (m, 1H) , 1.85-2 .08 (m, 4H), 2.11-2. 22 (m, 2H), 3 . 10-3. 22 (m, 1H) , 3.26 (d, J = 6.6 Hz , 2H) , 6 .78 (dd , J = 3 .3 , 2 .4 Hz, 1H) , 7 .29 (t, J = 2 .7 Hz, 1H), 9.14 369 (br s , 1H) , 9.22 (s , 1H). LC/M S: condition 3 , retention time = 2 .09 min LC/M S(ESI +) m/z; 297 [M+H] + LC/MS (ESI ) m/z; 295 [-  ' H-NMR (DMSO- ) : 1.22- 1.40 ( , 2H) , 1.47 (s, 6H) , 1.64- 1.83 (m, 3H) , 1.9 1-2 .09 (m, 3H) , 2 .41 -2.57 (m, 1H) , 3.2 1-3.36 ( , 1H) , 3 .30 (br s , 1H), 4 .26 (d, J = 6 .9 Hz, 1H), 5.07 (s, 1H), 6 .85-6. 90 370 (m, 1H) , 7.42-7.52 (m, 1H) , 7.89 (s, 1H) , 9.52 (s, 1H) , 12 .53 (s, 1H) . LC/M S: condition 3 , retention time = 1.53 min LC/MS (ESI +) m/z; 38 1 [M+H] + LC/M S(ESI ) m/z; 379 [M-Hl ' H-NMR (DMSO- ) : 1.06- 1.24 (m, 2H) , 1.29- 1.45 (m, 1H), 1.66-1 .84 (m, 2H) , 1.87-2 .07 (m, 4H) , 2 .40-2 .54 (m, 2H) , 3.05-3. 20 371 ( , 1H) , 3.30 (br s, 1H) , 6 .79 (d, J = 3 .3 Hz, 1H) , 7.48 (d , J = 3 .3 Hz , 1H) , 9 .50 (s, 1H). LC/M S: condition 3 , retention time = 0 .99 min LC/M S(ESI +) m/z; 27 1 [M+H] + H-NMR (DMSO- ) : 1.12- 1.3 1 (m, 2H) , 1.52- 1.63 (m, 1H) , 1.64-1 .82 (m, 2H), 1.82-2.07 (m, 4H) , 3 .04 (t, J = 6 .6 Hz, 2H) , 3 .08-3.20 (m, 1H) , 3 .65 (s, 2H) , 6 .80 (dd , J = 3 .0 , 1.8 Hz , 1H), 7 .48 372 (t, J = 3.0 Hz, 1H), 8. 19-8 .28 (m, 1H), 9 .51 (s, 1H), 12.5 1 (br s , 1H) . LC/M S: condition 3 , retention tim e = 1.5 1 min LC/M S(ESI +) m/z; 338 [M+H] + LC/MS(ESI ) m/z; 336 [M- H] -NMR (DMSO- ) : 1.12- 1.32 (m, 2H) , 1.46- 1.64 ( , 1H) , 1.65-1 .82 (m, 2H) , 1.82-2 .07 ( , 4H), 3 .05 (t, J = 6 .0 Hz, 2H) , 3 .07-3. 20 (m, 1H), 3 .23 (d, J = .6 Hz, 1H) , 3.27-3 .35 ( , 1H) , 373 6 .79 (dd, J = 3 .0 , 1.8 Hz, 1H) , 7 .48 (t, J = 3 .0 Hz , 1H) , 8 . 8-8. 3 1 (m, 1H) , 9 .5 1 (s, H), 12 .5 1 (br s , 1H). LC/M S: condition 3 , retention time = 1.75 min LC/MS (ESI +) m/z; 38 1 [M+H] + LC/M S(ESI ) m/z; 379 [M- H] TABLE 140 Ex Data H-NMR (DMSO- c ) : 1.85-2.02 ( , 4H) , 2 .13-2.30 (m, 2H), 2.36 (s, 3H) , 2.8 6-2 .99 ( , 2H), 3 .10-3. 24 (m, 1H) , 3.67 (s, 2H) , 5.09 (q, J = 9 .0 Hz, 2 H) , 6.81 (d , J = 3.3 Hz, 1H) , 7 .49 (d, J = 3 .3 Hz, 1H) , 374 9 .52 (s, 1H) , 12 .54 (br s , 1H) . LC/M S: condition 3, retention tim e = 1.50 min LC/M S(ESI +) m/z; 381 [M+H] + LC/MS (ES ) m/z; 379 [M- H] H-NMR (DMSO- ) : 1.86-2 .04 (m, 4H) , 2 .16-2 .32 (m, 2H) , 2 .62 (t, J = 7.5 Hz, 2H), 2 .89 (t, J = 7.5 Hz, 2H), 3 .0 1-3. 12 ( , 2H), 3 .12-3. 24 (m, 1H), 6.76 (d, J = 3 .3 Hz, 1H) , 7.47 (d, J = 3.3 Hz, 1H) , 7 .49 (d, J = 7.8 Hz, 2H) , 375 7.76 (d , J = 7 .8 Hz, 2H), 9.52 (s, 1H) , 12.53 (br s, 1H) . LC/M S: condition 3 , retention time = 1.38 min LC/M S(ESI +) m/z; 372 [M+H] + LC/MS (ESI ) m/z; 370 [M- H] Ή -NMR ( C D C I3) : 2 .19-2.28 (m, 4 H) , 3 .14-3.23 (m, 2H) , 3.46-3.53 (m, 1H) , 4 .06 (d, J = 12.6 Hz, 2H) , 6.67 (dd , J = 3.3, 2 .4 Hz, 1H) , 6 .96 (d, J = 9.0 Hz, 2 H) , 7.53 (d, J = 9.0 Hz , 2H) , 9 .06 (br s, 1H) , 376 9 .24 (s, 1H). LC/M S: condition 3, retention time = 2 .07 min LC/M S(ESI +) m/z; 344 [M+H] + LC/M S(ESI ' ) m/z; 342 [M- H] Ή -NMR (DMSO- ) : 1.90-2 .08 (m, 4H) , 2 .11-2 .30 (m, 2H), 2 .70-2 .76 (m, 1H), 2 .87-3. 0 1 (m, 2H), 3.62 (s, 2H), 7 .56 (d , J = 8 .3 Hz, 2H) , 7 .66 (s, 1H) , 7 .80 (d, J = 3 .3 Hz, 2H) , 9.5 1 (s, 1H) , 12.5 1 377 (br s, 1H) . LC/M S: condition 3 , retention tim e = 1.45 min LC/M S(ESI +) m/z; 392 , 394 [M+H] + LC/M S(ESI ) m/z; 390, 392 [M- H] H-N MR ( C D C I 3) : 1.56 ( , 2H) , 1.94-2.07 (m, 8H) , 2.20 -2.33 ( , 6H), 3 .0 1-3. 26 (m, 7H) , 3.4 1 (m, 1H) , 4.26 (d, J = 5.4 Hz, 1H), 4 .34 (d, J = 5.4 Hz, 1H), 4.44 (m, 2H) , 6.77 (m, 1H), 6 .80 (m, 1H) , 378 7 .22-7. 32 (m, 10H), 9 .22 (s, 2H) , 10.04 (br s , 2H) . LC/M S: condition 1, retention time = 0 .99, 1.25 mi n (cis/trans mixtu re) LC/M S(ESI +) m/z; 389 [M+H] + LC/M S(ESI ) m/z; 387 [M-H] H-NMR ( C D C I3) : 1.57 (m, 2H) , 1.94-2.07 (m, 8H) , 2 .19-2 .32 (m, 6H) , 3.0 1-3. 22 (m, 7H), 3.4 1 (m, 1H) , 4.27 (d, J = 5.4 Hz, 1H) , 4.34 (d, J = 5.4 Hz, 1H), 4.44 (m, 2H) , 6.76 (m, 1H), 6 .80 (m, 1H), 379 7 .22-7. 30 (m, 10H), 9 .22 (s, 2H), 10 .28 (br s , 2H) . LC/M S: condition 1, retention time = 0 .87, 1.03 mi n (cis/trans mixtu re) LC/M S(ESI +) m/z; 389 [M+H] + LC/M S(ESI ) m/z; 387 [M- H] TABLE 141 Ex Data H-NMR (DMSO- ) : 1.58 (m, 6H) , 1.75- 1.84 ( , 12H) , 2 .02 (m, 4H), 2 . 17 (m, 2H) , 2.60 ( , 12H) , 2.75 ( , 3H) , 2 .82 (m, 12H) , 3 . 17 ( , 2H), 3 .5 1 ( , 1H) , 6.82 (m, 1H) , 6.88 ( , 2H) , 7.48 (m, 3H) , 380 9.50 (s, 2H) , 9 .52 (s, 1H) . LC/M S: condition 1, retention time = 2 .75 min LC/M S(ESI +) m/z; 363 [M+H] + LC/M S(ESI ) m/z; 361 [M-H] -NMR (DMSO- ) : 1.76- 1.96 (m, 6H) , 2 .10-2.23 (m, 2H) , 3.30-3.40 (m, 1H), 3.49-3.57 (m, 1H) , 5.57 (d, J = 6.9 Hz, 1H) , 6 .6 1-6. 68 ( , 2H), 6.86-6. 94 (38 1 m, 3H), 7.50 (t, J = 2 .6 Hz, 1H), 9.53 a (s, 1H) , 12 .53 (br s , 1H) . LC/M S: condition 1, retention tim e = 3 .22 min LC/M S(ESI +) m/z; 35 1 [M+H] + LC/M S(ESI ) m/z; 349 [M- H] H-NMR (DMSO- ) : 1.4 1 (qd, J = 12 .9, 3.6 Hz, 2H) , 1.84-2. 19 (m, 6H), 3.20 (tt, J = 11.9, 3.6 Hz, 1H), 3.31 -3.39 (m, 1H) , 5 .37 (d , 38 1 J = 8.3 Hz, 1H) , 6.60 -6.66 (m, 2H) , 6 .86-6 .95 (m, 3H), 7 .50 (d, J = b 3.3 Hz, 1H) , 9.53 (s, 1H) , 12.54 (br s, 1H) . LC/M S: condition 1, retention tim e = 2 .82 min LC/M S(ESI +) m/z; 351 [M+H] + LC/M S(ESI ) m/z; 349 [M- H] 382 LC/M S: condition 3 , retention tim e = 1.5 1 min LC/M S(ESI +) m/z; 392, 399 [M+H] + a LC/M S(ESI ) m/z; 390, 397 [M- H] 1H-NMR (CDCI 3) : 1.26- 1.46 (m, 2 H) , 1.87-2.05 (m, 2H) , 2 .08-2 .23 (m, 4H) , 2.76-2. 91 (m, 1H) , 3 .10-3.24 (m, 1H) , 3.44 (d, J = 12 .5 Hz, 382 1H), 3 .48 (d , J = 12.5 Hz, 1H) , 6.76 (dd , J = 3.3, 1.8 Hz, 1H) , 7.29 (t, J - 3.3 Hz, 1H), 9 .08 (br s , 1H) , 9.2 1 (s , 1H) . b LC/M S: condition 3 , retention time = 1.28 min LC/M S(ESI +) m/z; 399 [M+H] + LC/M S(ESI ) m/z; 397 [M- H] H-NMR (DMSO- d ) : 1.60- 1.75 (m, 4H) , 1.77- 1.88 (m, 2H), 2 . 12-2. 25 (m, 1H) , 2 .25-2. 37 (m, 1H) , 2 .85-2 .92 (m, 1H) , 3.20-3.40 383 (m, 3H), 6 .98 (dd, J = 3 .3 , 2.0 Hz, H), 7.45 (t, J = 2.6 Hz, H) , a 9.52 (s, 1H) , 12 .5 1 (br s , 1H) . LC/M S: condition 1, retention time = 2 .90 min LC/MS (ESI +) m/z; 389 [M+H] + LC/M S(ESI ) m/z; 387 [M- H] Ή -NMR (DMSO- ) : 1.23- 1.39 (m, 2H) , 1.70- 1.86 ( , 2H) , 1.96-2. 09 (m, 4H) , 2 .17-2 .28 (m, 1H) , 2 .54-2. 65 (m, 1H) , 3.14 (tt , J = 12.2 , 3.0 Hz, 1H) , 3.33 -3.4 5 (m, 2H), 6 .82 (d , J = 2 . 6 Hz , 1H) , 383 7 .49 (d, J = 2 .6 Hz, 1H) , 9.52 (s, 1H) , 12 .53 (br s , 1H) . b LC/MS : condition 1, retention time = 1.84 min LC/MS (ESI +) m/z; 389 [M+H] + LC/M S(ESI ) m/z; 387 [M- H] TABLE 142 Ex Data -N R (DMSO-d ) : 1.58- 1.86 (m, 6H) , 2 .09-2 .30 (m, 2 H), 2.4 1-2.54 ( , 1H) , 2.6 9-2.8 1 (m, 1H) , 3 .25 (s , 2H) , 3.88-4.05 (m, 2H) , 6 .94-6 .98 (m , 1H) , 7 .44 (t, J = 384 3 .0 Hz , 1H) , 8 .32-8 .45 (m , 1H) , a 9.5 1 (s , 1H) , 12 .49 (s, 1H) . LC/M S: co ndition 3 , retenti on time = 1.35 mi n LC/M S(ES I+) m/z; 396 [M+H]+ LC/M S(ES I ) m/z ; 394 [M-H] 'H-NMR (DMSO-cf ) : 1.25-1 .41 (m, 2H) , 1.67 - 1 .84 ( , 2 H), 1.94-2.05 (m, 4H) , 2.44-2.57 ( , 1H) , 3 .06-3 .20 ( , 1H) , 3 .26 (s , 384 2H) , 3 .87-4 .02 (m, 2H) , 6 .78 (dd, J = 3.0 , 1.5 Hz, 1H) , 7 .48 (t, J = b 3.0 Hz, 1H) , 8.41 (br s , 1H) , 9.50 (s , 1H) , 12.5 1 (s, 1H) . LC/M S: co ndition 3 , retenti on time = 1.22 mi n LC/M S(ES I+) m/z; 396 [M+H]+ LC/M S(ES I ) m/z; 394 [M-Hl Ή -N R (CD 3OD) : 1.35 (m, 2H) , 1.84 (m, 2H) , 2.07 (m, 4H) , 2.58 (tt, J = 11.4 , 3 .3 Hz, 1H) , 3 .16 (tt, J = 12.3 , 3 .3 Hz, 1H) , 3 .36 (d , J = 13.5 Hz, 1H) , 3 .46 (d, J = 12.9 Hz , 1H) , 6 .77 (d, J = 3.3 Hz , 1H) , 385 7.38 (d , J = 3.3 Hz, 1H) , 7.5 0 (d d , J = 7 .5 , 4 .2 Hz , 1H) , 8 .10 (d, J = b 8.1 Hz , 1H), 8 .55 (dd , J = 5 .1, 1.2 Hz, 1H) , 8.8 1 (d, J = 1.2 Hz, 1H) , 9.27 (s , 1H) . LC/M S: co ndition 1, retenti on time = 0.39 min LC/M S(ESI +) m/z; 446 [M+H]+ LC/M S(ES I ) m/z ; 444 [M-Hl Ή -NMR (CD 3OD) : 1.43 ( , 2H) , 1.84 (m, 2H) , 2.09 (m, 4H) , 2.49 (s, 3H) , 2.69 (tt, J = 11.1, 3.6 Hz, 1H) , 3 .17 (tt, J = 12 .3, 3.3 Hz , 1H) , 3.38 (d, J = 13 .2 Hz, 1H) , 3.45 (d, J = 2.9 Hz , 1H) , 6.77 (d , J 386 = 3.3 Hz, 1H) , 7.3 1 (d, J = 8 .7 Hz, 2H) , 7 .38 (d , J = 3.3 Hz , 1H) , b 7.5 7 (d, J = 8.7 Hz, 2H) , 9.27 (s , 1H) . LC/M S: co ndition 1, retention time = 2.92 mi n LC/M S(ES I+) m/z; 491 [M+H]+ LC/M S(ES I ) m/z ; 48 9 [M-Hl Ή -NMR (CD3OD) : 1.40 (m, 2H) , 1.85 (m, 2H) , 2 .10 (m, 4H) , 2.65 (tt, J = 11.4 , 3 .6 Hz, 1H) , 3 .17 (tt, J = 12.3 , 3.6 Hz, 1H) , 3 .35 (d , J = 13 .5 Hz , 1H) , 3.42 (d, J = 13.2 Hz, 1H) , 3.93 (s , 3H) , 6.77 (d, J = 387 3.3 Hz, 1H) , 6 .84 (d, J = 8.7 Hz , 1H) , 7 .38 (d, J = 3 .3 Hz , 1H) , 7.89 b (s, 1H) , 8.38 (d, J = 2 .4 Hz, 1H) , 9.27 (s , 1H) . LC/M S: co ndition 1, retenti on time = 2.49 mi n LC/M S(ES I+) m/z; 476 [M+H]+ LC/M S(ESI ) m/z ; 474 [- H-N MR (CD3OD) : 1.42 (m, 2H) , 1.82 (m, 2H) , 2 .10 (m, 4H) , 2.68 (tt, J = 11.4 , 3.6 , 1H) , 3.17 (tt , J = 12 .6, 3.3 Hz, 1H) , 3 .37 (d , J = 13 .2 Hz, 1H) , 3 .43 (d, 13 .2 Hz, 1H) , 3.81 (s , 3H) , 6.77 (d, J = 3 .3 388 Hz, 1H) , 6.97 (d , J = 9.0 Hz, 2H) , 7.38 (d , J = 3.3 Hz, 1H) , 7.56 (d, b J = 8 .4 Hz, 2H) , 9.27 (s , 1H) . LC/M S: co ndition 1, retenti on time = 2.75 mi n LC/M S(ES I+) m/z; 475 [M+H]+ LC/M S(ES I ) m/z ; 473 [M-H] TABLE 43 Ex Data H-NMR (CDCI 3) : 0.87 (m, 2H) , 1.34 (m, 2 H) , 1.73 (m, 2 H) , 1.96 (m, 2H) , 2 .15 (m, 4H) , 2 .68-2 .79 ( , 3H) , 3 .18 (m, 1H) , 6.77 (d, J = 3.3 Hz, 1H) , 6.90-7.04 (m, 389 4H) , 7.2 8 (d, J = 3.3 Hz, 1H) , 9. 16 (br s , b 1H) , 9 .2 1 (s , 1H) . LC/M S: co ndition 1, ret enti on time = 2.75 i n LC/M S(ESI +) m/z; 405 [M+H]+ LC/M S(ES I ) m/z ; 403 [M-H] Ή -NMR ( C D C I3) : 1.33 (m, 2H) , 1.92 (m, 2 H) , 2 .17 (m, 4 H) , 2.68 (tt, J = 11. 1, 3 .3 , 1H), 3.08 (d, J = 12 . 6Hz, 1H) , 3. 16 (tt, J = 12 .3, 3.9 Hz, 1H) , 3.58 (d, J = 12 Hz , 1H) , 3 .89 (s, 3 H), 3.60 (s, 3H) , 390 6.73 (d, J = 3.0 Hz, 1H) , 6.88 (d , J = 8 .7 Hz, 1H) , 7.07 (d, J = 8 .4 b Hz, 1H), 7.2 1 (m, 1H) , 7.29 (m, 1H) , 9.2 1 (s , 1H) , 9 .41 (br s , 1H) . LC/M S: co ndition 1, retention time = 2.67 mi n LC/M S(ESI +) m/z; 505 [M+H]+ LC/M S(ES I ) m/z ; 503 [M-H] Ή -NMR ( C D 3O D ) : 1.40 (m, 2H) , 1.90 (m, 2H) , 2 .14 (m, 4H) , 2.7 1 (m, 1H) , 2.94 (s , 4H) , 3.29 (m, 1H) , 6 .82 (d, J = 3 .3 Hz, 1H) , 39 1 7.40(d, J = 3 .3 Hz, 1H) , 7.46 (d , J = 8 . 1 Hz, 2H) , 7.67 (d, J = 8 .4 b Hz, 2 H) 9.30 (s, 1H) . LC/M S: condition 1, retention time = 1.62 mi n LC/M S(ESI +) m/z; 386 [M+H]+ LC/M S(ES I ) m/z; 384 [- 'H- MR ( C D C I3) : 0.40 (m, 2H) , 0 .50 (m, 2 H) , 1.37 (m, 2 H) , 1.98 (m, 2H) , 2 .14-2. 26(m , 5H) , 2. 82 (m, 1H) , 3 . 18 (tt , J = 12.3 , 3.3 Hz, 392 1H) , 3 .71 , 6.78 (d, J = 3.3 Hz , 1H) , 7 .30 (d, J = 3.3 Hz , 1H) , 9.23 b (s, 1H) . LC/M S: co ndition 1, retenti on time = 3.55 mi n LC/MS(ESI +) m/z; 424 [M+ H]+ LC/M S(ESI ) m/z ; 422 [- 'H-N MR ( C D C I3) : 1.42 (m, 2H) , 1.95-2. 20 (m, 6H) , 2 .92 (m , 1H) , 3.2 1 (tt, J = 12 .6, 3 .6 Hz , 1H) , 3 .71 (d , J = 7 .8 Hz , 2H) , 6 .78 (d, J = 393 3.3 Hz, 1H) , 7.31 (d, J = 3.3 Hz , 1H) , 9.23 (s, 1H) . b LC/M S: co ndition 1, retenti on time = 0.35 mi n LC/M S(ESI +) m/z; 296 [M+H]+ LC/M S(ES I ) m/z ; 294 [M-H Ή -NMR ( C D C I3) : 1.37 (m, 2H) , 1.96 ( , 2 H) , 2 .16 (m, 4 H) , 2.56 (t, J = 6.6 Hz , 2 H) , 2.71 (tt, J = 11.7 , 3 .6 Hz, 1H) , 3.04 (t, J = 6.6 394 Hz, 2H), 3 .18 (tt, J = 11.7, 3 .9 Hz, 1H) , 6 .77 (dd, J = 3.3, 2 . 1 Hz, b 1H) , 7 .30 (t , J = 2 . 7 Hz, 1H) , 9.22 (s , 1H) , 9 .36 (br s , 1H) . LC/M S: condition 1, retenti on time = 0.35 mi n LC/M S(ESI +) m/z; 3 10 [M+H]+ LC/M S(ES I ) m/z ; 30 8 [- TABLE 144 Ex Data H-NMR (CDCI 3) : 1.38 (m, 2H) , 1.96 ( , 2H) , 2 . 17 (m, 4H), 2 .78 (tt , J = 11. 1, 3 .3 Hz, 1H) , 3 . 18 (tt , J = 12.4, 3 .3 Hz , 1H) , 3 .29 (q , J = 9.6 Hz , 2H) , 6 .76 (dd , J = 395 3 .3 , 2 . 1 Hz, H), 7 .30 (t , J = 2 .7 Hz, 1H) , 9 .22 (s, 1H) , 9.43 (br s , 1H) . b LC/M S: condition 1, retention tim e = 0 .37 min LC/M S(ESI +) m/z; 339 [M+H] + LC/M S(ESI ) m/z; 337 [M- H] H-NMR (CDCI 3) : 0 .16 (m, 2H) , 0.5 1 (m, 2H) , 1.0 1 (m, 1H) , 1.42 (m, 2H) , 1.98 ( , 2H) , 2 .17 (m, 4H) , 2.60 (d , J = 6.9 Hz, 2H) , 2 .72 396 (tt , J = 11. 1, 3 .9 Hz, 1H) , 3 . 19 (tt , J = 12.3, 3 .3 Hz, 1H), 6 .77 (d , J b = 3 .3 Hz , 1H) , 7 .3 1 (d, J = 3 .3 Hz, 1H) , 9.23 (s , 1H) . LC/M S: condition 1, retention tim e = 0 .37 min LC/MS (ESI +) m/z; 3 11 [M+H] + LC/M S(ESI ) m/z; 309 [M-H] H-NMR (CD3OD) : 1.5 1 (m, 2H), 1.95 (m, 2H), 2 . 18 (m, 4H) , 2 .39 (s, 6H) , 2 .42 (m, 1H), 3 .15 (tt, J = 11.7 , 3.9 Hz, 1H) , 6.79 (d , J = 397 3 .3 Hz, 1H) , 7 .29 (d, J = 3 .3 Hz, 1H) , 9.22 (s, 1H) . b LC/M S: condition 1, retention tim e = 0 .35 min LC/M S(ESI +) m/z; 285 [M+H] + LC/M S(ESI ) m/z; 283 [-  Ή -NMR (CDCI 3) : 1.33 (m, 2H) , 1.93 (m, 2H) , 2 . 15 (m, 4H) , 2 .5 1 (s, 3H) , 2.5 6 (m , 1H) , 3 . 18 (tt , J = 12.3, 3 .6 Hz, 1H) , 6 .78 (d , J = 398 3 .6 Hz, 1H) , 7 .28 (d , J = 3.3 Hz, 1H), 9.2 1 (s, 1H). b LC/M S: condition 1, retention tim e = 0 .35 min LC/M S(ESI +) m/z; 27 1 [M+H] + LC/M S(ESI ) m/z; 269 [M- H] H-NMR (CDCI 3) : 1.37 (m, 2H) , 1.97 (m, 2H) , 2 . 17 (m, 4H) , 2 .72 (tt, J = 11.4 , 3.6 Hz, 1H) , 3 .08 (td , J = 15 .3 , 4.5 Hz, 2H) , 3 .18 (tt, J 399 = 12 .3, 3.3 Hz, 1H) , 5.88 (m, 1H), 6 .77 (m, 1H) , 7 .3 1 (m, 1H) , 9.23 b (s, 1H) , 9.5 9 (b r s , 1H). LC/M S: condition 3 , retention tim e = 0 .81 min LC/M S(ESI +) m/z; 32 1 [M+H] + LC/MS (ESI ) m/z; 3 19 [M-H] Ή -NMR (CDCI 3) : 1.45 ( , 2H) , 1.96 ( , 2H) , 2 . 16 ( , 4H) , 2 .97 ( , 1H) , 3 . 18 (tt, J = 12.0, 3 .6 Hz, 1H), 3.79 (m, 1H) , 6 .77 (m, 1H), 400 7 .3 1 (m, 1H) , 9 . 17 (br s , 1H), 9.23 (s, 1H) . b LC/M S: condition 1, retention tim e = 4 .04 min LC/MS(ESI +) m/z; 407 [M+H] + LC/M S(ESI ) m/z; 405 [M- H] ' H-NMR (CD 3OD) : 1.7 1-2 .18 (m, 9H) , 3 .33-3.45 ( , 1H) , 3.67 (d , J = 6 .6 Hz, 2H), 6 .80 (d , J = 3 .3 Hz, 1H), 7 .39 (d , J = 3.3 Hz, 1H) , 40 1 9 .30 (s, 1H) . LC/MS : condition 3 , retention time = 1.53 min LC/M S(ESI +) m/z; 272 [M+H] + LC/M S(ESI ) m/z; 270 [M- H] TABLE 145 Ex Data -NMR (CDCI 3) : 1.76- 1.9 1 (m, 2 H) , 1.95-2 .06 (m, 4H) , 2.32-2.44 (m, 2H), 2 .54-2.64 (m, 1H) , 3.26-3.38 (m, 1H) , 6.78 (dd , J = 3.3, 1.8 Hz, H) , 7 .29 (t, J = 3 .0 Hz, 1H) , 9.19 (br s , 1H) , 9 .22 (s, 1H) , 402 9.84 (s, 1H) . LC/M S: condition 3, retention tim e = 1.7 1 min LC/M S(ESI +) m/z; 270 [M+H] + LC/M S(ESI ) m/z; 268 [M- H] -NMR (DMSO- ) : 1.56- 1.99 ( , 10H) , 2.39 (d , J = 6 .3 Hz, 2H) , 2 .65 (dd , J = 7 .4 , 6 .0 Hz, 2H) , 3 .50 (dd , J = 7 .4 , 6 .0 Hz, 2H), 4. 14 (dd, J = 9 .8 , 3.3 Hz, 2H) , 6.76 (d, J = 3 .3 403 Hz , 1H) , 7 .47 (d, J = 3.3 Hz, 1H) , 9.50 (s, 1H) , 12.50 (br s, 1H) . LC/M S: condition 1, retention time = 0 .94 min LC/M S(ESI +) m/z; 327 [+ H-N MR (DMSO- d ) : 1.47- 1.62 (m, 1H) , 1.63- 1.85 (m, 4H), 1.89-2 .07 (m, 3H) , 2 .24-2 .59 (m, 6H), 2 .65-2 .75 (m, 1H) , 3.22-3. 44 (m, 1H) , 4 .08-4. 29 (m, 1H) , 4.62 (d, J = 4.5 Hz , 1H) , 2.86-2.98 (m, 404 1H), 3 .29-3. 39 (m, 1H), 6.77 (d, J = 3.3 Hz, 1H) , 7.48 (d, J = 3 .3 Hz, 1H), 9 .5 1 (s, 1H) , 12 .5 1 (br s , 1H) . LC/M S: condition 3 , retention tim e = 0 .95 min LC/M S(ESI +) m/z; 34 1 [+ H-N MR ( C D C I3) : 1.59- 1.96 (m, 7 H) , 2.06-2.3 1 (m, 5H) , 2.42-2 .6 1 (m, 3H) , 2 .75 (d, J = 9.8 Hz, 1H) , 2.86-2 .98 (m, 1H) , 3.29-3.39 ( , 405 1H) , 4 .26-4. 37 (m, 1H) , 6 .77 (d , J = 3.3 Hz, 1H) , 7.28 (d, J = 3 .3 Hz, 1H) , 9.22 (s, 1H) , 9 .30 (br s , 1H) . LC/M S: condition 3 , retention time = 1.20 min LC/MS (ESI +) m/z; 34 1 [M+H] + ' H-NMR ( C D C I3) : 0 .3 1-0.49 (m, 4 H) , 1.54- 1.98 (m, 7H) , 2.09-2.42 (m, 3H) , 2 .78 (d , J = 6 .6 Hz, 2H) , 3 .36-3 .44 ( , 1H) , 6 .78 (d , J = 406 3.0 Hz, 1H), 7 .29 (d, J = 3 .0 Hz, 1H) , 9.23 (s, 1H) , 9.27 (br s, 1H) . LC/M S: condition 3 , retention tim e = 1.29 min LC/M S(ESI +) m/z; 3 11 [M+H] + H-NMR (DMSO- ) : 1.2 1- 1.38 (m, 2H) , 1.70- 1.83 (m , 4H) , 1.9 1-2. 07 (m, 3H), 3 .08-3. 19 ( , 1H) , 3 .33 (dd, J = 18.4, 7 .8 Hz , 2H), 4 . 11 (s, 1H) , 4.20-4. 27 (m, 3H) , 6 .79-6. 83 (m, 1H) , 7.49 (q, J 407 = 2 .5 Hz, 1H) , 9 .5 1 (s, 1H), 12 .52 (br s , 1H) . LC/M S: condition 1, retention tim e = 3 .60 min LC/M S(ESI +) m/z; 420 [M+H] + LC/M S(ESI ) m/z; 4 18 [M- H] H-N MR (DMSO- ) : 1.2 1- 1.36 (m, 2H) , 1.69- 1.90 (m , 5H) , 1.98-2. 07 (m, 2H), 3 .08-3. 19 (m, 1H), 3 .26-3. 34 (m, 2H) , 4.18 (s, 2H), 4.43 (s, 2H), 6 .78-6. 83 (m, 1H) , 7 .49-7. 52 (m, 1H) , 9.52 (s, 408 1H) , 12 .54 (br s, 1H). LC/MS : condition 1, retention tim e = 3 .09 min LC/M S(ESI +) m/z; 377 [M+H] + LC/MS(ESI ) m/z; 375 [M- H] TABLE 146 Ex Data H-NMR (DMSO- ) : 0.8 1-0.89 (m, 4H) , 1.17- 1.30 ( , 2H) , 1.70- 1.89 (m, 5H) , 1.98-2. 07 (m, 2H) , 2 .74-2. 8 1 (m, 1H) , 3 .10-3. 20 ( , 1H) , 3.25 (d , J = 7 .6 Hz, 2H) , 4 .16 (s, 2H) , 6.8 1-6.85 (m, 1H) , 409 7 .47-7. 52 (m, 1H), 9 .52 (s, 1H) , 12.53 (br s , 1H). LC/M S: condition 1, retention tim e = 3 .38 min LC/M S(ESI +) m/z; 378 [M+H] + LC/M S(ESr) m/z; 376 [M- H] LC/M S: condition 1, retention time = 3 .72 min 4 10 LC/M S(ESI +) m/z; 432 [M+H] + LC/M S(ESI ) m/z; 430 [M- H] ' H-N R (DMSO- ) : 1.13- 1.38 (m, 2H) , 1.70- 1.85 (m, 4H) , 1.89-2 .06 (m, 4H) , 3 .08-3. 2 1 (m, 1H), 3 .2 1-3. 32 (m, 1H) , 3 .38 (d, J = 7.3 Hz , 2H), 3 .76-3. 89 (m, 1H) , 4 .2 1-4. 32 (m, 1H) , 6.80-6.84 (m, 4 1 1 1H), 7 .47-7 .52 ( , 1H), 9.52 (s, 1H), 12 .53 (br s , 1H). LC/M S: condition 1, retention tim e = 3 .97 min LC/M S(ESI +) m/z; 463 [M+H] + LC/M S(ESI ) m/z; 461 [- Ή -NMR (DMSO- d ) : 1.22- 1.41 ( , 2H) , 1.69- 1.96 (m, 5H) , 1.98-2 .08 (m, 2H) , 3 . 10-3.22 ( , 1H) , 3 .37 (d , J = 7.3 Hz, 2H) , 3 .7 1-3. 86 ( , 2H) , 4 .44 (s, 2H) , 6 .79-6. 82 ( , 1H), 7.48-7. 53 (m, 4 12 1H) , 9 .53 (s, 1H) , 12 .54 (br s , 1H) . LC/MS : condition 1, retention tim e = 3 .54 min LC/M S(ESI +) m/z; 420 [M+H] + LC/MS (ESI ) m/z; 4 18 [M- H] H-NMR (CDCI 3) : 0 .15 (m, 2H) , 0.55 (m, 2H) , 0 .90 (m, 1H) , 1.48 (m, 2H) , 1.90-2. 04 (m, 4H) , 2 .18 (m, 2H) , 2 .6 1 (d, J = 6.0 Hz, 2H), 2 .97 (m, 1H) , 3 . 12 (m, 1H) , 3 .18 (q , J = 9.6 Hz, 2H) , 6 .79 (d, J = 4 13 3 .3 Hz, 1H) , 7 .30 (m, 1H) , 9.22 (s, 1H) , 9 .29 ( br s , 1H) . LC/M S: condition 1, retention tim e = 3 .85 min LC/M S(ESI +) m/z; 393 [M+H] + LC/M S(ESI ) m/z; 39 1 [M-H] H-NMR (DMSO- ) : 0 .12-0. 19 (m, 2H) , 0.48-0.55 (m, 2H) , 0 .78-0. 90 (m, 1H) , 1.08- 1.25 ( , 2H) , 1.69-2 .05 (m, 6H) , 2 .33-2. 39 (m, 5H) , 3 .09-3.2 1 (m, 1H) , 3.87 (s, 2H) , 6 .83-6. 86 (m, 1H) , 7 .49 (t , 4 14 J = 3.0 Hz, 1H) , 9.5 1 (s , 1H) , 12.52 (br s , 1H) . LC/M S: condition 1, retention tim e = 3 .74 min LC/MS (ESI +) m/z; 364 [M+H] + LC/M S(ESI ) m/z; 362 [M- H] ' H-N MR (DMSO- ) : 0 .10-0. 16 (m, 2H) , 0.44-0.52 (m, 2H) , 0 .83-0. 94 (m, 1H), 1.05- 1.2 1 ( , 2H), 1.54-1 .68 (m, 1H) , 1.68-1 .84 (m, 2H) , 1.92-2. 06 (m, 4H) , 2.44-2.58 ( , 4H) , 3.09-3.2 1 (m, 1H) , 3 .25-3. 39 (m, 2H), 6 .80-6. 4 5 84 ( , 1H) , 7.47-7. 5 1 (m, 1H) , 9.5 1 (s, 1H), 12 .52 (br s , 1H). LC/M S: condition 1, retention time = 4 .45 min LC/MS(ESI +) m/z; 407 [M+H] + LC/M S(ESI ) m/z; 405 [M- H] TABLE 147 Ex Data H- MR (DMSO- ) : 1.16- 1.28 (m, 3H) , 1.67- 1.88 (m, 3H), 1.93-2.0 1 (m, 2H) , 2 .11-2. 19 (m, 2H) , 2.40 (d , J = 5.7 Hz, 2H) , 3.10 (tt, J = 11.9, 3 .7 Hz, 1H) , 6 .77-6. 80 (m, 1H) , 7.48 (t, J = 2 .9 Hz, 4 16 1H), 9 .50 (s, 1H) , 12 .50 ( br s , 1H). LC/M S: condition 1, retention time = 2 .75 in LC/MS (ESI +) m/z; 336 [M+H] + LC/M S(ESI ) m/z; 334 [M- H] LC/M S: condition 1, retention tim e = 3 .30 min 4 17 I LC/M S(ESI +) m/z; 375 [M+H] + LC/MS( ESI ) m/z; 373 [M- H] NMR (DMSO- ) : 1.39 (qd, J = 12 .6 , 3.0 Hz, 2H) , 1.72- 1.87 (m, 2H) , 1.97-2 .15 (m, 4H) , 2.7 1-2.80 ( , 1H) , 2 .79 (s , 6H) , 2 .99 (d, J = 6 .6 Hz , 2H) , 3 .15 (tt, J = 12.2 , 3.3 Hz, 1H) , 6.8 1 (dd , J = 3 .3 , 2.0 Hz, 1H) , 7 .50 (t, J = 3 .0 Hz, 1H) 4 18 , 9 .52 (s, 1H), 12 .54 (br s , 1H) . LC/M S: condition 1, retention tim e = 3.30 min LC/M S(ESI +) m/z; 363 [M+H] + LC/M S(ESI ) m/z; 36 1 [M- H] LC/M S: condition 1, retention time = 3.13 min 4 19 LC/M S(ESI +) m/z; 374 [M+H] + LC/MS (ESI ) m/z; 372 [M- H] LC/M S: condition 3 , retention tim e = 1.89 min 420 LC/M S(ESI +) m/z; 4 17 [M+H] + LC/M S(ESr) m/z; 4 15 [M- H] 'H-NMR (CDCI 3) : 1.07- 1.30 (m, 2H) , 1.80-2 .04 (m , 4H) , 2 .06-2. 19 (m, 2H) , 2.44 (d, J = 6.6 Hz, 2H) , 2.92-3.04 (m, 2H), 3.07-3. 19 (m, 1H), 3 .67-3. 78 (m, 2H) , 3 .76 (d, J = 8.3 Hz, 1H) , 3.82 (d , J = 8.3 42 1 I Hz , 1H) , 4.20-4. 32 (m, 1H) , 6 .75-6.80 (m, 1H) , 7.23-7.29 ( , 1H) , 9. 10 (br s , 1H) , 9 .20 (s, 1H). LC/M S: condition 3 , retention tim e = 1.52 min LC/M S(ESI +) m/z; 409 [M+H] + H-NMR ( C D C I3) : 1.12- 1.30 (m, 3 H) , 1.5 1 (s, 3H), 1.84-2. 18 (m, 7H) , 2.43 (d , J = 6.9 Hz, 2H) , 3.06 (d , J = 8.3 Hz, 2H) , 3 .09-3. 20 (m, 1H), 3 .35 (d , J = 8.3 Hz, 2H) , 6.75-6.8 1 (m, 1H) , 7 .22-7.29 (m, 1H) , 9 . 13 (br s, 1H) , 9.2 1 (s, 1H) . LC/M S: condition 3 , retention time = 1. 12 min LC/M S(ESI +) m/z; 34 1 [M+H] + H-N MR (DMSO- c ) : 1.08- 1.24 (m, 2H) , 1.35- 1.50 (m , 1H) , 1.65-1 .8 1 (m, 2H), 1.83-2 .0 1 (m, 4H) , 2 .00 (s, 6H), 2 .29 (d, J = 6 .6 Hz , 2H) , 2 .68-2. 75 (m, 3H) , 3 .11 (tt, J = 12 .6, 3 .6 Hz, 1H) , 423 3 .37-3.42 (m, 2H) , 6 .79 (d, J = 3 .3 Hz, 1H) , 7.47 (d, J = 3.3 Hz, 1H) , 9.49 (s, 1H), 12 .55 (br s , 1H) . LC/MS : condition 1, retention tim e = 0 .34 min LC/M S(ESI +) m/z; 354 [M+H] + LC/MS(ESI ) m/z; 352 [M- H] TABLE 48 Ex Data H-NMR (DMSO- ) : 0.94 (t , J = 7.3 Hz , 3H) , 1. 15 (qd , J = 12.6, 2 .6 Hz, 2H) , 1.36- 1.50 (m, 1H) , 1.73 (qd , = 12.6 , 2.6 Hz, 2H) , 1.84-2 .03 ( , 4H) , 1.98 (s, 3H) , 2 .20 (q, J = 7 .3 Hz , 2H), 2 .29 (d , J = 6 .6 Hz, 2H) , 2 .69 (t, J = 6 .9 Hz , 2H) , 2 .8 1-2. 92 ( , 1H) , 3. 11 (tt , 424 J = 11.6, 3 .3 Hz, 1H), 3 .43 (t, J = 6 .9 Hz , 2H), 6 .80 (d , J = 3.3 Hz, 1H) , 7 .48 (d , J = 3.3 Hz , 1H) , 9.5 1 (s, 1H) , 12 .53 (br s , 1H) . LC/M S: condition 1, retention time = 0 .34 min LC/M S(ESI +) m/z; 368 [ +H] + LC/M S(ESI ) m/z; 366 Ϊ -  H-N MR (DMSO- d ) : 1.05- 1.27 ( , 2H) , 1.27- 1.45 (m, 1H), 1.54-1 .82 ( , 2H), 1.83-2 .04 (m, 4H) , 2 .38 (d , J = 6.6 Hz, 1H) , 3 .03-3. 12 (m, 1H) , 3 . 13 (d, J = 9 .5 Hz , 2 H) , 3.55 (d, J = 9.5 Hz, 2H), 6 .80 (dd , J = 3.0, 2.1 425 Hz, 2H) , 6 .82 (s, 1H), 7.47 (t, J = 3.0 Hz , 1H) , 9 .50 (s, 1H), 12 .50 (s , 1H) . LC/M S: condition 3 , retention tim e = 1.32 min LC/M S(ESI +) m/z; 395 [M+H] + LC/M S(ESI ) m/z; 393 [M- H] LC/MS : condition 3 , retention tim e = 1.42 min 426 LC/M S(ESI +) m/z; 436 [M+H] + LC/MS (ESI ) m/z; 434 [-  H-N MR (DMSO- e) : 1.10- 1.30 (m, 2H) , 1.49- 1.64 (m, 1H) , 1.66- 1.84 (m, 2H), 1.86-2 .08 ( , 4H) , 2 . 82-2. 93 (m, 5H) , 3.06-3. 22 ( , 1H) , 6 .80 (dd , J = 3 .0 , 2 . 1 Hz, 1H), 7 .0 1 (t, J = 6 .3 Hz, 1H) , 427 7.48 (t, J = 3.0 Hz, 1H) , 9.51 (s, 1H), 12 .5 (s, 1H) . LC/M S: condition 3 , retention tim e = 1.57 min LC/MS (ESI +) m/z; 349 [M+H] + LC/M S(ESI ) m/z; 347 [M- H] Ή -NMR (DMSO- d ) : 1.09- 1.28 (m, 2H) , 1.40 (s, 9H) , 1.64- 1.85 (m, 2H) , 1.87-2. 07 (m, 5H) , 2 .39-2.57 (m, 2H) , 3.05-3.26 ( , 1H) , 428 3 .57 (brs, 2H) , 4.32 (d , J = 10.2Hz, 2H) , 4 .62 (d , J = 10.2 Hz, 2H) , 6 .93 (d, J = 3 .3 Hz, 1H) , 7.75 (d , J = 3.3 Hz , 1H), 9.62 (s, 1H) . LC/MS : condition 3 , retention tim e = 2 .09 min LC/M S(ESI +) m/z; 465 [M+H] + H-N MR (DMSO- c ) : 1.40- 1.59 (m, 2H) , 1.7 1-2. 10 (m , 6H) , 2 .26-2. 40 (m, 1H) , 3.09-3. 26 (m, 1H) , 6 .80-6. 87 (m, 1H) , 6.54 (d, J 429 = 6 .8 Hz , 0.2H) , 7 .3 1 (d , J = 4 .8 Hz , 0 .8H) , 9 .5 1 (s , 1H) , 10 .4 (s, 0 .8H) , 10.7 (s , 0.2H), 12 .5 1 (s, 1H) . LC/MS : condition 3 , retention tim e = 1.5 1 min LC/M S(ESI +) m/z; 27 1 [M+H] + 1H-N MR (CDCIg) : 1.76-2.06 (m, 4 H) , 2 .16-2.28 (m, 2H) , 2 .30-2 .4 1 (m, 2H) , 2 .58-2 .73 (m, 1H) , 3 .17-3.30 (m, 1H) , 6.75 (dd , J = 3 .3, 430 1.8 Hz, H) , 7 .3 1 (t, J = 3.3 Hz, 1H) , 9 . 15 (br s , H), 9 .22 ( s , 1H). LC/M S: condition 3 , retention tim e = 1.68 min LC/MS (ESI +) m/z; 267 [M+H] + LC/M S(ESI ) m/z; 265 [M- H] TABLE 149 Ex Data H-NMR (CDCI 3) : 1.48- 1.65 (m, 2 H) , 1.95-2 .13 ( , 4H) , 2 .19-2.33 ( , 2H) , 2 .85-3. 02 ( , 1H) , 3.15-3.29 (m, 1H) , 6.76 (dd , J = 3.3, 2 . 1 Hz, 1H) , 7.23 (d, J = 10 .4 Hz, 1H) , 7.3 1 (t , J = 3 .3 Hz, 1H) , 43 1 9 .20 (br s , 1H) , 9.23 (s, 1H) . LC/M S: condition 3, retention time = 1.99 min LC/M S(ESI +) m/z; 3 18 [M+H] + LC/M S(ESI ) m/z; 3 16 [M- H] H-N MR (DMSO- ) : 1.2 1- 1.39 ( , 2H) , 1.54- 1.67 ( , 1H) , 1.68-1 .86 (m, 2H) , 1.87-2. 11 (m, 6H), 3 .08-3. 22 (m, 1H) , 4.92 (t, J = 7.4 Hz, 1H) , 6 .80 (dd, J = 3 .0 , 1.8 Hz, 1H) , 7 .49 (t , J = 3 .0 Hz, 432 1H), 9 .5 1 (s , 1H) , 12 .5 1 (s, 1H) . LC/M S: condition 3 , retention tim e = 1.93 min LC/M S(ESI +) m/z; 320 [M+H] + LC/M S(ESI ) m/z; 3 18 [M-H] H-NMR (DMSO- ) : 1.70- 1.90 (m, 2H) , 2 .00-2. 18 (m, 2H) , 2 .23-2 .80 (m, 4H) , 3 .20-3. 50 (m, 1H) , 4 .72 (s, 2H), 6 .8 1 (d, J = 2 .7 Hz , 1H) , 7 .49 (d, J = 1.8 Hz, 1H) 433 , 9 .5 1 (s, 1H) , 12 .52 (br s , 1H) . LC/M S: condition 1, retention time = 3 .79 min LC/M S(ESI +) m/z; 254 [M+H] + LC/M S(ESI ) m/z; 252 [-  H-NMR (CDC I3) : 2 .13 (m, 2H) , 2 .30 (m, 2H), 2 .45 (m, 2H), 2 .68 (m, 1H) , 3.13 ( , 1H) , 3.50 (tt, J = 11.4, 3.9 Hz, 1H) , 5 .2 1 (s, 1H) , 6.77 (t, J = 3.0 Hz, 1H) , 7 .34 (t, J = 3.0 Hz, 1H), 9.25 (s, 1H) , 9.38 434 (br s , 1H) . LC/M S: condition 1, retention time = 3 .37 min LC/M S(ESI +) m/z; 279 [M+H] + LC/M S(ESI ) m/z; 277 [M- H] -NMR (CDCI3) : 1.86 (m, 4H) , 1.96 (m, 2H), 2 .09 (m, 1H) , 2.19 (m, 2H) , 2 .42 (d, J = 7.5 Hz, 2H) , 3.46 ( , 1H), 6 .75 (t, J = 3.0 Hz, 435 1H), 7 .30 (t, J = 3 .0 Hz, 1H), 9.23 (s, 1H) , 9 .25 (br s , 1H) . a LC/M S: condition 1, retention tim e = 3 .38 min LC/M S(ESI +) m/z; 28 1 [M+H] + LC/M S(ESI ) m/z; 279 [M- H] Ή -NMR (CDC I3) : 1.43 (m, 2H) , 1.84-2.0 1 (m, 3H) , 2 .05 -2 .26 ( , 2H), 2 .20 (m, 2H) , 2 .4 1 (m, 2H) , 3 .18 (tt, J = 12 , 3.6 Hz, 1H), 6 .78 435 (m, 1H) , 7 .3 1 (m, 1H) , 9.23 (s, 1H) , 9 .47 (br s, 1H) . b LC/M S: condition 1, retention time = 3 .27 min LC/MS(ESI +) m/z; 28 1 [M+H] + LC/MS(ESI ) m/z; 279 [M- H] ' H-N MR (CDCI3) : 1.3 1 (t , 3H) , 2.03-2 .32 ( , 5H) , 2 .40-2 .58 (m, 2H), 3 .50 (tt , J = 11.1, 3.6 Hz, 1H) , 3 .96 (m, 1H) , 4.2 0 (q , J = 6 .9 Hz , 2H) , 5.76 (s, H) , 6.78 (dd , J = 3.3, 2 . 1 Hz, 1H) , 7 .33 (t, J = 436 3 .3 Hz, 1H), 9.26 (s, 1H), 10 .02 (br s, 1H) . LC/M S: condition 1, retention tim e = 3 .80 min LC/M S(ESI +) m/z; 326 [M+H] + LC/MS(ESI ) m/z; 324 [M- H] TABLE 150 Ex Data ' H-NMR (CDCI 3) : 1.97 (s, 3H) , 2 .00-2. 28 (m, 5H) , 2.44 (m, 1H) , 2 .90 (m, 1H), 3 . 13 (m, 1H) , 3.48 (tt, J = 10 .8 , 3.9 Hz, 1H) , 6.76 (m, 1H) , 7 .3 1 (m, 1H) , 437 9 .17 (br s, 1H) , 9 .23 (s, 1H) . LC/M S: condition 1, retention tim e = 3 .54 min LC/M S(ESI +) m/z; 293 [M+H] + LC/M S(ESI ) m/z; 29 1 [M- H] Ή -NMR (CDCI 3) : 1.28 (m, 6H) , 1.75 (m, 4H) , 1.8 1-2 .02 (m, 8H) , 2 . 13-2. 32 (m, 8H) , 2.43 (d , J = 7 .2 Hz , 2H) , 3 .17 (tt , J = 11.7 , 3 .6 Hz, 1H), 3 .39 (m, 1H), 4. 16 (m, 4H) , 6.78 (m, 2H) , 7.32 (m, 2H) , 438 9.25 (s, 1H) , 9 .26 (s, 1H) , 10.00 (br s , 2H) . LC/M S: condition 1, retention time = 3 .80 min (cis/trans mixture) LC/M S(ESI +) m/z; 328 [M+H] + LC/M S(ESI ) m/z; 326 [M- Hl H-NMR (CDCI 3) : 1.34 (d , J = 7 .2 Hz, 3H), 1.42-1 .6 1 (m, 5H), 1.80 (m, 2H) , 1.93 (m, 2H) , 2.68 (qu in, J = 7 .2 Hz , 1H) , 3 .5 1 ( , 439 1H) , 6 .76 (m, 1H) , 7.29 ( , 1H) , 9.23 (s, 1H) . a LC/M S: condition 1, retention time = 3 .65 min LC/M S(ESI +) m/z; 295 [M+H] + LC/M S(ESI ) m/z; 293 [M- H] ' H-NMR (CDCI 3) : 1.40 (m, 3H) , 1.42- 1.6 1 (m, 5H), 1.97 (m, 2H) , 2 .20 ( , 2H), 2 .65 (qu in, J = 6 .6 Hz, 1H) , 3 . 19 (m, 1H) , 6.79 ( , 439 1H), 7 .3 1 ( , 1H) , 9.15 (br s , 1H) , 9 .23 (s, 1H) . b LC/M S: condition 1, retention tim e = 3 .49 min LC/M S(ESI +) m/z; 295 [M+H] + LC/MS(ESI ) m/z; 293 [M- Hl H-NMR (CDCI 3) : 1.42 (m, 2H) , 1.9 1-2.04 (m, 4H) , 2 .20 (m, 2H) , 2 .36 (m, 1H) , 3 . 16 (tt , J = 12.0, 3.6 Hz, H), 5 .37 (dd , J = 6.5 , 1.5 Hz , 1H) , 6.76 (dd , J = 16.5, 6.9 Hz, 1H), 6.77 (d, J = 3 .3, 1H) , 7 .29 440 (d, J = 3 .3 Hz, 1H), 9 .16 (br s, 1H) , 9.22 (s , 1H). LC/M S: condition 1, retention time = 3 .54 min LC/M S(ESI +) m/z; 293 [M+H] + LC/M S(ESI ) m/z; 29 1 [M- H] H-NMR (CDCI 3) : 1.24 (m, 2H) , 1.59- 1.73 (m, 5H) , 1.87 -2.04 (m, 2H), 2 . 16 ( , 2H) , 2 .44(t, J = 7.2 Hz, 2H) , 3 .17 (tt, J = 12 .3 , 3.3 Hz, 1H) , 6 .78 (dd , J = 3 .3 , 2 .1, 1H) , 7.30 (t , J = 3.3 Hz, 1H) , 9.22 44 1 (s, 1H) , 9.2 8 (b r s , 1H) . LC/M S: condition 1, retention time = 3.47 min LC/M S(ESI +) m/z; 295 [M+H] + LC/M S(ESI ) m/z; 293 [M- H] -NMR (CDCI 3) : 1.74 (m, 4H) , 1.9 1-2. 17 (m, 6H) , 2 .3 1 (m, 1H) , 3 .40 (m, 1H), 3 .93 (m, 2H) , 6.77 ( , 1H) , 7.25 (m, 1H), 9. 12 (br s, 442 1H) , 9 .22 (s, 1H) . a LC/M S: condition 1, retention tim e = 3 .42 min LC/M S(ESI +) m/z; 38 1 [M+H] + LC/M S(ESI ) m/z; 379 [M-H] TABLE 151 Pharmacological assay Now, a pharmacological assay of the tricyclic pyrimidine compounds of the present invention will be described. ASSAY EXAMPLE 1. Enzyme assay JAK1 , JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd.(PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 mM HEPES pH.7.5, 1 mM EGTA, 1 mM MgCI2, 2 mM DTT, 0.01 % Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 , and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ehylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS. From the plot of logarithm of a compound concentration and inhibitory activity, the IC50 was calculated. The results of JAK3, JAK1 , JAK2 and Tyk2 enzyme assays of the compounds of Synthetic Examples are shown in Tables 152 to 155. "* " in the Tables indicates IC50 > 1 . TABLE 152 I 5 o ) I C M ) NO. J A K 3 J A K 1 1 1 . 4 0 . 2 3 2 0 . 0 6 1 0 . 0 1 4 3 1 . 4 0 . 0 5 7 4 0 . 2 9 0 . 0 1 3 5 0 . 2 6 0 . 0 2 0 6 0 . 1 5 0 . 0 0 3 8 7 0 . 0 5 5 0 . 0 0 4 2 8 0 . 4 3 0 . 0 2 0 9 0 . 4 3 0 . 0 3 0 1 0 0 . 1 9 0 . 0 0 3 1 TABLE3 53 1 0 . 3 1 0 . 5 9 2 0 . 0 1 7 0 . 0 5 9 3 0 . 1 3 * 4 0 . 0 2 6 0 . 2 3 5 0 . 1 3 0 . 1 3 6 0 . 0 1 2 0 . 0 4 6 7 0 . 0 1 2 0 . 0 5 6 8 0 . 0 3 0 0 . 0 3 6 9 0 . 0 4 6 0 . 0 7 8 1 0 0 . 0 1 9 0 . 0 3 7 TABLE 154 Exa. I 0 ( M ) I 5 0 ( M ) I C 5 0 ( M ) I C 5 0 ( No. J A K 1 J A K 2 J A K 3 T Y K 2 1 0 . 2 0 0 . 3 4 0 . 4 4 4 . 1 2 0 . 0 2 1 0 . 2 2 0 . 4 0 0 . 9 1 3 0 . 1 2 0 . 2 5 * 4 0 . 0 2 1 0 1 1 1 . 0 2 . 2 5 0 . 2 9 2 . 5 4 . 3 6 0 . 2 8 0 . 5 7 5 . 3 2 . 6 7 0 . 0 2 9 0 . 0 7 6 2 1 0 . 5 7 8 0 . 2 1 0 . 6 2 * 9 0 . 0 7 2 0 . 2 7 1 . 0 1 . 0 0 0 . 0 1 9 0 . 0 3 2 0 . 3 3 0 . 4 2 1 0 . 0 1 5 0 . 1 1 0 . 9 0 0 . 7 1 2 0 . 0 6 1 0 . 5 6 * 0 . 8 8 3 0 . 5 5 * * 4 0 . 1 6 0 . 5 1 6 . 9 5 . 3 5 0 , 0 1 6 0 . 0 4 7 0 . 4 4 0 . 1 6 6 0 . 0 2 8 0 . 2 1 7 0 . 1 8 * * * 8 0 . 0 1 9 0 . 0 4 0 0 . 2 2 1 . 5 9 0 . 0 9 4 0 . 3 4 0 0 . 0 0 9 5 0 . 0 6 4 0 . 4 8 0 . 2 0 1 0 . 0 2 3 0 . 2 1 2 0 . 0 0 9 8 0 . 0 3 6 0 . 3 8 0 . 9 9 3 0 . 0 0 2 5 0 . 0 1 9 0 . 0 7 8 0 . 6 3 4 0 . 0 0 3 3 0 . 0 1 0 0 . 0 3 1 0 . 1 7 5 0 . 0 0 4 9 0 . 0 1 7 0 . 2 6 0 . 4 6 6 0 . 0 7 3 0 1 8 * * 7 0 . 0 0 5 4 0 . 0 4 1 0 . 3 1 8 0 . 0 0 4 6 0 . 0 3 2 0 . 2 2 9 0 . 0 0 4 9 0 . 0 2 8 0 . 5 3 0 0 . 0 0 2 2 0 . 0 0 6 4 0 . 0 3 7 0 . 1 5 1 0 . 0 0 1 1 0 . 0 0 6 1 0 . 0 4 2 0 . 1 5 2 0 . 0 8 2 0 . 4 1 * 3 0 . 0 0 2 7 0 . 0 1 4 0 . 0 5 4 0 . 1 0 4 0 . 0 0 4 9 0 . 0 1 3 0 . 0 4 2 0 . 1 2 5 0 . 0 6 6 1 . 0 * 6 0 . 0 2 5 0 . 1 7 * * 7 0 . 7 8 * 8 0 . 0 2 2 0 . 0 5 4 0 . 4 4 0 . 4 6 9 0 . 0 0 0 6 1 0 . 0 0 2 7 0 . 0 4 1 0 . 0 5 7 0 0 . 0 1 1 * * * 1 0 . 2 5 * 2 0 . 0 0 2 1 0 . 0 1 8 0 . 0 4 1 0 . 3 6 3 0 . 0 0 0 3 2 0 . 0 0 1 5 0 . 0 2 4 0 . 0 4 7 4 0 . 0 0 1 2 0 . 0 1 5 0 . 0 7 1 . 2 1 5 0 . 0 0 6 1 0 . 0 3 0 0 . 2 2 0 . 3 9 a 0 . 5 * 0 . 0 3 5 0 . 6 0 * * 0 . 0 6 9 * 0 . 1 8 0 . 8 !2 * * 0 . 0 3 2 0 . 1 8 * * 0 . 0 0 5 1 0 . 0 3 2 * 4 . 2 0 . 0 1 6 0 . 1 5 0 . 5 3 0 . 4 4 0 . 0 0 9 9 0 . 0 3 1 0 . 4 7 0 . 1 4 0 . 0 1 1 0 . 0 4 0 0 . 7 8 0 . 2 0 0 . 0 3 3 0 . 1 2 0 . 9 3 0 . 3 1 0 . 0 0 3 1 0 . 0 1 3 0 . 1 5 0 . 0 2 5 0 . 0 0 3 3 0 . 0 1 3 0 . 0 8 6 0 . 0 2 7 0 . 0 5 2 0 . 2 0 0 . 6 5 0 . 4 1 0 . 0 0 4 7 0 . 0 2 6 * 0 . 0 4 1 0 . 0 0 0 9 4 0 . 0 0 2 8 0 . 0 5 5 0 . 0 2 8 0 . 0 0 2 1 0 . 0 0 7 7 0 . 0 4 8 0 . 0 3 2 0 . 0 0 1 9 0 . 0 1 4 0 . 0 6 5 0 . 0 1 1 0 . 0 0 0 4 0 0 . 0 0 3 0 . 0 7 4 0 . 0 0 2 6 0 . 0 0 0 2 0 0 . 0 0 1 0 0 . 0 3 2 0 . 0 0 1 2 0 . 0 0 0 3 3 0 . 0 0 2 2 0 . 0 3 0 0 . 0 0 9 7 0 . 0 0 1 3 0 . 0 5 4 0 . 0 5 3 0 . 4 4 0 . 0 0 3 3 0 . 0 1 5 0 . 1 7 0 . 0 5 5 0 . 0 0 3 0 0 . 0 2 0 0 . 3 9 0 . 0 4 3 0 . 0 1 2 0 . 0 5 3 0 . 6 4 0 . 1 5 0 . 0 4 1 0 . 3 0 * 0 . 5 5 0 . 0 0 9 1 0 . 0 4 8 0 . 2 8 0 . 0 9 6 0 . 0 1 8 0 . 0 8 9 0 . 6 2 0 . 5 4 0 . 0 5 3 0 . 3 1 * 0 . 5 0 0 . 0 2 0 0 . 1 7 0 . 4 8 * 0 . 0 0 5 5 0 . 0 2 6 0 . 2 1 0 . 1 5 0 . 0 2 5 0 . 2 0 * 0 . 6 1 0 . 0 0 4 7 0 . 0 2 6 0 . 2 0 0 . 0 4 4 0 . 0 1 8 0 . 0 9 4 0 . 6 4 0 . 3 2 0 . 0 0 5 8 * * * 0 . 0 0 7 5 0 . 0 6 1 0 . 3 1 0 . 0 0 5 9 0 . 0 0 4 1 0 . 0 4 1 0 . 8 3 0 . 2 5 0 . 0 0 9 9 0 . 0 8 3 * 0 . 4 3 0 . 0 2 7 0 . 2 1 * * 0 . 0 2 1 0 . 1 0 0 . 9 7 * 0 . 0 0 3 3 0 . 0 7 0 0 . 3 0 0 . 0 0 2 6 0 . 0 6 0 0 . 4 2 * * 0 . 0 0 9 3 0 . 0 4 5 0 . 2 4 0 . 4 7 0 . 0 0 2 6 0 . 0 4 6 . 2 2 0 . 0 0 2 3 0 . 0 1 9 0 . 1 5 * 0 . 0 1 6 0 . 1 7 * 0 . 4 7 0 . 0 8 9 * * * 0 . 0 2 1 0 . 1 9 * 0 . 3 7 0 . 0 0 1 9 0 . 0 4 1 0 . 2 8 0 . 0 0 3 6 0 . 0 0 2 8 0 . 0 5 5 0 . 2 8 0 . 0 3 6 0 . 0 0 3 9 0 . 0 2 4 0 . 5 8 0 . 5 8 0 . 0 0 1 6 0 . 0 1 1 0 . 1 6 0 . 0 7 2 0 . 0 0 5 6 0 . 0 9 1 0 5 1 0 . 0 0 4 0 . 0 0 1 9 0 . 0 2 7 0 2 2 0 . 0 2 8 0 . 0 0 4 9 0 . 0 7 9 0 2 5 0 . 0 0 3 0 . 0 0 7 8 0 . 0 8 9 0 7 1 0 . 0 0 8 0 . 0 9 5 0 . 4 3 * 0 . 8 7 0 . 1 3 0 . 4 0 * 0 . 0 0 3 3 0 . 0 3 2 0 5 6 0 . 1 9 0 . 0 3 9 0 . 3 6 * 0 . 0 1 5 0 . 0 3 5 * 0 . 1 3 0 . 0 0 4 0 0 . 0 3 9 0 5 9 0 . 1 0 0 . 0 1 4 0 . 2 0 * 0 . 1 2 0 . 0 0 3 9 0 . 0 4 2 0 4 6 0 . 1 4 0 . 0 2 3 0 . 4 7 0 . 3 4 0 . 0 0 6 1 0 . 1 9 0 8 7 0 . 2 3 0 . 0 2 9 0 . 2 3 * 0 . 5 5 0 . 0 7 1 * * 0 . 0 7 3 * * 0 . 0 1 7 0 . 1 9 * 0 . 4 2 0 . 1 4 0 . 0 0 7 1 0 . 0 7 8 * 0 . 1 8 0 . 0 1 1 0 . 0 2 4 0 . 1 8 0 . 0 0 5 4 0 . 0 3 2 0 5 6 0 . 1 3 0 . 0 0 5 0 0 . 0 3 4 * 0 . 1 1 0 . 1 2 * a 0 . 0 2 2 0 . 0 9 5 1 0 0 . 3 7 b 0 . 0 0 2 2 0 . 0 2 4 0 6 6 0 . 0 5 6 a 0 . 0 9 7 0 . 9 4 * b 0 . 0 0 6 3 0 . 0 9 4 0 . 1 8 a 0 . 1 4 * b 0 . 0 1 0 . 2 9 * 0 . 4 5 a 0 . 0 3 2 0 . 4 9 * 0 . 3 1 b 0 . 0 0 4 1 0 . 0 3 9 0 3 8 0 . 0 8 8 a 0 . 0 2 3 0 . 7 4 * 0 . 2 5 b 0 . 0 0 4 3 0 . 0 4 3 0 4 0 0 . 0 4 6 a 0 . 2 6 0 . 4 0 0 4 3 * b 0 . 0 2 1 0 . 0 7 6 * 0 . 5 0 0 . 0 2 8 0 . 0 3 9 0 5 0 0 . 1 3 0 . 0 0 2 8 0 . 0 1 4 0 2 4 0 . 0 3 8 0 . 0 0 8 0 0 . 0 1 4 0 3 6 0 . 2 8 0 . 0 0 2 5 0 . 0 0 5 6 0 1 8 0 . 1 2 0 . 0 0 0 6 0 . 0 0 4 0 0 0 5 4 0 . 0 6 2 0 . 0 0 3 7 0 . 0 1 5 0 0 2 6 0 . 2 0 0 . 0 0 9 1 0 . 0 2 0 0 3 1 0 . 1 7 0 . 0 0 2 4 0 . 0 0 4 9 0 1 8 0 . 1 6 0 . 0 0 4 3 0 . 0 1 0 0 2 0 0 . 2 1 0 . 0 0 1 4 0 . 0 0 2 8 0 0 6 0 0 . 0 9 8 0 . 0 0 0 9 0 . 0 2 2 0 0 0 9 8 0 . 0 9 1 0 . 0 4 9 0 . 0 7 2 0 6 3 0 . 0 0 1 8 0 . 0 0 3 7 0 0 3 2 0 . 1 1 0 . 0 0 1 0 0 . 0 0 2 3 0 0 1 5 0 . 1 1 0 . 0 0 8 6 0 . 0 2 4 0 . 6 2 0 . 7 0 0 . 0 1 1 0 . 0 3 2 0 . 9 5 * 0 . 0 0 3 2 0 . 0 4 2 0 . 5 2 0 . 6 5 0 . 0 0 2 0 0 . 0 2 0 0 . 2 4 0 . 3 1 0 . 0 0 0 7 0 0 . 0 0 4 4 0 . 0 5 9 0 . 0 9 7 0 . 0 0 1 6 0 . 0 1 1 0 . 0 8 0 0 . 3 0 0 . 0 0 5 3 0 . 0 2 1 0 . 3 5 0 . 2 6 0 . 0 0 3 4 0 . 0 1 1 0 . 3 1 0 . 1 4 0 . 0 3 2 0 . 2 0 0 . 6 8 0 . 0 1 0 0 . 0 3 4 0 . 4 1 0 . 3 1 0 . 0 0 5 8 0 . 0 3 0 0 . 2 3 0 . 2 9 0 . 0 0 4 4 0 . 0 2 0 0 . 1 0 0 . 3 4 0 . 0 0 5 3 0 . 0 2 3 0 . 1 7 0 . 4 9 0 . 0 0 3 1 0 . 0 3 0 0 . 1 7 0 . 9 8 0 . 0 8 4 0 . 7 1 * 0 . 0 0 5 0 0 . 0 5 2 0 . 5 8 * 0 . 0 2 1 0 . 1 1 0 . 5 2 0 . 1 0 0 . 9 4 * 0 . 0 1 3 0 . 0 9 3 * 0 . 6 3 0 . 0 3 4 0 . 2 6 * 0 . 4 6 0 . 0 0 5 7 0 . 0 7 2 0 . 6 1 0 . 0 9 9 0 . 0 0 5 6 0 . 0 0 7 4 0 . 3 4 0 . 0 4 5 0 . 0 3 4 0 . 1 9 * * 0 . 0 0 2 9 0 . 0 3 1 0 . 2 0 0 . 0 0 2 8 0 . 0 0 2 6 0 . 0 2 4 0 . 1 7 0 . 5 3 0 . 0 2 8 0 . 0 9 4 * 0 . 0 0 1 3 0 . 0 0 1 9 0 . 0 3 0 0 . 0 2 2 0 . 0 2 4 0 . 1 3 * 0 . 4 9 0 . 0 0 5 4 0 . 0 3 9 0 . 2 8 0 . 0 1 6 0 . 0 0 6 1 0 . 0 5 5 0 . 8 0 0 . 0 4 1 0 . 0 0 3 5 0 . 0 4 2 0 . 5 8 0 . 0 8 7 0 . 0 0 8 1 0 . 0 5 1 0 . 3 2 0 . 1 3 0 . 0 0 2 7 0 . 0 2 7 0 . 0 9 9 0 . 0 4 4 0 . 0 0 7 6 0 . 0 3 8 0 . 3 7 0 . 3 6 0 . 0 0 1 2 0 . 0 0 8 4 0 . 1 1 0 . 0 6 3 0 . 0 1 1 0 . 0 3 8 0 . 6 1 0 . 3 8 0 . 0 2 2 0 . 0 9 8 * 0 . 6 1 0 . 0 1 0 0 . 0 8 4 0 . 9 2 0 . 1 8 0 . 0 0 3 9 0 . 0 3 8 0 . 3 2 0 . 1 0 0 . 0 0 5 3 0 . 0 4 1 0 . 2 8 0 . 0 0 5 5 a . 0 3 2 0 . 7 4 0 . 3 3 b 0 . 0 0 8 4 0 . 0 4 6 0 . 5 0 0 . 1 1 a 0 . 0 3 0 0 . 5 5 * 0 . 3 1 b 0 . 0 0 7 0 0 . 0 4 2 0 . 5 6 0 . 1 2 a 0 . 0 6 0 0 . 7 5 * * b 0 . 0 0 3 2 0 . 0 3 6 0 . 2 9 0 . 2 7 a 0 . 0 1 6 0 . 4 0 * 0 . 1 5 b 0 . 0 0 5 4 0 . 0 4 5 0 . 5 2 0 . 1 1 b 0 . 0 0 2 5 0 . 0 3 7 0 . 4 0 0 . 0 6 5 b 0 . 0 0 3 5 0 . 0 3 5 0 . 1 8 0 . 4 4 b 0 . 0 0 2 5 0 . 0 3 2 0 . 0 7 6 0 . 2 4 b 0 . 0 0 3 9 0 . 0 6 6 0 . 4 1 0 . 1 0 b 0 . 0 0 3 4 0 . 0 8 5 0 . 6 8 0 . 2 6 b 0 . 0 0 4 1 0 . 1 6 1 . 0 0 . 3 3 b 0 . 0 0 7 2 0 . 1 9 * 0 . 3 5 0 . 0 2 6 0 . 2 5 * 0 . 7 5 0 . 2 7 * 0 . 0 0 9 0 0 . 0 5 5 * 0 . 0 0 2 8 0 . 0 3 3 0 . 3 6 0 . 3 7 0 . 0 6 1 0 . 4 2 * 0 . 0 0 4 7 0 . 0 1 9 0 . 0 7 7 0 . 2 9 0 . 1 2 0 . 7 4 * * 0 . 0 0 5 4 0 . 0 4 7 0 . 6 2 0 . 4 5 TABLE 155 Exa I 0 ( M ) I C 5 o ( M ) I C 5 □ ( M ) I C 5 0 (  No. J A K 1 J A K 2 J A K 3 T Y K 2 2 1 3 0 . 0 2 4 0 . 1 9 2 1 4 0 . 0 0 2 6 0 . 0 1 3 0 . 4 0 0 . 2 9 2 1 5 0 . 0 2 6 0 . 2 5 * 2 1 6 0 . 3 8 2 1 7 0 . 0 8 0 0 . 1 8 0 . 3 8 2 1 8 0 . 0 2 8 0 . 1 4 * * 2 1 9 0 . 0 3 9 0 . 0 8 1 0 . 6 2 0 . 9 7 2 2 0 0 . 0 1 3 0 . 0 8 6 0 . 6 2 * 2 2 1 0 . 0 1 8 0 . 0 9 0 * 2 2 2 0 . 0 0 3 5 0 . 0 3 3 0 . 3 2 0 . 7 7 2 2 3 0 . 0 1 5 0 . 0 3 1 0 . 9 4 * 2 2 4 0 . 0 0 2 0 0 . 0 1 2 0 . 4 3 0 . 9 5 2 2 5 0 . 0 2 1 0 . 2 0 * * 2 2 6 0 . 2 8 * * 2 2 7 0 . 0 0 2 5 0 . 0 2 1 0 . 0 7 9 0 . 5 7 2 2 8 0 . 0 0 1 6 0 . 0 0 4 4 0 . 1 7 0 . 1 0 2 2 9 0 . 0 3 9 0 . 0 8 7 * * 2 3 0 0 . 0 3 5 0 1 3 2 3 1 0 . 0 0 4 3 0 . 0 2 3 0 . 2 3 0 . 6 1 2 3 2 0 . 0 0 5 3 0 . 0 3 3 0 . 7 4 2 3 3 0 . 0 2 1 0 . 0 7 1 2 3 4 0 . 3 6 0 . 8 8 2 3 5 0 . 5 6 0 . 3 7 * 2 3 6 0 . 0 0 6 8 0 . 0 5 2 0 . 4 5 * 2 3 7 0 . 0 0 1 5 0 . 0 1 0 0 . 4 1 2 3 8 0 . 0 0 0 7 9 0 . 0 0 4 6 0 . 0 5 5 0 . 1 1 2 3 9 0 . 0 0 8 1 0 . 0 3 5 0 . 6 1 0 . 6 5 2 4 0 0 . 0 3 9 0 . 1 1 0 . 6 0 * 2 4 1 0 . 0 4 6 0 1 7 * 2 4 2 0 . 0 0 6 5 0 . 0 5 2 0 . 9 6 2 4 3 0 . 0 4 4 0 . 2 9 * 2 4 4 0 . 0 0 5 4 0 . 0 3 8 0 . 4 4 0 . 7 9 2 4 5 0 . 0 1 7 0 . 0 6 2 2 4 6 0 . 0 0 5 3 0 . 0 1 9 0 . 2 8 0 . 1 4 2 4 7 0 . 0 1 3 0 . 0 9 0 0 . 9 2 * 2 4 8 0 . 0 4 1 0 . 1 4 * 2 4 9 0 . 0 1 7 0 . 0 5 6 0 . 4 9 0 . 8 6 2 5 0 0 . 0 3 1 0 1 8 * * 2 5 1 0 . 0 3 1 0 . 2 0 2 5 2 0 . 0 1 7 0 . 0 6 0 2 5 3 0 . 0 0 1 1 0 . 0 0 6 6 0 . 1 4 0 . 0 4 4 2 5 4 0 . 0 0 7 1 0 . 0 2 4 0 . 5 3 0 . 1 6 2 5 5 0 . 0 0 2 5 0 . 0 1 5 0 . 2 4 0 . 1 4 2 5 6 0 . 0 1 5 0 . 0 6 2 0 . 9 9 0 . 2 7 2 5 7 0 . 0 0 1 7 0 . 0 1 6 0 . 4 9 0 . 0 4 9 2 5 8 0 . 0 1 2 0 . 0 8 1 * 0 . 7 4 0 . 0 0 2 1 0 . 0 0 8 1 0 . 2 7 0 . 0 3 0 . 0 2 4 0 . 0 4 8 * 0 . 9 7 0 . 0 2 3 0 . 0 9 1 * 0 . 6 4 0 . 0 0 4 7 0 . 0 4 5 0 . 5 9 0 . 9 1 0 . 0 2 7 0 . 2 2 * 0 . 0 1 1 0 . 0 3 2 * 0 . 0 4 6 0 . 1 8 * * 0 . 0 2 5 0 . 1 1 * 0 . 3 5 0 . 0 0 1 0 0 . 0 3 2 0 . 7 9 0 . 0 1 0 . 0 0 4 4 0 . 0 3 6 0 . 7 2 0 . 1 2 0 . 0 0 1 3 0 . 0 1 2 0 . 0 5 7 0 . 1 0 0 . 0 1 2 0 . 1 0 0 . 7 5 0 . 0 0 0 . 0 2 0 0 . 0 6 3 * 0 . 4 3 0 . 0 0 3 5 ϋ . 0 5 3 0 . 4 3 0 . 0 9 0 . 0 0 4 6 0 . 0 2 1 0 . 5 7 0 . 2 4 0 . 0 0 3 5 0 . 0 2 9 * 0 . 2 0 0 . 0 0 6 7 0 . 0 6 5 0 . 8 5 0 . 5 2 0 . 0 0 2 9 0 . 0 4 9 0 . 0 6 3 0 . 0 3 0 . 0 0 1 5 0 . 0 3 3 0 . 2 Ί 0 . 0 5 0 . 0 0 4 3 0 . 0 3 4 0 . 4 5 0 . 4 0 0 . 0 0 7 4 0 . 0 4 4 0 . 5 3 0 . 2 0 0 . 0 0 1 9 0 . 0 6 2 0 . 6 8 0 . 1 0 0 . 0 0 7 7 0 . 0 5 0 0 . 1 5 0 . 4 8 0 . 0 0 5 2 0 . 0 7 0 0 . 3 9 0 . 0 8 0 . 0 1 4 . 1 1 0 . 9 0 0 . 2 3 0 . 0 1 7 0 . 1 5 * 0 . 3 2 0 . 0 0 9 1 0 . 1 2 0 . 6 1 0 . 0 6 0 . 0 0 5 9 0 . 0 3 5 0 . 5 7 0 . 2 3 0 . 0 0 6 5 0 . 0 7 7 * 0 . 3 3 0 . 0 4 6 0 . 1 5 0 . 1 5 0 . 3 7 0 . 0 2 1 0 . 1 5 0 . 8 5 0 . 1 6 0 . 0 0 7 6 0 . 0 3 9 0 . 5 0 0 . 2 7 0 . 0 0 5 3 0 . 1 0 0 . 6 7 0 . 1 4 0 . 0 0 2 7 0 . 0 1 7 0 . 3 9 0 . 2 7 0 . 0 2 4 0 . 1 0 0 . 9 4 0 . 3 1 0 . 0 2 2 0 . 1 2 . 4 8 0 . 3 4 0 . 0 0 6 9 0 . 0 6 4 0 . 8 4 0 . 3 3 0 . 0 0 3 8 0 . 0 6 5 0 . 7 3 0 . 1 9 0 . 0 0 9 5 0 . 1 0 * 0 . 3 2 0 . 0 1 9 0 . 1 1 * 0 . 5 9 0 . 0 1 6 0 . 1 7 * * 0 . 0 2 5 0 . 0 5 9 0 . 7 5 0 . 0 2 4 0 . 0 7 2 0 . 9 6 0 . 0 1 2 0 . 0 2 9 0 . 4 9 0 . 3 6 0 . 0 5 7 0 . 3 5 * * 0 . 0 4 9 0 . 2 7 * * 0 . 0 4 6 0 . 2 9 * * 0 . 0 1 5 0 . 0 5 4 * 0 . 6 2 0 . 0 0 6 6 0 . 2 6 * * 0 . 0 0 2 4 0 . 0 1 2 0 . 2 4 0 . 7 9 0 . 0 0 7 6 0 . 0 9 7 0 . 3 1 0 . 0 7 1 0 . 3 8 * 0 . 0 2 5 0 . 1 6 0 . 9 4 0 . 0 1 2 0 . 0 4 5 0 . 3 7 0 . 0 0 8 4 0 . 0 5 1 * 0 . 5 1 0 . 0 0 8 0 0 . 1 9 * 0 . 7 5 0 . 0 1 0 0 . 2 0 * 0 . 5 3 0 . 0 1 3 0 . 0 9 9 0 . 5 9 0 . 0 0 1 3 0 . 0 1 6 0 . 4 7 0 . 6 2 0 . 0 0 4 8 0 . 0 5 7 * 0 . 6 1 0 . 0 2 7 0 . 2 3 * 0 . 0 0 7 6 0 . 0 5 7 0 . 8 6 0 . 0 2 4 0 . 2 1 * 0 . 0 0 1 3 0 . 0 0 7 1 0 . 2 0 0 . 4 3 0 . 0 0 5 1 0 . 0 3 4 0 . 8 3 0 . 7 8 0 . 0 0 3 4 0 . 0 3 4 0 . 6 6 0 . 7 5 0 . 0 1 1 0 . 0 5 8 * 0 . 8 8 0 . 0 4 8 0 . 3 1 * * 0 . 0 0 7 0 0 . 0 5 4 0 . 7 9 0 . 5 5 0 . 0 0 7 3 0 . 0 3 3 0 . 5 3 0 . 9 0 0 . 0 0 4 8 0 . 0 2 9 0 . 8 0 0 . 2 1 0 . 0 0 7 4 0 . 0 4 7 0 . 1 4 0 . 0 0 8 8 0 . 0 5 4 0 . 4 2 0 . 0 1 2 0 . 0 4 5 0 . 4 9 0 . 0 0 8 5 0 . 0 4 4 0 . 2 7 0 . 0 6 4 * * 0 . 0 2 9 0 . 2 9 0 . 7 1 0 . 0 2 5 0 . 3 7 * 0 . 0 2 9 0 . 3 4 0 . 5 1 0 . 0 0 6 9 0 . 0 6 0 0 . 4 8 0 . 5 9 0 . 0 1 8 0 . 0 5 2 0 . 2 6 0 . 8 6 0 . 0 2 1 0 . 2 3 * 0 . 0 1 0 0 . 0 5 9 0 . 3 1 0 . 3 2 0 . 0 3 9 0 . 0 3 4 0 . 1 3 0 . 3 5 0 . 0 1 0 0 . 0 6 3 0 . 3 3 0 . 4 4 0 . 0 1 2 0 . 0 6 8 0 . 5 2 0 . 3 9 0 . 0 2 5 0 . 2 0 * 0 . 0 0 5 1 0 . 0 6 0 0 . 0 0 6 9 0 . 1 1 0 . 5 * 0 . 0 0 9 9 0 . 0 5 1 0 . 7 5 0 . 2 9 0 . 0 0 5 9 0 . 0 4 8 0 . 2 5 0 . 0 0 8 0 0 . 0 4 7 0 . 5 4 0 . 0 1 2 0 . 0 8 9 * 0 . 0 0 5 0 0 . 0 2 9 * * 0 . 0 0 2 9 0 . 0 3 1 0 . 3 5 0 . 4 6 0 . 0 0 1 8 0 . 0 2 6 0 . 6 9 0 . 1 6 0 . 0 0 4 2 0 . 0 3 3 * 0 . 1 5 0 . 0 0 3 6 0 . 0 3 6 0 . 1 6 0 . 0 6 7 0 . 3 3 * 0 . 8 7 0 . 6 3 0 . 9 1 * 0 . 0 4 2 0 . 2 2 * 0 . 5 6 0 . 0 2 6 0 . 1 0 * 0 . 3 3 0 . 0 8 9 0 . 2 5 * * 0 . 0 0 7 4 0 . 0 5 7 * 0 . 0 4 4 0 . 2 9 * * 0 . 0 0 5 7 0 . 0 1 1 0 . 3 9 0 . 2 1 0 . 0 0 5 4 0 . 0 1 6 . 7 4 0 . 3 4 0 . 0 1 1 0 . 0 2 8 0 . 2 8 0 . 2 6 0 . 0 0 0 9 9 0 . 0 0 4 3 0 . 0 5 4 0 . 0 0 0 . 0 0 1 3 0 . 0 0 6 1 0 . 3 7 0 . 0 3 0 . 0 0 0 3 3 0 . 0 0 1 7 0 . 0 4 8 0 . 0 0 0 . 0 0 7 4 0 . 0 9 7 0 . 5 9 * 0 . 0 0 3 3 0 . 0 3 5 0 . 3 9 0 . 1 8 0 . 0 0 4 1 0 . 0 1 6 0 . 2 3 0 . 4 1 0 . 0 0 1 5 0 . 0 1 1 0 . 0 3 5 0 . 5 3 0 . 0 3 8 0 . 1 8 * * 0 . 0 4 7 0 . 3 3 * * 0 . 0 1 9 0 . 1 9 * * 0 . 0 0 4 5 0 . 0 1 7 0 . 0 5 4 * 0 . 0 0 4 0 0 . 0 7 1 0 . 4 1 0 . 2 0 0 . 0 1 3 0 . 1 1 0 . 6 6 0 . 2 9 0 . 0 0 2 0 0 . 0 0 2 5 0 . 2 0 0 . 0 2 a 0 . 0 6 9 0 . 2 2 0 . 2 6 * b 0 . 0 0 6 6 0 . 0 5 7 0 . 4 2 0 . 2 4 a 0 . 0 1 5 0 . 0 6 3 0 . 7 5 0 . 7 6 b 0 . 0 0 0 3 1 0 . 0 0 2 8 0 . 0 7 0 0 . 0 1 a 0 . 0 9 0 0 . 3 7 * * b 0 . 0 0 1 5 0 . 0 1 3 0 . 5 0 0 . 1 7 a 0 . 0 8 7 0 . 5 6 * b 0 . 0 2 2 0 . 0 8 0 * b 0 . 0 0 1 9 0 . 0 3 1 0 . 1 8 0 . 2 1 b 0 . 0 0 1 7 0 . 0 2 7 0 . 2 8 0 . 3 9 b 0 . 0 0 1 9 0 . 0 3 2 0 . 1 2 0 . 1 8 b 0 . 0 0 1 2 0 . 0 2 5 0 . 2 6 0 . 2 1 b 0 . 0 0 7 9 0 . 1 4 * 0 . 6 7 b 0 . 0 0 2 4 0 . 0 8 9 0 . 5 2 0 . 3 6 b 0 . 0 1 8 0 . 3 9 * 0 . 5 8 b 0 . 0 1 4 0 . 0 8 0 0 . 6 1 0 . 3 3 b 0 . 0 0 6 2 0 . 0 3 0 0 . 7 9 0 . 3 8 b 0 . 0 1 5 0 . 0 9 0 * * b 0 . 0 0 2 2 0 . 0 1 0 0 . 6 1 0 . 1 5 b 0 . 0 2 2 0 . 1 9 * 0 . 7 1 b 0 . 0 2 3 0 . 2 1 0 . 8 0 b 0 . 0 2 9 0 . 1 1 * 0 . 7 5 b 0 . 0 0 7 5 0 . 0 2 9 0 . 2 0 b 0 . 0 4 2 0 . 1 9 * 0 . 8 4 0 . 0 1 2 0 . 0 3 6 0 . 3 6 0 . 1 5 0 . 0 1 1 0 . 0 3 0 0 . 1 3 . 1 0 0 . 0 4 0 0 . 3 0 0 . 4 4 0 . 8 1 0 . 1 1 0 . 3 5 0 . 3 2 4 0 5 0 . 0 2 5 0 . 2 5 * 0 . 7 7 4 0 6 0 . 0 8 3 0 . 5 * 0 . 9 4 4 0 7 0 . 0 0 3 4 0 . 0 0 7 3 0 . 3 1 0 . 1 3 4 0 8 0 . 0 0 5 2 0 . 0 1 3 0 . 2 2 0 . 3 1 4 0 9 0 . 0 1 9 0 . 0 3 2 0 . 9 2 0 . 8 4 4 1 0 0 . 0 2 2 0 . 0 4 0 0 . 3 2 0 . 5 8 4 1 1 0 . 0 0 4 3 0 . 0 1 5 0 . 1 7 0 . 3 6 4 1 2 0 . 0 0 2 6 0 . 0 0 5 6 0 . 0 5 4 0 . 3 2 4 1 3 0 . 2 0 0 . 0 3 1 0 . 6 2 4 1 4 0 . 0 0 9 5 0 . 1 3 * 0 . 1 1 4 1 5 0 . 0 3 0 0 . 0 9 5 * * 4 1 6 0 . 0 2 9 0 . 0 4 7 0 . 6 8 4 1 7 0 . 0 0 7 8 0 . 0 2 6 0 . 3 8 0 . 4 2 4 1 8 0 . 0 0 4 3 0 . 0 0 8 4 0 . 3 3 0 . 1 7 4 1 9 0 . 0 0 3 5 0 . 0 0 6 1 0 . 0 6 9 0 . 2 7 4 2 0 0 . 0 0 5 7 0 . 0 1 5 0 . 4 1 0 . 3 0 4 2 1 0 . 0 1 0 0 . 1 7 * 4 2 2 0 . 0 0 2 8 0 . 0 5 1 * 0 . 1 3 4 2 3 0 . 0 7 7 0 . 7 2 4 2 4 0 0 4 4 0 . 4 8 * * 4 2 5 0 . 0 0 2 5 0 . 0 2 2 0 . 0 8 2 0 . 3 7 4 2 6 0 . 0 1 1 0 . 0 6 2 0 . 8 7 0 . 5 8 4 2 7 0 . 0 0 0 1 6 0 . 0 0 1 2 0 . 0 3 0 0 . 0 1 6 4 2 8 0 . 1 9 0 . 7 5 * * 4 2 9 0 . 0 1 7 0 . 0 3 5 0 . 7 9 0 . 5 2 4 3 0 0 . 0 0 8 6 0 . 0 4 9 * 0 . 4 1 4 3 1 0 . 0 0 4 8 0 . 0 1 3 0 . 2 9 0 . 2 4 4 3 2 0 . 0 0 2 6 0 . 0 0 8 8 0 . 1 7 0 . 0 6 7 4 3 3 0 . 0 0 8 1 0 . 0 2 7 0 . 7 1 0 . 1 2 4 3 4 0 . 0 0 2 3 0 . 0 1 4 0 . 4 9 0 . 0 3 4 4 3 5 a 0 . 0 0 5 4 0 . 0 2 1 0 . 7 2 0 . 1 7 4 3 5 b 0 . 0 0 0 1 1 0 . 0 0 2 5 0 . 0 3 2 0 . 0 0 2 9 4 3 6 0 . 0 3 5 0 . 1 7 * * 4 3 7 0 . 0 2 0 0 . 0 5 5 • 5 7 0 . 4 5 4 3 8 0 . 0 1 7 0 . 0 4 4 0 . 3 4 0 . 5 8 4 3 9 a 0 . 1 3 0 . 3 4 * 4 3 9 b 0 . 0 0 3 1 0 . 0 0 7 0 . 3 3 0 . 0 2 5 4 4 0 0 . 0 0 5 3 0 . 0 3 1 0 . 5 4 . 1 4 4 4 1 0 . 0 0 1 6 0 . 0 0 4 6 0 . 1 2 0 . 0 2 4 4 4 2 a 0 . 0 2 7 0 . 0 6 1 0 . 5 2 0 . 7 9 4 4 2 b 0 . 0 0 3 2 0 . 0 1 4 0 . 1 0 0 . 8 8 4 4 3 a 0 . 0 2 6 0 . 0 6 0 0 . 7 3 0 . 5 4 4 4 3 b 0 . 0 1 0 0 . 0 3 0 0 . 3 4 4 4 4 0 . 0 0 3 4 0 . 0 0 9 0 0 . 2 5 0 . 0 4 5 4 4 5 0 . 0 3 1 0 . 1 3 0 . 2 2 0 . 0 5 2 The tricyclic pyrimidine compounds of the present invention have favorable inhibitory activity against JAKs as shown above. ASSAY EXAMPLE a 2 . Signal assay in human whole blood To be a effective pharmaceutical compound for the target diseases of the present invention, especially for rheumatoid arthritis, it is more favorable that the compounds indicate excellent inhibitory activity against JAKs in human whole blood. Inhibitory activity against JAKs in human whole blood can be assessed by, for example, STAT phosphorylation assay in human whole blood as described below. Compounds are added at the various concentrations to human whole blood which is collected from healthy volunteers and preincubated for 30 minutes. Next, cytokine such as IL-2 or IL-6 is added to the mixture and incubated for 15 minutes. Cytokines can be purchased, for example, from PeproTech Inc. Cytokines are added to mixture at 100 ng/mL as final concentration. The mixture including the blood cells are hemolyzed, fixed, permeabilized, washed, and resuspended in stain buffer. BD Cytofix/Cytoperm® solution (manufactured by Becton, Dickinson and Company (BD)), for example, can be used to hemolyze, fix, and permeabilize. Staining buffer (manufactured by BD), for example, can be used as stain buffer according to each protocol issued by BD. Fluorescence-labeled anti-phosphorylated STAT antibody and fluorescence-labeled anti-CD3 antibody are added to the cell suspension and incubated for 30 minutes. Then, cells are washed and resuspended in stain buffer. Fluorescence-labeled anti-phosphorylated STAT antibody and fluorescence-labeled anti-CD3 antibody can be purchased, for example from BD, and final concentration of antibodies can be determined according to each protocols issued by BD. Fluorescence intensity of fluorescence-labeled cells in cell suspension is detected by flow-cytometory. Because the detected fluorescence intensity is proportional to the concentration of the phosphorylated STAT protein in CD3 positive cells, inhibitory activity against STAT phosphorylation by the compounds can be calculated from the ratio between the above mentioned fluorescence intensity and the blank fluorescence intensity which is measured simultaneously without the compounds. From the plot of logarithm of the compound concentrations and the inhibitory activities, the IC o value can be calculated. ASSAY EXAMPLE 3. Inhibition of proliferation of erythro-leukemic cell line The inhibitory activity of the tricyclic pyrimidine compounds of the present invention on cell proliferation mediated by JAK signal can be assayed using a human erythro-leukemic cell line, TF-1 . TF-1 cells can be purchased from ATCC (American Type Culture Collection). TF- 1 cells can be expanded in RPMI1640 media containing 5% FBS and 1 ng/mL GM-CSF (Granulocyte Macrophage Colony-Stimulating Factor) using a C0 2 incubator (5% C0 , 37°C). At the assay, TF-1 cells washed by PBS (Phosphate Buffered Saline) are resuspended in RPMI1640 media containing 5% FBS, and dispensed in 96-well culture plate at 1 x 104 cells/well. Compounds at various concentrations are added to the cells and preincubated for 30 minutes, and then cytokine such as IL-4 or IL-6 is added to the cells. Culture plates are incubated using a CO2 incubator (5% C0 2, 37°C) for 3 days. Cell proliferation can be assayed using WST-8 reagent (Kishida Chemical Co., Ltd.) according to instructions by the manufacturer. The formazan pigment is generated by the addition of WST-8 reagent solution to each well of the culture plates and the subsequent incubation in a C0 2 incubator (5% C0 2, 37°C) for 4 hours, and then detected by measuring the absorbance at 450 nm with a microplate reader. From the plot of logarithm of the compound concentrations and the inhibitory activities, the IC50 value can be calculated. REFERENCE SYNTHETIC EXAMPLE 1 1 Methyl 4-methylpyridin-3-ylcarbamate Potassium tert-butoxide (10.3 g , 92.5 mmol) in tetrahydrofuran (25 mL) was stirred at 23 to 27°C for 30 minutes, and dimethyl carbonate (4.67 mL, 55.5 mmol) was added while the temperature was kept at 35°C or below. To the reaction mixture, 3-amino-4- methylpyridine (5.00 g, 46.2 mmol) in tetrahydrofuran (40 mL) stirred at 32 to 38°C for 90 minutes was added dropwise at 20 to 35°C over 2 hours with stirring. The resulting reaction mixture was cooled to 15 to 20°C , stirred with water (25 mL) at 25°C or below for 1 hour and extracted with tetrahydrofuran. The organic layer was azeotropically distilled with toluene under reduced pressure to a volume of about 50 mL and stirred at 23 to 27°C for one day. The precipitated solid was collected by filtration, washed with toluene and dried under reduced pressure to give the title compound as a brown solid (6.77 g, yield 88%). REFERENCE SYNTHETIC EXAMPLE1 2 Methyl rac-(3R,4R)-1 -benzyl-4-methylpiperidin-3-ylcarbamate Methyl 4-methylpyridin-3-ylcarbamate (30.6 g, 184 mmol) and 5% rhodiumcarbon (12 g) in acetic acid (120 mL) were stirred at 72 to 78°C under a hydrogen atmosphere (70-80 psi). After disappearance of the starting materials was confirmed by NMR, the reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give a concentrate (40.9 g). The concentrate (31 .7 g) was stirred with benzaldehyde (2 .5 mL, 202 mmol) in toluene (184 mL) at 20 to 30°C for 30 minutes. The resulting toluene solution was added dropwise at 30°C or below to a toluene (40 mL) solution of sodium triacetoxyborohydride (9.35 g, 44.0 mmol) stirred at 20 to 30°C for 1 hour. The resulting reaction mixture was stirred for 2 hours, adjusted to pH 6-7 with 3 M aqueous sodium hydroxide at 20°C to 30°C and extracted with toluene. The organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give a brown oil (38.1 g) containing the title compound. The oil was used for the next step without further purification. REFERENCE SYNTHETIC EXAMPLE13 3 rac-(3R,4R)-1-Benzyl-4-methylpiperidin-3-amine Crude methyl rac-(3R,4R)-1-benzyl-4-methylpiperidin-3-ylcarbamate (2.3 g) in concentrated hydrochloric acid (15 mL) was refluxed for one day under heating and allowed to cool to room temperature. The hydrochloric acid was removed under reduced pressure, and the reaction mixture was partitioned between chloroform and saturated aqueous sodium chloride. The aqueous layer was basified with saturated aqueous sodium carbonate and extracted with ethyl acetate twice, and the organic layers were combined, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting brown oil (4.94 g) containing the title compound was used for the next step without further purification. REFERENCE SYNTHETIC EXAMPLE 13 4 1H-Pyrrolo[2,3-b1pyridine 7-oxide m-Chloroperbenzoic acid (25 wt% water content, 12.7 g, 55.2 mmol) in ethyl acetate (30 mL) was gradually added dropwise to 1H-pyrrolo[2,3-b]pyridine (5.14 g, 43.5 mmol) in ethyl acetate (45 mL) cooled to 0°C, and the reaction mixture was stirred at room temperature for one day and then stirred with m-chloroperbenzoic acid (25 wt% water content, 3.93 g, 17.1 mmol) in ethyl acetate (4 mL) at room temperature for 4 hours. The reaction mixture was cooled with ice and filtered, and the resulting solid was purified by silica gel column chromatography (silica gel NH type manufactured by Fuji Silysia Chemical Ltd.: chloroform / methanol = 10/1 (v/v)) to give the title compound as a yellow solid (4.95 g, yield 85%). REFERENCE SYNTHETIC EXAMPLE" 5 4-Chloro-1 H-pyrrolo| 2,3-b1pyridine 1H-Pyrrolo[2,3-b]pyridine 7-oxide (4.95 g, 36.9 mmol) in N,N-dimethylformamide (10 mL) was heated to 50°C, mixed with methanesulfonyl chloride (8.00 mL, 103 mmol) and stirred at 73°C for 3 hours. The reaction mixture was cooled with ice and diluted with water (70 mL), neutralized with sodium hydroxide and stirred for 10 minutes under cooling with ice. The precipitated solid was collected by filtration, washed with water and dried under reduced pressure to give the title compound as a reddish brown solid (4.65 g, yield 83%). REFERENCE SYNTHETIC EXAMPLE 3 6 4-Chloro-1 -(triisopropylsilyl)-l H-pyrrolof2 3-b1pyridine 4-Chloro-1 H-pyrrolo[2,3-b]pyridine (2.84 g, 18.6 mmol) in N,N-dimethylformamide (10 mL) and tetrahydrofuran (10 mL) was stirred with sodium hydride (55 wt% dispersion in mineral oil, 1.08 g, 27.0 mmol) under cooling with ice for 1 hour. The reaction mixture was stirred with triisopropylsilyl chloride (6.0 mL, 28 mmol) at room temperature for one day. After addition of water, the reaction mixture was warmed to room temperature and extracted with hexane twice. The resulting organic layers were combined, washed with saturated aqueous sodium chloride dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane) to give the title compound as a reddish brown oil (5.74 mg, yield 99%). REFERENCE SYNTHETIC EXAMPLE 7 4-Chloro-1 H-pyrrolo[2,3-b1pyridine-5-carbaldehvde s-Butyllithium - hexane/cyciohexane solution ( 1 .06 M, 27 mL, 29 mmol) was added to 4-chloro-1-(triisopropylsilyl)-1 H-pyrrolo[2,3-b]pyridine (5.74 g , 18.6 mmol) in tetrahydrofuran (50 mL) cooled to -78°C, and the reaction mixture was stirred for 1 hour. The reaction mixture was stirred with N,N-dimethylformamide (7.0 mL, 90 mmol) for another 1 hour and then with 4 M hydrogen chloride - ,4-dioxane solution (20 mL) for 30 minutes, and after addition of water, extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in dichloromethane (15 mL) and stirred with trifluoroacetic acid (15 mL) for one day. The reaction mixture was concentrated under reduced pressure, diluted with water and neutralized with saturated aqueous sodium hydrogen carbonate, and the residue was collected by filtration and dried under reduced pressure. The crude product was mixed with ethyl acetate (20 mL) and hexane (20 mL), and the solid was collected by filtration, washed with hexane and dried under reduced pressure to give the title compound as a pale yellow solid (2.72 g, yield 8 1%). REFERENCE SYNTHETIC EXAMPLE 8 4-(Cvclohexylamino)-1 H-pyrrolof2,3-b1pyridine-5-carbaldehyde 4-Chloro-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde (845 mg, 4.68 mmol) and cyclohexylamine (2.5 mL, 22 mmol) in ethylene glycol (2 mL) were stirred at 170°C for 1 hour under microwave irradiation. The reaction mixture was allowed to cool to room temperature and, after addition of water, extracted with chloroform. The organic layer was stirred with 2 M hydrochloric acid (20 mL) for 1 hour, and the organic layer was separated. The aqueous layer was adjusted to pH 9 or above with 10 M aqueous sodium hydroxide and extracted with chloroform. The organic layers were combined, washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 10/1 (v/v)) to give the title compound as a pale yellow oil (804 mg, yield 7 1%). REFERENCE SYNTHETIC EXAMPLE 9 4-(CvclohexylaminoV1-(r2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolof2,3-blpyridine-5- carbaldehvde 4-(Cyclohexylamino)-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde (273 mg, 1.12 mmol) in N,N-dimethylformamide (3 ml_) was stirred with sodium hydride (55 wt% dispersion in mineral oil, 6 .2 mg, 1.53 mmol) for 1 hour under cooling with ice. The reaction mixture was stirred with [2-(chloromethoxy)ethyl]trimethylsilane (260 , 1.47 mmol) at room temperature for one day, and after addition of water, extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (hexane/ ethyl acetate = 5/1 (v/v)) to give the title compound as a pale yellow oil (265 mg, yield 63%). REFERENCE SYNTHETIC EXAMPLE 1 0 (4-(Cvclohexylamino)-1 -(r2-(trimethylsilyl)ethoxylmethyl)-1 H-pyrrolor2,3-blPyridin-5-yl) methanol 4-(Cyclohexylamino)-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine- 5-carbaldehyde ( 104 mg, 0.279 mmol) in methanol (3 mL) was stirred with sodium borohydride (15.8 mg, 0.418 mmol) at room temperature for 2 hours, after addition of water, the reaction mixture was extracted with chloroform twice, and the organic layers were combined, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting pale yellow oil containing the title compound was used for the next step without further purification. REFERENCE SYNTHETIC EXAMPLE 1 1 1-Cvclohexyl-7-(r2-(trimethylsilyl)ethoxy1methyl)-1 ,2.4,7- tetrahvdropyrrolor3'.2':5,61pyridor4,3-din ,31oxazine [4-(Cyclohexylamino)-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin- 5-yl)methanol (38 mg, 0.10 mmol) and aqueous formaldehyde (35 wt%, 0.6 mL, 8 mmol) in ethanol (2 mL) were stirred at 75°C for 1 hour. The reaction mixture was then stirred with acetic acid ( 1 mL) at 75°C for 1 hour, allowed to cool to room temperature, and after addition of saturated aqueous sodium hydrogen carbonate, extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 2/1 (v/v)) to give the title compound as a colorless oil ( 19.8 mg, yield 51%). REFERENCE SYNTHETIC EXAMPLE 12 5-(Aminomethvn-N-cvclohexyl-1-(r2-(trimethylsilyl)ethoxylmethyll-1 H-pyrrolof2,3- blpyridin-4-amine (4-(Cyclohexylamino)-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin- 5-yl)methanol (870 mg, 2,31 mmol) obtained in Reference Synthetic Example 1 10, phthalimide (681 mg, 4.63 mmol) and triphenylphosphine ( 1 .21 , 4.63 mmol) in tetrahydrofuran (10 mL) were stirred at room temperature for 30 minutes and then stirred with diisopropyl azodicarboxylate (936 mg, 4.63 mmol) for one day. The reaction mixture was concentrated under reduced pressure, and after addition of water, extracted with ethyl acetate. The organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ ethyl acetate = 10/1 (v/v)) to remove triphenylphosphine oxide. The resulting crude product was dissolved in ethanol (30 mL) and stirred with hydrazine monohydrate ( 1 .0 mL, 12 mmol) at 80°C for 1 hour and allowed to cool to room temperature. The precipitated solid was collected by filtration and washed with ethanol and chloroform. The filtrate and the washings were combined and concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (chloroform / methanol = 20/1 (v/v) to give the title compound as a colorless oil (513 mg, yield 59%). REFERENCE SYNTHETIC EXAMPLE 1 13 1-Cvclohexyl-7-([2-(trimethylsilyl)ethoxy1methyl)-3,4-dihvdro-1 HPyrrolof3', 2':5,6lpyridor4,3-dlpyrimidin-2(7H)-one 5-(Aminomethyl)-N-cyclohexyl-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridin-4-amine (127 mg, 0.339 mmol) in dichloromethane was stirred with 1, 1 '- carbonyldiimidazole (65.9 mg, 0.407 mmol) at 60°C for 2 hours. The reaction mixture was concentrated under reduced pressure and, after addition of water, extracted with chloroform. The organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give the title compound as a colorless oil (93.2 mg, yield 69%). REFERENCE SYNTHETIC EXAMPLE 14 1-Cvclohexyl-1 ,4-dihvdro-7-(i2-(trimethylsilyl)ethoxy1methyl}-pyrrolor3',2':5,61pyrido[3,4- elpyrimidine 5-(Aminomethyl)-N-cyclohexyl-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridin-4-amine (104 mg, 0.278 mmol) obtained in Reference Synthetic Example 12 in ethyl orthoformate ( 1 mL) was reacted at 180°C for 30 minutes under microwave irradiation and allowed to cool to room temperature. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: hexane/ ethyl acetate = 1/1 (v/v) to give the title compound as a pale yellow oil (48.8 mg, yield 45%). REFERENCE SYNTHETIC EXAMPLE 1 15 2,3-Dihvdro-1 H-pyrrolof2,3-blpyridine 1H-Pyrrolo[2,3-b]pyridine (8.78 g, 74.3 mmol) and 5% palladium-carbon in a mixture of triethylamine (5 mL) and formic acid (30 mL) was stirred at 80°C for 4 days. The reaction mixture was allowed to cool to room temperature and filtered, and the filtrate was concentrated under reduced pressure. The resulting residue was adjusted to pH 12 with 6 M aqueous sodium hydroxide and stirred at 65°C for 5 hours. The reaction mixture was allowed to cool to room temperature and extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/2 ethyl acetate / methanol = 20/1 (v/v)) to give the title compound as a pale yellow solid (2.15 g, yield 24%). REFERENCE SYNTHETIC EXAMPLE 16 5-Bromo-2,3-dihvdro-1 H-pyrrolor2,3-b1pyridine 2,3-Dihydro-1 H-pyrrolo[2,3-b]pyridine (4.40 g, 36.6 mmol) in a mixture of pyridine (4.4 mL) and dichloromethane (20 mL) was gradually added dropwise to bromine (7.00 g , 43.8 mmol) in dichloromethane (20 mL) cooled to 0°C, and the resulting reaction mixture was stirred at 0°C for 20 minutes, after addition of saturated aqueous sodium thiosulfate, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ ethyl acetate = 1/1 0/1 (v/v)) to give the title compound as a brown solid (2.83 g, yield 39%). REFERENCE SYNTHETIC EXAMPLE 3 17 5-Bromo-1 H-pyrroloF2,3-b1pyridine 5-Bromo-2,3-dihydro-1 H-pyrrolo[2,3-b]pyridine (2.83 g, 14.2 mol) and manganese dioxide (5.0 g, 58 mmol) in chloroform (30 mL) were stirred at 65°C for 3 hours. The reaction mixture was allowed to cool to room temperature and filtered, and the solid was washed with chloroform, and the filtrate and the washings were combined and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ ethyl acetate / chloroform = 2/1/1 1/1/0 (v/v/v)) to give the title compound as a brown solid (2.14 g, yield 76%). REFERENCE SYNTHETIC EXAMPLE 1 18 5-Bromo-1 H-pyrrolof2,3-b1pyridine 7-oxide m-Chloroperbenzoic acid (25 wt% water content, 322 mg, 1.40 mmol) in ethyl acetate (5 mL) was gradually added dropwise to 5-bromo-1 H-pyrrolo[2,3-b]pyridine ( 184 mg, 0.934 mmol) in ethyl acetate (10 mL), and the reaction mixture was stirred at room temperature for 6 hours. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was mixed with a mixture of ethyl acetate / hexane = 1/1 (v/v), and the solid was collected by filtration, washed with hexane and dried under reduced pressure to give the title compound as a light brown solid (150 mg, yield 75%). REFERENCE SYNTHETIC EXAMPLE 19 5-Bromo-4-chloro-1 -([2-(trimethylsilyl)ethoxy1methyl|-1 H-pyrrolo[2,3-b1pyridine 5-Bromo-1 H-pyrrolo[2,3-b]pyridine 7-oxide (150 mg, 0.704 mmol) in N,Ndimethylformamide (2 mL) was heated to 50°C and stirred with methanesulfonyl chloride (58 L, 0.75 mmol) at 70°C for 2 hours and allowed to cool to room temperature. After addition of saturated aqueous sodium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in N,N-dimethylformamide (2 mL), cooled to 0°C, mixed with sodium hydride (55 wt% dispersion in mineral oil, 45 mg, 1.03 mmol) and [2- (chloromethoxy)ethyl]trimethylsilane (186 , 1.05 mmol) and stirred at room temperature for 3 hours. After addition of saturated aqueous sodium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 20/1 (v/v)) to give the title compound as a pale yellow oil (158 mg, yield 62%). REFERENCE SYNTHETIC EXAMPLE 20 5-Bromo-N-cvclohexyl-1-(f2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolof2,3-b1pyridin-4- amine 5-Bromo-4-chloro-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine (150 mg, 0.415 mmol) and cyclohexylamine ( 1 mL, 9 mmol) in ethylene glycol ( 1 mL) were stirred at 200°C for 2 hour under microwave irradiation. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium chloride, extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ ethyl acetate = 10/1 (v/v)) to give the title compound as an orange oil (141 mg, yield 80%). REFERENCE SYNTHETIC EXAMPLE 2 1 1-(4-(Cvclohexylamino)-1 -(i2 -(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolof2,3-b]pyridin-5- vOethanone 5-Bromo-N-cyclohexyl-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin- 4-amine ( 160 mg, 0.377 mmol) in toluene (3 mL) was stirred with bis(triphenylphosphine)palladium (II) dichloride (35 mg, 0.050 mmol) and tributyl(1 - ethoxyvinyl)tin (382 L, 1.13 mmol) at 75°C for 3 hours. The reaction mixture was allowed to cool to room temperature and stirred with 1 M hydrochloric acid (2 mL) and potassium fluoride (100 mg, 1.73 mmol) at room temperature for 30 minutes. The reaction mixture was filtered, and the solid was washed with ethyl acetate. The filtrate and the washings were mixed with water and extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 20/1 5/1 (v/v)) to give the title compound as a yellow oil (58 mg, yield 40%). REFERENCE SYNTHETIC EXAMPLE 1 22 1-(4-(Cvclohexylamino)-1 -([2-(trimethylsilyl)ethoxylmethyl)-1 H-pyrrolof2 3-blpyridin-5- vDethanol 1-(4-(Cyclohexylamino)-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridin-5-yl)ethanone (13 mg, 0.034 mmol) in methanol ( 1 mL) was stirred with sodium borohydride (30 mg, 0.79 mmol) at room temperature for 1 hour and at 60°C for another 5 hours. The reaction mixture was allowed to cool to room temperature and, after addition of water, extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 4/1 3/1 (v/v)) to give the title compound as a colorless oil (9.1 mg, yield 70%). REFERENCE SYNTHETIC EXAMPLE 13 23 1-Cvclohexyl-4-methyl-7 -(f2-(trimethylsilvnethoxy1methyl)-1 .2,4,7- tetrahvdropyrrolof3',2':5,6lpyrido[4,3-d1f1 ,31oxazine 1-(4-(Cyclohexylamino)-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridin-5-yl)ethanol (9 mg, 0.02 mmol) and aqueous formaldehyde (35 wt%, 0.3 mL, 4 mmol) in ethanol ( 1 mL) were stirred at 75°C for 1 hour. The reaction mixture was allowed to cool to room temperature and, after addition of water, extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting pale yellow oil (9 mg) containing the title compound was used for the next step without further purification. REFERENCE SYNTHETIC EXAMPLE 13 24 1-Cvclohexyl-7 - r2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolof2,3-h1[1 ,61naphthyridin- 4(7H)-one 1-(4-(Cyclohexylamino)-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridin-5-yl)ethanone (25 mg, 0.065 mmol) obtained in Reference Synthetic Example 13 2 1 in ,-dimethylformamide dimethyl acetal (0.5 mL) was stirred at 180°C for 3 hours under microwave irradiation. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure, and the resulting residue was dissolved in tetrahydrofuran ( 1 mL) and stirred with 1 M hydrochloric acid ( 1 mL) at 80°C for 1 hour. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium hydrogen carbonate, extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate / methanol = 1/1/0 0/10/1 (v/v/v)) to give the title compound as a colorless oil (13.6 mg, yield 53%). REFERENCE SYNTHETIC EXAMPLE 25 4-Chloro-5-(methylsulfonyl)-1-(triisopropylsilyl)-1 H-pyrrolo[2,3-b1pyridine s-Butyllithium - hexane/cyclohexane solution ( 1 .06 M, 0.700 mL, 0.742 mmol) was gradually added dropwise to 4-chloro-1-(triisopropylsilyl)-1 H-pyrrolo[2,3-b]pyridine (100 mg, 0.324 mmol) obtained in Reference Synthetic Example 1 6 in tetrahydrofuran ( 1 mL) cooled to -78°C, and the reaction mixture was stirred at -78°C for 30 minutes and stirred with dimethyl disulfide (30 pL, 0.33 mmol) at -78°C for 30 minutes. After addition of 1 M aqueous sodium hydroxide, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in ethanol (2 mL) and stirred with ammonium molybdate tetrahydrate (40 mg, 0.032 mmol) and aqueous hydrogen peroxide (30 wt%, 132 pL, 1.29 mmol) at room temperature for 5 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 20/1 5/1 (v/v)) to give the title compound as a pale yellow oil (61 .4 mg, yield 49%). REFERENCE SYNTHETIC EXAMPLE 1 26 N-Cvclohexyl-5-(methylsulfonyl)-1 H-pyrrolo[2,3-b1pyridin-4-amine 4-Chloro-5-(methylsulfonyl)-1-(triisopropylsilyl)-1 H-pyrrolo[2,3-b]pyridine (61 mg, 0.16 mmol) in cyclohexylamine (200 pL, 1.74 mmol) was stirred with N,Ndiisopropylethylamine (40 pL, 0.23 mmol) at 120°C for 30 minutes The reaction mixture was allowed to cool to room temperature and, after addition of water, extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate =20/1 5/1 (v/v)) to give the title compound as a colorless solid (7.0 mg, yield 15%). REFERENCE SYNTHETIC EXAMPLE 13 27 N-Cvclohexyl-5-(methylsulfonyl)-1-{f2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolof2,3- blpyridin-4-amine N-Cyclohexyl-5-(methylsulfonyl)-1 H-pyrrolo[2,3-b]pyridin-4-amine (7.0 mg, 0.024 mmol) in N,N-dimethylformamide ( 1 mL) was stirred with sodium hydride (55 wt% dispersion in mineral oil, 3.0 mg, 0.069 mmol) and [2- (chloromethoxy)ethyl]trimethylsilane (10 pL, 0.057 mmol) at room temperature for 2 hours. After addition of saturated aqueous sodium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 10/1 3/1 (v/v)) to give the title compound as a colorless oil (6.1 mg, yield 60%). REFERENCE SYNTHETIC EXAMPLE 13 28 1-Cvclohexyl-7-{r2-(trimethylsilyl)ethoxy1methyl)-1 ,4-dihvdropyrrolof3',2':5.61pyridor3,4- bi ,41thiazine-4,4(7H)-dione N-Cyclohexyl-5-(methylsulfonyl)-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-p b]pyridin-4-amine (6.1 mg, 0.014 mmol) in ,-dimethylformamide dimethyl acetal (2.5 ml_) was stirred at 170°C for 3 hours under microwave irradiation. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure. The resulting residue was dissolved in tetrahydrofuran ( 1 ml_) and stirred with 1 M hydrochloric acid ( 1 mL) at 80°C for 1 hour. The reaction mixture was allowed to cool to room temperature and, after addition of water, extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting pale yellow oil (8.5 mg) containing the title compound was used for the next step without further purification. REFERENCE SYNTHETIC EXAMPLE 29 4-(Cvclohexylamino)-1-|[2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolo[2,3-blpyridine-5- carboxylic acid 4-(Cyclohexylamino)-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine- 5-carbaldehyde (380 mg, .02 mmol) obtained in Reference Synthetic Example 3 9 in acetic acid (4 mL) was stirred with sulphamic acid (150 mg, 1.54 mmol) and 2-methyl-2- butene (500 , 4.71 mmol) under cooling with ice, and then sodium chlorite (100 mg, 1.11 mmol) in water (0.5 mL) was added dropwise, and the resulting reaction mixture was stirred at room temperature for 1 hour. Sodium chlorite (30 mg, 0.33 mmol) in water (0.3 mL) was further added dropwise, and the resulting reaction mixture was stirred for 1 hour. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/ 1 0/1 (v/v)) to give the title compound as a pale yellow oil (207 mg, yield 52%). REFERENCE SYNTHETIC EXAMPLE 1 30 4-(Cvclohexylamino )-1 -f[2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolof2,3-blpyridine-5- carboxamide 4-(Cyclohexylamino )-1 -{[2-(trimethylsilyl)ethoxy]methyl }-1 H-pyrrolo[2,3-b]pyridine- 5-carboxylic acid (100 mg, 0.257 mmol) in dichloromethane (2 mL) was stirred with 1-(3- dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (10 mg, 0.052 mmol), Nhydroxybenzotriazole (50 mg, 0.37 mmol) and 7 M ammonia - methanol solution (0.2 mL, 1.4 mmol) at room temperature for one day. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 0/1 (v/v)) to give the title compound as a pale yellow amorphous (7 1. 1 mg, yield 7 1%). REFERENCE SYNTHETIC EXAMPLE 5 3 1 4-(Cvclohexylamino)-N-formyl -1-(r2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolof2.3- blpyridine-5-carboxamide 4-(Cyclohexylamino )-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine- 5-carboxamide (45 mg, 0.12 mmol) in triethyl orthoformate (2 mL) was stirred at 120°C for one day. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/ 1 0/1 (v/v)) to give the title compound as a pale yellow amorphous (12 .4 mg, yield 27%). REFERENCE SYNTHETIC EXAMPLE 1 32 1-Cvclohexyl-7-(r2-(trimethylsilvnethoxylmethyll-1 H-pyrrolor3\2':5.61Pyridor4,3- d1pyrimidin-4(7H)-one 4-(Cyclohexylamino)-N-formyl-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[^ b]pyridine-5-carboxamide (12.4 mg, 0.0311 mmol) in N-methyl-2-pyrrolidinone (0.5 mL) was stirred at 200°C for 30 minutes under microwave irradiation. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous ammonium chloride, extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a pale yellow amorphous (9.2 mg, yield 74%). REFERENCE SYNTHETIC EXAMPLE 33 1-(4-Chloro-1 -{r2-(trimethylsilyl)ethoxylmethyl)-1 H-pyrrolof2,3-blpyridin-5-yl)ethanone 5-Bromo-4-chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine (47 mg, 0.13 mmol) obtained in Reference Synthetic Example 1 19 in toluene ( 1 mL) was stirred with bis(triphenylphosphine)palladium (II) dichloride (10 mg, 0.014 mmol) and tributyl(1 -ethoxyvinyl)tin (50 L, 0.15 mmol) at 120°C for 4 hours. The reaction mixture was allowed to cool to room temperature and stirred with water (2 mL) and potassium fluoride (100 mg, 1.73 mmol) at room temperature for 1 hour. The reaction mixture was filtered, and the solid was washed with ethyl acetate. The filtrate and the washings were mixed with water and extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and filtered. The filtrate was stirred with hydrogen chloride - methanol solution (10 wt%, 0.1 mL) at room temperature for 10 minutes. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (hexane / ethyl acetate = 10/1 2/1 (v/v)) to give the title compound as a pale yellow oil (20 mg, yield 47%). REFERENCE SYNTHETIC EXAMPLE 3 34 rac-1 -(4-([(3R,4R)-1 -Benzyl-4-methylpiperidin-3-vnamino)-1 - 2- (trimethylsilvnethoxy1methyl)-1 H-pyrrolo[2,3-blpyridin-5-yl)ethanone 1-(4-Chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5- yl)ethanone ( 15 mg, 0.46 mmol) and rac-(3R,4R)-1-benzyl-4-methylpiperidin-3-amine (34 mg, 0.17 mmol) obtained in Reference Synthetic Example 13 3 in ethylene glycol (3 mL) was stirred with ,-diisopropylethylamine ( 10 pL, 0.057 mmol) at 200°C for 1 hour under microwave irradiation. The reaction mixture was allowed to cool to room temperature and stirred with methanol (2 mL) and 1 M hydrochloric acid ( 1 mL) at 50°C for 30 minutes. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium hydrogen carbonate, extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 0/ 1 4/1 (v/v)) to give the title compound as a yellow oil (7.0 mg, yield 3 1%). REFERENCE SYNTHETIC EXAMPLE* 35 rac-1 -f(3R.4R)-1 -Benzyl-4-methylpiperidin-3-yll-7-(r2-(trimethylsilyl)ethoxylmethyl)-1 HPyrrolor2.3- hlf1 .61naphthyridin-4(7H)-one rac-1 -(4-{[(3R,4R)-1 -Benzyl-4-methylpiperidin-3-yl]amino}-1 -{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5-yl)ethanone (20 mg, 0.041 mmol) in ,-dimethylformamide dimethyl acetal ( 1 mL) was stirred at 170°C for 6 hours under microwave irradiation. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure, and the resulting residue was dissolved in tetrahydrofuran ( 1 mL) and stirred with 1 M hydrochloric acid ( 1 mL) at 80°C for 1 hour. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium hydrogen carbonate, extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate / methanol = 1/1/0 0/5/1 (v/v/v)) to give the title compound as a yellow oil (6.1 mg, yield 30%). REFERENCE SYNTHETIC EXAMPLE 13 36 rac-1 -r(3R,4R)-4-Methylpiperidin-3-yll-7-(r2-(trimethylsilyl)ethoxylmethyl)-1 H-pyrrolof2,3- h ,61naphthyridin-4(7H)-one rac-1-[(3R,4R)-1-Benzyl-4-methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}- 1H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)-one (98 mg, 0.20 mmol) and 5% palladiumcarbon (65 mg) in methanol (2 mL) were stirred at room temperature for 2 hours under a hydrogen atmosphere, then at 40°C for 5 hours and at room temperature for one day. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give the title compound as a pale yellow amorphous (76.8 mg, yield 95%). REFERENCE SYNTHETIC EXAMPLE 1 37 rac-1 -r(3R,4R)-1 -(lsobutylsulfonyl)-4-methylpiperidin-3-yl1-7 -(f2- (trimethylsilvnethoxylmethyl)-1 H-pyrrolo[2,3 -hin,61naphthyridin-4(7H)-one rac-1-[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one (23 mg, 0.056 mmol) in dichloromethane (2 mL) was mixed with N,N-diisopropylethylamine (30 L, 0.17 mmol) and 2- methylpropane-1-sulfonyl chloride (12 L, 0.092 mmol) under cooling with ice and stirred at room temperature for 2 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate / methanol = 1/1/0 0/10/1 (v/v/v)) to give the title compound as a pale pink solid (18.3 mg, yield 62%). REFERENCE SYNTHETIC EXAMPLE 3 38 rac-4-(f(3R 4R)-1-Benzyl-4-methylpiperidin-3-yl1amino)-1 H-pyrrolor2,3-b1pyridine-5- carbaldehvde 4-Chloro-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde (247 mg, 1.36 mmol) obtained in Reference Synthetic Example 1 7 and rac-(3R,4R)-1-benzyl-4-methylpiperidin-3-amine (700 mg, 3,42 mmol) obtained in Reference Synthetic Example 13 3 in ethylene glycol (3 mL) were stirred at 180°C for 3 hours under microwave irradiation. The reaction mixture was allowed to cool to room temperature and, after addition of water and 1 M aqueous sodium hydroxide, extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was stirred with 1,4-dioxane (5 mL), 4 M hydrogen chloride - 1,4- dioxane solution (10 mL) and water (2 mL) at room temperature for one day. The reaction mixture was concentrated under reduced pressure, adjusted to pH 9 or above with 1M aqueous sodium hydroxide and extracted with chloroform and water, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a brown oil (154 mg, yield 33%). REFERENCE SYNTHETIC EXAMPLE 13 39 rac-4-lf(3R.4R)-1 -Benzyl-4-methylpipericlin-3-yllamino)-1 -If2- (trimethylsilyl)ethoxy1methyl)-1 H-pyrrolo[2,3-b1pyridine-5-carbaldeh rac-4-{[(3R,4R)-1 -Benzyl-4-methylpiperidin-3-yl]amino}-1 H-pyrrolo[2,3-b]pyridine- 5-carbaldehyde (118 mg, 0.338 mmol) in N,N-dimethylformamide (3 m ) was cooled to 0°C and stirred with sodium hydride (55 wt% dispersion in mineral oil, 1 6 mg, 0.586 mmol) for 30 minutes and then with [2-(chloromethoxy)ethyl]trimethylsilane (104 _. 0.586 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a brown oil (67.5 mg, yield 42%). REFERENCE SYNTHETIC EXAMPLE 13 40 rac-(4-(r(3R,4R)-1 -Benzyl-4-methylpiperidin-3-vnamino)-1-([2- (trimethylsilvnethoxylmethyl)-1 H-pyrrolor2,3-b1pyridin-5-yl)methanol rac-4-{[(3R,4R)-1 -Benzyl-4-methylpiperidin-3-yl]amino}-1-{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde (112 mg, 0.234 mmol) in methanol was stirred with sodium borohydride (13.3 mg, 0.351 mmol) at room temperature for 1 hour. The reaction mixture was concentrated under reduced pressure and, after addition of water, extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a colorless oil (55 mg, yield 49%). REFERENCE SYNTHETIC EXAMPLE 1 4 1 rac-1-r(3R,4R)-1 -Benzyl-4-methylpiperidin-3-yll-7-(f2-(trimethylsilvnethoxy1methyl)- 1.2.4.7-tetrahvdropyrrolor3',2':5,61pyridor4,3-d1f1 ,31oxazine rac-(4-{[(3R,4R)-1 -Benzyl-4-methylpiperidin-3-yl]amino}-1-{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5-yl)methanol (55 mg, 0.1 1 mmol) was stirred with formic acid (2 mL) and acetic acid (200 L) at 75°C for 4 hours. The reaction mixture was concentrated under reduced pressure and, after addition of water, extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 2/1 (v/v)) to give the title compound (34.3 mg, yield 6 1%). REFERENCE SYNTHETIC EXAMPLE 1 42 6-Bromo-3H-imidazo[4,5-b1pyridine 2,3-Diamino-5-bromopyridine (4.10 g, 2 1.8 mmol) in formic acid (25 mL) was stirred at 100°C for 4 hours. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure, and the resulting residue was mixed with water and adjusted to pH 8 or above with saturated aqueous sodium hydrogen carbonate. The precipitated solid was collected by filtration, washed with water and chloroform and dried under reduced pressure to give the title compound as a dark brown solid (4.13 g, yield 96%). REFERENCE SYNTHETIC EXAMPLE" 43 6-Bromo-3H-imidazo[4,5-b1pyridine 4-oxide m-Chloroperbenzoic acid (25 wt% water content, 2.77 g, 12.0 mmol) was gradually added dropwise to 6-bromo-3H-imidazo[4,5-b]pyridine ( .58 mg, 7.98 mmol) in ethyl acetate (15 mL), and the reaction mixture was stirred at room temperature for one day. The precipitated solid was collected by filtration and washed with ethyl acetate and diethyl ether and dried under reduced pressure to give the title compound as a pale yellow solid ( 1 .67 g, yield 98%). REFERENCE SYNTHETIC EXAMPLE 44 6-Bromo-7-chloro-3H-imidazo[4,5-b1pyridine 6-Bromo-3H-imidazo[4,5-b]pyridine 4-oxide ( 1 .88 g, 8.82 mmol) in N,Ndimethylformamide (12 ml_) was heated to 50°C, mixed with methansulfonyl chloride (8.00 ml_, 03 mmol) and stirred at 73°C for 3 hours. The reaction mixture was cooled with ice and gradually poured into saturated aqueous sodium hydrogen carbonate (75 ml_), and the precipitated solid was collected by filtration, washed with water and chloroform and dried under reduced pressure to give the title compound as a dark brown solid ( 1 .07 g, yield 52%). REFERENCE SYNTHETIC EXAMPLE 45 6-Bromo-7-chloro-3-(r2-(trimethylsilyl)ethoxy1methyl)-3H-imidazof4,5-blpyridine 6-Bromo-7-chloro-3H-imidazo[4,5-b]pyridine ( 1 .07 g, 4.60 mmol) in N,Ndimethylformamide (12 mL) was cooled to 0°C, mixed with sodium hydride (55 wt% dispersion in mineral oil, 300 mg, 6.88 mmol) and [2- (chloromethoxy)ethyl]trimethylsilane (12.0 mL, 6.78 mmol) and stirred at room temperature for 3 hours. After addition of saturated aqueous sodium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (hexane / ethyl acetate = 10/1 5/1 (v/v)) to give the title compound as a yellow oil (640 mg, yield 38%). REFERENCE SYNTHETIC EXAMPLE1 46 1- 7-Chloro-3-(f2-(trimethylsilyl)ethoxylmethyl)-3H-imidazor4,5-b1pyridin-6-yl )ethanone 6-Bromo-7-chloro-3-{[2-(trimethylsilyl)ethoxy]methyl}-3H-imidazo[4,5-b]pyridine (379 mg, 1.05 mmol) in toluene (6 mL) was stirred with bis(triphenylphosphine)palladium(ll) dichloride (106 mg, 0.151 mmol) and tributyl(1- ethoxyvinyl)tin (435 mg, 1.21 mmol) at 120°C 4 hours. The reaction mixture was allowed to cool to room temperature and stirred with water (20 mL) and potassium fluoride (0.5 g) at room temperature for 1 hour. The reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and filtered. The filtrate was stirred with hydrogen chloride - methanol solution ( 10 wt%, 4 mL) at room temperature for 10 minutes. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (hexane / ethyl acetate = 5/1 3/1 (v/v)) to give the title compound as a yellow solid (89.6 mg, yield 26%). REFERENCE SYNTHETIC EXAMPLE1 47 1-r7-(Cvclohexylamino)-3-(r2-(trimethylsilyl)ethoxy1methyl)-3H-imidazor4,5-blpyridin-6- yllethanone 1-[7-Chloro-3-{[2-(trimethylsilyl)ethoxy]methyl}-3H-imidazo[4,5-b]pyridin-6- yl]ethanone (89.6 mg, 0.275 mmol) and cyclohexylamine (214 mg, 2.1 6 mmol) in ethylene glycol (2 mL) were stirred at 180°C for 1 hour under microwave irradiation. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium chloride, extracted with chloroform. The organic layer was stirred with 2 M hydrochloric acid (12 mL) at room temperature for 1 hour. The reaction mixture was basified with 0 M aqueous sodium hydroxide and extracted with chloroform, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a dark brown oil (88.9 mg, yield 83%). REFERENCE SYNTHETIC EXAMPLE 5 48 9-Cvclohexyl-3 -(r2 -(trimethylsilyl)ethoxylmethyl)-3H-imidazof4 5-hiri ,61naphthyridin- 6(9H)-one 1-[7-(Cyclohexylamino)-3-{[2-(trimethylsilyl)ethoxy]methyl}-3H-imidazo[4,5- b]pyridin-6-yl]ethanone (88.9 mg, 0.229 mmol) in ,-dimethylformamide dimethyl acetal (2.0 mL) was stirred at 180°C for 5 hours. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure, and the resulting residue was dissolved in tetrahydrofuran (5 mL) and stirred with 1 M hydrochloric acid (2 mL) at 80°C for 1 hour. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium hydrogen carbonate, extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate / methanol = 1/1/0 0/10/1 (v/v/v)) to give the title compound as a yellow solid (57.5 mg, yield 63%). REFERENCE SYNTHETIC EXAMPLE 1 49 1-(3-Bromo-4-chloro-1 -U2-(trimethylsilyl)ethoxy1methylH H-pyrrolo[2,3-blpyridin-5- vDethanone 1-(4-Chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5- yl)ethanone (91 mg, 0.28 mmol) obtained in Reference Synthetic Example 33 in dichloromethane (3 mL) was mixed with N-bromosuccinimide (75 mg, 0.42 mmol) under cooling with ice and stirred at room temperature for 2 hours. After addition of saturated aqueous sodium thiosulfate, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 5/1 (v/v)) to give the title compound as a colorless oil (61 .0 mg, yield 54%). REFERENCE SYNTHETIC EXAMPLE 50 rac-1 -(4-(r(3R,4R)-1 -Benzyl-4-methylpiperidin-3-yl1amino)-3-bromo-1 - 2- (trimethylsilyl)ethoxy1methyll-1 H-pyrrolor2,3-blpyridin-5-yl)ethanone 1-(3-Bromo-4-chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5- yl)ethanone (61 mg, 0.1 5 mmol) was stirred with rac-(3R,4R)-1-Benzyl-4- methylpiperidin-3-amine (85 mg, 0.42 mmol) obtained in Reference Synthetic Example 3 and N,N-diisopropylethylamine (50 L, 0.29 mmol) at 130°C for 5 hours. The reaction mixture was allowed to cool to room temperature and purified by silica gel column chromatography (hexane / ethyl acetate = 10/1 (v/v)) to give the title compound as a pale yellow oil (28.7 mg, yield 33%). REFERENCE SYNTHETIC EXAMPLE 5 1 rac-1 -f(3R,4R)-1 -Benzyl-4-methylpiperidin-3-yll-9-bromo-7 -{r2- arimethylsilyl)ethoxy1methyl)-1 H-pyrrolor2,3 -hiri ,61naphthyridin-4-(7H)-one The reactions in Reference Synthetic Example 6 35 were carried out in substantially the same manners except that rac-1 -(4-{[(3R,4R)-1 -benzyl-4- methylpiperidin-3-yl]amino}-3-bromo-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridin-5-yl)ethanone was used instead of rac-1 -(4-{[(3R,4R)-1 -benzyl-4- methylpiperidin-3-yl]amino}-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin5- yl)ethanone to give the title compound as a colorless oil (1 .3 mg, yield 45%). REFERENCE SYNTHETIC EXAMPLE 1 52 1-(3,4-Dichloro-1 -(r2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolor2,3-b1pyridin-5- vQethanone 1-(4-Chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5- yl)ethanone (80 mg, 0.25 mmol) obtained in Reference Synthetic Example 1 33 in N,Ndimethylformamide (2 ml_) was stirred with N-chlorosuccinimide (66 mg, 0.49 mmol) at 80°C for 3 hours. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium chloride, extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 10/1 5/1 (v/v)) to give the title compound as a colorless solid (23.8 mg, yield 27%). REFERENCE SYNTHETIC EXAMPLE 13 53 rac-1 - 4-f (3R 4R -1-Benzyl-4-methylpiperidin-3-vnamino|-3-chloro-1 - f2- (trimethylsilyl)ethoxy1methyl)-1 H-pyrrolor2,3-blpyridin-5-yl)ethanone The reactions in Reference Synthetic Example 13 50 were carried out in substantially the same manners except that 1-(3,4-dichloro-1-{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5-yl)ethanone was used instead of 1-(3-bromo-4-chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5- yl)ethanone to give the title compound as a pale yellow oil (13.4 mg, yield 39%). REFERENCE SYNTHETIC EXAMPLE 3 54 rac-1 -[(3R,4R)-1 -Benzyl-4-methylpiperidin-3 -vn-9-chloro-7 -(r2- (trimethylsilyl)ethoxylmethyl)-1 H-pyrrolof2,3 -h .61naphthyridin-4(7H)-one The reactions in Reference Synthetic Example 35 were carried out in substantially the same manners except that rac-1 -(4-{[(3R,4R)-1 -benzyl-4- methylpiperidin-3-yl]amino}-3-chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridin-5-yl)ethanone was used instead of rac-1 -(4-{[(3R,4R)-1 -benzyl-4- methylpiperidin-3-yl]amino}-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin- 5-yl)ethanone to give the title compound as a colorless oil (5.6 mg, yield 42%). REFERENCE SYNTHETIC EXAMPLE 6 55 4-Chloro-1 -(f2-(trimethylsilyl)ethoxylmethyl)-1 H-pyrrolof2,3-blpyridine-5-carbaldehvde 4-Chloro-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde (550 mg, 3.05 mmol) obtained in Reference Synthetic Example 7 in N,N-dimethylformamide (5 mL) was stirred with sodium hydride (60 wt% dispersion in liquid paraffin, 150 mg, 3.75 mmol) for 10 minutes under cooling with ice and then stirred with [2-(chloromethoxy)ethyl]trimethylsilane (650 , 3.67 mmol) at room temperature for 30 minutes. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 5/1 (v/v)) to give the title compound as a colorless solid (815 mg, yield 86%). REFERENCE SYNTHETIC EXAMPLE 56 1-(4-Chloro-1 -(i2-(trimethylsilyl)ethoxy1methyll-1 H-pyrrolo[2,3-blpyridin-5-vQpropan-1 -ol 4-Chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-5- carbaldehyde (117 mg, 0.360 mmol) in tetrahydrofuran (2 mL) was mixed with ethylmagnesium bromide - tetrahydrofuran solution ( 1 .0 M, 1.0 mL, 1.0 mmol) under cooling with ice and stirred at room temperature for one day. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 4/1 (v/v)) to give the title compound as a colorless oil (75.6 mg, yield 62%). REFERENCE SYNTHETIC EXAMPLE 3 57 1-(4-Chloro-1 -(r2-(trimethylsilyl)ethoxylmethyl)-1 H-pyrrolo| 2,3-b1pyridin-5-yl)propan-1 - one 1-(4-Chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5- yl)propan-1-ol (75.6 mg, 0.222 mmol) in 1,2-dimethoxyethane (5 mL) was vigorously stirred with manganese dioxide (450 mg, 5.17 mmol) at 60°C for 3 hours and then at 80°C for 3 hours. The reaction mixture was filtered, the solid was washed with chloroform, and the filtrate and the washings were concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 10/1 5/1 (v/v)) to give the title compound as a colorless oil (39.9 mg, yield 53%). REFERENCE SYNTHETIC EXAMPLE 3 58 rac-1 -(4-([(3R,4R)-1 -Benzyl-4-methylpiperidin-3-vnamino)-1 -([2- (trimethylsilvDethoxylmethvD-I H-pyrrolo^.S-blpyridin-S-vDpropan-l -one The reactions in Reference Synthetic Example 3 50 were carried out in substantially the same manners except that 1-(4-chloro-1-{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5-yl)propan-1-one was used instead of 1-(3-bromo-4-chloro-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridin-5-yl)ethanone to give the title compound as a pale yellow oil (40.1 mg, yield 7 1%). REFERENCE SYNTHETIC EXAMPLE 59 rac-1 - r(3R.4R)-1-Benzyl-4-methylpiperidin-3 -vn-3-methyl-7 -(r2- (trimethylsilv0ethoxy1methyl)-1 H-pyrrolo[2,3-h1f1 ,6lnaphthyridin-4(7H)-one The reactions in Reference Synthetic Example 3 35 were carried out in substantially the same manners except that rac-1 -(4-{[(3R,4R)-1 -benzyl-4- methylpiperidin-3-yl]amino}-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin- 5-yl)propan-1-one was used instead of rac-1 -(4-{[(3R,4R)-1-benzyl-4-methylpiperidin-3- yl]amino}-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5-yl)ethanone to give the title compound as a colorless oil (18.0 mg, yield 44%). REFERENCE SYNTHETIC EXAMPLE 3 60 rac-1 -f(3R,4R)-1 -Benzyl-4-methylpiperidin-3 -vn-3-bromo-7 -(r2- (trimethylsilvnethoxy1methylj-1 H-pyrrolor2,3 -hi ,6lnaphthyridin-4(7H)-one rac-1 -[(3R,4R)-1-Benzyl-4-methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}- 1H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)-one (70 mg, 0.14 mmol) obtained in Reference Synthetic Example 1 35 in dichloromethane (5 mL) was mixed with N-bromosuccinimide (25 mg, 0.14 mmol) under cooling with ice and stirred at room temperature for one day and then with N-bromosuccinimide (8 mg, 0.04 mmol) for one day. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane /ethyl acetate = 5/1 2/1 (v/v)) to give a mixture (22.4 mg) containing the title compound. The mixture was used for the next step without further purification. REFERENCE SYNTHETIC EXAMPLE 6 1 rac-2-(f(3R,4R)-4-Methyl-3-(4-oxo-7-^ pyrrolo[2,3 -hi ,61naphthyridin-1 -yl)piperidin-1 -yllsulfonyllbenzonitrile rac-1-[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]meth pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)-one (20 mg, 0.049 mmol) obtained in Reference Synthetic Example 1 36 in dichloromethane (2 ml_) was stirred with 2- cyanobenzenesulfonyl chloride (15 mg, 0.074 mmol) and N,N-diisopropylethylamine (20 _, 0.11 mmol) at room temperature for 1 hour. The reaction mixture was purified by silica gel column chromatography (hexane / ethyl acetate / methanol = 1/1/0 0/ 0/ 1 (v/v/v)) to give the title compound as a colorless solid (24.5 mg, yield 87%). REFERENCE SYNTHETIC EXAMPLES' 62 TO 7 1 The reactions in Reference Synthetic Example 6 1 were carried out in substantially the same manners except that 3-cyanobenzensulfonyl chloride, ethyl chloroformate, 1-isocyanato-2-(trifluoromethyl)benzene, 1-isocyanato-3- (trifluoromethyl)benzene, 2-(trifluoromethyl)benzoyl chloride, 3-(trifluoromethyl)lbenzoyl chloride, 2-(4-fluorophenyl)acetyl chloride, 3-(trifluoromethyl)benzenesulfonyl chloride, 4-(trifluoromethyl)benzoyl chloride or benzyl chloroformate was used instead of 2- cyanobenzenesulfonyl chloride to give the compounds of Reference Synthetic Examples 62 to 7 1. The names, morphologies and yields of the compounds synthesized are shown in Tables 3 to 4. TABLE 3 Rf Compound Name Morpho logy Yi el d rac-3- {[ (3R, 4R) -4-me t h l -3- (4-oxo -7- {[2- (tr i me thy l si l yl ) et ho ] met 62 hyl }-4, 7-d i hydro- lH-pyrrol o [2, 3-h col or l es s 65% ] s ol i d [ 1, 6]naph hy - 1-yl ) i peri d n - l-y l ] sulfony l }benzon itr i l e rac- (3R, 4R) -ethy l 4-me t hy 1- 3- (4- 0 X0 -7- {[2- (t r ime t hy col or l es s 63 1s i 1 1) ethoxy ] me h 1}-4, 7- i hydro 85% - lH-pyrrol o [2, 3-h ] [ 1, oi l 6] naphthyr i d i n- l -yl ) pi per i di ne- l ~carboxylat e rac - (3R, 4R) -4-me hy 1-3- (4-oxo- 7- { [2- (tri met hyl s i l yl ) e hoxy] methy l } -4, 7-di hydro- lH-pyrro l o [2, 3-h] [ 1, col or l es s 64 87% 6] naphthyr i di n-l -yl ) -N- [2- (tri f l u oi l orome thyl) phenyl ] pi peri dine- l-car boxam ide rac - (3R, 4R) -4-me thy 1-3- (4-oxo-7- { [2- (tri met hyl s i l yl ) ethoxy] me thyl} 65 -4, 7- di hydro- lH-pyrro l o [ 2, 3-h] [ 1, col orle s s 98% 6] naphthyr i di n-l -yl ) -N- [3- (tri f l u oi l orome thyl) phenyl ] pi peri di ne- l-car boxam ide rac- l - {(3R, 4R) -4-methyl - 1- [2- (tri f luoromethy l ) benz oy l ] pi e i din-3- col or l es s 66 yl }- 7- {[2- (tr i met hy l s l yl ) ethoxy] 94% methy o i l l }- lH-pyrro l o[2, 3-h] [ 1, 6] nap hthyr i di n-4 (7H) - one rac- 1- (3R, R) -4-me thyl - l - [3- (tri f luoromethy l ) benz oy l ] pi per i din-3- col or l es s 67 y1 } - 7- {[2- (tr i me thyl s i l yl ) ethoxy] 92% methy l }- lH-pyrro l o[2, 3-h] [ 1, 6] nap oi l hthyr i di n-4 (7H) -one rac- l - {(3R, 4R) - 1- [2- (4-f luorophen yl ) a cety l ] -4-methylp i per i di n- 3-yl col or l es s 68 }-7- {[2- (tr ime thy l s i l yl ) et hoxy] me 80% thy l }-lH-pyrro l o [ o i l 2, 3-h] [ 1, 6] napht hyr i din-4 (7H) -one rac- l - ( (3R, 4R) -4-methyl - l - {[3- (t r i f l uoro methyl ) phenyl ] su l fony l }pi p col or les s 69 eri di n-3-y l ) -7- {[2- (trimethy l s i l y 78% l ) ethoxy]methy o i l l }- lH-pyrrol o [2, 3-h ] [ 1, 6]naph t hyr i di n-4 (7H) -one rac- l - {(3R, 4R) -4-methyl - l - [4- (tri f luoromethy l ) benz oy l ] piper i din-3- col or l es s 70 yl} - 7- {[2- (t r i met hyl s i l yl) ethoxy] 69% methy oi l l }- lH-pyrro l o[2, 3-h] [ 1, 6] nap hthyr i di n-4 (7H) -one TABLE b 4 REFERENCE SYNTHETIC EXAMPLE 1 72 Phenyl ,3,4-thiadiazol-2-ylcarbamate 1,3,4-Thiadiazol-2-amine (253 mg, 2.50 mmol) in N,N-dimethylacetamide (3 ml_) was stirred with phenyl chloroformate (392 , 3.13 mmol) at room temperature for one day. Water was added to the reaction mixture, and the precipitated solid was collected by filtration, washed with water and hexane and dried under reduced pressure to give the title compound as a colorless solid (418 mg, yield 76%). REFERENCE SYNTHETIC EXAMPLE 13 73 rac-(3R,4R)-4-Methyl-3-(4-oxo-7 -(r2-(trimethylsilyl)ethoxy1methyl)-4,7-dihvdro-1 Hpyrrolor2,3 -h ,6]naphthyridin-1 -yl)-N-(1 ,3,4-thiadiazol-2-yl)piperidine-1 -carboxamide rac-1-[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one (30.2 mg, 0.0732 mmol) obtained in Reference Synthetic Example 13 36 in tetrahydrofuran (3 mL) was refluxed with phenyl 1,3,4-thiadizol-2-ylcarbamate (19.6 mg, 0.0886 mmol) and triethylamine (17.9 L , 0.128 mmol) for 3 hours under heating. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (ethyl acetate chloroform / methanol = 10/1 (v/v)) to give the title compound as a pale yellow solid (44.0 mg, quantitative yield). REFERENCE SYNTHETIC EXAMPLE* 3 74 Phenyl (3-methylisothiazol-5-vDcarbamate 3-Methylisothiazol-5-amine (156 mg, 1.04 mmol) in pyridine ( 1 .2 mL) was mixed with phenyl chloroformate (260 L, 2.07 mmol) under cooling with ice and stirred at room temperature for 3 hours. The reaction mixture was concentrated under reduced pressure, and after addition of water, extracted with chloroform twice, and the organic layer was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a pale yellow solid (173 mg, yield 71%). REFERENCE SYNTHETIC EXAMPLE 75 rac-(3R,4R)-4-Methyl-N-(3-methylisothiazol-5-yl)-3-(4-oxo-7-([2- (trimethylsilyl)ethoxy1methyl)-4,7-dihvdro-1 H-pyrroloi2.3 -h i ,61naphthyridin-1 - yl)piperidine-1 -carboxamide rac-1 -[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one (29.5 mg, 0.0715 mmol) obtained in Reference Synthetic Example 3 36 in tetrahydrofuran (3 mL) was refluxed with phenyl (3-methylthiazol-5-yl)carbamate (21 .2 mg, 0.0905 mmol) and triethylamine (17.5 pL, 0.125 mmol) for 3 hours under heating. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (ethyl acetate chloroform / methanol = 10/1 (v/v)) to give the title compound as a yellow oil (38.4 mg, yield 97%). REFERENCE SYNTHETIC EXAMPLE b 76 rac-1 -[(3R,4R)-1-(CvclopentanecarbonvO-4-methylpiperidin-3-yll-7-([2- (trimethylsilyl)ethoxy1methyl)-1 H-pyrrolof2.3-h1f1 ,61naphthyridin-4(7H)-one rac-1 -[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one (31 .0 mg, 0.751 mmol) obtained in Reference Synthetic Example 13 36 and triethylamine (30.0 , 0.215 mmol) in tetrahydrofuran (4 mL) were stirred with cyclopentanecarbonyl chloride (20.0 , 0.1 65 mmol) at room temperature for one day. After addition of 1 M aqueous sodium hydroxide, the reaction mixture was extracted with chloroform, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 10/1 v/v)) to give the title compound as a pale yellow oil (44.5 mg, quantitative yield). REFERENCE SYNTHETIC EXAMPLE 13 77 rac-1 -((3R,4R)-4-methyl-1-[3-(trifluoromethyl)ben2vnpiperidin-3-yll-7 - f2- (trimethylsilyl)ethoxy1methyl)-1 H-pyrrolo[2,3 -h ,61naphthyridin-4(7H)-one rac-1-[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one (24.8 mg, 0.0601 mmol) obtained in Reference Synthetic Example b 36 in tetrahydrofuran (4 mL) was stirred sodium hydride (55 wt% dispersion in mineral oil, 49.4 mg, .23 mmol) and 3-(trifluoromethyl)benzyl bromide (38.2 mg, 0.160 mmol) at room temperature for one day. After addition of water under cooling with ice, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate chloroform / methanol = 20/1 (v/v)) to give the title compound as a pale yellow oil (26.8 mg, quantitative yield). REFERENCE SYNTHETIC EXAMPLE 1 78 rac- -((3R.4R)-4-methyl-1-[4-(trifluoromethyl)benzvnpiperidin-3-yl)-7 -(f2- (trimethylsilyl)ethoxylmethyl)-1 H-pyrrolor2,3-h1f1 ,61naphthyridin-4(7H)-one The reactions in Reference Synthetic Example 13 77 were carried out in substantially the same manners except that 4-(trifluoromethyl)benzyl bromide was used instead of 3-(trifluoromethyl)benzyl bromide to give the title compound as a pale yellow oil (32.8 mg, quantitative yield). REFERENCE SYNTHETIC EXAMPLE 13 79 rac-1 -f(3R,4R)-4-methyl-1 -r2-(trifluoromethyl)benzvnpiperidin-3-yl)-7-lf2- (trimethylsilyl)ethoxy1methyl)-1 H-pyrrolo[2,3-h1f1 ,6lnaphthyridin-4(7H)-one rac-1-[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one ( 13.4 mg, 0.0325 mmol) obtained in Reference Synthetic Example 36 in tetrahydrofuran (4 mL) was stirred with sodium hydride (55 wt% dispersion in mineral oil, 30.6 mg, 0.765 mmol) and 2- (trifluoromethyl)benzyl bromide (27.8 mg, 0.11 6 mmol) at room temperature for one day. After addition of water under cooling with ice, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate chloroform / methanol = 20/1 (v/v)) to give the title compound as a pale yellow oil, which was used for the next step. REFERENCE SYNTHETIC EXAMPLE 13 80 rac-3-(r(3R^R)-4-Methyl-3-(4-oxo-7-(r2-(trimethylsilyl)ethoxylmethyl)-4.7-dihvdro-1 Hpyrrolof2,3- hiri ,61naphthyridin-1 -yl)piperidin-1 -yllmethvDbenzonitrile rac-1 -[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one (25.0 mg, 0.0606 mmol) obtained in Reference Synthetic Example 3 36 in tetrahydrofuran (3 ml_) was stirred with sodium hydride (55 wt% dispersion in mineral oil, 15.4 mg, 0.385 mmol) and 3-cyanobenzyl bromide (12.8 mg, 0.0653 mmol) at room temperature for one day. The reaction mixture was further stirred with sodium hydride (55 wt% dispersion in mineral oil, 20.8 mg, 0.520 mmol) and 3-cyanobenzyl bromide (11 .6 mg, 0.0592 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with chloroform twice, and the organic layer was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate chloroform / methanol = 10/1 (v/v)) to give the title compound as a pale yellow oil (32.4 mg, quantitative yield). REFERENCE SYNTHETIC EXAMPLE 3 8 1 rac-2-(f(3R,4RV4-Methyl-3-(4-oxo-7-(r2-(trimethylsilyl)ethoxy1methyl)-4,7-dihvdro-1 Hpyrrolor2,3- hin ,6]naphthyridin-1 -yl)piperidin-1 -yllmethvDbenzonitrile The reactions in Reference Synthetic Example 13 77 were carried out in substantially the same manners except that 2-cyanobenzyl bromide was used instead of 3-(trifluoromethyl)benzyl bromide to give the title compound as a pale yellow oil (31 .4 mg, yield 97%). REFERENCE SYNTHETIC EXAMPLE 13 82 rac-4-(r(3R,4R)-4-Methyl-3-(4-oxo-7-(f2-(trimethylsilyl)ethoxylmethyl)-4.7-dihvdro-1 Hpyrrolo[ 2,3-hiri ,6lnaphthyridin-1 -yl)piperidin-1 -vnmethvDbenzonitrile The reactions in Reference Synthetic Example 3 77 were carried out in substantially the same manners except that 4-cyanobenzyl bromide was used instead of 3-(trifluoromethyl)benzyl bromide to give the title compound as a pale yellow oil (28.5 mg, yield 89%). REFERENCE SYNTHETIC EXAMPLE 3 83 tert-Butyl rac-(3R,4R)-4-methyl-3-(4-oxo-7-(i2-(trimethylsilyl)ethoxy1methyl)-4.7-dihvdro- 1H-pyrrolo[2,3-hin ,61naphthyridin-1 -yl)piperidin-1 -carboxylate rac-1-[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one (20 mg, 0.049 mmol) obtained in Reference Synthetic Example 13 36 in 1,4-dioxane (2 mL) was stirred with di-tert-butyl bicarbonate (40 mg, 0.18 mmol) and 1 M aqueous sodium hydroxide (200 L. 0.200 mmol) at room temperature for 1 hour. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / methanol = 1/0 0/ 1 (v/v)) to give the title compound as a colorless oil (21 . 1 mg, yield 85%). REFERENCE SYNTHETIC EXAMPLE 13 84 rac-1 -r(3R,4R)-1-(4-Fluorophenethyl)-4-methylpiperidin-3-vn-7-(f2- (trimethylsilvhethoxylmethylM H-pyrrolor2,3-hin ,61naphthyridin-4(7H)-one rac-1-[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one (20 mg, 0.049 mmol) obtained in Reference Synthetic Example 13 36 in a mixture of N,N-dimethylformamide (2 mL) and dichloromethane ( 1 mL) was stirred with 4-fluorophenethyl bromide (22 L, 0.1 6 mmol) and N,N-diisopropylethylamine (20 pL, 0.11 mmol) at 50°C for 2 hours and then with sodium hydride (60 wt% dispersion in liquid paraffin, 10 mg, 0.24 mmol) at 70°C for 5 hours. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium chloride, extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ ethyl acetate = 1/1 0/1 (v/v)) to give a mixture (4.4 mg) containing the title compound. The mixture was used for the next step without further purification. REFERENCE SYNTHETIC EXAMPLE 13 85 rac-1-f(3R,4R)-1-cvclopentyl-4-methylpiperidin-3-yl1-7 -(r2-(trimethylsilyl)ethoxy1methyl)- 1H-pyrrolo[2,3 -h ,61naphthyridin-4(7H)-one rac-1-[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one (32 mg, 0.078 mmol) obtained in Reference Synthetic Example 36 in a mixture of methanol (2 mL) and acetic acid (0.2 mL) was stirred with cyclopentanone (100 pL, 1.13 mmol) and 2-picoline borane (50 mg, 0.47 mmol) at room temperature for 1 hour. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting colorless oil (38 mg) containing the title compound was used for the next step without further purification. REFERENCE SYNTHETIC EXAMPLE 86 1-(1-f4-(tert-Butyl)cvclohexanecarbonyl1-4-methylpiperidin-3-yl)-7 -(r2- (trimethylsilyl)ethoxy1methyl)-1 H-pyrrolof2,3 -hi ,61naphthyridin-4(7H)-one rac-1-[(3R,4R)-4-Methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-h][1 ,6]naphthyridin-4(7H)-one (20 mg, 0.049 mmol) obtained in Reference Synthetic Example*336 in chloroform (2 mL) was stirred with 4-(tert-butyl) cyclohexanecarboxylic acid (20 mg, 0.11 mmol), 1-(3-dimethylaminopropyl)-3- ethylcarbodidimide hydrochloride (20 mg, 0.10 mmol) and ,-diisopropylethylamine (50 L, 0.29 mmol) at room temperature for 2 hours. After addition of 0.1 M aqueous sodium hydroxide, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with 0.1 M hydrochloric acid, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate) to give two isomers of the title compound in a less polar fraction (Reference Synthetic Example 13 86a: colorless oil, 9.0 mg, yield 32%) and in more polar fraction (Reference Synthetic Example 13 86b: colorless oil, 9.3 mg, yield 33%). REFERENCE SYNTHETIC EXAMPLE 13 87 4-Chloro-1 -(F2-(trimethylsilyl)ethoxy1methyl|-1 H-pyrrolo[2,3-b1pyridine-5-carboxylic acid 4-Chloro-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-5- carbaldehyde (486 mg, 1.56 mmol) obtained in Reference Synthetic Example 13 55 in acetic acid (10 mL) was mixed with sulfamic acid (227 mg, 2.34 mmol) and 2-methyl-2- butene (486 pL, 4.58 mmol), and then sodium chlorite (254 mg, 2.81 mmol) in water (0.5 mL) was added dropwise. The resulting reaction mixture was stirred at room temperature for 2 hours, and after addition of water, adjusted to pH 7 with 1 M aqueous sodium hydroxide and extracted with chloroform. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / methanol = 10/1 1/1 (v/v)) to give the title compound as a colorless solid (484 mg, yield 95%). REFERENCE SYNTHETIC EXAMPLE 1 88 4-Chloro-1-(f2-(trimethylsilyl)ethoxylmethyl)-1 H-pyrrolor2,3-b1pyridine-5-carboxam 4-Chloro-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-5-ca^ acid (480 mg, 1.47 mmol) in thionyl chloride (3 mL) was stirred at room temperature for 2 hours. After addition of toluene, the reaction mixture was concentrated under reduced pressure, and after addition of toluene, concentrated under reduced pressure. The residue was dissolved in dichloromethane (5 mL), and ammonia - methanol solution (7.0 M, 1.0 mL, 7.0 mmol) was added dropwise, and the resulting reaction mixture was stirred for 1 hour. After addition of saturated aqueous sodium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give the title compound as a colorless solid (461 mg, yield 96%). REFERENCE SYNTHETIC EXAMPLE 3 89 4-f(1 -Benzylpiperidin-4-yl)aminol-1 -([2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolo[2,3- blpyridine-5-carboxamide 4-Chloro-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-5- carboxamide (456 mg, 1.40 mmol) was stirred with 1-benzyl-4-aminopiperidine (900 mg, 4.73 mmol) and N,N-diisopropylethylamine (250 pL, 1.44 mmol) at 140°C for 3 hours. The reaction mixture was allowed to cool to room temperature and, after addition of water, extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform ethyl acetate / methanol = 1/0 5/1 (v/v)) to give the title compound as a colorless solid (542 mg, yield 8 1%). REFERENCE SYNTHETIC EXAMPLE 13 90 1-(1 -Benzylpiperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxylmethyl)-1 Hpyrrolor3', 2':5.6lpyridor4,3-dlpyrimidine-2,4(3H,7H)-dione 4-[(1 -Benzylpiperidin-4-yl)amino]-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-b]pyridine-5-carboxamide (484 mg, 1.01 mmol) in N,N-dimethylacetamide (5 mL) was stirred with 1, 1 '-carbonyldiimidazole (486 mg, 3.00 mmol) at 120°C for 3 hours. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium chloride, extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 20/1 (v/v)) to give the title compound as a colorless solid (360 mg, yield 70%). REFERENCE SYNTHETIC EXAMPLE 13 9 1 1-(Piperidin-4-yl)-7-([2-(trimethylsilyl)ethoxylmethyl)-1 H-pyrrolof3',2':5,6lpyridor4,3- d1pyrimidine-2,4(3H,7H)-dione hydrochloride 1-(1 -Benzylpiperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidine-2,4(3H,7H)-dione (360 mg, 0.712 mmol) and 5% palladium-carbon (100 mg) in a mixture of methanol and 10 wt % hydrogen chloride - methanol solution (0.5 mL) were stirred with at room temperature for 2 hours under a hydrogen atmosphere, then at 40°C for 5 hours and at room temperature for one day. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give the title compound as a colorless solid (324 mg, quantitative yield). REFERENCE SYNTHETIC EXAMPLE 13 92 4-(r4-(2,4-Dioxo-7-{r2-(trimethylsilvnethoxylmethyl)-2.3.4,7-tetrahvdro-1 HPyrrolo[ 3',2':5,61pyrido[4,3-d1pyrimidin-1 -yl)piperidin-1 -yllmethyl|benzonitrile 1-(Piperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 3\2^5,6]pyrido[4,3-d]pyrimicline-2,4(3H,7H)-dione hydrochloride (50 mg, 0.111 mmol) and 4-cyanobenzaldehyde (29 mg, 0.22 mmol) in a mixture of methanol (2 ml) and acetic acid (0.2 mL) were stirred with 2-picoline borane (50 mg, 0.47 mmol) at room temperature for 2 days. After addition of 1 M aqueous sodium hydroxide, the reaction mixture was extracted with a mixture of ethyl acetate and 2-propanol, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 10/1 (v/v)) to give the title compound as a colorless solid (23.4 mg, yield 40%). REFERENCE SYNTHETIC EXAMPLE 5 93 1-(1 -f(5-Chlorothiophen-2-yl)methyl1piperidin-4-yl)-7-(r2-(trimethylsilyl)ethoxylmethyl)- 1H-pyrrolor3',2':5,6lpyridor4,3-d1pyrimidine-2,4(3H,7H)-dione The reactions in Reference Synthetic Example 1 92 were carried out in substantially the same manners except that 5-chlorothiophene-2-carbaldehyde was used instead of 4-cyanobenzaldehyde to give the title compound as a colorless solid (21 . 1 mg, yield 58%). REFERENCE SYNTHETIC EXAMPLE 1 94 1- -[4-(Trifluoromethyl)benzyllpiperidin-4-yl)-7-([2-(trimethylsilyl)ethoxy1methyl|-1 HPyrrolor3'. 2':5,6lpyridof4,3-dlpyrimidine-2,4(3H.7H)-dione The reactions in Reference Synthetic Example 13 92 were carried out in substantially the same manners except that 4-(trifluoromethyl)benzaldehyde was used instead of 4-cyanobenzaldehyde to give the title compound as a colorless amorphous (28.1 mg, yield 44%). REFERENCE SYNTHETIC EXAMPLE 13 95 1-Cvclohexyl-7-(r2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolor3',2':5,6lpyridor4,3- d1pyrimidine-2,4(3H,7H)-dione 4-(Cyclohexylamino)-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine- 5-carboxamide (26 mg, 0.067 mmol) obtained in Reference Synthetic Example 13 30 in N,N-dimethylacetamide ( 1 mL) was stirred with 1,1 '-carbonyldiimidazole (22 mg, 0.14 mmol) at 170°C for 2 hours under microwave irradiation. The reaction mixture was allowed to cool to room temperature and, after addition of water, extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a colorless solid (13.7 mg, yield 49%). REFERENCE SYNTHETIC EXAMPLE 96 1-(4-Chloro-1 -(r2-(trimethylsilyl)ethoxy1methyll-1 H-pyrrolo[2.3-b1pyridin-5-yl)ethanone Methylmagnesium bromide - diethyl ether solution (3.0 M, 10 mL, 30 mmol) was added dropwise to 4-chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridine-5-carbaldehyde (4.89 g, 15.7 mmol) obtained in Reference Synthetic Example 55 in tetrahydrofuran (50 mL) under cooling with ice, and the reaction mixture was stirred for 2 hours. After dropwise addition of water and addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was dissolved in 1,2-dimethoxyethane (25 mL) and vigorously stirred with manganese dioxide (9.0 g, 0.10 mol) at 80°C for 4 hours. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was dissolved in 1,2-dimethoxyethane (25 mL) and vigorously stirred with manganese dioxide (9.0 g, 0.10 mol) at 80°C for 4 hours. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 10/1 (v/v)) to give the title compound as an orange oil (3.09 g, yield 6 1%). (alternative to Reference Synthetic Example b 33) REFERENCE SYNTHETIC EXAMPLE 97 1-(4- -Benzylpiperidin-4-yl)amino1-1 -([2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrroloi2,3- b1pyridin-5-yl)ethanone 1-(4-Chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5- yl)ethanone (400 mg, 1.23 mmol) and 1-benzylpiperidin-4-amine ( 1 .70 mL, 8.93 mmol) was stirred with N,N-diisopropylethylamine (251 L. 1.47 mmol) at 140°C for one day. The reaction mixture was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound (343 mg, yield 58%). REFERENCE SYNTHETIC EXAMPLE 15 98 1-(1 -Benzylpiperidin-4-yl)-7 -{r2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolo[2,3- hi ,61naphthyridin-4(7H)-one 1-{4-[(1 -Benzylpiperidin-4-yl)amino]-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-b]pyridin-5-yl}ethanone (343 mg, 0.720 mmol) in N,N-dimethylformamide dimethyl acetal (2 mL) was stirred at 170°C for 6 hours under microwave irradiation. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure, and the residue was dissolved in tetrahydrofuran (5 mL) and stirred with 1 M hydrochloric acid (3 mL) at 80°C for 1 hour. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 9/1 (v/v)) to give the title compound (299 mg, yield 85%). REFERENCE SYNTHETIC EXAMPLE 3 99 1-(Piperidin-4-yl)-7 -(r2-(trimethylsilyl)ethoxylmethyl)-1 H-pyrrolor2,3 -hiri,6lnaphthyridin- 4(7H)-one 1-(1 -Benzylpiperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one (341 mg, 0.697 mmol) in methanol was stirred with 5% palladium-carbon (500 mg) for one day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 9/1/ (v/v)) to give the title compound (189 mg, yield 68%). REFERENCE SYNTHETIC EXAMPLE 100 1-(1 -f(5-Chlorothiophen-2-yl)methyllpiperidin-4-yl)-7 -(i2-(trimethylsilyl)ethoxy1methyl)- 1H-pyrrolor2,3 -hi ,61naphthyridin-4(7H)-one 1-(Piperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one (20 mg, 0.050 mmol) in methanol was stirred with 5- chlorothiophen-2-carbaldehyde (6.3 pL, 0.06 mmol), 2-picoline borane (6.4 mg, 0.06 mmol) and acetic acid (100 L) for one day. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (chloroform / methanol = 10/1 (v/v)) to give the title compound as a colorless oil (20 mg, yield 75%). REFERENCE SYNTHETIC EXAMPLE 1 101 1-(1 -[4-(Trifluoromethyl)benzvnpiperidin-4-yl)-7-([2-(trimethylsilyl)eth pyrrolor2.3-hin .61naphthyridin-4(7H)-one 1-(Piperidin-4-yl)-7-[{2-(trimethylsilyl)ethoxy}methyl]-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one (20 mg, 0.050 mmol) obtained in Reference Synthetic Example 3 99 in dichloromethane was stirred with 4-(trifluoromethyl)benzyl bromide (14.3 mg, 0.0600 mmol) and triethylamine ( 10.5 , 0.0750 mmol) for one day. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer as dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 9/1 (v/v)) to give the title compound (20 mg, yield 72%). REFERENCE SYNTHETIC EXAMPLE 102 4-(r4-(4-Oxo-7-(f2-(trimethylsilyl)ethoxylmethyl)-4,7-dihvdro-1 H-pyrrolor2,3- h f 1 ,6lnaphthyridin-1 -yl)piperidin-1 -vnmethyllbenzonitrile The reactions in Reference Synthetic Example 101 were carried out in substantially the same manners except that 4-cyanobenzyl bromide was used instead of 4-(trifluoromethyl)benzyl bromide to give the title compound (29.7 mg, yield 77%). REFERENCE SYNTHETIC EXAMPLE 103 3-Fluoro-4 -ir4-(4-oxo-7-(r2-(trimethylsilyl)ethoxylmethyl)-4,7-dihvdro-1 H-pyrrolor2,3- h f 1 ,61naphthyridin-1 -yl)piperidin-1 -yllmethvDbenzonitrile The reactions in Reference Synthetic Example 6 101 were carried out in substantially the same manners except that 4-(bromomethyl)-3-fluorobenzonitrile was used instead of 4-(trifluoromethyl)benzyl bromide to give the title compound as a yellow oil (17.6 mg, yield 66%). REFERENCE SYNTHETIC EXAMPLE 6 104 4-[(1 -Benzylpiperidin-4-yl)amino1-1 H-pyrrolo[2,3-blpyridine-5-carbaldehvde 4-Chloro-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde (600 mg, 3.32 mmol) obtained in Reference Synthetic Example 6 7 and 1-benzylpiperidin-4-amine (2.53 g, 13.3 mmol) in ethylene glycol (300 L) were stirred at 80°C for 2 hours under microwave irradiation. The reaction mixture was allowed to cool to room temperature and, after addition of water, extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in 1,4-dioxane (5 mL) and stirred with 4 M hydrogen chloride - 1,4-dioxane solution (5 mL) and water (2 mL) at room temperature for one day. The reaction mixture was concentrated under reduced pressure, adjusted to pH 9 or above with 1M aqueous sodium hydroxide and extracted with chloroform and water, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: hexane / ethyl acetate = 1/1 (v/v)) to give the title compound ( 672 mg, yield 60%). REFERENCE SYNTHETIC EXAMPLE 6 105 4-i(1 -Benzylpiperidin-4-yl)amino1-1 -(r2-(trimethylsilyl)ethoxylmethyl)-1 H-pyrrolof2,3- blpyridine-5-carbaldehvde 4-[(1 -Benzylpiperidin-4-yl)amino]-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde (672 mg, 2.01 mmol) in N,N-dimethylformamide (5 mL) was mixed with sodium hydride (55 wt% dispersion in mineral oil, 436 mg, 10.0 mmol) under cooling with ice, and the reaction mixture was stirred for 30 minutes. The reaction mixture was stirred with [2- (chloromethoxyl)ethyl]trimethylsilane (885 pL, 5.00 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound (392 mg, yield 42%). REFERENCE SYNTHETIC EXAMPLE 106 (4-f(1 -Benzylpiperidin-4-yl)aminol-1 -(r2-(trimethylsilyl)ethoxy1methyl)-1 H-pyrrolor2.3- b1pyridin-5-yl)methanol 4-[(1 -Benzylpiperidin-4-yl)amino]-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-b]pyridine-5-carbaldehyde (289 mg, 0.620 mmol) in methanol was stirred with sodium borohydride (35.3 mg, 0.93 mmol) at room temperature for 1 hour. The reaction mixture was concentrated under reduced pressure and, after addition of water, extracted with ethyl acetate. The organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane/ ethyl acetate = 1/1 (v/v)) to give the title compound (258 mg, yield 89%). REFERENCE SYNTHETIC EXAMPLE1 107 5-(Aminomethyl)-N-(1 -benzylpiperidin-4-yl) - 1-{f2-(trimethylsilyl)ethoxy1methyl)-1 Hpyrrolo[ 2,3-blpyridin-4-amine {4-[(1 -Benzylpiperidin-4-yl)amino]-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-b]pyridin-5-yl}methanol (212 mg, 0.454 mmol), phthalimide (134 mg, 0.909 mmol) and triphenylphosphine (238 mg, 0.909 mmol) in tetrahydrofuran was stirred at room temperature for 30 minutes and with diisopropyl azodicarboxylate ( 184 mg, 0.909 mmol) for one day. The reaction mixture was concentrated under reduced pressure and, after addition of water, extracted with ethyl acetate. The residue was purified by silica gel column chromatography (hexane/ ethyl acetate = 1/1/ (v/v)) to remove triphenylphosphine oxide. The residue was dissolved in ethanol (10 mL) and stirred with hydrazine monohydrate ( 1.00 mL, 1 1 .6 mmol) at 80°C for 1 hour. The reaction mixture was concentrated under reduced pressure and, after addition of water, extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound (5 .1 mg, yield 24%). REFERENCE SYNTHETIC EXAMPLE" 108 1-(1 -Benzylpiperidin-4-yl)-7-(r2-(trimethylsilyl)ethoxy1methyl|-3,4-dihvdro-1 Hpyrrolor3'. 2':5,61pyridor4,3-d1pyrimidin-2(7H)-one 5-(Aminomethyl)-N-(1 -benzylpiperidin-4-yl) - 1-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-b]pyridin-4-amine (38 mg, 0.081 mmol) in dichloromethane was stirred with ,1 '-carbonyldiimidazole (20.0 mg, 0. 23 mmol) at 80°C for 1 hour. The reaction mixture was concentrated under reduced pressure and, after addition of water, extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 10/1 (v/v)) to give the title compound (30.9 mg, yield 77%). REFERENCE SYNTHETIC EXAMPLE 109 1-(Piperidin-4-yl)-7-(f2-(trimethylsilyl)ethoxy1methyll-3.4-dihvdro-1 Hpyrrolor3 ' ,2' :5,6lPyridor4,3-d1pyrimidin-2 7H)-one 1-(1 -Benzylpiperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-3,4-dihydro-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidin-2(7H)-one (61 mg, 0.12 mmol) in ethanol was stirred with 5% palladium-carbon (60 mg) for one day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give the title compound (48 mg, yield 100%). REFERENCE SYNTHETIC EXAMPLE" 110 1-1-(Benzylsulfonyl)piperidin-4-yl1-7 -(r2-(trimethylsilyl)ethoxy1methyl)-3,4-dihvdro - 1Hpyrrolor3', 2':5,61pyridor4,3-d1pyrimidin-2(7H)-one 1-(Piperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-3,4-dihydro-1 Hpyrrolo[ 3',2':5 6]pyrido[4,3-d]pyrimidin-2(7H)-one ( 18.5 mg, 0.0460 mmol) in dichloromethane was mixed with phenylmethanesulfonyl chloride (17.5 mg, 0.092 mmol) and triethylamine (12.8 _, 0.0920 mmol) for 1 hour under cooling with ice. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 9/1 (v/v)) to give the title compound as a pale yellow solid ( 18.4 mg, yield 72%). REFERENCE SYNTHETIC EXAMPLE" 1 11 1-[1 -(Pyridin-3-ylmethyl)piperidin-4-yll-7 -(r2-(trimethylsilyl)ethoxylmethyl)-3,4-dihydro- 1H-pyrrolor3',2':5,61pyridof4,3-dlpyrimidin-2(7H)-one The reactions in Reference Synthetic Example" 110 were carried out in substantially the same manners except that 3-picolyl bromide was used instead of phenylmethanesulfonyl chloride to give the title compound (14 mg, yield 46%). REFERENCE SYNTHETIC EXAMPLE" 112 4-(r4-(2-Oxo-7 -(f2-(trimethylsilyl)ethoxylmethyl)-2,3,4.7-tetrahvdro-1 HPyrrolo[ 3',2':5,6lpyridor4,3-d1pyrimidin - 1-yl)piperidin - 1-yl1methyl)benzonitrile The reactions in Reference Synthetic Example" 110 were carried out in substantially the same manners except that 4-cyanobenzyl bromide was used instead of phenylmethanesulfonyl chloride to give the title compound (20.6 mg, yield 54%). REFERENCE SYNTHETIC EXAMPLE" 113 1-{1 -[4-(Trifluoromethyl)benzyl1piperidin-4-yl)-7 -(f2-(trimethylsilyl)ethoxy1methyl)-3,4- dihvdro-1 H-pyrrolor3',2':5,61pyridor4,3-d1pyrimidin-2(7H)-one The reactions in Reference Synthetic Example" 110 were carried out in substantially the same manners except that 4-(trifluoromethyl)benzyl bromide was used instead of phenylmethanesulfonyl chloride to give the title compound ( 18.9 mg, yield 46%). REFERENCE SYNTHETIC EXAMPLE" 114 4-(2-Oxo-7 -(r2-(trimethylsilyl)ethoxy1methyl)-2,3,4,7-tetrahvdro-1 Hpyrrolor3', 2':5,61pyridoi4,3-d1pyrimidin- 1-yl)-N -(1 ,3,4-thiadiazol-2-yl)piperidine - 1- carboxamide 1-(Piperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-3,4-dihydro-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidin-2(7H)-one (16.3 mg, 0.0407 mmol) obtained in Reference Synthetic Example" 109 and phenyl 1,3,4-thiadiazol-2-ylcarbamate ( 10.8 mg, 0.0488 mol) obtained in Reference Synthetic Example" 72 in tetrahydrofuran was stirred with triethylamine (8.1 L, 0.061 mmol) at 60°C for 2 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 9/1 (v/v)) to give the title compound as a colorless solid (20 mg, yield 93%). REFERENCE SYNTHETIC EXAMPLE" 115 1-ri -(3.3.3-Trifluoropropanoyl)piperidin-4-yl1-7 -(r2-(trimethylsilyl)ethoxy1methyl)-3.4- dihvdro-1 H-pyrrolof3\2':5,61pyridor4,3-dlpyrimidin-2(7H)-one 1-(Piperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-3,4-dihydro-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidin-2(7H)-one (25 mg, 0.062 mmol) obtained in Reference Synthetic Example 109 in ,-dimethylformamide was stirred with 3,3,3- trifluoropropionic acid (8.7 mg, 0.068 mmol), 0-(7-azabenzotriazol-1-yl)-N,N,N',N'- tetramethyluronium hexafluorophosphate (28.1 mg, 0.0740 mmol) and N,Ndiisopropylethylamine (21 .2 , 0.124 mmol) at room temperature for 2 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 10/1 (v/v)) to give the title compound as a yellow oil ( 15.5 mg, yield 49%). REFERENCE SYNTHETIC EXAMPLE 1 116 1-[1-(Thiazol-5-ylmethvnpiperidin-4-vn-7-([2-(trimethylsilvnethoxylmethyl)-3,4-dihvdro- 1H-pyrrolor3',2':5,61pyridor4,3-dlpyrimidin-2(7H)-one 1-(Piperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-3,4-dihydro-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidin-2(7H)-one (20 mg, 0.050 mmol) obtained in Reference Synthetic Example 1 109 in methanol was stirred with thiazol-5-carbaldehyde (6.6 _, 0.075 mmol), 2-picoline borane (8.0 mg, 0.075 mmol) and acetic acid (100 ) for one day. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (chloroform / methanol = 0/ 1 (v/v)) to give the title compound (12 mg, yield 48%). REFERENCE SYNTHETIC EXAMPLE 117 rac-4-(r(3R,4R)-1-Benzyl-4-methylpiperidin-3-vnamino)-1 H-pyrrolor2,3-blpyridine-5- carbaldehvde The reactions in Reference Synthetic Example 104 were carried out in substantially the same manners except that rac-(3R,4R)-1-benzyl-4-methylpiperidin-3- amine obtained in Reference Synthetic Example 1 3 was used instead of 1- benzylpiperidin-4-amine to give the title compound as a brown oil (282 mg, yield 30%). (alternative to Reference Synthetic Example 3 38) REFERENCE SYNTHETIC EXAMPLE 1 118 rac-4-([(3R,4R)-1 -Benzyl-4-methylpiperidin-3-yl1amino)-1 - 2- (trimethylsilyl)ethoxylmethyl)-1 H-pyrrolor2,3-b1pyridine-5-carbaldehvde The reactions in Reference Synthetic Example 105 were carried out in substantially the same manners except that rac-4-{[(3R,4R)-1-benzyl-4-methylpiperidin- 3-yl]amino}-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde was used instead of 4-[(1 - benzylpiperidin-4-yl)amino]-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde to give the title compound (231 mg, yield 60%). (alternative to Reference Synthetic Example 1 39) REFERENCE SYNTHETIC EXAMPLE 1 119 rac-(4-(r(3R,4R)-1-Benzyl-4-methylpiperidin-3-yl1amino)-1-(r2- (trimethylsilvDethoxylmethvD-I H-pyrrolo^^-blpyridin-S-vDmethanol The reactions in Reference Synthetic Example 1 106 were carried out in substantially the same manners except that rac-4-{[(3R,4R)-1-benzyl-4-methylpiperidin- 3-yl]amino}-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde was used instead of 4-[(1-benzylpiperidin-4-yl)amino]-1-{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-5-carbaldehyde to give the title compound as a yellow oil (105 mg, yield 84%). (alternative to Reference Synthetic Example 6 40) REFERENCE SYNTHETIC EXAMPLE 120 rac-5-(Aminomethyl)-N-f(3R.4R - 1-benzyl-4-meth^ (trimethylsilvnethoxylmethyl)-1 H-pyrrolor2.3-blpyridin-4-amine The reactions in Reference Synthetic Example 107 were carried out in substantially the same manners except that rac-(4-{[(3R,4R )-1 -benzyl-4-methylpiperidin- 3-yl]amino }-1 -{[2-(trimethylsilyl)ethoxy]methyl }-1 H-pyrrolo[2,3-b]pyridin-5-yl)methanol was used instead of {4-[(1 -benzylpiperidin-4-yl)amino ]-1 -{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5-yl}methanol to give the title compound (20.8 mg, yield 21%). REFERENCE SYNTHETIC EXAMPLE 121 rac-1 -r 3R,4R)-1 -benzyl-4-methylpiperidin-3-yl1-7-(r2 -(trimethylsilyl)ethoxylmethyll-3.4- dihvdro-1 H-pyrrolor3',2':5,61pyridor4,3-dlpyrimidin-2(7H)-one The reactions in Reference Synthetic Example 108 were carried out in substantially the same manners except that rac-5-(aminomethyl)-N-[(3R,4R )-1 -benzyl-4- methylpiperidin-3-yl ]-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-4- amine was used instead of 5-(aminomethyl)-N -(1 -benzylpiperidin-4-yl) - 1-{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-4-amine to give the title compound (22 mg, yield 100%). REFERENCE SYNTHETIC EXAMPLE 122 (trans-4-Aminocvclohexyl)methanol trans-4-Aminocyclohexanecarboxylic acid (314 mg, 2.1 9 mmol) was gradually added to sodium bis(2-methoxyethoxy)aluminum hydride - toluene solution (65 wt%, 3.0 mL) in toluene (3mL) at 75°C, and the reaction mixture was stirred for 7 hours. The reaction mixture was allowed to cool to room temperature and stirred with 1 M aqueous sodium hydroxide (20 mL) at 80°C for 0 minutes. The reaction mixture was allowed to cool to room temperature and partitioned between water and toluene, and the aqueous layer was extracted with chloroform three times. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give the title compound as a colorless solid (170 mg, yield 60%). REFERENCE SYNTHETIC EXAMPLE 123 1-(4-([trans-4-(Hvdroxymethyl)cvclohexyl1amino )-1 -([2-(trimethylsilyl)ethoxylmethyl - 1HPyrrolo[ 2,3-b1pyridin-5-yl)ethanone (trans-4-Aminocyclohexyl)methanol (170 mg, 1.32 mmol) and 1-(4-chloro - 1-{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5-yl)ethanone (120 mg, 0.369 mmol) obtained in Reference Synthetic Example6 96 in N,N-dimethylacetamide ( 1 mL) were stirred with N,N-diisopropylethylamine (128 L, 0.735 mmol) at 140°C for 7 hours. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium chloride, extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate) to give the title compound as a pale yellow oil (11 8 mg, yield 77%). REFERENCE SYNTHETIC EXAMPLE 124 1-rtrans-4-(Hvdroxymethyl)cvclohexyl1-7- 2-(trimethylsilyl)ethoxy1methyl)-1 HPyrrolof2,3- hiri ,61naphthyridin-4(7H)-one The reactions in Reference Synthetic Example6 98 were carried out in substantially the same manners except that 1-(4-{[trans-4- (Hydroxymethyl)cyclohexyl]amino }-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridin-5-yl)ethanone was used instead of 1-{4-[(1 -benzylpiperidin-4-yl)amino ]-1 -{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5-yl}ethanone to give the title compound as a pale yellow solid (35 mg, yield 29%). REFERENCE SYNTHETIC EXAMPLE 1 125 tert-Butyl (trans-4-methoxycvclohexyl)carbamate tert-Butyl (trans-4-hydroxycyclohexyl)carbamate ( 1 .0 g, 4.6 mmol) in tetrahydrofuran (20 mL) was stirred with sodium hydride (55 wt% dispersion in mineral oil, 24 mg, 6.4 mmol) and 15-crown-5 ether (965 L) for 30 minutes under cooling with ice and then with iodomethane (289 L) at room temperature for 1 hour. Methanol (2 mL) was added to the reaction mixture, and the precipitated solid was removed by filtration. The filtrate was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 8/1 (v/v)) to give the title compound (708 mg, yield 67%). REFERENCE SYNTHETIC EXAMPLE 1 126 trans-4-Methoxycvclohexanamine hydrochloride tert-Butyl (trans-4-methoxycyclohexyl)carbamate in ethanol (5 mL) was stirred with acetyl chloride ( .5 mL) for one day under cooling with ice, and the solvent was concentrated under reduced pressure to give the title compound (475 mg, yield 95%). REFERENCE SYNTHETIC EXAMPLE 1 127 1-(4-f(trans-4-Methoxycvclohexyl)amino1-1 -{[2-(trimethylsilyl)ethoxy1methyl)-1 Hpyrrolof2,3- b1pyridin-5-yl)ethanone 1-(4-Chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5- yl)ethanone (228 mg, 0. 70 mmol) obtained in Reference Synthetic Example b 96 in ethylene glycol ( 1 mL) was stirred with trans-4-methoxycyclohexanamine hydrochloride and ,-diisopropylethylamine at 180°C for 1 hour under microwave irradiation. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/9 (v/v)) to give the title compound as a yellow oil (179 mg, yield 61%). REFERENCE SYNTHETIC EXAMPLE 1 128 1-(trans-4-Methoxycvclohexyl)-7-(r2-(trimethylsilyl)ethoxy1methyl}-1 H-pyrrolor2,3- hl ,61naphthyridin-4(7H)-one 1-(4-[(trans-4-Methoxycyclohexyl)amino]-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-b]pyridin-5-yl)ethanone ( 79 mg, 0.428 mmol) in N,N-dimethylformamide dimethyl acetal (3 mL) was stirred at 170°C for 6 hours under microwave irradiation. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure, and the resulting residue was dissolved in tetrahydrofuran (3 mL) and stirred with 1 M hydrochloric acid (3 mL) at 80°C for 1 hour. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous sodium hydrogen carbonate, extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 9/1 (v/v)) to give the title compound (141 mg, yield 77%). REFERENCE SYNTHETIC EXAMPLES' 129 TO 134 The reactions in Reference Synthetic Example 1 10 1 were carried out in substantially the same manners except that 2-(bromomethyl)-5-(trifluoromethyl)furan, 2- (bromomethyl)-5-nitrofuran, ethyl 5-(chloromethyl)furan-2-carboxylate, 4-(chloromethyl)- 1,2-difluorobenzene, 1,2-dichloro-4-(chloromethyl)benzene or 5-(chloromethyl)-2- (trifluoromethyl)pyridine was used instead of 4-(trifluoromethyl)benzyl bromide to give the compounds of Reference Examples' 129 to 134. The names, morphologies and yields of the compounds synthesized are shown in Table 5. TABLE*35 REFERENCE SYNTHETIC EXAMPLES' 135 TO 143 The reactions in Reference Synthetic Example 100 were carried out in substantially the same manners except that 2-chlorothiazole-5-carbaldehyde, 4-fluoro-3- (trifluoromethyl)benzaldehyde, 5-nitrothiophene-3-carbaldehyde, 5-bromofuran-2- carbaldehyde, 5-bromothiophene-2-carbaldehyde, 4-bromothiophene-2-carbaldehyde, 2-bromothiazole-5-carbaldehyde, 2,2-difluorobenzo[d][1 ,3]dioxole-5-carbaldehyde or 1H-indole-5-carbaldehyde was used instead of 5-chlorothiophene-2-carbaldehyde to give the compounds of Reference Examples' 135 to 143. The names, morphologies and yields of the compounds synthesized are shown in Table3 6. TABLEb 6 REFERENCE SYNTHETIC EXAMPLE 144 1- -(5-Chlorothiophene-2-carbonv^ 1-ΐ 2,3-,61naphthyridin-4(7H)-one 1-(Piperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one (20 mg, 0.050 mmol) obtained in Reference Synthetic Example 99 in N,N-dimethylformamide (2 ml_) was stirred with 5-chlorothiophene-2- carboxylic acid (13.4 mg, 0.0825 mmol), N,N-diisopropylethylamine (25.5 , 0.1 50 mmol) and 0-(7-azabenzotriazol-1 -yl)-N,N,N\N'-tetramethyluronium hexafluorophosphate (34.2 mg, 0.0899 mmol) for one day. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 9/1 (v/v)) to give the title compound (40.0 mg, quantitative yield). REFERENCE SYNTHETIC EXAMPLES 145 TO 150 The reactions in Reference Synthetic Example 92 were carried out in substantially the same manners except that tert-butyl (2-oxoethyl)carbamate, 5- bromothiophene-2-carbaldehyde, 2-(tetrahydro-2H-thiopyran-4-yl)acetaldehyde, cyclopropanecarbaldehyde, 2-methylbutanal or 2-(tetrahydro-2H-pyran-4- yl)acetaldehyde was used instead of 4-cyanobenzaldehyde to give the compounds of Reference Synthetic Examples' 145 to 150. The names, morphologies and yields of the compounds synthesized are shown in Tableb 7. TABLE 3 7 REFERENCE SYNTHETIC EXAMPLE1 151 2-r4-(2,4-Dioxo-7-{r2-(trimethylsilyl)ethoxy1methyll-2,3.4,7-tetrahvdro-1 Hpyrrolo[ 3',2':5,6lpyrido[4,3-d1pyrimidin-1 -yl)piperidin-1-yl1acetonitrile 1-(Piperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidine-2,4(3H,7H)-dione hydrochloride (40.0 mg, 0.0885 mmol) obtained in Reference Synthetic Example1 9 1 in acetonitrile ( 1 mL) was mixed with 2-chloroacetonitrile (8.2 L, 0.133 mmol) and N,N-diisopropylethylamine (31 .0 pL, 0.177 mmol) and stirred at 60°C for 26 hours. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (chloroform methanol / chloroform = 8/92 (v/v)) to give the title compound as a colorless solid (31 .2 mg, yield 78%). REFERENCE SYNTHETIC EXAMPLES' 152 TO 156 The reactions in Reference Synthetic Example 15 1 were carried out in substantially the same manners except that 2,2,2-trifluoroethyl trifluoromethanesulfonate, 5-bromopentanenitrile, 6-bromo-1 ,1 ,1-trifluorohexane, 4- bromobutanenitrile or 2-(bromomethyl)tetrahydrofuran was used instead of 2- chloroacetonitrile to give the compounds of Reference Synthetic Examples' 152 to 156. > The names, morphologies and yields of the compounds synthesized are shown in Tableb 8 . TABLE 8 REFERENCE SYNTHETIC EXAMPLE" 157 3-f4-(2.4-Dioxo-7-(r2-(trimethylsilyl)ethoxylmethyl)-2,3,4.7-tetrahvdro-1 HPyrrolof3', 2':5,61pyridoF4,3-d1pyhmidin-1-yl)piperidin-1-yllpropanenitrile 1-(Piperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrroloi3', 2':5,6]pyrido[4,3-d]pyrimidine-2,4(3H,7H)-dione hydrochloride (40.0 mg, 0.0885 mmol) obtained in Reference Synthetic Example" 9 1 in ethanol ( 1 mL) was refluxed with acrylonitrile (11 .5 pL, 0.176 mmol) and N,N-diisopropylethylamine ( 18.9 pL, 0.110 mmol) for 8.5 hours. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (chloroform methanol / chloroform = 6/94 (v/v)) to give the title compound as a colorless solid (27.3 mg, yield 66%). REFERENCE SYNTHETIC EXAMPLE" 158 4-Aminoadamantan-1 -ol Concentrated sulfuric acid (35 mL) was mixed with concentrated nitric acid (4.5 mL) and 2-adamantylamine (5.10 g, 4.57 mmol) under cooling with ice, and the reaction mixture was stirred at room temperature for 2 hours. The reaction mixture was added to ice water and adjusted to pH 10 with 7.5 M aqueous sodium hydroxide. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give the title compound as a yellow solid (2.79 g, yield 6 1%). REFERENCE SYNTHETIC EXAMPLE 1 159 159a: Benzyl ( 1 R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl1carbamate 159b: Benzyl ( 1 R,2r,3S,5s,7s)-5-hvdroxyadamantan-2-yllcarbamate 4-Aminoadamantan-1-ol (2.57 g, 15.4 mmol) in tetrahydrofuran (25 ml_) was mixed with benzyl chloroformate (2.30 ml_, 16.1 mmol) and 1 M aqueous sodium hydroxide (16.0 ml_, 16.0 mmol) under cooling with ice and then stirred at room temperature for one day. After addition of 10% aqueous potassium hydrogen sulfate, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/2 (v/v)) to give benzyl [(1 R,2s,3S,5s,7s)-5- hydroxyadamantan-2-yl]carbamate (Reference Synthetic Example 1 159a; yellow oil, 1.72 g, yield 37%) in a more polar fraction and benzyl [(1 R,2r,3S,5s,7s)-5- hydroxyadamantan-2-yl]carbamate (Reference Synthetic Example 159b; yellow oil, 2.24 g, yield 48%) in a less polar fraction. REFERENCE SYNTHETIC EXAMPLE 160 ( 1s,3R,4s,5S,7s)-4-Aminoadamantan-1 -ol Benzyl [(1 R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl]carbamate (31 8 mg, 1.05 mmol) obtained in Reference Synthetic Example 159a and 5% palladium-carbon (63 mg) in methanol (2 mL) were stirred at room temperature for one day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give the title compound as a colorless solid (144 mg, yield 82%). REFERENCE SYNTHETIC EXAMPLE 13 161 ( 1s,3R,4r,5S,7s)-4-Aminoadamantan-1 -ol Benzyl [(1 R,2r,3S,5s,7s)-5-hydroxyadamantan-2-yl]carbamate (2.24 g, 7.46 mmol) obtained in Reference Synthetic Example 13 159b and 5% palladium-carbon (700 mg) in methanol (30 mL) were stirred at room temperature for one day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give the title compound as a colorless solid ( 1 .29 g, quantitative yield). REFERENCE SYNTHETIC EXAMPLE 162 tert-Butyl 3-oxoazetidine-1 -carboxylate tert-Butyl 3-hydroxyazetidine-1-carboxylate (4.02 g, 23.2 mmol) in dichloromethane (305 mL) was mixed with Dess-Martin Periodinane (9.55 g, 22.5 mmol) under cooling with ice and then stirred at room temperature for 3 hours. After addition of 10% aqueous sodium thiosulfate and saturated aqueous sodium hydrogen carbonate under cooling with ice, the reaction mixture was extracted with chloroform, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 2/1 (v/v)) to give the title compound as a colorless solid (3.39 g, yield 85%). REFERENCE SYNTHETIC EXAMPLE 163 tert-Butyl 3-(cvanomethylene)azetidine-1 -carboxylate Diethyl cyanomethylphosphonate (3.54 g, 20.0 mmom) in tetrahydrofuran (20 mL) was added to potassium tert-butoxide (2.03 g, 2 1. 1 mmol) in tetrahydrofuran (30 mL) under cooling with ice and stirred for 30 minutes. The reaction mixture was mixed with tert-butyl 3-oxoazetidine-1 -carboxylate (2.96 g , 17.3 mmol) in tetrahydrofuran (15 mL) and stirred at room temperature for 1 day, and after addition of water, extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/1 (v/v)) to give the title compound as a colorless solid ( 1 .93 g, yield 58%). REFERENCE SYNTHETIC EXAMPLE 1 164 tert-Butyl 3-(cvanomethyl)azetidine-1 -carboxylate tert-Butyl 3-(cyanomethylene)azetidine-1-carboxylate (823 mg, 4.24 mmol) in a mixture of methanol (20 mL) and 1,4-dioxane ( 10 mL) was stirred with 5% palladiumcarbon (129 mg) for one day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (hexane / ethyl acetate = 1/1 (v/v)) to give the title compound as a colorless oil (657 mg, yield 79%). REFERENCE SYNTHETIC EXAMPLE 165 2-(Azetidin-3-yl)acetonitrile hydrochloride tert-Butyl 3-(cyanomethyl)azetidine-1-carboxylate (621 mg, 3.17 mmol) in 1,4- dioxane (4 mL) was stirred with 4 M hydrogen chloride - 1,4-dioxane solution (6 mL) at room temperature for 1 day. The reaction mixture was concentrated under reduced pressure to give the title compound as a colorless oil (543 mg, quantitative yield). REFERENCE SYNTHETIC EXAMPLE 166 4-([trans-4-(Hvdroxymethvncvclohexyllamino)-1-{r2-(trimethylsilyl)ethoxylmethyl)-1 Hpyrrolo[ 2,3-b1pyridine-5-carboxamide 4-Chloro-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-5- carboxamide (680 mg, 2.09 mmol) obtained in Reference Synthetic Example 88 in N,N-dimethylacetamide ( 1 . 1 mL) was mixed with N,N-diisopropylethylamine ( 1 . 1 mL) and (trans-4-Aminocyclohexyl)methanol (945 mg, 7.31 mmol) obtained in Reference Synthetic Example 122 and stirred at 130°C for 3 hours. The reaction mixture was allowed to cool to room temperature and, after addition of saturated aqueous ammonium chloride, extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 5/1 (v/v)) to give the title compound as a colorless solid (781 mg, yield 89%). REFERENCE SYNTHETIC EXAMPLE 167 1-[trans-4-(Hvdroxymethyl)cvclohexyl1-7-([2-(trimethylsilyl)ethoxy1methyl)-1 Hpyrrolo[ 3',2':5.6lpyridor4.3-d1pyrimidine-2.4(3H,7H)-dione 4-{[trans-4-(Hydroxymethyl)cyclohexyl]amino}-1 -{[2-(trimethylsilyl)ethoxy]methyl}- 1H-pyrrolo[2,3-b]pyridine-5-carboxamide (270 mg, 0.645 mmol) in N,Ndimethylacetamide (3 mL) was mixed with N,N-diisopropylethylamine (3 mL) and 1, 1 '- carbonyldiimidazole ( 1 .04 g, 6.45 mmol) and stirred at 120°C for 3 hours. The reaction mixture was allowed to cool to room temperature and stirred with 1M aqueous sodium hydroxide (3 mL) and acetonitrile (3 mL) for 5 hours. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 9/1 (v/v)) to give the title compound as a colorless solid (206 mg, yield 73%). REFERENCE SYNTHETIC EXAMPLE 168 trans-4-(2^-Dioxo-7-(r2-arimethylsilyl)ethoxy1methyl)-2,3,4J-tetrahvdro-1 Hpyrrolor3', 2':5,6lPyrido[4.3-dlPyrimidin-1-yl)cvclohexanecarbaldehvde 1-[trans-4-(Hydroxymethyl)cyclohexyl]-7-{[2-(trimethylsilyl)ethoxy]methy^ pyrrolo[3\2^5,6]pyrido[4,3-d]pyrimidine-2,4(3H,7H)-dione (107 mg, 0.240 mmol) in a mixture of toluene ( 1 ml_) and dimethyl sulfoxide (0.25 ml_) was mixed with 2- iodoxybenzoic acid (80.9 mg, 0.288 mmol) and stirred at 50°C for 2 hours. After addition of saturated aqueous sodium thiosulfate and saturated aqueous sodium hydrogen carbonate, the reaction mixture was stirred at room temperature for 30 minutes, and extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 1/1 7/3 (v/v)) to give the title compound as a colorless solid (70.1 mg, yield 66%). REFERENCE SYNTHETIC EXAMPLE 3 169 1-(4-([(2,2,2-Trifluoroethyl)amino1methyl|cvclohexyl)-7-([2-(trimethylsilyl)ethoxy1methyl)- 1H-pyrrolor3',2':5,61pyrido[4,3-d1pyrimidine-2,4(3H,7H)-dione trans-4-(2,4-Dioxo-7-{[2-(trimethylsilyl)ethoxy]methyl}-2,3,4,7-tetrahydro-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidin-1 -yl)cyclohexanecarbaldehyde (30.4 mg, 0.0680 mmol) in a mixture of methanol (0.5 ml_) and acetic acid (50 ) was stirred with 2,2,2- trifluoroethanamine hydrochloride (12.1 mg, 0.089 mmol) and 2-picoline borane (9.50 mg, 0.089 mmol) at room temperature for 1 day. After addition of 1 M aqueous sodium hydroxide, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate / hexane = 1/1 (v/v)) to give the title compound as a colorless solid (32.3 mg, yield 90%). REFERENCE SYNTHETIC EXAMPLE 170 3-rtrans-4-(2.4-Dioxo-7-(f2-(trimethylsilyl)ethoxylmethyl)-2,3,4,7-tetrahvdro-1 HPyrrolo[ 3',2':5,61pyrido[4,3-d1pyrimidin-1-yl)cvclohexynacrylonitrile trans-4-(2,4-Dioxo-7-{[2-(trimethylsilyl)ethoxy]methyl}-2,3,4,7-tetrahydro-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidin-1-yl)cyclohexanecarbaldehyde (34.2 mg, 0.0770 mmol) obtained in Reference Synthetic Example 1 168 in tetrahydrofuran (2 ml_) was mixed with diethyl cyanomethylphosphonate (37 , 0.235 mmol) and sodium hydride (55 wt% dispersion in mineral oil, 10 mg, 0.235 mmol) under cooling with ice and then stirred at room temperature for 30 minutes. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 1/2 1/0 (v/v)) to give the title compound as a colorless solid (32.0 mg, yield 92%). REFERENCE SYNTHETIC EXAMPLES" 171 AND 172 The reactions in Reference Synthetic Example13 89 were carried out in substantially the same manners except that (1s,3R,4r,5S,7s)-4-aminoadamantan-1-ol obtained in Reference Synthetic Example 161 or (1s,3R,4s,5S,7s)-4-aminoadamantan- 1-ol obtained in Reference Synthetic Example 160 was used instead of 1-benzyl-4- aminopiperidine to give the compounds of Reference Examples 17 1 and 172. The names, morphologies and yields of the compounds synthesized are shown in Tableb 9. TABLEb 9 REFERENCE SYNTHETIC EXAMPLES' 173 AND 174 The reactions in Reference Synthetic Example15 90 were carried out in substantially the same manners except that 4-{[(1 R,2r,3S,5s,7s)-5-hydroxyadamantan- 2-yl]amino}-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridine-5-carboxamide obtained in Reference Synthetic Example 171 or 4-{[(1 R,2s,3S,5s,7s)-5- hydroxyadamantan-2-yl]amino}-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridine-5-carboxamide obtained in Reference Synthetic Example1 172 was used instead of 4-[(1 -benzylpiperidin-4-yl)amino]-1 -{[2-(trimethylsilyl)ethoxy]methyl}-1 Hpyrrolo[ 2,3-b]pyridine-5-carboxamide to give the compounds of Reference Synthetic Examples' 173 and 174. The names, morphologies and yields of the compounds synthesized are shown in Table 10. TABLE 10 REFERENCE SYNTHETIC EXAMPLES" 175 AND 176 The reactions in Reference Synthetic Example 97 were carried out in substantially the same manners except that (1s,3R,4r,5S,7s)-4-aminoadamantan-1 -ol obtained in Reference Synthetic Example 161 or (1s,3R,4s,5S,7s)-4-aminoadamantan- 1-ol obtained in Reference Synthetic Example 160 was used instead of 1- benzylpiperidine-4-amine to give the compounds of Reference Synthetic Examples 6 175 and 176. The names, morphologies and yields of the compounds synthesized are shown in Table 1 1 . TABLEb 1 1 REFERENCE SYNTHETIC EXAMPLES' 177 AND 178 The reactions in Reference Synthetic Example 98 were carried out in substantially the same manners except that 1-(4-{[(1 R,2r,3S,5s,7s)-5- hydroxyadamantan-2-yl]amino}-1-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- b]pyridin-5-yl)ethanone obtained in Reference Synthetic Exampleb 175 or 1-(4- {[(1 R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl]amino}-1 -{[2-(trimethylsilyl)ethoxy]methyl}- 1H-pyrrolo[2,3-b]pyridin-5-yl)ethanone obtained in Reference Synthetic Example 1 176 was used instead of 1-{4-[(1-benzylpiperidin-4-yl)amino]-1 -{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-b]pyridin-5-yl}ethanone to give the compounds of Reference Synthetic Examples' 177 and 78. The names, morphologies and yields of the compounds synthesized are shown in Table1 12. TABLE1 12 REFERENCE SYNTHETIC EXAMPLE 179 3-Amino-1 , 1 ,1-trifluoro-2-(pyridin-3-yl)propan-2-ol Isopropylmagnesium chloride-lithium chloride complex - tetrahydrofuran solution ( .3 M, 20.7 mL, 27.0 mmol) was added dropwise to 5-bromo-2-chloropyridine (5.20 g, 27.0 mmol) in tetrahydrofuran (40 mL) under cooling with ice, and the reaction mixture was stirred for 30 minutes and then mixed with ethyl 2,2,2-trifluoroacetate ( 11.5 g , 8 1.0 mmol) under cooling with ice and stirred at room temperature for 0 minutes. After addition of 1M hydrochloric acid, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give a yellow oil. The yellow oil was dissolved in nitromethane (30 mL) and stirred with potassium carbonate (3.73 g, 27.0 mmol) at room temperature for 30 minutes. The reaction mixture was added to 1M hydrochloric acid and extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane / ethyl acetate = 3/1 (v/v)) to give a yellow oil. The yellow oil was dissolved in tetrahydrofuran (20 mL), mixed with 10% palladium-carbon (600 mg) and triethylamine (2.60 mL, 18.7 mmol) and then stirred at room temperature for one day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate ethyl acetate / methanol / triethylamine = 9/1/1 (v/v/v)) to give the title compound as a colorless solid (913 mg, yield 3 1%(4 steps)). SYNTHETIC EXAMPLE1 1-Cvclohexyl-4-methyl-1 ,2,4.7-tetrahvdropyrrolor3',2':5,6lpyridof4.3 -di ,31oxazine Crude 1-cyclohexyl-4-methyl-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 ,2,4,7- tetrahydropyrrolo[3',2':5,6]pyrido[4,3-d][1 ,3]oxazine (9 mg) obtained in Reference Synthetic Example 3 23 in ,-dimethylformamide ( 1mL) was stirred with ethylenediamine (50 pL, 0.75 mmol) and tetrabutylammonium fluoride ( 1 .0 M tetrahydrofuran solution, 100 pL, 0.100 mmol) at 80°C for 1 hour and allowed to cool to room temperature. After addition of saturated aqueous sodium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (hexane / ethyl acetate = 1/2 (v/v)) to give the title compound as a colorless amorphous ( 1 .8 mg, yield 29% (two steps)). SYNTHETIC EXAMPLE 3 2 1-Cvclohexyl-1 .2,4,7-tetrahvdropyrrolor3'.2':5,61pyridof4.3 -din ,31oxazine 1-Cyclohexyl-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 ,2,4,7- tetrahydropyrrolo[3',2':5,6]pyrido[4,3-d][1 ,3]oxazine (17 mg, 0.044 mmol) obtained in Reference Synthetic Example1 1 1 in N,N-dimethylformamide ( 1 mL) was stirred with ethylenediamine (50 pL, 0.75 mmol) and tetrabutylammonium fluoride ( 1 .0 M tetrahydrofuran solution, 120 pL, 0.120 mmol) at 80°C for 2 hours and allowed to cool to room temperature. After addition of saturated aqueous sodium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate / methanol = 20/1 (v/v)) to give the title compound as a colorless solid (2.0 mg, yield 18%). SYNTHETIC EXAMPLE 3 3 1-Cvclohexyl-1 H-pyrrolof2,3 -hi ,61naphthyridin-4(7H)-one 1-Cyclohexyl-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one (9 mg, 0.02 mmol) obtained in Reference Synthetic Example 3 24 in N,N-dimethylformamide ( 1 mL) was stirred with ethylenediamine (25 pL, 0.37 mmol) and tetrabutylammonium fluoride ( 1 .0 M tetrahydrofuran solution, 70 pL, 0.070 mmol) at 80°C for 30 minutes and allowed to cool to room temperature. After addition of saturated aqueous sodium chloride, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate / methanol = 20/1 (v/v)) to give the title compound as a colorless solid (3.3 mg, yield 54%). SYNTHETIC EXAMPLE 3 4 rac-1 -i(3R,4R)-1 -Benzyl-4-methylpiperidin-3-vn-1 H-pyrroloi2,3-hin ,61naphthyridin- 4(7H)-one rac-1 -[(3R,4R)-1-Benzyl-4-methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}- 1H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)-one (90 mg, 0.18 mmol) obtained in Reference Synthetic Example 1 35 in N,N-dimethylformamide (3 mL) was stirred with ethylenediamine (50 , 0.75 mmol) and tetrabutylammonium fluoride ( 1 .0 M tetrahydrofuran solution, 900 _, 0.900 mmol) at 80°C for 2 hours and allowed to cool to room temperature. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was mixed with ethyl acetate, and the solid was collected by filtration to give the title compound as a pale orange solid (46.5 mg, yield 70%). SYNTHETIC EXAMPLE" 5 rac-1 -r(3R,4R)-4-Methylpiperidin-3-yl1-1 H-pyrrolor2,3-h1i1 ,61naphthyridin-4(7H)-one hydrochloride rac-1 -[(3R,4R)-1 -Benzyl-4-methylpiperidin-3-yl]-1 H-pyrrolo[2,3-h][1 ,6]naphthyridin- 4(7H)-one (16 mg, 0.043 mmol) and 5% palladium-carbon ( 15 mg) in methanol (2 mL) was stirred with hydrogen chloride - methanol solution (10 wt%, 20 L) at 40°C for 2 hours under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give the title compound as a pale yellow solid ( 15 mg, quantitative yield). SYNTHETIC EXAMPLE 6 rac-1 -i(3R,4R)-1 -(2,3-Difluorobenzyl)-4-methylpiperidin-3-yl1-1 H-pyrrolof2,3- hl ,61naphthyridin-4(7H)-one (Synthetic Example 6 6a) rac-1 -r(3R,4R)-1 .4-Dimethylpiperidin-3-yl1-1 H-pyrrolor2,3-hlf 1,61naphthyridin-4(7H)-one (Synthetic Example 6 6b) rac-1 -[(3R,4R)-4-methylpiperidin-3-yl]-1 H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)- one hydrochloride (18 mg, 0.057 mmol) and 2,3-difluorobenzaldehyde ( 10 mg, 0.070 mmol) in a mixture of methanol ( 1 mL)/acetic acid ( 1 mL) was stirred with 2-picoline borane ( 10 mg, 0.094 mmol) at room temperature for one day. After addition of saturated aqueous sodium hydrogen carbonate and 1 M aqueous sodium hydroxide, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (chloroform / methanol = 20/1 (v/v)) to give rac-1 -[(3R,4R)-1 -(2,3-difluorobenzyl)-4-methylpiperidin-3-yl]-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one (less polar fraction: 6.1 mg, yield 26%) as a pale yellow solid and rac-1 -[(3R,4R)-1 ,4-dimethylpiperidin-3-yl]-1 H-pyrrolo[2,3-h][1 ,6]naphthyridin- 4(7H)-one (more polar fraction: 5.9 mg, yield 35%) as a colorless oil. SYNTHETIC EXAMPLE 7 rac-3-r(3R,4R)-4-Methyl-3-(4-oxo-4.7-dihvdro-1 H-pyrrolof2.3-h1f 1,61naphthyridin-1 - yl)piperidin-1vn-3-oxopropanenitrile rac-1 -[(3R,4R)-4-Methylpiperidin-3-yl]-1 H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)- one hydrochloride (15 mg, 0.040 mmol) obtained in Synthetic Example 5 , 1-(3- dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride ( 0 mg, 0.052 mmol), Nhydroxybenzotriazole (6 mg, 0.04 mmol), 2-cyanoacetic acid (5 mg, 0.06 mmol) and N,N-diisopropylethylamine (30 L, 0.017 mmol) in N,N-dimethylformamide (0.5 mL) was stirred at room temperature for 2 hours. After addition of water, the reaction mixture was extracted with chloroform, and the aqueous layer was extracted with a mixture of chloroform/2-propanol. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate / methanol = 20/1 (v/v)), and the crude product was further purified by silica gel thin layer chromatography (NH-PLC05 plate manufactured by Fuji Silysia Chemical Ltd.: chloroform / methanol = 10/1 (v/v)) to give the title compound as a colorless solid (2.5 mg, yield 17%). SYNTHETIC EXAMPLE" 8 rac-1 -f(3R.4R)-1 -(2-Cvclopropylacetyl)-4-methylpiperidin-3-yl1-1 H-pyrrolof2,3- hl ,61naphthyridin-4(7H)-one rac-1 -[(3R,4R)-4-Methylpiperidin-3-yl]-1 H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)- one hydrochloride (20 mg, 0.054 mmol) obtained in Synthetic Example" 5 , 1-(3- dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (20 mg, 0.10 mmol), 2- cyclopropylacetic acid (10 pL) and N,N-diisopropylethylamine (26 L, 0.015 mmol) in N,N-dimethylformamide ( 1 mL) was stirred at room temperature for 6 hours. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (chloroform / methanol = 15/1 (v/v)), and the crude product was further purified by silica gel thin layer chromatography (NH-PLC05 plate manufactured by Fuji Silysia Chemical Ltd.: chloroform / methanol = 30/1 (v/v)) to give the title compound as a colorless solid (7.9 mg, yield 40%). SYNTHETIC EXAMPLE" 9 rac-1 -f(3R.4RV4-Methyl-1 -(3.3,3-trifluoropropanovnpiperidin-3-yl1-1 H-pyrroloi2.3- h M,61naphthyridin-4(7H)-one rac-1 -[(3R,4R)-4-Methylpiperidin-3-yl]-1 H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)- one hydrochloride (15.6 mg, 0.0489 mmol) obtained in Synthetic Example" 5 , 1-(3- dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (12.5 mg, 0.0978 mmol), 3,3,3- trifluoropropionic acid (13 pL, 0.098 mmol) and N,N-diisopropylethylamine (26 pL, 0.015 mmol) in N,N-dimethylformamide ( 1 mL) was stirred at room temperature for one day. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (chloroform / methanol = 4/1 (v/v)) to give the title compound as a colorless solid (12.2 mg, yield 64%). SYNTHETIC EXAMPLE" 10 rac-1 -r(3R,4R)-1 -(lsobutylsulfonyl)-4-methylpiperidin-3-yll-1 H-pyrrolor2.3- hi ,61naphthyridin-4(7H)-one rac-1 -[(3R,4R)-1-(lsobutylsulfonyl)-4-methylpiperidin-3-yl]-7-{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)-one ( 8 mg, 0.034 mmol) obtained in Reference Synthetic Example" 37 in dichloromethane ( 1 mL) was stirred with trifluoroacetic acid ( 1 mL) at room temperature for 3 hours. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was dissolved in a mixture of dichloromethane ( 1 mL) and methanol ( 1 mL) and stirred with ethylenediamine (100 pL, 1.50 mmol) and 1 M aqueous sodium hydroxide ( 100 pL, 0.100 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate / methanol = 20/1 (v/v)) to give the title compound as a colorless solid (8.2 mg, yield 60%). SYNTHETIC EXAMPLE" 11 rac-1 -i(3R.4RV4-Methyl-1 -(2.2,2-trifluoroethylsulfonyl)piperidin-3-yl1-1 H-pyrroloi2,3- hl ,61naphthyridin-4(7H)-one rac-1 -[(3R,4R)-4-Methylpiperidin-3-yl]-1 H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)- one hydrochloride (16 mg, 0.050 mmol) obtained in Synthetic Example 13 5 in a mixture of dichloromethane ( 1 mL) and N,N-dimethylformamide ( 100 ) was mixed with N,Ndiisopropylethylamine (30 , 0.17 mmol) and 2,2,2-trifluoroethanesulfonyl chloride (20 mg, 0.1 1 mmol) under cooling with ice and stirred at room temperature for one day. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate / methanol = 0/ 1 (v/v)) to give the title compound as a colorless solid (2.5 mg, yield 12%). SYNTHETIC EXAMPLE" 12 1-Cvclohexyl-1 ,4-dihvdropyrrolor3',2':5,61pyridor3.4-blM ,41thiazine-4,4(7H)-dione Crude 1-cyclohexyl-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 ,4- dihydropyrrolo[3',2':5,6]pyrido[3,4-b][1 ,4]thiazine-4,4(7H)-dione (8.5 mg) obtained in Reference Synthetic Example 3 28 in dichloromethane ( 1 mL) was stirred with trifluoroacetic acid ( 1 mL) at room temperature for 3 hours. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in methanol ( 1 mL) and stirred with ethylenediamine (20 L, 0.30 mmol) and 1 M aqueous sodium hydroxide (20 pL, 0.020 mmol) at room temperature for 3 hours. The precipitated solid was collected by filtration to give the title compound as a colorless solid ( 1 .7 mg, yield 39% (two steps)). SYNTHETIC EXAMPLE 13 1-Cvclohexyl-1 H-pyrrolof3',2':5,6lpyridor4.3-d1pyrimidin-4(7H)-one 1-Cyclohexyl-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[3',2':5,6]pyrido[4,3- d]pyrimidin-4(7H)-one (9 mg, 0.02 mmol) obtained in Reference Synthetic Example 1 32 in dichloromethane (2 mL) was stirred with trifluoroacetic acid ( 1 mL) at room temperature for 2 hours. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was dissolved in methanol (2 mL) and dichloromethane ( 1 mL) and stirred with ethylenediamine (50 pL, 0.75 mmol) and 1 M aqueous sodium hydroxide (50 L, 0.050 mmol) at room temperature for 3 days. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (chloroform / methanol = 30/1 (v/v)) to give the title compound as a colorless solid (2.1 mg, yield 35%). SYNTHETIC EXAMPLE 13 14 rac-1 -f(3R.4R)-1 -Benzyl-4-methylpiperidin-3-yl1-1 ,2.4.7- tetrahvdropyrrolor3',2':5,61pyridor4 3-d1f1 ,31oxazine rac-1 -[(3R,4R)-1-Benzyl-4-methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}- 1,2,4,7-tetrahydropyrrolo[3',2':5,6]pyrido[4,3-d][1 ,3]oxazine (64.6 mg, 0.131 mmol) obtained in Reference Synthetic Example 3 4 1 in dichloromethane (2 mL) was stirred with trifluoroacetic acid ( 1 mL) at room temperature for 2 hours, and the reaction mixture was concentrated under reduced pressure. The resulting residue was stirred with dichloromethane (4mL), methanol (2 mL), ethylenediamine (200 _, 3.00 mmol) and 1 M aqueous sodium hydroxide (2 mL, 2 mmol) at room temperature for 1 hour. The reaction solution was concentrated under reduced pressure, and after addition of water, extracted with chloroform. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (chloroform / methanol = 10/1 (v/v)) to give the title compound as a pale yellow amorphous (28.2 mg, yield 59%). SYNTHETIC EXAMPLE 15 rac-1 - r(3R,4R)-4-Methylpiperidin-3-yll-1 .2,4.7-tetrahvdropyrrolor3'.2':5.6lpyridor4,3- d ,31oxazine rac-1 -[(3R,4R)-1 -Benzyl-4-methylpiperidin-3-yl]-1 ,2,4,7- tetrahydropyrrolo[3',2':5,6]pyrido[4,3-d][1 ,3]oxazine (28.2 mg, 0.0777 mmol) in ethanol was stirred with 5% palladium-carbon (30 mg) and concentrated hydrochloric acid (2 drops) at 50°C for 2 hours under a hydrogen atmosphere. The reaction mixture was allowed to cool to room temperature and filtered, and the filtrate was concentrated under reduced pressure to give the title compound (21 .2 mg, yield 100%). SYNTHETIC EXAMPLE* 16 rac-3-f(3R,4R)-4-Methyl-3-(pyrrolor3',2':5,61pyridor4.3 -di .3loxazin-1 (2H.4H.7H)- yl)piperidin-1-yll-3-oxopropanenitrile rac-1 -[(3R,4R)-4-Methylpiperidin-3-yl]-1 ,2,4,7- tetrahydropyrrolo[3',2':5,6]pyrido[4,3-d][1 ,3]oxazine (21 .2 mg, 0.0777 mmol) in N,Ndimethylformamide was stirred with cyanoacetic acid (15 mg, 0.18 mmol), 0-(7- azabenzotriazol-1 -yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate (67 mg, 0.18 mmol), N,N-diisopropylethylamine (44.9 L, 0.264 mmol) at room temperature for one day. After addition of water, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol =20/1 (v/v)) to give the title compound as a yellow oil (3 mg, yield 10%). SYNTHETIC EXAMPLE 17 1-Cvclohexyl-3,4-dihvdro-1 H-pyrrolof3',2':5.61pyridor4.3-d1pyrimidin-2(7H)-one 1-Cyclohexyl-7-{[2-(trimethylsilyl)ethoxy]methyl}-3,4-dihydro-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidin-2(7H)-one (46.6 mg, 0.1 16 mmol) obtained in Reference Synthetic Example 6 13 in dichloromethane (3 mL) was stirred with trifluoroacetic acid ( 1 mL) at room temperature for 2 hours. The reaction mixture was concentrated under reduced pressure, and the resulting residue was stirred with dichloromethane (2 mL), methanol ( 1 mL), ethylenediamine (200 pL, 3.00 mmol) and 1 M aqueous sodium hydroxide ( 1 mL, 1 mmol) for one day. The reaction mixture was concentrated under reduced pressure, and after addition of water, extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give the title compound as a colorless solid (22.2 mg, yield 70%). SYNTHETIC EXAMPLE 18 1-Cvclohexyl-1 H-pyrroloi3'.2':5.61pyridor4.3-d1pyrimidin-2(7H)-one 1-Cvclohexyl-3.4-dihvdro-1 H-pyrrolof3'.2':5.61pyridor4.3-d1pyrimidin-2(7H)-one (18 mg, 0.066 mmol) in chloroform (2 mL) was stirred with manganese dioxide ( 100 mg, 1.15 mmol) at 50°C for 5 hours. The reaction mixture was filtered, and the filtrate was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 10/1 (v/v)) to give the title compound as a colorless solid (0.58 mg, yield 3.2%). SYNTHETIC EXAMPLE 19 1-Cvclohexyl-1 ,4-dihvdro-7H-pyrrolof3',2':5,6lpyridof3.4-e1pyrimidine 1-Cyclohexyl-1 ,4-dihydro-7-{[2-(trimethylsilyl)ethoxy]methyl}- pyrrolo[3',2':5,6]pyrido[3,4-e]pyrimidine (48.8 mg, 0.127 mmol) obtained in Reference Synthetic Example 1 14 in dichloromethane (2 mL) was stirred with trifluoroacetic acid ( 1 mL) for one day. The reaction mixture was concentrated under reduced pressure and stirred with dichloromethane (2 mL), methanol ( 1 mL), ethylenediamine (300 L, 4.49 mmol) and 1 M aqueous sodium hydroxide ( 1 mL, 1 mmol) for one day. The reaction mixture was concentrated under reduced pressure and extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: chloroform / methanol = 10/1 (v/v)) to give the title compound as a colorless solid ( 11 mg, yield 34%). SYNTHETIC EXAMPLE 20 9-Cvclohexyl-3H-imidazo[4,5-hiri .61naphthyridin-6(9H)-one 9-Cyclohexyl-3-{[2-(trimethylsilyl)ethoxy]methyl}-3H-imidazo[4,5- h][1 ,6]naphthyridin-6(9H)-one (57.5 mg, 0.144 mmol) obtained in Reference Synthetic Example 13 48 in dichloromethane (2 mL) was stirred with trifluoroacetic acid (2mL) at room temperature for 1 hour. The reaction mixture was concentrated under reduced pressure, and the resulting residue was stirred with dichloromethane (4 mL), methanol ( 1 mL), ethylenediamine (200 L, 3.00 mmol) and 1 M aqueous sodium hydroxide ( 1 mL, 1 mmol) at room temperature for 2 hours. The reaction mixture was concentrated under reduced pressure, and the resulting residue was purified by silica gel chromatography (chloroform / methanol = 10/1 (v/v)) to give the title compound as a pale yellow solid (23.0 mg, yield 59%). SYNTHETIC EXAMPLES' 3 2 1 TO 47 The reactions in Synthetic Example 1 10 were carried out in substantially the same manners except that the compounds obtained in Reference Synthetic Examples' 3 5 1, 54, 59 to 7 1, 73 or 75 to 85 were used instead of rac-1-[(3R,4R)-1 -(isobutylsulfonyl)-4- methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one to give the compounds of Synthetic Examples' 2 1 to 47. The names, morphologies and yields of the compounds synthesized are shown in Tables" 13 to 15. TABLE 3 Ex Compound Name M hology Yi l rac-l-[(3R, 4R)-l-benzyl-4-methylpi 2 1 peridin-3-yl]-9-bromo-lH-pyrrolo[2 colorless oil 34% ,3-h] [1, 6]naphthyridin-4(7H)-one rac - l -[(3R, 4R)-l-benzyl-4-methylpi 22 peridin-3-yl]-9-chloro-lH-pyrrolo[ colorless oil 69% 2 , 3-h] [l, 6]naphthyridin-4(7H)-one rac-l-[(3R, 4R)-l-benzyl-4-methylpi 23 peridin-3-yl]-3-methyl-lH-pyrrolo[ col ess oil 60% 2 , 3-h] [l, 6]naphthyridin-4(7H)-one rac-1- [( R,4R) -l-benzyl-4-methylpi 2 . 3% 24 peridin-3-yl]-3-bromo-lH-pyrrolo[2 col ess oil (t o steps) ,3-h] [l, 6]naphthyridin-4(7H)-one c ~ 2-{[(3R, 4R)-4-methyl-3 - (4-oxo- 4 , 7-dihydro-lH-pyrrolo [2, 3-h] [l, 6 ] colorless 25 44% naphthyridin-l-yl)piperidin-l-yl]s solid ulfonyl} benzonitrile rac-3-{[(3R, 4R)-4-methyl-3-(4-oxo- 4 , 7- ih dro lH- y ol [2, 3-h] [l, 6 col less 26 52% naphthyridin-l-yl)piperidin-l-yl]s oli ulfonyl) be z r ile rac- (3R, R )-ethyl 4-methyl-3-(4-oxo-4, 7-dihydro-lH-p colorless 27 53% yrrolo[2, 3-h] [1,6]naphthyridin-l-y solid l)piperidine-l-carboxylate rac- (3R, 4R) -4-me hy 1 -3- (4-oxo-4, 7- dihydro-lH-pyrrolo[2, 3-h] [1, 6]naph colorless 28 75% thyridin - l -yl) -N- [2-(trifluorometh o id y 1 ) he yl]p ip rid i i e—1-carboxamide rac-(3R, 4R)-4-methyl-3-(4-oxo-4, 7- dihydro-lH-pyrrolo[2, 3-h] [1,6]naph lo ess 29 36% thyri din-l-yl) - - [3- (trifluorometh solid yl)phenyl]piperidine _ l-car box amide rac-l-{ (3R, 4R)-4-methyl-l-[2-(trif luoromethyl) benzoyl]piperidin-3-yl colorless 30 37% }-lH-pyrrolo[2, 3-h] [l, 6]naphthyrid solid in-4 ( H )-one rac - l - {(3R, 4R)-4-methyl-l-[3-(trif luoromethyl) benzoyl]piperidin-3-yl colorless 31 66% }-lH-pyrrolo[2, 3-h] [l, 6]naphthyrid solid in-4 (7H) -one rac-l-{(3R, 4R)-l- [2-(4-fluoropheny l)acetyl]-4-methylpiperidin-3-yl}- colorless 32 79% lH-pyrrolo[2, 3-h] [1,6]naphthyridin oli -4(7H)-one rac-l-((3R, 4R)-4-methyl-l-{ [3-(tri fluoromethyl)phenyl]sulfonyl}piper colorless 33 57% idin-3-yl)-lH-pyrrolo[2, 3-h] [l, 6]n solid aphthyridin-4(7H) -o TABLEb 14 Ex Compound Name Morphology Y ie rac-l-{(3R,4R)-4-methyl-l-[4-(trif luoromethyl) benzoyl]piperidin-3-yl colorless 34 70% }-lH-pyrrolo [2, 3-h] [1, 6]naphthyrid solid in- (7H) -one r ac- (3R, 4R) -benzy 1 4-methyl-3-(4-oxo-4, 7-dihydro-lH-p 35 co lo e s s oil 56% yrrolo[2, 3-h] [1,6 ] h th d i - l-y 1 )pipe ridi e-l-car boxy late rac - (3R, 4R)-4-meth yl-3- (4-0X0-4, 7- dihydro-lH-pyrrolo [2, 3-li] [1, 6]naph pale yellow 36 81% thyridin-l-yl)-N-(l, 3 , 4-thiadiazol solid _ 2-y1 )piperi dine- l carboxamide rac-(3R, 4R)-4-methyl-N-(3-methylis othiazol-5-yl)-3-(4-oxo-4, 7-dihydr pale yellow 3 7 9 % o-lH-pyrrolo [2, 3-h] [1, 6]naphthyrid solid in-l-yl)piperidine-l-carboxamide r ac- 1- [(3 ,4 )- 1- (eye lope ntanecarb y l) -4-methylpiperidin-3-yl]-lH-p pale yellow 38 76% o l o [2, 3-h] [1,6]naphthyridin-4(7 solid H )-one rac-l-{ (3R, 4R)-4-methyl-l-[3-(trif luoromethyl) en l]piperidin-3-yl) pale yellow 39 42% -lH-pyrrolo[2, 3-h] [1, 6]naphthyridi solid - (7H)-o e rac-l-{ (3R, 4R)-4-methyl-l-[4-(trif luoromethyl) enzyl]piperidin-3-yl} 40 yellow solid 85% -lH-pyrrolo[.2, 3-h] [l, 6]naphthyridi n-4 (7H) -one rac-l-{ (3R, 4R)-4-methyl-l-[2-(trif luoromethyl) benzyl]piperidin-3-yl) 57% 4 1 yel lo solid -lH-pyrrolo[2, 3-h] [l, 6]naphthyridi (two t p ) n-4 (7H) -one rac-3-{[(3R, 4R)-4-methyl-3-(4-oxo- 4 , 7-dihydro-lH-pyrrolo [2, 3-h] [l, 6 ] pale ye llo 42 88% naphthyridin-l-yl)piperidin-l-yl]m solid e h l }benzonitri le rac-2-{[(3R, 4R)-4-methyl-3- (4-oxo- 4 , 7-dihydro-lH-pyrrolo [2, 3-h] [l, 6 ] pale ye llo 43 88% naphthyridin-l-yl)piperidin-l-yl]m o id ethyljbenzo nit rile rac-4-{[(3R, 4R)-4-methyl-3-(4-oxo- 4 , 7-dihydro-lH-pyrrolo[2, 3-h] [l, 6 ] 44 llow solid 1% naphthyridin-l-yl)piperidin-l-yl]m ethyl }benzonitrile ac- (3R, 4R) - tert-buty 1 4-methyl-3-(4-oxo-4, 7-dihydro-lH-p colorless 45 53% r o1 o [2,3-h ] [1,6 ]nap h thyr id in- 1-y s id l)piperidine ~ l-carboxylate TABLE b 5 SYNTHETIC EXAMPLE" 48 1-(1 -r4-(tert-Butvncvclohexanecarbonyl1-4-methylpiperidin-3-yl)-1 H-pyrrolof2,3- h ,61naphthyridin-4(7H)-one The reactions in Synthetic Example 1 10 were carried out in substantially the same manners except that Reference Synthetic Examples' 5 86a or 86b obtained in Reference Synthetic Example 13 86 were used instead of rac-1-[(3R,4R)-1 -(isobutylsulfonyl)-4- methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one to give the two isomers of the title compound, Synthetic Example 13 48a (colorless amorphous, 5.0 mg, 71%) or Synthetic Example 13 48b (colorless amorphous, 4.1 mg, yield 56%). SYNTHETIC EXAMPLES" 49 TO 53 The reactions in Synthetic Example" 10 were carried out in substantially the same manners except that the compounds obtained in Reference Synthetic Examples" 90 and 92 to 95 were used instead of rac-1-[(3R,4R)-1-(isobutylsulfonyl)-4-methylpiperidin- 3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)-one to give the compounds of Synthetic Examples" 49 to 53. The names, morphologies and yields of the compounds synthesized are shown in Table" 16. TABLE" 16 SYNTHETIC EXAMPLES" 54 TO 58 The reactions in Synthetic Example" 10 were carried out in substantially the same manners except that the compounds obtained in Reference Synthetic Examples' 98 and 100 to 103 were used instead of rac-1 -[(3R,4R)-1-(isobutylsulfonyl)-4- methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one to give the compounds of Synthetic Examples' 354 to 58. The names, morphologies and yields of the compounds synthesized are shown in Tableb 17. TABLE 17 SYNTHETIC EXAMPLES 59 TO 67 The reactions in Synthetic Example 10 were carried out in substantially the same manners except that the compounds obtained in Reference Synthetic Examples' 108 and 1 10 to 116 and 121 were used instead of rac-1-[(3R,4R)-1-(isobutylsulfonyl)-4- methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one to give the compounds of Synthetic Examples' 59 to 67. The names, morphologies and yields of the compounds synthesized are shown in Table 18. TABLE 8 SYNTHETIC EXAMPLE 68 1-(Ptperidin-4-yl)-3.4-dihvdro-1 H-pyrrolof3\2^^ 1-(1-Benzylpiperidin-4-yl)-3,4-dihydro-1 H-pyrrolo[3\2':5,6]pyrido[4,3-d]pyrimidin- 2(7H)-one (25.6 mg, 0.0708 mmol) obtained in Synthetic Example 59 and 5% palladium-carbon (30 mg) in ethanol was stirred with 10 wt% hydrogen chloridemethanol (2 drops) at 50°C for 2 hours under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure to give the title compound as a colorless solid (9 mg, yield 46%). SYNTHETIC EXAMPLES' 69 TO 85 The reactions in Synthetic Example 10 were carried out in substantially the same manners except that the compounds obtained in Reference Synthetic Examples' 124 and 128 to 144 were used instead of rac-1-[(3R,4R)-1-(isobutylsulfonyl)-4- methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one to give the compounds of Synthetic Examples'369 to 85. The names, morphologies and yields of the compounds synthesized are shown in Tablesb 9 and 20. TABLE 9 Ex Compound Name Morphol ogy Yi e l d l (trans-4- (hydroxymethy l ) cycl oh pal e ye l low 69 exyl ) -lH-pyrro l o 2 , 3 -h] [ 1 , 6 ] naph 38% t hyr i di n-4 ( s ol i d 7H) - one l - (trans-4-methoxycyc l ohexy l ) - l H 70 - yr r ol o [2 , 3-h] [ 1, 6] naphthyr i di n brown sol i d 42% - 4 (7H) -one 1- (l - {[5- (t r i f l uorome thy l ) furan- 71 2- yl ]methy l }pi per i di n-4-y l ) - lH-p ye l low so l i d quan t yrro l o[2, 3-h] [ 1, 6] naph thyri din-4 (7H) -one l - {l - [ (5-n i trofuran-2-yl ) me thy l ] 72 pi per i di n-4-yl }-lH-pyrro l o[2, 3-h Ye l l ow oi l 33% ] [ 1, 6]naphthyr i di n-4 (7H) -one ethy l 5- {[4- (4-oxo-4, 7-d ihydro- lH-pyrr ye 11ow 73 o l o [ 2 , 3-h] [ 1, 6] napht hyri din- l-y l amorphous quant ) piperi din- l - yl ]me thy l }furan-2-c a bo xyl a t e l - [l - (3 , 4-d i f l uorobenzyl ) pi per i d 74 i n-4-yl ] -lH-pyrro l o 2, 3-h] [ 1, 6] n Ye l l ow oi l 80% aphthyr i di n-4 (7H) -one l - [l - (3 , 4-d i ch l orobenz yl ) pi per i d 75 i n-4-yl ] - l H-pyrro l o[2, 3-h] [ 1, 6] n ye 1low so 1i d quant aphthyr i di n-4 (7H) -one l - (l - {[6- (tr i f l uoromethy ) pyri di n-3-y l ] methyl} p iperi di n-4-yl ) - l H 76 -pyrrol o ye l low so l i d quant [2 , 3-h] [ 1, 6] naphthyr i di n - 4 (7H) -one l - {l - [ (2-chl oroth i azol -5-yl ) me t h 77 yl ]pi per i di n-4-yl }-lH-pyrro l o[2, Ye l l ow oi l 69% 3-h] [ 1, 6] naphthyr i di n-4 (7H) -one l - {l - [4-fl uoro-3- (t r i fluoromet hy 1) benzy l ]pi per i di n-4-y l } - lH-pyrr 78 ye 1low so l i d 96% ol o[2, 3-h] [ 1, 6] naphthyri din-4 (7H ) -one l - {l - [ (5-n i trothi ophen-3-yl ) me t h 79 yl ]pi per i di n-4-yl }- l H-pyrro l o[2, brown s ol i d 27% 3-h] [ 1, 6] naphthyr i di n-4 (7H) -one l - {l - [ (5-bromofuran-2-yl ) methy l ] 80 piper i di n-4-yl }-lH-pyrro l o[2, 3-h ye l low so l i d quant ] [ 1, 6]naphthyr i di n-4 (7H) -one l - {l - [ (5-bromothi ophen-2-yl ) m h 81 yl ]pi per i di n-4-yl }-lH-pyrro l o[2, ye l low so l i d quant 3-h] [ 1, 6] naphthyr i di n-4 (7H) -one l - {l - [ (4-bromo thi ophen-2-yl ) me t h 82 yl ]pi per i di n-4-yl }- l H-pyrro l o[2, ye l low so l i d quant 3-h] [ 1, 6] naphthyr i di n-4 (7H) -one TABLE 20 SYNTHETIC EXAMPLE 15 86 1-(1 -r(2-Methylthiazol-4-yl)methyllpiperidin-4-yl)-1 H-pyrrolo[2,3-hin ,61naphthyridin- 4(7H)-one 1-(Piperidin-4-yl)-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3- h][1 ,6]naphthyridin-4(7H)-one (30 mg, 0.075 mmol) obtained in Reference Synthetic Example 1 99 in dichloromethane was stirred with 4-(chloromethyl)-2-methylthiazole hydrochloride ( 3.3 mg, 0.0901 mmol) and triethylamine (16 , 0.11 mmol) at 40°C for one day. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was roughly purified by silica gel column chromatography (chloroform / methanol = 9/1 (v/v)), and the resulting crude product was dissolved in dichloromethane (2 mL) and stirred with trifluoroacetic acid ( 1mL) at room temperature for 1 hour. The reaction mixture was concentrated under reduced pressure, and the residue was dissolved in a mixture of dichloromethane (2 mL) and methanol ( 1 mL) and stirred with ethylenediamine (200 pL) and 1 M aqueous sodium hydroxide ( 1 mL) for one day. After addition of water, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give the title compound as a brown oil (6.3 mg, yield 22%). SYNTHETIC EXAMPLE 1 87 1-[1 -(5-Chlorothiophene-2-carbonvDpiperidin-4-vH-1 H-pyrrolor2,3-hlf1 ,61naphthyridin- 4(7H)-one 1-[1 -(5-Chlorothiophene-2-carbonyl)piperidin-4-yl]-7-{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[2,3-h][1 ,6]naphthyridin-4(7H)-one obtained in Reference Synthetic Example 1 144 in dichloromethane (2 mL) was stirred with trifluoroacetic acid ( 1 mL) at room temperature for 1 hour. The reaction mixture was concentrated under reduced pressure, and the residue was dissolved in a mixture of dichloromethane (2 mL) and methanol ( 1 mL) and stirred with ethylenediamine (200 L) and 1 M aqueous sodium hydroxide ( 1 mL) for one day. The precipitated solid was collected by filtration to give the title compound as a colorless solid (22.8 mg, yield 73%). SYNTHETIC EXAMPLES' 3 88 TO 107 The reactions in Synthetic Example 14 were carried out in substantially the same manners except that the compounds obtained in Reference Synthetic Examples' 145 to 157, 167, 169, 170, 173, 174, 177 or 178 were used instead of rac-1-[(3R, 4R)-1- Benzyl-4-methylpiperidin-3-yl]-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 ,2,4,7-tetrahydropyrrolo[ 3', 2':5,6]pyrido[4,3-d][1 ,3]oxazine to give the compounds of Synthetic Examples'388 to 107. The names, morphologies and yields of the compounds synthesized are shown in Tables 2 1 and 22. TABLE 2 1 Ex Compound Name Morpho logy Yield 1- [1- (2-aminoethyl) piperidin-4-yl] - 88 lH-pyrrolo[3' ,2 ' :5, 6]pyrido[4, 3-d] p brown solid 90% yrimidine-2, 4(3H, 7H)-dione 1- {1- [(5-bromothiophen-2-yl) methyl ] piperidin-4-yl}-lH-pyrrolo[3' ,2 ' :5, 89 Colorless solid 77% 6 ]pyrido [4, 3-d] pyrimidine-2, 4 (3H, 7H )-d ione l-{l-[2-(tetrahydro-2H-thiopyran-4- yl) ethyl]piperidin-4-yl} -lH-pyrrolo 90 Colorless solid 26% [3' ,2 ' :5, 6]pyrido[4, 3~ d]pyrimidine- 2 , 4 (3H, 7H) -dione 1- [1- (cyclopropylmethyl) piperidin-4 9 1 -yl ]- lH-pyrro lo [3' ,2 ' :5 , 6]pyrido[4, Colorless solid 24% 3-d]pyrimidine-2,4(3H, 7H)-dione 1- [1- (2-methylbutyl) piperidin-4-yl] 92 -lH-pyrrolo[3' ,2 ' :5 , 6]pyrido[4, 3-d] Colorless solid 4% pyrimidine-2, (3H,7H) -dione l-{l-[2-(tetrahydro-2H-pyran-4-yl) e thyl] piperidin-4-yl} -lH-pyrrolo [3' , 93 Col or less solid 13% 2 ' ;5 , 6]pyrido[4, 3-d]pyrimidine-2,4 ( 3H, 7H) -dione 2- [4- (2, 4-dioxo-2, 3 , 4 , 7-tetrahydrolH- pyrrolo[3' ,2 ' :5, 6]pyrido[4, 3-d] p 94 Colorless solid 3% yrimidin-l-yl) piperidin-l-yl] aceton itr i1e 1- [1- (2, 2 , 2-trifluoroethyl)piperidi 9 5 n-4-yl]-lH-pyrrolo[3' ,2 ' :5 , 6 ] pyrido Colorless solid 38% [4, 3-d] pyrimidine-2, 4 (3H. 7H) -dione 5- [4 - (2, 4-dioxo-2, 3 , 4 , 7-tetrahydrolH- pyrrolo[3' ,2 ' :5, 6]pyrido[4, 3-d] p 96 Colorless solid 88% yrimidin-l-yl) piperidin-l-yl] pentan enitrile 1- [1- (6,6 , 6-trifluorohexyl)piperidi 9 7 n-4-yl]-lH-pyrrolo[3' ,2 ' :5,6]pyrido Colorless solid 29% [4, 3-d] pyrimidine-2, 4 (3H, 7H) -dione 4- [4 - (2, 4-dioxo-2, 3 , 4 , 7-tetrahydrolH- pyrrolo[3' ,2 ' :5, 6]pyrido[4, 3-d]p 98 Colorless solid 4% yrimidin-l-yl) piperidin-l-yl] butane nitr i1e TABLEb 22 SYNTHETIC EXAMPLE 108 -1-(2-Morpholinoethyl)piperidin-4-yll-1 H-pyrrolor3',2':5,61pyridor4.3-dlpyrimicline- 2.4(3H.7H)-dione 1-(Piperidin-4-yl)-7-{[2-(trimethylsty d]pyrimidine-2,4(3H,7H)-dione hydrochloride (30.0 mg, 0.0664 mmol) obtained in Reference Synthetic Example 9 1 and 4-(2-chloroethyl)morpholine hydrochloride (36.8 mg, 0.198 mmol) in acetonitrile ( 1 .5 mL) were mixed with N,N-diisopropylethylamine (79.5 L, 0.462 mmol) and stirred at 60°C for 15 hours and then with 4-(2- chloroethyl)morpholine hydrochloride (36.8 mg, 0.198 mmol) and N,Ndiisopropylethylamine (34.1 pL, 0.1 98 mmol) for 30.5 hours. The reaction mixture was allowed to cool to room temperature and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (methanol / chloroform = 3/97 12/88 (v/v)). The resulting crude product was dissolved in dichloromethane ( 1 .5 mL) and stirred with trifluoroacetic acid (0.5 mL) at room temperature for 2 hours. The reaction mixture was azeotropically distilled with toluene under reduced pressure, and the residue was dissolved in methanol (2 mL) and stirred with ethylenediamine (75 pL, 1.12 mmol) and 1 M aqueous sodium hydroxide (0.8 mL) at room temperature for 2.5 hours. The reaction mixture was concentrated under reduced pressure and, after addition of water, extracted with 1-butanol four times. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: methanol / chloroform = 0/1 9/91 (v/v)) to give the title compound as a colorless solid ( 1 .5 mg, yield 6% (three steps)). SYNTHETIC EXAMPLE 1 09 tert-Butyl 4-((2-r4-(2,4-dioxo-2,3,4.7-tetrahvdro-1 H-pyrrolor3'.2':5,6lpyridor4,3- dlpyrimidin-1 -yl)piperidin-1 -vnethyl)amino)piperidine-1 -carboxylate 1-[1-(2-Aminoethyl)piperidin-4-yl]-1 H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidine- 2,4(3H,7H)-dione (20.0 mg, 0.0609 mmol) obtained in Synthetic Example b 88 and tertbutyl 4-oxopiperidine-1 -carboxylate (24.3 mg, 0.122 mmol) in a mixture of methanol ( 1 ml_) and acetic acid (100 pL) were stirred with 2-picoline borane (13.0 mg, 0.122 mmol) at room temperature for 17 hours. The reaction mixture was basified with 1 M aqueous sodium hydroxide and extracted with a mixture of chloroform and 2-propanol four times. The organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (methanol / chloroform = 0/1 1/0 (v/v)) to give the title compound as a colorless solid ( 18.0 mg, yield 57%). SYNTHETIC EXAMPLE 110 1-(1 -(2-i(Cvclopropylmethyl)amino1ethyl)piperidin-4-yl)-1 H-pyrrolo[3',2':5,6lpyridof4,3- d1pyrimidine-2,4(3H,7H)-dione The reactions in Synthetic Example 1 109 were carried out in substantially the same manners except that cyclopropanecarbaldehyde was used instead of tert-butyl 4- oxopiperidine-1 -carboxylate to give the title compound as a colorless solid (5.5 mg, yield 23%). SYNTHETIC EXAMPLE 1 1 11 1-(1 -f2-(Piperidin-4-ylamino)ethvnpiperidin-4-ylM H-pyrrolof3',2':5,61pyridoi4,3- dlPyrimidine-2,4(3H,7H)-dione tert-Butyl 4-({2-[4-(2,4-dioxo-2,3,4,7-tetrahydro-1 ΐ[3',2':5,6^^ [4,3- d]pyrimidin-1-yl)piperidin-1-yl]ethyl}amino)piperidine-1 -carboxylate (16.9 mg, 0.0330 mmol) obtained in Synthetic Example 109 in a mixture of dichloromethane ( 1 mL) and methanol ( 1 mL) was stirred with trifluoroacetic acid ( 100 pL, 1.31 mmol) at room temperature for 2.5 hours and then with trifluoroacetic acid (400 pL, 5.23 mmol) at room temperature for 2.5 hours and then with trifluoroacetic acid (500 pL, 6.53 mmol) at room temperature for 4.5 hours and then with trifluoroacetic acid (2 mL, 26.1 mmol) at room temperature for 16 hours. The reaction mixture was concentrated under reduced pressure, and the resulting residue was purified by silica gel chromatography (Hi Flash column amino type manufactured by Yamazen Corporation: methanol / ethyl acetate = 1/4 4/1 (v/v)) to give the title compound as a colorless solid (4.21 mg, yield 30%). SYNTHETIC EXAMPLE 112 1-(trans-4-[((R)-3-Hydroxypyrrolidin-1 -yl)methyllcvclohexyl)-1 HPyrrolor3'. 2':5.61pyridof4,3-d1pyrimidine-2,4(3H.7H)-dione trans-4-(2,4-Dioxo-7-{[2-(trimethylsilyl)ethoxy]methyl}-2,3,4,7-tetrahydro-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidin-1-yl)cyclohexanecarbaldehyde (30.0 mg, 0.067 mmol) obtained in Reference Synthetic Example 168 in a mixture of methanol (0.5 mL) and acetic acid (50 pL) was stirred with (R)-3-hydroxy-pyrrolidine (14.3 mg, 0.088 mmol) and 2-picoline borane (9.4 mg, 0.088 mmol) at room temperature for 1 day. After addition of M aqueous sodium hydroxide, the reaction mixture was extracted with ethyl acetate, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel thin layer chromatography (ethyl acetate / methanol = 10/1 (v/v)) to give the compound as a colorless solid. The resulting colorless solid was dissolved in dichloromethane ( 1 .0 mL) and stirred with trifluoroacetic acid (0.4 mL) at room temperature for 5 hours. The reaction mixture was concentrated under reduced pressure, and the resulting residue was stirred with methanol (0.7 mL), ethylenediamine (30 L) and 1 M aqueous sodium hydroxide (30 pL) at room temperature for 1 day. The reaction mixture was filtered and the resulting solid was washed with water and methanol to give the title compound as a colorless solid (20.0 mg, yield 52% (three steps)). SYNTHETIC EXAMPLES' 113 TO 132 The reactions in Synthetic Example 1 12 were carried out in substantially the same manners except that 3-hydroxyazetidine hydrochloride, thiomorpholine-1 ,1- dioxide, 4,4-difluoropiperidine, 3,3'-iminodipropionitrile, cyclopropylmethylamine, (R)-3- cyanopyrrolidine, 3,3-dimethylazetidine, 2-methylaminoethanol, 2-(phenylmethyl)aminoethanol, 1-trifluoromethyl-1 -cyclopropylamine, N-(2-aminoethyl)morpholine, 2-(azetidin- 3-yl)acetonitrile hydrochloride, 2,2-dimethylcyclopropylamine hydrochloride, 1- aminomethylcyclohexanol, aminoacetonitrile hydrochloride, 4-trifluoromethylpiperidine, 3-(trifluoromethyl)azetidin-3-ol hydrochloride, tetrahydrofurylmethylamine, 2- methoxyethanamine or 3-amino-1 , 1 ,1-trifluoro-2-(pyridin-3-yl)propan-2-ol obtained in Reference Synthetic Example 1 179 were used instead of (R)-3-hydroxy-pyrrolidine to give the compounds of Synthetic Examples' 113 to 132. The names, morphologies and yields of the compounds synthesized are shown in Tables'323 and 24. TABLEb 23 Ex Compound Name Morpho logy Yi el d l - {trans-4- [ (3-hydroxyaze t i di n-l -yl )m ethyl ] cyc l ohe yl }- l H- r r ol o[3' , 2' 5, Co 1orl ess 62 % 113 6] pyr i do [4, 3-d] pyri mid i ne-2, 4 (3H, 7H) - s ol i d (3 s teps) di one l - {trans-4-[ ( l , 1-di oxi do hi omorphol i n o) met hyl ] cyc l ohexyl }-lH-pyrro l o[3' , 2' Co 1orl ess 33 % 114 :5, 6] pyri do [4, 3-d] pyri mid i ne-2, 4 (3H, 7 s ol i d (3 s tep s ) H) -di one l - {trans-4- [ (4, 4-di f luorop i per i di n- l yl ) me thyl ] cyc lohexy l }- lH-pyrro l o [ 3' , Co orl ess 68% 115 ' : 5, 6] pyr i do [4, 3-d] pyr i mi di ne-2, 4 (3H, s ol i d (3 s teps ) 7H) - i one 3, 3' - ( {[tran s -4- (2, 4-d i oxo-2, 3, 4, 7-t e trahydro- -pyrro l o [3' , 2' : 5, 6] pyr ido [ Co l orl ess 63 % 116 4, 3-d] pyr imi din- l -yl ) cycl ohexy l ] methy sol i d (3 s teps) 1 } a zane di y1) dipr opan en i t r i 1e l - (trans-4- {[ (cyc lopropylmethy l ) ami no ]me thy 1}cycl ohexy 1) - lH-pyr r ol o [3 ' , 2' : Co 1orl ess 45% 117 5, 6]pyr ido [4, 3-d] pyr imi di ne-2 , 4 (3H, 7H s ol i d (3 s tep s ) ) - dione (R) - 1- {[trans -4- (2, 4-d i oxo-2, 3, 4, 7-t e trahydro- -pyrro l o [3' , 2' : 5, 6] pyr ido [ Co 1orl ess 63 % 118 4, 3-d] pyr imi din- l - yl ) cycl ohexyl] methy s ol i d (3 s tep s ) l }pyrro l i dine-3-carbon i t r i l e l - {trans - 4- [ (3, 3-di methyl az et i di n- l - y D methy l ] cyc l ohexyl }-lH-pyrro l o[3' , 2' Brown 47% 119 :5, 6] pyri do [4, 3-d ] pyrimid i ne- 2, 4 (3H, 7 oi l (3 s t eps ) H) -di one l - (trans-4- {[ (2-hydroxyethy l ) (met hy l ) a i no] methyl }cyc l ohe y ) - lH-pyrro l o [3 Co 1orl ess 52 % 120 ' , 2' : 5, 6] pyr i do [4, 3-d] pyr i mid i ne-2, 4 ( sol i d (3 s tep s ) 3H, 7H) -di one l - (trans ~ 4- {[benzyl (2- hydroxy ethy l ) a m ino]me thy l }cycl ohexyl) - lH-pyrrol o [3 ' , Co 1orl ess 56 % 121 2' : 5, 6] pyr ido [4, 3-d] pyr imi dine-2 , 4 (3H soli d (3 s teps) , 7H) - di one l - [ trans-4- ( {[l - (t r i f l uororaet hyl ) cyc l op op yl ] amino }methy l ) cycl ohexy l ] - lH-p Co 1orl ess 43% 122 yrrol o [3' , 2' 5, 6] pyr ido [4, 3-d] pyr imi d sol i d (3 s teps) ine-2 , 4 (3H, 7H) - di one TABLEb 24 SYNTHETIC EXAMPLE 133 trans-4-(2^-Dioxo-2,3^J-tetrahvdro-1 H-pyrrolor3\2^5,6lpyridor4,3-d1pyrimidin-1 - vQcvclohexanecarbaldehyde 1-[trans -4-(Hydroxymethyl)cyclohexyl]-1 H-pyrrolo^^!S^pyrido^Sd] pyrimidine-2,4(3H,7H)-dione (35.0 mg, 0.111 mmol) obtained in Synthetic Example 101 in a mixture of toluene ( 1 mL) and dimethyl sulfoxide (0.25 mL) was mixed with 2- iodoxybenzoic acid (37.4 mg, 0.133 mmol) and stirred at 50°C for 2 hours. The reaction mixture was allowed to cool to room temperature and stirred with saturated aqueous sodium thiosulfate and saturated aqueous sodium hydrogen carbonate at room temperature for 30 minutes. The precipitated solid was collected by filtration to give the title compound as a colorless solid (26.7 mg, yield 77%). SYNTHETIC EXAMPLE 134 3-rtrans-4-(2.4-Dioxo-2,3,4,7-tetrahvdro-1 H-pyrrolor3',2':5.6lPyridor4.3-dlpyrimidin-1 - vDcyclohexyllpropanenitrile 3-[trans-4-(2,4-Dioxo-7-{[2-(trimethylsilyl)ethoxy]methyl}-2,3,4,7-tetrahydro-1 Hpyrrolo[ 3',2':5,6]pyrido[4,3-d]pyrimidin-1-yl)cyclohexyl]acrylonitrile (16.2 mg, 0.0347 mmol) obtained in Reference Synthetic Example 170 in tetrahydrofuran ( 1 .0 mL) was stirred with 5% palladium-carbon (10 mg) at room temperature for 1 day under a hydrogen atmosphere. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The resulting residue was dissolved in dichloromethane ( 1 .0 mL) and stirred with trifluoroacetic acid (0.4 mL) at room temperature for 5 hours. The reaction mixture was concentrated under reduced pressure, and the resulting residue was stirred with methanol (0.7 mL), ethylenediamine (30 pL) and 1 M aqueous sodium hydroxide (30 pL) at room temperature for 1 day. The reaction mixture was filtered, and the resulting solid was washed with water and methanol to give the title compound as a colorless solid (2.73 mg, yield 25% (three steps)). SYNTHETIC EXAMPLE 135 2-Cvano-N-irtrans-4-(2.4-dioxo-2.3,4,7-tetrahvdro-1 H-pyrrolor3',2':5.61pyridor4,3- dlpyrimidin-1-yl)cvclohexyllmethyll-N-(2,2,2-trifluoroethyl)acetamide 1-(4-{[(2,2,2-Trifluoroethyl)amino]methyl}cyclohexyl)-7-{[2- (trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidine-2,4(3H,7H)- dione (25.0 mg, 0.048 mmol) obtained in Reference Synthetic Example 1 169 in N,Ndimethylformamide ( 1 mL) was stirred with 2-cyanoacetic acid (10 mg, 0.071 mmol), O- (7-azabenzotriazol-1 -yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate (27 mg, 0.071 mmol) and N,N-diisopropylethylamine (16 pL, 0.095 mmol) at room temperature for 3 days. After addition of saturated aqueous sodium hydrogen carbonate, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (chloroform / methanol = 19/1 (v/v)) to give the compound as a yellow oil. The resulting yellow oil was dissolved in dichloromethane ( 1 .0 mL) and stirred with trifluoroacetic acid (150 pL) at room temperature for 1 day. The reaction mixture was concentrated under reduced pressure, and the resulting residue was stirred with methanol ( 1 mL), ethylenediamine (50 L) and 1 M aqueous sodium hydroxide (50 pL) at room temperature for 1 day. The precipitated solid was collected by filtration to give the title compound as a colorless solid (2.70 mg, yield 14%(three steps)). SYNTHETIC EXAMPLE 6 136 1-(trans-4-([Methyl(2,2.2-trifluoroethyl)amino1methyllcvclohexyl)-1 HPyrrolor3', 2':5,6lPyridof4,3-d1pyrimidine-2,4(3H,7H)-dione 1-(4-{[(2,2,2-Trifluoroethyl)amino]methyl}cyclohexyl)-7-{[2- (trimethylsilyOethoxyJmethylJ-I H-pyrrolofS'^'iS.eipyridot^.S-dlpyrimidine^^iSHyH)- dione (30 mg, 0.048 mol) obtained in Reference Synthetic Example 169 in a mixture of methanol ( 1 mL) and acetic acid ( 100 pL) was stirred with formaldehyde solution (37%) (20 pL) and 2-picoline borane ( 15 mg, 0.14 mmol) at room temperature for 3 days. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (chloroform / methanol = 19/1 (v/v)) to give the compound as a colorless solid. The resulting colorless solid was dissolved in dichloromethane ( 1 mL) and stirred with trifluoroacetic acid ( 150 l_) at room temperature for 1 day. The reaction mixture was concentrated under reduced pressure, and the resulting residue was stirred with methanol ( 1 mL), ethylenediamine (50 pL) and 1 M aqueous sodium hydroxide (50 pL) at room temperature for 1 day. The precipitated solid was collected by filtration to give the title compound as a colorless solid (24.95 mg, quantitative yield (three steps)). SYNTHETIC EXAMPLE 137 2-(1-Cvclohexyl-2,4-dioxo-1 H-pyrrolor3'.2':5,6lpyridof4.3-dlpyrimidin-3(2H,4H.7H)- vDacetonitrile 1-Cyclohexyl-7-{[2-(trimethylsilyl)ethoxy]methyl}-1 H-pyrrolo[3',2':5,6]pyrido[4,3- d]pyrimidine-2,4(3H,7H)-dione (20 mg, 0.048 mmol) obtained in Reference Synthetic Example 15 95 in N,N-dimethylformamide ( 1 mL) was mixed with potassium carbonate ( 10 mg, 0.072 mmol) and 2-chloroacetonitrile (5.0 pL, 0.072 mmol) and stirred at 80°C for 1 day. After addition of saturated aqueous ammonium chloride, the reaction mixture was extracted with chloroform, and the organic layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane = 1/4 1/3 (v/v)) to give the compound as a yellow oil. The resulting yellow oil was dissolved in dichloromethane ( 1 mL) and stirred with trifluoroacetic acid (150 pL) at room temperature for 1 day. The reaction mixture was concentrated under reduced pressure, and the resulting residue was stirred with methanol ( 1 mL), ethylenediamine (50 pL) and 1 M aqueous sodium hydroxide (50 pL) at room temperature for 1 day. The precipitated solid was collected by filtration to give the title compound as a colorless solid (24.5 mg, yield 79%(three steps)). SYNTHETIC EXAMPLES' 138 TO 154 The reactions in Synthetic Example 137 were carried out in substantially the same manners except that iodomethane, 2,2,2-trifluoroethyl trifluoromethanesulfonate, 2-bromoethanol, 3-bromopropan-1-ol, 4-(2-chloroethyl)morpholine hydrochloride, chloro(methoxy)methane, 1-bromo-4-fluorobutane, 1-bromo-2-methoxyethane, 2- bromopropanenitrile, (chloromethyl)(methyl)sulfane, bromocyclopentane, (bromomethyl)cyclopropane, 2-(bromomethyl)tetrahydrofuran, 3-(chloromethyl)-3- methyloxetane, 2-chloro-N,N-dimethylacetamide, 2-chloro-N,N-dimethylethanamine hydrochloride or tert-butyl 4-bromopiperidine-1-carboxylate were used instead of 2- chloroacetonitrile to give the compounds of Synthetic Examples 138 to 154. The names, morphologies and yields of the compounds synthesized are shown in Tables 25 and 26. TABLE 25 Ex Compound Name Mor ho ogy Yi e l d l - cycl oh ex yl-3-me t hyl l H-p yrro l o [3' Co l orl es s 5 9 138 , 2' : 5, 6] pyri do [4, 3-d] pyrim i di ne-2, 4 so i d (3s t eps) (3H, 7H) -di one l-cy cl oh exyl- 3- (2 , 2, 2- t rif luor oe thy 139 Co or l es s 49% 1) - l H-pyrrolo [3 ' , 2' :5, 6] pyr i do [4 , 3 so l i d (3s teps) d] pyri mi di ne-2, 4 (3H, 7H) -di on e l - cycl oh ex yl- 3- (2 - hydroxye thyl ) - lH1 Co l orl es s 61% 40 pyrr ol o [3' , 2' :5, 6] pyr i do [4, 3 d] pyri so l (3s t eps) mi di ne-2 , 4 (3H, 7H) - dione l - cycl oh ex yl- 3- (3 - hydroxypropy l ) - 1H 141 - pyrro l o [3 ' , 2' : 5, 6] pyr i do [4, 3- d] py Co lorl es s 31% so l i d (3s teps) i mi di ne-2, 4 (3H, 7H) -di on e l - cy cl oh ex yl-3- (2 -morphol i no et hy l ) - Co lorl es s 68% 142 lH-p yrro l o [3' , 2' : 5, 6] pyrido [4, 3- d] p yr so i d (3s teps) i mi di ne-2, 4 (3H, 7H) -di one l - cyc l oh exyl- 3- (met hoxymet hy l ) - 1H-p 1 Co orl es s 49% 43 yrro l o [3 ' , 2' : 5, 6] pyri do [4, 3 d] pyrim so l i d (3s teps) i di ne-2, 4 (3H, 7H) - di on e l-cy cl oh ex yl- 3- (4-f luorobu t yl ) - 1H-p 144 yrro l o [3 ' , 2' : 5, 6] pyri do [4, 3-d] pyrim Co l orl es s 55% i di ne-2, 4 ( so (3s teps) 3H, 7H) - di on e l-cy cl oh ex yl- 3- (2 -met hoxye t hyl ) - lH145 pyrr ol o[3' , 2' Co l orl es s 60% ' 5 , 6] pyr i do [4 , 3 d] pyri so l i d (3s teps) mi di ne - 2, 4 (3H , 7H) - dione 2- ( l - c yc lohex yl - 2, 4-d i oxo- lH-pyrrol 146 o [3' , 2' Co lor 1es s 72% 5, 6] pyr ido [4, 3-d] pyr i mi din3 (2H, so i d (3s teps) 4H, 7H) - yl ) pr opan en itr i l e l-cy cl oh ex yl-3- [ (me t hyl thi o) me thyl ] Co l orl es s 80% 147 - l H-pyrrol o 3 ' , 2' :5, 6] pyri do [4 , 3-d] so l i d (3s teps) pyri mi di ne -2, 4 (3H, H) - dion e TABLEb 26 SYNTHETIC EXAMPLE 5 155 N-(ftrans-4-(2^-Dioxo-2,3.47-tetrahvdro-1 H-Pyrrolof3:2^5,61pyridof4,3-d1pyrimidin-1 - yl)cvclohexynmethyl)-3,3,3-trifluoro-N-(2,2,2-trifluoroethyl)propanamide The reactions in Synthetic Example1 135 were carried out in substantially the same manners except that 3,3,3-trifluoropropanoic acid was used instead of 2- cyanoacetic acid to give the title compound as a colorless solid ( 1 .95 mg, yield 8% (three steps)). The structural formulae of the compounds obtained the Reference Synthetic Examples' and Synthetic Examples are shown below in Tables'327 to 44. The physical property data on the compounds obtained the Reference Synthetic Examples'3 and Synthetic Examples are shown below in Tables'345 to 77. TABLE 27 TABLEb 28 TABLEb 29 TABLEb 30 TABLEb 3 1 TABLEb 32 TABLE 33 TABLEb 34 TABLEb 35 TABLEb 36 TABLEb 37 TABLE" 38 TABLEb 39 TABLEb 40 TABLEb 4 1 TABLEb 42 TABLEb 43 TABLE 44 TABLEb 45 Rf Da t a - NMR ( CD3 0 D) 3 . 3 1 ( s , 3H) , 3 . 7 6 ( s , 3H) , 7 . 2 8 ( d , = 5 . 3 6 Hz , 1 H) , 8 . 1 8 ( d , = 4 . 7 6 Hz , 1 H) , 8 . 5 7 ( s , 1H) . 1 L C/ MS : c o n i t i o n 1 , r e t e n t i o n t i me = 0 . 5 4 i n L C/ MS (E S I +) m/ z ; 16 7 [ + H] + H- NMR ( CDC 1 ) : 0 . 9 8 ( d , = 6 . 5 Hz , 3H) , 1 . 5 6 - 1 . 8 3 (m, 3H) , 2 . 2 0 - 2 . 3 5 (m, 1H) , 2 . 6 1 - 2 . 8 5 ( m, 1H) , 3 . 3 1 ( d , = 1 0 . 9 Hz , 1H) , 3 . 5 3 ( d , / = 1 4 . 9 Hz , 1H) , 3 . 6 7 ( s , 3 H) , 4 . 0 2 ( d d , J = 1 3 . 0 , 5 . 4 , 2 1H) , 4 . 1 3 - 4 . 2 6 (m, 2 H) , 7 . 4 7 ( d , J = 2 . 4 Hz , 2 H) , 7 . 5 5 ( d , J = 2 . 3 8 Hz , 3 H) , 12 . 4 ( b s , 1 H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me - 0 . 5 1 mi n L C/ MS (E S I +) m/ z ; 2 6 3 [ M+ H] + - NMR ( CDCl 3 ) 0 . 9 2 ( d , 3H) , 1 . 4 1- 1 . 5 3 (m, 3 H) , 1 . 9 0 - 2 . 1 8 ( m, 2 H) , 2 . 6 5 - 2 . 8 9 ( m, 3 H) , 3 . 4 6 ( s , 2H) , 7 . 1 8 - 7 . 4 0 (m, 5 H) . 3 LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 4 7 mi n L C/ MS ( E S I +) m/ z ; 2 0 5 [ M+ H] + ' H- NMR ( C DC I 3 ) : 6 . 5 5 ( d , J = 3 . 3 Hz , 1H) , 7 . 0 6 ( d d , J = 8 . 0 , 6 . 3H , 1H) , 7 . 4 3 ( d , J = 3 . 3 Hz , 1H) , 7 . 7 0 ( d , = 8 . 0 Hz , 1H) , 8 . 2 6 ( d , 4 J = 6 . 3 Hz , 1H) . L C/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 6 4 mi n L C/ MS (E S I +) m/ z ; 1 3 5 . 0 [ M+ H] + Ή - NMR ( C DC I 3 ) : 6 . 6 3 ( d , J = 3 . 6 Hz , 1H) , 7 . 14 ( d , J = 5 . 2 Hz , 1 H) , 7 . 3 9 ( d , J = 3 . 6 Hz , 1H) , 8 . 2 2 ( d , J = 5 . 2 Hz , 1H) , 1 0 . 4 ( b r 5 s , 1H) . L C/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 16 mi n LC/ MS ( E S I +) m/ z ; 15 3 , 1 5 5 [M+H] + - NMR ( CDC I 3 ) 1 . 1 1 ( d , J = 7 . 5 Hz , 1 8H) , 1 . 8 4 ( s e p t e t , J = 7 . 5 Hz , 3H) , 6 . 6 5 ( d , / = 3 . 6 Hz , 1H) , 7 . 0 6 ( d , 5 . 2 Hz , H) , 7 . 3 3 6 ( d , J = 3 . 6 Hz , 1H) , 7 . 7 5 ( d , J = 5 . 2 Hz , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 6 . 9 1 mi n L C/ MS ( E S I +) m/ z ; 3 0 9 , 3 1 1 [M+H] + H- NMR (DMS0 - f ) : 6 . 7 3 ( d d , J = 3 . 6 , 2 . 1 Hz , 1 H) , 7 . 7 5 ( b r t , J = 3 . 0 Hz , 1H) , 8 . 6 8 ( s , 1H) , 1 0 . 4 ( s , 1H) , 12 . 5 ( b s , 1 H) . 7 LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 1 9 mi n L C/ MS ( E S I +) m/ z ; 18 1 , 18 3 [M+H] + L C/ MS ( E S I - ) m/ z ; 1 7 9 , 18 1 [M- H] 1H- NMR ( C DC I 3 ) : 1 . 2 9 - 1 . 5 6 ( m, 4 H) , 1 . 6 0 - 1 . 7 5 (m, 2 H) , 1 . 7 8 - 1. 9 2 ( , 2 H) , 2 . 0 7 - 2 . 2 0 (m, 2 H) , 3 . 9 4 - 4 . 0 6 ( m, 1H) , 6 . 5 9 ( d , = 3 . 6 Hz , 1H) , 7 . 10 ( d , = 3 . 6 Hz , 1H) , 8 . 2 0 ( s , 1H) , 9 . 6 2 ( b r d , 8 = 7 . 6 Hz , 1H) , 9 . 8 0 ( s , 1H) , 1 1 . 0 ( b r s , 1H) . L C/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 0 2 mi n LC/ MS ( E S I +) m/ z ; 2 4 4 [ M+ H] + - NMR ( CDC l , ) : - 0 . 0 5 ( s , 9H) , 0 . 9 1 ( t , J = 8 . 5 Hz , 2H) , 1 . 2 5 - 1 . 7 5 ( m, 6H) , 1 . 7 5 - 1 . 9 0 (m, 2 H) , 2 . 0 7 - 2 . 2 0 ( m, 2H) , 3 . 5 4 ( t , = 8 . 5 Hz , 2 H) , 3 . 9 0 - 4 . 0 5 (m, 1H) , 5 . 6 1 ( s , 2 H) , 6 . 6 0 ( d , / = 3 . 8 Hz , 1H) , 9 7 . 0 9 ( d , J = 3 . 8 Hz , 1 H) , 8 . 1 8 ( s , 1H) , 9 . 5 8 ( b r d , J = 7 . 7 Hz , 1 H) , 9 . 8 0 ( s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 5 . 2 2 mi n LC/ MS (E S I +) m/ z ; 3 7 4 [ M+ H] + TABLEb 46 TABLE 47 Rf Da t a LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 5 . 0 1 mi n 2 1 LC/ MS ( E S I +) m/ z ; 3 8 8 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 4 . 0 1 mi n 2 3 L C/ MS ( E S I +) m/ z ; 4 0 2 [ M+H] + •H- NMR ( CDC1 3 ) - 0 . 0 6 ( s , 9 H) , 0 . 9 3 ( t , J = 8 . 1 Hz , 2 H) , 1 . 5 0 - 1 . 9 5 ( m, 6H) , 2 . 0 0 - 2 . 1 5 (m, 2H) , 2 . 2 0 - 2 . 3 0 (m, 2 H) , 3 . 5 6 ( t , J = 8 . 1 Hz , 2 H) , 4 . 8 5 - 5 . 0 0 (m, 1H) , 5 . 8 0 ( s , 2 H) , 6 . 4 3 ( d , = 8 . 1 Hz , 1H) , 2 4 6 . 8 1 ( d , J = 3 . 6 Hz , 1H) , 7 . 4 3 ( d , J = 3 . 9 Hz , 1 H) , 7 . 7 7 ( d , J = 8 . 1 Hz , 1H) , 9 . 4 1 ( s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 4 . 6 4 mi n L C/ MS (E S I +) m/ z ; 3 9 8 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 5 . 4 6 mi n 2 5 . L C/ MS ( E S I +) m/ z ; 3 8 7 , 3 8 9 [ M+H ] + Ή - NMR ( CDC I 3) 1 . 3 0 - 1 . 6 0 ( m, 4 H) , 1 . 6 0 - 1 . 8 0 (m, 2 H) , 1 . 8 0 - 1 . 9 5 ( , 2 H) , 2 . 1 0 - 2 . 2 5 ( , 2H) , 3 . 0 7 ( s , 3 H) , 3 . 9 5 - 4 . 10 (m, 1H) , 6 . 6 1 ( d , 2 6 J = 3 . 3 Hz , 1H) , 7 . 1 5 - 7 . 2 5 ( m, 2 H) , 8 . 5 4 ( s , 1H) , 1 1 . 8 2 ( b r s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 3 1 mi n LC/ MS ( E S T ) m/ z ; 2 9 4 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 4 . 8 7 mi n 2 8 L C/ MS ( E S I +) m/ z ; 4 3 4 [M+H ] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 4 . 2 6 mi n 2 9 LC/ MS ( E S I + ) m/ z ; 3 9 0 [M+ l ] + L C/ MS ( E S I - ) m/ z ; 3 8 8 [ M- l ] - 1H- NMR ( CDCI 3 ) - 0 . 0 5 ( s , 9 H) , 0 . 9 1 ( t , J = 8 . 1 Hz , 2 H) , 1 . 3 5 - 1 . 4 5 ( m, 5H) , 1 . 6 0 - 1 . 7 0 (m, 1H) , 1 . 7 5 - 1 . 9 0 (m, 2 H) , 2 . 0 5 - 2 . 2 0 ( m, 2 H) , 3 . 5 4 ( t , J = 7 . 8 Hz , 2 H) , 3 . 9 0 - 4 . 0 5 ( m, 1H) , 5 . 5 8 ( s , 2 H) , 5 . 5 5 - 5 . 7 0 3 0 ( m, 2 H) , 6 . 5 9 ( d , J = 3 . 6 Hz , 1H) , 7 . 0 8 ( d , J = 3 . 9 Hz , 1H) , 8 . 2 9 ( s , 1 H) , 9 . 3 2 ( d , J = 7 . 5 Hz , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 4 . 0 2 mi n L C/ MS ( E S I +) m/ z ; 3 8 9 [M+H ] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 4 . 9 7 mi n 3 1 LC/ MS ( E S I +) m/ z ; 4 1 7 [M+H ] + - NMR ( CD CI 3 ) : - 0 . 0 6 ( s , 9 H) , 0 . 9 3 ( t , J = 8 . 1 Hz , 2 H) , 1 . 5 0 - 2 . 0 0 ( m, 6 H) , 2 . 0 0 - 2 . 15 (m, 2H) , 2 . 2 0 - 2 . 4 0 (m, 2 H) , 3 . 5 6 ( t , J = 8 . 1 Hz , 2 H) , 4 . 7 0 - 4 . 8 5 (m, 1H) , 5 . 7 9 ( s , 2 H) , 6 . 7 7 ( d , J = 4 . 2 Hz , 1H) , 3 2 7 . 5 1 ( d , J = 3 . 9 Hz , 1H) , 8 . 5 0 ( s , 1H) , 9 . 3 2 ( s , 1H) . L C/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 4 . 4 2 mi n L C/ MS (E S I +) m/ z ; 3 9 9 [M+H] + ' H- NMR ( CDC I 3 ) - 0 . 0 6 ( s , 9H) , 0 . 8 5 - 1 . 0 .0 (m, 2H) , 2 . 7 6 ( s , 3H) , 3 . 5 0 - 3 . 6 0 (m, 2H) , 5 . 6 8 ( s , 2H) , 6 . 7 4 ( d , J = 3 . 6 Hz , 1H) , 7 . 4 4 3 3 ( s , J = 3 . 6 Hz , 1H) , 8 . 6 6 ( s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 4 . 8 7 mi n L C/ MS (E S I +) m/ z ; 3 2 5 , 3 2 7 [ M+H] + TABLEb 48 Rf Da t a - NMR ( CDC l ) - 0 . 0 6 ( s , 9 H) , 0 . 9 0 ( t , / = 8 . 1 Hz , 2 H) , 0 . 9 8 ( d , = 6 . 6 Hz , 3H) , 1 . 6 0 - 1 . 8 5 (m, 2 H) , 1 . 9 0 - 2 . 0 0 ( , 1H) , 2 . 2 0 - 2 . 3 0 ( , 1H) , 2 . 2 5 - 2 . 3 5 ( , 1H) , 2 . 6 7 ( s , 3 H) , 2 . 7 0 - 2 . 9 0 ( , 2 H) , 3 4 3 . 4 5 - 3 . 6 0 ( , 4 H) , 4 . 3 0 - 4 . 4 0 (m, 1H) , 5 . 5 7 ( s , 2 H) , 6 . 5 8 ( d , = 3 . 6 Hz , 1H) , 7 . 0 0 ( d , / = 3 . 9 Hz , 1H) , 7 . 1 0 - 7 . 4 0 (m, 5 H) , 8 . 6 6 ( s , 1 H) , 1 0 . 7 0 ( d , ; = 9 . 9 Hz , 1 H) . Ή - NMR ( CDC l ) : - 0 . 0 8 ( s , 9 H) , 0 . 8 6 ( d , = 6 . 9 Hz , 3 H) , 0 . 9 1 ( t , = 8 . 1 Hz , 2H) , 1 . 7 0 - 2 . 0 0 (m, 2H) , 2 . 4 0 - 2 . 6 0 ( m, 2 H) , 2 . 7 5 - 2 . 9 0 (m, 2H) , 2 . 9 5 - 3 . 0 5 (m, 1H) , 3 . 5 0 - 3 . 6 5 ( , 4 H) , 5 . 3 5 - 5 . 4 5 ( m, 1H) , 5 . 7 8 ( d d , 3 5 J = 10 . 5 , 1 5 . 0 Hz , 2 H) , 6 . 3 9 ( d , / = 8 . 1 Hz , 1 H) , 6 . 8 1 ( d , = 3 . 9 Hz , 1H) , 7 . 2 5 - 7 . 4 0 ( m, 5 H) , 7 . 4 1 ( d , = 3 . 6 Hz , 1H) , 8 . 5 4 ( b r s , 1H) , 9 . 4 1 ( s , 1H) . L C/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 5 9 mi n LC/ MS ( E S I +) m/ z ; 5 0 3 [ M+H ] + L C/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 0 6 mi n 3 6 LC/ MS ( E S I +) m/ z ; 4 1 3 [ M+H] + ' H- NMR ( CDC l j ) : - 0 . 0 6 ( s , 9 H) , 0 . 9 3 ( t , = 8 . 1 Hz , 2 H) , 1 . 0 2 ( d , J - 7 . 5 Hz , 3H) , 1 . 14 ( d , = 6 . 6 Hz , 6 H) , 1 . 8 0 - 1 . 9 0 (m, 1H) , 2 . 1 5 - 2 . 4 5 ( , 2 H) , 2 . 6 5 - 2 . 8 0 ( , 1H) , 2 . 8 7 ( d , J = 6 . 6 Hz , 2 H) , 3 . 1 5 - 3 . 3 5 ( m, 1H) , 3 . 5 6 ( t , J = 8 . 1 Hz , 2 H) , 3 . 5 5 - 3 . 7 5 ( m, 2 H) , 3 . 8 5.- 3 . 9 5 ( m, 1 H) , 5 . 3 5 - 5 . 4 5 (m, 1H) , 5 . 8 0 ( s , 2 H) , 6 . 4 0 ( d , / = 3 7 7 . 8 Hz , 1H) , 6 . 7 5 ( d , = 3 . 6 Hz , 1H) , 7 . 4 6 ( d , J = 3 . 9 Hz , 1 H) , 7 . 6 0 ( d , J = 8 . 1 Hz , 1H) , 9 . 4 2 ( s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 4 . 5 2 mi n LC/ MS ( E S I +) m/ z ; 5 3 3 [ M+H ] + LC/ MS ( E S r ) m/ z ; 5 7 7 [ M+HCOO] LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 5 4 mi n 3 8 LC/ MS ( E S I ) m/ z ; 3 4 9 [ M+H ] + ' H- NMR ( CDC 1 3 ) : - 0 . 0 6 ( s , 9 H) , 0 . 8 7 - 0 . 9 5 (m, 2 H) , 0 . 9 8 ( d , J = 6 . 9 Hz , 3 H) , 1 . 5 9 - 1 . 8 0 ( m, 2H) , 1 . 8 7 - 2 . 0 4 ( m, 1H) , 2 . 1 4 - 2 . 2 4 (m, 1H) , 2 . 3 8 - 2 . 4 1 (m, 1H) , 2 . 8 5 - 2 . 8 9 (m, 2 H) , 3 . 4 7 - 3 . 6 2 (m, 4 H) , 4 . 2 8 - 4 . 3 9 ( , 1H) , 5 . 5 9 ( s , 2 H) , 6 . 5 9 ( d , 3 9 J = 3 . 6 Hz , 1H) , 7 . 0 4 ( d , J = 3 . 9 Hz , 1H) , 7 . 1 7 - 7 . 3 9 (m, 5H) , 8 . 2 0 ( s , 1H) , 9 . 8 7 ( s , 1 H) , 1 0 . 0 ( d , J = 9 . 5 Hz , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 5 7 mi n L C/ MS ( E S I +) m/ z ; 4 7 9 [ M+H] + Ή - NMR ( CDC l ) : - 0 . 0 7 ( s , 9 H) , 0 . 8 6 - 0 . 9 2 (m, 2 H) , 1 . 0 1 ( d , J = 6 . 6 Hz , 3 H) , 1 . 4 3 - 1 . 9 6 ( , 3H) , 2 . 0 7 - 2 . 1 4 ( m, 1H) , 2 . 2 5 - 2 . 2 8 (m, 1H) , 2 . 7 8 - 2 . 9 3 (m, 2H) , 3 . 4 6 - 3 . 5 5 (m, 4 H) , 4 . 2 0 - 4 . 3 1 (m, 1 H) , 4 . 7 7 ( d d , 4 0 J = 2 0 . 8 , 1 2 . 2 Hz , 2 H) , 5 . 5 7 ( s , 2 H) , 5 . 9 5 ( d , = 9 . 8 Hz , 1 H) , 6 . 5 1 ( d , = 3 . 6 Hz , 1H) , 7 . 0 7 ( d , = 3 . 6 Hz , 1H) , 7 . 1 8 - 7 . 2 9 ( , 5 H) , 7 . 8 7 ( s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 0 4 mi n L C/ MS ( E S I +) m/ z ; 4 8 1 [ M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 2 . 9 1 mi n 4 1 L C/ MS ( E S I +) m/ z ; 3 6 3 [ M+H - S EM] + Ή - NMR (DMS f ) : 8 . 3 0 ( b r s , 1H) , 8 . 4 4 ( s , 1H) , 8 . 4 9 ( s , 1H) LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 8 9 mi n 4 2 LC/ MS ( E S I +) m/ z ; 1 9 8 , 2 0 0 [ M+H ] + L C/M S ( E S r ) m/ z ; 1 9 6 , 1 9 8 [ M-H ] - T ABLEb 4 9 Rf Da t a L C/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 5 4 mi n 4 3 L C/ MS ( E S I +) m/ z ; 2 14 , 2 1 6 [M+H] + Ή - NMR (DMSO- ) <5 : 8 . 5 0 ( s , 1H) , 8 . 5 6 ( s , 1H) , 8 . 5 7 ( d , J = 1 . 8 Hz , 1H) . 4 4 L C/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me - 2 . 7 4 mi n LC/ MS (E S I +) m/ z ; 2 3 2 , 2 3 4 , 2 3 6 [ M+H] + L C/ MS ( E S I ) m/ z ; 2 3 0 , 2 3 2 , 2 3 4 [ M-H ] Ή - NMR ( CD C1 ) - 0 . 0 4 ( s , 9H) , 0 . 9 4 ( t , J = 8 . 4 Hz , 2 H) , 2 . 7 9 ( s , 3H) , 3 . 6 2 ( t , 8 . 4 Hz , 2H) , 5 . 6 9 ( s , 2 H) , 8 . 3 0 ( s , 1 H) , 8 . 7 3 4 6 ( s , 1H) . L C/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 4 . 3 1 mi n L C/ MS ( E S I +) m/ z ; 3 2 6 , 3 2 8 [M+H] + ' H- NMR ( CDC I 3 ) - 0 . 0 3 ( s , 9 H) , 0 . 9 3 ( t , J = 8 . 4 Hz , 2H) , 1 . 2 2 - 1 . 7 8 ( m, 6 H) , 1 . 7 8 - 1 . 9 0 (m, 2 H) , 2 . 0 3 - 2 . 18 (m, 2 H) , 2 . 6 3 ( s , 3H) , 3 . 6 1 ( t , J = 8 . 4 Hz , 2 H) , 4 . 8 7 - 5 . 0 3 ( m, 1H) , 5 . 5 8 ( s , 2 H) , 7 . 8 8 ( s , 1H) , 4 7 8 . 6 9 ( s , 1H) , 1 0 . 1 0 ( b r s , 1H) . L C/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 5 . 19 mi n L C/ MS ( E S I +) m/ z ; 3 8 9 [ M+ H] + ' H- NMR ( CDC I 3 ) - 0 . 0 4 ( s , 9H) , 0 . 9 5 ( t , J = 8 . 4 Hz , 2 H) , 1 . 2 0 - 1 . 3 8 ( m, H) , 1 . 5 8 - 2 . 2 4 (m, 9 H) , 3 . 6 5 ( t , J = 8 . 4 Hz , 2 H) , 5 . 7 7 ( s , 2 H) , 6 . 4 6 ( d , J = 8 . 0 Hz , 1H) , 6 . 4 0 - 6 . 5 5 ( , 1H) , 7 . 8 1 ( d , = 8 . 0 Hz , 4 8 1 H) , 8 . 1 6 ( s , 1H) , 9 . 4 7 ( s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me - 4 . 6 6 mi n L C/ MS ( E S I +) m/ z ; 3 9 9 [ M+ H] + TABLEb 50 Rf Da t a Ή - NMR (CDC 13 ) - 0 . 0 4 ( s , 9 H) , 0 . 9 2 ( t , J = 8 . 4 Hz , 2 H) , 2 . 7 4 ( s , 3 H) , 3 . 5 3 ( t , J = 8 . 7 Hz , 2 H) , 5 . 6 4 ( s , 2 H) , 7 . 4 8 ( s , 1H) , 4 9 8 . 5 4 ( s , 1H) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 5 . 1 9 mi n LC/ MS ( ES m/ z ; 4 0 3 , 4 0 5 [M+H] + Ή - NMR (CDC 1 ) - 0 . 0 7 ( s , 9H) , 0 . 7 2 ( d , J = 6 . 3 Hz , 3 H) , 0 . 9 6 ( t , J = 8 . 1 Hz , 2H) , 1 . 4 5- 1. 6 0 (m, 1H) , 1 . 7 0 - 1 . 9 0 (m, 2H) , 2 . 0 5 - 2 . 1 8 (m, 1H) , 2 . 3 1 - 2 . 4 2 (m, 1H) , 2 . 7 1 ( s , 3H) , 2 . 8 8 - 3 . 0 0 (m, 5 0 1H) , 3 . 10 - 3 . 2 2 (m, 1H) , 3 . 5 1 - 3 . 6 9 (m, 4 H) , 4 . 6 0 - 4 . 8 0 (m, 1H) , 5 . 6 1 ( d d , J = 1 0 . 8 , 16 . 2 Hz , 2 H) , 7 . 2 1- 7 . 4 3 (m, 6H) , 8 . 6 5 ( s , 1H) . LC/ MS '. c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 8 6 mi n LC/ MS ( ES I +) m/ z ; 5 7 1, 5 7 3 [M+H] + - NMR (CDC I 3 ) - 0 . 0 8 ( s , 9H) , 0 . 2 0 ( d , J = 6 . 9 Hz , 3 H) , 0 . 9 0 ( t , J = 8 . 7 Hz , 2H) , 1 . 4 0 - 1. 5 2 (m, 1H) , 1 . 6 2 - 1 . 7 2 (m, 1H) , 1. 8 2 - 2 . 0 0 (m, 1H) , 2 . 0 5 - 2 . 2 0 ( , 1H) , 2 . 7 0 - 2 . 8 2 (m, 1H) , 3 . 0 2 - 3 . 1 7 (m, 1H) , 3 . 5 0 - 3 . 6 0 (m, 4H) , 3 . 6 0 - 3 . 7 1 (m, 1H) , 5 1 5 . 4 0 - 5 . 5 0 (m, 1H) , 5 . 74 ( d d , = 13 . 8 , 1 0 . 5 Hz , 2H) , 6 . 4 4 ( d , J 7 . 8 Hz , 1H) , 7 . 2 0 - 7 . 4 5 (m, 5 H) , 7 . 4 7 ( s , 1H) , 9 . 3 4 ( s , 1H) , 9 . 4 9 ( d , J = 7 . 8 Hz , 1H) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 4 . 8 9 mi n LC / MS ( ES I + ) m/ z ; 5 8 1, 5 8 3 [ M+ H] + -NMR (CDCI 3 ) : - 0 . 0 5 ( s , 9H) , 0 . 9 1 ( t , J = 8 . 4 Hz , 2 H) , 2 . 7 4 ( s , 3 H) , 3 . 5 2 ( t , = 8 . 1 Hz , 2 H) , 5 . 6 3 ( s , 2 H) , 7 . 4 0 ( s , 1H) , 5 2 8 . 54 ( s , 1H) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 5 . 0 0 mi n LC/ MS ( ES I + ) m/ z ; 3 5 9 , 3 6 1 [ M+ H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 6 7 mi n 5 3 LC/ MS ( ES m/ z 5 2 7 , 5 2 9 [M+H] + Ή -NMR (CDC I 3 ) - 0 . 10 ( s , 9H) , 0 . 2 7 ( d , J = 6 . 9 Hz , 3 H) , ( t , J = 8 . 4 Hz , 2H) , 1 . 4 1- 1. 5 6 (m, 1H) , 1 . 6 0 - 1 . 8 0 (m, 1. 86 - 2 . 0 3 (m, 1H) , 2 . 0 6 - 2 . 2 0 (m, 1H) , 2 . 6 8 - 2 . 8 0 ( , 3 . 0 5 - 3 . 2 0 (m, 1H) , 3 . 5 0 - 3 . 7 0 (m, 5 H) , 5 . 3 5 - 5 . 4 2 (m, 1H) , 5 . 74 5 4 2H) , 6 . 4 4 ( d , J = 8 . 1 Hz , 1H) , 7 . 2 2 - 7 . 4 8 (m, 6 H) , 9 . 3 4 ( s , 9 . 4 5 ( d , J = 8 . 1 Hz , 1H) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 4 . 6 0 mi n LC/ MS ( ES I +) m/ z ; 5 3 7 , 5 3 9 [ M+ H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 4 . 7 9 mi n 5 5 LC/ MS ( ES I + ) m/ z ; 3 1 1, 3 13 [M+H] + 'H- NMR (CDCI 3 ) : - 0 . 0 7 ( s , 9H) , 0 . 9 0 ( t , J = 8 . 4 Hz , 2 H) , 1. 0 0 ( t , J = 7 . 2 Hz , 3H) , 1 . 9 1 ( q u i n t , J = 7 . 2 Hz , 2 H) , 3 . 5 3 ( t , J = 8 . 4 Hz , 2H) , 5 . 1 0 - 5 . 2 0 ( m, 1H) , 5 . 6 5 ( s , 2 H) , 6 . 6 0 ( d , J = 3 . 6 5 6 Hz , 1H) , 7 . 3 6 ( d , J = 3 . 6 Hz , 1H) , 8 . 4 5 ( s , 1H) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 4 . 8 1 mi n LC/ MS ( ES I + ) m/ z ; 3 4 1, 3 4 3 [ M+ H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 5 . 2 1 mi n 5 7 LC/ MS ( ES I +) m/ z ; 3 3 9 , 3 4 1 [ M+ H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 7 1 mi n 5 8 LC/ S ( ES m/ z ; 5 0 7 [M+H] + TABLE 5 1 Rf Dat a Ή - N R (CDC1 3) : - 0 . 10 ( s , 9H) , 0 . 85 ( d, J = 1. 2 Hz , 3H) , 0 . 90 ( t , J = 9. 0 Hz, 2H) , 1. 7 0- 1. 85 (m, 1H) , 1. 8 5- 2. 00 (m, 1H) , 2. 19 ( s , 3H) , 2. 35-2. 58 (m, 2H) , 2 . 7 5- 2. 9 0 (m, 2H) , 3. 00-3 . 12 (m, 1H) , 3. 50-3. 70 (m, 4H) , 5 . 3 3-5 . 4 1 (m, 59 1H) , 5 . 7 7 (dd, J = 9. 9, 15 . 0 Hz, 2H) , 6. 79 (d , J - 3 . 6 Hz , 1H) , 7. 2 0- 7. 40 (m, 6H) , 8 . 5 1 (br s , 1H) , 9. 45 ( s , 1H) . LC/MS : cond i t i on 1, r e ten t i on t ime = 3 . 7 4 mi n LC/MS (ES I +) m/z ; 5 17 [ M+H] + LC/MS : cond i t ion 1, r e ten t i on t ime 6 0 LC/MS (ES I +) m/z ; 58 1, 58 3 [M+H] + -NMR (CDC 13) -0. 05 ( s , 9H) , 0. 85 - 0 . 9 5 (m, 2H) , 0 . 9 9 ( d, J = 7. 5 Hz , 3H) , 1 . 8 5-1 . 9 5 (m, 1H) , 2 . 2 5-2. 35 (m, 1H) , 2. 6 5- 2. 75 (m, 1H) , 3. 35 - 3 . 4 5 (m, 1H) , 3 . 58 ( t , J = 8. 1 Hz, 2H) , 3. 6 5- 3. 85 (m, 2H) , 3 . 9 0-4. 0 0 (m, 1H) , 5. 40-5 . 50 (m, 1H) , 5 . 8 0 ( s , 2H) , 6. 36 6 1 I (d , J 8 . 1 Hz, 1H) , 6 . 75 ( d, = 3. 6 Hz , 1H) , 7. 4 6 (d , J = 3 . 6 Hz , 1H) , 7. 53 (d, J = 8. 1 Hz, 1H) , 7 . 7 0- 7. 85 ( , 2H) , 7. 9 0- 7. 95 (m, 1H) , 8. 10-8. 15 (m, 1H) , 9 . 4 0 ( s , 1H) . LC/MS : cond i t ion 3 , r e ten t i on t ime = 2 . 5 6 mi n LC / MS (ES ) m/z ; 578 [ M+H] + -NMR (CDC I 3) : - 0 . 0 7 ( s , 9H) , 0. 88 - 0 . 9 6 (m, 5H) , 1. 8 2- 1. 98 (m, 1H) , 2. 10- 2. 29 (m, 1H) , 2 . 5 5- 2. 70 (m, 1H) , 3. 08-3 . 2 1 (to, 1H) , 3. 42-3. 64 (m, 4H) , 3 . 7 0- 3. 82 (m, 1H) , 5 . 40-5 . 5 0 (m, 1H) , 5. 80 ( s , 2H) , 6 . 4 0 (d , = 7. 8 Hz , 1H) , 6 . 6 8 (d , J = 3. 9Hz, 1H) , 7. 46 ( d, 6 2 | J = 3. 9 Hz , 1H) , 7 . 6 0 (d, J = 7 . 8 Hz , 1H) , 7. 76 ( t , J = 7 . 8 Hz , 1H) , 7. 95 (d , J = 7. 8 Hz, 1H) , 8. 06 ( d, J 7 . 8 Hz , 1H) , 8 . 12 ( s , 1H) , 9. 4 1 ( s , 1H) . LC/MS : cond i t ion 3 , r e ten t i on t ime = 2 . 5 9 mi n LC/MS (ES I +) m/z ; 578 [ M+H] + -NMR ( CDC I 3 ) -0. 07 ( s , 9H) , 0. 82 - 0 . 9 9 (m, 2H) , 1. 0 3 ( d, J = 6. 9 Hz , 3H) , 1. 2 6 ( t , / = 7 . 2 Hz , 3H) , 1. 70-1 . 8 5 (m, 1H) , 2. 65- 2. 80 (m, 1H) , 3. 24-3 . 4 2 (m, 1H) , 3. 57 ( t , J - 8 . 4 Hz, 2H) , 3. 66- 3. 84 (m, 1H) , 3 . 90-4 . 0 2 (m, 1H) , 4. 10-4. 29 (m, 4H) , 5. 12-5. 22 (m, 1H) , 5. 76-5 . 8 4 (m, 2H) , 6. 40 (d, J = 7 . 8 Hz, 1H) , 6 3 6. 72 (d, J = 3. 9 Hz , 1H) , 7. 44 (d, J = 3. 9 Hz , 1H) , 7. 54 (d , J = 3. 9 Hz, 1H) , 9 . 4 3 ( s , 1H) . LC/MS : cond i t i on 1, r e tent i on t ime = 4 . 2 7 mi n LC/MS (ES I +) m/z ; 485 [ M+H] + LC/MS (ESI _) m/z ; 529 [M+HCOO] -NMR (CD CI 3 ) : - 0 . 0 8 ( s , 9H) , 0 . 92 ( t , J = 8. 4 Hz , 2H) , 1. 04 (d, J = 6 . 9 Hz, 3H) , 1. 80-1 . 9 5 (m, 1H) , 2. 0 8-2. 25 ( , 1H) , 2. 70-2. 88 (m, 1H) , 3. 42-3 . 6 0 (m, 1H) , 3. 56 ( t , J = 8 . 4 Hz, 2H) , 3. 65 -3. 82 (m, 2H) , 4 . 3 2-4. 46 (m, 1H) , 5 . 2 1-5 . 3 8 (m, 1H) , 5. 78 ( s , 2H) , 6. 38 ( d, / = 7. 8 Hz, 1H) , 6 . 7 2 ( d, J = 4. 2 Hz , 1H) , 6. 9 5- 7. 10 6 4 (m, 1H) , 7. 20 ( t , J = 8. 1 Hz, 1H) , 7 . 4 4 (d, J = 3 . 6 Hz , 1H) , 7. 45-7. 60 (m, 3H) , 7 . 9 9 ( d, J = 8 . 1 Hz , 1H) , 9. 38 ( s , 1H) . LC/MS : cond i t ion 3 , r e ten t i on t ime = 2 . 6 0 mi n LC/MS (ES T ) m/z ; 600 [ M+H] + LC/MS (ESI ) m/z ; 598 [M-H] - TABLEb 52 Rf Dat a -NMR (CDC1 3) : - 0 . 0 9 ( s , 9H) , 0. 80-0 . 9 2 (m, 2H) , 0 . 9 5 (d , J = 7 . 2 Hz, 3H) , 1. 70- 1. 8 4 (m, 1H) , 2 . 06-2 . 2 2 (m, 1H) , 2. 60- 2. 73 (m, 1H) , 3. 11- 3 . 2 8 (m, 1H) , 3. 37- 3 . 5 9 (m, 2H) , 3. 78-3 . 9 1 (m, 1H) , 4. 27-4 . 4 1 (m, 1H) , 4. 50-4 . 6 3 (m, 1H) , 5. 09-5 . 2 0 (m, 1H) , 5. 47 (d, J = 10 . 8 Hz , 1H) , 5. 6 3 (d, J = 0 . H , ) , 6 . 0 4 ( d, 7. 8 Hz, 6 5 1H) , 6. 67 (d, / = 3 . 9 Hz , 1H) , 7. 17- 7 . 4 0 (m, 3H) , 7. 4 1 (d , J = 3. 6 Hz, 1H) , 7. 78 ( d, = 8 . 7 Hz , 1H) , 8. 07 (s, 1H) , 8. 74 (s, 1H) , 9 . 6 6 (br s , 1H) . LC/MS : c ondi t i on 3, r e t en t i on t i me = 2 . 74 mi n LC/MS (ES I +) m/ z ; 600 [ +H] + LC/MS (ES m/ z ; 59 8 [M-H] LC/MS : c on di t i on 3, r e t ent i on t i me = 2 . 6 2 mi n 6 6 LC/MS (ES I +) m/ z ; 58 5 [ +H] + LC/MS : c on di t i on 3, r e t en t i on t i me = 2 . 6 8 mi n 6 7 LC/MS (ES I +) m/ z ; 58 5 [M+H] + LC/MS : c ondi t i on 3, r e t en t i on t i me = 2 . 5 1 mi n 6 8 LC /MS (ES m/ z ; 549 [M+H] + -NMR ( CDC I 3 ) : -0. 06 ( s , 9H) , 0. 82-0. 99 (m, 5H) , 1. 80-1 . 96 (m, 1H) , 2. 09-2 . 2 8 (m, 1H) , 2. 5 1- 2 . 6 8 (m, 1H) , 3. 07-3 . 2 6 (m, 1H) , 3. 42-3 . 6 3 (m, 4H) , 3. 70-3 . 8 1 (m, 1H) , 5 . 3 9- 5. 4 8 ( , 1H) , 5 . 8 0 (d d, 10 . 5 , 12. 9 Hz, 2H) , 6 . 3 9 ( d, J = 7 . 8 Hz, 1H) , 6 . 67 ( d, J = 3 . 9 6 9 Hz , 1H) , 7. 45 (d, 4 . 2 Hz, 1H) , 7. 63 (d, = 8 1 Hz, 1H) , 7. 77 ( t , J = 7. 8 Hz, 1H) , 7. 95 (d , J = 8. 1 Hz , 1H) , 8 . 03 (d , J = 7 . 8 Hz , 1H) , 8 . 0 9 (s, 1H) , 9 . 42 ( s , 1H) . LC/MS : c ondi t i on 3, r e t en t i on t i me = 2 . 8 2 mi n LC/MS (ES I +) m/ z ; 62 1 [M+H] + LC/MS : c ondi t i on 1, r e t e n t i on t i me = 2 . 6 9 mi n 7 0 LC/MS (ES I +) m/ z ; 58 5 [M+H] + LC/MS ( ES I ) m/ z ; 629 [M+HC00] LC / MS : c ondi t i on 3, r e t en t i on t i me = 2 . 7 2 mi n 7 1 LC/MS (ES I +) m/ z ; 54 7 [M+H] + LC/ MS : c ondi t i on 1, r e t en t i on t i me = 2 . 8 8 mi n 7 2 LC/ MS ( ES I +) m/ z ; 22 2 [M+H] + LC/ MS : c ondi t i on 1, r e t en t i on t i me = 3 . 8 6 mi n 7 3 LC/ MS ( ES m/ z ; 540 [M+H] + LC/ MS ( ES m/ z ; 538 [M~H] LC / MS : c ondi t i on 1, r e t ent i on t i me = 3 . 5 2 mi n 7 4 | LC/ MS ( ES I +) m/ z ; 23 5 [M+H] + LC/ MS ( ES m/z ; 23 3 [M-H] LC/ MS : c ondi t i on 1, ret en t i on t i me = 3 . 9 7 mi n 7 5 j LC/ MS ( ES ) m/ z ; 55 3 [M+H] + LC / MS ( ES ) m/ z ; 55 1 [M-H] LC/MS : c ondi t i on 1, ret en t i on t i me = 4 . 34 mi n 76 j LC/MS (ES I +) m/ z ; 50 9 [M+H] + LC/MS (ES D m/ z ; 55 3 [M+HC00] LC/MS : c ondi t i on 1, r e t en t i on t i me = 1. 2 6 mi n 7 7 LC/MS ( ES I +) m/ z ; 57 1 [M+H] + TABLE 53 Dat a LC/MS : c ondi t i on 1, r e t ent i on t i me = 4 . 2 1 mi n I LC/MS ( ES I +) m/ z ; 57 1 [M+H ] + LC/MS (ES m/ z 6 15 [M+HCOO] LC/MS : c ondi t i on 1, r e t e n t i on t i me = 4 . 8 5 mi n 79 LC/MS (ES I +) m/ z ; 57 1 [M+H] + LC/MS : c on di t i on 1, r e t e n t i on 3 . 8 9 mi n I LC/MS (ES T ) m/ ; 52 8 [M+H] + LC/MS (ES m/ z ; 57 2 [M+HC00] LC/MS : c ondi t i on 1, ret e n t i on 4 . 4 5 mi n 8 1 LC/MS ( ES I +) m/ z ; 52 8 [M+H] + LC /MS : c ondi t i on 1, r e t e n t i on t i me = 3 . 8 9 mi n 8 2 LC/MS (ES I +) m/ z ; 52 8 [M+H] + -NMR (CDC 13 ) -0. 15 (s, 9H) , 0 . 9 3 ( t , J = 8. 1 Hz, 2H) , 1. 0 1 (d , J = 7 . 2 Hz , 3H) , 1. 44 ( s , 9H) , 1. 7 0- 1. 80 (m, 1H) , 1. 9 5-2. 10 (m, 1H) , 2 . 6 0-2. 7 7 (m, 1H) , 3. 25-3 . 45 (m, 1H) , 3 . 5 7 ( t , J = 8 . 1 Hz , 2H) , 3. 64-3 . 9 0 (m, 2H) , 4. 00-4 . 2 0 (m, 1H) , 5. 10-5 . 2 2 (m, 1H) , 5. 80 ( dd , J = 10. 8, 13. 2 Hz , 2H) , 6 8 3 . 4 8 (d , J = 8 . 1 Hz , 1H) , 6. 72 (d , J = 3. 6 Hz, 1H) , 7. 44 ( d , = 4. 2 Hz , 1H) , 7. 57 (d, J = 8 . 4 Hz , 1H) , 9 . 4 3 (s, 1H) . LC/MS : c ondi t i on 1, ret e n t i on t i me = 4 . 5 5 mi n LC/MS ( ES I +) m/ z ; 5 13 [M+H] + LC/MS (ES m/z ; 55 7 [M+HC00] 'H-NMR (CDC I 3 ) 8 : -0. 04 ( s , 9H) , 0. 87- 1. 08 (m, 5H) , 1. 7 1 - 2 . 10 (m, 2H) , 2. 40-3 . 3 0 (m, 8H) , 3. 58 - 3 . 7 2 (m, 2H) , 5. 40-5 . 5 4 (m, l H) , 5. 80-5 . 9 4 ( , 2H) , 6 . 3 7 ( d, J = 7. 8 Hz, 1H) , 6. 8 7 ( d, = 3. 9 Hz, 1H) , 6. 99-7. 15 (m, 2H) , 7. 15 - 7 . 3 0 (m, 2H) , 7. 30-7 . 4 5 ( , 1H) , 7. 49 (d , / = 3. 6 Hz , 1H) , 8. 44 (br s , 1H) , 9. 50 ( s , 1H) . LC/MS : c on d i t i on 3, r e t ent i on t i me = 2 . 14 mi n LC/MS ( ES I +) m/ z ; 53 5 [M+H] + LC/MS : c ondi t i on 3, r e t enti on t i me = 1. 8 9 mi n 8 5 LC/MS (ES I +) m/z ; 48 1 [M+H] + LC/MS : c on d i t i on 3, r e t e n t i on 3 . 17 mi n 86 a LC/MS (ES I +) m/ z ; 579 [M+H] + LC/MS : c ondi t i on 3, r e t ent i on 3 . 0 9 mi n 86b LC/MS (ES I +) m/ z ; 57 9 [M+H] + LC/MS : c on d i t i on 3, r e t e n t i on t i me = 2 . 6 6 mi n 8 7 I LC/MS (ES I +) m/ z ; 32 7, 3 29 [M+H] + LC/MS (ES m/ z ; 32 5, 3 27 [M-H] -NMR (CDC I 3) -0. 06 (s, 9H) , 0 . 9 1 ( t , J = 8. 4 Hz, 2H) , 3. 53 ( t , J = 8. 4 Hz, 2H) , 5 . 68 ( s , 2H) , 6. 7 1 (d, J = 3. 6 Hz, 1H) , 7. 4 5 (d , J = 3. 9 Hz , 1H) , 8 . 8 1 ( s , 1H) . LC/MS : c ondi t i on 3, r e t e n t i on t i me = 2 . 4 0 mi n LC/MS (ES I +) m/ z ; 32 6, 3 28 [M+H] + TABLEb 54 Rf Data -N R (CDC1 3) -0.06 (s, 9H), 0.90 (t, / = 7.5 Hz, 2H), 1 . 60-1. 84 (m, 2H) , 2.07-2. 19 (m, 2H), 2.21-2.38 (m, 2H), 2 . 77-2. 9 1 (m, 2H) , 3 . 46 (m, 4H), 3.92-4. 10 (m, IH), 5.57 (s, 4H), 89 6 . 58 (d, = 3.6 Hz, IH), 7 . 08 (d, / = 3.9 Hz, IH), 7 . 20-7. 38 (m, 5H), 8 . 30 (s, IH), 9.39 (d, J = 7.5 Hz, IH). LC/MS: condition 3 , retention time = 1 . 89 min LC/MS(ESI +) m/z; 480 [M+H] + -NMR (CDCI 3) -0.05 (s, 9H) , 0.93 (t, = 8.7 Hz, 2H), 1 . 80-1. 96 (m, 2H), 2 . 10-2. 28 ( , IH) , 2.94-3. 22 (m, 4H) , 3 . 56 (t, J = 8.7 Hz, 2H), 3.59 (s, 2H) , 4.68-4.85 ( , IH), 5.73 (s, 2H), 90 6 . 74 (d, J = 3 . 3 Hz, IH), 7.22-7.48 (m, 6H), 8.03 (s, IH), 9.04 (s, IH). LC /M S . condition 3 , retention time = 2 . 18 min LC/MS(ESI +) m/z; 506 [M+H] + LC/MS: condition 3 , retention time = 1 . 90 min 9 1 LC/MS(ESI +) m/z; 416 [M+H] + -NMR (CDCI 3) : -0.04 (s, 9H) , 0.94 (t, = 8 . 1 Hz, 2H), 1.84-1.98 (m, 2H), 2 . 18-2. 32 ( , 2H) , 3.00-3. 18 (m, 4H) , 3 . 57 (t, J = 8 . 1 Hz, 2H) , 3.65 (s, 2H) , 4.70-4.84 (m, IH), 5.75 (s, 2H), 6 . 73 (d, = 3.6 Hz, IH), 7.45 (d, J = 3.9 Hz, IH), 7.53 (d, J 92 = 8.4 Hz, 2H), 7 . 64 (d, J = 8 . 1 Hz, 2H) , 8 . 09 (s, IH), 9.06 (s, IH). LC/MS: condition 3 , retention time = 2 . 23 min LC/MS(ESI +) m/z; 531 [M+H] + 'H-NMR (CDC1 3) : -0.05 (s, 9H) , 0.93 (t, = 7.5 Hz, 2H), 1 . 81-1.96 (m, 2H) , 2 . 18-2. 30 (m, 2H) , 2.93-3.26 ( , 4H) , 3 . 51-3. 62 (m, 2H) , 3 . 7 1 (s, 2H), 4.66-4.83 ( , IH), 5.74 (s, 2H), 93 6 . 66-6. 80 (m, 2H) , 7.44 (d, = 4.2 Hz, IH) , 8 . 03 (br s , IH) , 9 . 05 (s, IH). LC/MS: condition 3 , retention time = 2 . 2 1 min LC/MS(ESD m/z; 546, 548 [M+H] + 'H-NMR (CDCI 3) : -0.05 (s, 9H) , 0.93 (t, J = 8 . 1 Hz, 2H), 1 . 80-1. 96 (m, 2H) , 2 . 13-2. 30 ( , 2H) , 2 . 95-3. 16 ( , 4H) , 3 . 56 (t, J = 8 . 1 Hz, 2H) , 3.64 (s, 2H) , 4.70-4.82 (m, IH), 5.74 (s, 2H), 94 6 . 73 (d, J = 3 . 9 Hz, IH), 7.40-7.68 (m, 5H), 8 . 14 (s, IH), 9.05 (s, IH). LC/MS: condition 3 , retention time = 2.43 min LC/MS(ESI +) m/z; 574 [M+H] + LC/MS: condition 3 , retention time = 2.87 min 95 LC/MS(ESI +) m/z; 415 [M+H] + 'H-NMR (CDCI 3) : -0. 06 (s, 9H) , 0.8 8 (t, = 8 . 1 Hz, 2H) , 2 . 76 96 (s, 3H), 3 . 48-3. 62 (m, 2H) , 5.67 (s, 2H) , 6.74 (d, J = 3 . 3 Hz, IH), 7 . 43 (d, J = 3 . 9 Hz, IH), 8.72 (s, IH). LC/MS: condition 1 , retention time = 3 . 32 min 97 LC/MS(ESI +) m/z; 479 [M+H] + LC/MS: condition 1 , retention time = 3 . 18 min 98 LC/MS(ESI +) m/z; 489 [M+H] + LC/MS: condition 1 , retention time = 2 . 88 min 99 LC/MS(ESI +) m/z; 399 [M+H] + TABLEb 55 Rf Da t a LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 5 0 mi n 10 0 LC/ MS ( ES m/ z 5 2 9 , 5 3 1 [ M+ H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 5 0 mi n 10 1 LC/ MS ( ES I + ) m/ z ; 5 5 7 [M+H] + LC / MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 2 6 mi n 10 2 LC/ MS ( ES I + ) m/ z 5 1 4 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 2 . 9 8 mi n 10 3 LC / MS ( ES I + ) m/ z ; 5 3 2 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 3 5 mi n 10 4 LC/ MS ( ES I + ) m/ z ; 3 3 5 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 3 0 mi n 10 5 LC/ MS ( ES m/ z ; 4 6 5 [M+H] + - NMR ( C DC 1 3 ) : - 0 . 0 7 ( s , 9H) , 0 . 8 5 - 0 . 9 8 (m, 2 H) , 1 . 5 2 - 1 . 7 9 (m, 2 H) , 2 . 0 4 - 2 . 3 8 (m, 4H) , 2 . 7 9 - 2 . 9 5 (m, 2H) , 3 . 4 4 - 3 . 6 2 (m, 4 H) , 1 0 6 3 . 8 9 - 4 . 0 6 ( m, I H) , 4 . 7 0 ( s , 2 H) . 5 . 5 8 ( s , 2H) , 6 . 4 9 ( d , J 3 . 6 Hz , I H) , 7 . 1 1 ( d , J = 3 . 9 Hz , I H) , 7 . 2 3 - 7 . 4 0 (m, 5H) , 7 . 8 2 ( s , I H) . - NMR ( CD3O D) : - 0 . 0 3 ( s , 9 H) , 0 . 9 2 ( t , J = 8 . 0 Hz , 2 H) , 1 . 7 0 - 1 . 9 1 (m, 2 H) , 2 . 1 2 - 2 . 5 1 ( m, 4 H) , 2 . 9 0 - 3 . 10 ( m, 2 H) , 3 . 5 4 - 3 . 7 8 ( m, 4 H) , 3 . 9 6 ( s , 2 H) , 4 . 0 2 - 4 . 19 ( , I H) , 5 . 6 1 ( s , 2 H) , 1 0 7 6 . 6 5 ( d , . Hz , I H) , 7 . 2 8 ( d , J = 3 . 6 Hz , I H) , 7 . 1- 7 . 5 3 ( m, 5H) , 7 . 8 4 ( s , I H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 3 7 mi n LC/ MS ( ES I + ) m/ z ; 4 6 6 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 2 4 mi n 1 0 8 LC/ MS ( ES I + ) m/ z ; 4 9 2 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 2 . 9 6 mi n 10 9 LC / MS ( ES I + ) m/ z ; 4 0 2 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 4 . 4 5 mi n 1 1 0 LC/ MS ( ES I + ) m/ z ; 5 5 6 [M+H] + - NMR ( C DC I 3 ) : - 0 . 0 5 ( s , 9 H) , 0 . 8 1 - 1 . 0 6 ( , 2 H) , 1 . 5 5 - 2 . 0 5 (m, 3 H) , 2 . 0 5 - 2 . 2 9 (m, H) , 2 . 9 3 - 3 . 2 0 (m, 4H) , 3 . 4 6 - 3 . 7 0 (m, 4 H) , 4 . 1 1 - 4 . 2 8 ( m, I H) , 4 . 2 9 - 4 . 4 9 ( m, 2 H) , 5 . 1 3 ( s , I H) , 5 . 6 5 ( s , 2H) , 1 1 6 . 4 7 ( d , J = 3 . 6 Hz , I H) , 7 . 2 1 - 7 . 4 1 ( , 2 H) , 7 . 7 8 ( d , J = 7 . 7 Hz , I H) , 7 . 9 8 ( s , I H) , 8 . 4 5 - 8 . 6 7 ( m, 2 H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 2 . 9 2 mi n LC / MS ( ES I + ) m/ z ; 4 9 3 [M+H] + LC / MS : c o n d i t i o n 1 , r e t e n t i o n t i me - 3 . 2 6 mi n 1 1 2 LC/ MS ( ES I + ) m/ z ; 5 1 7 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 4 8 mi n 1 1 3 LC / MS ( ES I + ) m/ z ; 5 6 0 [M+H] + ' H- NMR ( CDC I 3 ) : - 0 . 0 3 ( s , 9H) , 0 . 8 7 - 1 . 0 5 (m, 2 H) , 1 . 5 0 - 1 . 8 9 (m, 4 H) , 2 . 0 2 - 2 . 2 8 (m, 2 H) , 2 . 9 2 - 3 . 2 5 (m, 2H) , 3 . 6 0 ( t , J = 8 . 3 Hz , 2H) , 4 . 3 0 - 3 . 7 2 ( m, 3H) , 5 . 7 0 ( s , 2 H) , 6 . 4 4 ( d , J = 3 . 6 Hz , I H) , 1 1 4 7 . 3 7 ( d , J = 3 . 9 Hz , I H) , 7 . 7 9 ( s , I H) , 8 . 0 7 ( s , I H) , 8 . 6 9 ( s , I H) . LC / MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 8 7 mi n LC / MS ( ES I + ) m/ z ; 5 2 9 [M+H] + TABLE" 56 Rf Da t a - NMR ( CDC I 3 ) - 0 . 0 5 ( s , 9H) , 0 . 8 0 - 1. 0 3 ( m, 2H) , 1. 5 3 - 1 . 7 7 (m, 4 H) , 1 . 9 3 - 2 . 1 3 ( m, 2H) , 3 . 10 - 3 . 4 0 (m, 2 H) , 3 . 5 5 ( t , J = 8 . 3 Hz , 2 H) , 3 . 9 0 - 4 . 0 7 (m, I H) , 4 . 3 1 - 4 . 5 3 (m, 2 H) , 4 . 8 2 - 4 . 9 8 (m, I H) , 1 1 5 5 . 2 1 ( s , H) , 5 . 6 7 ( s , 2H) , 6 . 3 5 - 6 . 4 8 ( m, I H) , 7 . 3 5 ( d , J = 3 . 6 Hz , I H) , 8 . 0 1 ( s , I H) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 4 . 1 7 mi n LC/ MS ( ES I +) tn/ z ; 5 1 2 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 2 . 9 9 mi n 1 1 6 LC/ MS ( ES D m/ z ; 4 9 9 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 0 . 5 2 mi n 1 1 7 LC / MS ( ES D m/ z ; 34 9 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 5 7 mi n 1 1 8 LC/ MS ( ES I +) m/ z ; 4 7 9 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 2 . 9 1 mi n 1 1 9 LC/ MS ( ES I + ) m/ z ; 4 8 1 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 4 2 mi n 12 0 LC/ MS ( ES I + ) m/ z ; 4 8 0 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 3 6 mi n 12 1 LC/ MS ( ES D m/ z ; 5 0 6 [M+H] + ' H-NMR ( C DC I 3) 0 . 9 2 - 1 . 19 (m, 4 H) , 1 . 4 1- 1. 5 1 ( m, I H) , 1. 7 4 - 1. 9 6 (m, 4H) , 2 . 5 5 - 2 . 6 8 (m, I H) , 3 . 4 5 ( d , J = 6 . 3 Hz , 2H) . 12 2 LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 0 . 2 9 mi n LC/ MS ( ES I +) m/ z ; 13 0 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 3 3 mi n 12 3 LC/ MS ( ES I + ) m/ z ; 4 1 8 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 1 6 mi n 12 4 LC/ MS ( ES I + ) m/ z ; 4 2 8 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 6 2 mi n 12 5 LC/ MS ( ES I + ) m/ z ; 2 3 0 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 0 . 3 9 mi n 12 6 LC/ MS ( ES I +) m/ z ; 13 0 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 4 . 4 3 mi n 12 7 LC/ MS ( ES I +) m/ z ; 4 1 8 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 4 . 0 8 mi n 12 8 LC/ MS ( ES I + ) m/ z ; 4 2 8 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 5 8 mi n 12 9 LC/ MS ( ES I +) m/ z ; 54 7 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 5 2 mi n 13 0 LC/ MS ( ES I + ) m/ z ; 5 2 4 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 3 8 mi n 13 1 LC/ MS ( ES I + ) m/ z ; 5 5 1 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 3 4 mi n 13 2 LC/ MS ( ES m/ z ; 5 2 5 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 5 6 mi n 13 3 LC/ MS ( ES ) m/ z ; 5 5 7 , 5 5 8 , 5 5 9 [M+ H] + TABLEb 57 Rf Dat a LC/MS : c on d i t i on 1, r e t en t i on t i me - 3 . 4 6 mi n 134 LC/MS (ES I +) m/ z ; 558 [M+H ] + LC/MS : c ondi t i on 1, r e t en t i on t i me = 3 . 4 4 mi n 13 5 LC/MS (ES I +) m/ z ; 53 0, 5 32 [ M+H] + LC/MS : c ondi t i on 1, ret en t i on t i me = 3 . 5 6 mi n 136 LC/MS (ES I +) m/ z ; 57 5 [M+H] + LC/MS : c on d i t i on 1, r e t en t i on t i me = 3 . 2 8 mi n 13 7 LC/MS (ES I +) m/z ; 540 [M+H] + LC/MS : c ondi t i on 1, r e t en t i on t i me = 3 . 3 0 mi n 13 8 LC/MS (ES m/z ; 55 7, 5 59 [ M+H] + LC/MS : c on d i t i on 1, r e t en t i on t i me = 3 . 5 6 mi n 13 9 LC/MS (ES I +) m/z ; 57 3, 5 75 [M+H] + LC/MS : c ondi t i on 1, r e t en t i on t i me = 3 . 5 0 mi n 140 LC/MS (ES I +) m/z ; 57 3, 5 75 [M+H] + LC/MS : c on d i t i on 1, r e t e n t i on t i me = 3 . 4 4 mi n 14 1 LC/MS ( ES I +) m/z ; 574, 5 76 [ M+H] + LC/MS : c ondi t i on 1, r e t en t i on t i me = 3 . 4 6 mi n 14 2 LC/MS (ES D m/z ; 569 [M+H] + LC/MS : c ondi t i on 1, r e t e n t i on t i me - 3 . 19 mi n 14 3 LC/MS ( ES I +) m/ z ; 52 8 [M+H] + LC/MS : c on d i t i on 1, r e t e n t i on t i me = 4 . 3 3 mi n 144 LC/MS ( ES I +) m/ z ; 543, 545 [M+H] + TABLEb 58 Rf Da t a LC/MS : cond i t 145 ion 3, r e t ent ion t i me = 2. 2 1 mi n LC/MS (ESI +) m/z ; 55 9 [M+H] + LC/MS : cond i t ion 3, ret ent ion t i me = 2. 32 mi n 146 LC/MS (ESI +) m/z ; 590, 5 92 [M+H] + LC/MS : cond i t ion 3, r e t ent ion t i me = 2. 22 mi n 147 LC/MS (ESI +) m/z ; 544 [M+H] + LC/MS : cond i t ion 3, r e t ent ion t i me - 2. 05 mi n 148 LC/MS (ESI +) m/z ; 47 0 [M+H] + LC/MS : cond i t ion 3, r e t ent ion t i me - 2. 19 mi n 149 LC/MS (ESI +) m/z ; 48 6 [M+H] + LC/MS : cond i t ion 3, r e t ent ion t i me = 2. 02 mi n 150 LC/MS (ESI +) m/z ; 52 8 [M+H] + -NMR ( CDC 1 3 ) - 0 . 0 4 ( s , 9H) , 0. 9 1- 0 . 9 7 (m, 2H) , 1. 9 8 (d, J = 12. 3 Hz, 2H) , 2. 5 9 (t, J = 1 1. 7 Hz , 2H) , 3 . 00-3. 15 (m, 4H) , 3. 54-3. 59 (m, 2H) , 3. 66 ( s , 2H) , 4. 73 -4. 8 1 (m, 1H) , 5. 75 ( s , 2H) , 15 1 6. 84 (d, J = 3. 9 Hz, 1H) , 7 . 4 8 (d , J = 3 . 6 Hz, 1H) , 8. 32 (br s , 1H) , 9. 06 ( s , 1H) . LC/MS : cond i t ion 3, r e t ent ion t i me = 2. 35 mi n LC/MS (ESI +) m/z ; 45 5 [M+H] + Ή -NMR ( CDC I 3 ) -0. 05 ( s , 9H) , 0. 94 ( t , J = 8 . 3 Hz , 2H) , 1. 87 (d , J = 10 . 8 Hz, 2H) , 2. 67 ( t , J = 12 Hz , 2H) , 2 . 9 8- 3. 2 1 (m, 6H) , 3. 56 ( t , / = 8 . 3 Hz, 2H) , 4. 7 1- 4 . 7 9 (m, 1H) , 5 . 74 ( s , 2H) , 6. 7 1 152 (d , J = 3. 9 Hz, 1H) , 7 . 4 5 ( d, = 3 . 9 Hz , 1H) , 8 . 08 (br s , 1H) , 9. 05 ( s , 1H) . LC/MS : cond i t ion 3, r e t ent ion t i me = 2. 7 1 mi n LC/MS (ESI +) m/z ; 498 [M+H] + LC/MS : cond i t ion 3, r e t ent i o n t i me = 2. 00 mi n 153 LC/MS (ESI +) m/z ; 49 7 [M+H] + LC/MS : cond i t ion 3, r e t ent ion t i me = 2. 33 mi n 154 LC/MS (ESI +) m/z ; 554 [M+H] + LC/MS : cond i t ion 3, r e t ent i o n t i me - 1. 99 mi n 155 LC/MS (ESI +) m/z ; 48 3 [M+H] + LC/MS : c o nd i t ion 3, ret ent ion t i me = 2. 05 mi n 156 LC/MS (ES I +) m/z ; 500 [M+H] + -NMR ( CDC I 3 ) -0. 04 ( s , 9H) , 0. 93 ( t , J = 8 . 4 Hz, 2H) , 1. 90 (d, J = 1 . 3 Hz, 2H) , 2. 32 ( t , J = 11. 1 Hz , 2H) , 2 . 5 7 ( t , J = 7. 1 Hz, 2H) , 2 . 8 1 ( t , J = 6. 9 Hz , 2H) , 3. 0 1-3. 17 (m, 4H) , 3. 56 ( t , J = 8 . 3 Hz , 2H) , 4. 7 1- 4 . 79 (m, 1H) , 5 . 7 4 (s, 2H) , 6 . 7 2 ( d, 157 J = 3 . 9 Hz, 1H) , 7 . 45 ( d, J = 3. 9 Hz, 1H) , 8. 12 (br s , 1H) , 9 . 05 ( s , 1H) . LC/MS : cond i t ion 3, r e t ent ion t i me = 1. 97 mi n LC/MS (ESI +) m/z ; 46 9 [M+H] + LC/MS : cond i t ion 1, r e t ent ion t i me = 0 . 33 mi n 158 LC/MS (ESI +) m/z ; 16 8 [M+H] + TABLE 59 Rf Dat a Ή -NMR (CDC 13) : 1. 52 - 1. 80 (m, 9H) , 2 . 0 5- 2. 25 (m, 3H) , 3. 60-3. 75 (m, 1H) , 4 . 90- 5. 15 (m, 1H ) , 5. 10 ( s , 2H) , 7 . 25 - 7 . 4 5 159a (m, 5H) . LC/MS : cond i t ion 1, r e tent ion t ime = 3 . 6 3 i n LC/MS (ESI +) m/z 302 [ M+H] + Ή -NMR (CDC I 3 ) : 1. 4 1- 1. 53 (m, 3H) , 1. 5 3- 1. 9 1 (m, 7H) , 2. 0 1-2. 25 Cm , 3H) , 3. 73-3. 86 (m, 1H) , 4. 98-5. 02 (m, 1H) , 5. 10 159b ( s , 2H) , 7. 28-7. 43 (m, 5H) . LC/MS : cond i t ion 1, r e tent i o n t ime = 3 . 6 3 mi n LC/MS (ESI +) m/z ; 302 [M+H] + 'H-NMR (DMS0 - ) 1. 20 (d, J = 2. 3 Hz , 2H) , 1. 57 (to, 5H) , 1. 7 2 ( s , 1H) , 1. 92 - 1. 96 (m, 5H) , 2. 8 3 ( s , 1H) , 4. 26 (br s , 1H) . 160 LC/MS : cond i t ion 1, r e tent i o n t ime = 0 . 3 3 mi n LC/MS (ESI +) m/z ; 168 [M+H] + 'H-NMR (DMS0- f ) : 1. 27 ( d, / = 12. 7 Hz, 2H) , 1. 4 1- 1. 6 3 (m, 6H) , 1. 76-2. 02 (m, 5H) , 2 . 7 5-2. 80 (br s , 1H) . 16 1 LC/MS : cond i t ion 1, r e tent i o t ime = 0 . 3 3 mi n LC/MS (ESI +) m/z ; 168 [ M+H] + 162 Ή -NMR (CDC I 3 ) : 1. 48 ( s , 9H) , 4 . 70 ( s , 4H) . -NMR ( CDCI 3) : 1. 4 6 ( s , 9H) , 4. 5 8-4. 65 (m, 2H) , 4 . 68 - 4 . 7 4 (m, 2H) , 5. 36-5 . 4 1 (m, 1H) . 163 LC/MS : cond i t ion 1, r e tent i o n t ime = 3 . 4 4 mi n LC/MS (ESI +) m/z ; 195 [M+H] + Ή -NMR (CDCI 3 ) 8 : 1. 44 ( s , 9H) , 2 . 64 ( d, J = 7. 2 Hz , 2H) , 2. 79-2. 94 (m, 1H) , 3. 69 ( dd, J = 8. 8, 5. 5 Hz , 2H) , 4. 13 (d d, J 164 = 8. 8, 8. 3 Hz , 2H) . LC/MS : cond i t ion 1, r e t e n t i o n t ime = 3 . 2 0 mi n LC/MS (ESI +) m/z ; 197 [ M+H] + LC/MS : cond i t ion 1, r e t e nt ion t ime = 0 . 3 3 mi n 165 LC/MS (ESI +) m/z ; 97 [M+H ] + -NMR (CDC I 3 ) : -0. 0 5 ( s , 9H) , 0 . 9 5 ( t , J = 8. 4 Hz , 2H) , 1 . 2 3 (m, 2H) , 1. 4 7 (m, 3H) , 2. 0 0 ( d, J = 8. 7 Hz, 2H) , 2. 33 (d, J = 8. 7 Hz, 2H) , 3. 58 (m, 4H) , 5. 6 3 (br s , 4H) , 6 . 6 2 ( d, J = 4 . 0 Hz , 166 1H) , 7. 13 ( d, = 4 . 0 Hz , 1H) , 8 . 33 ( s , 1H) , 9 . 2 9 ( d, = 7 . 8 Hz , 1H) . LC/MS : cond i t ion 3 , r e tent ion t ime = 1. 9 9 mi n LC/MS (ESI +) m/z ; 419 [M+H] + Ή -NMR (CDC I 3 ) : -0. 04 ( s , 9H) , 0 . 9 7 ( t , J = 8. 4 Hz , 2H) , 1. 2 8 (m, 2H) , 1. 43 (m, 1H) , 1. 7 4 ( , 1H) , 2. 09 (m, 4H) , 2. 80 (m, 2H) , 3. 60 ( t , / = 8 . 4 Hz , 2H) , 3 . 6 0 (m, 2H) , 4 . 7 5 (m, 1H) , 5 . 78 ( s , 167 2H) , 6 . 7 4 (d, = 4 . 0 Hz , 1H) , 7 . 47 (d , = 4. 0 Hz, 1H) , 8. 4 1 ( s , 1H) , 9. 10 ( s , 1H) . LC/MS : cond i t ion 3 , r e t e nt ion t ime = 2 . 3 3 mi n LC/MS (ESI +) m/z ; 445 [ M+H] + TABLEb 60 Rf Da t a - NMR (CDC l ) : - 0 . 0 4 ( s , 9 H) , 0 . 9 5 ( t , J = 8 . 1 Hz , 2 H) , 1 . 5 3 ( , 2H) , 2 . 0 6 (m, 4H) , 2 . 4 2 (m, 1H) , 2 . 8 5 (m, 2H) , 3 . 6 0 ( t , J = 8 . 1 Hz , 2 H) , 4 . 7 5 (m, 1H) , 5 . 7 8 ( b r s , 2 H) , 6 . 7 0 ( d , 4 . 0 Hz , 1 6 8 1H) , 7 . 7 9 ( d , / = 4 . 0 Hz , 1H) , 8 . 6 7 (br s , 1H) , 9 . 10 ( s , 1H) , 9 . 7 9 ( s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 5 2 mi n LC/ MS ( ES I +) m/ z ; 4 4 3 [M+H] + H-NMR ( C DC I 3 ) - 0 . 0 6 ( s , 9 H) , 0 . 9 6 ( t , / = 8 . 1 Hz , 2 H) , 1 . 1 9 (m, 2 H) , 1 . 3 0 ( b r s , 1H) , 1 . 6 7 ( b r s , 1H) , 2 . 0 7 ( m, 4H) , 2 . 0 8 (m, 2H) , 2 . 8 0 ( m, 2 H) , 3 . 2 5 (m, 2H) , 3 . 6 0 ( t , J = 8 . 1 Hz , 2H) , 4 . 7 4 1 6 9 (m, 1H) , 5 . 7 8 ( b r s , 2H) , 6 . 7 3 ( d , = 4 . 0 Hz , 1H) , 7 . 4 7 ( d , J = 4 . 0 Hz , 1H) , 9 . 10 ( s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 2 7 mi n LC / MS ( ES I + ) m/ z ; 5 2 6 [ +H] + - NMR ( CDC I 3 ) : - 0 . 0 6 ( s , 9 H) , 0 . 9 2 ( t , = 8 . 1 Hz , 2 H) , 1 . 8 8 (m, 2H) , 2 . 0 3 (m, 4H) , 2 . 3 7 ( m, 1H) , 2 . 8 5 (m, 2H) , 3 . 5 3 ( t , J = 8 . 1 Hz , 2H) , 4 . 7 0 (m, 1H) , 5 . 3 4 (m, 1H) , 5 . 7 2 ( b r s , 2H) , 6 . 3 0 - 6 . 7 4 1 7 0 ( , 1H) , 6 . 7 0 ( d , / = 4 . 0 Hz , 1H) , 7 . 4 4 ( d , J = 4 . 0 Hz , 1H) , 9 . 0 4 ( s , 1H) , 9 . 3 1 ( s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 6 5 mi n LC/ MS ( ES I +) m/ z ; 4 4 6 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 2 3 mi n 1 7 1 LC/ MS ( ES I + ) m/ z ; 4 5 7 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 2 3 mi n 1 7 2 LC/ MS ( ES I + ) m/ z ; 4 5 7 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 4 6 mi n 1 7 3 LC/ MS ( ES I +) m/ z ; 4 8 3 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 2 8 mi n 1 7 4 LC / MS ( ES I +) m/ z ; 4 8 3 [M+H] + ' H- NMR ( CDC I 3 ) : - 0 . 0 4 ( s , 9H) , 0 . 9 1 ( t , J 7 . 3 Hz , 2 H) , 1 . 5 3 - 1 . 8 8 ( , 8 H) , 2 . 0 2 - 2 . 12 (m, 2H) , 2 . 1 8 - 2 . 2 7 (m, 1H) , 2 . 3 7 - 2 . 4 9 (m, 2 H) , 2 . 6 3 ( s , 3H) , 3 . 5 4 ( d , J = 7 . 3 Hz , 2 H) , 4 . 0 5 - 4 . 2 0 (m, 1H) , 5 . 6 1 ( s , 2 H) , 6 . 5 3 ( d , / = 3 . 6 Hz , 1H) , 7 . 0 7 1 7 5 ( d , J = 3 . 6 Hz , 1H) , 8 . 6 7 ( s , 1H) , 10 . 7 8 ( d , J = 7 . 6 Hz , 1H) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 4 . 2 3 mi n LC/ MS ( ES I + ) m/ z ; 4 5 6 [M+H] + LC/ MS ( ES ) m/ z ; 5 0 0 [M+HC 0 0 ] Ή - NMR ( CDC I 3) : - 0 . 0 5 ( s , 9H) , 0 . 9 1 ( t , / = 8 . 3 Hz , 2 H) , 1 . 4 0 - 1 . 6 2 (m, 4 H) , 1 . 7 3 - 2 . 13 ( m, 6H) , 2 . 1 8 - 2 . 2 8 (m, 1H) , 2 . 3 0 - 2 . 4 2 (m, 2 H) , 2 . 6 5 ( s , 3H) , 3 . 5 4 ( d , J = 8 . 3 Hz , 2 H) , 4 . 19 - 4 . 3 0 ( , 1H) , 5 . 5 8 ( s , 2 H) , 6 . 5 1 ( d , J = 4 . 0 Hz , 1H) , 7 . 0 7 1 7 6 ( d , J = 4 . 0 Hz , 1H) , 8 . 6 6 ( s , 1H) , 10 . 7 5 ( d , / = 8 . 0 Hz , 1H) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me - 4 . 0 7 mi n LC/ MS ( ES I +) m/ z ; 4 5 6 [M+H] + LC/ MS ( ES ) m/ z ; 5 0 0 [M+HC 0 0 ] TABLE 6 1 TABLEb 62 E x Da t a - NMR ( CDC 1 3 ) : 1 . 1 0 - 2 . 0 0 ( m, 1 0H) , 1 . 5 8 ( d , J = 6 . 3 Hz , 3H) , 3 . 9 0 - 4 . 1 0 ( m, 1H) , 4 . 6 7 ( d , J = 1 0 . 2 Hz , 1H) , 4 . 8 3 ( d , J = 1 0 . 2 Hz , 1H) , 5 . 1 3 ( q , / = 6 . 6 Hz , 1H) , 6 . 4 3 ( . d , = 3 . 6 Hz , 1H) , 7 . 1 7 1 ( d , J = 3 . 3 Hz , 1H) , 7 . 8 9 ( s , 1 H) , 9 . 2 9 ( b r s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 2 . 8 2 mi n LC/ MS ( ES I + ) m/ z ; 2 7 2 [M+H ] + - NMR ( CDC I 3 ) 1 . 1 0 - 1 . 9 0 (m, 8 H) , 1 . 9 5 - 2 . 1 0 (m, 2H) , 3 . 9 5 - 4 . 1 0 (m, 1H) , 4 . 7 8 ( s , 2H) , 4 . 9 6 ( s , 2 H) , 6 . 4 3 ( d , J = 3 . 6 Hz , 1H) , 7 . 1 7 2 ( d , J = 3 . 3 Hz , 1H) , 7 . 8 1 ( s , 1 H) , 9 . 4 5 ( b r s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 2 . 3 7 mi n LC/ MS ( ES I + ) m/ z ; 2 5 8 [M+H] + Ή - NMR ( CDC I 3 ) 1 . 5 0 - 2 . 0 0 ( , 6 H) , 2 . 0 0 - 2 . 1 5 (m, 2H) , 2 . 2 0 - 2 . 3 5 (m, 2 H) , 4 . 9 0 - 5 . 0 5 ( m, 1H) , 6 . 4 6 ( d , = 7 . 8 Hz , 1H) , 6 . 8 0 - 6 . 8 5 (m, 1H) , 7 . 4 0 - 7 . 5 0 ( , H) , 7 . 8 0 ( d, J = 8 . 1 Hz , 1H) , 9 . 4 6 ( s , 1H) , 3 1 1 . 2 5 ( b r s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 3 2 mi n LC/ MS ( ES I + ) m/ z ; 2 6 8 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 7 9 mi n 4 LC/ MS ( ES I + ) m/ z ; 3 7 3 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 5 0 mi n 5 LC/ MS ( ES I + ) m/ z ; 2 8 3 [M+H] + Ή - NMR ( CDC I 3 ) 0 . 8 7 ( d , J = 7 . 2 Hz , 3 H) , 1 . 6 0 - 2 . 0 0 ( m, 2H) , 2 . 4 0 - 2 . 6 0 ( m, 2H) , 2 . 7 5 - 3 . 0 0 (m, 2 H) , 3 . 0 0 - 3 . 2 0 (m, 1H) , 3 . 7 0 ( s , 2 H) , 5 . 4 0 - 5 . 5 0 (m, 1 H) , 6 . 4 2 ( d , J = 7 . 8 Hz , 1H) , 6 . 8 0 - 6 . 8 5 ( m, 6 a 1H) , 7 . 0 0 - 7 . 2 0 ( m, 3 H) , 7 . 4 5- 7 . 5 0 (m, 1H) , 8 . 5 1 ( b r s , 1 H) , 9 . 4 6 ( s , 1H) , 1 1 . 7 7 ( b r s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 2 . 8 6 mi n LC / MS ( ES I + ) m/ z ; 4 0 9 [M+H] + ' H- NMR ( CDC 3 ) : 0 . 8 8 ( d , J = 7 . 2 Hz , 3 H) , 1 . 6 0 - 2 . 0 0 ( , 2H) , 2 . 3 7 ( s , 3 H) , 2 . 4 0 - 2 . 5 5 ( m, 2 H) , 2 . 5 5 - 2 . 7 0 ( , 1H) , 2 . 8 0 - 2 . 9 0 (m, 1H) , 2 . 9 5 - 3 . 0 5 (m, 1H) , 5 . 4 0 - 5 . 5 0 ( m, 1H) , 6 . 4 2 ( d , J = 8 . 4 Hz , 6 b 1H) , 6 . 8 3 ( d , J = 3 . 3 Hz , 1H) , 7 . 4 0 - 7 . 5 0 ( m, 1H) , 8 . 3 0 - 8 . 5 0 ( m, 1H) , 9 . 4 8 ( s , 1H) , 1 1 . 8 5 ( b r s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 5 0 mi n LC/ MS ( ES I + ) m/ z ; 2 9 7 [M+H] + Ή - NMR ( CD3O D) : 1 . 0 0 - 1 . 1 0 (m, 3 H) , 1 . 8 0 - 1 . 9 5 (m, 1H) , 2 . 1 0 - 2 . 2 0 (m, 1 H) , 2 . 7 0 - 2 . 9 0 ( m, 1H) , 3 . 2 0 - 3 . 3 0 (m, 1H) , 3 . 3 5 ( s , 2H) , 3 . 6 0 - 3 . 7 5 (m, 1H) , 3 . 9 0 - 4 . 2 5 (m, 1 H) , 4 . 2 5 - 4 . 5 5 ( m, 1H) , 5 . 2 5 - 5 . 5 0 7 (m, 1 H) , 6 . 4 0 - 6 . 5 5 ( , 1H) , 6 . 8 5 - 7 . 0 0 ( , 1H) , 7 . 5 0 - 7 . 6 0 ( , 1 H) , 8 . 0 0 - 8 . 1 0 (m, 1H) , 9 . 2 1 ( s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 1 . 9 2 mi n LC/ MS ( ES I + ) m/ z ; 3 5 0 [M+H] + LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 0 9 mi n 8 LC/ MS ( ES I + ) m/ z ; 3 6 5 [M+H] + LC/ MS ( ES I ) m/ z ; 3 6 3 [M- H] TABLE b 63 Ex Da t a H -NMR (CD 3OD) 1.01-1.08 (m, 3H), 1.77-1. 9 1 (m, 1H), 2 . 11-2. 19 (m, 1H) , 2 . 74-2. 8 5 (m, 1H) , 3 . 1 1-3. 18 (m, 1H) , 3 . 59-3. 82 (m, 3H) , 4 . 00 (dd, = 9 . 1 , 12. 7 Hz, 1H) , 4 . 17 (d, / = 6 . 8 Hz, 1H) , 4 . 35-4. 49 (m, 1H), 5.30-5.44 (m, 1H) , 6.40-6.45 (m, 1H) , 6.86-6.88 (m, 1H) , 7.53-7. 55 (m, 1H) , 8.00-8.05 (m, 1H), 9.21 (s, 1H). LC/MS: condition 2 , retention time = 3.29 in LC/MS(ESI +) m/z; 393 [M + l ] + LC/MS(ESD m/z; 391 [ - l] H-NMR (CDCl ) 1.02 (d, / = 7.5 Hz, 3H) , 1 . 15 (d, J = 7 2 Hz, 6H), 1.80-1.95 (m, 1H), 2 . 10-2.40 (m, 2H) , 2 . 70-2. 80 (m, 1H) 2 . 9 1 (d, J =6.3 Hz, 2H), 3.25-3.40 (m, 1H), 3 . 50-3. 70 (m 1H) , 3 . 70-3. 80 (m, 1H), 3 . 85-4. 00 (m, 1H), 5 . 40-5.55 (m, 1H) , 6.41 (d, J = 7 . 8 10 Hz, 1H), 6 . 70-6. 80 (m, 1H), 7 . 40-7.50 (m, 1H) , 7.67 (d, J = 7.8 Hz, 1H), 9.39 (s, 1H), 11. 9 1 (br s , 1H). LC/MS: condition 1 , retention time = 3.44 min LC /M S (ES ) m/z; 403 [M +H ] + LC /M S (ESI ) m/z; 401 [M-H] -NMR (CD 3OD) 1.00 (d, / = 6 . 9 Hz, 3H) , 1.85-2.00 1H), 2 . 10-2. 25 ( , 1H) , 2.65-2.80 (m, 1H) , 3.50-3. 70 (m, 2H) 3 . 90 -4. 10 ( , 2H), 4.31 (q, / = 9.6 Hz, 2H), 5.50-5.60 ( , 1H) , 6 . 43 (d, J = 8 . lHz, 1H) , 6 . 92 (d, = 3 . 9 Hz, 1H) , 7 . 57 (d, J = 3 . 6 Hz, 1H), 1 1 8 . 15 (d, J = 8 . 1 Hz, 1H), 9 . 22 (s, 1H). LC/MS: condition 1 , retention time = 3.37 min LC/MS(ESI +) m/z; 429 [M+H] + LC/MS(ESr) m/z; 427 [ -H ] L C /MS: condition 1 , retention time = 3.51 min 12 LC/MS(ESI +) m/z; 304 [M+H] + L C /MS(ESr) m/z; 302 [M-H] LC/MS: condition 1 , retention time 2 . 94 min 13 LC/MS(ESI +) m/z; 269 [M +H ] + -NMR (CDCI 3) 1.01 (d, / = 7 . 2 Hz, 3H) , 1.53-1.92 (m, 4H) , 2 . 09-2. 38 (m, 2H), 2.48-2.73 (m, 2H) , 2.75-2.99 (m, 1H) , 3.37-2.58 14 (m, 2H) , 4.45-4. 62 (m, 1H), 4 . 88-5.01 (m, 2H) , 6.41 (d, = 3.6 Hz, 1H), 7 . 12 (d, = 3.6 Hz, 1H), 7.30-7.35 (m, 5H) , 7 . 75 (s, 1H), 9 . 40 (br s , 1H) . LC/MS: condition 1 , retention 0.50 min 15 LC/MS(ESI +) m/z; 273 [M +H ] + -NMR ( CDCI 3 ) : 1 . 15-1.27 (m, 3H) , 1 . 70-2. 05 (m, 2H) , 2 . 44- 2 . 55 (m, 1H), 3.48-3.94 (m, 5H), 4.32-4.36 (m, 1H), 4 . 65-4.85 (m, 2H), 4 . 95-5. 07 (m, 2H), 6.32-6.38 (m, 1H) , 7 . 19-7.29 (m, 2H) , 7.83- 7 . 88 16 (m, 1H), 9.60-9.49 (m, 1H) . LC/MS: condition 1 , retention time = 0.54 min LC/MS(ESI +) m/z; 340 [M+H] + LC/MS: condition 1 , retention time 17 LC/MS(ESD m/z; 271 [M+H] + LC/MS: condition 1 , retention time = 3.27 min 18 LC/MS(ESI +) m/z; 269 [M+H] + LC/MS: condition 1 , retention time = 0.54 min 19 LC/MS(ESI +) m/z; 255 [M+H] + TABLE*3 64 E x Da t a - N R ( DMS O- ) 1 . 2 0 - 2 . 1 0 ( m, 10 H) , 6 . 2 5 ( d , / = 8 . 0 Hz , 1 H) , 6 . 4 2 - 6 . 5 8 ( m, 1H) , 8 . 2 2 ( , = 8 . 0 Hz , 1H) , 8 . 4 9 ( s , 1H) , 9 . 1 0 ( s , 1H) . 2 0 LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 2 4 mi n LC/ MS ( ES D m/ z ; 2 6 9 [M+ l ] + LC/ MS ( ES m/ z ; 2 6 7 [M- l ] TABLE 65 Da t a H- NMR ( CDC1 3 ) : 0 . 2 3 ( d , J = 6 . 9 Hz , 3 H) , 1 . 4 2 - 1 . 5 6 (m, 1H) , 1 . 6 0 - 1 . 8 0 (m, 1H) , 1 . 8 6 - 2 . 0 1 (m, 1H) , 2 . 0 8 - 2 . 2 1 (m, 1H) , 2 . 7 2 - 2 . 8 2 ( , 1H) , 3 . 0 5 - 3 . 1 8 (m, 1H) , 3 . 6 0 ( s , 2 H) , 3 . 6 8 ( d , J = 1 1 . 4 Hz , 1H) , 5 . 5 0 - 5 . 5 8 ( m, 1H) , 6 . 4 8 ( d , = 7 . 8 Hz , 1H) , 2 1 7 . 2 5 - 7 . 4 2 ( m, 5 H) , 7 . 4 8 ( s , 1 H) , 9 . 3 8 ( s , 1H) , 9 . 5 4 ( d , J = 7 . 8 Hz , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 3 1 mi n LC/ MS ( ES m/ z ; 4 5 1 , 4 5 3 [ M+ H] + Ή - NMR ( CDC I 3 ) : 0 . 3 1 ( d , J = 6 . 6 Hz , 3 H) , 1 . 4 0 - 1 . 5 5 (m, 1H) , 1 . 6 0 - 1 . 8 5 (m, 1H) , 1 . 9 0 - 2 . 0 5 ( , 1H) , 2 . 1 0 - 2 . 2 5 (m, 1H) , 2 . 7 0 - 2 . 8 0 ( , 1H) , 3 . 0 5 - 3 . 2 0 (m, 1H) , 3 . 5 0 - 3 . 6 5 (m, 1H) , 3 . 5 9 ( s , 2H) , 5 . 4 5 - 5 . 5 0 (m, 1 H) , 6 . 4 8 ( d , = 8 . 1 Hz , 1H) , 7 . 2 5 - 7 . 5 0 ( m, 2 2 6H) , 9 . 3 9 ( s , 1H) , 9 . 4 9 ( d , J = 8 . 4 Hz , 1H) , 1 1 . 9 ( b r s , 1 H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 0 9 mi n LC / MS ( ES I + ) m/ z ; 4 0 7 , 4 0 9 [ M+ H] + LC/ MS ( ES D m/ z ; 4 0 5 , 4 0 7 [ M- H] 'H- NMR ( CD C I 3 ) : 0 . 8 6 ( d , J = 6 . 9 Hz , 3 H) , 1 . 6 0 - 1 . 8 0 ( , 1H) , 1 . 8 5 - 2 . 0 0 (m, 1H) , 2 . 2 2 ( s , 3H) , 2 . 4 0 - 2 . 6 0 (m, 2H) , 2 . 7 5 - 2 . 9 0 (m, 2H) , 3 . 0 0 - 3 . 1 0 ( m, 1H) , 3 . 6 5 ( d d , J = 2 2 . 2 , 9 . 6 Hz , 2 H) , 5 . 4 0 - 5 . 5 0 (m, 1 H) , 6 . 8 0 ( s , 1 H) , 7 . 2 0 - 7 . 5 0 (m, 6H) , 8 . 5 8 ( b r s , 1 H) , 9 . 4 9 2 3 ( s , 1H) , 1 1 . 9 3 ( b r s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 1 . 0 0 mi n LC/ MS ( ES I + ) m/ z ; 3 8 7 [M+H] + LC/ MS ( ES ) m/ z ; 3 8 5 [M- H] LC / MS : c o n d i t i o n 1, r e t e n t i o n t i me = 2 . 7 4 mi n 2 4 | LC/ MS ( ES m/ z ; 4 5 1 , 4 5 3 [ M+ H] + LC/ MS ( ES D m/ z ; 4 4 9 , 4 5 1 [ M- H] ' H- NMR ( CD 0 D) : 0 . 9 5 ( d , J = 7 . 2 Hz , 3 H) , 1 . 9 0 - 2 . 0 0 (m, 1H) 2 . 1 0 - 2 . 2 5 (m, 1H) , 2 . 6 0 - 2 , 7 0 (m, 1H) , 3 . 5 0 - 3 . 6 0 (m, 2H) 3 . 8 5 - 4 . 0 5 ( m, 2 H) , 5 . 4 5 - 5 . 6 0 (m, 1 H) , 6 . 4 0 ( d , = 8 . 1 Hz , 1H) 6 . 8 2 ( d , J = 3 . 9 Hz , 1 H) , 7 . 5 4 ( d , J - 3 . 6 Hz , 1H) , 7 . 8 0 - 7 . 9 0 ( m 2H) , 8 . 0 0 - 8 . 0 5 (m, 1 ) , 8 . 1 0 - 8 . 1 5 (m, 1H) , 8 . 16 ( d , J = 7 . 8 Hz 1H) , 9 . 2 0 ( s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 7 3 mi n LC / MS ( ES m/ z ; 4 4 8 [M+H] + LC/ MS ( ES m/ z ; 4 4 6 [M- H] LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 7 8 mi n 2 6 | LC/ MS ( ES I + ) m/ z ; 4 4 8 [M+H] + LC/ MS ( ES ) m/ z ; 4 4 6 [M- H] - Ή - NMR ( CDC I 3 ) : 1 . 0 4 ( d , J = 6 . 9 Hz , 3 H) , 1 . 2 6 ( t , = 6 . 9 3H) , 1 . 7 0 - 1 . 8 6 ( m, 1 H) , 2 . 0 0 - 2 . 1 8 (m, 1H) , 2 . 6 8 - 2 . 8 4 (m, 3 . 2 8 - 3 . 5 0 (m, 1H) , 3 . 6 8 - 3 . 8 8 (m, 1H) , 3 . 8 8 - 4 . 0 2 ( , 4 . 0 5 - 4 . 3 8 ( m, 3H) , 5 . 1 5 - 5 . 2 5 (m, 1 H) , 6 . 4 3 ( d , / = 7 . 8 Hz , 2 7 6 . 7 3 ( b r s , 1H) , 7 . 3 2 ( b r s , 1H) , 7 . 5 8 ( d , J = 8 . 1 Hz , 1H) , ( s , 1H) , 1 1 . 5 1 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 5 9 mi n LC/ MS ( ES I + ) m/ z ; 3 5 5 [M+H] + TABLE 66 E x Da t a ' H- NMR ( CDC1 ) 0 . 9 8 ( d , J = 6 . 9 Hz , 3 H) , 1 . 7 7 - 1 . 8 8 (m, 1H) , 2 . 16 - 2 . 3 1 (m, 1H) , 2 . 6 8 - 2 . 8 2 (m, 1H) , 3 . 2 6 - 3 . 4 2 (m, 1H) , 3 . 9 0 - 4 . 0 5 (m, 1H) , 4 . 1 0 - 4 . 2 8 (m, 1H) , 4 . 4 4 - 4 . 5 9 (m, 1H) , 5 . 3 8 - 5 . 5 0 ( m, 1H) , 6 . 18 ( d , = 7 . 8 Hz , 1 H) , 6 . 8 9 ( b r s , 1H) , 7 . 3 1 2 8 ( t , J = 7 . 5 Hz , 1H) , 7 . 4 9 - 7 . 6 2 ( , 3H) , 7 . 6 6 ( d , J - 7 . 8 Hz , 1H) , 7 . 7 5 ( d , J = 7 . 8 Hz , 1H) , 8 . 5 4 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 7 8 mi n LC/ MS ( ES I + ) m/ z ; 4 7 0 [M+H] + LC/ MS ( ES m/ z ; 4 6 8 [M- H] LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 9 8 mi n 2 9 LC / MS ( ES I + ) m/ z ; 4 7 0 [M+H] + LC/ MS ( ES I ) m/ z ; 4 6 8 [M- H] LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 7 8 mi n 3 0 I LC/ MS ( ES + ) m/ z ; 4 5 5 [M+H] + LC/ MS ( ES m/ z ; 4 5 3 [M~ H] ~ - NMR ( CDC I 3 ) : 1 . 1 0 ( d , = 7 . 2 Hz , 3 H) , 1 . 7 5 - 1 . 9 0 (m, 1H) , 2 . 0 0 - 2 . 2 0 (m, 1H) , 2 . 7 9 - 2 . 9 9 (m, 1H) , 3 . 4 1- 4 . 0 3 (m, 3H) , 4 . 6 0 - 5 . 0 8 ( m, 1H) , 5 . 2 0 - 5 . 4 0 (m, 1H) , 6 . 4 5 ( d , J = 7 . 8 Hz , 1H) , 3 1 6 . 7 0 ( s , 1H) , 7 . 4 2 - 7 . 8 6 ( m, 6H) , 9 . 4 6 ( s , 1 H) , 1 2 . 1 4 ( s , 1 H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 8 7 mi n LC / MS ( ES I + ) m/ z ; 4 5 5 [M+H] + LC/ MS ( ES m/ z ; 4 5 3 [M- H] LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 6 6 mi n 3 2 LC / MS ( ES m/ z ; 4 1 9 [M+H] + - NMR ( CDCI 3 ) : 0 . 9 0 ( s , 3H) , 1 . 8 1- 1 . 9 8 (m, 1H) , 2 . 1 0 - 2 . 2 6 (m, 1H) , 2 . 5 1- 2 . 6 9 (m, 1H) , 3 . 1 8 - 3 . 3 3 (m, 1H) , 3 . 3 4 - 3 . 5 2 (m, 1 H) , 3 . 5 2 - 3 . 6 9 (m, 1H) , 3 . 6 9 - 3 . 8 1 (m, 1H) , 5 . 4 0 - 5 . 5 2 (m, 1 H) , 6 . 4 2 ( d , / = 7 . 8 Hz , 1 H) , 6 . 6 7 ( s , 1H) , 7 . 4 6 ( s , 1H) , 7 . 6 5 - 7 . 8 6 ( m, 2H) , 3 3 7 . 9 5 ( d , J = 7 . 5 Hz , 1H) , 8 . 0 5 ( d , J = 7 . 2 Hz , 1H) , 8 . 1 0 ( s , 1H) , 9 . 4 3 ( s , 1H) , 1 1 . 4 0 ( s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 0 7 mi n LC/ MS (ES m/ z ; 4 9 1 [M+H] + LC/ MS ( ES m/ z ; 4 8 9 [M- H] LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 8 9 mi n 3 4 ILC/ MS ( ES I + ) m/ z ; 4 5 5 [M+H] + LC/ MS ( ES m/ z ; 4 5 3 [M- H] ~ LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me - 1 . 8 8 mi n 3 5 LC / MS (ES ) m/ z ; 4 1 7 [M+H] ÷ LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 2 . 5 7 mi n 3 6 LC/ MS ( ES I + ) m/ z ; 4 1 0 [M+H] + LC/ MS ( ES I ) m/ z ; 4 0 8 [M- H] LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 2 . 5 7 mi n 3 7 ILC/ MS ( ES I + ) m/ z ; 4 2 3 [M+H] + LC MS ( ES ) m/ z ; 4 2 1 [M- H] LC / MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 3 . 2 0 mi n 3 8 | LC/ MS ( ES r ) m/ z ; 3 7 9 [M+H] + LC/ MS (ES m/ z ; 3 7 7 [M- H] TABLEb 67 Ex Da t a LC / MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 0 0 mi n 3 9 LC/ MS ( ES I +) m/ z 4 4 1 +H] + LC/ MS ( ES m/ z ; 4 3 9 M- H] - LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me 3 . 0 2 mi n 4 0 LC/ MS ( ES m/ z ; 4 4 1 M+H] + LC/ MS ( ES m/ z ; 4 3 9 M- H] LC/ MS : c o n d i t i o n 1, r e t e n t t i me = 3 . 5 0 mi n 4 1 LC/ MS ( ES I +) m/ z ; 4 4 1 M+H] LC/ MS ( ES I ) m/ z ; 4 3 9 M- H] - LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 2 . 4 0 mi n 4 2 LC / MS ( ES I +) m/ z ; 3 9 8 M+H] + LC/ S ( ES I ) m/ z ; 3 9 6 M- H] LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me 3 . 0 7 mi n 4 3 LC/ MS ( ES I +) m/ z ; 3 9 8 M+H] + LC/ MS ( ES I ) m/ z ; 3 9 6 M- H] - LC/ MS : c o n d i t i o n 1, r t e n t i o n t i me 1 . 6 7 mi n 4 4 LC/ MS ( ES I + ) m/ z ; 3 9 8 M+H] + LC/ MS ( ES I ) m/ z ; 3 9 6 M- H] - LC/ MS : c on d i t i o n 3 , r t e n t i o n t i me 1 . 8 4 mi n 4 5 LC/ MS ( ES I +) m/ z ; 3 8 3 +H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t me 1 . 3 4 mi n 4 6 LC/ MS ( ES I +) m/ z ; 4 0 5 M+H] + -NMR (CDC l j ) : 0 . 8 8 ( d , J = 7 . 2 Hz , 3 H) , 1. 3 3 - 2 . 0 8 (m, 10H) , 2 . 4 0 - 2 . 7 9 (m, 4 H) , 2 . 8 6 - 3 . 1 2 (m, 2 H) , 5 . 3 8 - 5 . 4 9 (m, 1H) , 6 . 4 1 ( d , J = 8 . 4 Hz , 1H) , 6 . 8 0 - 6 . 9 0 (m, 1H) , 7 . 4 0 - 7 . 4 8 (m, 1H) , 8 . 3 8 ( b r 4 7 s , 1H) , 9 . 4 8 ( s , 1H) , 1 1. 3 3 ( s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 0 6 mi n LC/ MS ( ES I +) m/ z ; 3 5 1 [M+H] + Ή - NMR (CDCI 3 ) : 0 . 8 3 ( s , 9H) , 1 . 0 4 ( d , J = 6 . 6 Hz , 3H) , 1. 3 6 - 2 . 17 (m, 1 2H) , 2 . 7 0 - 3 . 0 0 (m, 2H) , 3 . 3 8 - 3 . 9 0 (m, 2 H) , 4 . 5 5 - 4 . 8 5 (m, 1H) , 5 . 10 - 5 . 3 0 ( m, 1H) , 6 . 4 1 ( d , 7 . 8 Hz , H) , 6 . 5 2 ( s , 1H) , 7 . 4 6 4 8 a ( s , 1H) , 7 . 5 7 ( d , J = 8 . 4 Hz , 1H) , 9 . 4 6 ( s , 1H) , 1 1. 74 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 3 7 mi n LC/ MS ( ES I + ) m/ z ; 4 4 9 [M+H] .+ LC/ MS : c o n d i t i o n 3 , r e t e n t i o n 2 . 2 8 mi n 4 8 b LC/ MS ( ES I + ) m/ z ; 4 4 9 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n 1 . 2 2 mi n 4 9 LC/ MS ( ES I + ) m/ z ; 3 7 6 [M+H] + LC/ MS ( ES D m/ z ; 3 7 4 [M- H] - - NMR ( DMS0 - ) : 1 . 79 - 1 . 9 0 (m, 2 H) , 2 . 12 - 2 . 2 8 (m, 2 H) , 2 . 7 0 - 2 . 9 0 (m, 2 H) , 2 . 9 0 - 3 . 0 4 (m, 2 H) , 3 . 6 3 ( s , 2H) , 4 . 6 2 - 4 . 8 7 (m, 1H) , 6 . 6 4 ( d , J = 3 . 6 Hz , 1H) , 7 . 5 6 ( d , = 8 . 1 Hz , 2 H) , 7 . 6 1 ( d , 5 0 J = 3 . 6 Hz , 1H) , 7 . 8 2 ( d , J = 8 . 4 Hz , 2H) , 8 . 74 ( s , 1H) . LC / MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 3 7 mi n LC/ MS ( ES I +) m/ z ; 4 0 1 [M+H] + LC/ MS ( ES m/ z ; 3 9 9 [M- H] TABLE" 68 Ex Data -NMR (DMSO- ) : 1.77-1.93 (m, 2H) , 2.08-2.30 (m, 2H), 2 . 66-2. 89 (m, 2H), 2 . 98-3. 14 (m, 2H) , 3 . 69 (s, 2H), 4 . 60-4. 80 (m, 1H), 6.60-6. 70 (m, 1H), 6.86 (d, = 3 . 6 Hz, 1H), 6.96 (d, J = 3 . 3 Hz, 1H), 7.61 (d, / = 3 . 0 Hz, 1H), 8.74 (s, 1H), 12.36 (br s , 1H). LC/MS: condition 3 , retention time = 1.43 in LC/MS(ESI +) m/z; 416, 418 [M+H] + LC/MS (ESr) m/z; 414, 416 [M-H] -NMR (DMS0- ) 1.78-1.90 (m, 2H) , 2 . 10-2.28 ( , 2H), 2 . 70-2. 90 ( , 2H), 2,90-3. 05 (m, 2H) , 3.63 (s, 2H), 4 . 61-4. 79 (m, 1H), 6.65 (d, J = 3 . 3 Hz, 1H) , 7.52-7.64 (m, 3H), 7.71 (d, J = 52 8 . 1 Hz, 2H) , 8 . 74 (s, 1H) . LC/MS: condition 3 , retention time = 1 . 75 min LC/MS(ESI +) m/z; 444 [M+H] + LC/MS (ESI ) m/z; 442 [M-H] ~ LC/MS: condition 3 , retention time = 1 . 79 min LC/MS (ES ) m/z; 285 [M+H] + -NMR (CDC1 ) 2.05-2.48 (m, 6H), 3 . 10-3.30 (m, 2H), 3 . 64 (s, 2H), 4.91-5. 10 (m, 1H), 6.46 (d, J = 8 . 3 Hz, 1H), 6 . 76-6.89 (m, 1H), 7.21-7. 4 1 (m, 5H) , 7.42-7.53 (m, 1H), 7 . 82 (d, J = 8 . 0 Hz, 1H) , 9 . 44 (s, 1H) , 12. 1 (s, 1H) . LC/MS: condition 1 , retention time = 0 . 37 min LC/MS (ES ) m/z; 359 [M+H] 'H-NMR (DMSO-^) : 1.98-2.22 (m, 4H) , 2.30-2.68 (m, 2H), 3 . 00-3. 18 ( , 2H) , 3.76 (s, 2H) , 4 . 83-5. 02 (m, 1H), 6 . 19 (d, J = 7 . 7 Hz, 1H), 6 . 80 (d, = 3.6 Hz, 1H), 6.90 (d, / = 3.6 Hz, 1H), 55 6 . 92-7. 03 (m, 1H), 7.60 (d, / = 3 . 3 Hz, 1H), 8 . 2 1 (d, = 8 . 0 Hz, 1H), 8 . 32 (s, 1H), 9.02 (s, 1H) . LC/MS: condition 1 , retention time = 0.94 min LC/MS(ESD m/z; 399 [M+H] Ή -NMR (CD 3OD) : 2 . 12-2. 32 (m, 4H) , 2.39-2.57 (m, 2H) , 3 . 08-3. 23 ( , 2H), 3 . 75 (s, 2H) , 5.09-5.25 (m, 1H), 6.47 (d, J = 8.04 Hz, 1H), 6.95 (d, = 4 . 2 Hz, 1H) , 7.50-7.70 (m, 5H), 8.28 (d, / = 8 . 0 Hz, 1H) , 9 . 19 (s, 1H) . LC/MS: condition 1 , retention time = 1 . 65 min LC/MS (ESr) m/z; 427 [M+H] + 'H-NMR (DMSO-i/g) fi : 1.98-2.43 (m, 6H), 2.95-3.09 (m, 2H), 3.69 (s, 2H), 4 . 86-5. 0 1 (m, 1H), 6 . 19 (d, J = 8.0 Hz, 1H) , 7.81 (d, = 3.9 Hz, 1H), 7.50-7.68 (m, 3H), 7.83 (d, = 8.3 Hz, 2H) , 8.21 (d, J = 8 . 9 Hz, 1H) , 9 . 02 (s, 1H) . LC/MS: condition 1 , retention time = 0 . 37 min LC /MS(ESr) m/z; 384 [M+H] + . 'H-NMR (DMSO- : 1.97-2.24 (m, 4H) , 2.35-2.60 (m, 2H), 2 . 92-3. 1 1 (m, 2H) , 3.73 (s, 2H), 4 . 85-5. 03 (m, 1H), 6 . 0 1 (d, = 8.0 Hz, 1H), 6 . 8 1 (d, = 3.6 Hz, 1H), 6.60 (d, J 3.6 Hz, 1H), 58 7 . 64-7. 79 (m, 2H) , 7.8 6 (d, / = 9 . 2 Hz, 1H) , 8 . 20 (d, = 8 . 0 Hz, 1H), 8 . 32 (s, 1H). LC/MS: condition 1 , retention time = 0.45 min LC/MS(ESD m/z; 402 [M+H] + TABLE 69 E x Da t a - NMR ( DMSO- i fi ) : 1 . 7 4 - 1 . 9 0 (m, 2 H) , 1 . 9 8 - 2 . 1 9 (m, 2 H) , 2 . 7 0 - 3 . 1 5 ( m, 4 H) , 3 . 5 0 ( s , 2 H) , 3 . 9 8 - 4 . 1 4 (m, I H) , 4 . 1 8 ( s , 2H) , 6 . 3 1 ( d , J = 3 . 0 Hz , I H) , 7 . 1 8 ( b r s , I H) , 7 . 2 2 - 7 . 2 9 ( m, I H) , 5 9 7 . 3 1 - 7 . 3 8 (m, 5 H) , 7 . 4 ( b r s , I H) , 7 . 9 3 ( s , I H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 3 5 mi n LC/ MS ( ES D m/ z ; 3 6 2 [M+H] + ' H- NMR ( DMS0 - ) : 1 . 8 0 - 1 . 9 8 (m, 2 H) , 2 . 6 8 - 3 . 0 0 (m, 4 H) , 3 . 6 3 - 3 . 6 0 ( m, 2 H) , 4 . 1 1 - 4 . 3 1 ( , 3 H) , 4 . 4 3 ( s , 2 H) , 6 . 2 9 ( b r s , 6 0 I H) , 7 . 2 7 ( s , I H) , 7 . 3 2 - 7 . 5 0 ( m, 5 H) , 7 . 9 5 ( s , I H) , 1 1 . 7 ( s , H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 2 . 7 8 mi n LC/ MS ( ES I + ) m/ z ; 4 2 6 [M+H] + Ή - NMR ( DMSO- '• 1 . 7 1 - 1 . 9 0 (m, 2 H) , 2 . 0 0 - 2 . 2 0 (m, 2 H) , 2 . 6 8 - 3 . 0 3 (m, 4 H) , 3 . 5 4 ( s , 2 H) , 3 . 9 8 - 4 . 2 6 ( m, 3 H) , 6 . 3 1 ( s , I H) , 7 . 19 ( s , I H) , 7 . 3 2 - 7 . 4 9 (m, 2 H) , 7 . 6 8 - 7 . 8 0 (m, I H) , 7 . 9 3 ( s , I H) , 6 1 8 . 4 0 - 8 . 6 1 (m, 2H) , 1 1 . 7 ( s , I H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 3 3 mi n LC/ MS ( ES I + ) m/ z ; 3 6 3 [M+H] + ' H- NMR ( DMSO- 1 . 8 0 - 1 . 9 2 (m, 2 H) , 2 . 0 2 - 2 . 2 0 (m, 2 H) , 2 . 6 8 - 3 . 0 9 ( , 4 H) , 3 . 6 0 ( s , 2 H) , 4 . 0 0 - 4 . 2 9 (m, 3 H) , 6 . 3 1 ( s , I H) , 7 . 2 1 ( s , I H) , 7 . 4 2 ( s , I H) , 7 . 5 5 ( d , J 7 . 7 Hz , 2 H) , 7 . 8 1 ( d , 6 2 J = 7 . 4 Hz , 2H) , 7 . 9 4 ( s , I H) , 1 1 . 7 ( s , I H) . LC / MS ' c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 3 5 mi n LC/ MS ( ES I + ) m/ z ; 3 8 7 [M+H] + Ή - NMR ( DMS0 - i ) : 1 . 7 0 - 1 . 9 2 (m, 2 H) , 2 . 0 1 - 2 . 2 0 (m, 2 H) , 2 . 7 1 - 3 . 1 2 (m, 4 H) , 3 . 6 0 ( s , 2 H) , 4 . 0 0 - 4 . 3 3 ( m, 3 H) , 6 . 3 2 ( d , J = 3 . 6 Hz , H) , . 7 . 2 1 ( s , I H) , 7 . 4 2 ( d , J = 3 . 6 Hz , I H) , 7 . 5 8 ( s , 6 3 J = 7 . 7 Hz , 2 H) , 7 . 7 1 ( d , J = 8 . 0 Hz , 2 H) , 7 . 9 4 ( s , I H) , 1 1 . 7 ( s , I H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 6 4 mi n LC/ MS ( ES I + ) m/ z ; 4 3 0 [M+H] + Ή - NMR ( DMS0 - ) : 1 . 8 0 - 2 . 0 0 (m, 2 H) , 2 . 5 5 - 2 . 7 9 (m, 2 H) , 2 . 8 5 - 3 . 1 0 ( , 2 H) , 4 . 2 0 ( s , 2 H) , 4 . 2 5 - 4 . 5 1 ( m, 3 H) , 6 . 3 9 ( d , J = 2 . 4 , I H) , 7 . 2 4 ( s , I H) , 7 . 4 3 ( s , I H) , 7 . 9 5 ( s , I H) , 8 . 9 4 ( s , 6 4 I H) , 1 1 . 7 ( s , I H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 3 9 mi n LC/ MS ( ES D m/ z ; 3 9 9 [M+H] + ' H- NMR ( CDC 13 ) : 1 . 9 5 - 2 . 1 3 (m, 2 H) , 2 . 8 0 - 3 . 1 0 ( m, 4 H) , 3 . 4 8 - 3 . 6 2 ( , 2 H) , 4 . 0 2 - 4 . 18 (m, I H) , 4 . 4 0 ( s , 2 H) , 4 . 8 0 - 4 . 9 8 ( m, I H) , 5 . 6 6 6 5 ( s , I H) , 6 . 3 3 - 6 . 5 1 (m, I H) , 7 . 1 5 - 7 . 4 5 ( , I H) , 7 . 9 9 ( s , I H) , 9 . 3 1 ( s , I H) . ' H- NMR ( CDC I 3) : 1 . 8 9 - 2 . 0 0 (m, 2 H) , 2 . 1 1- 2 . 2 8 ( m, 2 H) , 2 . 9 1- 3 . 2 4 (m, 4H) , 3 . 8 4 ( s , 2 H) , 4 . 1 4 - 4 . 3 0 (m, I H) , 4 . 3 9 ( s , 2 H) , 5 . 3 2 ( s , I H) , 6 . 4 5 ( d , J = 3 . 9 Hz , I H) , 7 . 3 0 ( d , J = 3 . 9 Hz , I H) , 7 . 7 3 ( s , 6 6 I H) , 7 . 9 7 ( s , I H) , 8 . 7 7 ( s , I H) , 9 . 6 2 ( s , I H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me = 0 . 3 3 mi n LC/ MS ( ES I + ) m/ z ; 3 6 9 [M+H] + ' H- NMR ( CD3OD) : 0 . 9 0 - 1 . 0 5 (m, 3 H) , 1 . 5 3 - 2 . 8 7 ( m, 7H) , 3 . 3 9 - 3 . 5 3 6 7 (m, 2 H) , 4 . 2 0 - 4 . 5 6 ( m, 3H) , 6 . 4 8 ( d , = 2 . 4 Hz , I H) , 7 . 0 0 - 7 . 3 5 (m, 5H) , 7 . 6 7 ( s , I H) , 7 . 9 0 ( s , I H) . TABLE 70 TABLEb 7 1 ' H- NMR ( DMS O- f ) : 1 . 9 8 - 2 . 7 0 (m, 6 H) , 2 . 9 2 - 3 . 10 (m, 2H) , 3 . 6 7 ( s , 2 H) , 4 . 8 4 - 5 . 0 3 (m, 1H) , 6 . 18 d , J = 7 . 7 Hz , 1H) , 6 . 8 1 ( d , J - 3 . 3 Hz , 1H) , 7 . 4 3 - 7 . 6 2 ( , 2 H) , 7 . 7 5 ( d , J = 6 . 9 Hz , 2H) , 8 . 2 2 7 8 ( d , J = 7 . 7 Hz , 1H) , 9 . 0 2 ( s , 1H) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me - 2 . 4 9 mi n LC/ MS ( ES I +) m/ z ; 4 4 5 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 0 . 3 7 mi n 7 9 LC / MS ( ES m/ z ; 4 1 0 [M+H] + - NMR ( CDC1 3) : 2 . 0 9 - 2 . 5 6 ( m, 6 H) , 3 . 1 3 - 3 . 3 6 (m, 2H) , 3 . 6 6 ( s , 2H) , 4 . 9 0 - 5 . 1 1 (m, 1H) , 6 . 2 8 ( d d , = 9 . 5 , 3 . 3 Hz , 2 H) , 6 . 4 0 - 6 . 5 5 ( d , 8 0 J = 8 . 3 Hz , 1H) , 6 . 78 ( d , J = 3 . 9 Hz , 1H) , 7 . 4 9 ( d , J = 3 . 6 Hz , 1H) , 7 . 7 9 ( d , J = 8 . 3 Hz , 1H) , 9 . 4 1 ( s , 1H) . LC/ MS ' c o n d i t i o n 1, r e t e n t i o n t i me = 0 . 6 2 mi n LC/ MS ( ES I +) m/ z ; 4 2 7 , 4 2 9 [ M+ H] + Ή -NMR ( CDC I 3 ) : 2 . 0 6 - 2 . 5 1 (m, 6H) , 3 . 15 - 3 . 3 3 (m, 2H) , 3 . 8 0 ( s , 2H) , 4 . 9 0 - 5 . 1 1 ( , 1H) , 6 . 4 7 ( d , J = 8 . 3 Hz , 1H) , 6 . 7 9 ( d , J = 3 . 9 Hz , 1H) , 6 . 8 9 ( d , 0 . 9 Hz , 1H) , 8 . 1 8 ( d , = 1. 5 Hz , 1H) , 8 1 7 . 4 7 ( d , J = 3 . 9 Hz , 1H) , 7 . 8 1 ( d , / = 8 . 3 Hz , 1H) , 9 . 4 4 ( s , 1H) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 0 . 8 7 mi n LC/ MS ( ES I + ) m/ z ; 4 4 3 , 4 4 5 [ M+ H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me - 0 . 8 4 mi n 8 2 LC/ MS ( ES I + ) m/ z ; 4 4 3 , 4 4 5 [ M+ H] + - NMR ( CDC I 3 ) : 2 . 0 5 - 2 . 5 2 (m, 6H) , 3 . 18 - 3 . 3 0 (m, 2H) , 3 . 8 2 ( s , 2H) , 4 . 9 3 - 5 . 1 2 (m, 1H) , 6 . 4 6 ( d , J = 7 . 7 Hz , 1H) , 6 . 7 8 ( d , J = 3 . 9 Hz , 1H) , 7 . 4 4 ( s , 1H) , 7 . 4 8 ( d , J = 3 . 9 Hz , 1H) , 7 . 7 9 ( d , J 8 3 = 8 . 0 Hz , 1H) , 9 . 4 2 ( s , 1Ή ) . LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 0 . 5 0 mi n LC/ MS ( ES I + ) m/ z ; 4 4 3 , 4 4 5 [ M+ H] + - NMR ( CDC I 3 ) : 2 . 0 5- 2 . 4 3 ( m, 6H) , 3 . 0 9 - 3 . 2 5 (m, 2H) , 3 . 6 0 ( s , 2H) , 4 . 9 1 - 5 . 1 1 ( , 1H) , 6 . 4 6 ( d , J = 8 . 2 Hz , 1H) , 6 . 8 0 ( d , J = 3 . 8 Hz , 1H) , 6 . 9 5 - 7 . 1 1 (m, 2H) , 7 . 1 5 ( s , 1H) , 7 . 4 6 ( d , J = 3 . 4 8 4 Hz , 1H) , 7 . 8 1 ( d , J = 8 . 2 Hz , 1H) , 9 . 4 3 ( s , 1H) . LC/ MS : c o n d i t i o n 1 , r e t e n t i o n t i me - 1 . 3 7 mi n LC/ MS ( ES I + ) m/ z ; 4 3 9 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 0 . 3 7 mi n 8 5 LC/ MS ( ES I +) m/ z ; 3 9 8 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 0 . 3 5 mi n 8 6 LC/ MS ( ES D m/ z ; 3 8 0 [M+H] + LC/ MS : c o n d i t i o n 1, r e t e n t i o n t i me = 3 . 3 2 mi n 8 7 LC / MS ( ES I + ) m/ z ; 4 1 3 , 4 15 [ M+H] + LC/ MS (ES r ) m/ z ; 4 1 1, 4 13 [M- H] TABLE1 72 LC / MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 0 . 3 7 mi n 8 8 LC / MS ( ES D m/ z ; 3 2 9 [M+H] + LC / MS ( ES I ) m/ z ; 3 2 7 [M- H] LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 4 3 mi n 8 9 LC/ MS ( ES m/ z ; 4 6 0 , 4 6 2 [ M+ H] + LC/ MS ( ES I ) m/ z ; 4 5 8 , 4 6 0 [M- H] LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 3 3 mi n 9 0 LC/ MS ( ES I + ) m/ z ; 4 1 4 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 0 . 7 5 mi n 9 1 LC/ MS ( ES I + ) m/ z ; 3 4 0 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 2 2 mi n 9 2 LC / MS ( ES I + ) m/ z ; 3 5 6 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 0 3 mi n 9 3 LC/ MS ( ES I + ) m/ z ; 3 9 8 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 1 6 mi n 9 4 LC/ MS ( ES I + ) m/ z ; 3 2 5 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 5 1 mi n 9 5 LC/ MS ( ES I + ) m/ z ; 3 6 8 [M+H] + LC/ MS ( ES I ) m/ z ; 3 6 6 [M- H] - LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 0 . 6 1 mi n 9 6 LC/ MS ( ES I + ) m/ z ; 3 6 7 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 4 9 mi n 9 7 LC/ MS ( ES I + ) m/ z ; 4 2 4 [M+H] + LC/ MS ( ES m/ z ; 4 2 2 [M- H] LC / MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 0 . 4 8 mi n 9 8 LC/ MS ( ES I + ) m/ z ; 3 5 3 [M+H] + LC/ MS ( ES m/ z ; 3 5 1 [M- H] LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me - 0 . 8 5 mi n 9 9 LC/ MS ( ES I + ) m/ z ; 3 7 0 [M+H] + - NMR ( DMSO- ) : 1 . 8 2 ( d , J = 1 1 . 7 Hz , 2H) , 2 . 1 8 ( t , J = 1 1 . 3 Hz , 2 H) , 2 . 6 1- 2 . 7 8 (m, 6 H) , 3 . 0 5 ( d , J = 1 1 . 4 Hz , 2 H) , 4 . 6 6 ( t , J = 1 1 . 7 Hz , 1H) , 6 . 6 4 ( d , J = 3 . 3 Hz , 1H) , 7 . 6 0 ( d , = 3 . 3 Hz , 1 0 0 1H) , 8 . 7 3 ( s , 1H) , 1 1 . 4 8 ( b r s , 1H) , 1 2 . 3 6 ( b r s , 1 H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 0 . 4 3 mi n LC / MS ( ES D m/ z ; 3 3 9 [M+H] + LC/ MS ( ES D m/ z ; 3 3 7 [M~ H] Ή - NMR (DMS 0 - ) 1 . 1 3 ( m, 2 H) , 1 . 4 3 ( b r s , 1H) , 1 . 9 0 (m, 4 H) , 2 . 5 2 (m, 2 H) , 3 . 3 0 (m, 2 H) , 4 . 4 3 ( t , J = 8 . 1 Hz , 1H) , 4 . 6 2 ( m, 1H) , 6 . 6 1 ( d , J = 3 . 9 Hz , 1H) , 7 . 6 0 ( d , / = 3 . 9 Hz , 1H) , 8 . 7 3 ( s , 1 0 1 1H) , 1 1 . 4 2 ( b r s , 1H) , 1 2 . 3 4 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 2 8 mi n LC/ MS ( ES m/ z ; 3 1 5 [M+H] + ' H- NMR (DMS O- : 1 . 1 0 ( m, 2 H) , 1 . 4 5 ( b r s , 1H) , 1 . 9 3 (m, 4 H) , 2 . 3 1 (m, 1H) , 3 . 2 3 ( , 6 H) , 4 . 6 4 ( m, 1H) , 6 . 6 2 ( d , = 3 . 3 Hz , 1H) , 7 . 6 0 ( d , J = 3 . 3 Hz , 1H) , 8 . 7 4 ( s , 1H) , 1 1 . 4 2 ( b r s , 1H) , 1 0 2 1 2 . 3 5 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 2 0 mi n LC/ MS ( ES m/ z ; 3 9 6 [M+H] + TABLE 73 H- NMR ( DMS O- : 1 . 2 3 - 1. 6 0 (m, 2 H) , 1 . 8 1- 1 . 9 2 ( , 4H) , 2 16 ( b r s , 1H) , 2 . 6 0 (m, 2H) , 4 . 6 6 ( m, 1H) , 5 . 6 4 - 5 . 7 7 ( m, 1H) , 10 3 6 . 5 6 - 6 . 9 2 (m, 2H) , 7 . 6 0 ( d , J = 3 . 6 Hz , 1H) , 8 . 7 3 ( s , 1H) . LC / MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 7 0 mi n LC/ MS ( E S I + ) m/ z ; 3 3 6 [M+H] + LC / MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 4 5 mi n 10 4 LC / MS ( E S m/ z ; 3 5 3 [ M+H] + LC/ MS ( ES I ) m/ z ; 3 5 1 [M- H] LC / MS : c o n d i t i o n 3 , r e t e n t i o n 1 . 2 7 mi n 10 5 LC/ MS ( E S I + ) m/ z ; 3 5 3 [M+H ] + -NMR ( DMS0 - ) 1 . 4 3 - 1 . 8 4 (m, 7 H) , 2 . 0 0 - 2 . 2 3 (m, 4 H) , 2 . 6 3 - 2 . 7 7 ( m, 2 H) , 4 . 5 7 ( b r s , 1H) , 4 . 9 1- 4 . 9 8 (m, 1H) , 6 . 2 1 ( d , J = 8 . 3 Hz , 1H) , 6 . 9 0 ( d , J = 3 . 6 Hz , 1H) , 7 . 5 8 ( d , J = 3 . 6 Hz , 10 6 1H) , 8 . 17 ( d , = 8 . 3 Hz , 1H) , 9 . 0 5 ( s , 1H) , 1 2 . 0 6 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 3 9 mi n LC/ MS ( ES I + ) m/ z ; 3 3 6 [M+H] + 'H- NMR ( DMSO- g : 1 . 4 0 - 1 . 5 4 ( , 2 H) , 1. 6 0 - 1 . 8 4 ( , 5 H) , 2 . 0 3 - 2 . 1 8 (m, 4 H) , 2 . 6 3 ( b r s , 2H) , 4 . 6 5 ( b r s , 1H) , 5 . 0 6 ( b r s , 1H) , 6 . 19 ( d , 10 7 J = 8 . 3 Hz , 1H) , 6 . 8 5 ( s , 1H) , 7 . 5 7- 7 . 6 3 (m, 1H) , 8 . 2 0 ( d , J = 8 . 3 Hz , 1H) , 9 . 0 3 ( s , 1H) , 1 2 . 2 6 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me - 1 . 2 4 mi n LC/ MS ( ES I +) m/ z ; 3 3 6 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me 0 . 6 2 mi n 10 8 LC/ MS ( ES I + ) m/ z ; 3 9 9 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 2 . 1 6 mi n 10 9 LC/ MS ( ES I + ) m/ z ; 5 1 2 [M+H] + LC / MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 0 . 7 4 mi n 1 1 0 LC/ MS ( ES I + ) m/ z 3 8 3 [M+H] + LC/ MS : c o n d i t i o n 3 , r e t e n t i o n 0 . 4 7 mi n 1 1 1 LC/ MS ( ES I +) m/ z ; 4 1 2 [M+H] + Ή - NMR ( DMS0 - f ) : 1 . 0 7 (m, 2 H) , 1 . 5 1 ( m, 2H) , 1 . 9 6 (m, 5H) , 2 . 2 7 (m, 3H) , 2 . 4 0 ( d d , J = 1 3 . 5 , 7 . 8 Hz , 1H) , 2 . 5 0 - 2 . 5 7 (m, 3H) , 2 . 6 8 ( d d , J = 9 . 6 , 6 . 3 Hz , 1H) , 4 . 17 ( b r s , 1H) , 4 . 6 3 , ( d , J = 1 1 2 1. 5 Hz , 2 H) , 6 . 6 2 ( d , J = 4 . 0 Hz , 1H) , 7 . 5 9 ( d , J = 4 . 0 Hz , 1H) , 8 . 7 3 ( s , 1H) , 1 1. 4 4 ( b r s , 1H) , 12 . 3 4 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me - 0 . 8 1 mi n LC/ MS ( ES I + ) m/ z ; 3 8 4 [M+H] + Ή - NMR ( DMS0 - ) : 1. 0 4 (m, 2 H) , 1 . 2 7 ( b r s , 1H) , 1. 8 6 ( d , J = 8 . 7 Hz , 4 H) , 2 . 2 2 ( d , J = 6 . 9 Hz , 2H) , 2 . 5 0 ( , 2H) , 2 . 6 2 ( d d , J = 7 . 5 , 6 . 6 Hz , 2H) , 3 . 4 8 ( d d , J = 7 . 5 , 6 . 3 Hz , 2H) , 4 . 1 1 ( b r 1 1 3 s , 1H) , 4 . 5 8 (m, 1H) , 5 . 1 8 (b r s , 1H) , 6 . 5 7 ( d , J = 3 . 3 Hz , 1H) , 7 . 5 6 ( d , J = 3 . 3 Hz , 1H) , 8 . 7 0 ( s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 0 . 7 4 mi n LC/ MS ( ES I + ) m/ z ; 3 7 0 [M+H] + TABLE 74 - NMR (DMS 0 - ) : 1 . 0 4 (m, 2 H) , 1 . 5 1 ( b r s , 1H) , 1. 9 0 (m, 4H) , 2 . 3 0 ( d , / = 7 . 5 Hz , 2 H) , 2 . 5 0 (m, 2 H) , 2 . 8 6 ( b r s , 4H) , 3 . 4 ( b r s , 4H) , 4 . 6 1 (m, 1H) , 6 . 5 7 ( d , J = 3 . 3 Hz , 1H) , 7 . 5 6 ( d , J = 3 . 3 1 1 4 Hz , 1H) , 8 . 7 1 ( s , 1H) , 1 1 . 4 0 ( b r s , 1H) , 12 . 3 2 (b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 1 7 i n LC/ MS ( ES m/ z ; 4 3 2 [M+H] + Ή - NMR (DMS .) : 1 . 1 8 (m, 2 H) , 1 . 5 6 ( b r s , 1H) , 1. 9 3 (m, 8H) , 2 . 2 1 ( d , / = 7 . 8 Hz , 2 H) , 2 . 5 0 (m, 6H) , 4 . 6 4 (m, 1H) , 6 . 6 2 ( d , 1 1 5 J = 3 . 9 Hz , 1 ) , 7 . 59 ( d , J = 3 . 9 Hz , 1H) , 8 . 7 4 ( d , J = 2 . Hz , 1H) , 1 1. 3 9 ( b r s , 1H) , 12 . 3 5 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 1 9 mi n C/ MS ( ES I +) m/ z ; 4 1 8 [M+H] + -NMR ( D S0 - . f ) : 1. 0 9 (m, 2 H) , 1 . 5 3 (b r s , 1H) , 1. 9 0 ( d , J = 12 . 0 Hz , 2H) , 2 . 0 1 ( d , J = 12 . 0 Hz , 2H) , 2 . 3 3 ( d , 7 . 2 Hz , 2H) , 2 . 5 5 (m, 2 H) , 2 . 6 1 ( , 4 H) , 2 . 7 6 (m, 4 H) , 4 . 64 (m, 1H) , 6 . 6 2 1 1 6 ( d , = 3 . 6 Hz , 1H) , 7 . 6 0 ( d , 3 . 6 Hz , 1H) , 8 . 7 5 ( s , 1H) , 1 1. 3 3 ( b r s , 1H) , 12 . 34 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 6 2 mi n LC/ S ( ES D m/ z ; 4 2 0 [M+H] + -NMR ( DMS0 - f ) : 0 . 0 9 (m, 2 H) , 0 . 3 9 (m, 2H) , 0 . 8 7 ( m, 1H) , 1. 1 1 ( , 2 H) , 1 . 4 5 ( b r s , 1H) , 1 . 9 2 ( m, 4H) , 2 . 4 0 ( d , J = 6 . 6 Hz , 2H) , 2 . 4 3 ( d , J = 6 . 6 Hz , 2 H) , 2 . 5 1 (m, 3 H) , 4 . 6 4 ( , 1H) , 6 . 6 1 1 1 7 ( d , J = 3 . 9 Hz , l H) , 7 . 5 9 ( d , J = 3 . 3 Hz , 1H) , 8 . 7 3 ( s , 1H) , 1 1. 4 0 ( b r s , 1H) , 12 . 3 2 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 2 3 mi n LC/ MS ( ES D m/ z ; 3 6 8 [M+H] + Ή - NMR (DMSO- 1 . 0 9 (m, 2 H) , 1 . 5 2 ( b s , 1H) , 1. 9 3 (m, 4H) , 2 . 2 9 (m, 4 H) , 2 . 5 8 - 2 . 6 8 (m, 7 H) , 4 . 6 4 (m, 1H) , 6 . 6 1 ( d , J = 3 . 6 Hz , 1H) , 7 . 5 8 ( d , J - 3 . 6 Hz , 1H) , 8 . 7 4 ( s , 1H) , 1 1. 3 1 (b r s , 1H) , 1 1 8 12 . 3 2 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 0 . 9 7 mi n LC / MS ( ES m/ z ; 3 9 3 [M+H] + 'H- NMR (DMS 0 - ) : 1 . 0 4 ( , 2 H) , 1 . 1 6 ( s , 6 H) , 1 . 2 8 ( b r s , 1H) , 1. 89 (m, 4 H) , 2 . 2 4 ( d , J = 5 . 4 Hz , 2H) , 2 . 5 1 (m, 2H) , 2 . 8 4 (m, 4H) , 4 . 6 1 (m, 1H) , 6 . 5 9 ( d , / = 3 . 3 Hz , 1H) , 7 . 5 9 ( d , J = 3 . 3 Hz , 1 1 9 1H) , 8 . 7 3 ( s , 1H) , 1 1 . 4 2 ( b r s , 1H) , 1 2 . 3 4 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 1 . 2 3 mi n LC/ MS ( ES D m/ z ; 3 8 2 [M+H] + - NMR (DMS 0 - ) : 1 . 0 5 (m, 2 H) , 1 . 5 1 ( b r s , 1H) , 1. 9 2 (m, 4H) , 2 . 18 (m, 5H) , 2 . 3 9 ( t , J = 6 . 3 Hz , 2 H) , 2 . 5 5 (m, 2H) , 3 . 4 7 ( d d , = 12 . 0 , 5 . 4 Hz , 2 H) , 4 . 2 8 ( t , / = 5 . 4 Hz , 1H) , 4 . 6 4 ( m, 1H) , 12 0 6 . 6 2 ( d , = 3 . 6 Hz , 1H) , 7 . 5 9 ( d , J = 3 . 6 Hz , 1H) , 8 . 7 3 ( s , 1H) , 1 1 . 3 7 ( b r s , 1H) , 1 2 . 3 4 ( b r s , 1H) . LC/ MS : c o n d i t i o n 3 , r e t e n t i o n t i me = 0 . 7 5 mi n LC/ MS ( ES m/ z ; 3 7 2 [M+H] + TABLE b 75 -NMR (D S0- ) : 0.99 (m, 2H), 1.56 (br s , 1H) , 1.89 (d, J = 10. 8 Hz, 2H) , 2 . 00 (d, J = 10. 8 Hz, 2H) , 2 . 30 (d, J = 3 . 9 Hz, 2H), 2.60 (m, 4H), 3.47 (dd, J = 12.0, 6 . 6 Hz, 2H) , 3.59 (s, 2H) , 4 . 3 1 (t, J = 5 . 4 Hz, 1H), 4.61 (m, 1H), 6 . 58 (d, / = 3 . 6 Hz, 1H), 121 7.21-7.35 (m, 5H) , 7.57 (d, = 3.6 Hz, 1H), 8.73 (s, 1H), 11.41 (br s , 1H) , 12. 33 (br s , 1H) . LC/MS: condition 3 , retention time = 1 . 14 min LC/MS(ESr) m/z; 448 [M+H] + -NMR (DM S( f ) : 0.85 (s, 2H) , 0.92 (s, 2H), 1.13 (m, 2H) , 1.28 (br s , 1H), 1.90 (m, 4H), 2.26 (m, 1H), 2.56 (m, 4H), 4.61 ( , 1H), 6.61 (d, = 3.6 Hz, 1H), 7.59 (d, = 3.6 Hz, 1H), 8.73 122 (s, 1H), 11.45 (br s , 1H), 12.32 (br s , 1H) . LC /M S - condition 3 , retention time = 1.88 min LC/MS(ESI +) m/z; 422 [M+H] + Ή -NMR (DMS 0- fi ) <5 : 1.09 (m, 2H) , 1.46 (br s , 1H), 1.92 (m, 4H), 2.35-2.43 ( , 9H) , 2.60 (m, 4H), 3.56 ( , 4H), 4.63 ( , 1H) , 6.61 12 3 (d, J = 3.6 Hz, 1H) , 7 . 59 (d, J = 3 . 6 Hz, 1H) , 8 . 73 (s, 1H) . LC/MS: condition 3 , retention time = 1.40 min LC/MS(ESI +) m/z; 427 [M+H] + LC/MS: condition 3 , retention time = 1.05 min 124 LC/MS(ESI +) m/z; 393 [M+H] + 'H-NMR (DM S0 - ) 0 . 04 (t, J = 4 . 2 Hz, 1H) , 0.3 5 (dd, J = 7 . 2 , 4 . 2 Hz, 1H), 0.98 (s, 3H) , 1.11 (s, 3H), 1 . 13 (m, 2H) , 1.46 (br s , 1H), 1.82 (dd, J = 7.2, 3.6 Hz, 1H), 1.93 (m, 5H), 2.41 (m, 2H) , 2.5 5 (m, 2H) , 4 . 64 (m, 1H) , 6 . 62 (d, J = 3 . 6 Hz, 1H) , 7 . 59 125 (d, J = 3.6 Hz, 1H), 8.73 (s, 1H), 11.37 (br s , 1H), 12.34 (br s , 1H). LC/MS: condition 3 , retention time = 1.37 min LC/MS(ESI +) m/z; 382 [M+H] + -NMR (DMS0- f ) 1.05-1.27 (m, 3H), 1.36-1.58 (m, 6H), 1.94 (m, 4H), 2.41 (s, 1H), 2.42 (d, J = 6.6 Hz, 2H) , 2.55 (m, 6H), 3 . 93 (br s , 2H) , 4.6 5 (m, 2H) , 6.6 3 (d, J = 3 . 6 Hz, 1H) , 7 . 60 (d, 126 J = 3 . 6 Hz, 1H) , 8 . 73 (s, 1H) . LC/MS: condition 3 , retention time = 1.35 min LC/MS(ESI +) m/z; 426 [M+H] + 'H-NMR (DMSO-^) : 1.16 (m, 2H) , 1.48 (br s , 1H), 1.92 (m, 4H) , 2.55 (m, 5H), 3.61 (d, = 6.0 Hz, 2H), 4.65 (m, 1H), 6.62 (d, J = 3 . 6 Hz, 1H), 7.59 (d, J = 3.6 Hz, 1H), 8.73 (s, 1H), 11. 34 127 (br s , 1H) , 12. 34 (br s , 1H) . LC/MS: condition 3 , retention time = 1.02 min LC/MS(ESI +) m/z; 353 [M+H] + Ή -NMR (DMS 0- ) : 1.07 (m, 2H) , 1.47 (m, 2H) , 1.56 (br s , 1H), 1.78 (d, / = 17. 4 Hz, 2H), 1.95 (m, 6H), 2.15 (d, J = 6.9 Hz, 2H), 2.21 (m, 1H), 2.55 (m, 2H) , 2.92 (d, / = 17.4 Hz, 2H) , 4.64 (m, 12 8 1H) , 6 . 62 (d, J = 3 . 6 Hz, 1H) , 7 . 59 (d, J = 3 . 6 Hz, 1H) , 8 . 73 (s, 1H), 11.42 (br s , 1H), 12.34 (br s , 1H) . LC/MS: condition 3 , retention time = 1.36 min LC/MS(ESI +) m/z; 450 [M+H] + TABLEb 76 -NMR (DMS0- f ) 1 . 10 (m, 2H) , 1 . 3 4 (br s , 1H) , 1. 89 (m, 4H) , 2. 35 (d, J = 6 . 6 Hz, 2H) , 2 . 5 5 (m, 2H) , 3. 1 1 ( d , = 8 . 4 Hz, 2H) , 3. 53 (d , J = 8. 4 Hz, 2H) , 4 . 6 1 (m, 1H) , 6. 60 (d, J = 3 . 6 Hz, 1H) , 6. 82 ( s , 1H) , 7. 59 (d, J = 3. 6 Hz, 1H) , 8 . 7 0 ( s , 1H) , 11. 3 7 (br 12 9 s , 1H) , 12 . 3 4 (br s , 1H) . LC/MS : c ondi t i on 3, r e t en t i on t i me = 1 . 2 0 mi n LC/MS (ES I +) m/z ; 4 3 8 [M+H] + LC/MS ( ES m/ z ; 436 [M-H] 'H-NMR (DMS0- ) : 1. 0 9 (m, 2H) , 1 . 5 1 (m, 2H) , 1. 74-1 . 8 4 (m, 4H) , 1. 9 2 (m, 4H) , 2 . 43 (d , J = 6 . 6 Hz, 2H) , 2 . 5 5 (m, 4H) , 3. 59 (ddd, / = 14 . 4 , 7 . 8 , 1. 2 Hz, 1H) , 3. 72 ( ddd , J = 14 . 4 , 7 . 8 , 1 . 2 13 0 Hz , 1H) , 3 . 8 5 (m, 1H) , 4 . 64 (m, 1H) , 6. 62 (d, J = 3 . 6 Hz , 1H) , 7. 59 ( d, J = 3 . 6 Hz , 1H) , 8 . 73 ( s , 1H) . LC/MS : c on d i t i on 3, ret ent i on t i me = 1 . 2 1 mi n LC/MS (ES I +) m/ z ; 39 8 [M+H] + LC/MS : c ondi t i on 3, ret e n t i on t i me = 1. 10 mi n 13 1 LC/MS (ES I +) m/ z ; 3 7 2 [M+H] + LC/MS : c ondi t i on 3, r e t e n t i on t i me = 1 . 2 5 mi n 13 2 LC/MS (ES I +) m/z ; 503 [M+H] + LC/MS (ES m/ z ; 50 1 [M-H] LC/MS : c ondi t i on 3, r e t en t i on t i me - 1 . 3 9 mi n 13 3 LC/MS ( ES I +) m/z ; 3 13 [M+H ] + Ή -NMR (DMS0 - f ) 1 . 19 (m, 2H) , 1. 4 2 (br s , 1H) , 1. 56 ( dd, J = 14. 1, 7. 5 Hz , 2 H) , 1. 80 (m, 2H) , 1 . 9 2 (m, 4H) , 2 . 55 (m, 2H) , 4 . 64 (m, 1H) , 6 . 6 2 (d , J - 3 . 6 Hz, 1H) , 7. 59 (d, J = 3. 6 Hz, 1H) , 13 4 8 . 73 ( s , 1H) . LC/MS : c ondi t i on 3, r e t en t i on t i me = 1 . 6 6 mi n LC/MS (ES I +) m/z ; 33 8 [M+H] + LC/MS : c on d i t i on 3 , r e t e n t i on t i me = 1. 8 0 mi n 13 5 | LC/MS ( ES I +) m/ z ; 463 [M+H] + LC/MS (ES I ) m/z ; 46 1 [M-H] LC/MS : c ondi t i on 3 , r e t e n t i on t i me = 1. 8 5 mi n 13 6 ILC/MS ( ES I +) m/z ; 4 10 [M+H] + LC/MS (ES I ) m/z ; 408 [M-H] LC/MS : c ondi t i on 3 , r e t e n t i on t i me = 2 . 13 mi n 13 7 ILC/MS (ES I +) m/z ; 324 [M+H] + LC/MS ( ES I ) m/ z ; 32 2 [M-H] LC/MS : c ondi t i on 3 , r e t en t i on t i me = 2 . 13 mi n 13 8 ILC/MS (ES I +) m/z ; 299 [M+H] + LC/MS (ES I ) m/ z ; 297 [M-H] LC/MS : c ondi t i on 3, r e t en t i on t i me = 2 . 4 9 mi n 13 9 ILC/MS (ES I +) m/z ; 36 7 [M+H] + LC/MS (ES I ) m/ z ; 36 5 [M-H] LC/MS : c ondi t i on 3, r e t e n t i on t i me = 1. 8 6 mi n 14 0 | LC/MS ( ES I +) m/ z ; 329 [M+H] + LC/MS (ES I ) m/ z ; 32 7 [M-H] TABLEb 77 Pharmacological assay Now, a pharmacological assay of the tricyclic pyridine compounds of the present invention will be described. ASSAY EXAMPLE1 1. Enzyme assay JAK1 , JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer Co., Ltd.(PE)) was used. Dilute solutions of compounds and enzymes in assay buffer (50 m HEPES pH7.5, 1 mM EGTA, 1 mM MgCI2, 2 mM DTT, 0.01 % Tween20) were dispensed into wells of a 384-well black plate. After 5 minutes of preincubation, dilute solutions of the substrate and ATP (adenosine triphosphate) were added at a final concentration of 100 , and the plate was incubated at room temperature for 2 hours. After addition of a termination reagent containing EDTA (ehylenediamine tetraacetic acid) at a final concentration of 10 mM, LANCE Eu-W1024 Anti-phosphotyrosine (PT66) (manufactured by PE) was added, and after 1 hour of incubation, the fluorescences were measured with ARVO-HTS. From the plot of logarithm of a compound concentration and inhibitory activity, the IC5owas calculated. The results of JAK3, JAK1 , JAK2 and Tyk2 enzyme assays of the compounds of Synthetic Examples' 3 are shown in Tables'378 to 8 1. "* " in the Tables indicates IC 0 > 1 . TABLEb 78 Exb. I C 5 0 ( M ) I c 5 0 ( M ) No. J A K 3 J A K 1 1 2 . 0 0 . 3 8 2 1 . 2 0 . 3 3 3 0 . 2 2 0 . 0 1 7 4 0 . 0 6 5 0 . 0 3 0 6 a 0 . 3 1 0 . 0 2 7 6 b 0 . 2 5 0 . 1 9 7 0 . 0 0 3 2 0 . 0 0 1 7 8 0 . 0 4 1 0 . 0 2 6 9 0 . 0 1 0 0 . 0 0 4 0 1 0 0 . 0 3 4 0 . 0 0 8 1 1 1 0 . 0 3 4 0 . 0 1 2 1 2 1 . 3 0 . 1 3 1 3 1 . 3 0 . 0 4 2 1 6 0 . 1 1 0 . 0 3 8 1 7 0 . 6 9 0 . 0 2 7 1 8 1 . 2 0 . 0 4 5 1 9 2 . 2 0 . 2 9 2 0 0 . 5 1 0 . 2 8 TABLEb 79 Exb. I C 5 0 ( M ) I 5 ( No. J A K 2 T Y K 2 1 2 . 2 4 . 1 2 1 . 9 3 . 1 3 0 . 1 5 0 . 1 3 4 0 . 1 0 * 6 a 0 . 0 4 6 0 . 6 3 6 b 0 . 3 8 3 . 9 7 0 . 0 0 4 0 . 0 6 0 8 0 . 0 7 5 1 . 5 9 0 . 0 0 9 4 0 . 1 5 1 0 0 . 0 3 9 1 . 6 1 1 0 . 0 3 3 0 . 4 4 1 2 0 . 4 6 * 1 "3 0 . 5 6 * 1 6 0 . 0 8 8 0 . 5 7 1 7 0 . 0 2 0 0 . 0 9 3 1 8 0 . 1 2 0 . 2 5 1 9 1 . 3 1 . 5 2 0 1 . 6 0 . 7 6 TABLEb 80 I C I C „ I Ex 5 ( M ) ( M ) ( / M ) ( M ) No. J A K 1 J A K 2 J A K 3 T Y K 2 2 1 0 . 5 6 1 . 3 0 . 8 2 * 2 2 0 . 3 3 o . 2 8 0 . 3 7 2 3 0 . 0 3 5 0 . 2 2 0 . 1 0 * 2 4 0 . 0 2 5 0 . 7 4 0 . 5 6 2 5 0 . 0 5 5 0 . 2 3 0 . 0 7 0 0 . 7 0 2 6 0 . 0 0 6 6 0 . 0 4 8 0 . 1 0 0 . 4 1 2 7 0 . 0 1 8 0 . 0 4 0 0 . 0 4 2 0 . 4 3 2 8 0 . 3 1 2 . 0 2 . 3 7 . 9 2 9 0 . 0 1 5 0 . 1 9 0 . 2 0 0 . 4 1 3 0 0 . 1 8 * * 3 1 0 . 2 4 * * * 3 2 0 . 0 8 1 0 . 7 7 0 . 5 5 3 3 0 . 0 0 9 8 0 . 1 2 0 . 0 9 6 0 . 4 0 3 4 0 . 1 6 0 . 8 6 * 3 5 0 . 0 1 8 0 . 0 8 9 o . 1 1 0 . 9 9 3 6 0 . 0 0 0 5 8 0 . 0 0 3 2 0 . 0 0 3 8 0 . 0 5 3 7 0 . 0 0 1 5 0 . 0 0 6 1 0 . 0 0 2 8 0 . 0 6 3 8 0 . 0 0 4 6 0 . 0 2 8 0 . 0 3 1 0 . 2 7 3 9 0 . 0 4 8 0 . 1 5 0 . 1 8 * 4 0 0 . 0 8 8 0 . 5 0 0 . 2 6 * 4 1 0 . 2 0 0 . 2 9 0 . 3 2 4 2 0 . 0 1 6 0 . 1 5 0 . 0 9 3 * 4 3 0 . 0 3 0 0 . 1 6 0 . 1 5 0 . 5 1 4 4 0 . 0 1 4 0 . 1 5 0 . 0 5 7 0 . 8 4 4 5 0 . 0 1 2 0 . 0 3 8 0 . 0 4 0 0 . 4 4 4 6 0 . 0 3 3 0 . 2 1 0 . 0 4 6 * 4 7 0 . 1 1 0 . 2 3 0 . 1 1 * 4 8 a 0 . 1 4 1 . 0 * * 4 8 b 0 . 0 9 4 0 . 4 6 0 . 3 6 4 9 0 . 0 0 7 9 0 . 1 0 * * 5 0 0 . 0 0 8 7 * * * 5 1 0 . 0 0 5 0 0 . 3 6 * 5 2 0 . 0 2 1 * * 5 3 0 . 0 0 7 4 0 . 0 4 8 0 . 0 4 7 0 . 0 4 5 4 0 . 0 0 3 0 0 . 0 3 2 0 . 4 7 0 . 3 2 5 5 0 . 0 0 1 2 0 . 0 2 0 . 2 1 0 . 2 2 5 6 0 . 0 1 9 0 . 2 4 * * 5 7 0 . 0 1 3 0 . 2 5 * 0 . 8 6 5 8 0 . 0 3 7 0 . 5 7 * 5 9 0 . 0 4 2 0 . 1 6 2 . 1 4 . 3 6 0 0 . 3 5 0 . 4 8 * * 6 1 0 . 0 7 7 0 . 2 2 5 . 4 3 . 6 6 2 0 . 0 5 4 0 . 3 6 * 0 . 1 2 * 0 . 0 1 2 0 . 0 2 0 0 . 2 2 0 . 1 7 0 . 1 9 0 . 1 1 9 . 5 2 . 9 0 . 0 8 0 0 . 1 4 0 . 9 9 0 . 5 0 2 . 4 9 . 1 * 0 . 0 3 6 0 . 4 6 * 0 . 3 0 0 . 1 6 * 0 . 0 0 1 9 0 . 0 3 6 0 . 4 6 0 . 3 8 0 . 0 0 9 8 0 . 3 3 * 0 . 8 8 0 . 0 5 3 * 0 . 0 0 5 0 . 0 6 9 0 . 8 6 0 . 8 4 0 . 0 0 8 9 0 . 0 6 2 * 0 . 0 2 8 0 . 4 5 * 0 . 0 0 7 9 0 . 0 7 7 1 . 0 * 0 . 0 0 3 9 0 . 0 6 6 * * 0 . 0 0 0 4 0 0 . 0 0 6 3 0 . 0 9 4 0 . 1 2 0 . 0 0 1 6 0 . 0 2 0 0 . 3 4 0 . 2 4 0 . 0 0 0 0 8 4 0 . 0 0 1 6 0 . 0 3 1 0 . 0 3 4 0 . 0 0 2 1 0 . 0 2 1 0 . 3 2 0 . 3 2 0 . 0 0 5 2 0 . 0 4 3 0 . 6 2 0 . 8 1 0 . 0 0 0 7 5 0 . 0 1 7 0 . 1 3 0 . 3 3 0 . 0 7 5 0 . 6 8 * * 0 . 0 4 3 * * 0 . 0 2 5 0 . 3 8 TABLEb 8 1 M 8 8 0 . 0 8 2 * 8 9 0 . 0 1 1 * * 9 0 0 . 2 2 * 9 1 0 . 0 8 3 * 9 2 0 . 0 9 7 * 9 3 0 . 3 7 * 9 4 0 . 0 3 4 * 0 . 9 3 9 5 0 . 0 1 7 0 . 3 4 9 6 0 . 0 1 9 9 7 0 . 2 3 * 9 8 0 . 0 2 1 0 . 6 7 * 9 9 0 . 0 6 9 * * * 1 0 0 0 . 0 0 6 6 0 . 0 4 6 * 0 . 4 5 1 0 1 0 . 0 1 5 0 . 4 0 * 0 . 4 6 1 0 2 0 . 0 0 2 8 0 . 0 8 0 0 . 3 2 0 . 0 9 1 0 3 0 . 0 0 4 3 0 . 0 8 3 * 0 . 1 2 1 0 4 0 . 0 3 4 0 . 0 4 6 0 . 3 8 0 . 3 8 1 0 5 3 . 2 * * 1 0 6 0 . 0 4 7 0 . 2 5 0 . 6 1 0 . 3 8 1 0 7 0 . 3 1 0 . 6 0 0 . 4 1 1 0 8 0 . 3 7 * * 1 0 9 0 . 9 2 * 1 1 0 0 . 4 2 * * 1 1 1 0 . 4 4 * 1 1 2 0 . 0 0 2 6 0 . 2 5 * . 0 3 1 1 3 0 . 0 0 3 3 0 . 2 2 * 0 . 1 9 1 1 4 0 . 0 1 0 0 . 2 3 0 . 5 2 0 . 2 5 1 1 5 0 . 0 3 0 * * * 1 1 6 0 . 0 0 1 2 0 . 0 1 2 0 . 0 3 6 0 . 0 3 1 1 7 0 . 0 3 0 0 . 8 5 0 . 8 0 1 1 8 0 . 0 2 7 0 . 3 4 * 1 1 9 0 . 0 3 9 * 1 2 0 0 . 0 2 9 0 . 7 3 * * 1 2 1 0 . 0 0 7 4 0 . 2 1 * 1 2 2 0 . 0 0 3 2 0 . 4 9 * 1 2 3 0 . 1 5 * * * 1 2 4 0 . 0 2 5 0 . 6 1 * 1 2 5 0 . 0 2 0 0 . 4 3 * 1 2 6 0 . 0 2 8 0 . 3 6 * * 1 2 7 0 . 0 0 5 5 0 . 1 9 * 0 . 1 2 1 2 8 0 . 0 6 7 * 1 2 9 0 . 0 0 7 9 0 . 1 8 0 . 8 1 0 . 3 6 1 3 0 0 . 0 4 8 * 1 3 1 0 . 0 3 6 * 0 . 7 8 1 3 2 0 . 0 0 9 2 0 . 3 2 * 1 3 3 0 . 0 1 2 0 . 2 7 0 . 4 1 1 3 4 0 . 0 0 2 0 0 . 0 2 5 0 . 8 1 0 . 0 3 1 3 5 0 . 0 0 4 9 0 . 0 6 0 0 . 5 0 0 . 3 3 1 3 6 0 . 0 0 3 2 0 . 0 5 1 0 . 7 5 0 . 3 2 1 3 7 0 . 0 5 7 * 0 . 9 1 * 1 3 8 0 . 0 4 0 0 . 4 2 0 . 5 1 1 3 9 0 . 1 0 . 7 7 * 1 4 0 0 . 0 1 8 0 . 2 5 0 . 7 8 0 . 3 6 1 4 1 0 . 0 4 6 0 . 2 3 0 . 8 0 0 . 6 0 1 4 2 0 . 3 4 * * * 1 4 3 0 . 0 7 3 0 . 8 5 * 1 4 4 0 . 0 5 3 0 . 7 0 * * 1 4 5 0 . 0 4 7 0 . 6 9 * 1 4 6 0 . 2 1 * * 1 4 7 0 . 0 9 8 0 . 8 2 * * 1 4 8 0 . 4 4 * * 1 4 9 0 . 2 7 * * 1 5 0 0 . 0 9 2 0 . 2 3 0 . 6 4 * 1 5 1 0 . 2 1 * 1 5 2 0 . 0 6 7 0 . 2 1 0 . 4 8 * 1 5 3 0 . 3 3 * * 1 5 4 0 . 2 9 * 1 5 5 0 . 0 0 2 1 0 . 0 5 5 0 . 2 0 0 . 1 4 The tricyclic pyridine compounds of the present invention have favorable inhibitory activity against JAKs as shown above. ASSAY EXAMPLE 2. Signal assay in human whole blood To be a effective pharmaceutical compound for the target diseases of the present invention, especially for rheumatoid arthritis, it is more favorable that the compounds indicate excellent inhibitory activity against JAKs in human whole blood. Inhibitory activity against JAKs in human whole blood can be assessed by, for example, STAT phosphorylation assay in human whole blood as described below. Compounds are added at the various concentrations to human whole blood which is collected from healthy volunteers and preincubated for 30 minutes. Next, cytokine such as IL-2 or IL-6 is added to the mixture and incubated for 15 minutes. Cytokines can be purchased, for example, from PeproTech Inc. Cytokines are added to mixture at 100 ng/mL as final concentration. The mixture including the blood cells are hemolyzed, fixed, permeabilized, washed, and resuspended in stain buffer. BD Cytofix/Cytoperm® solution (manufactured by Becton, Dickinson and Company (BD)), for example, can be used to hemolyze, fix, and permeabilize. Staining buffer (manufactured by BD), for example, can be used as stain buffer according to each protocol issued by BD. Fluorescence-labeled anti-phosphorylated STAT antibody and fluorescence-labeled anti-CD3 antibody are added to the cell suspension and incubated for 30 minutes. Then, cells are washed and resuspended in stain buffer. Fluorescence-labeled anti-phosphorylated STAT antibody and fluorescence-labeled anti-CD3 antibody can be purchased, for example from BD, and final concentration of antibodies can be determined according to each protocols issued by BD. Fluorescence intensity of fluorescence-labeled cells in cell suspension is detected by flow-cytometory. Because the detected fluorescence intensity is proportional to the concentration of the phosphorylated STAT protein in CD3 positive cells, inhibitory activity against STAT phosphorylation by the compounds can be calculated from the ratio between the above mentioned fluorescence intensity and the blank fluorescence intensity which is measured simultaneously without the compounds. From the plot of logarithm of the compound concentrations and the inhibitory activities, the IC50 value can be calculated. ASSAY EXAMPLE b 3. Inhibition of proliferation of erythro-leukemic cell line The inhibitory activity of the tricyclic pyridine compounds of the present invention on cell proliferation mediated by JAK signal can be assayed using a human erythroleukemic cell line, TF-1 . TF-1 cells can be purchased from ATCC (American Type Culture Collection). TF- 1 cells can be expanded in RPMI1640 media containing 5% FBS and 1 ng/mL GM-CSF (Granulocyte Macrophage Colony-Stimulating Factor) using a CO2 incubator (5% CO2, 37°C). At the assay, TF-1 cells washed by PBS (Phosphate Buffered Saline) are resuspended in RPMI1640 media containing 5% FBS, and dispensed in 96-well culture plate at 1 x 04 cells/well. Compounds at various concentrations are added to the cells and preincubated for 30 minutes, and then cytokine such as IL-4 or IL-6 is added to the cells. Culture plates are incubated using a C0 2 incubator (5% C0 2, 37°C) for 3 days. Cell proliferation can be assayed using WST-8 reagent (Kishida Chemical Co., Ltd.) according to instructions by the manufacturer. The formazan pigment is generated by the addition of WST-8 reagent solution to each well of the culture plates and the subsequent incubation in a C0 2 incubator (5% C0 2, 37°C) for 4 hours, and then detected by measuring the absorbance at 450 nm with a microplate reader. From the plot of logarithm of the compound concentrations and the inhibitory activities, the IC50 value can be calculated. Now, examples of formulations of tricyclic pyrimidine compounds represented by the formula (la) and tricyclic pyridine compounds represented by the formula (l ) of the present invention (hereinafter referred to collectively as compounds represented by the formula (I)) will be shown. FORMULATION EXAMPLE 1 A granule preparation containing the following ingredients is prepared. Ingredients Compound represented by the formula (I) 0 mg Lactose 700 mg Corn Starch 274 mg HPC-L 16 mg Total 1000 mg A compound represented by the formula (I) and lactose are sifted through a 60- mesh sieve. Corn starch is sifted though a 120-mesh sieve. They are mixed in a Vtype blender. The powder mixture is kneaded with a low-viscosity hydroxypropylcellulose (HPC-L) aqueous solution, granulated (extrusion granulation, die size 0.5-1 mm) and dried. The resulting dry granules are sifted through a shaking sieve (12/60 mesh) to obtain a granule preparation. FORMULATION EXAMPLE 2 A powder preparation for capsulation containing the following ingredients is prepared. Ingredients Compound represented by the formula (I) 0 mg Lactose 79 mg Corn Starch 10 mg Magnesium Stearate 1 mg Total 00 mg A compound represented by the formula (I) and lactose are sifted through a 60- mesh sieve. Corn starch is sifted though a 120-mesh sieve. They are mixed with magnesium stearate in a V-type blender. The 10% powder is put in hard gelatin capsules No. 5, 100 mg each. FORMULATION EXAMPLE 3 A granule preparation for capsulation containing the following ingredients is prepared. Ingredients Compound represented by the formula (1) 15 mg Lactose 90 mg Corn Starch 42 mg HPC-L 3 mg Total 50 mg A compound represented by the formula (I) and lactose are sifted through a 60- mesh sieve. Corn starch is sifted though a 120-mesh sieve. They are mixed in a Vtype blender. The powder mixture is kneaded with a low-viscosity hydroxypropylcellulose (HPC-L) aqueous solution, granulated and dried. The resulting dry granules are sifted through a shaking sieve (12/60 mesh). The granules are put in hard gelatin capsules No. 4 , 150 mg each. FORMULATION EXAMPLE 4 A tablet preparation containing the following ingredients is prepared. Ingredients Compound represented by the formula (I) 10 mg Lactose 90 mg Microcrystalline cellulose 30 mg Magnesium Stearate 5 mg CMC-Na 15 mg Total 150 mg A compound represented by the formula (I), lactose, microcrystalline cellulose and CMC-Na (carboxymethylcellulose sodium salt) are sifted through a 60-mesh sieve and mixed. The powder mixture is mixed with magnesium stearate to give a bulk powder mixture. The powder mixture is compressed directly into 150 mg tablets. FORMULATION EXAMPLE 5 An intravenous preparation is prepared as follows. Compound represented by the formula (I) 100 mg Saturated Fatty Acid Glyceride 000 ml Solutions having the above-mentioned composition are usually administered to a patient intravenously at a rate of 1 ml per 1 minute. INDUSTRIAL APPLICABILITY The compounds of the present invention have excellent JAK inhibitory activities and are useful for prevention or treatment of autoimmune diseases, especially rheumatoid arthritis, inflammatory diseases and allergic diseases. CLAI M S A compound represented by the formula (la) [wherein the ring A a is represented by the following formula (lla-1) or the formula (lla-2): ( I I a-l ) ( I I a-2 ) (wherein T1a is a nitrogen atom or C R 4 a , U1a is a nitrogen atom or C R5 a , T a is a single bond or C R 7aR a , and E2a is an oxygen atom or a sulfur atom), Xa is a nitrogen atom or C R 9a , Ya is C R 10a , R a is a hydrogen atom, a halogen atom, a C -6 alkyl group or a Ci- 6 haloalkyl group, the ring Ba is a C3-11 cycloalkane, a C 3 -n cycloalkene (a ring-constituting methylene group of the C 3 - cycloalkane and the C 3 - cycloalkene may be replaced by a carbonyl group), a 3 to 14-membered non-aromatic heterocycle, a C 6 -14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L a is a single bond, a C -6 alkylene group, a C 2-6 alkenylene group or a C 2 -6 alkynylene group (the C -6 alkylene group, the C 2-6 alkenylene group and the C 2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L2 a is a single bond, a C -6 alkylene group, a C 2 -6 alkenylene group, a C 2 -6 alkynylene group (the C -6 alkylene group, the C-2-6 alkenylene group and the C 2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), =C(R 1 a ) - (wherein R 15a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L2 a is a double bond) or =C(R 1 a)-CH 2 - (wherein R 15a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L a is a double bond), L3 a is a single bond or represented by any of the following formulae (llla- 1) to (lll a-20) and the formula (Xlll a) : ( IIIa-12 ) ( IIIa-13 ) ( -14 ) ( IIIa-15 ) ( IIIa-16 ) ( IIIa-17 ) ( IIIa ( IIIa-19 ) ( IIIa-20 ) ( XIIIa ) (wherein E is an oxygen atom, a sulfur atom or NR a) , when L3a is a single bond, R a is a hydrogen atom, a halogen atom, an azido group, a C3-11 cycloalkyl group, a 3 to 14-membered non-aromatic heterocyclyl group, a C6 -14 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 14-membered partially saturated aromatic cyclic group or a 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3-11 cycloalkyl group, the 3 to 14-membered nonaromatic heterocyclyl group, the Ce-14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 14-membered partially saturated aromatic cyclic group and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of the substituent set V4a, substituent set V 9a and C i -6 alkyl groups (the C -6 alkyl groups are substituted with a C -6 alkoxycarbonylamino group (the C -6 alkoxycarbonylamino group is unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms))), when L3a is not a single bond, R a is a hydrogen atom, a C -6 alkyl group, a C2 -6 alkenyl group, a C2 -6 alkynyl group (the C -6 alkyl group the C 2 -6 alkenyl group and the C 2-e alkynyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V6a and the substituent set V a) , a C3- cycloalkyl group, a 3 to 14-membered non-aromatic heterocyclyl group, a C-6-14 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 14-membered partially saturated aromatic cyclic group or a 8 to 14-membered aromatic ringcondensed alicyclic hydrocarbon group (the C3.11 cycloalkyl group, the 3 to 14- membered non-aromatic heterocyclyl group, the C e-14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 14-membered partially saturated aromatic cyclic group and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one o r more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) , na is 0, 1 or 2 , R3a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a sulfamoyl group, a phosphono group, a phosphonooxy group, a sulfo group, a sulfoxy group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C i - alkyl group, a C i -6 haloalkyl group, a C3-11 cycloalkyl group, a C 2 -6 alkenyl group, a C 2-6 haloalkenyl group, a C i -6 alkoxy group, a C -6 haloalkoxy group, a C -6 alkylthio group, a C 1-6 haloalkylthio group, a C -6 alkylcarbonyl group, a C -6 haloalkylcarbonyl group, a - 6 alkylsulfonyl group, a C -6 haloalkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono -Ci -6 alkylamino group, a di-Ci -6 alkylamino group, a mono-Ci -6 alkylaminocarbonyl group, a di-Ci -e alkylaminocarbonyl group or a C i -6 alkylcarbonylamino group (when na is 2 , R a's may be identical or different), each of R a, R5a, R a and R8a is independently a hydrogen atom, a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a C i -6 alkyl group, a C 2-6 alkenyl group, a C i -6 alkoxy group, a C i -6 alkylthio group, a C -6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a mono-Ci -6 alkylamino group, a di-Ci -6 alkylamino group (the C - alkyl group, the C 2-6 alkenyl group, the C 1-6 alkoxy group, the C 1-6 alkylthio group, the C 1- alkylcarbonyl group, the C 1-6 alkylsulfonyl group, the mono-Ci - alkylamino group and the di-Ci -6 alkylamino group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3a) , a C 1-6 alkoxycarbonyl group, a C 3 - 11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C 6 -14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3-n cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C 6 - 14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , R a is a hydrogen atom, a C -6 alkyl group, a C 2-6 alkenyl group, a Ci- 6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-Ci -6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group (the C i -6 alkyl group, the C 2 -6 alkenyl group, the C -6 alkylcarbonyl group, the C 1-6 alkylsulfonyl group, the C i -6 alkoxycarbonyl group, the mono-Ci-6 alkylaminocarbonyl group and the di-Ci -6 alkylaminocarbonyl group are unsubstituted or substituted with one or more identical o r different substituents independently selected from the substituent set V a) , a C3.11 cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a C - 14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3 .n cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C 6 -14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , each of R 9a and R 10a is independently a hydrogen atom, a halogen atom, a cyano group, a carbamoyl group, a C -6 alkyl group, a -6haloalkyl group, a C 3-n cycloalkyl group, a C- -6 alkoxy group, a -6haloalkoxy group, a 1-6 alkylthio group, a C -6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C e- 4 aryl group or a 5 to 10-membered aromatic heterocyclyl group, R a is a hydrogen atom, a hydroxy group, a cyano group, a nitro group, a C -6 alkyl group or a C -6 alkoxy group, each of R 1 a , R 13a and R 14a is independently a hydrogen atom, a C -6 alkyl group, a C -6 haloalkyl group (the C -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a, the substituent set V8a and the substituent set V9a) , a C 3- cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C 6- i 4 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 14-membered partially saturated aromatic cyclic group or a 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group (the C 3. cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C 6 -14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 14-membered partially saturated aromatic cyclic group and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a and the substituent set V9a) , the substituent set V a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, - alkyl groups, C i -6 haloalkyl groups, C 3-n cycloalkyl groups, C 2 -6 alkenyl groups, C 2 -6 haloalkenyl groups, C i -6 alkoxy groups, C i -6 haloalkoxy groups, Ci- 6 alkylthio groups, Ci- 6 haloalkylthio groups, C -6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, C i -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, Ci- 6 alkoxycarbonyl groups, 3 to 11- membered non-aromatic heterocyclyl groups, mono-d-6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di-C -6 alkylaminocarbonyl groups and C -6 alkylcarbonylamino groups, the substituent set V2a consists of the groups in the substituent set V a and C e-1 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 6-i 4 aryl groups and 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , the substituent set V3a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkoxy groups, C -6 haloalkoxy groups, C -6 alkylthio groups, C i -6 haloalkylthio groups, C -6 alkylcarbonyl groups, C i -6 haloalkylcarbonyl groups, C i -6 alkylsulfonyl groups, C i -6 haloalkylsulfonyl groups, C i -6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C i -6 alkylcarbonylamino groups, C 3- cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C-6-14 aryl groups and 5 to 10- membered aromatic heterocyclyl groups (the C 3-11 cycloalkyl groups, the 3 to 11- membered non-aromatic heterocyclyl groups, the C e- aryl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) the substituent set V a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C- -6 alkyl groups, C2. alkenyl groups, C 1-6 alkoxy groups, -6alkylthio groups, C -6 alkylcarbonyl groups, C -6 alkylsulfonyl groups, C i -6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di- C-1 -6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups (the C -6 alkyl groups, the C-2-6 alkenyl groups, the C -6 alkoxy groups, the C i -6 alkylthio groups, the C -6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the C i -6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the Ci- 6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , C3.11 cycloalkyl groups, 3 to 1 1-membered non-aromatic heterocyclyl groups, C e- 4 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 3 -n cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C e- aryl group and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , the substituent set V5a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C 1-6 alkoxy groups, C -6 alkylthio groups, C 1-6 alkylcarbonyl groups, C 1-6 alkylsulfonyl groups, C 1-6 alkoxycarbonyl groups, mono-Ci- 6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C i -6 alkylcarbonylamino groups, C3-11 cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C e-1 aryl group and 5 to 10-membered aromatic heterocyclyl groups (the C -6 alkoxy groups, the C i -6 alkylthio groups, the C -6 alkylcarbonyl groups, the C 1-6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci 6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di- C 1-6 alkylaminocarbonyl groups, the C i -6 alkylcarbonylamino groups, the C3.11 cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C e-14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , the substituent set V6a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkoxy groups, C i -6 alkylthio groups, C 1-6 alkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C -e alkylcarbonylamino groups (the C -6 alkoxy groups, the Ci- 6 alkylthio groups, the C -6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the C - alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci- 6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the C alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V ) , C 3. cycloalkyl groups, 3 to -membered non-aromatic heterocyclyl groups, C-6-14 aryl groups, 5 to 10-membered aromatic heterocyclyl groups, 8 to 14-membered partially saturated aromatic cyclic groups and 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups (the C 3-11 cycloalkyl groups, the 3 to 11-membered nonaromatic heterocyclyl groups, the C-6-14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups, the 8 to 14-membered partially saturated aromatic cyclic groups and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) , the substituent set V8a consists of C 3- 11 cycloalkyl groups, 3 to 11 -membered nonaromatic heterocyclyl groups (the C 3-11 cycloalkyl groups and 3 to 11-membered nonaromatic heterocyclyl groups are substituted with one or more identical o r different substituent independently selected from the substituent set V2a) , 8 to 14-membered partially saturated aromatic cyclic groups and 8 to 14-membered aromatic ringcondensed alicyclic hydrocarbon groups (the 8 to 14-membered partially saturated aromatic cyclic groups and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups are unsubstituted or substituted with one or more identical o r different substituents independently selected from the substituent set V2a) , and the substituent set V9a consists of mono -Ci- 6 alkylaminosulfonyl groups, di-Ci -6 alkylaminosulfonyl groups, -6 alkylsulfonylamino groups, C -6 alkoxycarbonylamino groups (the mono -Ci -6 alkylaminosulfonyl groups, the di-Ci -6 alkylaminosulfonyl groups the C -6 alkylsulfonylamino groups and the C i -6 alkoxycarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3a) , C3-6 cycloalkoxy groups, C3-6 cycloalkylamino groups, C3-6 cycloalkylthio groups, C3 -6 cycloalkylcarbonyl groups and C3-6 cycloalkylsulfonyl groups (the C3-6 cycloalkoxy groups, the C3 - 6 cycloalkylamino groups, the C3-6 cycloalkylthio groups, the C3-6 cycloalkylcarbonyl groups and the C3-6 cycloalkylsulfonyl groups are unsubstituted or substituted with one or more identical o r different substituents independently selected from the substituent set V2a)], a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. aim 1, which is represented by the formula (la) : [wherein the ring Aa is represented by the following formula (ll a-1) or the formula (ll a-2): ( I I a-l ) ( I I a-2 ) (wherein T a is a nitrogen atom or CR4a, U1a is a nitrogen atom or a CR a, T a is a single bond or CR7aR a, E a is an oxygen atom or a sulfur atom), Xa is a nitrogen atom or CR9a, Ya is CR 0a, R1a is a hydrogen atom, a halogen atom, a C -6 alkyl group or a C1-6 haloalkyl group, the ring Ba is a C3-n cycloalkane, a C3-11 cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a C6-i 4 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L a is a single bond, a C1-6 alkylene group, a C2 -6 alkenylene group or a C2-6 alkynylene group (the C -6 alkylene group, the C2 -6 alkenylene group and the C2 -6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L a is a single bond, a C -6 alkylene group, a C2 -6 alkenylene group or a C2 -6 alkynylene group (the C -6 alkylene group, the C2-6 alkenylene group and the C2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L3a is a single bond or represented by any of the following formulae (lll a-1) to (lll -20) ( III a-3 ) ( IIIa-4 ) ( III a-5 ) ( - ) ( III a-7 ) ( IIIa-8 ) ( IIIa-9 ) ( III O) (  ( -12 ) ( IIIa-13 ) ( III a-14 ) ( III a-15 ) ( III a-16 ) 1a 14a (wherein E a is an oxygen atom, a sulfur atom or NR11a) , when L3a is a single bond, R2a is a hydrogen atom, a halogen atom, a C3-11 cycloalkyl group, a 3 to -membered non-aromatic heterocyclyl group, a C6 - 14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3-n cycloalkyl group, the 3 to 11- membered non-aromatic heterocyclyl group, the C6-14 aryl group and the 5 to 10- membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a) , when L3a is not a single bond, R a is a hydrogen atom, a C-i-6 alkyl group, a C2 -6 alkenyl group (the C -6 alkyl group and the C-2-6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5a) , a C3- cycloalkyl group, a 3 to 1-membered non-aromatic heterocyclyl group, a C6 - 14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3- cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the Ce- aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a) , na is 0 , 1 or 2, R a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a sulfamoyl group, a phosphono group, a phosphonooxy group, a sulfo group, a sulfoxy group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C -6 alkyl group, a C -6 haloalkyl group, a C3-11 cycloalkyl group, a C2 -6 alkenyl group, a C-2-6 haloalkenyl group, a C -6 alkoxy group, a Ci-6 haloalkoxy group, a C1-6 alkylthio group, a C 1-6 haloalkylthio group, a C-| .6 alkylcarbonyl group, a -6 haloalkylcarbonyl group, a Ci- 6 alkylsulfonyl group, a C -6 haloalkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-C -6 alkylamino group, a di-C- -6 alkylamino group, a mono-C- -6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group or a C -6 alkylcarbonylamino group (when na is 2, R3a's may be identical or different), each of R4a, R5a, R a and R8a is independently a hydrogen atom, a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a C-i -6 alkyl group, a C 2-6 alkenyl group, a C- -6 alkoxy group, a C i -6 alkylthio group, a C -6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a mono-C -6 alkylamino group, a di-Ci -6 alkylamino group (the C -6 alkyl group, the C 2 -6 alkenyl group, the C -6 alkoxy group, the C -6 alkylthio group, the Ci- 6 alkylcarbonyl group, the C 1-6 alkylsulfonyl group, the mono-Ci -6 alkylamino group and the di-C -6 alkylamino group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , a Ci- 6 alkoxycarbonyl group, a C 3 - cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a C-6-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3-n cycloalkyl group, the 3 to 1 1-membered non-aromatic heterocyclyl group, the C 6 -i 4 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , R6a is a hydrogen atom, a Ci- alkyl group, a C 2 -6 alkenyl group, a C -6 alkylcarbonyl group, a C 1-6 alkylsulfonyl group, a Ci- 6 alkoxycarbonyl group, a mono-Ci -6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group (the C -6 alkyl group, the C 2 -6 alkenyl group, the Ci- 6 alkylcarbonyl group, the C -6 alkylsulfonyl group, the C 1-6 alkoxycarbonyl group, the mono-Ci -6 alkylaminocarbonyl group and the di-Ci-6 alkylaminocarbonyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3a) , a C 3 -n cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C 6 -14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3 -n cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C 6- i 4 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , each of R9a and R10a is independently a hydrogen atom, a halogen atom, a cyano group, a carbamoyl group, a C -6 alkyl group, a C i -6 haloalkyl group, a C 3-n cycloalkyl group, a C 1-6 alkoxy group, a C 1-6 haloalkoxy group, a C -6 alkylthio group, a Ci- 6 alkylcarbonyl group, a C 1-6 alkylsulfonyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C e-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group, R11a is a hydrogen atom, a hydroxy group, a cyano group, a nitro group, a C -6 alkyl group or a C 1-6 alkoxy group, each of R a, R13a and R1 a is independently a hydrogen atom, a C 1-6 alkyl group or a C i - 6 haloalkyl group (the C 1-6 alkyl group and the C 1-6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , the substituent set V1a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkyl groups, C -6 haloalkyl groups, C 3 -n cycloalkyl groups, C 2-6 alkenyl groups, C -6 haloalkenyl groups, C -6 alkoxy groups, C -6 haloalkoxy groups, C -6 alkylthio groups, d . 6 haloalkylthio groups, C -6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, 3 to 11- membered non-aromatic heterocyclyl groups, mono-Ci-6 alkylamino groups, di-C -6 alkylamino groups, mono-C-i -6 alkylaminocarbonyl groups, di-C -6 alkylaminocarbonyl groups and C -6 alkylcarbonylamino groups, the substituent set V2a consists of the groups in the substituent set V1a , C-6-14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 6 - 4 aryl group and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) the substituent set V3a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkoxy groups, -6haloalkoxy groups, C -6 alkylthio groups, -6haloalkylthio groups, C i-6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, d-6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, d -6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C i-6 alkylcarbonylamino groups, C 3-n cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6 -14 aryl groups and 5 to 10- membered aromatic heterocyclyl groups (the C 3- cycloalkyl groups, the 3 to 11- membered non-aromatic heterocyclyl groups, the C 6 -14 aryl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , the substituent set V4a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkyl groups, C 2 -6 alkenyl groups, C 1-6 alkoxy groups, d -6 alkylthio groups, C 1-6 alkylcarbonyl groups, C i-6 alkylsulfonyl groups, C i-6 alkoxycarbonyl groups, mono-Ci-6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di- C -6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups (the C -6 alkyl groups, the C 2-6 alkenyl groups, the C 1-6 alkoxy groups, the C - alkylthio groups, the d -6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the C i-6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , C 3-11 cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C6-14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 3 -n cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C6-14 aryl groups and 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1a) , and the substituent set V5a consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C 1-6 alkoxy groups, C -6 alkylthio groups, C -6 alkylcarbonyl groups, C i-6 alkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-C- -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups, C3- cycloalkyl groups, 3 to 1 1-membered non-aromatic heterocyclyl groups, C6 - 14 aryl groups and 5 to 0-membered aromatic heterocyclyl groups (the C -6 alkoxy groups, the C -6 alkylthio groups, the C -6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-C -6 alkylamino groups, the mono-Ci-6 alkylaminocarbonyl groups, the di- C -6 alkylaminocarbonyl groups, the C -6 alkylcarbonylamino groups, the C3- cycloalkyl groups, the 3 to 1 1-membered non-aromatic heterocyclyl groups, the C - aryl groups and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3a)], a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 3. The compound according to Claim 2, wherein R1a is a hydrogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 4. The compound according to Claim 2 or 3 , wherein Ya is CR10a (wherein R 0a is a hydrogen atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 5 . The compound according to any one of Claims 2 to 4, wherein Xa is a nitrogen atom or CR9a (wherein R9a is a hydrogen atom, a halogen atom, a cyano group, a C -3 alkyl group, a C -3 haloalkyl group or a C 3-6 cycloalkyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 6. The compound according to any one of Claims 2 to 5 , wherein the ring Aa is represented by any of the following formulae (IVa-1) to (IVa-3): ( IV ) ( I Va-2 ) ( IVa-3 ) (wherein E2a is an oxygen atom or a sulfur atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 7. The compound according to any one of Claims 2 to 6, wherein L a is a single bond, L a is a single bond, a C 1-6 alkylene group or a C2 -6 alkenylene group (the C -6 alkylene group and the C 2-6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), the ring Ba is a C3- cycloalkane, a C3-n cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a C e- 4 aromatic carbocycle or a 5 to 10-membered an aromatic heterocycle, na is 0 or , R3a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C -3 alkyl group, a C 1-3 haloalkyl group, a C3 -6 cycloalkyl group, a C -3 alkoxy group, a C -3 haloalkoxy group or a C -3 alkylsulfonyl group, L3a is a single bond, and R a is a hydrogen atom, a halogen atom, a C 3-11 cycloalkyl group, a 3 to -membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 10- membered aromatic heterocyclyl group (the C3-n cycloalkyl group, the 3 to 1 1 - membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 8 . The compound according to any one of Claims 2 to 6 , wherein L a is a single bond or a C1-3 alkylene group, L a is a single bond or a C 3 alkylene group (the C-1 3 alkylene group is unsubstituted or substituted with a cyano group or a C -3 haloalkyl group), the ring Ba is a C3.n cycloalkane, a C3-11 cycloalkene, a 3 to 1 1-membered non-aromatic heterocycle, benzene or a 5 to 6-membered aromatic heterocycle, na is 0 or 1, R a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C-i -3 alkyl group, a -3 haloalkyl group, a C3-6 cycloalkyl group, a C -3 alkoxy group, a C -3 haloalkoxy group or a C1-3 alkylsulfonyl group, L3a is a single bond, and R a is a hydrogen atom, a halogen atom, a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 9. The compound according to Claim 7, wherein the ring Ba is a C3-1 1 cycloalkane, a 4 to 7-membered non-aromatic heterocycle or benzene, na is, 0 or 1, and R3a is a hydroxy group, a halogen atom, a cyano group or a C 1.3 alkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 10. The compound according to Claim 7 or 9 , wherein L2a is a single bond, a C1-6 alkylene group, a C2-6 alkenylene group or a C1-6 haloalkylene group (the C -6 alkylene group, the C2 -6 alkenylene group and the C -6 haloalkylene group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups and cyano groups), the ring Ba is a C3- cycloalkane or a 4 to 7-membered non-aromatic heterocycle, and R a is a hydrogen atom, a halogen atom, a C3-6 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the C3 -6 cycloalkyl group, the 3 to 1 1-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, nitro groups, carboxy groups, carbamoyl groups, sulfamoyl groups, C1-6 alkyl groups, C -6 alkoxy groups, mono-Ci-6 alkylamino groups, di-Ci -6 alkylamino groups, C -6 alkylthio groups, C -6 alkylcarbonyl groups, C - alkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C-i -6 alkylcarbonylamino groups (the Ci-e alkyl groups, the C -6 alkoxy groups, the mono-Ci -6 alkylamino groups, the i-C -6 alkylamino groups, the C-i -6 alkylthio groups, the Ci-e alkylcarbonyl groups, the C i -6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the C -6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and C -3 alkoxy groups), C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C 3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, - alkyl groups and C -6 haloalkyl groups)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 1 1 . The compound according to Claim 7 or 9, wherein L a is a single bond, a C 1-3 alkylene group, a C 2-3 alkenylene group (the C i -3 alkylene group and the C 2-3 alkenylene group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups and cyano groups) or a C -3 haloalkylene group, and R a is a hydrogen atom or a halogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 12. The compound according to any one of Claims 7, 9 and 10, wherein the ring Ba is a C4 -7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, and R2a is a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the 3 to 1 1-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, carbamoyl groups, C i -3 alkyl groups, C -3 alkoxy groups, mono-C -3 alkylamino groups, di-Ci -3 alkylamino groups (the C 1-3 alkyl groups, the C -3 alkoxy groups, the mono-Ci -3 alkylamino groups and the di-Ci -3 alkylamino groups are unsubstituted or substituted with a hydroxy group or a cyano group), C 1-3 haloalkyl groups, C 1-3 haloalkoxy groups, C i -3 alkylthio groups, C 1-3 haloalkylthio groups, C i -3 alkylsulfonyl groups, C -3 haloalkylsulfonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a C -3 alkyl group and a C 1-3 haloalkyl group)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 13. The compound according to any one of Claims 7, 9 and 10, wherein the ring Ba is a C4-7 cycloalkane, and R2a is a 4 to 7-membered non-aromatic heterocyclyl group (the 4 to 7-membered nonaromatic heterocyclyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, carboxy groups, C 1-3 alkyl groups (the C 1 3 alkyl groups are unsubstituted or substituted with a hydroxy group or a cyano group), C 1-3 haloalkyl groups, C1-3 alkoxy groups, di-Ci -3 alkylamino groups, mono-C -3 alkylaminocarbonyl groups, Ci -3 alkylsulfonyl group, C1 3 alkylcarbonylamino groups (the C 1-3 alkoxy groups, the di-Ci -3 alkylamino groups, the mono-C- -3 alkylaminocarbonyl groups, the Ci -3 alkylsulfonyl group and the Ci-3 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), 4 to 7-membered non-aromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, -3 alkyl groups and Ci -3 haloalkyl groups)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 14. The compound according to any one of Claims 2 to 6, wherein L1a is a single bond, L2a is a single bond, a C -6 alkylene group or a C2 -6 alkenylene group (the C -6 alkylene group and the C2-6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), the ring Ba is a C3- cycloalkane, a C3- cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a C-6-14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, na is 0 or 1, R a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a halogen atom, a cyano group, a Ci- 3 alkyl group, a C1-3 haloalkyl group, a C 3-6 cycloalkyl group, a C -3 alkoxy group, a C -3 haloalkoxy group or a C -3 alkylsulfonyl group, 3a is represented by any of the following formulae (XIVa-1) to (XIVa-15): (wherein E a is an oxygen atom, a sulfur atom or NR11a (wherein R a is a hydroxy group or a C -3 alkoxy group), each of R12a and R 3a is independently a hydrogen atom, a C -6 alkyl group or a C1-6 haloalkyl group (the C1-6 alkyl group and the Ci -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, cyano groups, C3-11 cycloalkyl groups, C1-6 alkoxy groups, C -6 haloalkoxy groups, C -6 alkylthio groups, C -6 alkylsulfonyl groups, C - haloalkylsulfonyl groups, C1-6 alkoxycarbonyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, mono-Ci-6 alkylamino groups, di-C1-6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di- C- -6 alkylaminocarbonyl groups, C1-6 alkylcarbonylamino groups, phenyl groups and 5 to 10-membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a))), and R a .is a hydrogen atom, a C -6 alkyl group, a C2 -6 alkenyl group (the C 1-6 alkyl group and the C-2-6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5a) , a C3- cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 10-membered aromatic heterocyclyl group (the C3- cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 15. The compound according to any one of Claims 2 to 6 , wherein L1a is a single bond or a C 1-3 alkylene group, L2a is a single bond or a C 1-3 alkylene group (the C -3 alkylene group is unsubstituted or substituted with a cyano group or a C 1-3 haloalkylene group), the ring Ba is a C3-n cycloalkane, a C3- cycloalkene, a 3 to 11-membered non-aromatic heterocycle, benzene or a 5 to 6-membered aromatic heterocycle, na is 0 or 1 R3a is a hydroxy group, an amino group, a carbamoyl group, a halogen atom, a cyano group, a C -3 alkyl group, a C -3 haloalkyl group, a C3-6 cycloalkyl group, a C -3 alkoxy (Va-7) (Va-8) (Va-9) (Va-10) (Va-ll) (wherein E1a is an oxygen atom, each of R1 a and R 3a is independently a hydrogen atom, a C 1-6 alkyl group or a C -6 haloalkyl group), and R a is a hydrogen atom, a Ci-6 alkyl group (the Ci-6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5a) , a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C 3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 16. The compound according to Claim 14, wherein L a is a single bond, a C -3 alkylene group, a C-2-3 alkenylene group (the C -3 alkylene group and the C-2-3 alkenylene group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups and cyano groups) or a C-1-3 haloalkylene group, the ring Ba is a C3-11 cycloalkane, a 4 to 7-membered non-aromatic heterocycle or benzene, na is 0 or 1, R is a halogen atom, a cyano group or a C1-3 alkyl group, and L3 is represented by any of the following formulae (XV -1) to (XV-12): ( XVa- l ) ( XV a-2 ) ( XVa-3 ) ( XVa-4 ) ( X Va-5 ) ( XVa- ) ( XV a-7 ) ( XV a-8 ) ( XVa-9 ) ( XV O) ( XVa-ll ) ( X V a-12 ) (wherein E a is an oxygen atom or NR a (wherein R11a is a hydroxy group), and R12a is a hydrogen atom, a C -6 alkyl group or a C - -6 haloalkyl group (the C -6 alkyl group and the Ci-6 haloalkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C -3 alkoxy group, a C3-6 cycloalkyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a cyano group, a C -3 alkyl group and a C -3 haloalkyl group))), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 17. The compound according to Claim 14 or 16, wherein L2a is a single bond or a C-i-3 alkylene group, the ring Ba is a C4-7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, and R a is a hydrogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group (the C -6 alkyl group and the Ci-6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C 6 alkoxy groups, mono-C-i -6 alkylaminocarbonyl groups, di- C1-6 alkylaminocarbonyl groups (the mono-Ci-6 alkylaminocarbonyl groups and the di- C -6 alkylaminocarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), C3 -6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups or 5 to 0- membered aromatic heterocyclyl groups (the C3-6 cycloalkyl groups, the 4 to 7- membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with identical or different one , two or three substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, -6alkoxy groups, C - haloalkoxy groups, C -6 alkylthio groups, C -6 haloalkylthio groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with a halogen atom))), a C 3- cycloalkyl group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 0-membered aromatic heterocyclyl group (the C3 - cycloalkyl group, the 4 to 7- membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -6 alkyl groups (the Ci-6 alkyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, hydroxy groups and C -3 alkoxy groups), C -6 alkoxy groups, Ci-6 haloalkoxy groups, C -6 alkylthio groups, C -6 haloalkylthio groups, Ci-6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups (the C1-6 alkoxycarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), 4 to 7-membered nonaromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with a halogen atom)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 18. The compound according to any one of Claims 14, 16 and 17, wherein L a is represented by any of the following formulae (XXIIIa- 1) to (XXIIIa-7): ( XXIII ) ( XXIIIa-5 ) ( XXIIIa-6 ) ( XXIIIa-7 ) (wherein E1a is an oxygen atom, and R a is a hydrogen atom, a C -3 alkyl group (the Ci- 3 alkyl group is unsubstituted or substituted with a cyano group) or a C -3 haloalkyl group), and R a is a C -6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with a cyano group), a C -6 haloalkyl group, a C 3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group or a phenyl group (the 4 to 7-membered non-aromatic heterocyclyl group and the phenyl group are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a hydroxy group, a cyano group, a C1-3 alkyl group and a C 3 haloalkyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 19. The compound according to any one of Claims 4 and 16 to 18, wherein L3a is (XXIVa-4): ( XXIV ) ( XXIV ) ( XXIV a-2 ) ( XXIV a-3 ) ( XXIV ) (wherein E1a is an oxygen atom, and R a is a hydrogen atom, a C -3 alkyl group (the - 3 alkyl group is unsubstituted or substituted with a cyano group) or a C -3 haloalkyl group), and R a is a Ci-3 alkyl group (the C1-3 alkyl group is unsubstituted or substituted with a cyano group), a C -3 haloalkyl group or a C3-6 cycloalkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 20. The compound according to any one of Claims 14, 16 and 17, wherein L3a is represented by the formula (XVIa) : N ( XVI a ) R 12a (wherein R 2a is a hydrogen atom, a C -3 alkyl group (the C 1-3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C -3 alkoxy group, a C3-6 cycloalkyl group and a phenyl group) or a C -3 haloalkyl group), and R a is a hydrogen atom, a C -6 alkyl group (the Ci_6 alkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C 1-3 alkoxy groups, mono- Ci-3 alkylaminocarbonyl groups (the mono-Ci-3 alkylaminocarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), C3-6 cycloalkyl groups, 4 to 7-membered nonaromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C-1 .3 alkoxy groups, Ci-3 haloalkoxy groups, C -3 alkylsulfonyl groups, C -6 alkoxy carbonyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with a halogen atom))), a C -6 haloalkyl group (the C -6 haloalkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 6- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, C1.3 alkoxy groups and C -3 alkylthio groups)), a C3- cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10- membered aromatic heterocyclyl group (the C 3-11 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -3 alkyl groups (the C -3 alkyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group and a C -3 alkoxy group), C-1 3 haloalkyl groups, C1-3 alkoxy groups, C -3 haloalkoxy groups, C -3 alkylsulfonyl groups, Ci-3 haloalkylsulfonyl groups, -6 alkoxycarbonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with a halogen atom)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 2 1. The compound according to any one of Claims 2 to 12 and 14 to 19, wherein the ring Ba is cyclohexane or piperidine, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 22. The compound according to Claim 13 or 20, wherein the ring Ba is cyclohexane, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 23. The compound according to any one of Claims 5 to 22, wherein Xa is CR9a (wherein R9a is a hydrogen atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 24. The compound according to any one of Claims 6 to 23, wherein the ring Aa is re resented by any of the following formulae (IVa- 1) to (IVa-3): ( IVa-l ) ( IVa-2 ) ( I Va-3 ) (wherein E is an oxygen atom or a sulfur atom, and each of R and R is independently a hydrogen atom or a C -3 alkyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 25. The compound according to any one of Claims 8, 23 and 24, wherein L a is a single bond, L2a is a single bond or a C -3 alkylene group, the ring Ba is a C4-7 cycloalkane, benzene or a 4 to 7-membered non-aromatic heterocycle, na is 0, L3a is a single bond, and R2a is a hydrogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 26. The compound according to any one of Claims 15, 23 and 24, wherein L a is a single bond, L2a is a single bond, the ring Ba is a C4 -7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, na is 0 , L3a is represented by any of the following formulae (Vla-1) to (Vla-3): o o ( VIM ) ( VIa-2 ) ( VI -3 ) n d R2a is a hydrogen atom or a C -3 alkyl group (the C -3 alkyl group is unsubstituted or substituted with a cyano group or a phenyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 27. The compound according to any one of Claims 2 to 6, 8 , 15, 25 and 26, wherein the ring Ba is cyclohexane, benzene or piperidine, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 28. The compound according to Claim 1, wherein R a is a hydrogen atom, Xa is CR9a (wherein R9a is a hydrogen atom or a halogen atom), Ya is CR 0a (wherein R10a is a hydrogen atom), the ring Aa is represented by any of the following formulae (IVa-1) to (IVa-3): ( IVM ) ( IVa-2 ) ( IVa- ) (wherein E a is an oxygen atom or a sulfur atom, R4a is a hydrogen atom or a -3 alkyl group, and R6a is a hydrogen atom), L1a is a single bond, the ring Ba is a C3-11 cycloalkane, a C3- cycloalkene (a ring-constituting methylene group of the C3- cycloalkane and the C3-1 1 cycloalkene may be replaced by a carbonyl group), a 3 to 11-membered non-aromatic heterocycle, a C - aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, na is 0 , 1 or 2 , R3a is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a halogen atom, a cyano group, a C -3 alkyl group, a C -3 haloalkyl group or a C -3 alkoxy group (when na is 2 , R3a's may be identical or different), L2a is a single bond, a -6alkylene group, a C2- alkenylene group (the alkylene group and the C2-6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), =C (R15a)- (wherein R1 a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L a is a double bond) or =C (R15a)-CH 2- (wherein R15a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L2a is a double bond), L3a is a single bond or represented by any of the following formulae (XIVa-1) to (XIVa- 15) and (Xlll a) ( XIV ) ( XIVa-2 ) ( XIVa-3 ) ( XIVa-4 ) ( XIVa-5 ) ( XIVa- ) ( XIVa-7 ) ( XIVa-8 ) ( XIVa-9 ) ( XIV O) ( XIV l ) ( XIVa-l 2 ) ( XIV 3 ) ( XIV 4 ) ( XIVa-15 ) (wherein E1a is an oxygen atom), when L3a is a single bond, R a is a hydrogen atom, a halogen atom, an azido group, a C-3-11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C e- 4 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 11-membered partially saturated aromatic cyclic group o r a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3- cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C-6-14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 1 1 -membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon groupg are unsubstituted o r substituted with one o r more identical o r different substituents independently selected from the group consisting of the substituent set V4a , the substituent set V a and C - alkyl groups (the C -6 alkyl groups are substituted with a C-i -6 alkoxycarbonylamino group (the C -6 alkoxycarbonylamino group is unsubstituted o r substituted with one o r more identical o r different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms))), when L3a is not a single bond, R2a is a hydrogen atom, a C -6 alkyl group, a C 2 - 6 alkenyl group, a C 2 - 6 alkynyl group (the C -6 alkyl group, the C 2-6 alkenyl group and the C-2-6 alkynyl group are unsubstituted or substituted with one o r more identical o r different substituents independently selected from the substituent set V6a and the substituent set V a) , a C-3- cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C-6-14 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 1 1 -membered partially saturated aromatic cyclic group o r a 8 to 11-membered aromatic ringcondensed alicyclic hydrocarbon group (the C 3 - cycloalkyl group, the 3 to 11- membered non-aromatic heterocyclyl group, the C e-14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 11-membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) , and each of R a and R a is independently a hydrogen atom, a -6alkyl group, a -6 haloalkyl group (the -6alkyl group and the Ci-6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V2a, the substituent set V a and the substituent set V9a) , a C3- 1 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C6 - 14 aryl group, a 5 to 10-membered aromatic heterocyclyl group or a 8 to 11-membered partially saturated aromatic cyclic group (the C3-n cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C6 -14 aryl group, the 5 to 10-membered aromatic heterocyclyl group and the 8 to 11-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 29. The compound according to Claim 1 or 28, wherein L a is a single bond, a C1-6 alkylene group, a C2 -6 alkenylene group (the C -6 alkylene group and the C-2-6 alkenylene group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups and cyano groups) or a C-i -6 haloalkylene group, the ring Ba is a C4-7 cycloalkane (a ring-constituting methylene group of the C4.7 cycloalkane may be replaced by a carbonyl group) or a 4 to 7-membered non-aromatic heterocycle, na is 0, 1 or 2, R3a is a cyano group, a C -3 alkyl group or a halogen atom (when na is 2 , R3a's may be identical or different), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 30. The compound according to any one of Claims , 28 and 29, wherein L3a is a single bond, R2a is a hydrogen atom, a halogen atom, an azido group, a C 3.11 cycloalkyl group, a 3 to 1 1-membered non-aromatic heterocyclyl group, a phenyl group, a 5 to 10-membered aromatic heterocyclyl group or a 8 to 11-membered partially saturated aromatic cyclic group (the C3- cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group, the 5 to 10-membered aromatic heterocyclyl group and the 8 to 11-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of the substituent set V4a, the substituent set V9a and C -6 alkyl groups (the C -6 alkyl groups are substituted with a Ci-6 alkoxycarbonylamino group (the Ci-6 alkoxycarbonylamino group is unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms))), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 3 1. The compound according to Claim 30, wherein L2a is a Ci-3 alkylene group, the ring Ba is a 4 to 7-membered non-aromatic heterocycle, L3a is a single bond, R a is a phenyl group or a 5 to 10-membered aromatic heterocyclyl group or a 8 to 11- membered partially saturated aromatic cyclic group (the phenyl group, the 5 to 10- membered aromatic heterocyclyl group and the 8 to -membered partially saturated aromatic cyclic group are unsubstituted or substituted with one, two or three identical o r different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, carbamoyl groups, C -6 alkyl groups, -6 haloalkyl groups, Ci-6 alkoxy groups, C1-6 haloalkoxy groups, di-Ci-6 alkylamino groups, Ci-6 alkylthio groups, C -6 haloalkylthio groups, Ci-6 alkylsulfonyl groups, 4 to 7- membered non-aromatic heterocyclyl groups and 5 to 6-membered aromatic heterocyclyl groups), a tautomer o r a pharmaceutically acceptable salt of the compound or a solvate thereof. 32. The compound according to any one of Claims 28 to 30, wherein the ring Ba is a C-4-7 cycloalkane, L3a is a single bond, R a is a 3 to 11-membered non-aromatic heterocyclyl group (the 3 to 11-membered nonaromatic heterocyclyl group is unsubstituted or substituted with one or more identical o r different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, carbamoyl groups, carboxy groups, Ci-6 alkyl groups (the C1-6 alkyl groups are unsubstituted o r substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms or with a substituent selected from the group consisting of a hydroxy group, a cyano group and a Ci-6 alkoxycarbonylamino group), C -3 alkoxy groups, mono-Ci -3 alkylaminocarbonyl groups, C -3 alkylcarbonylamino groups (the C -3 alkoxy groups, the mono-Ci -3 alkylaminocarbonyl groups, the C -3 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), di-Ci -3 alkylamino groups, C -3 alkylsulfonyl groups, di-Ci -3 alkylaminosulfonyl groups, C -6 alkoxycarbonylamino groups, 4 to 7-membered non-aromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with a halogen atom)), a tautomer or a pharmaceutically acceptable salt of the compound o r a solvate thereof. 33. The compound according to any one of Claims 1, 28 and 29, wherein L3a is represented by any of the following formulae (XV a- 1) to (XV a-12) and (Xlll a) : ( XIII ) (wherein E a is an oxygen atom, and R1 a is a hydrogen atom, a Ci -6 alkyl group (the - 6 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a Ci-3 alkoxy group, a C3-6 cycloalkyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a cyano group, a C i-3 alkyl group and a C -3 haloalkyl group)), a Ci- 6 haloalkyl group, a C3- 6 cycloalkyl group or a phenyl group (the phenyl group is unsubstituted or substituted with a halogen atom or a cyano group)), R2a is a hydrogen atom, a C -6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V6a and the substituent set V9a) , a C2 -6 alkynyl group, a C3- cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3- cycloalkyl group, the 3 to -membered nonaromatic heterocyclyl group, the phenyl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 1 1-membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4a and the substituent set V9a) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 34. The compound according to Claim 33, wherein the ring Ba is a C4-7 cycloalkane or a 4 to 7-membered non-aromatic heterocycle, L3a is represented by the following formulae (XXVa- ) or (XXVa-2): (XXV ) ( XXV -2 ) (wherein R1 a is a hydrogen atom, a C -3 alkyl group (the C -3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C -3 alkoxy group, a C3-6 cycloalkyl group and a phenyl group), a C -3 haloalkyl group, a C3-6 cycloalkyl group or a phenyl group (the phenyl group is unsubstituted or substituted with a halogen atom or a cyano group)), R a is a hydrogen atom, a Ci-6 alkyl group, a Ci -6 haloalkyl group (the C-i-6 alkyl group and the Ci-6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, C -3 alkoxy groups, C -3 alkylthio groups, C -3 alkylsulfonyl groups, mono-Ci -3 alkylaminocarbonyl groups, di-Ci -3 alkylaminocarbonyl groups (the mono-Ci -3 alkylaminocarbonyl groups and the di-Ci- 3 alkylaminocarbonyl groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3 -6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, C -3 alkyl groups, C -3 haloalkyl groups, C1-3 alkoxy groups, C1-3 haloalkoxy groups, C -3 alkylthio groups, Ci-3 haloalkylthio groups, .3 alkylsulfonyl groups, C -3 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci -3 alkylamino groups, di- C -3 alkylamino groups, mono-Ci -3 alkylaminocarbonyl groups, di-Ci -3 alkylaminocarbonyl groups, C -3 alkylcarbonylamino group (the C1-6 alkoxycarbonyl groups, the mono-Ci -3 alkylamino groups, the di-Ci -3 alkylamino groups, the mono-C -3 alkylaminocarbonyl groups, the di-Ci -3 alkylaminocarbonyl groups and the C -3 alkylcarbonylamino group are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), 4 to 7-membered nonaromatic heterocyclyl groups, phenyl groups (the phenyl groups are unsubstituted or substituted with a halogen atom) and 5 to 6-membered aromatic heterocyclyl groups)), a C-2-6 alkynyl group, a C 3 - 6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group, a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group, the 8 to 1 1-membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, halogen atoms, cyano groups, C -3 alkyl groups (the C -3 alkyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group and a C1-3 alkoxy group), Ci-3 haloalkyl groups, Ci-3 alkoxy groups, C -3 haloalkoxy groups, C -3 alkylthio groups, C -3 haloalkylthio groups, C -3 alkylsulfonyl groups, C -3 haloalkylsulfonyl groups, C-i -6 alkoxycarbonyl groups, mono-Ci -3 alkylamino groups, di-Ci -3 alkylamino groups, mono-Ci -3 alkylaminocarbonyl groups, di-C1-3 alkylaminocarbonyl groups, C- -3 alkylcarbonylamino groups (the C -6 alkoxycarbonyl groups, the mono-Ci- 3 alkylamino groups, the di-Ci -3 alkylamino groups, the mono-C -3 alkylaminocarbonyl groups, the di-C -3 alkylaminocarbonyl groups and the C -3 alkylcarbonylamino group are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), 4 to 7-membered nonaromatic heterocyclyl groups and phenyl groups (the phenyl groups are unsubstituted or substituted with a halogen atom)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 35. The compound according to Claim 33, wherein the ring Ba is a C4-7 cycloalkane, ( XXVI ) ( XXVIa-2 ) ( XXVIa-3 ) ( XXVIa-4 ) ( XXVI -5 ) (wherein E a is an oxygen atom, and R1 a is a hydrogen atom, a C -3 alkyl group (the C^. alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a C -3 alkoxy group, a C3-6 cycloalkyl group, a phenyl group and a 5 to 6-membered aromatic heterocyclyl group (the 5 to 6- membered aromatic heterocyclyl group is unsubstituted o r substituted with a Ci-3 alkyl group)), a C-i-3 haloalkyl group, a C3 -6 cycloalkyl group or a phenyl group (the phenyl group is unsubstituted or substituted with a halogen atom o r a cyano group)), and R2a is a C -3 alkyl group (the C -3 alkyl group is unsubstituted or substituted with a cyano group), a C -3 haloalkyl group or a C3.6 cycloalkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 36. The compound according to Claim 34 o r 35, wherein L3a is represented by the formula (XVI a) : (wherein R1 a is a hydrogen atom, a C 1 3 alkyl group (the C i -3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a hydroxy group, a cyano group, a Ci -3 alkoxy group, a C-3-6 cycloalkyl group and a phenyl group), a Ci -3 haloalkyl group, a C3-6 cycloalkyl group or a phenyl group (the phenyl group is unsubstituted or substituted with a halogen atom or a cyano group)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 37. The compound according to Claim 33, wherein L3a is represented by the formula a) : (wherein E a is an oxygen atom), R2a is a C 1-3 alkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 38. The compound according to any one of Claims 1 to 24, 28 to 30 and 32 to 37, wherein L a is a single bond or a C -3 alkylene group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 39. The compound according to Claim 1 or 28, wherein L a is a single bond, the ring Ba is a C4-7 cycloalkane, L2a is =C(R 5a)- (wherein R1 a is a hydrogen atom or a cyano group, and the bond connecting the ring Ba and L2a is a double bond) or =C(R 1 a)-CH 2- (wherein R15a is a hydrogen atom o r a cyano group, and the bond connecting the ring Ba and L2a is a double bond), and when L3a is a single bond, R2a is a hydrogen atom, and when L3a is the formula (Xa-2): R2a is a Ci -3 alkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 40. The compound according to any one of Claims 1 to 39, wherein na is 0 , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. formula (lb) the formula (ll b) : (wherein T b is CR4bR5b, C(=0), C(=S), C(=NR 17b) , a sulfur atom, S(=0) or S(=0) 2, U b R6b, and W b is a nitrogen atom or CR b) , the formula (lll b) : (wherein is CR , r is a nitrogen atom or CR , and W is CR R , C(=0), C(=S), C(=NR 17b) , NR10b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2 (provided that when b is CR6b, W b is not C(=0))) or the formula (IV b) : (wherein T3 is CR4bR5b, C(=0), C(=S), C(=NR b) , a sulfur atom, S(=0) or S(=0) 2, U b is CR6bR b, C(=0), C(=S), C(=NR b) , NR10b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2, and W3b is CR bR9b, C(=0), C(=S), C(=NR b) , NR b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2 (provided that when T3b is CR4bR5b and U3b is CR6bR b, W b is not CR8bR9b)), Xb is a nitrogen atom or CR15b, Yb is CR 6b, R b is a hydrogen atom, a halogen atom, a C -6 alkyl group or a C -6 haloalkyl group, the ring Bb is a C3-n cycloalkane, a C3- cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a Ce-14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L b is a single bond, a Ci-6 alkylene group, a C2-6 alkenylene group or a C2 - 6 alkynylene group (the C-i-6 alkylene group, the C2 -6 alkenylene group and the C2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L b is a single bond, a - alkylene group, a C2-6 alkenylene group or a C2-6 alkynylene group (the C -6 alkylene group, the C2 -6 alkenylene group and the C-2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L b is a single bond or represented by any of the following formulae (Vb-1) to (Vb-20): ( V b-12 ) ( Vb-13 ) ( V -14 ) ( Vb-15 ) ( V b-16 ) ( V -17 ) ( Vb-18 ) ( V b-19 ) ( V b-20 ) (wherein E b is an oxygen atom, a sulfur atom or NR18b) , when L3b is a single bond, R b is a hydrogen atom, a halogen atom, a C3-11 cycloalkyl group, a 3 to 14-membered non-aromatic heterocyclyl group, a C6- aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 14-membered partially saturated aromatic cyclic group or a 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3 - cycloalkyl group, the 3 to 14-membered non-aromatic heterocyclyl group, the C6 - 14 ry group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 14-membered partially saturated aromatic cyclic group and the 8 to 14- membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b and the substituent set V9 ) , when L3b is not a single bond, R2 is a hydrogen atom, a C -6 alkyl group, a C2 -6 alkenyl group (the C -6 alkyl group and the C2 -6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V6 and the substituent set V9b) , a C 3- cycloalkyl group, a 3 to 14- membered non-aromatic heterocyclyl group, a C6 - 14 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 14-membered partially saturated aromatic cyclic group or a 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon group (the C 3 1 cycloalkyl group, the 3 to 14-membered non-aromatic heterocyclyl group, the C e-14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 14-membered partially saturated aromatic cyclic group and the 8 to 14-membered aromatic ringcondensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b and substituent set V9b) , n is 0 , 1 or 2 , R3 is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a sulfamoyl group, a phosphono group, a phosphonooxy group, a sulfo group, a sulfoxy group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C -6 alkyl group, a C -6 haloalkyl group, a C 3.n cycloalkyl group, a C 2-6 alkenyl group, a C 2 -6 haloalkenyl group, a C i-6 alkoxy group, a C 1-6 haloalkoxy group, a C i-6 alkylthio group, a C i-6 haloalkylthio group, a C 1-6 alkylcarbonyl group, a C i- haloalkylcarbonyl group, a Ci- 6 alkylsulfonyl group, a C -6 haloalkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-Ci -6 alkylamino group, a di-Ci -6 alkylamino group, a mono-Ci -6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group or a C i-6 alkylcarbonylamino group (when nb is 2, R3b's may be identical or different), each of R4b, R5b, R6b, R b, R8b and R9 is independently a hydrogen atom, a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a C 16 alkyl group, a C 2 -6 alkenyl group, a C i-6 alkoxy group, a C i-6 alkylthio group, a C -6 alkylcarbonyl group, a C i-6 alkylsulfonyl group, a mono-Ci -6 alkylamino group, a di-Ci -6 alkylamino group (the C -6 alkyl group, the C 2 -6 alkenyl group, the C -6 alkoxy group, the C 1-6 alkylthio group, the C -6 alkylcarbonyl group, the C i-6 alkylsulfonyl group, the mono-Ci -6 alkylamino group and the di-Ci -6 alkylamino group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , a -6 alkoxycarbonyl group, a C3-11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C e- 4 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3- cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the C e-14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , each of R10b and R is independently a hydrogen atom, a Ci-6 alkyl group, a C 2-6 alkenyl group, a C 1-6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a Ci-6 alkoxycarbonyl group, a mono-Ci -6 alkylaminocarbonyl group, a di-Ci-6 alkylaminocarbonyl group (the Ci-6 alkyl group, the C 2 -6 alkenyl group, the Ci-6 alkylcarbonyl group, the C 1-6 alkylsulfonyl group, the C 1-6 alkoxycarbonyl group, the mono-Ci -6 alkylaminocarbonyl group and the di-Ci - alkylaminocarbonyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , a C3.11 cycloalkyl group, a 3 to 11- membered non-aromatic heterocyclyl group, a C6-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3-11 cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C 6 -14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , each of R b, R b and R14b is independently a hydrogen atom, a Ci-6 alkyl group or a Ci- 6 haloalkyl group (the C - alkyl group and the Ci- haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b, the substituent set V8b and the substituent set V9b) , each of R 5b and R16b is independently a hydrogen atom, a halogen atom, a cyano group, a carbamoyl group, a -6alkyl group, a C -6 haloalkyl group, a C 3-11 cycloalkyl group, a -6 alkoxy group, a C -6 haloalkoxy group, a C -6 alkylthio group, a C -6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C-6-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group, each of R b and R b is independently a hydrogen atom, a hydroxy group, a cyano group, a nitro group, a C -6 alkyl group or a C 1-6 alkoxy group, the substituent set V1b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkyl groups, C i-6 haloalkyl groups, C3-11 cycloalkyl groups, C-2-6 alkenyl groups, C 2 -6 haloalkenyl groups, C i-6 alkoxy groups, C -6 haloalkoxy groups, C -6 alkylthio groups, Cihaloalkylthio groups, C-1-6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, C-i -6 alkylsulfonyl groups, C i-6 haloalkylsulfonyl groups, C - alkoxycarbonyl groups, 3 to 11- membered non-aromatic heterocyclyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups and C1-6 alkylcarbonylamino groups, the substituent set V b consists of the groups in the substituent set V1b, and C e-14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C e-14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1b) , the substituent set V3b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkoxy groups, C -6 haloalkoxy groups, C -6 alkylthio groups, C -6 haloalkylthio groups, C -6 alkylcarbonyl groups, C -6 haloalkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-C -6 alkylamino groups, di-C-i -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups, C 3.11 cycloalkyl groups, 3 to 1 1-membered non-aromatic heterocyclyl groups, C 6 -i4 aryl group and 5 to 10-membered aromatic heterocyclyl groups (the C 3 -n cycloalkyl groups, the 3 to 11-membered nonaromatic heterocyclyl groups, the C e-14 y groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1b) , the substituent set V4b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkyl groups, C 2 -6 alkenyl groups, C i-6 alkoxy groups, C i-6 alkylthio groups, C -6 alkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di- C 1- alkylaminocarbonyl groups, C 1-6 alkylcarbonylamino groups (the C 6 alkyl groups, the C 2-6 alkenyl groups, the C 1-6 alkoxy groups, the C -6 alkylthio groups, the C 1-6 alkylcarbonyl groups, the Ci-6 alkylsulfonyl groups, the Ci-6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the C-1-6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , C 3. cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C-6-14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 3 1 1 cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C 6 -14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1b) , the substituent set V5b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkoxy groups, C -6 alkylthio groups, C i-6 alkylcarbonyl groups, -6 alkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci-6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups, C 3.11 cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C e- 4 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C -6 alkoxy groups, the C 1-6 alkylthio groups, the C 1-6 alkylcarbonyl groups, the C i-6 alkylsulfonyl groups, the C-1 -6 alkoxycarbonyl groups, the mono-Ci-6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di- C 1-6 alkylaminocarbonyl groups, the C i-6 alkylcarbonylamino groups, the C 3.1 cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C e-14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , the substituent set V6b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C 1-6 alkoxy groups, Ci-6 alkylthio groups, Ci-6 alkylcarbonyl groups, Ci-6 alkylsulfonyl groups, C i-6 alkoxycarbonyl groups, mono-Ci-6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci-6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C i-6 alkylcarbonylamino groups (the C -6 alkoxy groups, the C -6 alkylthio groups, the C -6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the C i-6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-Ci -6 alkylaminocarbonyl groups and the C i-6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , C 3 11 cycloalkyl groups, 3 to 1 1-membered non-aromatic heterocyclyl groups, C 6 -14 aryl groups, 5 to 10-membered aromatic heterocyclyl groups, 8 to 14-membered partially saturated aromatic cyclic groups and 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups (the C 3-11 cycloalkyl groups, the 3 to 1 1-membered nonaromatic heterocyclyl groups, the C6- aryl groups, the 5 to 10-membered aromatic heterocyclyl groups, the 8 to 14-membered partially saturated aromatic cyclic groups and the 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b and the substituent set V9b) , and the substituent set V8b consists of 8 to 14-membered partially saturated aromatic cyclic groups and 8 to 14-membered aromatic ring-condensed alicyclic hydrocarbon groups (the 8 to 14-membered partially saturated aromatic cyclic groups and the 8 to 14- membered aromatic ring-condensed alicyclic hydrocarbon groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , the substituent set V9b consists of, mono-Ci -6 alkylaminosulfonyl groups, di-C-i -6 alkylaminosulfonyl groups, Ci-6 alkylsulfonylamino groups (the mono-Ci -6 alkylaminosulfonyl groups, di-Ci -6 alkylaminosulfonyl groups and C -6 alkylsulfonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , C3.6 cycloalkoxy groups, C3-6 cycloalkylamino groups, C3-6 cycloalkylthio groups, C3-6 cycloalkylcarbonyl groups and C3-6 cycloalkylsulfonyl groups (the C3-6 cycloalkoxy groups, the C3-6 cycloalkylamino groups, the C3-6 cycloalkylthio groups, the C3-6 cycloalkylcarbonyl groups and the C3 -6 cycloalkylsulfonyl groups unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b)], a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. aim 4 1, which is represented by the formula (lb) : the formula (ll ) : (wherein T b is CR4bR b, C(=0), C(=S), C(=NR 1 b) , a sulfur atom, S(=0) or S(=0) 2, U b R6b, and W b is a nitrogen atom or CR b) , the formula (lll b) : (wherein is CR , T is a nitrogen atom or CR , and W is CR R9 , C(=0), C(=S), C(=NR 17b) , NR10b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2 (provided that when U2 is CR6b,W2b is not C(=0))), or the formula (IVb) : (wherein T3b is CR4bR , C(=0), C(=S), C(=NR 1 b) , a sulfur atom, S(=0) o r S(=0) 2, U3b is CR6bR b, C(=0), C(=S), C(=NR b) , NR 0b, an oxygen atom, a sulfur atom, S(=0) o r S(=0) 2, and W3b is CR bR9b, C(=0), C(=S), C(=NR 7b) , NR b, an oxygen atom, a sulfur atom, S(=0) or S(=0) 2 (provided that when T3b is CR bR5b and U3b is CR6bR b, W3b is not CR8bR9b)), Xb is a nitrogen atom or CR 5b, Yb is CR 6 , R b is a hydrogen atom, a halogen atom, a C -6 alkyl group or a C - -6 haloalkyl group, the ring Bb is a C3-11 cycloalkane, a C3-n cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a C6 - 14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L b is a single bond, a C -6 alkylene group, a C-2-6 alkenylene group or a C2 -6 alkynylene group (the C -6 alkylene group, the C2-6 alkenylene group and the C2-6 alkynylene group are unsubstituted or substituted with one or more identical o r different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L b is a single bond, a Ci-6 alkylene group, a C2 - 6 alkenylene group or a C2 -6 alkynylene group (the C -6 alkylene group, the C2-6 alkenylene group and the C2-6 alkynylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), L3b is a single bond or represented by any of the following formulae (Vb-1) to (Vb-20): (wherein E1b is an oxygen atom, a sulfur atom or NR b) , when L3b is a single bond, R b is a hydrogen atom, a halogen atom, a C3-11 cycloalkyl group, a 3 to -membered non-aromatic heterocyclyl group, a Ce- y group or a 5 to 10-membered aromatic heterocyclyl group (the C3-11 cycloalkyl group, the 3 to 11 - membered non-aromatic heterocyclyl group, the C 6- i 4 aryl group and the 5 to 10- membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b) , when L3b is not a single bond, R2b is a hydrogen atom, a C -6 alkyl group, a C2 -6 alkenyl group (the C -6 alkyl group and the C2-6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5b) , a C3- cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C6- 4 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C3.11 cycloalkyl group, the 3 to 1 1-membered non-aromatic heterocyclyl group, the Ce-1 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b) , nb is 0 , 1 or 2, R is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a sulfamoyl group, a phosphono group, a phosphonooxy group, a sulfo group, a sulfoxy group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C 1-6 alkyl group, a C -6 haloalkyl group, a C3-n cycloalkyl group, a C2-6 alkenyl group, a C2 -6 haloalkenyl group, a C i -6 alkoxy group, a C i -6 haloalkoxy group, a C i-6 alkylthio group, a C i -6 haloalkylthio group, a C -6 alkylcarbonyl group, a C -6 haloalkylcarbonyl group, a . 6 alkylsulfonyl group, a C i -6 haloalkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-C -6 alkylamino group, a di-Ci -6 alkylamino group, a mono-C-1 -6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group or a C -6 alkylcarbonylamino group (when nb is 2, R3b's may be identical or different), each of R b, R5b, R6b, R b, R8b and R9 is independently a hydrogen atom, a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a C -6 alkyl group, a C2 -6 alkenyl group, a C-i -6 alkoxy group, a C -6 alkylthio group, a C -6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a mono-Ci -6 alkylamino group, a di-Ci -6 alkylamino group (the C -6 alkyl group, the C 2 -6 alkenyl group, the C i -6 alkoxy group, the C -6 alkylthio group, the Ci- 6 alkylcarbonyl group, the C -6 alkylsulfonyl group, the mono-Ci-6 alkylamino group and the di-Ci -6 alkylamino group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , a C i -6 alkoxycarbonyl group, a C3-11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C-6-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3- cycloalkyl group, the 3 to 1-membered non-aromatic heterocyclyl group, the C e-14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1b) , each of R 0b and R 1b is independently a hydrogen atom, a C -6 alkyl group, a C 2-6 alkenyl group, a C -6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a C -6 alkoxycarbonyl group, a mono-Ci -6 alkylaminocarbonyl group, a di-Ci -6 alkylaminocarbonyl group (the C i -6 alkyl group, the C2 - alkenyl group, the C i -6 alkylcarbonyl group, the C -6 alkylsulfonyl group, the C -6 alkoxycarbonyl group, the mono-Ci -6 alkylaminocarbonyl group and the di-Ci -6 alkylaminocarbonyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , a C3.11 cycloalkyl group, a 3 to 1 1 - membered non-aromatic heterocyclyl group, a C e-14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3-n cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C 6 -14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , each of R 2 , R 3b and R 4b is independently a hydrogen atom, a C i -6 alkyl group or a Ci- 6 haloalkyl group (the C -6 alkyl group and the C i -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , each of R 5b and R 6b is independently a hydrogen atom, a halogen atom, a cyano group, a carbamoyl group, a C -6 alkyl group, a C 1-6 haloalkyl group, a C3.11 cycloalkyl group, a C 1-6 alkoxy group, a C i -6 haloalkoxy group, a C i -6 alkylthio group, a C i -6 alkylcarbonyl group, a C -6 alkylsulfonyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a C 6 -14 aryl group or a 5 to 10-membered aromatic heterocyclyl group, each of R 7b and R b is independently a hydrogen atom, a hydroxy group, a cyano group, a nitro group, a C i -6 alkyl group or a C i -6 alkoxy group, the substituent set V b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyi groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C- -6 alkyl groups, C -6 haloalkyl groups, C3-11 cycloalkyl groups, C 2 -6 alkenyl groups, C 2 -6 haloalkenyl groups, C -6 alkoxy groups, C -6 haloalkoxy groups, C-1 -6 alkylthio groups, C i - 6 haloalkylthio groups, Ci- 6 alkylcarbonyl groups, C i - haloalkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, 3 to 11- membered non-aromatic heterocyclyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups and C i -6 alkylcarbonylamino groups, the substituent set V2b consists of the groups in the substituent set V b and C 6 -i 4 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C 6 -i 4 aryl groups and 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , the substituent set V3b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C 1-6 alkoxy groups, C -6 haloalkoxy groups, Ci- 6 alkylthio groups, C -6 haloalkylthio groups, Ci- 6 alkylcarbonyl groups, Ci- 6 haloalkylcarbonyl groups, Ci- 6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-Ci- 6 alkylamino groups, di-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups, C 3 -n cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6 -14 aryl groups and 5 to 10- membered aromatic heterocyclyl groups (the C3-11 cycloalkyl groups, the 3 to 11- membered non-aromatic heterocyclyl groups, the C e-14 aryl groups and the 5 to 10- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , the substituent set V4 consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C 1-6 alkyl groups, C 2-6 alkenyl groups, Ci- 6 alkoxy groups, C-1 -6 alkylthio groups, C -6 alkylcarbonyl groups, C -6 alkylsulfonyl groups, C i -6 alkoxycarbonyl groups, mono-Ci -6 alkylamino groups, di-d-6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di- C 1-6 alkylaminocarbonyl groups, C 1-6 alkylcarbonylamino groups (the C -6 alkyl groups, the C 2 -6 alkenyl groups, the C -6 alkoxy groups, the C -6 alkylthio groups, the Ci- 6 alkylcarbonyl groups, the C -6 alkylsulfonyl groups, the Ci- 6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di-Ci-e alkylaminocarbonyl groups and the C 1-6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , C3-11 cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C 6 -14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C3-11 cycloalkyl groups, the 3 to 1 1-membered non-aromatic heterocyclyl groups, the C 6 -14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , and the substituent set V b consists of hydroxy groups, amino groups, carboxy groups, carbamoyl groups, sulfamoyl groups, phosphono groups, phosphonooxy groups, sulfo groups, sulfoxy groups, tetrazolyl groups, halogen atoms, cyano groups, nitro groups, C-1 -6 alkoxy groups, -6alkylthio groups, C i-6 alkylcarbonyl groups, C -6 alkylsulfonyl groups, C -6 alkoxycarbonyl groups, mono-C -6 alkylamino groups, i-Ci -6 alkylamino groups, mono-Ci -6 alkylaminocarbonyl groups, di-Ci -6 alkylaminocarbonyl groups, C-1 -6 alkylcarbonylamino groups, C 3. cycloalkyl groups, 3 to 11-membered non-aromatic heterocyclyl groups, C6 -14 aryl groups and 5 to 10-membered aromatic heterocyclyl groups (the C i-6 alkoxy groups, the C 1-6 alkylthio groups, the C i-6 alkylcarbonyl groups, the C i-6 alkylsulfonyl groups, the C -6 alkoxycarbonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci -6 alkylamino groups, the mono-Ci -6 alkylaminocarbonyl groups, the di- C -6 alkylaminocarbonyl groups, the C i-6 alkylcarbonylamino groups, the C3-n cycloalkyl groups, the 3 to 11-membered non-aromatic heterocyclyl groups, the C6 -14 aryl groups and the 5 to 10-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b)], a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 43. The compound according to Claim 42, wherein R b is a hydrogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 44. The compound according to Claim 42 or 43, wherein Xb is a nitrogen atom or CR b (wherein R15b is a hydrogen atom, a halogen atom, a cyano group, a C i-3 alkyl group, a C i-3 haloalkyl group or a C3-6 cycloalkyl group), and Y is CR 6b (wherein R 6b is a hydrogen atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 45. The compound according to Claim 44, wherein Xb is a nitrogen atom or CR 5b (wherein R15b is a hydrogen atom or a halogen atom), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 46. The compound according to any one of Claims 42 to 45, wherein the ring Ab is ula (ll ) : (wherein T is CR4bR5b, C(=0), C(=S) or S(=0) 2, U b is a nitrogen atom or CR6b, and b is CR b) , the formula (lll b) : (wherein T is CR , U is a nitrogen atom, and Vr is C(=0) or C(=S)) or the formula b) : ) (wherein T3b is CR4 R5b, U3b is NR10b or an oxygen atom, and W3b is CR8bR9b, C(=0) or C(=S)), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. ring Ab is ( XVIII b ) ( XVIII -5 ) ( XVIII b-6 ) ( XVIII -7 ) ( XVIII b-8 ) (wherein each of E and E b is independently an oxygen atom or a sulfur atom, each of R b, R5b, R6b, R8b and R9b is independently a hydrogen atom, a halogen atom or a C -3 alkyl group, and R 0b is a hydrogen atom or a -3 alkyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 48. The compound according to any one of Claims 42 to 47, wherein L b is a single bond, L2b is a single bond, a C -6 alkylene group or a C2-6 alkenylene group (the C-i-6 alkylene group and the C2 -6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of a halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), the ring Bb is a C3-11 cycloalkane, a C3-11 cycloalkene, a 3 to 11-membered non-aromatic heterocycle, a C e- 4 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, nb is, 0 or 1, R3b is a hydroxy group, an amino group, a halogen atom, a cyano group, a Ci-3 alkyl group, a C 1-3 haloalkyl group, a C3-6 cycloalkyl group, a C1-3 alkoxy group, a C1-3 haloalkoxy group or a C 1-3 alkylsulfonyl group, L b is a single bond, and R2b is a hydrogen atom, a halogen atom, a C3-11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 10- membered aromatic heterocyclyl group (the C 3- cycloalkyl group, the 3 to 1 1 - membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 49. The compound according to any one of Claims 42 to 47, wherein L is a single bond or a C 1-3 alkylene group, L2b is a single bond or a C -3 alkylene group (the C -3 alkylene group is unsubstituted or substituted with a cyano group or a C -3 haloalkyl group), the ring Bb is a C3-n cycloalkane, a C 3.11 cycloalkene, a 3 to 1 1-membered non-aromatic heterocycle, benzene or a 5 to 6-membered aromatic heterocycle, nb is, 0 or 1, R3b is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C-1 .3 alkyl group, a C i -3 haloalkyl group, a C3-6 cycloalkyl group, a C -3 alkoxy group, a C -3 haloalkoxy group or a Ci-3 alkylsulfonyl group, L3b is a single bond, and R b is a hydrogen atom, a halogen atom, a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 50. The compound according to Claim 48, wherein the ring Bb is a C3- cycloalkane or a 4 to 7-membered non-aromatic heterocycle, n is 0 or , and R3b is a hydroxy group, a C-i-3 alkyl group or a C 1-3 alkoxy group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 5 1. The compound according to Claim 48 or 50, wherein L b is a single bond, a C1-6 alkylene group, a C2-6 alkenylene group or a C -6 haloalkylene group (the C -6 alkylene group, the C2 - 6 alkenylene group and the -6 haloalkylene group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups and cyano groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 52. The compound according to any one of Claims 48, 50 and 5 , wherein R2 is a hydrogen atom, a C3.6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the 4 to 7- membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10- membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, carbamoyl groups, sulfamoyi groups, halogen atoms, cyano groups, nitro groups, C -6 alkyl groups, C i -6 alkoxy groups, C -6 alkylthio groups, C 1-6 alkylsulfonyl groups, mono-C1-6 alkylamino groups, di-Ci-6 alkylamino groups, C -6 alkoxycarbonyl groups, mono-C^ alkylaminocarbonyl groups, di-Ci- 6 alkylaminocarbonyl groups, C -6 alkylcarbonylamino groups (the C -6 alkyl groups, the C 1-6 alkoxy groups, the C -6 alkylthio groups, the C -6 alkylsulfonyl groups, the mono-Ci -6 alkylamino groups, the di-Ci-6 alkylamino groups, the C1-6 alkoxycarbonyl groups, the mono-Ci-6 alkylaminocarbonyl groups, the di-Ci-6 alkylaminocarbonyl groups and the Ci- 6 alkylcarbonylamino groups are unsubstituted or substituted with one or more identical or different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms or with a hydroxy group or a cyano group), C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 53. The compound according to Claim 52, wherein R2b is a hydrogen atom, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 10-membered aromatic heterocyclyl group (the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, nitro groups, C-1-3 alkyl groups (the -3 alkyl groups are unsubstituted or substituted with a cyano group), C -3 haloalkyl groups and C -6 alkoxycarbonyl groups), a tautomer o r a pharmaceutically acceptable salt of the compound or a solvate thereof. 54. The compound according to any one of Claims 48 and 50 to 53, wherein L b is a C -6 alkylene group, a C2 -3 alkenylene group (the Ci- 6 alkylene group and the C2-3 alkenylene group are unsubstituted o r substituted with a cyano group) or C-|.6 haloalkylene group, and R b is, a hydrogen atom, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 55. The compound according to any one of Claims 42 to 47, wherein L b is a single bond, L b is a single bond, a C -6 alkylene group or a C2-6 alkenylene group (the -e alkylene group and the C2-6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), the ring Bb is a C3-n cycloalkane, a C3-n cycloalkene, a 3 to 1 1-membered non-aromatic heterocyclyl group, a C-6-14 aryl group or a 5 to 10-membered aromatic heterocycle, nb is 0 or , R b is a hydroxy group, an amino group, a halogen atom, a cyano group, a C -3 alkyl group, a C1-3 haloalkyl group, a C3-6 cycloalkyl group, a C-1-3 alkoxy group o r a C1-3 haloalkoxy group, L b is represented by any of the following formulae (Vl b-1) to (Vl b-11 ) : ( I - l ) ( I b -2 ) ( I b -3 ) ( I b - ) ( V I b -5 ) ( I b -6 ) ( V I b-7 ) ( V I b-8 ) ( V I -9 ) ( V I b -10 ) ( V I b -ll ) (wherein E1b is an oxygen atom or a sulfur atom, each of R b and R13 is independently a hydrogen atom, a Ci -6 alkyl group or a C -6 haloalkyl group (the Ci- 6 alkyl group and the Ci-6 haloalkyl group are unsubstituted or substituted with one o r more identical o r different substituents independently selected from the group consisting of halogen atoms, cyano groups, hydroxy group, C -6 alkoxy groups, C -6 alkylthio groups, C -6 alkylsulfonyl groups, C 3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a cyano group, a C1 3 alkyl group and a C1-3 haloalkyl group))), and R is a hydrogen atom, a Ci-6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5b) , a C3-11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group or a 5 to 10-membered aromatic heterocyclyl group (the C3-11 cycloalkyl group, the 3 to 11-membered non-aromatic heterocyclyl group, the phenyl group, the naphthyl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 56. The compound according to any one of Claims 42 to 47, wherein L is a single bond or a Ci-3 alkylene group, L2b is a single bond or a C1-3 alkylene group (the C-1 .3 alkylene group is unsubstituted or substituted with a cyano group or a Ci-3 haloalkyl group), the ring Bb is a C3- cycloalkane, a C3-n cycloalkene, a 3 to 1 1-membered non-aromatic heterocycle, benzene or a 5 to 6-membered aromatic heterocycle, n is 0 or 1, R3b is a hydroxy group, an amino group, a carbamoyl group, a halogen atom, a cyano group, a -3 alkyl group, a C1-3 haloalkyl group, a C3-6 cycloalkyl group, a C1-3 alkoxy group, a C -3 haloalkoxy group or a C -3 alkylsulfonyl group, 3b is represented by any of the following formulae (Vlb-1) to (Vlb-11): b-l ) (V I -2 ) ( Ib- ) ( Ib-4 ) (V Ib-5 ) ( I - ) (VIb-7) (VI -8) (VIb-9) (VIb-10) (VI -ll) (wherein E1b is an oxygen atom, each of R1 b and R 3 is independently a hydrogen atom, a Ci-6 alkyl group or a C -6 haloalkyl group), and R2b is a hydrogen atom, a C -6 alkyl group (the C -6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V5b), a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V1b) , a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 57. The compound according to Claim 55, wherein the ring Bb is a C 3. cycloalkane or a 4 to 7-membered non-aromatic heterocycle, L3b is represented by any of the following formulae (XIXb- ) to (XIXb-7): XIX -l ) ( XIX -2 ) ( XIX -3 ) ( XIX -4 ) ( XIXb-5 ) ( XIX ) ( XIXb-6 ) ( XIX -7 ) (wherein E b is an oxygen atom, and R 12b is a hydrogen atom, a C -6 alkyl group (the Ci- 6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C -3 alkoxy groups, C3-6 cycloalkyl groups and phenyl groups) or a C -6 haloalkyl group), and R b is a hydrogen atom, a C i -6 alkyl group, a C - haloalkyl group (the C i -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, cyano groups, C-i -3 alkoxy groups, C -3 alkylthio groups, C -3 alkylsulfonyl groups, C 3 -6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, cyano groups, C i -6 alkoxy groups, C1-6 haloalkoxy groups and C -6 alkoxycarbonyl groups)), a C3.6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, cyano groups, C i -6 alkyl groups, C -6 haloalkyl groups, C -6 alkoxy groups, C -6 haloalkoxy groups and C -6 alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 58. The compound according to Claim 55 or 57, wherein L b is represented by any of the following formulae (XX -1) to (XXb-4): ( XXb-l ) ( XX -2 ) ( XX -3 ) ( XX -4 ) (wherein E b is an oxygen atom, and R 2b is a hydrogen atom, a C -3 alkyl group (the Ci- 3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group, a C -3 alkoxy group, a C3-6 cycloalkyl group and a phenyl group) or C -3 haloalkyl group)), and R b is a hydrogen atom, a C -3 alkyl group, a C -3 haloalkyl group (the C -3 alkyl group and the -3 haloalkyl group are unsubstituted or substituted with one or two identical or different substituent selected from the group consisting of hydroxy groups, cyano groups, C 1-3 alkoxy groups, C3- cycloalkyi groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C-3-6 cycloalkyi groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a hydroxy group or a halogen atom)), a C3-6 cycloalkyi group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C 3-6 cycloalkyi group, the 4 to 7-membered nonaromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one o r two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C-i -6 alkyl groups, C -3 haloalkyl groups and C-i -6 alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 59. The compound according to any one of Claims 48 to 53 or 55 to 58, wherein L b is a single bond or a C 1-3 alkylene group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 60. The compound according to any one of Claims 44 to 59, wherein Xb is a nitrogen atom o r CR15b (wherein R is a hydrogen atom), and Yb is CR 6b (wherein R b is a hydrogen atom), a tautomer or a pharmaceutically acceptable salt of the compound o r a solvate thereof. 6 1. The compound according to any one of Claims 46 to 60, wherein the ring Ab is ( VII b- l ) ( VII -2 ) ( VII -3 ) ( VII ( VII b-5 ) ( VII -6 ) ( VII b-7 ) (wherein E2b is an oxygen atom, and each of R4b, R , R , R8b, R9b and R 0b is independently a hydrogen atom or a C 1.3 alkyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 62. The compound according to any one of Claims 46 to 60, wherein the ring Ab is represented by any of the following formulae (XXXIII b- 1) to (XXXIII b-3): ( XXXIII" ) ( XXXIII b - l ) ( XXXIII b -2) ( XXXIII b -3 ) (wherein E b is a n oxygen atom, and each of R4b , R5b , R8b , R9b and R10b are hydrogen atoms, and R6b is a hydrogen atom, a halogen atom o r a -3 alkyl group), a tautomer o r a pharmaceutically acceptable salt of the compound o r a solvate thereof. 63. The compound according to any one of Claims 49, 6 0 and 6 1, wherein L b is a single bond, L2b is a Ci-3 alkylene group, the ring B b is a C4-7 cycloalkane o r a 4 to 7-membered non-aromatic heterocycle, nb is 0 o r 1, R3b is a C 1-3 alkyl group, L3b is a single bond, and R2b is a hydrogen atom o r a phenyl group (the phenyl group is unsubstituted o r substituted with one o r more identical o r different halogen atoms independently selected from the group consisting of fluorine atoms, chlorine atoms, bromine atoms and iodine atoms), a tautomer o r a pharmaceutically acceptable salt of the compound o r a solvate thereof. 64. The compound according to any one of Claims 49, 6 0 and 6 1, wherein L is a single bond, L b is a single bond, the ring Bb is a C4-7 cycloalkane o r a 4 to 7-membered non-aromatic heterocycle, nb is 0 , L is a single bond, and R 2b iiss a hhyyddrrooggeenn aattoomm,, a tautomer o r a pharmaceutically acceptable salt of the compound o r a solvate thereof. 65. The compound according to any one of Claims 56, 6 0 and 6 1, wherein L 1b is a single bond, L2b is a single bond, the ring Bb is a C4-7 cycloalkane o r a 4 to 7-membered non-aromatic heterocycle, nb is 0 o r 1, R3b is a C-i-3 alkyl group, L3b is represented by any of the following formula (Vlll -1) o r (Vlll b-2): ( VIII b - l ) ( VIII b -2 ) and R2b is a C -6 alkyl group (the C 1-6 alkyl group is unsubstituted o r substituted with a cyano group o r a C 3-e cycloalkyl group) o r a C -3 haloalkyl group, a tautomer o r a pharmaceutically acceptable salt of the compound o r a solvate thereof. 66. The compound according to any one of Claims 4 2 to 65, wherein the ring B b is cyclohexane o r piperidine, a tautomer o r a pharmaceutically acceptable salt of the compound or a solvate thereof. 67. The compound according to any one of Claims 42 to 62, wherein the ring Bb is a 4 to 7-membered non-aromatic heterocycle, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. or CR 5b III -8): ( XVIII ) ( XVIII b-5 ) ( XVIII -6 ) ( XVIII b-7 ) ( XVIII -8 ) (wherein each of E2b and E3b is independently an oxygen atom or a sulfur atom, each of R b, R5 , R6b, R b and R9 is independently a hydrogen atom, a halogen atom or a C -3 alkyl group, and R 0 is a hydrogen atom, a C -6 alkyl group (the -6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V3b) , a C 3-n cycloalkyl group, a 3 to 11- membered non-aromatic heterocyclyl group, a C 6 - 14 aryl group or a 5 to 10-membered aromatic heterocyclyl group (the C 3-n cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the C 6 -14 aryl group and the 5 to 10-membered aromatic heterocyclyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V b)), the ring Bb is a C 3-n cycloalkane, a 3 to 11-membered non-aromatic heterocycle, a C 6 -14 aromatic carbocycle or a 5 to 10-membered aromatic heterocycle, L1 is single bond or a C -3 alkylene group, L b is a single bond, a C -6 alkylene group or a C2-6 alkenylene group (the C 1-6 alkylene group and the C 2 -6 alkenylene group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, hydroxy groups, amino groups, cyano groups and nitro groups), nb is 0 or 1, R3 is a hydroxy group, an amino group, a carboxy group, a carbamoyl group, a tetrazolyl group, a halogen atom, a cyano group, a nitro group, a C 1-3 alkyl group, a C -3 haloalkyl group, a C 3-6 cycloalkyl group, a C 1.3 alkoxy group, a C1-3 haloalkoxy group or a C -3 alkylsulfonyl group, L3b is a single bond or represented by any of the following formulae (XXIIb-1) to (XXIIb- 15): XXII b-l ) ( XXII b-2 ( XXII b-3 ) ( XXII b- ) XXII b-5 ) 0 o E E E X X b Rl2b R 13b Rl2b Rl3b Rl2b ( XXII b-6 ) ( XXII b-7 ) ( XXII b-8 ) ( XXII -9 ) ( XXII -10 ) (wherein E b is an oxygen atom or a sulfur atom, and each of R12b and R 3b is independently a hydrogen atom, a C -6 alkyl group or a C -6 haloalkyl group (the C -6 alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, hydroxy groups, C -6 alkoxy groups, C -6 alkylthio groups, C -6 alkylsulfonyl groups, C 3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the phenyl groups and 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a cyano group, a C 1-3 alkyl group and a -3haloalkyl group))), when L3b is a single bond, R is a hydrogen atom, a halogen atom, a C3.11 cycloalkyl group, a 3 to 11-membered non-aromatic heterocyclyl group, a phenyl group, a naphthyl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 1 1-membered partially saturated aromatic cyclic group or a 8 to 1 1-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3-n cycloalkyl group, the 3 to 11-membered nonaromatic heterocyclyl group, the phenyl group, the naphthyl group, the 5 to 10- membered aromatic heterocyclyl group, the 8 to 11-membered partially saturated aromatic cyclic group and the 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V4b and the substituent set V9b) , when L3b is not a single bond, R2b is a hydrogen atom, a C -6 alkyl group, a C2-6 alkenyl group (the Ci-6 alkyl group and the C2-6 alkenyl group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set V6b and the substituent set V b) , a C3-n cycloalkyl group, a 3 to 11- membered non-aromatic heterocyclyl group, a Ce-14 aryl group, a 5 to 10-membered aromatic heterocyclyl group, a 8 to 11-membered partially saturated aromatic cyclic group or a 8 to 11-membered aromatic ring-condensed alicyclic hydrocarbon group (the C3-11 cycloalkyl group, the 3 to 1 1-membered non-aromatic heterocyclyl group, the Ce-14 aryl group, the 5 to 10-membered aromatic heterocyclyl group, the 8 to 1 1-membered partially saturated aromatic cyclic group or the 8 to 11-membered aromatic ringcondensed alicyclic hydrocarbon group are unsubstituted or substituted with one or more identical or different substituents independently selected from the substituent set e y ( XXI b-l ) ( XXI -2) ( XXI b-3 ) ( XXI b-4 ) (wherein each of E and E is independently an oxygen atom or a sulfur atom, R , R , R8b and R9b are hydrogen atoms, R6 is a hydrogen atom, a halogen atom or a C -3 alkyl group, and R 0b is a hydrogen atom, a C -6 alkyl group (the C1-6 alkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C -3 alkoxy groups, -3 alkylthio groups, mono-Ci -3 alkylamino groups, di-Ci -3 alkylamino groups, mono-Ci -3 alkylaminocarbonyl groups, di-Ci -3 alkylaminocarbonyl groups, C 3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the phenyl groups and the 5 to 6- membered aromatic heterocyclyl groups are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of halogen atoms, C1-3 alkyl groups and C -3 haloalkyl groups)), a C -6 haloalkyl group, a C3 -6 cycloalkyl group or a 4 to 7-membered non-aromatic heterocyclyl group), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. ims 4 1, 68 and 69, wherein the ring Ab ) or (XXIXb-2): ( XXK - l ) ( X K -2 ) (wherein E and E are oxygen atoms, R is a hydrogen atom, a halogen atom or a C -3 alkyl group, R b is a hydrogen atom, and R 0b is a hydrogen atom, a C -6 alkyl group (the C 1-6 alkyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C 1-3 alkoxy groups, C-1 .3 alkylthio groups, di-Ci- 3 alkylamino groups, C 3-6 cycloalkyl groups and 4 to 7-membered non-aromatic heterocyclyl groups), a C-i-e haloalkyl group, a C3-6 cycloalkyl group or a 4 to 7-membered non-aromatic heterocyclyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 7 1. The compound according to any one of Claims 4 1 and 68 to 7 , wherein L1b is a single bond, L2b is a single bond, a -6 alkylene group, a C2-6 alkenylene group or a C -6 haloalkylene group (the C 1-6 alkylene group, the C2 -6 alkenylene group and the C1-6 haloalkylene group are unsubstituted or substituted with a hydroxy group or a cyano group), the ring Bb is a C3-n cycloalkane or a 4 to 7-membered non-aromatic heterocycle, nb is 0 or 1, and R3b is a hydroxy group, a Ci-3 alkyl group or a C -3 alkoxy group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 72. The compound according to any one of Claims 4 1 and 68 to 70, wherein L3b is a single bond, and R2b is a hydrogen atom, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group, a 5 to 10-membered aromatic heterocyclyl group or a 8 to 11-membered partially saturated aromatic cyclic group (the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group, the 5 to 10-membered aromatic heterocyclyl group and the 8 to 11- membered partially saturated aromatic cyclic group are unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of hydroxy groups, amino groups, carbamoyl groups, sulfamoyl groups, halogen atoms, cyano groups, nitro groups, C -6 alkyl groups (the C1-6 alkyl groups are unsubstituted or substituted with a cyano group), C -.6 haloalkyl groups, C3- cycloalkyl groups, C1-6 alkoxy groups, C1-6 haloalkoxy groups, Ci-6 alkylthio groups, Ci-6 haloalkylthio groups, C -6 alkylsulfonyl groups, C -6 haloalkylsulfonyl groups, Ci -6 alkoxycarbonyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, mono-Ci -6 alkylamino groups, di-Ci -6 alkylamino groups, phenyl groups, 5 to 6-membered aromatic heterocyclyl groups, mono-Ci-6 alkylaminosulfonyl groups and di-C-i-6 alkylaminosulfonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 73. The compound according to Claim 72, wherein R2b is a hydrogen atom, a phenyl group, a 5 to 10-membered aromatic heterocyclyl group or a 8 to 11-membered partially saturated aromatic cyclic group (the phenyl group, the 5 to 10-membered aromatic heterocyclyl group and the 8 to 11-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, nitro groups, C 1.3 alkyl groups, C1-3 haloalkyl groups and C - alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 74. The compound according to Claim 72, wherein R b is a 4 to 7-membered nonaromatic heterocyclyl group (the 4 to 7-membered non-aromatic heterocyclyl group is unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C -3 alkyl groups (the C1-3 alkyl groups are unsubstituted or substituted with a cyano group) and Ci-3 haloalkyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 75. The compound according to any one of Claims 4 1 and 68 to 7 1, wherein L3b is represented by any of the following formulae (XIX - 1) to (XIXb-7): ( XIX -l ) ( XIX -2 ) ( XIX -3 ) ( XIXb-4 ) ( XIX -5 ) ( XIX ) ( XIX - ) ( XIX -7 ) (wherein E is an oxygen atom, and R1 is a hydrogen atom or a C - alkyl group (the C-1 -6 alkyl group is unsubstituted or substituted with one or more identical or different substituents independently selected from the group consisting of halogen atoms, cyano groups, hydroxy groups, C -3 allkoxy groups, C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups)), and R is a hydrogen atom, a C -6 alkyl group, a Ci -6 haloalkyl group (the -6 alkyl group and the C - haloalkyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of cyano groups, hydroxy groups, C -6 alkoxy groups, C -6 alkylthio groups, C -6 alkylsulfonyl groups, C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6- membered aromatic heterocyclyl groups are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of the substituent set V b, mono-Ci -6 alkylaminosulfonyl groups and di-Ci -6 alkylaminosulfonyl groups)), a C3-6 cycloalkyl group, a 4 to 7-membered non-aromatic heterocyclyl group, a phenyl group, a 5 to 6-membered aromatic heterocyclyl group or a 8 to 11-membered partially saturated aromatic cyclic group (the C3-6 cycloalkyl group, the 4 to 7-membered non-aromatic heterocyclyl group, the phenyl group, the 5 to 6- membered aromatic heterocyclyl group and the 8 to 11-membered partially saturated aromatic cyclic group are unsubstituted or substituted with one, two or three identical or different substituents independently selected from the group consisting of the substituent set V2b, mono-C-1 -6 alkylaminosulfonyl groups and di-Ci -6 alkylaminosulfonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 76. The compound according to Claim 75, wherein L3 is represented by any of the ( XXXI -l ) ( XXXIb-2 ) ( XXXI -3 ) ( XXXI -4 ) ( XXXIb-5 ) (wherein E1b is an oxygen atom, and R1 b is a hydrogen atom, a C 1-3 alkyl group (the C 3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group, a C 1-3 allkoxy group, a C3-6 cycloalkyl group and a phenyl group) or -3 haloalkyl group), and R b is a hydrogen atom, a C -6 alkyl group, a C -6 haloalkyl group (the C - alkyl group and the C -6 haloalkyl group are unsubstituted or substituted with one or two identical or different substituent selected from the group consisting of hydroxy groups, cyano groups, Ci-3 alkoxy groups, C3-6 cycloalkyl groups, 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups (the C3-6 cycloalkyl groups, the 4 to 7-membered non-aromatic heterocyclyl groups, the phenyl groups and the 5 to 6-membered aromatic heterocyclyl groups are unsubstituted or substituted with a hydroxy group or a halogen atom)), a C3-6 cycloalkyl group, a 4 to 7- membered non-aromatic heterocyclyl group, a phenyl group or a 5 to 6-membered aromatic heterocyclyl group (the C3-6 cycloalkyl group, the 4 to 7-membered nonaromatic heterocyclyl group, the phenyl group and the 5 to 6-membered aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of hydroxy groups, halogen atoms, cyano groups, C1-3 alkyl groups, C -3 haloalkyl groups and C -6 alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 77. The compound according to Claim 75, wherein L3b is represented by the formula (XXXI l ) : A ( XXXII b ) R 2b (wherein R b is a hydrogen atom, a C1-3 alkyl group (the Ci-3 alkyl group is unsubstituted or substituted with a substituent selected from the group consisting of a cyano group, a hydroxy group, a Ci-3 allkoxy group, a C3-6 cycloalkyl group and a phenyl group) or a C -3 haloalkyl group), and R2b is a hydrogen atom, a C -3 alkyl group, a C -3 haloalkyl group (the C1-3 alkyl group and the C1-3 haloalkyl group are unsubstituted or substituted with one or two identical or different substituent selected from the group consisting of hydroxy groups, cyano groups, C1-3 alkoxy groups, C3-6 cycloalkyl groups (the C3-6 cycloalkyl groups are unsubstituted or substituted with a hydroxy groups), 4 to 7-membered non-aromatic heterocyclyl groups, phenyl groups and 5 to 6-membered aromatic heterocyclyl groups), a C 3-6 cycloalkyl group or a 4 to 7-membered non-aromatic heterocyclyl group (the C3.6 cycloalkyl group and the 4 to 7-membered non-aromatic heterocyclyl group are unsubstituted or substituted with one or two identical or different substituents independently selected from the group consisting of C -3 alkyl groups, Ci-3 haloalkyl groups and C -6 alkoxycarbonyl groups), a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 78. The compound according to any one of Claims 4 1 or 68 to 77, wherein L2b is a single bond or a Ci-3 alkylene group, and the ring Bb is cyclohexane or piperidine, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 79. The compound according to any one of Claims 4 1 to 78, wherein nb is 0 or 1, and R3b is a Ci-3 alkyl group, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof. 80. A JAK inhibitor containing the compound as defined in any one of Claims 1 to 79, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof, as an active ingredient. 81 . A preventive, therapeutic or improving agent for diseases against which inhibition of JAK is effective, which contains the JAK inhibitor as defined in Claim 80. 82. A therapeutic agent for articular rheumatism, which contains the JAK inhibitor as defined in Claim 80. 83. Medicament containing the compound as defined in any one of Claims 1 to 79, a tautomer or a pharmaceutically acceptable salt of the compound or a solvate thereof, as an active ingredient.