DESCRIPTION

AMIDE COMPOUNDS AND THROMBOPOIETIN RECEPTOR ACTIVATORS

TECHNICAL FIELD
The present invention relates to preventive, therapeutic and improving agents having affinity for and agonistic action on the thrombopoietin receptor for diseases against which activation of the thrombopoietin receptor is effective. Specifically, it relates to pharmaceutical compositions comprising compounds which increase platelets through stimulation of differentiation and proliferation of hematopoietic stem cells, megakaryocytic progenitor cells and megakaryocytes or compounds for therapeutic angiogenesis or with anti-arteriosclerosis action that stimulate differentiation and proliferation of vascular endothelial cells and endothelial progenitor cells.

BACKGROUND ART
Thrombopoietin is a cytokine consisting of 332 amino acids that increases platelet production by stimulating differentiation and proliferation of hematopoietic stem cells, megakaryocytic progenitor cells and megakaryocytes mediated by its receptor and therefore is promising as a drug for hematological disorders. Recent reports that it stimulates differentiation and proliferation of vascular endothelial cells and endothelial progenitor cells have raised expectations of therapeutic angiogenesis, anti-arteriosclerosis and prevention of cardiovascular events (for example, non-patent document 1, non-patent document 2 and non-patent document 3).
Biologically active substances which have been known so far to regulate platelet production through the thrombopoietin receptor include, in addition to thrombopoietin itself, low molecular weight peptides having affinity for the thrombopoietin receptor (for example, patent document 1, patent document 2, patent document 3 and patent document 4).
As a result of search for nonpeptidic low molecular weight compounds that increase platelet production mediated by the thrombopoietin receptor, low molecular weight compounds having affinity for the thrombopoietin receptor have been reported (for example, patent document 5 to patent document 25).
1) Applications filed by Hokuriku Seiyaku Co., Ltd. relating to 1,4-benzodiazepine derivatives (patent documents 5 and 6)
2) International Laid-open Patent Applications filed by Shionogi & Co., Ltd. (patent documents 7-10)
3) International Laid-open Patent Applications filed by SmithKline Beecham Corp (patent documents 11-19)
4) Japanese Laid-open Patent Application filed by Torii Pharmaceutical Co., Ltd. (patent document 20)
5) International Laid-open Patent Application filed by Roche Diagnostics GMBH (patent document 21)
6) International Laid-open Patent Applications filed by Yamanouchi Pharmaceutical Co., Ltd. (patent documents 22 and 23)
7) Japanese Laid-open Patent Application filed by Japan Tabacco Inc. (patent document 24)
8) Japanese Laid-open Patent Applications filed by Nissan Chemical Industries, Ltd. (patent documents 25 and 26)
Patent document 1 JP-A-10-72492
Patent document 2 WO96/40750
Patent document 3 WO96/40189
Patent document 4 WO98/25965
Patent document 5 JP-A-11-1477
Patent document 6 JP-A-11-152276
Patent document 7 WO01/07423
Patent document 8 WO01/53267
Patent document 9 WO02/059099
Patent document 10 WO02/059100
Patent document 11 WO00/35446
Patent document 12 WO00/66112
Patent document 13 WO01/34585
Patent document 14 WO01/17349
Patent document 15 WO01/39773
Patent document 16 WO01/21180
Patent document 17 WO01/89457
Patent document 18 WO02/49413
Patent document 19 WO02/085343
Patent document 20 JP-A-2001-97948
Patent document 21 WO99/11262
Patent document 22 WO02/062775
Patent document 23 WO03/062233
Patent document 24 JP-A-2003-238565
Patent document 25 WO04/033433
Patent document 26 WO04/108683
Non-patent document 1 Microvasc. Res., 1999: 58, p.108-113
Non-patent document 2 Circ. Res., 1999: 84, p.785-796
Non-patent document 3 Blood 2001:98, p.71a-72a

DISCLOSURE OF THE INVENTION
Thrombopoietin and low molecular weight peptides having affinity for the thrombopoietin receptor are likely to be easily degraded in the gastrointestinal tract and are usually difficult to orally administer. As to thrombopoietin itself, the appearance of anti-thrombopoietin antibodies have been reported.
Besides, though it is probably possible to orally administer nonpeptidic low molecular weight compounds, no practical drugs have been put on the market.
Therefore, orally administrable low molecular weight compounds having excellent affinity for and agonistic action on the thrombopoietin receptor as preventive,
therapeutic and improving agents for diseases against which activation of the thrombopoietin receptor is effective have been demanded. Specifically, low molecular weight compounds which can serve as platelet increasing agents or increasing agents for other blood cells by stimulating differentiation and proliferation of hematopoietic stem cells, megakaryocytic progenitor cells and megakaryocytes or low molecular weight compounds which can be used for therapeutic angiogenesis or as preventive and therapeutic agents for arteriosclerosis by stimulating endothelial cells and endothelial progenitor cells have been demanded.
The present inventors conducted extensive research to find low molecular weight compounds having affinity for and agonistic action on the thrombopoietin receptor, and as a result, found that the compounds of the present invention have high affinity and agonistic action which enable them to show potent platelet increasing action by stimulating differentiation and proliferation of megakaryocytic progenitor cells and megakaryocytes. The present invention was accomplished on the basis of this discovery.
Namely, the present invention relates to:
1. A compound represented by the formula (1):
wherein A is a nitrogen atom or CR4 (wherein R4 is a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted with a C2?6 alkenyl group or a C2?6 alkynyl group), a thiol group (the thiol group may be substituted with a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group or a C1?10 alkylcarbonyl group), an amino group (the amino group may be substituted with one or two C2?6 alkenyl groups or one or two C2?6 alkynyl groups), a formyl group, a halogen atom, a nitro group, a cyano group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkylcarbonylamino group, a mono- or di-C1?10 alkylamino group, a C1?10 alkoxy group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkylcarbonylamino group, the mono- or di-C1?10 alkylamino group and the C1?10 alkoxy group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups), a C2?14 aryloxy group (the C2?14 aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups), SO2R5, SOR5 or COR5 (wherein R5 is a hydroxyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group and the C1?10 alkoxy group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxylgroups, C2?14 aryl groups and C2?14 aryloxy groups), a C2?14 aryloxy group (the C2?14 aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups) or NR6R7 (wherein each of R6 and R7 is independently a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups), or R6 and R7 mean, together with each other, ?(CH2)m1-E-(CH2)m2- (wherein E is an oxygen atom, a sulfur atom, CR26R27 (wherein each of R26 and R27 is independently a hydrogen atom, a C1?10 alkyl group, a C2?14 aryl group, a C1?10 alkoxy group, a C2?14 aryloxy group, a hydroxyl group or a protected hydroxyl group) or NR8 (wherein R8 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)), and each of m1 and m2 is independently an integer of from 0 to 5 provided that m1+m2 is 3, 4 or 5)))),B is an oxygen atom, a sulfur atom or NR9 (wherein R9 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups) or a C2?14 aryloxy group (the C2?14 aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)) (provided that when A is a nitrogen atom, B is not NH),
R1 is a C2?14 aryl group (the C2?14 aryl group may be substituted with one or more substituents selected from the group consisting of: halogen atoms, carboxyl groups, nitro groups, formyl groups, cyano groups, hydroxyl groups, protected hydroxyl groups, C1?10 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups (the C1?10 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups, the C1?10 alkoxy groups, the C1?10 alkylcarbonyl groups, the C1?alkylcarbonyloxy groups and the C1?10 alkoxycarbonyl groups may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), C2?14 aryl groups (the C2?14 aryl groups may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups), thiol groups and amino groups (the thiol groups and the amino groups may be optionally substituted with one or two substituents selected from the group consisting of: formyl groups, C1?10 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups and C1?10 alkylcarbonyl groups (the C1?10 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups and the C1?10 alkylcarbonyl groups may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)))),
L1 is a bond, CR10R11 (wherein each of R10 and R11 is independently a hydrogen atom or a C1?6 alkyl group (the C1?6 alkyl group may be substituted with one or more halogen atoms)), an oxygen atom, a sulfur atom or NR12 (wherein R12 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyloxy group, the C1?1alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)),
X is OR13, SR13 or NR14R15 (wherein R13 is a hydrogen atom, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group or a C1?10 alkylcarbonyl group (the C1?alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), and each of R14 and R15 is independently a hydrogen atom, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)),
R2 is a hydrogen atom, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups),
L2 is a bond, CR34R35 (wherein each of R34 and R35 is independently a hydrogen atom or a C1?6 alkyl group (the C1?6 alkyl group may be substituted with one or more halogen atoms)), an oxygen atom, a sulfur atom or NR16 (wherein R16 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)),
L3 is a bond, CR17R18 (wherein each of R17 and R18 is independently a hydrogen atom, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group,a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)), an oxygen atom, a sulfur atom or NR19 (wherein R19 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group, the C1?10 alkoxy group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)),
L4 is a bond, CR20R21 (wherein each of R20 and R21 is independently a hydrogen atom, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)), an oxygen atom, a sulfur atom or NR22 (wherein R22 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)),
Y is an oxygen atom, a sulfur atom or NR23 (wherein R23 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)), and
R3 is a C2?14 aryl group (the C2?14 aryl group is optionally substituted with one or more substituents independently represented by –V1 (wherein V1 is a hydrogen atom, a hydroxyl group, a protected hydroxyl group, an amino group, a thiol group, a nitro group, a cyano group, a halogen atom, a carboxyl group, a carbamoyl group, a sulfamoyl group, a sulfo group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyl group, a C1?10 alkylcarbonylamino group, a mono- or di-C1?10 alkylamino group, a C1?10 alkylaminosulfonyl group, a C1?10 alkylaminocarbonyl group,a C1?10 alkylsulfonylamino group, a C1?10 thioalkyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyl group, the C1?10 alkylcarbonylamino group, the mono- or di-C1?10 alkylamino group, the C1?10 alkylaminosulfonyl group, the C1?10 alkylaminocarbonyl group, the C1?10 alkylsulfonylamino group and the C1?10 thioalkyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, carbamoyl groups, sulfamoyl groups, sulfo groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C2?14 aryl group or a C2?14 aryloxy group (the C2?14 aryl group and the C2?14 aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)) and with one or more substituents independently represented by –W1(CW2W3)mW4 (wherein W1 is (CR24R25)n (wherein each of R24 and R25 is independently a hydrogen atom, a hydroxyl group, an amino group, a C1?6 alkyl group or a C1?6 alkoxy group (the C1?6 alkyl group and the C1?6 alkoxy group may be substituted with one or more halogen atoms), and n is 0, 1, 2 or 3), an oxygen atom, a sulfur atom or NR36 (wherein R36 is a hydrogen atom, a C1?6 alkyl group, a formyl group or a C1?6 alkylcarbonyl group), each of W2 and W3 is independently a hydrogen atom or a C1?3 alkyl group (the C1?3 alkyl group may be substituted with one or more halogen atoms), m is 0, 1, 2 or 3, and W4 is SO2R28, SOR28 or COR28 (wherein R28 is NR29R30 (wherein R29 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C2?14 aryl group or a C2?14 aryloxy group (the C2?14 aryl group and the C2?14 aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups), and R30 is an amino group, a mono- or di-C1?10 alkylamino group, a C1?10 alkylcarbonylamino group, a C1?10 alkylaminocarbonyl group, a C2?9 heterocyclyl group (the amino group, the mono- or di-C1?10 alkylamino group, the C1?10 alkylcarbonylamino group, the C1?10 alkylaminocarbonyl group and the C2?9 heterocyclyl group may be substituted with one or more substituents selected from the group consisting of: hydrogen atoms, carboxyl groups, carbamoyl groups, sulfamoyl groups, sulfo groups, nitro groups, cyano groups, halogen atoms, hydroxyl groups, formyl groups, C1?10 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonyl groups (the C1?10 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups, the C1?10 alkylcarbonyloxy groups, the C1?10 alkoxycarbonyl groups and the C1?10 alkylcarbonyl groups may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substitutedwith one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)), a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group are optionally substituted with one or more substituents selected from the group consisting of: hydrogen atoms, carboxyl groups, carbamoyl groups, sulfamoyl groups, sulfo groups, nitro groups, cyano groups, halogen atoms, hydroxyl groups, formyl groups, C1?10 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonyl groups (the C1?10 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups, the C1?10 alkylcarbonyloxy groups, the C1?10 alkoxycarbonyl groups and the C1?10 alkylcarbonyl groups may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups) and with one or more substituents selected from the group consisting of: carboxyl groups, carbamoyl groups, sulfo groups, sulfamoyl groups and C2?9 heterocyclyl groups (the C2?9 heterocyclyl groups may be optionally substituted with one or more substituents selected from the group consisting of: hydrogen atoms, hydroxyl groups, formyl groups, C1?10 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonyl groups, C2?9 heterocyclyl groups (the C1?10 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups, the C1?10 alkylcarbonyloxy groups, the C1?10 alkoxycarbonyl groups, the C1?10 alkylcarbonyl groups and the C2?9 heterocyclyl groups may be optionally substituted with one or more substituents selected from the group consisting of: hydrogen atoms, carboxyl groups, carbamoyl groups, sulfamoyl groups, sulfo groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups))), or R29 and R30 mean, together with each other, –(CH2)m3-G-(CH2)m4? (wherein G is CR31R32 (wherein R31 is a hydrogen atom, a C1?10 alkyl group, a C2?14 aryl group, a C1?10 alkoxy group, a C2?14 aryloxy group (the C1?10 alkyl group, the C2?14 aryl group, the C1?10 alkoxy group and the C2?14 aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), a hydroxyl group or a protected hydroxyl group, and R32 is an amino group, a mono- or di-C1?10 alkylamino group, a C1?10 alkylcarbonylamino group, a C1?10 alkylaminocarbonyl group or a C2?9 heterocyclyl group (the mono- or di-C1?10 alkylamino group, the C1?10 alkylcarbonylamino group, the C1?10 alkylaminocarbonyl group and the C2?9 heterocyclyl group may be substituted with one or more substituents selected from the group consisting of: hydrogen atoms, carboxyl groups, carbamoyl groups, sulfamoyl groups, sulfo groups, nitro groups, cyano groups, halogen atoms, amino groups, hydroxyl groups, formyl groups, C1?10 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonyl groups (the C1?10 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups, the C1?10 alkylcarbonyloxy groups, the C1?10 alkoxycarbonyl groups and the C1?10 alkylcarbonyl groups may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups))) or NR33 (wherein R33 is an amino group, a mono- or di-C1?10 alkylamino group, a C1?10 alkylcarbonylamino group, a C1?10 alkylaminocarbonyl group or a C2?9 heterocyclyl group (the mono- or di-C1?10 alkylamino group, the C1?10 alkylcarbonylamino group, the C1?10 alkylaminocarbonyl group and the C2?9 heterocyclyl group may be substituted with one or more substituents selected from the group consisting of: hydrogen atoms, carboxyl groups, carbamoyl groups, sulfamoyl groups, sulfo groups, nitro groups, cyano groups, halogen atoms, amino groups, hydroxyl groups, formyl groups, C1?10 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonyl groups (the C1?10 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups, the C1?10 alkylcarbonyloxy groups, the C1?10 alkoxycarbonyl groups and the C1?10 alkylcarbonyl groups may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups))), and each of m3 and m4 is independently an integer of from 0 to 5, proSequence Listing Electronic Form NO YES vided that m3+m4 is 3, 4 or 5), or NR29R30, as a whole, means a nitrogen-containing C2?9 cyclyl group (the nitrogen-containing C2?9 cyclyl group may be optionally substituted with one or more hydrogen atoms and is substituted with two or three substituents independently selected from the group consisting of: hydroxyl groups, amino groups, thiol groups, nitro groups, cyano groups, halogen atoms, carboxyl groups, carbamoyl groups, sulfamoyl groups, formyl groups, C1?10 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups, C1?10 alkoxy groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonylamino groups, mono- or di-C1?10 alkylamino groups, C1?10 alkylsulfonylamino groups, C1?10 thioalkyl groups, C2?9 heterocyclyl groups (the C1?10 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups, the C1?10 alkoxy groups, the C1?10 alkylcarbonyloxy groups, the C1?10 alkoxycarbonyl groups, the C1?10 alkylcarbonyl groups, the C1?10 alkylcarbonylamino groups, the mono- or di-C1?10 alkylamino groups, the C1?10 alkylsulfonylamino groups, the C1?10 thioalkyl groups and the C2?9 heterocyclyl groups may be optionally substituted with one or more substituents selected from the group consisting of: hydrogen atoms, carboxyl groups, carbamoyl groups, sulfamoyl groups, sulfo groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups))) or a substituted C2?9 heterocyclyl group (the substituted C2?9 heterocyclyl group may be optionally substituted with one or more substituents selected from the group consisting of: hydrogen atoms, hydroxyl groups, amino groups, thiol groups, nitro groups, cyano groups, halogen atoms, carboxyl groups, carbamoyl groups, sulfamoyl groups, formyl groups, C1?10 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups, C1?10 alkoxy groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonylamino groups, mono- or di-C1?10 alkylamino groups, C1?10 alkylsulfonylamino groups, C1?10 thioalkyl groups, C2?9 heterocyclyl groups (the C1?10 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups, the C1?10 alkoxy groups, the C1?10 alkylcarbonyloxy groups, the C1?10 alkoxycarbonyl groups, the C1?10 alkylcarbonyl groups, the C1?10 alkylcarbonylamino groups, the mono- or di-C1?10 alkylamino groups, the C1?10 alkylsulfonylamino groups, the C1?10 thioalkyl groups and the C2?9 heterocyclyl groups may be optionally substituted with one or more substituents selected from the group consisting of: hydrogen atoms, carboxyl groups, carbamoyl groups, sulfamoyl groups, sulfo groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups))))), a C2?14 aryl group (the C2?14 aryl group is optionally substituted with one or more substituents independently represented by –V1 (wherein V1 is the same as defined above) and with one or more substituents selected from the group consisting of: C1?6 alkyl groups, C2?6 alkenyl groups and C2?6 alkynyl groups (the C1?6 alkyl groups, the C2?6 alkenyl groups and the C2?6 alkynyl groups are optionally substituted with one or more substituents selected from the group consisting of: hydroxyl groups, amino groups, mono- or di-C1?10 alkylamino groups and C1?6 alkoxy groups (the mono- or di-C1?10 alkylamino groups and the C1?6 alkoxy groups may be substituted with one or more halogen atoms), with one or more substituents independently represented by –V2 (wherein V2 is the same as V1, and V1 is the same as defined above) and with –W5 (wherein W5 is SO2R42, SOR42, COR42 (wherein R42 is a hydrogen atom, a hydroxyl group or NR43R44, R43 is the same as R6, R44 is the same as R7, and R6 and R7 are the same as defined above) or W4, and W4 is the same as defined above))), a C2?14 aryl group (the C2?14 aryl group is optionally substituted with one or more substituents independently represented by –V1 (wherein V1 is the same as defined above) and with one or more substituents selected from the group consisting of: C1?6 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups, C1?10 alkylcarbonyl groups, C1?10 alkylthiocarbonyl groups and C1?10 alkylsulfonyl groups (the C1?6 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups, the C1?10 alkylcarbonyl groups, the C1?10 alkylthiocarbonyl groups and the C1?10 alkylsulfonyl groups are optionally substituted with one or more substituents independently represented by –V2 (wherein V2 is the same as V1, and V1 is the same as defined above) and with one or more substituents selected from C2?9 heterocyclyl groups (the C2?9 heterocyclyl groups are optionally substituted with one or more substituents independently represented by –V3 (wherein V3 is the same as V1, and V1 is the same as defined above)))), a C2?14 aryl group (the C2?14 aryl group is optionally substituted with one or more substituents independently represented by –V1 (wherein V1 is the same as defined above) and with one or more substituents selected from the group consisting of: C1?6 alkyl groups, C2?6 alkenyl groups, C2?6 alkynyl groups, C1?10 alkylcarbonyl groups, C1?10 alkylthiocarbonyl groups and C1?10 alkylsulfonyl groups (the C1?6 alkyl groups, the C2?6 alkenyl groups, the C2?6 alkynyl groups, the C1?10 alkylcarbonyl groups, the C1?10 alkylthiocarbonyl groups and the C1?10 alkylsulfonyl groups are optionally substituted with one or more substituents independently represented by –V2 (wherein V2 is the same as V1, and V1 is the same as defined above) and with one or more substituents selected from the group consisting of: amino groups (the amino groups are substituted with a C1?10 alkyl group (the C1?10 alkyl group is optionally substituted with one or more substituents independently represented by –V3 (wherein V3 is the same as V1, and V1 is the same as defined above)) and with a C2?9 heterocyclyl group or a C2?14 aryl group (the C2?9 heterocyclyl group and the C2?14 aryl group are optionally substituted with one or more substituents independently represented by –V4 (wherein V4 is the same as V1, and V1 is the same as defined above))), amino groups, mono- or di-C1?10 alkylamino groups, C1?10 alkoxy groups, C1?10 thioalkyl groups, C1?10 alkylsulfonyl groups, sulfonyl groups, sulfinyl groups and thiol groups (the amino groups, the mono- or di-C1?10 alkylamino groups, the C1?10 alkoxy groups, the C1?10 thioalkyl groups, the C1?10 alkylsulfonyl groups, the sulfonyl groups, the sulfinyl groups and the thiol groups are optionally substituted with one or more C2?9 heterocyclyl groups or one or more C2?14 aryl groups (the C2?9 heterocyclyl groups and the C2?14 aryl groups are optionally substituted with one or more substituents independently represented by –V5 (wherein V5 is the same as V1, and V1 is the same as defined above))))) or a C2?14 substituted aryl group (the C2?14 substituted aryl group may be optionally substituted with one or more substituents independently represented by –V1 (wherein V1 is the same as defined above)), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
2. The compound according to 1, wherein A is a nitrogen atom, and B is a sulfur atom, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
3. The compound according to 1, wherein A is a nitrogen atom, and B is an oxygen atom, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
4. The compound according to 1, wherein A is a nitrogen atom, and B is NR9 other than NH (wherein R9 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups) or a C2?14 aryloxy group (the C2?14 aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)), atautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
5. The compound according to 1, wherein A is CR4 (wherein R4 is a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted with a C2?6 alkenyl group or a C2?6 alkynyl group), a thiol group (the thiol group may be substituted with a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group or a C1?10 alkylcarbonyl group), an amino group (the amino group may be substituted with one or two C2?6 alkenyl groups or one or two C2?6 alkynyl groups), a formyl group, a halogen atom, a nitro group, a cyano group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkylcarbonylamino group, a mono- or di-C1?10 alkylamino group, a C1?10 alkoxy group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkylcarbonylamino group, the mono- or di-C1?10 alkylamino group and the C1?10 alkoxy group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups), a C2?14 aryloxy group (the C2?14 aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups), SO2R5, SOR5 or COR5 (wherein R5 is a hydroxyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group and the C1?10 alkoxy group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkySequence Listing Electronic Form lcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups), a C2?14 aryloxy group (the C2?14 aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups) or NR6R7 (wherein each of R6 and R7 is independently a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups), or R6 and R7 mean, together with each other, ?(CH2)m1-E-(CH2)m2- (wherein E is an oxygen atom, a sulfur atom, CR26R27 (wherein each of R26 and R27 is independently a hydrogen atom, a C1?10 alkyl group, a C2?14 aryl group, a C1?10 alkoxy group, a C2?14 aryloxy group, a hydroxyl group or a protected hydroxyl group) or NR8 (wherein R8 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituenselected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)), and each of m1 and m2 is independently an integer of from 0 to 5 provided that m1+m2 is 3, 4 or 5)))), and B is an oxygen atom, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
6. The compound according to 1, wherein A is the same as defined in 5, and B is a sulfur atom, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
7. The compound according to 1, wherein A is the same as defined in 5, and B is NR9 (wherein R9 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups) or a C2?14 aryloxy group (the C2?14 aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
8. The compound according to any one of 1 to 7, wherein L1 is a bond, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
9. The compound according to any one of 1 to 8, wherein L2 is a bond, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
10. The compound according to any one of 1 to 9, wherein L3 is NR19 (wherein R19 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group, the C1?10 alkoxy group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups (the C2?14 aryl groups and the C2?14 aryloxy groups may be substituted with one or more C1?6 alkyl groups (the C1?6 alkyl groups may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C2?14 aryl group (the C2?14 aryl group may be optionally substituted with one or more substituents selected from the group consisting of: C1?10 alkyl groups (the C1?10 alkyl groups may be substituted with one or more halogen atoms), C2?6 alkenyl groups, C2?6 alkynyl groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl groups, C2?14 aryl groups and C2?14 aryloxy groups)), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
11. The compound according to any one of 1 to 10, wherein L3 is NH, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
12. The compound according to 10, wherein L4 is NR22 (wherein R22 is a hydrogen atom, a hydroxyl group, a formyl group, a C1?10 alkyl group, a C2?6 alkenyl group, a C2?6 alkynyl group, a C1?10 alkoxy group, a C1?10 alkylcarbonyloxy group, a C1?10 alkoxycarbonyl group, a C1?10 alkylcarbonyl group (the C1?10 alkyl group, the C2?6 alkenyl group, the C2?6 alkynyl group, the C1?10 alkoxy group, the C1?10 alkylcarbonyloxy group, the C1?10 alkoxycarbonyl group and the C1?10 alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: carboxyl groups, nitro groups, cyano groups, halogen atoms, C1?10 alkoxy groups, C1?10 alkylcarbonyl groups, C1?10 alkylcarbonyloxy groups, C1?10 alkoxycarbonyl groups, C1?10 alkylcarbonylamino groups, amino groups, mono- or di-C1?10 alkylamino groups, hydroxyl groups, protected hydroxyl

The present invention provides compounds useful for prevention, treatment or alleviation of diseases against which activation of the thrombopoietin receptor is effective. A compound represented by the formula (1): wherein A, B, R1, L1, R2, L2, L3, Y, L4, R3 and X are the same as defined in the description, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.