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Novel 3 5 Disubstitued 3 H Imidazo[4 5 B]Pyridine And 3 5 Disubstitued 3 H [1 2 3]Triazolo[4 5 B] Pyridine Compounds As Modulators Of Protein Kinases

Abstract: The present invention provides inter alia compounds of formula ?? ??? and III as protein kinase modulators methods of preparing them pharmaceutical compositions containing them and methods of treatment prevention and/or amelioration of kinase mediated diseases or disorders with them.

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Patent Information

Application #
Filing Date
06 December 2012
Publication Number
46/2015
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
Parent Application

Applicants

INCOZEN THERAPEUTICS PVT. LTD.
"Spectrum" Discovery Zone SP Biotech Park Phase I Shameerpet Hyderabad 500 078
RHIZEN PHARMACEUTICALS SA
Fritz Courvoisier 40 CH 2300 La Chaux de Fonds

Inventors

1. MUTHUPPALANIAPPAN Meyyappan
c/o Incozen Therapeutics Pvt. Ltd. "Spectrum" Discovery Zone SP Biotech Park Phase I Shameerpet Hyderabad 500 078
2. VISWANADHA Srikant
c/o Incozen Therapeutics Pvt. Ltd. "Spectrum" Discovery Zone SP Biotech Park Phase I Shameerpet Hyderabad 500 078
3. BABU Govindarajulu
c/o Incozen Therapeutics Pvt. Ltd. "Spectrum" Discovery Zone SP Biotech Park Phase I Shameerpet Hyderabad 500 078
4. VAKKALANKA Swaroop K. V. S.
c/o Rhizen Pharmaceuticals SA Fritz Courvoisier 40 CH 2300 La Chaux de Fonds

Specification

Claims
1. A compound of the formula
or a tautomer, stereoisomer, enantiomer, diastereomer, salt, prodrug, or N-oxide thereof, wherein
R2 is hydrogen, nitro, hydroxy, cyano, halogen, -0Ra, -S(=0) qRa, -NRaRb, -C(=0)-R a, or -C(=0)-R a, wherein Ra and Rb in the R2 group are independently hydrogen, hydroxy, or substituted or unsubstituted Ci_6 alkyl;
XisCRiorN;
Cy and Cy may be same or different and are independently selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl;
L2 is selected from -0-, -S(=0) q-, -NRa-, (CRaRb)n-, -C(=Y)-, -C(=Y)-C(=Y)-, -CRaRb-C(=Y)-CR aRb-, -CRaRb-Y-CRaRb-, -C(=Y)-NR aRb-, -NRaRb-C(=Y)-NR aRb-, -S(=0) q-NRaRb-, -NRaRb-S(=0) q-NRaRb, -NRaRb-NRaRb, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocyclyl;
RMs selected from hydrogen, nitro, hydroxy, cyano, halogen, -0Ra, -S(=0) q-Ra, -NRaRb, -C(=Y)-Ra, -CRaRb-C(=Y)-R a, -CRaRb-Y-CRaRb-, -C(=Y)-NR aRb-, -NRaRb-C(=Y)-NR aRb-, -S(=0) q-NRaRb-, -NRaRb-S(=0) q-NRaRb-, -NRaRb-NRaRb-, substituted or unsubstituted Ci_6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C3J5 cycloalkyl, substituted or unsubstituted C3J5 cycloalkylalkyl, substituted or unsubstituted C3J5 cycloalkenyl;
each occurrence of Ra and Rb may be same or different and are independently selected from hydrogen, nitro, hydroxy, cyano, halogen, substituted or unsubstituted Ci_6 alkyl, substituted

or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C3^ cycloalkyl, substituted or unsubstituted C3^ cycloalkylalkyl, and substituted or unsubstituted c3 6 cycloalkenyl, or when two Ra and/or Rb substituents are directly bound to a common atom, they may be joined to form a substituted or unsubstituted, saturated or unsaturated 3 10 member ring, which may optionally include one or more heteroatoms which may be same or different and are selected from 0, NRC or S;
each occurrence of Rc is independently selected from hydrogen, nitro, hydroxy, cyano, halogen, substituted or unsubstituted Ci_6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-e alkynyl, substituted or unsubstituted c3_6 cycloalkyl, substituted or unsubstituted C3-6 cycloalkylalkyl, and substituted or unsubstituted C3-6 cycloalkenyl;
each occurrence of Y is independently selected from 0,S,and NRa;
each occurrence of n independently represents 0, 1, 2, 3 or 4; and
each occurrence of q independently represents 0, 1 or 2.
2. A compound of claim 1, wherein Cy1 is substituted or unsubstituted aryl or
substituted or unsubstituted heteroaryl.
3. A compound of claim 1, wherein Cy * is selected from

or a tautomer, stereoisomer, enantiomer, diastereomer, salt, prodrug, or N-oxide thereof, wherein
D is substituted or unsubstituted monocyclic aryl or substituted or unsubstituted monocyclic heteroaryl;
each occurrence of R2 is independently hydrogen, nitro, hydroxy, cyano, halogen, -0Ra, -S(=0) q-Ra, -NRaRb, -C(=0)-R a, -C(=0)-R a, wherein Ra and Rb in the R2 group are independently hydrogen, hydroxy, or substituted or unsubstituted Ci_6 alkyl;
L2is-CRaRb-;and
X, Cy2, Ra, Rb, and q are as defined in claim 1.
5. A compound of claim 4, wherein, D is substituted with one to five substituents
selected from halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, -CORx, -CONRxRy, -S(0) qNRxRy or -NRxRy, wherein
each occurrence of Rx and Ry is independently selected from hydrogen, hydroxy, halogen, carboxyl, cyano, nitro, oxo (=0), thio (=S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenylalkyl, substituted or unsubstituted heterocycyl, substituted or unsubstituted heterocyclylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, -COOR z, -C(0)R z, -C(S)RZ, -C(0)NR ZR, -C(0)ONR zRz, -NRZRZ, -NRzCONRzRz, -N(Rz)SORz, -N(Rz)S0 2Rz, -

(=N-N(RZ)RZ), -NRZC(0)ORZ, -NRzC(0)R\ -NRxC(S)Ry-NRZC(S)NRZRZ, -SONRzR\ -S02NRzR\ -0RZ, -ORZC(0)NRZRZ, -ORZC(0)OR\ -OC(0)RZ, -OC(0)NRZRZ, -RzNRzC(0)Rz, -RzORz, -RZC(0)ORZ, -RzC(0)NRzRz, -RzC(0)Rz, -RZOC(0)RZ, -SRZ, -SORz, s02Rz, and -ONO 2, or any two of RX and Ry which are directly bound to a common atom may be joined to form (i) a substituted or unsubstituted, saturated or unsaturated 3-14 membered ring, which may optionally include one or more heteroatoms which may be the same or different and are selected from O, NRZ or S, or (ii) an oxo (=0), thio (=S) or imino (=NRZ);
each occurrence of Rz is independently hydrogen, hydroxy, halogen, carboxyl, cyano, nitro, oxo (=0), thio (=S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenylalkyl, substituted or unsubstituted heterocycyl, substituted or unsubstituted heterocyclcyalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, and -ONO 2, or any two of Rz which are directly bound to a common atom may bejoined to form (i) a substituted or unsubstituted, saturated or unsaturated 3-14 membered ring, which may optionally include one or more heteroatoms which may be the same or different and are selected from O, NR (where R' is H or alkyl) or S, or (ii) an oxo (=0), thio (=S) or imino (=NRZ); and
q in the group D is 0, 1 or 2.
6. A compound of claim 4 or 5, wherein D is selected from

or a tautomer, stereoisomer, enantiomer, diastereomer, salt, prodrug, or N-oxide thereof, wherein

XisCRiorN;
Cy2 is selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl;
L2is-CRaRb-;
each occurrence of R^nd R^ may be same or different and is independently selected from hydrogen, nitro, hydroxy, cyano, halogen, -0Ra, -S(=0) q-Ra, -NRaRb, -C(=Y)-R a, -CRaRb-C(=Y)-Ra, -CRaRb-Y-CRaRb-, -C(=Y)-NR aRb-, -NRaRb-C(=Y)-NR aRb-, -S(=0) q-NRaRb-, -NRaRb-S(=0) q-NRaRb,-NRaRb-NRaRb, substituted or unsubstituted Ci_6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C3_6 cycloalkyl, substituted or unsubstituted C3-6 cycloalkylalkyl, and substituted or unsubstituted C3_6 cycloalkenyl;
each occurrence of Ra and Rb may be same or different and are independently selected from hydrogen, nitro, hydroxy, cyano, halogen, substituted or unsubstituted Ci_6 alkyl, substituted or unsubstituted C2 6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C3_6 cycloalkyl, substituted or unsubstituted C3-6 cycloalkylalkyl, and substituted or unsubstituted C3-6 cycloalkenyl, or when two Ra and/or Rb substituents are directly bound to a common atom, they may be joined to form a substituted or unsubstituted, saturated or unsaturated 3 10 member ring, which may optionally include one or more heteroatoms which may be same or different and are selected from 0, NRC or S (where each occurrence of Rc here independently refers to hydrogen, nitro, hydroxy, cyano, halogen, substituted or unsubstituted Ci_6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C3_6 cycloalkyl, substituted or unsubstituted C3_6 cycloalkylalkyl, and substituted or unsubstituted C3_6 cycloalkenyl);
Rc and Rd together with the nitrogen to which they are attached form a substituted or unsubstituted, saturated or unsaturated 3 10 member ring, which may optionally include one or more heteroatoms which may be same or different and are selected from 0, NReor S;
Re is selected from hydrogen, hydroxy, halogen, carboxyl, cyano, nitro, oxo (=0), thio (=S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted

cycloalkenyl, substituted or unsubstituted cycloalkenylalkyl, substituted or unsubstituted heterocyclic ring, substituted or unsubstitituted heterocycylalkyl ring, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted guanidine, -COORx, -C(0)Rx, -C(S)Rx, -C(0)NRxRy, -C(0)ONRxRy, -NRyRz, -NRxCONRyRz, -N(Rx)SORy, -N(Rx)S02Ry, -(=N-N(Rx)Ry), - NRxC(0)ORy, -NRxRy, -NRxC(0)Ry-, -NRxC(S)Ry, -NRxC(S)NRyRz, -SONRxRy-, -S02NRxRy-, -ORx, -ORxC(0)NRyRz, -ORxC(0)ORy-, -OC(0)RX, -OC(0)NRxRy, - RxNRyC(0)Rz, -RxORy, -RxC(0)ORy, -RxC(0)NRyRz, -RxC(0)Rx, -RxOC(0)Ry, -SRx, -SORx, -S02Rx, and -ON02, wherein each occurrence of Rx, Ry and Rz is independently hydrogen, substituted or unsubstituted amino, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenylalkyl, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocyclylalkyl ring, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, and substituted or unsubstituted heteroarylalkyl, or any two of Rx, Ry and Rz which are directly bound to a common atom may be joined to form (i) an oxo (C=0), thio (C=S) or imino (C=NR) group (where R' is H or alkyl) or (ii) substituted or unsubstituted, saturated or unsaturated 3-10 membered ring, which may optionally include one or more heteroatoms which may be the same or different and are selected from O, NR (where R' is H or alkyl) or S;
each occurrence of Y is independently selected from O, S, and NRa; and
each occurrence of q independently represents 0, 1 or 2.
8. A compound of claim 7, wherein NRcRd is selected from

wherein each occurrence of Rx and Ry is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, or any two of Rx and Ry which are directly bound to a common atom may be joined to form an oxo (C=0), thio (C=S) or imino (C=NR') group (where R' is H or alkyl), or any two of Rx and Ry may be joined to form a substituted or unsubstituted, saturated or unsaturated 3-6 membered ring, which may optionally include heteroatoms which may be the same or different and are selected from O, NR' (where R' is H or alkyl) or S.
9. A compound of claim 8, wherein NRcRd is selected from

or a tautomer, stereoisomer, enantiomer, diastereomer, salt, prodrug, or N-oxide thereof, wherein
XisCRiorN;
U and V are each independently selected from CR3 or N;
W is selected from O, S, or NR4;
each occurrence of R*and R may be same or different and is independently selected from hydrogen, nitro, hydroxy, cyano, halogen, -ORa, -S(=0) q-Ra, -NRaRb, -C(=Y)-Ra, -CRaRb-C(=Y)-Ra, -CRaRb-Y-CRaRb-, -C(=Y)-NRaRb-, -NRaRb-C(=Y)-NRaRb-, -S(=0) q-NRaRb-, -NRaRb-S(=0) q-NRaRb-, -NRaRb-NRaRb-, substituted or unsubstituted Ci_6 alkyl, substituted or unsubstituted C2 6 alkenyl, substituted or unsubstituted C2 6 alkynyl, substituted or unsubstituted C3_6 cycloalkyl, substituted or unsubstituted C3_6 cycloalkylalkyl, and substituted or unsubstituted C3_6 cycloalkenyl;
R4 is selected from hydrogen, hydroxy, carboxyl, cyano, oxo (=0), thio(=S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted C3 6 cycloalkyl, substituted or unsubstituted C3_6 cycloalkylalkyl, and substituted or unsubstituted C3_6 cycloalkenyl;
each occurrence of R3 is independently hydrogen, halogen, cyano (CN), -ORc, -S(=0) q-Rc, -NRcRd, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted C3^ cycloalkyl, substituted or unsubstituted C3_6 cycloalkylalkyl, or substituted or unsubstituted C3_6 cycloalkenyl;
R5 is selected from hydrogen, hydroxy, halogen, carboxyl, cyano, nitro, oxo (=0), thio (=S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocyclylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted guanidine, -COORx, -C(0)Rx, -C(S)Rx, -C(0)NRxRy, -C(0)ONRxRy, -NRxRy, -NRxCONRyRz, -N(Rx)SORy, -N(Rx)S02Ry, -(=N-N(Rx)Ry), -NRxC(0)ORy, -NRxC(0)Ry-, -NRxC(S)Ry-NRxC(S)NRyRz, -SONRxRy-, -S02NRxRy-, -ORx,

-ORXC(0)NR yRz, -ORXC(0)OR V-, -OC(0)R x, -OC(0)NR xRy, -RxNRyC(0)R z, -RxORy, -RXC(0)OR y -RxC(0)NR yRz, -RxC(0)R x, -RXOC(0)R y, -SRX, -SORx, -SO 2RX, and -ON0 2;
or optionally when W is NR4, R4 and R5 together with the nitrogen to which they are attached form a substituted or unsubstituted, saturated or unsaturated 3 10 member ring, which may optionally include one or more heteroatoms which may be same or different and are selected from 0,NReorS;
Cy is selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl;
L2 is selected from -0-, -S(=0) q-, -NRa-, (CRaRb)n-, -C(=Y)-, -C(=Y)-C(=Y)-, -CRaRb-C(=Y)-CR aRb-, -CRaRb-Y-CRaRb-, -C(=Y)-NR aRb-, -NRaRb-C(=Y)-NR aRb-, -S(=0) q-NRaRb-, -NRaRb-S(=0) q-NRaRb, -NRaRb-NRaRb, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocyclyl;
each occurrence of Ra and Rb may be same or different and are independently selected from hydrogen, nitro, hydroxy, cyano, halogen, substituted or unsubstituted Ci_6 alkyl, substituted or unsubstituted C2j, alkenyl, substituted or unsubstituted C2 6 alkynyl, substituted or unsubstituted c3_6 cycloalkyl, substituted or unsubstituted C3-6 cycloalkylalkyl, and substituted or unsubstituted C3-6 cycloalkenyl, or when two Ra and/or Rb substituents are directly bound to a common atom, they may be joined to form a substituted or unsubstituted, saturated or unsaturated 3 10 member ring, which may optionally include one or more heteroatoms which may be same or different and are selected from 0, NRC or S;
each occurrence of Rc, Rd, and Re are independently selected from hydrogen, hydroxy, halogen, carboxyl, cyano, nitro, oxo (=0), thio (=S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenylalkyl, substituted or unsubstituted heterocyclic ring, substituted or unsubstitituted heterocycylalkyl ring, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted guanidine, -COOR x, -C(0)R X, -C(S)Rx, -

C(0)NRxRy, -C(0)ONRxRy, -NRyRz, -NRxCONRyRz, -N(Rx)SORy, -N(Rx)S02Ry, -(=N-N(Rx)Ry), - NRxC(0)ORy, -NRxRy, -NRxC(0)Ry-, -NRxC(S)Ry -NRxC(S)NRyRz, -SONRxRy-, -S02NRxRy-, -0RX, -ORxC(0)NRyRz, -ORxC(0)ORy-, -OC(0)RX, -OC(0)NRxRy, -RxNRyC(0)Rz, -RxORy, -RxC(0)ORy, -RxC(0)NRyRz, -RxC(0)Rx, -RxOC(0)Ry, -SRX, -SORx)-S02Rx)and-ON02;
each occurrence of Rx, Ry and Rz is independently hydrogen, substituted or unsubstituted amino, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenylalkyl, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocyclylalkyl ring, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, and substituted or unsubstituted heteroarylalkyl, or any two of Rx, Ry and Rz which are directly bound to a common atom may be joined to form (i) an oxo (C=0), thio (C=S) or imino (C=NR') group (where R' is H or alkyl) or (ii) substituted or unsubstituted, saturated or unsaturated 3-10 membered ring, which may optionally include one or more heteroatoms which may be the same or different and are selected from 0, NR' (where R' is H or alkyl) or S;
each occurrence of Y is independently selected from O, S, and NRa;
each occurrence of n independently represents 0, 1, 2, 3 or 4; and
each occurrence of q independently represents 0, 1 or 2.
11. A compound of claim 10, wherein U is CR3.
12. A compound of claim 10 or ll, wherein V is N.
13. A compound of any of claims 10-12, wherein W is O or NR4.
14. A compound of claim 10, wherein -U=V-W-R 5is selected from

18. A compound of any one of claims 1-17, wherein X is CR1.
19. A compound of any one of claims 1-17, wherein X is N.
20. A compound of any one of claims 1-19, wherein R1 is H.
21. A compound of any one of claims 1-20, wherein each occurrence of R2 is H.
22. A compound of any one of claims 1-21, wherein L2 is -CRaCRb-.
23. A compound of claim 22, wherein L2 is -CH 2-, -CH(OH)-, -CHF-, -CF2-, -CH
(CH3)-or-C(CH3)r.
24. A compound of claim 22, wherein L2 is -CH 2- or -CH (CH3)-.
25. A compound of any one of claims 1-24, wherein Cy2 is substituted or
unsubstituted aryl or substituted or unsubstituted heteroaryl.
26. A compound of claim 25, wherein Cy2 is selected from

or a tautomer, stereoisomer, enantiomer, diastereomer, salt, prodrug, or N-oxide thereof, wherein
B is selected from Cy1, -NRcRd or -U=V-W-R 5;
Cy1 is selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl;
XisCRiorN;
R * is selected from hydrogen, nitro, hydroxy, cyano, halogen, -0Ra, -S(=0)q-Ra, -NRaRb, -C(=Y)-Ra, -CRaRb-C(=Y)-R a, -CRaRb-Y-CRaRb-, -C(=Y)-NR aRb-, -NRaRb-C(=Y)-NR aRb-, -S(=0)q-NRaRb-, -NRaRb-S(=0)q-NRaRb-, -NRaRb-NRaRb-, substituted or unsubstituted Ci_6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C26 alkynyl, substituted or unsubstituted C3_6 cycloalkyl, substituted or unsubstituted C3_6 cycloalkylalkyl, substituted or unsubstituted C3_6 cycloalkenyl;
R2 is hydrogen, nitro, hydroxy, cyano, halogen, -ORa,-S(=0) -Ra,-NRaRb, - C(=0)-Ra, or-C(=0)-Ra, wherein Ra and Rb in the R2 group are independently hydrogen, hydroxy, or substituted or unsubstituted Ci_6 alkyl;
each occurrence of Ra and Rb may be same or different and are independently selected from hydrogen, halogen, or substituted or unsubstituted (Ci-e) alkyl, or both together with the carbon atom to which they are attached form a saturated 3 to 6 member cyclic ring which may optionally include heteroatoms which may be same or different and are selected from 0, NReorS;

Rc and Rd together with the nitrogen to which they are attached form a substituted or unsubstituted, saturated or unsaturated 3-10 member ring, which may optionally include one or more heteroatoms which may be same or different and are selected from O, NRe or S;
Re is selected from hydrogen, hydroxy, halogen, carboxyl, cyano, nitro, oxo (=0), thio (=S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenylalkyl, substituted or unsubstituted heterocyclic ring, substituted or unsubstitituted heterocycylalkyl ring, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted guanidine, -COORx, -C(0)Rx, -C(S)Rx, -C(0)NRxRy, -C(0)ONRxRy, -NRyRz, -NRxCONRyRz, -N(Rx)SORy, -N(Rx)S02Ry, -(=N-N(Rx)Ry), - NRxC(0)ORy, -NRxRy, -NRxC(0)Ry-, -NRxC(S)Ry, -NRxC(S)NRyRz, -SONRxRy-, -S02NRxRy-, -ORx, -ORxC(0)NRyRz, -ORxC(0)ORy-, -OC(0)RX, -OC(0)NRxRy, - RxNRyC(0)Rz, -RxORy, -RXC(0)OR y, -RxC(0)NR yRz, -RxC(0)R x, -RXOC(0)R y, -SRX, -SORx, -SO 2RX, and -ON0 2;
each occurrence of Rx, Ry and Rz is independently hydrogen, substituted or unsubstituted amino, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenylalkyl, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocyclylalkyl ring, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, and substituted or unsubstituted heteroarylalkyl, or any two of Rx, Ry and Rz which are directly bound to a common atom may be joined to form (i) an oxo (C=0), thio (C=S) or imino (C=NR) group (where R' is H or alkyl) or (ii) substituted or unsubstituted, saturated or unsaturated 3-10 membered ring, which may optionally include one or more heteroatoms which may be the same or different and are selected from O, NR (where R' is H or alkyl) or S;
U and V are each independently selected from CR3 or N;
W is selected from O, S, or NR4;

each occurrence of R3 is independently hydrogen, halogen, cyano (CN), -ORc, -S(=0) q-Rc, -NRcRd, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted C3 6 cycloalkyl, substituted or unsubstituted C3_6 cycloalkylalkyl, or substituted or unsubstituted C3_6 cycloalkenyl;
R4 is selected from hydrogen, hydroxy, carboxyl, cyano, oxo (=0), thio (=S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted C3_6 cycloalkyl, substituted or unsubstituted C3_6 cycloalkylalkyl, and substituted or unsubstituted C3_6 cycloalkenyl;
R5 is selected from hydrogen, hydroxy, halogen, carboxyl, cyano, nitro, oxo (=0), thio (=S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocyclylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted guanidine, -COORx, -C(0)Rx, -C(S)Rx, -C(0)NRxRy, -C(0)ONRxRy, -NR*RZ, -NRxCONRyRz, -N(Rx)SORy, -N(Rx)S02Ry, -(=N-N(Rx)Ry), -NRxC(0)ORy, -NRxC(0)Ry-, -NRxC(S)Ry-NRxC(S)NRyRz, -SONRxRy-, -S02NRxRy-, -0Rx, -ORC^NR^, -ORxC(0)ORy-, -OC(0)RX, -OC(0)NRxRy, -RxNRyC(0)Rz, -RxORy, -RxC(0)ORy, -RxC(0)NRyRz, -RC^R X, -RxOC(0)Ry, -SRX, -SORx, -SO 2RX, and -ON0 2;
or when W is NR4, R4 and R5 together with the nitrogen to which they are attached form a substituted or unsubstituted, saturated or unsaturated 3-10 member ring, which may optionally include one or more heteroatoms which may be same or different and are selected fromO,NReorS;
Z is selected from CRC, S, O, NRC, RCC=CRC , -N=CRC-, -RCC=N-;
Zi is selected from N, NRC or CRC;
each occurrence of Y is independently selected from O, S, and NRa;
each occurrence of n independently represents 0, 1, 2, 3 or 4; and
each occurrence of q independently represents 0, 1 or 2.
Rc is absent or selected from hydrogen, hydroxy or halogen;

29. The compound of claim 28, wherein X is N.
30. The compound of claim 28 or 29, wherein each occurrence ofR2isH.
31. The compound of any one of claim 28-30, wherein each of Raand Rb are same
or different and selected from hydrogen, methyl or fluoro.
32. The compound of claim 31, wherein each of Ra and Rb is selected from
hydrogen or methyl.
33. The compound of any one of claim 28-32, wherein Z is CRC, N, S, O,
HC=CH-, -N=CH-;
34. The compound of any one of claim 28-33, wherein Zi is CH or N.
35. The compound of any one of claim 33-34, wherein Z is -HC=CH-, -S- or -0-
and ZL is CH.
36. The compound of claim 35, wherein Z is -HC=CH- and Zt is CH.
37. The compound of claim 33-34, wherein Z is -S- and Zl is CH.
38. The compound of claim 28-36, wherein each occurrence of Rc is hydrogen or
fluoro.
39. The compound of claim 28-37, wherein B is Cy*.
40. The compound of claim 39, wherein Cy1 is selected from

41. The compound of any one of claim 28-37, wherein Cy1 is substituted or
unsubstituted monocyclic aryl or substituted or unsubstituted monocyclic heteroaryl.
42. The compound of claim 41, wherein Cy1 is substituted monocyclic aryl.
c d
43. The compound of any one of claim 28-37, wherein B is NR R .
44. The compound of any one of claim 43, wherein wherein NRcRd is selected
from
wherein each occurrence of Rx and Ry is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, or any two of Rx and Ry which are directly bound to a common atom may be joined to form an oxo (C=0), thio (C=S) or imino (C=NR') group (where R' is H or alkyl), or any two of Rx and Ry may be joined to form a substituted or unsubstituted, saturated or unsaturated 3-6 membered ring, which may optionally include heteroatoms which may be the same or different and are selected from 0, NR' (where R' is H or alkyl) or S.
45. The compound of any one of claims 28-37, wherein B is -U=V-W-R5.
46. The compound of claim 45, wherein -U=V-W-R5 is same as defined in claim
9.
47. A compound selected from
6-((5-(4-Methoxyphenyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl)quinoline
6-((5-(3-Methoxyphenyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl)quinoline
3-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzaldehyde
(3-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)phenyl)methanol
4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzaldehyde

(4-(3-(quinolin-6-ylmethyl)-3H-[l,23]triazolo[4,5-b]pyridin-5-yl)phenyl)methanol
Methyl 4-(3-(quinolin-6-ylmethyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl)benzoate
4-(3-(quinolin-6-ylmethyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl)benzoic acid
N-Methyl-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzamide
4-(3-(4-Fluorobenzyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl) benzaldehyde
(4-(3-(4-Fluorobenzyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl)phenyl)methanol
Methyl 2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-yl) benzoate
2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-yl)benzoic acid
2-Fluoro-N-methyl-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl) benzamide
2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzamide
(2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)phenyl) methanol
Methyl 4-(3-(2-chloro-3,6-difluorobenzyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)-2-fluoro benzoate
4-(3-(2-Chloro-3,6-difluorobenzyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl)-2-fluoro benzoic acid
4-(3-(2-Chloro-3,6-difluorobenzyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl)-2-fluoro-N-methyl benzamide
N-(2-Hydroxyethyl)-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
4- (3- (quinolin-6-ylmethyl) -3H- [1,2,3] triazolo [4,5-b] pyridin- 5-yl) benzamide
Lithium 4-(3-(quinolin-6-ylmethyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl)benzoate
6-((5-(3-(trifluoromethoxy)phenyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl)quinoline
3- (3-(quinolin-6-ylmethyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl) phenol
6-((5-(3-(difluoromethoxy)phenyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
(4-Methylpiperazin-l-yl)(4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl) phenyl) methanone

N-(2-(dimethylamino)ethyl)-4-(3-(qumA lin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzamide
4-(3-(quinolin-6-ylmethyl)-3H-[l ,23] triazolo [4,5-b]pyridin-5-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide
tert-Butyl 4- (4- (3- (quinolin-6-ylmethyl) -3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl)
benzamido) piperidine- 1 -carboxylate
N-(Bperidin-4-yl)-4-(3-(quinolin-6-ylme%l)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide hydrochloride
N-(2-(dimethylamino)ethyl)-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo [4,5-b]
pyridin- 5-yl) benzamide
(S)-(2-(pyrrolidin- l-ylmethyl)pyrrolidin- l-yl)(4-(3-(quinolin-6-ylmethyl)-3H- [1,2,3] triazolo [4,5-b] pyridin- 5-yl) phenyl) methanone hydrochloride
(4-(2-hydroxyethyl)piperazin-l-yl)(4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin- 5-yl) phenyl) methanone
(R)-(3-hydroxypyrrolidin-l-yl) (4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-
5 -yl) phenyl) methanone hydrochloride
N-(2-(piperidin-l-yl)ethyl)-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-
yl) benzamide
N-(2-morpholinoethyl)-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
N-(2-(pyrrolidin-l-yl)ethyl)-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-
yl) benzamide
(4- (pyrrolidin-l-yl)piperidin-l-yl) (4- (3- (quinolin-6-ylmethyl) -3H- [1,2,3] triazolo [4 ,5-b]
pyridin- 5-yl) phenyl) methanone
N-(3-(dimethylamino)propyl)-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-
yl) benzamide
N,N-Bis(2-methoxyethyl)-4-(3-(quinolin-6-ylmethyl)-3H41,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide hydrochloride

(2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) phenyl) methanol hydrochloride
6-((5-(3-Fluoro-4-(methoxymethyl)phenyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl) methyl) quinoline
N-ethyl-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
2-Fluoro-N-(2-(pyrrolidin4-yl)ethyl)-4-(3-(quinolin-6-ylmethyl)-3H-[l)2,3]triazolo [4,5-b]
pyridin-5-yl) benzamide
N-cyclohexyl-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
N-Cyclopropyl-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo[4,5-b] pyridin-5-yl) benzamide
2-Fluoro-N-(pyridin-4-yl)-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-
yl) benzamide
N-Benzyl-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
2-Fluoro-N,N-dimethyl-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
Methyl 2-(2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)
benzamido)acetate.
2-(2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamido)acetic acid
2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)-N-(lH-l,2,4-triazol-3-yl)benz amide
Methyl 3-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzoate
3-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzoic acid
N-Methyl-3-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
6-((5-(3-Fluorophenyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl)quinoline

Methyl 3-(2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) phenyl amino) propanoate
3-(2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) phenylamino) propanoic acid
2-Fluoro-N-methoxy-N-methyl-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-yl) benzamide hydrochloride
N-tert-Butyl-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l)2)3]triazolo[4,5-b]pyridin-5-yl) benzamide
N-Allyl-2-nuoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
2-Fluoro-N-methoxy-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
N-(4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)phenyl) acetamide
4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)aniline
6-((5-(3,4-Dimethoxyphenyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl)quinoline
6-((5-(3-Fluoro-4-methoxyphenyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
6-((5-(4-Fluorophenyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl)quinoline
6-((5-(2-Fluorophenyl)-3H-[1,2,3] triazolo [4,5-b]pyridin-3-yl)methyl) quinoline
N-(3-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)phenyl) acetamide
6-((5-(3-(2,2,2-Trifluoroethoxy)phenyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
3-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)aniline
N-(3-(dimethylamino)propyl)-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b]pyridin-5-yl)benzamide
N-Ethyl-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide hydrochloride
2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b]pyridin-5-yl)benzamide hydrochloride

6-((5-(3-Fluoro-4-isopropoxyphenyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
N-(3-(dimethylamino)-3-oxopropyl)-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b]pyridin-5-yl)benzamide
N-(2-(dimethylamino)-2-oxoethyl)-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b]pyridin-5-yl)benzamide
2 -Fluoro-N- (2-oxo-2- (pyrrolidin-1-yl) ethyl) -4- (3- (quinolin-6-ylmethyl) -3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl)benzamide
6- ((5- (4- (Cyclopropylmethoxy) -3-fluorophenyl) -3H- [1,2,3] triazolo [4,5-b] pyridin-3-yl) methyl) quinoline
6-((5-(3-Fluoro-4-isobutoxyphenyl)-3H- [1,2,3]triazolo[4,5-b]pyridin-3-yl) methyl)quinoline
3-(2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) phenoxy)-
N,N-dimethylpropan- 1-amine
Methyl 2-fluoro-4-(3-(2-(quinolin-6-yl)propan-2-yl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl) benzoate
2-Fluoro-4-(3-(2-(quinolin-6-yl)propan-2-yl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl) benzoic acid
2-Fluoro-4-(3-(2-(quinolin-6-yl)propan-2-yl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl) benzamide
6-((5-(3-Fluoro-4-(tetrahydro-2H-pyran-4-yloxy)phenyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-3-yl) methyl) quinoline
6-((5-(3-Fluoro-4-(2-methoxyethoxy)phenyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-3-yl) methyl) quinoline
2-Fluoro-N-propyl-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl) benzamide
6-((5-(4-(Cyclopropylcarbamoyl)-3-fluorophenyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-3-yl) methyl) quinoline 1-oxide
N-Cyclopropyl-2-fluoro-4- (3- (quinolin-6-ylmethyl) -3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl) benzamide hydrochloride

N-(Cyclopropylmethyl)-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-yl)benzamide
N-Butyl-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2)3]triazolo[4,5-b]pyridin-5-yl) benzamide
2-Fluoro-N-(furan-2-ylmethyl)-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-yl)benzamide
2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2)3]triazolo[4)5-b]pyridin-5-yl)-N-(2)2,2-trifluoroethyl) benzamide
2-Fluoro-N-(2-methoxyethyl)-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-yl) benzamide
N-Isopropyl-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzenesulfonamide
N,N-Dimethyl-3-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) aniline
2-Fluoro-N-isobutyl-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
N-Cyclopentyl-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
2-Fluoro-N-isopropyl-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo[4,5-b] pyridin-5-yl) benzamide
Methyl 2-chloro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzoate
2-Chloro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzoic acid
2-Chloro-N-propyl-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo[4,5-b] pyridin-5-yl) benzamide
2-Fluoro-N-methyl-4-(3-(2-(quinolin-6-yl)propan-2-yl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-yl) benzamide
N-Cyclobutyl-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-
yl) benzamide
2-Fluoro-N-propyl-4-(3-(2-(quinolin-6-yl)propan-2-yl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-yl) benzamide

N-Cyclopropyl-2-fluoro-4-(3-(2-(quinolin-6-yl)propan-2-yl)-3H-[l,2,3]triazolo [4,5-b]
pyridin-5-yl) benzamide:
N-Ethyl-2-fluoro-4-(3-(2-(quinolin-6-yl)propan-2-yl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-
yl) benzamide
2-Chloro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide:
2-Chloro-N-methyl-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
2-Fluoro-N-methoxy-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide hydrochloride
2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)-N- (thiazol-2-
yl) benzamide
N- (3-Aminopropyl) -2-fluoro-4- (3- (quinolin-6-ylmethyl) -3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl) benzamide
2-Chloro-N-cyclopropyl-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-
yl) benzamide
2-Fluoro-N-(3-oxo-3-(pyrrolidin-l-yl)propyl)-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3] triazolo [4,5-b] pyridin-5 -yl)benzamide
2-Fluoro-N-hydroxy-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
N-Isopropyl-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
2-Fluoro-N- (3-oxo-3-(piperidin-l-yl) propyl) -4- (3- (quinolin-6-ylmethyl) -3H- [1,2,3] triazolo [4,5-b] pyridin-5 -yl)benzamide
l-Ethyl-3-(4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-yl) phenyl) urea
2-Chloro-N-ethyl-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
2-Fluoro-N-(3-morpholino-3-oxopropyl)-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo[4,5-b]pyridin-5-yl) benzamide
N- (3- (dimethylamino) propyl) -2-fluoro-4- (3- (quinolin-6-ylmethyl) -3H- [1,2,3] triazolo [4,5-
b] pyridin-5-yl)benzamide dihydrochloride

2-chloro-4-(3-(quinolin-6-ylmethyl)-3H-[l)2)3]Mazolo[4)5-b]pyridin-5-yl)-N-(lH-l)2,4-triazol-3-yl)benz amide
2-Chloro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
hydrochloride
2-Fluoro-N-(3-(piperidin-l-yl)propyl)-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo[4,5-
b]pyridin-5-yl) benzamide
N-(3-Aminopropyl)-2-fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-yl) benzamide dihydrochloride
2-Chloro-N-(3-(dimethylamino)propyl)-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo[4,5-b]pyridin-5-yl)benzamide dihydrochloride
2-Ruoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]Mazolo[4,5-b]pyridin-5-yl)-N-(lH-l,2,4-triazol-3-yl)benzamide hydrochloride
Methyl 2,6-difluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)
benzoate
2,6-Difluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzoic acid
2,6-Difluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
Methyl 2-chloro-4-(3-((7-fluoroquinolin-6-yl)methyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-yl) benzoate
2-Chloro-4-(3-((7-fluoroquinolin-6-yl)methyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzoic acid
2-Chloro-N-ethyl-4-(3-((7-fluoroquinolin-6-yl)methyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-yl) benzamide
2-Chloro-4-(3-((7-fluoroquinolin-6-yl)methyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
Methyl 2-fluoro-4-(3-((7-fluoroquinolin-6-yl)methyl)-3H-[l,2,3]triazolo[4,5-b] pyridin-5-yl) benzoate
2-Fluoro-4-(3-((7-fluoroquinolin-6-yl)methyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzoic acid

2-Fluoro-4-(3-((7-fluoroquinolin-6-yl)methyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
3-(3-(Quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzamide
2,6-Difluoro-4- (3- (quinolin-6-ylmethyl) -3H- [1,23] triazolo [4,5-b] pyridin-5-yl) benzamide hydrochloride
2-Chloro-4-(3-((7-fluoroquinolin-6-yl)methyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl) benzamide hydrochloride
2-Fluoro-4-(3-((7-fluoroquinolin-6-yl)methyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl) benzamide hydrochloride
2-Methyl-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
Methyl 2-fluoro-5-(3-(quinolin-6-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-yl) benzoate
2-Fluoro-5-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzoic acid
2-Fluoro-5-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
2-Chloro-4- (3- ((5,7-difluoroquinolin-6-yl) methyl) -3H- [1,2,3] triazolo [4,5-b] pyridin-5-
yl) benzamide
4-(3-(Benzo[d]thiazol-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)-2-chloro benzamide
2-(2-Fluoro-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) phenyl) pro pan- 2-ol
2-Chloro-5-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl) benzamide
2-Chloro-4-(3-(l-(quinolin-6-yl)ethyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl)benzamide
2-Chloro-4-(3-(quinolin-6-ylmethyl)-3H-imidazo[4,5-b]pyridin-5-yl)benz amide
(-)-2-Chloro-4-(3-(l-(quinolin-6-yl)ethyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl)benzamide
(+)-2-Chloro-4-(3-(l-(quinolin-6-yl)ethyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl)benzamide
4-(3-(quinolin-6-ylmethyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl)-2-(trifluoromethyl) benzamide6-((5-(4-carbamoyl-3-chlorophenyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-3-yl) methyl) quinoline 1-oxide

2-chloro-N-ethyl-4-(3-(quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)benzamide hydrochloride
6-((5-(4-carbamoyl-3-chlorophenyl)-3H-[l ,2,3]triazolo[4,5-b]pyridin-3-yl)methyl)quinoline 1-oxide
and pharmaceutically acceptable salts thereof.
48. A compound selected from
6-((5-(lH-Pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl)quinoline
6-((5-(l-Methyl-lH-pyrazol-4-yl)-3H-[l,2)3]triazolo[4,5-b]pyridin-3-yl) methyl) quinoline
6-((5-(l-(2-(Tetrahydro-2H-pyran-2-yloxy)ethyl)-lH-pyrazol-4-yl)-3H-[l)2)3]triazolo[4,5-b] pyridin-3-yl) methyl) quinoline
2-(4-(3-(Quinolin-6-ylmethyl)-3H-[l)2)3]triazolo[4,5-b]pyridin-5-yl)-lH-pyrazol-l-yl) ethanol
6-((5-(lH-Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-3-yl)methyl)quinoline
6-((5-(l-Methyl-lH-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-3-yl)methyl)quinoline
6-((5-(l-(2-(Tetrahydro-2H-pyran-2-yloxy)ethyl)-lH-pyrazol-4-yl)-3H-imidazo [4,5-b]
pyridin-3-yl) methyl)quinoline
2-(4-(3-(Quinolin-6-ylmethyl)-3H-imidazo[4,5-b]pyridin-5-yl)-lH-pyrazol-l-yl) ethanol
6-((5-(lH-Imidazol-l-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl)quinoline
6-((5-(l-Propyl-lH-pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
Ethyl 2-(4-(3-(quinolin-6-ylmethyl)-3H-[l)2)3]triazolo[4,5-b]pyridin-5-yl)-lH-pyrazol-l-yl) acetate
2-(4-(3-(Quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)-lH-pyrazol-l-yl) acetic acid
tert-Butyl 4-(4-(3-(quinolin-6-ylmethyl)-3H-[l)2)3]triazolo[4,5-b]pyridin-5-yl)-lH-pyrazol-l-yl)piperidine- 1-carboxylate
6-((5-0-(Piperidin-4-yl)-lH-pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl) methyl)
quinoline
3-(4-Fluorobenzyl)-5-(lH-pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b]pyridine

3-(4-Fluorobenzyl)-5-(l-(2-(tetrahydro-2H-pyran-2-yloxy)ethyl)-lH-pyrazol-4-yl)-3H-[1,2,3] triazolo [4,5-b] pyridine
2-(4-(3-(4-Fluorobenzyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)-lH-pyrazol-l-yl) ethanol
6- (1- (5- (lH-Pyrazol-4-yl) -3H- [1,2,3] triazolo [4,5-b] pyridin-3-yl) ethyl) quinoline
6-(l-(5-(l-(2-(Tetrahydro-2H-pyran-2-yloxy)ethyl)-lH-pyrazol-4-yl)-3H-[l,2,3] triazolo[4,5-b] pyridin-3-yl) ethyl) quinoline
2-(4-(3-(l-(Quinolin-6-yl)ethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)-lH-pyrazol-l-yl) ethanol
2-(4-(3-(2-Chloro-3,6-difluorobenzyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)-lH-pyrazol-l-yl) ethanol
tert-Butyl 4-(4-(3-(2-chloro-3,6-difluorobenzyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)-lH-pyrazol- l-yl)piperidine- 1-carboxylate
3-(2-Chloro-3,6-difluorobenzyl)-5-(l-(piperidin-4-yl)-lH-pyrazol-4-yl)-3H-[l,2,3] triazolo [4,5-b] pyridine hydrochloride
6-((5-(3-Methyl-lH-indazol-6-yl)-3H- [1,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
6-((5-(lH-Indol-5-yl)-3H-[1,2,3] triazolo [4,5-b] pyridin-3-yl) methyl) quinoline
6-((5-(lH-Indol-6-yl)-3H- [1,2,3] triazolo [4,5-b] pyridin-3-yl) methyl) quinoline
6-((5-(2-Chloropyridin-4-yl)-3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
6-((5-(3-Methyl-lH-indazol-5-yl)-3H- [1,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
6- ((5- (Pyridin-3-yl) -3H- [1,2,3] triazolo [4,5-b] pyridin-3-yl) methyl) quinoline
(5)-6-((5-(l-(Pyrrolidin-3-yl)-lH-pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl) methyl) quinoline
(5)-6-((5-(l-(Pyrrolidin-3-yl)-lH-pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl) methyl) quinoline hydrochloride
4 - (2- (4- (3- (Quinolin-6-ylmethyl) -3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl) -lH-pyrazol-1-yl) ethyl) morpholine hydrochloride
6-((5-(l-(Tetrahydro-2H-pyran-4-yl)-lH-pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b] pyridin-3-yl) methyl) quinoline

6-((5-(l-(2-Hydroxyethyl)-lH-pyrazol-4-yl)-3H-[l,2)3]triazolo[4,5-b]pyridin-3-yl) methyl) quinoline 1-oxide
6-((5-(l,3-Dimethyl-IH-indazol-6-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl) methyl)
quinoline
5-(3-(Quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)pyrimidin-2-amine
tert-Butyl 3-ethyl-6-(3-(quinolin-6-ylmethyl)-3H-[l,2)3]triazolo[4,5-b]pyridin-5-yl)-lH-
indazole- 1-carboxylate
4-(3-(Quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)thiophene-2-carbaldehyde
6-((5-(2-Methoxypyrimidin-5-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
6-((5-(Benzo[d][l,3]dioxol-5-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
6-((5-(2,3-Dihydrobenzofuran-5-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
5-(3-(Quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)pyridin-2-amine
6-((5-(l-(2-fluoroethyl)-lH-pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl) methyl)
quinoline
(4-(3-(Quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)thiophen-2-yl) methanol
6-(2-(5-(l-(2-(Tetrahydro-2H-pyran-2-yloxy)ethyl)-lH-pyrazol-4-yl)-3H-[l,2,3] triazolo
[4,5-b] pyridin-3-yl)propan-2-yl)quinoline
2-(4-(3-(2-(Quinolin-6-yl)propan-2-yl)-3H-[1,2,3] triazolo [4,5-b]pyridin-5-yl)-lH-pyrazol-l-yl) ethanol
6-((5-(3-ethyl-lH-indazol-6-yl)-3H-[1,2,3] triazolo[4,5-b] pyridin-3-yl)methyl) quinoline
6-(2-(5-(lH-Pyrazol-4-yl)-3H-[1,2,3] triazolo [4,5-b] pyridin-3-yl)propan-2-yl) quinoline
6-((5-(4-Methylthiophen-2-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
6-((5-(5-Methylthiophen-2-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
4-(5-(3-(Quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b] pyridin-5-yl)pyridin-2-yl) morpholine
6-((5-(6-(Piperidin-l-yl)pyridin-3-yl)-3H-[1,2,3] triazolo [4,5-b] pyridin-3-yl) methyl)
quinoline
6-((5-(l-Ethyl-lH-pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl) methyl) quinoline

6-((5-(l-Isopropyl-lH-pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl) methyl) quinoline
6-((5-(l-Isobutyl-lH-pyrazol-4-yl)-3H-[l,2,3]triazolo[4,5-b]pyridin-3-yl)methyl) quinoline
1 - (Pyn-olidin4-yl) -2- (4- (3- (quinolin-6-ylmethyl) -3H41,23] triazolo [4,5-b] pyridin-5-yl) -1H-pyrazol- l-yl)ethanone
6-((5-(l-(2-Methoxyethyl)-lH-pyrazol-4-yl)-3H-[l,2)3]triazolo[4,5-b]pyridin-3-yl) methyl) quinoline
3-(2-Chloro-3,6-difluorobenzyl)-5-(lH-pyrazol-4-yl)-3H-[1,2,3] triazolo [4,5-b] pyridine
6-((5-(3-methyl-lH-pyrazol-4-yl)-3H- [1,2,3] triazolo [4,5-b]pyridin-3-yl)methyl)quinoline
and pharmaceutically acceptable salts thereof.
49. A compound selected from
2-(3-(Quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-ylamino)ethanol
N-Phenyl-3-(quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b]pyridin-5-amine
6-((5-Phenoxy-3H-[1,2,3] triazolo [4,5-b]pyridin-3-yl)methyl)quinoline
l-(3-(Quinolin-6-ylmethyl)-3H-[1,2,3] triazolo [4,5-b]pyridin-5-yl)ethanone
and pharmaceutically acceptable salts thereof.
50. A compound selected from
(R)-l-(3-(Quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)pyrrolidin-3-ol
6-((5-(4-Methylpiperazin-l-yl)-3H-[1,2,3] triazolo [4,5-b]pyridin-3-yl)methyl) quinoline
and pharmaceutically acceptable salts thereof.
51. A compound selected from
2-(l-(3-(Quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)ethylidene) hydrazinecarboxamide
1-(3-(Quinolin-6-ylmethyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl)ethanone oxime
1-(3-(Quinolin-6-ylmethyl)-3H- [1,2,3] triazolo [4,5-b] pyridin-5-yl)ethanoneO-methyl oxime
N'-(l-(3-(Quinolin-6-ylmethyl)-3H-[l,2,3]triazolo[4,5-b]pyridin-5-yl)ethylidene) acetohydrazide

N'-(l-(3- (quinolin-6-ylme%l) - 3H- [1,2,3] triazolo [4,5-b] pyridin- 5-yl) ethylidene) isonicotinohydrazide
and pharmaceutically acceptable salts thereof.
52. A pharmaceutical composition, comprising a compound of any one of claims
1-51 and a pharmaceutically acceptable carrier.
53. The pharmaceutical composition of claim 52, further comprising one or more
additional therapeutic agents and mixtures thereof.
54. The pharmaceutical composition of claim 53, wherein the one or more
additional therapeutic agent is an anti-cancer agent, anti-inflammatory agent,
immunosuppressive agent, steroid, non-steroidal anti-inflammatory agent, antihistamine,
analgesic, or a mixture thereof.
55. Use of a compound of any one of claims 1-51 in the manufacture of a
medicament for the treatment of a disease, disorder, or condition that would benefit from
inhibiting catalytic activity of a kinase.
56. Use of a compound of claim 55, wherein the kinase is c-Met kinase.
57. A method of inhibiting the HGF/c-Met kinase signaling pathway in a cell
comprising contacting said cell with a compound of any one of claims 1 to 51.
58. A method of inhibiting the proliferative activity of a cell comprising
contacting said cell with a compound of any one of claims 1 to 51.
59. A method of inhibiting tumor growth in a patient comprising administering to
said patient a therapeutically effective amount of a compound of any one of claims 1 to 51.
60. A method of inhibiting tumor metastasis in a patient comprising administering
to said patient a therapeutically effective amount of a compound of any one of claims 1 to 51.
61. A method for the treatment of a c-Met associated disease or disorder,
comprising the step of administering to a subject in need thereof an effective amount of
compound of any one of claims 1-51.

62. A method of claim 61, further comprising the step of administering
simultaneously or sequentially to a subject in need thereof at least one other anti-cancer
agent, anti-inflammatory agent, immunosuppressive agent, steroid, non-steroidal anti¬
inflammatory agent, antihistamine, analgesic, or a mixture thereof.
63. A method of claim 6 1 or 62, wherein the c-Met associated disease, disorder or
condition is an immune system-related disease, a disease or disorder involving inflammation,
cancer or other proliferative disease, a hepatic disease or disorder, or a renal disease or
disorder.
64. A method of treating a cancer in a patient comprising administering to said
patient a therapeutically effective amount of a compound of any one of claims 1 to 51.
65. The method of claim 64, wherein said cancer is a carcinoma, musculoskeletal
sarcoma, soft tissue sarcoma, or hematopoietic malignancy.
66. The method of claim 65, wherein said cancer is carcinoma of the bladder,
carcinoma of the breast, carcinoma of the colon, carcinoma of the kidney, carcinoma of the
liver, carcinoma of the lung, small cell lung cancer, esophageal cancer, gall bladder cancer,
ovarian cancer, pancreatic cancer, stomach cancer, cervical cancer, thyroid cancer, prostate
cancer, skin cancer, squamous cell carcinoma; cholangiocarcinoma cancer .tumors of
mesenchymal origin, fibrosarcoma, rhabdomyosarcoma; tumors of the central and peripheral
nervous system, astrocytoma, neuroblastoma, glioma, schwannoma; melanoma, seminoma,
teratocarcinoma, osteosarcoma, xenoderoma pigmentosum, keratoctanthoma, thyroid
follicular cancer and Kaposi's sarcoma, synovial sarcoma, rhabdomyosarcoma,
MFH/fibrosarcoma, leiomyosarcoma, multiple myeloma, lymphoma, glioblastoma,
astrocytoma, melanoma, mesothelioma, Wilms tumor , hematopoietic tumors of lymphoid
lineage, leukemia, acute lymphocytic leukemia, acute lymphoblastic leukemia, B-cell
lymphoma, T-cell lymphoma, Hodgkin's lymphoma, non-Hodgkins lymphoma, hairy cell
lymphoma and Burkett's lymphoma; hematopoietic tumors of myeloid lineage, acute
myelogenous leukemias, chronic myelogenous leukemias, myelodysplasia syndrome, or
promyelocytic leukemia.

Documents

Application Documents

# Name Date
1 10246-CHENP-2012 PCT 06-12-2012.pdf 2012-12-06
1 10246-CHENP-2012-FORM-26 [21-06-2021(online)].pdf 2021-06-21
2 10246-CHENP-2012 ASSIGNMENT 06-12-2012.pdf 2012-12-06
2 Correspondence by Applicant_Form3_23-06-2017.pdf 2017-06-23
3 Form3_After Filing_23-06-2017.pdf 2017-06-23
3 10246-CHENP-2012 FORM-5 06-12-2012.pdf 2012-12-06
4 10246-CHENP-2012-Correspondence-F3-060516.pdf 2016-07-15
4 10246-CHENP-2012 FORM-3 06-12-2012.pdf 2012-12-06
5 10246-CHENP-2012-Form 3-060516.pdf 2016-07-15
5 10246-CHENP-2012 FORM-2 FIRST PAGE 06-12-2012.pdf 2012-12-06
6 10246-CHENP-2012 CORRESPONDENCE OTHERS 17-02-2015.pdf 2015-02-17
6 10246-CHENP-2012 FORM-1 06-12-2012.pdf 2012-12-06
7 10246-CHENP-2012 FORM-3 17-02-2015.pdf 2015-02-17
7 10246-CHENP-2012 DESCRIPTION (COMPLETE) 06-12-2012.pdf 2012-12-06
8 10246-CHENP-2012 CORRESPONDENCE OTHERS 10-02-2014.pdf 2014-02-10
8 10246-CHENP-2012 CORRESPONDENCE OTHERS 06-12-2012.pdf 2012-12-06
9 10246-CHENP-2012 CLAIMS 06-12-2012.pdf 2012-12-06
9 10246-CHENP-2012 FORM-3 10-02-2014.pdf 2014-02-10
10 10246-CHENP-2012 CORRESPONDENCE OTHERS 11-07-2013.pdf 2013-07-11
10 10246-CHENP-2012.pdf 2012-12-07
11 10246-CHENP-2012 FORM -18 11-07-2013.pdf 2013-07-11
11 10246-CHENP-2012 CORRESPONDENCE OTHERS 26-12-2012.pdf 2012-12-26
12 10246-CHENP-2012 FORM-1 26-12-2012.pdf 2012-12-26
12 10246-CHENP-2012 CORRESPONDENCE OTHERS 17-05-2013.pdf 2013-05-17
13 10246-CHENP-2012 FORM-3 17-05-2013.pdf 2013-05-17
14 10246-CHENP-2012 FORM-1 26-12-2012.pdf 2012-12-26
14 10246-CHENP-2012 CORRESPONDENCE OTHERS 17-05-2013.pdf 2013-05-17
15 10246-CHENP-2012 FORM -18 11-07-2013.pdf 2013-07-11
15 10246-CHENP-2012 CORRESPONDENCE OTHERS 26-12-2012.pdf 2012-12-26
16 10246-CHENP-2012 CORRESPONDENCE OTHERS 11-07-2013.pdf 2013-07-11
16 10246-CHENP-2012.pdf 2012-12-07
17 10246-CHENP-2012 FORM-3 10-02-2014.pdf 2014-02-10
17 10246-CHENP-2012 CLAIMS 06-12-2012.pdf 2012-12-06
18 10246-CHENP-2012 CORRESPONDENCE OTHERS 06-12-2012.pdf 2012-12-06
18 10246-CHENP-2012 CORRESPONDENCE OTHERS 10-02-2014.pdf 2014-02-10
19 10246-CHENP-2012 FORM-3 17-02-2015.pdf 2015-02-17
19 10246-CHENP-2012 DESCRIPTION (COMPLETE) 06-12-2012.pdf 2012-12-06
20 10246-CHENP-2012 CORRESPONDENCE OTHERS 17-02-2015.pdf 2015-02-17
20 10246-CHENP-2012 FORM-1 06-12-2012.pdf 2012-12-06
21 10246-CHENP-2012-Form 3-060516.pdf 2016-07-15
21 10246-CHENP-2012 FORM-2 FIRST PAGE 06-12-2012.pdf 2012-12-06
22 10246-CHENP-2012-Correspondence-F3-060516.pdf 2016-07-15
22 10246-CHENP-2012 FORM-3 06-12-2012.pdf 2012-12-06
23 Form3_After Filing_23-06-2017.pdf 2017-06-23
23 10246-CHENP-2012 FORM-5 06-12-2012.pdf 2012-12-06
24 Correspondence by Applicant_Form3_23-06-2017.pdf 2017-06-23
24 10246-CHENP-2012 ASSIGNMENT 06-12-2012.pdf 2012-12-06
25 10246-CHENP-2012 PCT 06-12-2012.pdf 2012-12-06
25 10246-CHENP-2012-FORM-26 [21-06-2021(online)].pdf 2021-06-21