US2023322772A1PendingUtilityA1
Azaindolylpyridone and diazaindolylpyridone compounds
Est. expiryAug 23, 2037(~11.1 yrs left)· nominal 20-yr term from priority
C07D 471/04A61K 31/444A61K 31/4545A61K 31/496A61K 31/506A61K 31/5377A61K 38/45A61P 35/00A61N 5/10A61P 35/02A61P 29/00A61P 37/00A61P 37/06A61P 25/00A61P 9/00A61P 31/12
68
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Claims
Abstract
The invention provides novel azaindolylpyridone and diazaindolylpyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory diseases, autoimmune diseases, neurodegenerative disorders, cardiovascular disorders and viral infections;wherein R2, R3 and X are as defined in the specification.
Claims
exact text as granted — not AI-modified1 - 46 . (canceled)
47 . A method of treating cancer in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound represented by Formula (I):
wherein: X is N or CR 1 ; R 1 is selected from the group consisting of H, C 1 -C 3 alkyl, C 1 -C 3 haloalkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 3 -C 6 cycloalkyl, cyano, phenyl, and monocyclic heteroaryl, wherein said phenyl and said heteroaryl are optionally and independently substituted with one or more substituents selected from the group consisting of halo, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, C 3 -C 6 cycloalkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 1 -C 3 haloalkyl, C 1 -C 3 haloalkoxy, C 1 -C 3 alkoxy and C 1 -C 3 alkyl; R 2 is selected from the group consisting of hydrogen, C 1 -C 3 haloalkyl and C 1 -C 3 alkyl; R 3 is selected from the group consisting of A, phenyl and monocyclic heteroaryl, said phenyl and said heteroaryl being optionally and independently substituted with one or more R 4 ; each R 4 is independently selected from the group consisting of COR 5 , halogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, amino, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-azetidinyl, NHSO 2 R 6 , SO 2 R 7 , hydroxy, C 3 -C 6 cycloalkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 1 -C 3 cyanoalkyl and C 1 -C 6 haloalkyl; R 5 is selected from the group consisting of C 1 -C 3 alkoxy, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, 1-pyrrolidinyl, 1-piperidinyl and 1-azetidinyl; R 6 is C 1 -C 3 haloalkyl or C 1 -C 3 alkyl; R 7 is selected from the group consisting of R 8 , C 1 -C 6 alkyl, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino and C 1 -C 3 alkoxyC 1 -C 3 alkyl, said C 1 -C 6 alkyl and said C 1 -C 3 alkoxyC 1 -C 3 alkyl being optionally substituted with one R 8 and/or one or more halo; R 8 is selected from the group consisting of phenyl, monocyclic heteroaryl, C 3 -C 6 cycloalkyl, heterocyclyl, each optionally substituted with one or more R 9 ; R 9 is selected from the group consisting of halo, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, C 1 -C 3 alkoxyC 1 -C 3 alkyl, amino, C 1 -C 3 haloalkyl, C 1 -C 3 alkoxy, C 1 -C 3 haloalkoxy, C 3 -C 6 cycloalkyl and C 1 -C 3 alkyl; A is:
R 10 is selected from the group consisting of hydrogen, halogen, COR 11 , C 1 -C 6 alkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 1 -C 6 alkoxy, C 3 -C 6 cycloalkyl, C 1 -C 3 cyanoalkyl, C 1 -C 3 haloalkyl, phenyl and heteroaryl, wherein said phenyl and said heteroaryl are optionally and independently substituted with one or more R 12 , and provided that when R 10 is phenyl or heteroaryl, then X is N or CH; R 11 is selected from the group consisting of C 1 -C 3 alkoxy, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, 1-pyrrolidinyl, 1-piperidinyl and 1-azetidinyl; Y is CH 2 , S, SO, SO 2 , NR 13 , NCOR 7 , NCOOR 14 , NSO 2 R 7 , NCOCH 2 R 7 , O, or a bond; R 12 is selected from the group consisting of C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 1 -C 3 haloalkyl, halogen, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, C 1 -C 3 haloalkoxy and C 1 -C 3 alkoxy; R 13 is selected from the group consisting of H, C 1 -C 3 haloalkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 1 -C 3 alkyl, C 3 -C 6 cycloalkyl; R 14 is selected from the group consisting of R 8 , C 1 -C 6 alkyl and C 1 -C 3 alkoxyC 1 -C 3 alkyl, said C 1 -C 6 alkyl and said C 1 -C 3 alkoxyC 1 -C 3 alkyl being optionally substituted with one R 8 and/or one or more halo; or a pharmaceutically acceptable salt thereof.
48 . The method of claim 47 , wherein the cancer is selected from the group consisting of breast cancer, such as triple negative breast cancer, bladder cancer, liver cancer, cervical cancer, pancreatic cancer, leukemia, lymphoma, renal cancer, colon cancer, glioma, prostate cancer, ovarian cancer, melanoma, and lung cancer.
49 . The method of claim 47 , wherein R 1 is selected from the group consisting of H, C 1 -C 3 alkyl, C 1 -C 3 haloalkyl, C 3 -C 6 cycloalkyl, cyano, phenyl, heteroaryl, wherein said phenyl and said heteroaryl are optionally and independently substituted with one or more substituents selected from C 1 -C 3 haloalkyl, halo, C 3 -C 6 cycloalkyl and C 1 -C 3 alkyl;
or a pharmaceutically acceptable salt thereof.
50 . The method of claim 47 , wherein R 1 is selected from the group consisting of the group consisting of:
or a pharmaceutically acceptable salt thereof.
51 . The method of claim 47 , wherein R 3 is selected from the group consisting of A, phenyl and monocyclic heteroaryl selected from pyridyl, thienyl, furyl, pyrimidinyl and pyrazolyl, wherein said phenyl and said heteroaryl are optionally and independently substituted with one or two R 4 ;
or a pharmaceutically acceptable salt thereof.
52 . The method of claim 47 , wherein R 4 is selected from the group consisting of fluoro, chloro, C 1 -C 3 alkyl, C 3 -C 6 cycloalkyl, C 1 -C 3 fluoroalkyl and SO 2 R 7 ;
or a pharmaceutically acceptable salt thereof.
53 . The method of claim 47 , wherein R 10 is selected from the group consisting of hydrogen, C 1 -C 3 alkyl, C 3 -C 6 cycloalkyl, phenyl, monocyclic heteroaryl and C 1 -C 3 haloalkyl, wherein said phenyl and said heteroaryl are optionally and independently substituted with one R 12 ; and R 12 is selected from C 1 -C 3 alkyl, cyclopropyl, CF 3 , halogen, C 1 -C 3 haloalkoxy and C 1 -C 3 alkoxy;
or a pharmaceutically acceptable salt thereof.
54 . The method of claim 47 , wherein R 7 is selected from the group consisting of R 8 , N,N-diC 1 -C 3 alkylamino, C 1 -C 3 alkyl and methoxyC 1 -C 3 alkyl, said C 1 -C 3 alkyl being optionally substituted with one R 8 ;
or a pharmaceutically acceptable salt thereof.
55 . The method of claim 47 , wherein R 3 is selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
56 . The method of claim 47 , wherein
R 1 is selected from the group consisting of:
R 2 is hydrogen; and R 3 is selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
57 . The method of claim 47 , wherein the compound is selected from the group consisting of:
4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)phenyl]-1H-pyridin-2-one; 6-(3-Methyl-4-pyridyl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-(2-phenylpyrrolidin-1-yl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-(3-pyridyl)-1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-morpholino-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-(2-oxazol-5-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-[2-(3-pyridyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[3-(trifluoromethyl)morpholin-4-yl]-1H-pyridin-2-one; 6-[3-(Trifluoromethyl)morpholin-4-yl]-4-[2-[3-(trifluoromethyl)phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 4-[2-(5-Methyl-2-thienyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-6-[3-(trifluoromethyl)morpholin-4-yl]-1H-pyridin-2-one; 4-(1H-pyrazolo[3,4-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[2-(trifluoromethyl)pyrimidin-5-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[6-(trifluoromethyl)-3-pyridyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[5-(trifluoromethyl)-3-pyridyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 4-(2-cyclopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[4-ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-1H-pyridin-2-one; 6-[4-ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-[4-[(4-fluorophenyl)methylsulfonyl]-2-(trifluoromethyl)piperazin-1-yl]-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)- 1H-pyridin-2-one; 6-[4-Ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 4-[2-[4-Ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-6-oxo-1H-pyridin-4-yl]-1H-pyrrolo[2,3-b]pyridine-2-carbonitrile; 4-(2-cyclopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)phenyl]-1H-pyridin-2-one; 4-[2-Oxo-6-[2-(trifluoromethyl)phenyl]-1H-pyridin-4-yl]-1H-pyrrolo[2,3-b]pyridine-2-carbonitrile; 4-(1H-pyrazolo[3,4-b]pyridin-4-yl)-6-[2-(trifluoromethyl)phenyl]-1H-pyridin-2-one; 6-[4-Methylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-4-(1H-pyrazolo[3,4-b]pyridin-4-yl)-1H-pyridin-2-one; and a pharmaceutically acceptable salt thereof.
58 . The method of claim 47 , wherein the compound is selected from the group consisting of:
4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)phenyl]-1H-pyridin-2-one; 6-(3-Methyl-4-pyridyl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-(2-phenylpyrrolidin-1-yl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)- 1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-(3-pyridyl)-1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-morpholino-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-(2-oxazol-5-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-[2-(3-pyridyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[3-(trifluoromethyl)morpholin-4-yl]-1H-pyridin-2-one; 6-[3-(Trifluoromethyl)morpholin-4-yl]-4-[2-[3-(trifluoromethyl)phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 4-[2-(5-Methyl-2-thienyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-6-[3-(trifluoromethyl)morpholin-4-yl]-1H-pyridin-2-one; 4-(1H-pyrazolo[3,4-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[2-(trifluoromethyl)pyrimidin-5-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[6-(trifluoromethyl)-3-pyridyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[5-(trifluoromethyl)-3-pyridyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 4-(2-cyclopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[4-ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-1H-pyridin-2-one; 6-[4-ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-[4-[(4-fluorophenyl)methylsulfonyl]-2-(trifluoromethyl)piperazin-1-yl]-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)- 1H-pyridin-2-one; and a pharmaceutically acceptable salt thereof.
59 . A method of treating a disease selected from the group consisting of inflammatory diseases, autoimmune diseases, neurodegenerative disorders, cardiovascular disorders and viral infections in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound represented by Formula (I):
wherein: X is N or CR 1 ; R 1 is selected from the group consisting of H, C 1 -C 3 alkyl, C 1 -C 3 haloalkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 3 -C 6 cycloalkyl, cyano, phenyl, and monocyclic heteroaryl, wherein said phenyl and said heteroaryl are optionally and independently substituted with one or more substituents selected from the group consisting of halo, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, C 3 -C 6 cycloalkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 1 -C 3 haloalkyl, C 1 -C 3 haloalkoxy, C 1 -C 3 alkoxy and C 1 -C 3 alkyl; R 2 is selected from the group consisting of hydrogen, C 1 -C 3 haloalkyl and C 1 -C 3 alkyl; R 3 is selected from the group consisting of A, phenyl and monocyclic heteroaryl, said phenyl and said heteroaryl being optionally and independently substituted with one or more R 4 ; each R 4 is independently selected from the group consisting of COR 5 , halogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, amino, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-azetidinyl, NHSO 2 R 6 , SO 2 R 7 , hydroxy, C 3 -C 6 cycloalkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 1 -C 3 cyanoalkyl and C 1 -C 6 haloalkyl; R 5 is selected from the group consisting of C 1 -C 3 alkoxy, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, 1-pyrrolidinyl, 1-piperidinyl and 1-azetidinyl; R 6 is C 1 -C 3 haloalkyl or C 1 -C 3 alkyl; R 7 is selected from the group consisting of R 8 , C 1 -C 6 alkyl, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino and C 1 -C 3 alkoxyC 1 -C 3 alkyl, said C 1 -C 6 alkyl and said C 1 -C 3 alkoxyC 1 -C 3 alkyl being optionally substituted with one R 8 and/or one or more halo; R 8 is selected from the group consisting of phenyl, monocyclic heteroaryl, C 3 -C 6 cycloalkyl, heterocyclyl, each optionally substituted with one or more R 9 ; R 9 is selected from the group consisting of halo, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, C 1 -C 3 alkoxyC 1 -C 3 alkyl, amino, C 1 -C 3 haloalkyl, C 1 -C 3 alkoxy, C 1 -C 3 haloalkoxy, C 3 -C 6 cycloalkyl and C 1 -C 3 alkyl; A is:
R 10 is selected from the group consisting of hydrogen, halogen, COR 11 , C 1 -C 6 alkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 1 -C 6 alkoxy, C 3 -C 6 cycloalkyl, C 1 -C 3 cyanoalkyl, C 1 -C 3 haloalkyl, phenyl and heteroaryl, wherein said phenyl and said heteroaryl are optionally and independently substituted with one or more R 12 , and provided that when R 10 is phenyl or heteroaryl, then X is N or CH; R 11 is selected from the group consisting of C 1 -C 3 alkoxy, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, 1-pyrrolidinyl, 1-piperidinyl and 1-azetidinyl; Y is CH 2 , S, SO, SO 2 , NR 13 , NCOR 7 , NCOOR 14 , NSO 2 R 7 , NCOCH 2 R 7 , O, or a bond; R 12 is selected from the group consisting of C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 1 -C 3 haloalkyl, halogen, N-C 1 -C 3 alkylamino, N,N-diC 1 -C 3 alkylamino, C 1 -C 3 haloalkoxy and C 1 -C 3 alkoxy; R 13 is selected from the group consisting of H, C 1 -C 3 haloalkyl, C 1 -C 3 alkoxyC 1 -C 3 alkyl, C 1 -C 3 alkyl, C 3 -C 6 cycloalkyl; R 14 is selected from the group consisting of R 8 , C 1 -C 6 alkyl and C 1 -C 3 alkoxyC 1 -C 3 alkyl, said C 1 -C 6 alkyl and said C 1 -C 3 alkoxyC 1 -C 3 alkyl being optionally substituted with one R 8 and/or one or more halo;
or a pharmaceutically acceptable salt thereof.
60 . The method of claim 59 , wherein R 1 is selected from the group consisting of H, C 1 -C 3 alkyl, C 1 -C 3 haloalkyl, C 3 -C 6 cycloalkyl, cyano, phenyl, heteroaryl, wherein said phenyl and said heteroaryl are optionally and independently substituted with one or more substituents selected from C 1 -C 3 haloalkyl, halo, C 3 -C 6 cycloalkyl and C 1 -C 3 alkyl; or a pharmaceutically acceptable salt thereof.
61 . The method of claim 59 , wherein R 1 is selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
62 . The method of claim 59 , wherein R 3 is selected from the group consisting of A, phenyl and monocyclic heteroaryl selected from pyridyl, thienyl, furyl, pyrimidinyl and pyrazolyl, wherein said phenyl and said heteroaryl are optionally and independently substituted with one or two R 4 ;
or a pharmaceutically acceptable salt thereof.
63 . The method of claim 59 , wherein R 4 is selected from the group consisting of fluoro, chloro, C 1 -C 3 alkyl, C 3 -C 6 cycloalkyl, C 1 -C 3 fluoroalkyl and SO 2 R 7 ; or a pharmaceutically acceptable salt thereof.
64 . The method of claim 59 , wherein R 10 is selected from the group consisting of hydrogen, C 1 -C 3 alkyl, C 3 -C 6 cycloalkyl, phenyl, monocyclic heteroaryl and C 1 -C 3 haloalkyl, wherein said phenyl and said heteroaryl are optionally and independently substituted with one R 12 ; and R 12 is selected from C 1 -C 3 alkyl, cyclopropyl, CF 3 , halogen, C 1 -C 3 haloalkoxy and C 1 -C 3 alkoxy;
or a pharmaceutically acceptable salt thereof.
65 . The method of claim 59 , wherein R 7 is selected from the group consisting of R 8 , N,N-diC 1 -C 3 alkylamino, C 1 -C 3 alkyl and methoxyC 1 -C 3 alkyl, said C 1 -C 3 alkyl being optionally substituted with one R 8 ;
or a pharmaceutically acceptable salt thereof.
66 . The method of claim 59 , wherein R 3 is selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
67 . The method of claim 59 , wherein R 1 is selected from the group consisting of:
R 2 is hydrogen; and
R 3 is selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
68 . The method of claim 59 , wherein the compound is selected from the group consisting of:
4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)phenyl]-1H-pyridin-2-one; 6-(3-Methyl-4-pyridyl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-(2-phenylpyrrolidin-1-yl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-(3-pyridyl)-1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-morpholino-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-(2-oxazol-5-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-[2-(3-pyridyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[3-(trifluoromethyl)morpholin-4-yl]-1H-pyridin-2-one; 6-[3-(Trifluoromethyl)morpholin-4-yl]-4-[2-[3-(trifluoromethyl)phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 4-[2-(5-Methyl-2-thienyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-6-[3-(trifluoromethyl)morpholin-4-yl]-1H-pyridin-2-one; 4-(1H-pyrazolo[3,4-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[2-(trifluoromethyl)pyrimidin-5-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[6-(trifluoromethyl)-3-pyridyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[5-(trifluoromethyl)-3-pyridyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 4-(2-cyclopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[4-ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-1H-pyridin-2-one; 6-[4-ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-[4-[(4-fluorophenyl)methylsulfonyl]-2-(trifluoromethyl)piperazin-1-yl]-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)- 1H-pyridin-2-one; 6-[4-Ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 4-[2-[4-Ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-6-oxo-1H-pyridin-4-yl]-1H-pyrrolo[2,3-b]pyridine-2-carbonitrile; 4-(2-cyclopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)phenyl]-1H-pyridin-2-one; 4-[2-Oxo-6-[2-(trifluoromethyl)phenyl]-1H-pyridin-4-yl]-1H-pyrrolo[2,3-b]pyridine-2-carbonitrile; 4-(1H-pyrazolo[3,4-b]pyridin-4-yl)-6-[2-(trifluoromethyl)phenyl]-1H-pyridin-2-one; 6-[4-Methylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-4-(1H-pyrazolo[3,4-b]pyridin-4-yl)-1H-pyridin-2-one; and a pharmaceutically acceptable salt thereof.
69 . The method of claim 59 , wherein the compound is selected from the group consisting of:
4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)phenyl]-1H-pyridin-2-one; 6-(3-Methyl-4-pyridyl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-(2-phenylpyrrolidin-1-yl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)- 1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-(3-pyridyl)-1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-morpholino-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-(2-oxazol-5-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-[2-(3-pyridyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-(2-Chlorophenyl)-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 4-(2-Methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[3-(trifluoromethyl)morpholin-4-yl]-1H-pyridin-2-one; 6-[3-(Trifluoromethyl)morpholin-4-yl]-4-[2-[3-(trifluoromethyl)phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 4-[2-(5-Methyl-2-thienyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-6-[3-(trifluoromethyl)morpholin-4-yl]-1H-pyridin-2-one; 4-(1H-pyrazolo[3,4-b]pyridin-4-yl)-6-[2-(trifluoromethyl)-1-piperidyl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[2-(trifluoromethyl)pyrimidin-5-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[6-(trifluoromethyl)-3-pyridyl]-1H-pyrrolo[2,3- b]pyridin-4-yl]-1H-pyridin-2-one; 6-[2-(Trifluoromethyl)-1-piperidyl]-4-[2-[5-(trifluoromethyl)-3-pyridyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1H-pyridin-2-one; 4-(2-cyclopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-6-[4-ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-1H-pyridin-2-one; 6-[4-ethylsulfonyl-2-(trifluoromethyl)piperazin-1-yl]-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyridin-2-one; 6-[4-[(4-fluorophenyl)methylsulfonyl]-2-(trifluoromethyl)piperazin-1-yl]-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)- 1H-pyridin-2-one; and a pharmaceutically acceptable salt thereof.Cited by (0)
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