US2019084981A1PendingUtilityA1

Bromodomain Inhibitors

Assignee: ABBVIE INCPriority: Jun 28, 2013Filed: Nov 16, 2018Published: Mar 21, 2019
Est. expiryJun 28, 2033(~6.9 yrs left)· nominal 20-yr term from priority
A61P 9/04A61P 9/12A61P 9/10A61P 5/14A61P 37/06A61P 43/00A61P 3/10A61P 9/00A61P 5/06A61P 37/00A61P 7/00A61P 37/02A61P 5/40A61P 3/06A61P 37/08A61P 31/12A61P 3/00A61P 29/00A61P 25/28A61P 31/00A61P 3/04A61P 31/04A61P 35/00A61P 35/02A61P 27/02A61P 31/18A61P 17/16A61P 1/18A61P 11/08A61P 11/00A61P 17/00A61P 1/00A61P 19/06A61P 25/00A61P 1/04A61P 13/12A61P 15/16A61P 1/16A61P 11/06A61P 13/02A61P 21/00A61P 17/06A61P 19/02A61K 31/497A61K 31/437A61K 31/506A61K 31/496A61K 31/5377A61K 45/06C07D 471/04A61K 31/4545A61K 31/541A61K 31/551
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Claims

Abstract

wherein Rx, Ry, Rx1, L1, G1, A1, A2, A3, and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Claims

exact text as granted — not AI-modified
1 . A compound of formula (I), or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         wherein
 R x  is hydrogen or C 1 -C 3  alkyl; 
 R y  is hydrogen or C 1 -C 3  alkyl; 
 A 1  is N or CR 1 , A 2  is N or CR 2 , A 3  is N or CR 3 ; and A 4  is N or CR 4 ; wherein zero, one, two, or three of A 1 , A 2 , A 3 , and A 4  are N; 
 R 1  is hydrogen, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, halogen, C 1 -C 6  haloalkyl, CN, or NO 2 ; 
 R 2  is hydrogen, —S(O) 2 R 2a , —S(O) 2 NR 2b R 2c , —N(R 2b )S(O) 2 R 2a , or —(C 1 -C 6  alkylenyl)-S(O) 2 R 2a ; wherein R 2a  is C 1 -C 6  alkyl or C 1 -C 6  haloalkyl; and R 2b  and R 2c  are each independently hydrogen, C 1 -C 6  alkyl, or C 1 -C 6  haloalkyl; 
 L 1  is O, N(H), or OCH 2  wherein the CH 2  moiety of OCH 2  is attached to G 1 ; 
 R x1 , G 1 , R 3 , and R 4 , are selected from (i), (ii), (iii), or (iv); 
 (i) R x1  is —CN, -G x1 -G x2 , —(C 1 -C 6  alkylenyl)-G x1 -G x2 , —C(O)N(R xa )(R xb ), C 1 -C 6  alkyl substituted with one substituent selected from the group consisting of —CN, —OR xb , —SR xb , —S(O)R xb , —S(O) 2 R xb , —NR xa R xb , —C(O)R xb , —C(O)OR xb , —C(O)NR xa R xb , and —S(O) 2 NR xa R xb ; C 2 -C 6  alkenyl, or C 2 -C 6  alkynyl; wherein the C 2 -C 6  alkenyl and C 2 -C 6  alkynyl are each independently substituted with one substituent selected from the group consisting of —CN, —OR xc , —SR xc , —S(O)R xc , —S(O) 2 R xc , —NR xa R xc , —C(O)R xc , —C(O)OR xc , —C(O)NR xa R xc , —S(O) 2 NR xa R xc , and G x1 ;
 G 1  is phenyl, C 3 -C 6  cycloalkyl, C 5 -C 6  heteroaryl, or C 4 -C 6  heterocycle; wherein each G 1  is independently unsubstituted or substituted with 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of R u  and R v  groups; 
 R 3  is R 1a , —C(O)OH, —C(O)NR 3a R 3b , —NR 3a R 3b , G 3a , -G 3a -G 3b , —(C 1 -C 6  alkylenyl)-OR 3a , —(C 1 -C 6  alkylenyl)-NR 3a R 3b , —(C 1 -C 6  alkylenyl)-G 3a , or —(C 1 -C 6  alkylenyl)-G 3a -G 3b ; and 
 R 4  is R 1a  or G 4 ; 
 
 (ii) R x1  is —CN, -G x1 -G x2 , —(C 1 -C 6  alkylenyl)-G x1 -G x2 , —C(O)N(R xa )(R xb ), hydrogen, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, —C(O)OR ax1 , —C(O)NR bx1 R cx1 , —C(O)R dx1 , —S(O) 2 R dx1 , —S(O) 2 NR bx1 R cx1 , G x1 , C 1 -C 6  haloalkyl, or C 1 -C 6  alkyl; wherein the C 1 -C 6  alkyl, C 2 -C 6  alkenyl, and C 2 -C 6  alkynyl are each optionally substituted with one substituent selected from the group consisting of —CN, —OR xc , —SR xc , —S(O)R xc , —S(O) 2 R xc , —NR xa R xc , —C(O)R xc , —C(O)OR xc , —C(O)NR xa R xc , —S(O) 2 NR xa R xc , and G x1 ;
 G 1  is phenyl, C 3 -C 6  cycloalkyl, C 5 -C 6  heteroaryl, or C 4 -C 6  heterocycle; wherein each G 1  is substituted with one R u  group and is optionally further substituted with 1, 2, 3, 4, or 5 R v  groups; 
 R 3  is R 1a , —C(O)OH, —C(O)NR 3a R 3b , —NR 3a R 3b , G 3a , -G 3a -G 3b , —(C 1 -C 6  alkylenyl)-OR 3a , —(C 1 -C 6  alkylenyl)-NR 3a R 3b , —(C 1 -C 6  alkylenyl)-G 3a , or —(C 1 -C 6  alkylenyl)-G 3a -G 3b ; and 
 R 4  is R 1a  or G 4 ; 
 
 (iii) R x1  is —CN, -G x1 -G x2 , —(C 1 -C 6  alkylenyl)-G x1 -G x2 , —C(O)N(R xa )(R xb ), hydrogen, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, —C(O)OR ax1 , —C(O)NR bx1 R cx1 , —C(O)R dx1 , —S(O) 2 R dx1 , —S(O) 2 NR bx1 R cx1 , G x1 , C 1 -C 6  haloalkyl, or C 1 -C 6  alkyl; wherein the C 1 -C 6  alkyl, C 2 -C 6  alkenyl, and C 2 -C 6  alkynyl are each optionally substituted with one substituent selected from the group consisting of —CN, —OR xc , —SR xc , —S(O)R xc , —S(O) 2 R xc , —NR xa R xc , —C(O)R xc , —C(O)OR xc , —C(O)NR xa R xc , —S(O) 2 NR xa R xc , and G x1 ;
 G 1  is phenyl, C 3 -C 6  cycloalkyl, C 5 -C 6  heteroaryl, or C 4 -C 6  heterocycle; wherein each G 1  is independently unsubstituted or substituted with 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of R u  and R v  groups; 
 R 3  is —C(O)OH, —C(O)NR 3a R 3b , —NR 3a R 3b , G 3a , -G 3a -G 3b , —(C 1 -C 6  alkylenyl)-OR 3a , —(C 1 -C 6  alkylenyl)-NR 3a R 3b , —(C 1 -C 6  alkylenyl)-G 3a , or —(C 1 -C 6  alkylenyl)-G 3a -G 3b ; and 
 R 4  is R 1a  or G 4 ; 
 
 (iv) R x1  is —CN, -G x1 -G 2 , —(C 1 -C 6  alkylenyl)-G x1 -G x2 , —C(O)N(R xa )(R xb ), hydrogen, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, —C(O)OR ax1 , —C(O)NR bx1 R cx1 , —C(O)R dx1 , —S(O) 2 R dx1 , —S(O) 2 NR bx1 R cx1 , G x1 , C 1 -C 6  haloalkyl, or C 1 -C 6  alkyl; wherein the C 1 -C 6  alkyl, C 2 -C 6  alkenyl, and C 2 -C 6  alkynyl are each optionally substituted with one substituent selected from the group consisting of —CN, —OR xc , —SR xc , —S(O)R xc , —S(O) 2 R xc , —NR xa R xc , —C(O)R xc , —C(O)OR xc , —C(O)NR xa R xc , —S(O) 2 NR xa R xc , and G x1 ;
 G 1  is phenyl, C 3 -C 6  cycloalkyl, C 5 -C 6  heteroaryl, or C 4 -C 6  heterocycle; wherein each G 1  is independently unsubstituted or substituted with 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of R u  and R v  groups; 
 R 3  is R 1a , —C(O)OH, —C(O)NR 3a R 3b , —NR 3a R 3b , G 3a , -G 3a -G 3b , —(C 1 -C 6  alkylenyl)-OR 3a , —(C 1 -C 6  alkylenyl)-NR 3a R 3b , —(C 1 -C 6  alkylenyl)-G 3a , or —(C 1 -C 6  alkylenyl)-G 3a -G 3b ; and 
 R 4  is G 4 ; 
 
 R xa , at each occurrence, is independently hydrogen, C 1 -C 6  alkyl, or C 1 -C 6  haloalkyl; 
 R xb , at each occurrence, is independently C 1 -C 6  alkyl substituted with one substituent selected from the group consisting of —CN, —OR ax1 , —SR ax1 , —S(O)R dx1 , —S(O) 2 R dx1 , —NR bx1 R cx1 , —C(O)R ax1 , —C(O)OR ax1 , —C(O)NR bx1 R cx1 , and —S(O) 2 NR bx1 R cx1 ; 
 R xc , at each occurrence, is independently hydrogen, C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, G a , —(C 1 -C 6  alkylenyl)-G a , or R xb ; 
 R ax1 , R bx1 , and R cx1 , at each occurrence, are each independently hydrogen, C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, G a , or —(C 1 -C 6  alkylenyl)-G a ; 
 R dx1 , at each occurrence, is independently C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, G a , or —(C 1 -C 6  alkylenyl)-G a ; 
 R 1a , at each occurrence, is independently hydrogen, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, halogen, C 1 -C 6  haloalkyl, CN, or NO 2 ; 
 R 3a  and R 3b , at each occurrence, are each independently hydrogen, C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, G 3a , -G 3a -G 3b , —(C 1 -C 6  alkylenyl)-G 3a , —(C 1 -C 6  alkylenyl)-G 3a -G 3b , or C 1 -C 6  alkyl substituted with one substituents selected from the group consisting of —CN, —OR h , —SR h , —S(O)R i , —S(O) 2 R h , —NR j R k , —C(O)R h , —C(O)OR h , —C(O)NR j R k , and —S(O) 2 NR j R k ; 
 G 4 , at each occurrence, is independently phenyl, C 3 -C 6  cycloalkyl, C 5 -C 6  heteroaryl, or C 4 -C 6  heterocycle; each of which is optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of C 1 -C 6  alkyl, NO 2 , halogen, C 1 -C 6  haloalkyl, —CN, oxo, —OR h , —SR h , —S(O) 2 R h , and —NR j R k ; 
 R u , at each occurrence, is independently —(C 1 -C 6  alkylenyl)-G u , —(C 2 -C 6  alkynylene)-G u , —(C 1 -C 6  alkylenyl)-SR h , —C(O)—Z 1 , —C(O)—NZ 1 Z 2 , —S(O) 2 —Z 1 , —N(Z 2 )Z 1 , or —N(Z 2 )S(O) 2 —Z 1 ; wherein Z 1  is G u , —(C 1 -C 6  alkylenyl)-G u , —(C 2 -C 6  alkenylene)-G u , —(C 1 -C 6  alkylenyl)-CN, —(C 1 -C 6  alkylenyl)-SR h , —(C 1 -C 6  alkylenyl)-OR h , —(C 1 -C 6  alkylenyl)-NR j R k , or —(C 1 -C 6  alkylenyl)-C 1 -C 4  alkoxy-C 1 -C 4  alkoxy, and Z 2  is hydrogen, C 1 -C 6  alkyl, or C 1 -C 6  haloalkyl; 
 G u , at each occurrence, is independently aryl, heteroaryl, heterocycle, cycloalkyl, or cycloalkenyl, wherein each G u  is independently unsubstituted or substituted with 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, halogen, C 1 -C 6  haloalkyl, —CN, oxo, NO 2 , —OR h , —O—(C 2 -C 6  alkylenyl)-NR j R k , —OC(O)R i , —OC(O)NR j R k , —O—(C 1 -C 6  alkylenyl)-NR j R k , —SR h , —S(O) 2 R h , —S(O) 2 NR j R k , —C(O)R h , —C(O)OR h , —C(O)NR j R k , —NR j R k , —N(R h )C(O)R, —N(R h )S(O) 2 R i , —N(R h )C(O)O(R), —N(R h )C(O)NR j R k , G ua , —(C 1 -C 6  alkylenyl)-OR h , —(C 1 -C 6  alkylenyl)-OC(O)R i , —(C 1 -C 6  alkylenyl)-OC(O)NR j R k , —(C 1 -C 6  alkylenyl)-SR h , —(C 1 -C 6  alkylenyl)-S(O) 2 R h , —(C 1 -C 6  alkylenyl)-S(O) 2 NR j R k , —(C 1 -C 6  alkylenyl)-C(O)R h , —(C 1 -C 6  alkylenyl)-C(O)OR h , —(C 1 -C 6  alkylenyl)-C(O)NR j R k , —(C 1 -C 6  alkylenyl)-NR j R k , —(C 1 -C 6  alkylenyl)-N(R h )C(O)R i , —(C 1 -C 6  alkylenyl)-N(R h )S(O) 2 R i , —(C 1 -C 6  alkylenyl)-N(R h )C(O)O(R i ), —(C 1 -C 6  alkylenyl)-N(R h )C(O)NR j R k , —(C 1 -C 6  alkylenyl)-CN, and —(C 1 -C 6  alkylenyl)-G a ; 
 G a , G x1 , G x2 , G 3a , G 3b , and G ua , at each occurrence, are each independently aryl, heteroaryl, heterocycle, cycloalkyl, or cycloalkenyl, each of which is optionally substituted with 1, 2, 3, 4, or 5 R z  groups; 
 R z  and R v , at each occurrence, are each independently C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, halogen, C 1 -C 6  haloalkyl, —CN, oxo, NO 2 , —OR h , —OC(O)R i , —OC(O)NR j R k , —SR h , —S(O) 2 R h , —S(O) 2 NR j R k , —C(O)R h , —C(O)OR h , —C(O)NR j R k , —NR j R k , —N(R h )C(O)R, —N(R h )S(O) 2 R i , —N(R h )C(O)O(R i ), —N(R h )C(O)NR j R k , —(C 1 -C 6  alkylenyl)-OR h , —(C 1 -C 6  alkylenyl)-OC(O)R i , —(C 1 -C 6  alkylenyl)-OC(O)NR j R k , —(C 1 -C 6  alkylenyl)-SR h , —(C 1 -C 6  alkylenyl)-S(O) 2 R h , —(C 1 -C 6  alkylenyl)-S(O) 2 NR j R k , —(C 1 -C 6  alkylenyl)-C(O)R h , —(C 1 -C 6  alkylenyl)-C(O)OR h , —(C 1 -C 6  alkylenyl)-C(O)NR j R k , —(C 1 -C 6  alkylenyl)-NR j R k , —(C 1 -C 6  alkylenyl)-N(R h )C(O)R i , —(C 1 -C 6  alkylenyl)-N(R h )S(O) 2 R i , —(C 1 -C 6  alkylenyl)-N(R h )C(O)O(R i ), —(C 1 -C 6  alkylenyl)-N(R h )C(O)NR j R k , or —(C 1 -C 6  alkylenyl)-CN; 
 R h , R, R k , at each occurrence, are each independently hydrogen, C 1 -C 6  alkyl, or C 1 -C 6  haloalkyl; and 
 R i , at each occurrence, is independently C 1 -C 6  alkyl or C 1 -C 6  haloalkyl. 
 
       
     
     
         2 . The compound of  claim 1  or a pharmaceutically acceptable salt thereof, wherein
 R x  is hydrogen, and 
 R y  is C 1 -C 3  alkyl. 
 
     
     
         3 . The compound of  claim 2  or a pharmaceutically acceptable salt thereof, wherein
 A 1  is CR 1 , A 2  is CR 2 , A 3  is CR 3 ; and A 4  is CR 4 . 
 
     
     
         4 . The compound of  claim 2  or a pharmaceutically acceptable salt thereof, wherein one of A 1 , A 2 , A 3 , and A 4  is N. 
     
     
         5 . The compound of  claim 2  or a pharmaceutically acceptable salt thereof, wherein
 R 2  is hydrogen, —S(O) 2 R 2a , or —N(R 2b )S(O) 2 R 2a ; 
 R 2a  is C 1 -C 3  alkyl; and 
 R 2b  is hydrogen. 
 
     
     
         6 . The compound of  claim 3  or a pharmaceutically acceptable salt thereof, wherein
 R y  is methyl, 
 R 1  is hydrogen, and 
 R x1 , G 1 , R 3 , and R 4 , are selected from (i). 
 
     
     
         7 . The compound of  claim 6  or a pharmaceutically acceptable salt thereof, wherein
 R 3  is R 1a ; 
 R 4  is R 1a ; and 
 G 1  is phenyl, C 3 -C 6  cycloalkyl, or C 4 -C 6  heterocycle, each of which is optionally substituted with 1, 2, 3, 4, or 5 R v  groups. 
 
     
     
         8 . The compound of  claim 7  or a pharmaceutically acceptable salt thereof, wherein
 R 1a  is hydrogen; and 
 G 1  is phenyl or C 3 -C 6  cycloalkyl, each of which is optionally substituted with 1, 2, 3, 4, or 5 R v  groups. 
 
     
     
         9 . The compound of  claim 8  or a pharmaceutically acceptable salt thereof, wherein
 R x1  is -G x1 -G 2 , —(C 1 -C 6  alkylenyl)-G x1 -G x2 , —C(O)N(R xa )(R xb ), C 2 -C 6  alkenyl, or C 2 -C 6  alkynyl; wherein the C 2 -C 6  alkenyl and C 2 -C 6  alkynyl are each independently substituted with one substituent selected from the group consisting of —CN, —OR xc , —SR xc , —S(O)R xc , —S(O) 2 R xc , —NR xa R xc , —C(O)R xc , —C(O)OR xc , —C(O)NR xa R xc , —S(O) 2 NR xa R xc , and G x1 . 
 
     
     
         10 . The compound of  claim 9  or a pharmaceutically acceptable salt thereof, wherein
 R 2  is hydrogen, —S(O) 2 R 2a , or —N(R 2b )S(O) 2 R 2a . 
 
     
     
         11 . The compound of  claim 6  or a pharmaceutically acceptable salt thereof, wherein the compound is selected from the group consisting of
 4-{2-[(2,2-difluorocyclopropyl)methoxy]-5-(ethylsulfonyl)phenyl}-6-methyl-2-{[4-(pyridin-4-yl)piperazin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-{2-[(2,2-difluorocyclopropyl)methoxy]-5-(ethylsulfonyl)phenyl}-6-methyl-2-{[4-(1,3-thiazol-2-yl)piperazin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-{2-[(2,2-difluorocyclopropyl)methoxy]-5-(ethylsulfonyl)phenyl}-6-methyl-2-{[4-(pyrazin-2-yl)piperazin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-{2-[(2,2-difluorocyclopropyl)methoxy]-5-(ethylsulfonyl)phenyl}-6-methyl-2-{[4-(pyrimidin-2-yl)piperazin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-{2-[(2,2-difluorocyclopropyl)methoxy]-5-(ethylsulfonyl)phenyl}-6-methyl-2-{[4-(pyridin-3-yl)piperazin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-{2-[(2,2-difluorocyclopropyl)methoxy]-5-(ethylsulfonyl)phenyl}-2-[3-(dimethylamino)prop-1-yn-1-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-{[4-(1,3-thiazol-2-yl)piperazin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 2-[(4-cyclopropylpiperazin-1-yl)methyl]-4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-{[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 N-{4-(2,4-difluorophenoxy)-3-[2-(3-methoxyprop-1-yn-1-yl)-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl]phenyl}ethanesulfonamide; 
 4-[2-(2,4-difluorophenoxy)-5-(ethylsulfonyl)phenyl]-6-methyl-2-(1-phenyl-1H-pyrazol-5-yl)-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,4-difluorophenoxy)-5-(ethylsulfonyl)phenyl]-6-methyl-2-[2-(morpholin-4-yl)pyridin-3-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2-chloro-6-methylphenoxy)-5-(ethylsulfonyl)phenyl]-N-(cyanomethyl)-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 4-[2-(2-chloro-6-methylphenoxy)-5-(ethylsulfonyl)phenyl]-6-methyl-N-[1-(methylamino)-1-oxopropan-2-yl]-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 4-[2-(2-chloro-6-methylphenoxy)-5-(ethylsulfonyl)phenyl]-6-methyl-7-oxo-N-[2-oxo-2-(piperidin-1-yl)ethyl]-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 4-[2-(2-chloro-6-methylphenoxy)-5-(ethylsulfonyl)phenyl]-N-(2-cyanoethyl)-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 4-[2-(2-chloro-6-methylphenoxy)-5-(ethylsulfonyl)phenyl]-6-methyl-N-[2-(methylamino)-2-oxoethyl]-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-{[4-(1-methylpiperidin-4-yl)piperazin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-{[4-(pyridin-2-yl)-1,4-diazepan-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-2-{[3-(furan-2-yl)morpholin-4-yl]methyl}-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-2-{[4-(3,5-dimethyl-4H-1,2,4-triazol-4-yl)piperidin-1-yl]methyl}-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-2-{[3-(3,5-dimethyl-1H-pyrazol-1-yl)azetidin-1-yl]methyl}-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-{[4-(morpholin-4-yl)piperidin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-{[2-(3-methyl-1,2,4-oxadiazol-5-yl)pyrrolidin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-{[4-(pyridin-2-yl)piperazin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 (2E)-3-{4-[2-(2,6-dimethylphenoxy)-5-(ethylsulfonyl)phenyl]-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-2-yl}-N-ethylprop-2-enamide; 
 2-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-4-[2-(2,6-dimethylphenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 2-(3-cyclohexyl-1,2,4-oxadiazol-5-yl)-4-[2-(2,6-dimethylphenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,6-dimethylphenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-(3-phenyl-1,2,4-oxadiazol-5-yl)-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,6-dimethylphenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-[3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,6-dimethylphenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-[3-(pyridin-2-yl)-1,2,4-oxadiazol-5-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,6-dimethylphenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-[3-(pyrazin-2-yl)-1,2,4-oxadiazol-5-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,6-dimethylphenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-[3-(tetrahydro-2H-pyran-4-yl)-1,2,4-oxadiazol-5-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(2,6-dimethylphenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-[3-(1,3-thiazol-4-yl)-1,2,4-oxadiazol-5-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 N-[2-(diethylamino)-2-methylpropyl]-4-[2-(2,6-dimethylphenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 N-[4-(diethylamino)butyl]-4-[2-(2,6-dimethylphenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 4-[2-(cyclohexyloxy)-5-(ethylsulfonyl)phenyl]-6-methyl-2-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 1-({4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-2-yl}methyl)-N,N-dimethyl-4-(2-oxopyrrolidin-1-yl)piperidine-4-carboxamide; 
 4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-2-{[3-(1H-1,2,4-triazol-1-yl)azetidin-1-yl]methyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; and 
 3-[({4-[2-(2,4-difluorophenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-2-yl}methyl)amino]propanamide. 
 
     
     
         12 . The compound of  claim 3  or a pharmaceutically acceptable salt thereof, wherein
 R y  is methyl, 
 R 1  is hydrogen, and 
 R x1 , G 1 , R 3 , and R 4 , are selected from (ii). 
 
     
     
         13 . The compound of  claim 12  or a pharmaceutically acceptable salt thereof, wherein
 R x1  is hydrogen or —C(O)NR bx1 R cx1 ; 
 R 3  is R 1a ; 
 R 4  is R 1a ; and 
 G 1  is phenyl, C 3 -C 6  cycloalkyl, or C 4 -C 6  heterocycle, wherein each G 1  is substituted with one R u  group and is optionally further substituted with 1, 2, or 3 R v  groups. 
 
     
     
         14 . The compound of  claim 13  or a pharmaceutically acceptable salt thereof, wherein
 R 1a  is hydrogen; and 
 R 2  is hydrogen, —S(O) 2 R 2a , or —N(R 2b )S(O) 2 R 2a . 
 
     
     
         15 . The compound of  claim 12  or a pharmaceutically acceptable salt thereof, wherein the compound is selected from the group consisting of
 N-cyclopropyl-3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]benzamide; 
 6-methyl-4-[2-{3-[(4-methylpiperazin-1-yl)carbonyl]phenoxy}-5-(methylsulfonyl)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-{2-[3-({4-[2-(1H-imidazol-1-yl)ethyl]piperazin-1-yl}carbonyl)phenoxy]-5-(methylsulfonyl)phenyl}-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-(3-{[4-(pyrrolidin-1-yl)piperidin-1-yl]carbonyl}phenoxy)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 N-cyclohexyl-3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]benzamide; 
 4-[2-(3-{[4-(2-hydroxyethyl)piperazin-1-yl]carbonyl}phenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]-N-[3-(2-oxopyrrolidin-1-yl)propyl]benzamide; 
 4-[2-{3-[(4-cyclopentylpiperazin-1-yl)carbonyl]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-{2-[3-({4-[2-(dimethylamino)ethyl]piperazin-1-yl}carbonyl)phenoxy]-5-(methylsulfonyl)phenyl}-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{3-[(4-acetylpiperazin-1-yl)carbonyl]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-(3-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenoxy)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 N-(cyanomethyl)-N-methyl-3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]benzamide; 
 N-[2-(dimethylamino)ethyl]-3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]benzamide; 
 3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]-N-[(2R)-tetrahydrofuran-2-ylmethyl]benzamide; 
 3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]-N-[2-(pyrrolidin-1-yl)ethyl]benzamide; 
 N-(3,5-difluorobenzyl)-3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]benzamide; 
 N-(2,4-difluorobenzyl)-3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]benzamide; 
 N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}-1-phenylmethanesulfonamide; 
 4-methoxy-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 3-fluoro-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 4-fluoro-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 3-methoxy-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}-4-nitrobenzenesulfonamide; 
 4-acetyl-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 5-(dimethylamino)-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}naphthalene-1-sulfonamide; 
 N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}-4-(propan-2-yl)benzenesulfonamide; 
 2,4-difluoro-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 3-(difluoromethoxy)-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}cyclopropanesulfonamide; 
 3-methyl-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}-3-nitrobenzenesulfonamide; 
 4-fluoro-2-methyl-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 3,4-dimethoxy-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}-4-(methylsulfonyl)benzenesulfonamide; 
 2-cyano-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 4-cyano-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 3-cyano-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 2-chloro-4-fluoro-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}benzenesulfonamide; 
 1-methyl-N-{3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}-1H-imidazole-4-sulfonamide; 
 3-[({3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}amino)methyl]benzonitrile; 
 4-[({3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}amino)methyl]benzonitrile; 
 4-[2-{3-[(4-fluorobenzyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{3-[(2-methoxyethyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-{3-[(tetrahydrofuran-2-ylmethyl)amino]phenoxy}phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{3-[(3-methoxybenzyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{3-[(2-fluorobenzyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{3-[(3-fluorobenzyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-(3-{[3-(trifluoromethoxy)benzyl]amino}phenoxy)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{3-[(2,4-dimethylbenzyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 2-[({3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}amino)methyl]benzonitrile; 
 4-[2-{3-[(2-chloro-4-fluorobenzyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{3-[(3,5-difluorobenzyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-{2-[3-({4-[3-(dimethylamino)propoxy]benzyl}amino)phenoxy]-5-(methylsulfonyl)phenyl}-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-(3-{[3-(dimethylamino)benzyl]amino}phenoxy)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{3-[(2,3-dihydro-1,4-benzodioxin-6-ylmethyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-{3-[(tetrahydrofuran-3-ylmethyl)amino]phenoxy}phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 N-{4-[({3-[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenoxy]phenyl}amino)methyl]phenyl}acetamide; 
 4-[2-{3-[(4-methoxybenzyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{3-[(cyclopropylmethyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{3-[(2-cyclopentylethyl)amino]phenoxy}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{4-chloro-2-[3-(morpholin-4-yl)prop-1-yn-1-yl]phenoxy}-5-(ethylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{4-chloro-2-[3-(morpholin-4-yl)propyl]phenoxy}-5-(ethylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-{[1-(phenylsulfonyl)piperidin-4-yl]amino}phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-({1-[(dimethylamino)acetyl]piperidin-4-yl}amino)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[2-({1-[3-(methylsulfanyl)propyl]piperidin-4-yl}amino)-5-(methylsulfonyl)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 N-{4-[(4-{[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenyl]amino}piperidin-1-yl)methyl]phenyl}acetamide; 
 6-methyl-4-[5-(methylsulfonyl)-2-{[1-(3,4,5-trimethoxybenzyl)piperidin-4-yl]amino}phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-{[1-(thiophen-2-ylmethyl)piperidin-4-yl]amino}phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-{2-[(1-{4-[3-(dimethylamino)propoxy]benzyl}piperidin-4-yl)amino]-5-(methylsulfonyl)phenyl}-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[2-({1-[(methylsulfanyl)acetyl]piperidin-4-yl}amino)-5-(methylsulfonyl)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-({1-[3-(2,3,4-trimethoxyphenyl)propanoyl]piperidin-4-yl}amino)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 1-[(4-{[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenyl]amino}piperidin-1-yl)carbonyl]cyclopropanecarboxamide; 
 4-[2-({1-[(4-methoxycyclohexyl)carbonyl]piperidin-4-yl}amino)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{[1-(methoxyacetyl)piperidin-4-yl]amino}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[2-({1-[(4-methylpiperazin-1-yl)acetyl]piperidin-4-yl}amino)-5-(methylsulfonyl)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-{[1-(pyrrolidin-1-ylacetyl)piperidin-4-yl]amino}phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-({1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}amino)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-({1-[3-(morpholin-4-yl)propanoyl]piperidin-4-yl}amino)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[2-({1-[(4-methylphenyl)acetyl]piperidin-4-yl}amino)-5-(methylsulfonyl)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{[1-(benzylsulfonyl)piperidin-4-yl]amino}-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-{5-(methylsulfonyl)-2-[(1-{[(E)-2-phenylethenyl]sulfonyl}piperidin-4-yl)amino]phenyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 N-{4-[(4-{[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenyl]amino}piperidin-1-yl)sulfonyl]phenyl}acetamide; 
 4-[2-({1-[(4-methoxyphenyl)sulfonyl]piperidin-4-yl}amino)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 3-[(4-{[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenyl]amino}piperidin-1-yl)sulfonyl]benzonitrile; 
 6-methyl-4-[5-(methylsulfonyl)-2-{[1-(thiophen-2-ylsulfonyl)piperidin-4-yl]amino}phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-({trans-4-[(thiophen-2-ylmethyl)amino]cyclohexyl}amino)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 N-(4-{[(trans-4-{[2-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(methylsulfonyl)phenyl]amino}cyclohexyl)amino]methyl}phenyl)acetamide; 
 4-[2-({trans-4-[(2,4-difluorobenzyl)amino]cyclohexyl}amino)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-[5-(methylsulfonyl)-2-({trans-4-[(naphthalen-2-ylmethyl)amino]cyclohexyl}amino)phenyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-({trans-4-[(2-methoxyethyl)amino]cyclohexyl}amino)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 6-methyl-4-{2-[(trans-4-{[3-(methylsulfanyl)propyl]amino}cyclohexyl)amino]-5-(methylsulfonyl)phenyl}-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-({trans-4-[(4-chlorobenzyl)amino]cyclohexyl}amino)-5-(methylsulfonyl)phenyl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 4-[2-{2-[(cyclopropylmethyl)amino]-6-methylphenoxy}-5-(ethylsulfonyl)phenyl]-N-ethyl-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 N-ethyl-4-[5-(ethylsulfonyl)-2-{2-methyl-6-[(tetrahydrofuran-3-ylmethyl)amino]phenoxy}phenyl]-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 N-ethyl-4-{5-(ethylsulfonyl)-2-[2-methyl-6-(1H-pyrazol-1-ylmethyl)phenoxy]phenyl}-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 N-ethyl-4-{5-(ethylsulfonyl)-2-[2-methyl-6-(morpholin-4-ylmethyl)phenoxy]phenyl}-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 N-ethyl-4-{5-(ethylsulfonyl)-2-[2-methyl-6-(piperidin-1-ylmethyl)phenoxy]phenyl}-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 N-ethyl-4-{5-(ethylsulfonyl)-2-[2-methyl-6-(2-phenylethyl)phenoxy]phenyl}-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 N-ethyl-4-{5-(ethylsulfonyl)-2-[2-(1H-imidazol-1-ylmethyl)-6-methylphenoxy]phenyl}-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 N-ethyl-4-[5-(ethylsulfonyl)-2-{2-methyl-6-[(2-oxopyrrolidin-1-yl)methyl]phenoxy}phenyl]-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 4-[2-{2-[(1,1-dioxido-1,2-thiazolidin-2-yl)methyl]-6-methylphenoxy}-5-(ethylsulfonyl)phenyl]-N-ethyl-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 N-ethyl-4-[5-(ethylsulfonyl)-2-{2-methyl-6-[(2-oxoazetidin-1-yl)methyl]phenoxy}phenyl]-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; and 
 N-ethyl-4-[5-(ethylsulfonyl)-2-{2-methyl-6-[(2-oxopyridin-1 (2H)-yl)methyl]phenoxy}phenyl]-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide. 
 
     
     
         16 . The compound of  claim 3  or a pharmaceutically acceptable salt thereof, wherein
 R y  is methyl, 
 R 1  is hydrogen, and 
 R x1 , G 1 , R 3 , and R 4 , are selected from (iii). 
 
     
     
         17 . The compound of  claim 16  or a pharmaceutically acceptable salt thereof, wherein
 R x1  is hydrogen or —C(O)NR bx1 R cx1 ; 
 R 4  is R 1a ; and 
 G 1  is phenyl, C 3 -C 6  cycloalkyl, or C 4 -C 6  heterocycle, each of which is optionally substituted with 1, 2, 3, 4, or 5 R v  groups. 
 
     
     
         18 . The compound of  claim 17  or a pharmaceutically acceptable salt thereof, wherein
 R 1a  is hydrogen; and 
 G 1  is phenyl or C 3 -C 6  cycloalkyl, each of which is optionally substituted with 1, 2, 3, 4, or 5 R groups. 
 
     
     
         19 . The compound of  claim 18  or a pharmaceutically acceptable salt thereof, wherein
 R 3  is —C(O)OH, —C(O)NR 3a R 3b , G 3a , —(C 1 -C 6  alkylenyl)-OR 3a , —(C 1 -C 6  alkylenyl)-NR 3a R 3b , —(C 1 -C 6  alkylenyl)-G 3a , or —(C 1 -C 6  alkylenyl)-G 3a -G 3b . 
 
     
     
         20 . The compound of  claim 19  or a pharmaceutically acceptable salt thereof, wherein
 R 2  is hydrogen, —S(O) 2 R 2a , or —N(R 2b )S(O) 2 R 2a . 
 
     
     
         21 . The compound of  claim 16  or a pharmaceutically acceptable salt thereof, wherein the compound is selected from the group consisting of
 4-[2-(cyclopropylmethoxy)-4-(3-methyl-H-pyrazol-5-yl)phenyl]-6-methyl-,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; 
 N-[4-(2,4-difluorophenoxy)-2-[(dimethylamino)methyl]-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide; 
 N-[4-(2,4-difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-2-(piperidin-1-ylmethyl)phenyl]ethanesulfonamide; 
 N-[4-(2,4-difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-2-(morpholin-4-ylmethyl)phenyl]ethanesulfonamide; 
 N-{4-(2,4-difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-2-[(4-methylpiperazin-1-yl)methyl]phenyl}ethanesulfonamide; 
 N-[4-(2,4-difluorophenoxy)-2-(hydroxymethyl)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide; 
 N-{2-[(cyclopentylamino)methyl]-4-(2,4-difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl}ethanesulfonamide; 
 5-(2,4-difluorophenoxy)-2-[(ethylsulfonyl)amino]-4-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)benzamide; 
 N-cyclopentyl-5-(2,4-difluorophenoxy)-2-[(ethylsulfonyl)amino]-4-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)benzamide; 
 5-(2,4-difluorophenoxy)-2-[(ethylsulfonyl)amino]-N,N-dimethyl-4-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)benzamide; 
 5-(2,4-difluorophenoxy)-2-[(ethylsulfonyl)amino]-4-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)benzoic acid; 
 5-(2,4-difluorophenoxy)-2-[(ethylsulfonyl)amino]-4-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide; 
 N-[4-(2,4-difluorophenoxy)-2-{[(2-hydroxyethyl)amino]methyl}-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide; 
 N-{4-(2,4-difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-2-[(2-phenylpyrrolidin-1-yl)methyl]phenyl}ethanesulfonamide; 
 4-[2-(2,6-dimethylphenoxy)-4-{[2-(methylamino)-2-oxoethyl](pyridin-2-ylmethyl)carbamoyl}phenyl]-N-ethyl-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 4-[2-(2,6-dimethylphenoxy)-4-{methyl[1-(propanoyloxy)piperidin-4-yl]carbamoyl}phenyl]-N-ethyl-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; 
 methyl 3-[{3-(2,6-dimethylphenoxy)-4-[2-(ethylcarbamoyl)-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl]benzoyl}(phenyl)amino]propanoate; 
 4-[4-{benzyl[3-(morpholin-4-yl)propyl]carbamoyl}-2-(2,6-dimethylphenoxy)phenyl]-N-ethyl-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide; and 
 4-[4-{(3,4-dichlorophenyl)[2-(thiomorpholin-4-yl)ethyl]carbamoyl}-2-(2,6-dimethylphenoxy)phenyl]-N-ethyl-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide. 
 
     
     
         22 . The compound of  claim 3  or a pharmaceutically acceptable salt thereof, wherein
 R y  is methyl, 
 R 1  is hydrogen, and 
 R x1 , G 1 , R 3 , and R 4 , are selected from (iv). 
 
     
     
         23 . The compound of  claim 22  or a pharmaceutically acceptable salt thereof, wherein
 R x1  is hydrogen; 
 R 3  is R 1a ; and 
 G 1  is phenyl, C 3 -C 6  cycloalkyl, or C 4 -C 6  heterocycle, each of which is optionally substituted with 1, 2, 3, 4, or 5 R v  groups. 
 
     
     
         24 . The compound of  claim 23  or a pharmaceutically acceptable salt thereof, wherein
 R 1a  is hydrogen; and 
 G 1  is phenyl or C 3 -C 6  cycloalkyl, each of which is optionally substituted with 1, 2, 3, 4, or 5 R v  groups. 
 
     
     
         25 . The compound of  claim 24  or a pharmaceutically acceptable salt thereof, wherein
 R 4  is optionally substituted C 3 -C 6  cycloalkyl. 
 
     
     
         26 . The compound of  claim 25  or a pharmaceutically acceptable salt thereof, wherein
 R 4  is optionally substituted cyclopropyl, and 
 R 2  is hydrogen, —S(O) 2 R 2a , or —N(R 2b )S(O) 2 R 2a . 
 
     
     
         27 . The compound of  claim 22  or a pharmaceutically acceptable salt thereof, wherein the compound is
 N-[3-cyclopropyl-4-(2,4-difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide. 
 
     
     
         28 . A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) according to  claim 1 , or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier. 
     
     
         29 . A method for treating cancer in a subject comprising administering a therapeutically effective amount of a compound of formula (I) according to  claim 1  or a pharmaceutically acceptable salt thereof, to a subject in need thereof. 
     
     
         30 . The method of  claim 29  wherein the cancer is selected from the group consisting of: acoustic neuroma, acute leukemia, acute lymphocytic leukemia, acute myelocytic leukemia (monocytic, myeloblastic, adenocarcinoma, angiosarcoma, astrocytoma, myelomonocytic and promyelocytic), acute t-cell leukemia, basal cell carcinoma, bile duct carcinoma, bladder cancer, brain cancer, breast cancer, bronchogenic carcinoma, cervical cancer, chondrosarcoma, chordoma, choriocarcinoma, chronic leukemia, chronic lymphocytic leukemia, chronic myelocytic (granulocytic) leukemia, chronic myelogenous leukemia, colon cancer, colorectal cancer, craniopharyngioma, cystadenocarcinoma, diffuse large B-cell lymphoma, dysproliferative changes (dysplasias and metaplasias), embryonal carcinoma, endometrial cancer, endotheliosarcoma, ependymoma, epithelial carcinoma, erythroleukemia, esophageal cancer, estrogen-receptor positive breast cancer, essential thrombocythemia, Ewing's tumor, fibrosarcoma, follicular lymphoma, germ cell testicular cancer, glioma, glioblastoma, gliosarcoma, heavy chain disease, hemangioblastoma, hepatoma, hepatocellular cancer, hormone insensitive prostate cancer, leiomyosarcoma, leukemia, liposarcoma, lung cancer, lymphagioendotheliosarcoma, lymphangiosarcoma, lymphoblastic leukemia, lymphoma (Hodgkin's and non-Hodgkin's), malignancies and hyperproliferative disorders of the bladder, breast, colon, lung, ovaries, pancreas, prostate, skin and uterus, lymphoid malignancies of T-cell or B-cell origin, leukemia, lymphoma, medullary carcinoma, medulloblastoma, melanoma, meningioma, mesothelioma, multiple myeloma, myelogenous leukemia, myeloma, myxosarcoma, neuroblastoma, NUT midline carcinoma (NMC), non-small cell lung cancer, oligodendroglioma, oral cancer, osteogenic sarcoma, ovarian cancer, pancreatic cancer, papillary adenocarcinomas, papillary carcinoma, pinealoma, polycythemia vera, prostate cancer, rectal cancer, renal cell carcinoma, retinoblastoma, rhabdomyosarcoma, sarcoma, sebaceous gland carcinoma, seminoma, skin cancer, small cell lung carcinoma, solid tumors (carcinomas and sarcomas), small cell lung cancer, stomach cancer, squamous cell carcinoma, synovioma, sweat gland carcinoma, thyroid cancer, Waldenstrom's macroglobulinemia, testicular tumors, uterine cancer and Wilms' tumor. 
     
     
         31 . A method for treating a disease or condition in a subject comprising administering a therapeutically effective amount of a compound of formula (I) according to  claim 1  or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein said disease or condition is selected from the group consisting of Addison's disease, acute gout, ankylosing spondylitis, asthma, atherosclerosis, Behcet's disease, bullous skin diseases, cardiac myopathy, cardiac hypertrophy, chronic obstructive pulmonary disease (COPD), Crohn's disease, dermatitis, eczema, giant cell arteritis, glomerulonephritis, heart failure, hepatitis, hypophysitis, inflammatory bowel disease,), Kawasaki disease, lupus nephritis, multiple sclerosis, myocarditis, myositis, nephritis, organ transplant rejection, osteoarthritis, pancreatitis, pericarditis, Polyarteritis  nodosa , pneumonitis, primary biliary cirrhosis, psoriasis, psoriatic arthritis, rheumatoid arthritis, scleritis, sclerosing cholangitis, sepsis systemic lupus erythematosus, Takayasu's Arteritis, toxic shock, thyroiditis, type I diabetes, ulcerative colitis, uveitis, vitiligo, vasculitis, and Wegener's granulomatosis. 
     
     
         32 . A method for treating a disease or condition in a subject comprising administering a therapeutically effective amount of a compound of formula (I) according to  claim 1  or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein said disease or condition is selected from the group consisting of: diabetic nephropathy, hypertensive nephropathy, HIV-associated nephropathy, glomerulonephritis, lupus nephritis, IgA nephropathy, focal segmental glomerulosclerosis, membranous glomerulonephritis, minimal change disease, polycystic kidney disease and tubular interstitial nephritis. 
     
     
         33 . A method for treating an acquired immunodeficiency syndrome (AIDS) in a subject comprising administering a therapeutically effective amount of a compound of formula (I) according to  claim 1  or a pharmaceutically acceptable salt thereof, to a subject in need thereof. 
     
     
         34 . A method for treating a disease or condition in a subject comprising administering a therapeutically effective amount of a compound of formula (I) according to  claim 1  or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein said disease or condition is selected from the group consisting of: obesity, dyslipidemia, hypercholesterolemia, Alzheimer's disease, metabolic syndrome, hepatic steatosis, type II diabetes, insulin resistance, diabetic retinopathy and diabetic neuropathy. 
     
     
         35 . A method of contraception in a male subject comprising administering a therapeutically effective amount of a compound of formula (I) according to  claim 1  or a pharmaceutically acceptable salt thereof, to a subject in need thereof. 
     
     
         36 . A method for treating an acute kidney disease or condition in a subject comprising administering a therapeutically effective amount of a compound of formula (I) according to  claim 1  or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein said acute kidney disease or condition is selected from the group consisting of: ischemia-reperfusion induced kidney disease, cardiac and major surgery induced kidney disease, percutaneous coronary intervention induced kidney disease, radio-contrast agent induced kidney disease, sepsis induced kidney disease, pneumonia induced kidney disease, and drug toxicity induced kidney disease. 
     
     
         37 . The method of  claim 36 , further comprising administering a therapeutically effective amount of at least one additional therapeutic agent. 
     
     
         38 . A method of treating a chronic kidney disease or condition in a subject comprising administering a therapeutically effective amount of a compound of formula (I) according to  claim 1  or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein said disease or condition is selected from the group consisting of: diabetic nephropathy, hypertensive nephropathy, HIV-associated nephropathy, glomerulonephritis, lupus nephritis, IgA nephropathy, focal segmental glomerulosclerosis, membranous glomerulonephritis, minimal change disease, polycystic kidney disease and tubular interstitial nephritis. 
     
     
         39 . The method of  claim 38 , further comprising administering a therapeutically effective amount of at least one additional therapeutic agent.

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