IP Library › Granted Patent US 9,399,640

Granted Patent B2

US 9,399,640 · App. 14/554,306 · Granted Jul 26, 2016

Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors

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Patent No.: US 9,399,640
App. No.: 14/554,306
Granted: Jul 26, 2016
Kind: B2

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Abstract

The present invention relates to compounds represented by the general Formula I which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

Claims (261)

1. A compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

represents a single or double bond;

Ring B is phenyl, 5-6 membered heteroaryl, C 5-6 cycloalkyl, or 5-6 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 R B ;

L is absent, —(CR a R b ) p —, —(CR a R b ) n —O—(CR a R b ) m —, —(CR a R b ) n —S—(CR a R b ) m —, —(CR a R b ) n —S(═O)—(CR a R b ) m —, —(CR a R b ) n —S(═O) 2 —(CR a R b ) m —, —(CR a R b ) n —C(═O)—(CR a R b ) m —, —(CR a R b ) n —C(═O)O—(CR a R b ) m —, —(CR a R b ) n —OC(═O)—(CR a R b ) m —, —(CR a R b ) n —NR c —(CR a R b ) m —, —(CR a R b ) n —C(═O)NR—(CR a R b ) m —, —(CR a R b ) n —NR c C(═O)—(CR a R b ) m —, or —(CR a R b ) n —NR c C(═O)NR d —(CR a R b ) m —;

A1 is CR 3 or N;

A2 is CR 4 or N;

A3 is C or N;

A4 is C or N;

wherein when one of A3 and A4 is N, then the other of A3 and A4 is C;

W is CR 5 ;

X is CR 6 ;

Y is CR 7 or N;

(i) Z is C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, or 4-10 membered heterocycloalkyl, each of which is optionally substituted by 1, 2, 3, 4, or 5 R Z ; and R 3 and R 4 are each independently selected from H, halo, CN, NO 2 , C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, C 1-6 alkylamino-C 1-6 alkyl, di-C 1-6 -alkylamino-C 1-6 alkyl, C 2-6 alkenyl, and C 2-6 alkynyl, wherein said C 1-6 alkylamino-C 1-6 alkyl and di-C 1-6 -alkylamino-C 1-6 alkyl are each optionally substituted with 1 or 2 substituents independently selected from C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl; or

(ii) Z is C 1-6 alkyl optionally substituted by 1, 2, 3, 4, or 5 R Z ; R 3 is selected from H, halo, CN, NO 2 , C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, C 1-6 alkylamino-C 1-6 alkyl, di-C 1-6 -alkylamino-C 1-6 alkyl, C 2-6 alkenyl, and C 2-6 alkynyl; and R 4 is selected from H, halo, CN, NO 2 , C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, C 1-6 alkylamino-C 1-6 alkyl, di-C 1-6 -alkylamino-C 1-6 alkyl, C 2-6 alkenyl, and C 2-6 alkynyl, wherein said C 1-6 alkylamino-C 1-6 alkyl and di-C 1-6 -alkylamino-C 1-6 alkyl are each optionally substituted with 1 or 2 substituents independently selected from C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl;

R 1 is H or C 1-4 alkyl;

R 2 is H, C 1-4 alkyl, C 1-4 haloalkyl, C 1-4 hydroxyalkyl, C 1-4 cyanoalkyl, or C 6-10 aryl-C 1-6 alkyl;

R 5 is H, halo, C 1-6 alkyl, or C 1-6 haloalkyl;

R 6 is H, C 1-6 alkyl, C 1-6 haloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C(O)R b1 , C(O)NR c1 R d1 , C(O)OR a1 , S(O)R b1 , S(O)NR c1 R d1 , S(O) 2 R b1 , or S(O) 2 NR c1 R d1 , wherein said C 1-6 alkyl, C 2-6 alkenyl, and C 2-6 alkynyl are each optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from halo, C 1-4 haloalkyl, CN, NO 2 , OR a1 , SR a1 , C(O)R b1 , C(O)N c1 R d1 , C(O)OR a1 , OC(O)R b1 , OC(O)NR c1 R d1 , NR c1 R d1 , NR c1 C(O)R b1 , NR c1 C(O)OR a1 , NR c1 C(O)NR c1 R d1 , C(═NR e1 )R b1 , C(═NR e1 )NR c1 R d1 , NR c1 C(═NR e1 )NR c1 R d1 NR c1 S(O)R b1 , NR c1 S(O) 2 R b1 , NR c1 S(O) 2 NR c1 R d1 , S(O)R b1 , S(O)NR c1 R d1 , S(O) 2 R b1 , and S(O) 2 NR c1 R d1 ;

R 7 is H, C 1-6 alkyl, C 1-6 haloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 , S(O)R b2 , S(O)NR c2 R d2 , S(O) 2 R b2 , or S(O) 2 NR c2 R d2 , wherein said C 1-6 alkyl, C 2-6 alkenyl, and C 2-6 alkynyl are each optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from halo, C 1-4 haloalkyl, CN, NO 2 , OR a2 , SR a2 , C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 , OC(O)R b2 , OC(O)NR c2 R d2 , NR c2 R d2 , NR c2 C(O)R b2 , NR c2 C(O)OR a2 , NR c2 C(O)NR c2 R d2 C(═NR e2 )R b2 , C(═NR e2 )NR c2 R d2 , NR c2 C(═NR e2 )NR c2 R d2 , NR c2 S(O)R b2 , NR c2 S(O) 2 R b2 NR c2 S(O) 2 NR c2 R d2 , S(O)R b2 , S(O)NR c2 R d2 , S(O) 2 R b2 , and S(O) 2 NR c2 R d2 ;

each R B is independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, CN, NO 2 , OR a3 , SR a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 , OC(O)R b3 , OC(O)NR c3 R d3 , NR c3 R d3 , NR c3 C(O)R b3 , NR c3 C(O)OR a3 , NR c3 C(O)NR c3 R d3 , C(═NR e3 )R b3 , C(═NR e3 )NR c3 R d3 , NR c3 C(═NR e3 )NR c3 R d3 , NR c3 S(O)R b3 , NR c3 S(O) 2 R b3 , NR c3 S(O) 2 NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O) 2 R b3 , and S(O) 2 NR c3 R d3 ; wherein said C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl are each optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, phenyl, C 3-7 cycloalkyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, CN, NO 2 , OR a3 , SR a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 , OC(O)R b3 , OC(O)NR c3 R d3 , C(═NR e3 )NR c3 R d3 , NR c3 C(═NR e3 )NR c3 R d3 , NR c3 R d3 , NR c3 C(O)R b3 , NR c3 C(O)OR a3 , NR c3 C(O)NR c3 R d3 , NR c3 S(O)R b3 , NR c3 S(O) 2 R b3 , NR c3 S(O) 2 NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O) 2 R b3 , and S(O) 2 NR c3 R d3 , and wherein said phenyl, C 3-7 cycloalkyl, 5-6 membered heteroaryl, and 4-7 membered heterocycloalkyl are each independently substituted by 1, 2, or 3 substituents independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, CN, NO 2 , OR a3 , SR a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 , OC(O)R b3 , OC(O)NR c3 R d3 , C(═NR e3 )NR c3 R d3 , NR c3 C(═NR e3 )NR c3 R d3 , NR c3 R d3 , NR c3 C(O)R b3 NR c3 C(O)OR a3 , NR c3 C(O)NR c3 R d3 , NR c3 S(O)R b3 , NR c3 S(O) 2 R b3 , NR c3 S(O) 2 NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O) 2 R b3 , and S(O) 2 NR c3 R d3 ;

each R Z is independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, CN, NO 2 , OR a4 , SR a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 , OC(O)R b4 , OC(O)NR c4 R d4 , NR c4 R d4 , NR c4 C(O)R b4 , NR c4 C(O)OR a4 , NR c4 C(O)NR c4 R d4 , C(═NR e4 )R b4 , C(═NR e4 )NR c4 R d4 , NR c4 C(═NR e4 )NR c4 R d4 , NR c4 S(O)R b4 , NR c4 S(O) 2 R b4 , NR c4 S(O) 2 NR c4 R d4 , S(O)R b4 , S(O)NR c4 R d4 , S(O) 2 R b4 , and S(O) 2 NR c4 R d4 ; wherein said C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl are each optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, CN, NO 2 , OR a4 , SR a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 , OC(O)R b4 , OC(O)NR c4 R d4 , C(═NR e4 )NR c4 R d4 , NR c4 C(═NR e4 )NR c4 R d4 , NR c4 R d4 , NR c4 C(O)R b4 , NR c4 C(O)OR a4 , NR c4 C(O)NR c4 R d4 , NR c4 S(O)R b4 , NR c4 S(O) 2 R b4 , NR c4 S(O) 2 NR c4 R d4 , S(O)R b4 , S(O)NR c4 R d4 , S(O) 2 R b4 , and S(O) 2 NR c4 R d4 ;

each R a and R b is independently selected from H, halo, OH, methyl, and ethyl;

each R c and R d is independently selected from H, C 1-4 alkyl, C 1-4 haloalkyl, C 1-4 hydroxyalkyl, and cyclopropyl;

each R a1 , R b1 , R c1 , R d1 , R a2 , R b2 , R c2 , R d2 , R a3 , R b3 , R c3 , R d3 , R a4 , R b4 , R c4 , and R d4 is independently selected from H, C 1-6 alkyl, C 1-4 haloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6-10 aryl-C 1-6 alkyl, C 3-10 cycloalky-C 1-6 alkyl, (5-10 membered heteroaryl)-C 1-6 alkyl, and (4-10 membered heterocycloalkyl)-C 1-6 alkyl, wherein said C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C 6-10 aryl-C 1-6 alkyl, C 3-10 cycloalky-C 1-6 alkyl, (5-10 membered heteroaryl)-C 1-6 alkyl, and (4-10 membered heterocycloalkyl)-C 1-6 alkyl is optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from C 1-4 alkyl, C 1-4 haloalkyl, halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 ;

or any R c1 and R d1 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, 5-6 membered heteroaryl, C 1-6 haloalkyl, halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 , wherein said C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, and 5-6 membered heteroaryl are optionally substituted by 1, 2, or 3 substituents independently selected from halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 ;

or any R c2 and R d2 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, 5-6 membered heteroaryl, C 1-6 haloalkyl, halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 , wherein said C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, and 5-6 membered heteroaryl are optionally substituted by 1, 2, or 3 substituents independently selected from halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 ;

or any R c3 and R d3 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, 5-6 membered heteroaryl, C 1-6 haloalkyl, halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 (═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 , wherein said C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, and 5-6 membered heteroaryl are optionally substituted by 1, 2, or 3 substituents independently selected from halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 (═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 ;

or any R c4 and R d4 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, 5-6 membered heteroaryl, C 1-6 haloalkyl, halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 , wherein said C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, and 5-6 membered heteroaryl are optionally substituted by 1, 2, or 3 substituents independently selected from halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 ;

each R e1 , R e2 , R e3 , and R e4 is independently selected from H, C 1-4 alkyl, CN, OR a5 , SR b5 , S(O) 2 R b5 , C(O)R b5 , S(O) 2 NR c5 R d5 , and C(O)NR c5 R d5 ;

each R a5 , R b5 , R c5 , and R d5 is independently selected from H, C 1-4 alkyl, C 1-4 haloalkyl, C 2-4 alkenyl, and C 2-4 alkynyl, wherein said C 1-4 alkyl, C 2-4 alkenyl, and C 2-4 alkynyl, is optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio, C 1-4 alkylamino, di(C 1-4 alkyl)amino, C 1-4 haloalkyl, and C 1-4 haloalkoxy;

each R e5 is independently selected from H, C 1-4 alkyl, and CN;

n is 0, 1, or 2;

m is 0, 1, or 2; and

p is 1, 2, 3, or 4;

wherein any aforementioned heterocycloalkyl group is optionally substituted by 1 or 2 oxo groups.

2. The compound of claim 1 having Formula II:

or a pharmaceutically acceptable salt thereof, wherein:

the 5-membered ring formed by A3, A4, B1, B2, and B3 is (1) 5-membered heteroaryl wherein B1, B2, and B3 are each independently selected from CH, N, NH, O, and S, (2) C 5 -cycloalkyl wherein B1, B2, and B3 are each independently selected from CH, CH 2 , and C(O), or (3) 5-membered heterocycloalkyl wherein B1, B2, and B3 are each independently selected from CH, CH 2 , C(O), N, NH, O, S, S(O), and S(O) 2 ; and

q is 0, 1, 2 or 3.

3. The compound of claim 2 having Formula IIa:

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 2 having Formula IIb:

or a pharmaceutically acceptable salt thereof.

5. The compound of claim 2 having Formula IIc:

or a pharmaceutically acceptable salt thereof, wherein r is 0, 1, 2, 3, 4, or 5.

6. The compound of claim 2 having Formula IId, Formula IIe, Formula IIf, or Formula IIf-1:

or a pharmaceutically acceptable salt thereof, wherein:

r is 0, 1, 2, 3, 4, or 5; and

each RB is independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, CN, NO 2 , OR a3 , SR a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 , OC(O)R b3 , OC(O)NR c3 R d3 , NR c3 R d3 , NR c3 C(O)R b3 , NR c3 C(O)OR a3 , NR c3 C(O)NR c3 R d3 , C(═NR e3 )R b3 , C(═NR e3 )NR c3 R d3 , NR c3 C(═NR e3 )NR c3 R d3 , NR c3 S(O)R b3 , NR c3 S(O) 2 R b3 , NR c3 S(O) 2 NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O) 2 R b3 , and S(O) 2 NR c3 R d3 ; wherein said C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl are each optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, phenyl, C 3-7 cycloalkyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, CN, NO 2 , OR a3 , SR a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 , OC(O)R b3 , OC(O)NR c3 R d3 , C(═NR e3 )NR c3 R d3 , NR c3 C(═NR e3 )NR c3 R d3 NR c3 R d3 NR c3 C(O)R b3 NR c3 C(O)OR a3 , NR c3 C(O)NR c3 R d3 , NR c3 S(O)R b3 , NR c3 S(O) 2 R b3 , NR c3 S(O) 2 NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O) 2 R b3 , and S(O) 2 NR c3 R d3 , and wherein said phenyl, C 3-7 cycloalkyl, 5-6 membered heteroaryl, and 4-7 membered heterocycloalkyl are each independently substituted by 1, 2, or 3 substituents independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, CN, NO 2 , OR a3 , SR a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 , OC(O)R b3 , OC(O)NR c3 R d3 , C(═NR e3 )NR c3 R d3 , NR c3 C(═NR e3 )NR c3 R d3 , NR c3 R d3 NR c3 C(O)R b3 , NR c3 C(O)OR a3 , NR c3 C(O)NR c3 R d3 , NR c3 S(O)R b3 , NR c3 S(O) 2 R b3 , NR c3 S(O) 2 NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O) 2 R b3 , and S(O) 2 NR c3 R d3 .

7. The compound of claim 2 having Formula IId, Formula IIe, or Formula IIf:

or a pharmaceutically acceptable salt thereof, wherein:

r is 0, 1, 2, 3, 4, or 5; and

R 8 , R 9 , and R 10 are each independently selected from H, C 1-6 alkyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl, wherein said C 1-6 alkyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl are each optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from halo, C 1-6 alkyl, C 1-6 haloalkyl, CN, NO 2 , OR a3 , SR a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 , NR c3 R d3 , NR c3 C(O)R b3 , NR c3 C(O)NR c3 R d3 , NR c3 S(O)R b3 , NR c3 S(O) 2 R b3 , NR c3 S(O) 2 NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O) 2 R b3 , and S(O) 2 NR c3 R d3 .

8. The compound of claim 1 having Formula III:

or a pharmaceutically acceptable salt thereof, wherein:

the 6-membered ring formed by A3, A4, B4, B5, B6, and B7 is (1) phenyl, (2) 6-membered heteroaryl wherein B4, B5, B6, and B7 are each independently selected from CH and N, (3) C 6 -cycloalkyl wherein B4, B5, B6, and B7 are each independently selected from CH, CH 2 , and C(O), or (4) 6-membered heterocycloalkyl wherein B4, B5, B6, and B7 are each independently selected from CH, CH 2 , C(O), N, NH, O, S, S(O), and S(O) 2 ; and

s is 0, 1, 2, 3, or 4.

9. The compound of claim 8 having Formula IIIa:

or a pharmaceutically acceptable salt thereof.

10. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein B1, B2, and B3 are each independently selected from CH, C(O), N, O, and NH.

11. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein B1, B2, and B3 are each independently selected from CH, C(O), N, and NH.

12. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein B1 is N, NH, CH, or O.

13. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein B1 is NH.

14. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein B2 is N, C(O), or CH.

15. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein B3 is N, NH, or CH.

16. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein B3 is N or NH.

17. The compound of claim 5 , or a pharmaceutically acceptable salt thereof, wherein r is 0, 1, 2, or 3.

18. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein the 6-membered ring formed by A3, A4, B4, B5, B6, and B7 is 6-membered heterocycloalkyl wherein B4, B5, B6, and B7 are each independently selected from CH, CH 2 , C(O), N, NH, O, S, S(O), and S(O) 2 .

19. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein B4 is selected from O or N.

20. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein B5 is selected from CH or CH 2 .

21. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein B6 is selected from CH or C(O).

22. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein B7 is selected from N or NH.

23. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is H.

24. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 2 is C 1-4 alkyl, C 1-4 cyanoalkyl, or C 6-10 aryl-C 1-6 alkyl.

25. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 2 is C 1-4 alkyl.

26. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 2 is methyl, cyanomethyl, or benzyl.

27. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 2 is methyl.

28. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Y is CR 7 .

29. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Y is N.

30. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein L is —(CR a R b ) p —, —(CR a R b ) n —O—(CR a R b ) m —, —(CR a R b ) n —S—(CR a R b ) m —, or —(CR a R b ) n —S(═O) 2 —(CR a R b ) m —.

31. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein L is —(CR a R b ) n —O—(CR a R b ) m —.

32. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein L is —CH 2 —O—.

33. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein L is O, S, or S(═O) 2 .

34. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein L is O.

35. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Z is C 1-4 alkyl, C 6-10 aryl, C 3-10 cycloalkyl, or 4-10 membered heterocycloalkyl, each of which is optionally substituted by 1, 2, 3, 4, or 5 R Z .

36. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Z is C 6-10 aryl or C 3-10 cycloalkyl, each of which is optionally substituted by 1, 2, 3, 4, or 5 R Z .

37. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Z is phenyl optionally substituted by 1, 2, 3, 4, or 5 R Z .

38. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Z is C 1-4 alkyl.

39. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Z is C 3-7 cycloalkyl optionally substituted by 1, 2, 3, 4, or 5 R Z .

40. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Z is cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl, each of which is optionally substituted by 1, 2, 3, 4, or 5 R Z .

41. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Z is 4-10 membered heterocycloalkyl optionally substituted by 1, 2, 3, 4, or 5 R Z .

42. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Z is tetrahydropyranyl.

43. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein each R Z is independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, CN, NO 2 , OR a4 , SR a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 , OC(O)R b4 , OC(O)NR c4 R d4 , NR c4 R d4 , NR c4 C(O)R b4 , NR c4 C(O)OR a4 , NR c4 C(O)NR c4 R d4 , C(═NR e4 )R b4 , C(═NR e4 )NR c4 R d4 , NR c4 C(═NR e4 )NR c4 R d4 , NR c4 S(O)R b4 , NR c4 S(O) 2 R b4 , NR c4 S(O) 2 NR c4 R d4 , S(O)R b4 , S(O)NR c4 R d4 , S(O) 2 R b4 , and S(O) 2 NR c4 R d4 .

44. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein each R Z is independently selected from F, Cl, and Br.

45. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein A1 is CR 3 .

46. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein A2 is CR 4 .

47. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein A2 is N.

48. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 4 is H, C 1-6 hydroxyalkyl, or C 1-6 alkylamino-C 1-6 alkyl, wherein said C 1-6 alkylamino-C 1-6 alkyl is optionally substituted with 1 or 2 substituents independently selected from C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl.

49. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 4 is H.

50. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 4 is 1-hydroxyethyl.

51. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 4 is C 1-6 alkylamino-C 1-6 alkyl substituted with 2-(morpholin-N-yl)ethyl, benzyl, or cyclopropylmethyl.

52. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein A3 is C.

53. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein A4 is C.

54. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein A4 is N.

55. The compound of claim 1 selected from:

4-(2,4-Difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-[4-(2,4-Difluorophenoxy)-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; and

4-[4-(2,4-Difluorophenoxy)-2-methyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-1-methyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-1,2-dimethyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-(2,4-Difluorophenoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(2,4-Difluorophenoxy)-1,3-dimethyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-[4-(2,4-Difluorophenoxy)-1H-1,2,3-benzotriazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-1-methyl-1H-1,2,3-benzotriazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-1H-1,2,3-benzotriazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

4-(Cyclopropylmethoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-[4-(Cyclopropylmethoxy)-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one; and

4-[4-(Cyclopropylmethoxy)-2-methyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one,

or a pharmaceutically acceptable salt thereof.

56. The compound of claim 1 selected from:

4-[4-(2,4-Difluorophenoxy)-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-2-methyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-1-(2-morpholin-4-ylethyl)-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-1-methyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-1,2-dimethyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-1-methyl-1H-1,2,3-benzotriazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-1-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

5-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1,3-dihydro-2H-benzimidazol-2-one;

4-[(4,4-Difluorocyclohexyl)oxy]-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(4-Fluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(3-Fluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

5-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(tetrahydro-2H-pyran-3-yloxy)-1,3-dihydro-2H-benzimidazol-2-one;

4-(Benzyloxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-[(2,4-Difluorobenzyl)oxy]-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

1-Methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(tetrahydro-2H-pyran-4-yloxy)-1,3-dihydro-2H-benzimidazol-2-one;

4-[7-(2,4-Difluorophenoxy)-1-(2-morpholin-4-yl-2-oxoethyl)-1H-benzimidazol-6-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-[4-(2,4-difluorophenoxy)-1-(2-morpholin-4-yl-2-oxoethyl)-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-Methoxy-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

2-[7-(2,4-Difluorophenoxy)-6-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1H-benzimidazol-1-yl]-N,N-dimethylacetamide;

2-[4-(2,4-difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1H-benzimidazol-1-yl]-N,N-dimethylacetamide;

2-[7-(2,4-Difluorophenoxy)-6-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1H-benzimidazol-1-yl]-N-methylacetamide;

2-[4-(2,4-difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1H-benzimidazol-1-yl]-N-methylacetamide;

4-(Cyclobutylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

1-Methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1,3-dihydro-2H-benzimidazol-2-one;

4-(2-Fluorophenoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin 4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(3-Fluorophenoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin 4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(4-Fluorophenoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin 4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

6-Methyl-4-[1-(2-morpholin-4-ylethyl)-7-phenoxy-1H-benzimidazol-6-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

6-methyl-4-[1-(2-morpholin-4-ylethyl)-4-phenoxy-1H-benzimidazol-5-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

3-Benzyl-4-methoxy-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(1-Benzyl-7-phenoxy-1H-benzimidazol-6-yl)-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-(1-Benzyl-4-phenoxy-1H-benzimidazol-5-yl)-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

6-Methyl-4-[7-phenoxy-1-(2-phenylethyl)-1H-benzimidazol-6-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

6-Methyl-4-[4-phenoxy-1-(2-phenylethyl)-1H-benzimidazol-5-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-Methoxy-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-3-(2-phenylethyl)-1,3-dihydro-2H-benzimidazol-2-one;

4-Methoxy-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-3-(2-morpholin-4-ylethyl)-1,3-dihydro-2H-benzimidazol-2-one;

4-[6-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-7-phenoxy-1H-benzimidazol-1-yl]butanenitrile;

4-[5-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1H-benzimidazol-1-yl]butanenitrile;

4-[7-Methoxy-3-methyl-6-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl]butanenitrile;

3-[7-Methoxy-3-methyl-6-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl]propanenitrile;

3-[6-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-7-phenoxy-1H-benzimidazol-1-yl]propanenitrile;

6-Methyl-4-(1-methyl-4-phenoxy-1H-benzimidazol-5-yl)-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-[4-(2-Fluorophenoxy)-1-methyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-[4-(3-Fluorophenoxy)-1-methyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-[4-(4-Fluorophenoxy)-1-methyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-(Cyclobutylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-3-(2-morpholin-4-ylethyl)-1,3-dihydro-2H-benzimidazol-2-one;

4-[7-(Cyclobutylmethoxy)-3-methyl-6-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl]butanenitrile;

3-[7-(Cyclobutylmethoxy)-3-methyl-6-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl]propanenitrile;

4-(Cyclobutylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-3-(2-phenylethyl)-1,3-dihydro-2H-benzimidazol-2-one;

3-Benzyl-4-(cyclobutylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(Cyclobutylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-3-(2-piperidin-4-ylethyl)-1,3-dihydro-2H-benzimidazol-2-one;

3-(2-(4-Acetylpiperazin-1-yl)ethyl)-4-(cyclobutylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1H-benzo[d]imidazol-2(3H)-one;

4-(Cyclobutylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-3-{2-[4-(methylsulfonyl)piperazin-1-yl]ethyl}-1,3-dihydro-2H-benzimidazol-2-one;

4-(Cyclobutylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-3-[2-(4-methylpiperazin-1-yl)ethyl]-1,3-dihydro-2H-benzimidazol-2-one;

5-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1-(2-morpholin-4-ylethyl)-4-phenoxy-1,3-dihydro-2H-benzimidazol-2-one;

1-{2-[(2R,6S)-2,6-Dimethylmorpholin-4-yl]ethyl}-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1,3-dihydro-2H-benzimidazol-2-one;

4-(2-(Benzylamino)-1-{2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]ethyl}-4-phenoxy-1H-benzimidazol-5-yl)-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-(2-[(Cyclopropylmethyl)amino]-1-{2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]ethyl}-4-phenoxy-1H-benzimidazol-5-yl)-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-(Cyclopropylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

8-(2,4-Difluorophenoxy)-7-(6-methyl-7-oxo-6,7-dihydro-1H-pyrazolo[3,4-c]pyridin-4-yl)quinoxalin-2(1H)-one;

4-[4-(Cyclopropylmethoxy)-1-methyl-1H-indazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-[4-(Cyclopropylmethoxy)-1-methyl-1H-indazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-7-(1-hydroxyethyl)-1-methyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one;

4-(2,4-Difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-7-{[(2-morpholin-4-ylethyl)amino]methyl}-1,3-dihydro-2H-benzimidazol-2-one;

7-[(Benzylamino)methyl]-4-(2,4-difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

7-{[(Cyclopropylmethyl)amino]methyl)}-4-(2,4-difluorophenoxy)-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-[4-(2,4-Difluorophenoxy)-1-methyl-1H-benzimidazol-5-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

4-[4-(2,4-Difluorophenoxy)-1-methyl-1H-benzimidazol-5-yl]-6-ethyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

6-Benzyl-4-[4-(2,4-difluorophenoxy)-1-methyl-1H-benzimidazol-5-yl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

{4-[4-(2,4-Difluorophenoxy)-1-methyl-1H-benzimidazol-5-yl]-7-oxo-1,7-dihydro-6H-pyrrolo[2,3-c]pyridin-6-yl}acetonitrile;

4-(4-Chlorophenoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(3-Chlorophenoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(Cyclohexylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(Cyclobutyloxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(Cyclohexyloxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

1-Methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(tetrahydro-2H-pyran-3-yloxy)-1,3-dihydro-2H-benzimidazol-2-one;

4-(Cyclopentylmethoxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(Cyclopentyloxy)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

6-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-5-phenoxy-2H-1,4-benzoxazin-3(4H)-one;

2,2-Dimethyl-6-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-5-phenoxy-2H-1,4-benzoxazin-3(4H)-one;

6-Methyl-4-(4-phenoxy-1,3-benzoxazol-5-yl)-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

1-Methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(phenylthio)-1,3-dihydro-2H-benzimidazol-2-one;

4-(Ethylthio)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-(Ethylsulfonyl)-1-methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one;

4-Methyl-6-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-5-phenoxy-2H-1,4-benzoxazin-3(4H)-one;

4-Benzyl-6-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-5-phenoxy-2H-1,4-benzoxazin-3(4H)-one;

6-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(2-morpholin-4-ylethyl)-5-phenoxy-2H-1,4-benzoxazin-3(4H)-one;

4-[2-(Aminomethyl)-4-phenoxy-1,3-benzoxazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

N-{[5-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1,3-benzoxazol-2-yl]methyl}acetamide;

N-{[5-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1,3-benzoxazol-2-yl]methy}methanesulfonamide′

N-{[5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1,3-benzoxazol-2-yl]methyl}benzamide;

N-{[5-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1,3-benzoxazol-2-yl]methy}-2-phenylacetamide;

N-{[5-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1,3-benzoxazol-2-yl]methy}cyclopropanecarboxamide;

2-Cyclopentyl-N-{[5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1,3-benzoxazol-2-yl]methyl}acetamide;

6-Methyl-4-(5-phenoxy-3-phenyl-3,4-dihydro-2H-1,4-benzoxazin-6-yl)-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one;

N-{[1-Methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1H-benzimidazol-2-yl]methyl}cyclobutanecarboxamide;

N-{[1-Methyl-5-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1H-benzimidazol-2-yl]methy}cyclopropanecarboxamide;

3-[5-(6-Methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-1H-benzimidazol-1-yl]propanenitrile; and

4-(7-Ethoxy-2,5-dimethylpyrazolo[1,5-a]pyrimidin-6-yl)-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one,

or a pharmaceutically acceptable salt thereof.

57. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

58. A method of inhibiting a bromodomain and extra-terminal protein comprising contacting a compound of claim 1 , or a pharmaceutically acceptable salt thereof, with said bromodomain and extra-terminal protein.

59. A method of inhibiting bromodomain and extra-terminal protein activity in a patient comprising administering to the patient a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

60. A compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

represents a single or double bond;

Ring B is phenyl, 5-6 membered heteroaryl, C 5-6 cycloalkyl, or 5-6 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 R B ;

L is absent, —(CR a R b ) p —, (CR a R b ) n —O—(CR a R b ) m —, —(CR a R b ) n —S—(CR a R b ) m —, —(CR a R b ) n —S(═O)—(CR a R b ) m —, —(CR a R b ) n —S(═O) 2 —(CR a R b ) m —, —(CR a R b ) n —C(═O)—(CR a R b ) m —, —(CR a R b ) n —C(═O)O—(CR a R b ) m —, —(CR a R b ) n —OC(═O)—(CR a R b ) m —, —(CR a R b ) n —NR—(CR a R b ) m —, —(CR a R b ) n —C(═O)NR—(CR a R b ) m —, —(CR a R b ) n —NR c C(═O)—(CR a R b ) m —, or —(CR a R b ) n —NR c C(═O)NR d —(CR a R b ) m —;

A1 is CR 3 or N;

A2 is CR 4 or N;

A3 is C or N;

A4 is C or N;

wherein when one of A3 and A4 is N, then the other of A3 and A4 is C;

W is CR 5 ;

X is CR 6 ;

Y is CR 7 or N;

Z is C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, or 4-10 membered heterocycloalkyl, each of which is optionally substituted by 1, 2, 3, 4, or 5 R Z ;

R 1 is H or C 1-4 alkyl;

R 2 is C 1-4 alkyl, C 1-4 haloalkyl, or C 1-4 hydroxyalkyl;

R 3 and R 4 are each independently selected from H, halo, CN, NO 2 , C 1-6 alkyl, C 1-6 haloalkyl, C 2-6 alkenyl, and C 2-6 alkynyl;

R 5 is H, halo, C 1-6 alkyl, or C 1-6 haloalkyl;

R 6 is H, C 1-6 alkyl, C 1-6 haloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C(O)R b1 , C(O)NR c1 R d1 , C(O)OR a1 , S(O)R b1 , S(O)NR c1 R d1 , S(O) 2 R b1 , or S(O) 2 NR c1 R d1 , wherein said C 1-6 alkyl, C 2-6 alkenyl, and C 2-6 alkynyl are each optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from halo, C 1-4 haloalkyl, CN, NO 2 , OR a1 , SR a1 , C(O)R b1 , C(O)NR c1 R d1 , C(O)OR a1 , OC(O)R b1 , OC(O)NR c1 R d1 , NR c1 R d1 NR c1 C(O)R b1 NR c1 C(O)OR a1 , NR c1 C(O)NR c1 R d1 , C(═NR e1 )R b1 , C(═NR e1 )NR c1 R d1 , NR c1 C(═NR e1 )NR c1 R d1 NR c1 S(O)R b1 , NR c1 S(O) 2 R b1 , NR c1 S(O) 2 NR c1 R d1 , S(O)R b1 , S(O)NR c1 R d1 , S(O) 2 R b1 , and S(O) 2 NR c1 R d1 ;

R 7 is H, C 1-6 alkyl, C 1-6 haloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 , S(O)R b2 , S(O)NR c2 R d2 , S(O) 2 R b2 , or S(O) 2 NR c2 R d2 , wherein said C 1-6 alkyl, C 2-6 alkenyl, and C 2-6 alkynyl are each optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from halo, C 1-4 haloalkyl, CN, NO 2 , OR a2 , SR a2 , C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 , OC(O)R b2 , OC(O)NR c2 R d2 , NR c2 R d2 , NR c2 C(O)R b2 , NR c2 C(O)OR a2 , NR c2 C(O)NR c2 R d2 C(═NR e2 )R b2 , C(═NR e2 )NR c2 R d2 NR c2 C(═NR e2 )NR c2 R d2 NR c2 S(O)R b2 , NR c2 S(O) 2 R b2 , NR c2 S(O) 2 NR c2 R d2 , S(O)R b2 , S(O)NR c2 R d2 , S(O) 2 R b2 , and S(O) 2 NR c2 R d2 ;

each R Z is independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, CN, NO 2 , OR a4 , SR a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 , OC(O)R b4 , OC(O)NR c4 R d4 , NR c4 R d4 , NR c4 C(O)R b4 NR c4 C(O)OR a4 , NR c4 C(O)NR c4 R d4 C(═NR e4 )R b4 , C(═NR e4 )NR c4 R d4 , NR c4 C(═NR e4 )NR c4 R d4 , NR c4 S(O)R b4 , NR c4 S(O) 2 R b4 , NR c4 S(O) 2 NR c4 R d4 , S(O)R b4 , S(O)NR c4 R d4 , S(O) 2 R b4 , and S(O) 2 NR c4 R d4 ; wherein said C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 6-10 aryl, C 3-10 cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl are each optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from halo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, CN, NO 2 , OR a4 , SR a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 , OC(O)R b4 , OC(O)NR c4 R d4 , C(═NR e4 )NR c4 R d4 , NR c4 C(═NR e4 )NR c4 R d4 , NR c4 R d4 , NR c4 C(O)R b4 , NR c4 C(O)OR a4 , NR c4 C(O)NR c4 R d4 , NR c4 S(O)R b4 , NR c4 S(O) 2 R b4 , NR c4 S(O) 2 NR c4 R d4 , S(O)R b4 , S(O)NR c4 R d4 , S(O) 2 R b4 , and S(O) 2 NR c4 R d4 ;

each R a and R b is independently selected from H, halo, OH, methyl, and ethyl;

each R c and R d is independently selected from H, C 1-4 alkyl, C 1-4 haloalkyl, C 1-4 hydroxyalkyl, and cyclopropyl;

or any R c2 and R d2 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, 5-6 membered heteroaryl, C 1-6 haloalkyl, halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 SR d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 NR c5 C(O)R b5 NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 , wherein said C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, and 5-6 membered heteroaryl are optionally substituted by 1, 2, or 3 substituents independently selected from halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 ;

or any R c3 and R d3 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, 5-6 membered heteroaryl, C 1-6 haloalkyl, halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 , wherein said C 1-6 alkyl, C 3-7 cycloalkyl, 4-7 membered heterocycloalkyl, C 6-10 aryl, and 5-6 membered heteroaryl are optionally substituted by 1, 2, or 3 substituents independently selected from halo, CN, OR a5 , SR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , OC(O)R b5 , OC(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)NR c5 R d5 , NR c5 C(O)OR a5 , C(═NR e5 )NR c5 R d5 , NR c5 C(═NR e5 )NR c5 R d5 S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , NR c5 S(O) 2 R b5 , NR c5 S(O) 2 NR c5 R d5 , and S(O) 2 NR c5 R d5 ;

each R e1 , R e2 , R e3 , and R e4 is independently selected from H, C 1-4 alkyl, CN, OR a5 , SR b5 , S(O) 2 R b5 , C(O)R b5 , S(O) 2 NR c5 R d5 , and C(O)NR c5 R d5 ;

each R a5 , R b 5, R c5 , and R d5 is independently selected from H, C 1-4 alkyl, C 1-4 haloalkyl, C 2-4 alkenyl, and C 2-4 alkynyl, wherein said C 1-4 alkyl, C 2-4 alkenyl, and C 2-4 alkynyl, is optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio, C 1-4 alkylamino, di(C 1-4 alkyl)amino, C 1-4 haloalkyl, and C 1-4 haloalkoxy;

each R e5 is independently selected from H, C 1-4 alkyl, and CN;

n is 0, 1, or 2;

m is 0, 1, or 2; and

p is 1, 2, 3, or 4;

wherein any aforementioned heterocycloalkyl group is optionally substituted by 1 or 2 oxo groups.

Assignments (2)

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 10, 2021

From: INCYTE CORPORATION

To: INCYTE CORPORATION; INCYTE HOLDINGS CORPORATION

Reel/Frame 058815/0857 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 4, 2015

From: YUE, EDDY W.; COMBS, ANDREW P.; DOUTY, BRENT

To: INCYTE CORPORATION

Reel/Frame 034883/0963 →