| 主权项 |
1. A compound of formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof, wherein in formula I: Y is carbon and the subscript b is the integer 1; R1 is C1-2 alkyl, C1-2 haloalkyl or —CH2—OH; R2 is C1-6 alkyl, C1-6 haloalkyl, 3-7 membered cycloalkyl, C1-6 alkylene-C3-7 membered cycloalkyl, phenyl, 5-6 membered heteroaryl, —C(═O)Rx2a, —C(═O)ORx2a or —C(═O)NRx2aRx2b, wherein Rx2a is selected from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, 3-8 membered cycloalkyl, 3-8 membered heteroalkyl, —(C1-6 alkylene)-(3-8 membered cycloalkyl), —(C1-6 alkylene)-(3-8 membered heterocycloalkyl), —(C1-6 alkylene)-(6-membered aryl) and —(C1-6 alkylene)-(5-6 membered heteroaryl) and Rx2b is selected from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and C1-6 heteroalkyl, and wherein Rx2a and Rx2b, when attached to the same nitrogen atom, are optionally combined to form a 3-7 membered heterocycloalkyl further comprising 0-2 additional heteroatoms selected from N, O and S; or alternatively R1 and R2 are combined to form a 3-8 membered cycloalkyl or 3-8 membered heterocycloalkyl and optionally fused thereto is a 5-6 membered heteroaryl ring comprising 1-3 heteroatoms selected from N, O and S; and
wherein the aliphatic and/or aromatic portions of R1 and R2 either independently or when combined, are optionally substituted with 1 to 5 RR1/2 substituents selected from the group consisting of F, Cl, Br, I, —OH, —NH2, —SH, —CF3, —OCF3, —SF5, —OCH3, —(Xa)0-1—CN, —(Xa)0-1—NO2, —(Xa)0-1—N3, —(Xa)0-1—OH, —(Xa)0-1—H, —(Xa)0-1—ORa, —(Xa)0-1—N(H)Ra, —(Xa)0-1—N(H)2, —(Xa)0-1—N(Ra)2, —(Xa)0-1—SRa, —(Xa)0-1—SH, —(Xa)0-1—C(O)Ra, —(Xa)0-1—S(O)2Ra, —(Xa)0-1—S(O)Ra, —(Xa)0-1—N(H)S(O)2Ra, —(Xa)0-1—N(H)S(O)2Ra, —(Xa)0-1—N(Ra)S(O)2Ra, —(Xa)0-1—OC(O)Ra, —(Xa)0-1—N(H)C(O)ORa, —(Xa)0-1—N(Ra)C(O)ORa, —(Xa)0-1—C(═O)ORa, —(Xa)0-1—C(═O)OH, —(Xa)0-1—C(═O)N(H)Ra, —(Xa)0-1—C(═O)N(Ra)Ra, —(Xa)0-1—N(H)C(═O)Ra, —(Xa)0-1—N(Ra)C(═O)Ra, —(Xa)0-1—N(H)C(═O)ORa and —(Xa)0-1—N(Ra)C(═O)ORa, wherein Xa is selected from the group consisting of C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, C1-6 heteroalkylene, 3-6 membered cycloalkylene and 3-6 membered heterocycloalkylene, and Ra at each occurrence is independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, 3-7 membered cycloalkyl and 3-7 membered heterocycloalkyl; A is selected from the group consisting of: wherein
X1, X2 and X3 are independently CR5, wherein R5 is selected from the group consisting of hydrogen, C1-4 alkyl, C1-4 haloalkyl, halogen, —OC1-6 alkyl, 3-6 membered heterocycloalkyl-C1-3 alkyleneoxy-, —CN, —NO2, —NH(C1-6 alkyl), —NH2 and —N(C1-6 alkyl)2;R3 is 5-10 membered heteroaryl optionally substituted with —NRx3aRx3b, wherein Rx3a and Rx3b are each independently selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 heteroalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, and wherein R3 and the Rx3a and Rx3b groups of R3, if present, are further each independently optionally substituted with 1 to 5 RR3 substituents selected from the group consisting of F, Cl, Br, I, —OH, —NH2, —SH, —CF3, —OCF3, —SF5, —OCH3, —(Xb)0-1—CN, —(Xb)0-1—NO2, —(Xb)0-1—N3, —(Xb)—OH, —(Xb)—H, —(Xb)0-1—ORb, —(Xb)0-1—N(H)Rb, —(Xb)—N(H)2, —(Xb)0-1—N(Rb)2, —(Xb)0-1—SRb, —(Xb)0-1—SH, —(Xb)0-1—C(O)Rb, —(Xb)0-1—S(O)2Rb, —(Xb)0-1—S(O)Rb, —(Xb)0-1—N(H)S(O)2Rb, —(Xb)0-1—N(Rb)S(O)2Rb, —(Xb)0-1—OC(O)Rb, —(Xb)0-1—N(H)C(O)ORb, —(Xb)0-1—N(Rb)C(O)ORb, —(Xb)0-1—C(═O)ORb, —(Xb)0-1—C(═O)OH, —(Xb)0-1—C(═O)N(H)Rb, —(Xb)0-1—C(═O)N(Rb)Rb, —(Xb)0-1—N(H)C(═O)Rb, —(Xb)0-1—N(Rb)C(═O)Rb, —(Xb)0-1—N(H)C(═O)ORb and —(Xb)0-1—N(Rb)C(═O)ORb, wherein Xb is selected from the group consisting of C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, C1-6 heteroalkylene, C3-6 cycloalkylene and C3-6 heterocycloalkylene, and Rb at each occurrence is independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, 3-7 membered cycloalkyl and 3-7 membered heterocycloalkyl;R4 is -(L)0-1—Rx4a, wherein L is selected from the group consisting of —O—, —N(H)—, —C(═O)—, C1-4 alkylene, C1-4 haloalkylene, C2-4 alkenylene, C2-4 alkynylene and C1-4 heteroalkylene and Rx4a is selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl and C1-6 heteroalkyl, 3-6 membered cycloalkyl, 3-9 membered heterocycloalkyl, 6-10 membered aryl and 5-10 membered heteroaryl, wherein the aliphatic or aromatic portions of R4 are independently substituted with 0 to 5 RR4 substituents selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, C1-6 heteroalkyl, C1-6 alkoxy, C1-6 alkylamino, C1-6 dialkylamino, C3-6 heterocycloalkyl, F, Cl, Br, I, —OH, —NH2, —SH, —CF3, —OCF3, —SF5, —(Xc)0-1—CN, —(Xc)0-1—NO2, —(Xc)0-1—N3, —(Xc)—OH, —(Xc)0-1—ORc, —(Xc)—H, —(Xc)0-1—Rc, —(Xc)0-1—N(H)Rc, —(Xc)0-1—N(Rc)2, —(Xc)0-1—SRc, —(Xc)0-1—C(O)Rc, —(Xc)0-1—S(O)2Rc, —(Xc)0-1—S(O)Rc, —(Xc)0-1—N(H)S(O)2Rc, —(Xc)0-1—N(Rc)S(O)2Rc, —(Xc)0-1—C(═O)ORc, —(Xc)0-1—C(═O)OH, —(Xc)0-1—C(═O)N(H)Rc, —(Xc)0-1—C(═O)N(Rc)Rc, —(Xc)0-1—N(H)C(═O)Rc, —(Xc)0-1—N(Rc)C(═O)Rc, wherein Xc is selected from the group consisting of C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, C1-6 heteroalkylene, C3-6 cycloalkylene and C3-6 heterocycloalkylene, and Rc at each occurrence is independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, 3-7 membered cycloalkyl, 3-7 membered heterocycloalkyl, phenyl and 5-6 membered heteroaryl, wherein any two Rc groups attached to the same nitrogen atom are optionally combined to form a 3-7 membered heterocycloalkyl or 5-10 membered heteroaryl comprising 1-3 heteroatoms selected from N, O and S. |
