| 主权项 |
1. A compound of Formula (I): or a pharmaceutically acceptable salt, prodrug or stereoisomer thereof, wherein: R1 is H, OH, F or optionally substituted (C1-C3)alkyl; R2 is optionally substituted aryl, optionally substituted (C3-C8)cycloalkyl, optionally substituted heteroaryl or optionally substituted heterocyclyl; or R1 and R2 together can form an optionally substituted saturated or partially saturated carbocyclic ring or optionally substituted saturated or partially saturated heterocyclic ring; A1, A2, and A3 are independently C(RA2) or N, provided that at least one is C(RA2); X is N and Y is C, wherein:
Z is —C(Rz)2— and Z2 is —C(Rz)2—, —N(Rz1)— or —O—; orZ1 is —CH2— and Z2 is —Z2a-Z2b,
wherein Z2a is attached to Z1 and Z2b is attached to C(R1)(R2); andZ2a and Z2b are independently —C(Rz)2—, —C(Rz)2C(Rz)2—, —O— or —N(Rz1)— provided that one of Z2a and Z2b is —C(Rz)2— or —C(Rz)2C(Rz)2—; or—Z2a-Z2b-form —N(Rz1)C(O)— or —C(O)N(Rz1)—; or X is C and Y is N, provided that R1 is not —OH or —F, wherein:
Z1 is —C(Rz)2— and Z2 is —C(Rz)2—; orZ1 is —C(Rz)2— and Z2 is —Z2a-Z2b—
wherein Z2a is attached to Z1 and Z2b is attached to C(R1)(R2), andZ2a is —C(Rz)2—, —C(Rz)2C(Rz)2—, —O— or —N(Rz1), and Z2b is —C(Rz)2—, or—Z2a-Z2b-form —N(Rz1)C(O)— or —C(O)N(Rz1)—; R3 is —R3a—R3b, wherein:
R3a is an optionally substituted aryl, optionally substituted saturated or partially saturated heterocyclyl or optionally substituted heteroaryl;R3b is —CF3, —CN, —C(O)OH, —N(Ra)(Rb), —C(O)N(Ra)(Rb), —C(O)-optionally substituted heterocyclyl, —O(Ra), —S(O)2(C1-C3)alkyl, —S(O)2N(R)(Rd)—, alkyl, —S(O)2—Rc optionally substituted (C1-C5)alkyl, —(CH2)p-optionally substituted (C3-C6)cycloalkyl, —(CH2)p-optionally substituted heteroaryl or —(CH2)p-optionally substituted saturated, unsaturated or partially saturated heterocyclyl; provided that R3b is not methoxy when R2 is optionally substituted phenyl; Ra and Rb are independently selected from H, optionally substituted (C1-C5)alkyl, —C(O)-optionally substituted (C1-C5)alkyl, optionally substituted —(CH2)p—(C3-C6)cycloalkyl and —(CH2)p-optionally substituted heterocyclyl; Rc and Rd are independently selected from H, optionally substituted (C1-C5)alkyl, optionally substituted —(CH2)p—(C3-C6)cycloalkyl and —(CH2)p-optionally substituted heterocyclyl; RA2 is independently H, CF3, or (C1-C3)alkyl; Rz is independently H, F, CF3, —OH or (C1-C3)alkyl; Rz1 is independently H or (C1-C3)alkyl; and p is independently 0, 1 or 2; provided that R2 is not phenyl substituted with —OCHF2; and provided the compound is not
1-(2-methylphenyl)-7-[2-(morpholin-4-yl)pyrimidin-5-yl]-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazole;7-[2-(morpholin-4-yl)pyrimidin-5-yl]-1-phenyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazole;(1R or S)-7-(6-methylsulfonyl-3-pyridyl)-1-phenyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazole;[5-[(1R or S)-1-phenyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl]-2-pyridyl]methanol;tert-butyl 4-[5-[(1R or S)-1-phenyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl]-2-pyridyl]piperazine-1-carboxylate;(1R or S)-7-[6-chloromethyl)-3-pyridyl]-1-phenyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazole;(1R or S)-7-[(6-(methylsulfonylmethyl)-3-pyridyl]-1-phenyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazole; or(1R or S)-1-phenyl-7-[6-(piperazin-1-yl)pyridine-3-yl]-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazole. |
