| 主权项 |
1. A compound of formula (I): or a pharmaceutically acceptable salt, ester, amide, or radiolabelled form thereof, wherein: R1 is hydrogen, C1-C4-alkyl, C1-C4-fluoroalkyl, C3-C6-cycloalkyl or H2N—; R2 is hydrogen or R7O—; R3 and R6 are independently hydrogen or fluorine; R4 is hydrogen, G1-, G2-, or Y-L1-(CRaRb)f-L2-; R5 is hydrogen, R11C(O)—, R10N(H)C(O)—, R11C(O)NH—, R10N(H)SO2—, R11SO2NH—, R11CH(OH)—, R11C(O)C(O)NH—, or NC—; R7 is C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, C4-C8-cycloalkenyl, C4-C8-cycloalkenyl-C1-C4-alkyl, M4-M7-heterocycle or M4-M7-heterocycle-C1-C4alkyl, wherein:
the C1-C6-alkyl and C1-C6-fluoroalkyl are optionally substituted with 1, 2, 3, 4, or 5 substituents selected from halogen, cyano, oxo, O2N—, RsO—, RsO—(CRaRb)m—, RsC(O)O—, (Rs)(Rt)NC(O)O—, RsS—, RsS(O)—, RsS(O)2—, (Rs)(Rt)NS(O)2—, RsC(O)—, RsOC(O)—, (Rs)(Rt)NC(O)—, (Rs)(Rt)N—, RtC(O)N(Rs)—, RtOC(O)N(Rs)—, and (Rt)S(O)2N(Rs)—;the C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, C4-C8-cycloalkenyl, C4-C8-cycloalkenyl-C1-C4-alkyl, M4-M7-heterocycle and M4-M7-heterocycle-C1-C4alkyl are optionally substituted with 1, 2, 3, 4, or 5 substituents selected from C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, halogen, cyano, oxo, O2N—, RuO—, RuO—(CRaRb)m—, RuC(O)O—, (Ru)(Rv)NC(O)O—, RuS—, RuS(O)—, RuS(O)2—, (Ru)(Rv)NS(O)2—, RuC(O)—, RuOC(O)—, (Ru)(Rv)NC(O)—, (Ru)(Rv)N—, RvC(O)N(Ru)—, (Rv)OC(O)N(Ru)—, (Rv)S(O)2N(Ru)—, and C1-C4-haloalkyl; R10 is hydrogen, C1-C6-alkyl, or C3-C7-cycloalkyl; R11 is C1-C6-alkyl or C2-C6-alkenyl; Ra and Rb, at each occurrence, are each independently hydrogen, C1-C4-alkyl, or C1-C4-haloalkyl; Rc, at each occurrence, is independently hydrogen, C1-C4-alkyl, C3-C6-cycloalkyl or C1-C4-haloalkyl; Rs, Rt, Ru, and Rv are, at each occurrence, independently hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C6-haloalkyl; G1 is monocyclic M4-M7-heterocycle unsubstituted or optionally substituted with 1, 2, 3, or 4 substituents selected from C1-C8-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, halogen, cyano, oxo, O2N—, RuS(O)—, RuS(O)2—, G1aS(O)2—, (Ru)(Rv)NS(O)2—, RuC(O)—, RuOC(O)—, (Ru)(Rv)NC(O)—, RuO—, RuO—(CRaRb)h—, RuO—(CRaRb)k—O—(CRaRb)j—, RuO—(CRaRb)k—OC(O)—, G1a-, G1aC(O)—, G1a-(CRaRb)p—, G1a-(CRaRb)p—C(O)—, G1a-OC(O)—, G1a-(CRaRb)p—OC(O)—, G1b-, G1bC(O)—, G1b-(CRaRb)p—, G1bC(O)—(CRaRb)p, G1b-(CRaRb)p—OC(O)—, G1b-(CRaRb)p—C(O)—, G1c-, G1cC(O)—, G1c-(CRaRb)h—, G1cC(O)—(CRaRb)p—, G1c-(CRaRb)p—OC(O)—, G1c-(CRaRb)p—C(O)—, (Ru)(Rv)N—, RvC(O)N(Ru)—, (Rv)OC(O)N(Ru)—, (Rv)S(O)2N(Ru)—, and C1-C4-haloalkyl; G1a is aryl or heteroaryl wherein the aryl or heteroaryl are optionally substituted with 1, 2, 3, 4, or 5 substituents selected from C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, halogen, cyano, O2N—, RuO—, RuO—(CRaRb)m—, RuC(O)O—, (Ru)(Rv)NC(O)O—, RuS—, RuS(O)—, RuS(O)2—, (Ru)(Rv)NS(O)2—, RuC(O)—, RuOC(O)—, (Ru)(Rv)NC(O)—, (Ru)(Rv)N—, RvC(O)N(Ru)—, (Rv)OC(O)N(Ru)—, (Rv)S(O)2N(Ru)—, and C1-C4-haloalkyl; G1b is C3-C8-cycloalkyl or C4-C8-cycloalkenyl, wherein the C3-C8-cycloalkyl or C4-C8-cycloalkenyl are optionally substituted with 1, 2, 3, 4, or 5 substituents selected from C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, halogen, cyano, O2N—, RuO—, RuO—(CRaRb)m—, RuC(O)O—, (Ru)(Rv)NC(O)O—, RuS—, RuS(O)—, RuS(O)2—, (Ru)(Rv)NS(O)2—, RuC(O)—, RuOC(O)—, (Ru)(Rv)NC(O)—, (Ru)(Rv)N—, RvC(O)N(Ru)—, (Rv)OC(O)N(Ru)—, (Rv)S(O)2N(Ru)—, and C1-C4-haloalkyl; G1c is M4-M7-heterocycle M7-heterocycle wherein the M4-M7-heterocycle is optionally substituted with 1, 2, 3, 4, or 5 substituents selected from C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, halogen, cyano, O2N—, RuO—, RuO—(CRaRb)m—, RuC(O)O—, (Ru)(Rv)NC(O)O—, RuS—, RuS(O)—, RuS(O)2—, (Ru)(Rv)NS(O)2—, RuC(O)—, RuOC(O)—, (Ru)(Rv)NC(O)—, (Ru)(Rv)N—, RvC(O)N(Ru)—, (Rv)OC(O)N(Ru)—, (Rv)S(O)2N(Ru)—, and C1-C4-haloalkyl; G2 is a fused-bicyclic heterocycle or spirocyclic heterocycle unsubstituted or optionally substituted with 1, 2, 3, or 4 substituents selected from C1-C8-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, halogen, cyano, oxo, O2N—, RuS(O)—, RuS(O)2—, (Ru)(Rv)NS(O)2—, RuC(O)—, RuOC(O)—, (Ru)(Rv)NC(O)—, RuO—, RuO—(CRaRb)m—, RuO—(CRaRb)n—O—(CRaRb)m—, G1a-, G1aC(O)—, G1a-(CRaRb)q—, G1b-, G1bC(O)—, G1b-(CRaRb)q—, G1bC(O)—(CRaRb)q—, (Ru)(Rv)N—, RvC(O)N(Ru)—, (Rv)OC(O)N(Ru)—, (Rv)S(O)2N(Ra)—, and C1-C4-haloalkyl; L1 and L2 are independently selected from a bond, —O—, —NRc—, —C(O)—, —RcNC(O)—, —C(O)NRc—, —RcNC(O)O—, —OC(O)NRc—, —NRcC(O)NRc—, —S(O)—, —S(O)2—, —RcNS(O)2—, and —S(O)2NRc—; X is N, CH, or CF; Y is monocyclic C3-C8-cycloalkyl, monocyclic C3-C8-cycloalkenyl, or monocyclic M4-M7-heterocycle unsubstituted or optionally substituted with 1, 2, 3, or 4 substituents selected from C1-C8-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, halogen, cyano, oxo, O2N—, RuS(O)—, RuS(O)2—, (Ru)(Rv)NS(O)2—, RuC(O)—, RuOC(O)—, (Ru)(Rv)NC(O)—, RuO—, RuO—(CRaRb)p—, (Ru)(Rv)N—, RvC(O)N(Ru)—, (Rv)OC(O)N(Ru)—, (Rv)S(O)2N(Ra)—, and C1-C4-haloalkyl; or Y is aryl or heteroaryl unsubstituted or optionally substituted with 1, 2, 3, or 4 substituents selected from C1-C8-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, halogen, cyano, O2N—, RuS(O)—, RuS(O)2—, (Ru)(Rv)NS(O)2—, RuC(O)—, RuOC(O)—, (Ru)(Rv)NC(O)—, RuO—, RuO—(CRaRb)m—, (Ru)(Rv)N—, RvC(O)N(Ru)—, (Rv)OC(O)N(Ru)—, (Rv)S(O)2N(Ru)—, and C1-C4-haloalkyl; or Y is C1-C6-alkyl or C1-C6-fluoroalkyl optionally substituted with 1, 2, 3, 4, or 5 substituents selected from halogen, cyano, oxo, O2N—, RsO—, RsC(O)O—, (Rs)(Rt)NC(O)O—, RsS—, RsS(O)—, RsS(O)2—, (Rs)(Rt)NS(O)2—, RsC(O)—, RsOC(O)—, (Rs)(Rt)NC(O)—, (Rs)(Rt)N—, RtC(O)N(Rs)—, (Rt)OC(O)N(Rs)—, and (Rt)S(O)2N(Rs)—; f is 1, 2, 3, or 4; or f is 2, 3, or 4 when the moieties attaching to each side of —(CRaRb)f— are selected from O, NRc, or a ring nitrogen atom of a monocyclic M4-M7-heterocycle when L1 is a bond; h, j, k and n are independently 2, 3, or 4; and m, p and q are independently 1, 2, 3, or 4. |
