发明名称 CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
摘要 Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
申请公布号 US2016304471(A1) 申请公布日期 2016.10.20
申请号 US201615044966 申请日期 2016.02.16
申请人 NEUPHARMA, INC. 发明人 Qian Xiangping;Zhu Yong-Liang
分类号 C07D239/84;C07D473/30;C07D403/12;C07D401/04;C07D401/12 主分类号 C07D239/84
代理机构 代理人
主权项 1. A compound of Formula I: or a pharmaceutically acceptable salt thereof, whereinis aryl or heteroaryl;is selected from a group consisting of: wherein; a is point of attachment for L and b is point of attachment for G; X3 is C—R3, or N; X4 is C—R4, or N; X5 is C—R5, or N; X6 is C—R19, or N; X7 is C—R20, or N; X8 is C—R21, or N; Y is O, S, or N—R22; L is —[(CR30R31)x—O—(CR32R33)]z—, —[(CR30R31)x]z—, —[(CR30R31)x—S—(CR30R31)y]z—, —[(CR30R31)x—NR29—(CR30R31)y]z—, —[(CR30R31)x—CO—(CR30R31)y]z—, —[(CR30R31)x—SO2—(CR30R31)y]z—, —[(CR30R31)x—CO2—(CR30R31)y]z—, or —[(CR30R31)x—CONR29—(CR30R31)y]z—, or —[(CR30R31)y]z—; each of R3, R4, R5, R6, R14, R15, R16, R19, R20, R21, R30, R31, R32, R33, and G is independently hydrogen, cyano, halo, hydroxy, azido, nitro, carboxy, oxo, sulfinyl, sulfanyl, sulfonyl, optionally substituted alkoxy, optionally substituted cycloalkyloxy, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted heterocycloalkyloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted amino, optionally substituted acyl, optionally substituted alkoxycarbonyl, optionally substituted aminocarbonyl, optionally substituted aminosulfonyl, or optionally substituted carbamimidoyl; R17, R18, R22 and R29 are independently hydrogen, sulfonyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted acyl, optionally substituted alkoxycarbonyl, optionally substituted aminocarbonyl, optionally substituted aminosulfonyl, or optionally substituted carbamimidoyl; or R3 and R4, R4 and R5, R15 and R16, R15 and R17, R20 and R21, R20 and R22, or R21 and R22 may optionally be joined together with any intervening atoms to form an optionally substituted aryl, heteroaryl, cycloalkyl, or heterocycloalkyl ring; each Z is independently hydrogen, cyano, halo, hydroxy, azido, nitro, carboxy, oxo, sulfinyl, sulfanyl, sulfonyl, optionally substituted alkoxy, optionally substituted cycloalkyloxy, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted heterocycloalkyloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted amino, optionally substituted acyl, optionally substituted alkoxycarbonyl, optionally substituted aminocarbonyl, optionally substituted aminosulfonyl, optionally substituted carbamimidoyl, or E; wherein E is an electrophilic group capable of forming a covalent bond with a nucleophile; n is 0, 1, 2, 3, 4 or 5; and x, y, and z are independently 0, 1, 2, 3, or 4; provided that whenG iswhereinis aryl, heteroaryl, or heterocycloalkyl; m is 0, 1, 2, 3, 4, or 5 and each Q is independently hydrogen, cyano, halo, hydroxy, azido, nitro, carboxy, oxo, sulfinyl, sulfanyl, sulfonyl, optionally substituted alkoxy, optionally substituted cycloalkyloxy, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted heterocycloalkyloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted amino, optionally substituted acyl, optionally substituted alkoxycarbonyl, optionally substituted aminocarbonyl, optionally substituted aminosulfonyl, optionally substituted carbamimidoyl, or E; and L is —NH—; then n is 1, 2, 3, 4, or 5, and at least one Z is E.
地址 Foster City CA US