发明名称 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
摘要 Compounds of Formula I:;;or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein R1, R2, Q1, Q2, and Q3, are described in this disclosure, compositions thereof, and methods and uses thereof.
申请公布号 US2016326162(A1) 申请公布日期 2016.11.10
申请号 US201615093660 申请日期 2016.04.07
申请人 Plexxikon Inc. 发明人 Lin Jack;Pham Phuongly;Buell John;Dong Ken;Ibrahim Prabha;Spevak Wayne;Tsang Garson;Wu Guoxian;Zhang Ying
分类号 C07D471/04;A61K31/437;A61K31/506;A61K31/517;A61K31/5377;A61K31/538;C07D487/04;A61K31/4985;A61K31/541;A61K45/06;C07D519/00 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein: R1 is Formula (i) represents a single or double bond, provided that no more than one double bond to X2 exists;X1 is —O—, —S—, —N(R3), or —C(H)(R3)— when a single bond exists between X1 and X2; orX1 is —N═ when a double bond exists between X1 and X2;X2 is —N═, —C(R6)═, or ═C(R6)—N═ when a double bond exists between X2 and X1 or X2 and X3; orX2 is —N(R6)—, —C(R6)2—, or —C(H)(R6)—C(H)(R6)— when single bonds exist between X2 and both X1 and X3; orX3 is —O—, —S—, —N(R3)—, or —C(H)(R3)— when a single bond exists between X3 and X2; orX3 is —N═ or —C(R3)— when a double bond exists between X3 and X2;provided that at least one of X1, X2, or X3 is selected from —N═ or —O—;G is H, halo, alkyl optionally substituted with 1-3 halo, or alkoxy optionally substituted with 1-3 halo;Q1 is N or C(R6);Q2 is N or C(H);Q3 is N or C(R8);each R6 is independently H, halo, amino, C1-C3 alkyl optionally substituted with 1-3 halo, or C1-C3 alkoxy optionally substituted with 1-3 halo;R2 is L-Z—(R4)n;n is 1, 2 or 3;L is absent, alkynylene, —O-alkylene, —C(O)—, C(O)-alkylene-, -alkylene-C(O)—, —N(R7)—C(O)—, —C(O)—N(R7)—, —S(O)2—, —N(R7)—S(O)2—, or —S(O)2—N(R7)—;Z is absent, arylene, heteroarylene, or heterocycloalkylene; wherein Z is optionally substituted with halo, hydroxy, alkyl optionally substituted with 1-3 halo, or alkoxy optionally substituted with 1-3 halo;each R3 is independently H, amino, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, alkyl, alkoxy, hydroxyalkyl, alkoxy, arylalkyl, heteroarylalkyl, or alkylsulfonyl, wherein R3 is optionally substituted with 1-3 R5 groups;each R4 is independently H, alkyl, halo, alkoxy, hydroxy, cyano, C(O)(R7), cycloalkyl, heterocycloalkyl, heteroaryl, heterocycloalkylsulfonyl, —N(R8)(R8), —N(R7)—S(O)2-alkyl, —N(R7)—S(O)2-alkenyl, —S(O)2—N(R7)(R7), —N(H)—S(O)2-cycloalkyl, —S(O)2-cycloalkyl, cycloalkylamino, cycloalkylalkoxy, —N(H)—C(O)-alkyl, cycloalkylaminocarbonyl, carboxyl, carboxylalkyl, or carboxylalkoxy, wherein each alkyl, alkoxy, cycloalkyl, heteroaryl, or heterocycloalkyl moiety of R4 is optionally substituted with 1-3 groups independently selected from C1-C4 alkyl, C1-C3 alkoxy, cyano, hydroxy, oxo or halo;each R5 is independently halo, alkyl, alkoxy, cyano, —N(H)(R7), hydroxy, alkylsulfonyl, alkylcarbonyl, or alkoxycarbonyl, wherein each alkyl moiety of R5 is optionally substituted with 1-3 groups independently selected from halo, hydroxy, alkyl optionally substituted with 1-3 halo, or alkoxy optionally substituted with 1-3 halo;each R7 is independently H, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, alkyl, alkoxy, hydroxyalkyl, amino, hydroxy, arylalkyl, heteroarylalkyl, or alkylsulfonyl; andeach R8 is independently H or alkyl.
地址 Berkeley CA US