发明名称 Substituted quinazolines for inhibiting kinase activity
摘要 Chemical entities that are kinase inhibitors, pharmaceutical compositions containing the same, and methods of use thereof are described. Specifically quinazoline derivatives of Formula Ia:; and their uses in modulating kinase activities are disclosed.
申请公布号 US9550770(B2) 申请公布日期 2017.01.24
申请号 US201414466896 申请日期 2014.08.22
申请人 NeuPharma, Inc. 发明人 Qian Xiangping;Zhu Yong-Liang
分类号 C07D471/04;A61K31/5377;A61K45/06;A61K31/517;C07D239/84;C07D401/04;C07D401/12;C07D401/14;C07D403/04;C07D403/12;C07D405/12;C07D413/12 主分类号 C07D471/04
代理机构 Wilson Sonsini Goodrich & Rosati 代理人 Wilson Sonsini Goodrich & Rosati
主权项 1. A compound having the structure of Formula Ia: or a pharmaceutically acceptable salt thereof, wherein X1 is C—R2, or N;X2 is C—R11, or N;X3 is C—R12;X4 is C—R13;X5 is C—R14; R1, R2, R3, R4, R5, R6, R7, R11, R12, R13, and R14 are independently hydrogen, cyano, halo, hydroxy, azido, nitro, carboxy, 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; and R8, R9, and R10 are independently hydrogen, cyano, halo, hydroxy, azido, nitro, carboxy, 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; andwherein at least one of R8, R9, and R10 is E.
地址 Foster City CA US
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