发明名称 Pyridone and aza-pyridone compounds and methods of use
摘要 Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.;
申请公布号 US9505785(B2) 申请公布日期 2016.11.29
申请号 US201314059626 申请日期 2013.10.22
申请人 Gilead Connecticut, Inc.;Genentech, Inc. 发明人 Barbosa Antonio J. M.;Blomgren Peter A.;Currie Kevin S.;Krishnamoorthy Ravi;Kropf Jeffrey E.;Lee Seung H.;Mitchell Scott A.;Ortwine Daniel;Schmitt Aaron C.;Wang Xiaojing;Xu Jianjun;Young Wendy;Zhang Honglu;Zhao Zhongdong;Zhichkin Pavel E.
分类号 C07D519/00;C07D487/04;C07D495/04;C07D498/04;A61K31/497;A61K31/4985;A61K31/501;A61K31/5025;A61K31/506;A61K31/5377;A61K31/5383;A61K31/5386;A61K31/551;A61K45/06;C07D471/14 主分类号 C07D519/00
代理机构 Millen White Zelano & Branigan, P.C. 代理人 Millen White Zelano & Branigan, P.C.
主权项 1. A compound of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein: R1 is H, D, F, Cl, CN, —NH2, —NHCH3, —N(CH3)2, —OH, —OCH3, —OCH2CH3, —OCH2CH2OH, imidazolyl, pyrazolyl, oxetanyl, azetidinyl, or C1-C3 alkyl; R2, R3 and R4 are independently H, D, F, Cl, —NH2, —NHCH3, —N(CH3)2, —OH, —OCH3, —OCH2CH3, —OCH2CH2OH, or C1-C3 alkyl; R5 is optionally substituted C6-C20 aryl, C3-C12 carbocyclyl, C2-C20 heterocyclyl, C1-C20 heteroaryl, —(C6-C20 aryl)-(C2-C20 heterocyclyl), —(C1-C20 heteroaryl)-(C2-C20 heterocyclyl), —(C1-C20 heteroaryl)-(C1-C6 alkyl), or —(C1-C20 heteroaryl)-C(═O)—(C2-C20 heterocyclyl); R6 is H, F, —NH2, —OH, or optionally substituted C1-C3 alkyl; X is S, S(═O), S(═O)2, N, NR6, O, or CR7; R7 is independently H, D, F, Cl, —CH3, —CH2CH3, —CN, —CH2F, —CHF2, —CF3, —NH2, —OH, or —OCH3; Y1 and Y2 are independently CR6 or N; Z1, Z2, Z3, and Z4 are independently C, CR7, or N; Z5 is —C(R3)2C(R3)2—, —C(R3)2C(═O)—, —CR3═CR3—; one of Z1 and Z2, or X and Z1, where X is not S, S(═O), or S(═O)2, forms a five-, six-, or seven-membered aryl, carbocyclyl, heterocyclyl or heteroaryl ring; where alkyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl are optionally independently substituted with one or more of D, F, Cl, Br, I, —CH3, —CH2CH3, —CH2CH(CH3)2, —CH2OH, —CH2CH2OH, —C(CH3)2OH, —CH(OH)CH(CH3)2, —C(CH3)2CH2OH, —CH2CH2SO2CH3, —CH2OP(O)(OH)2, —CN, —CH2F, —CHF2, —CF3, —CO2H, —COCH3, —CO2CH3, —CO2C(CH3)3, —COCH(OH)CH3, —CONH2, —CONHCH3, —CON(CH3)2, —C(CH3)2CONH2, —NO2, —NH2, —NHCH3, —N(CH3)2, —NHCOCH3, —N(CH3)COCH3, —NHS(O)2CH3, —N(CH3)C(CH3)2CONH2, —N(CH3)CH2CH2S(O)2CH3, ═O, —OH, —OCH3, —OCH2CH2N(CH3)2, —OP(O)(OH)2, —S(O)2N(CH3)2, —SCH3, —CH2OCH3, —S(O)2CH3, cyclopropyl, azetidinyl, 1-methylazetidin-3-yl)oxy, N-methyl-N-oxetan-3-ylamino, azetidin-1-ylmethyl, oxetanyl, or morpholino.
地址 Foster City CA US