发明名称 BENZOXEPIN PI3K INHIBITOR COMPOUND AND USE THEREOF
摘要 Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z 1 is CR 1 or N; Z 2 is CR 2 or N; Z 3 is CR 3 or N; Z 4 is CR 4 or N; and where (i) X 1 is N and X 2 is S, (ii) X 1 is S and X 2 is N, (iii) X 1 is CR 7 and X 2 is S, (iv) X 1 is S and X 2 is CR 7 ; (v) X 1 is NR 8 and X 2 is N, (vi) X 1 is N and X 2 is NR 8 , (vii) X 1 is CR 7 and X 2 is O, (viii) X 1 is O and X 2 is CR 7 , (ix) X 1 is CR 7 and X 2 is C(R 7 ) 2 , (x) X 1 is C(R 7 ) 2 and X 2 is CR 7 ; (xi) X 1 is N and X 2 is O, or (xii) X 1 is O and X 2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
申请公布号 ZA201404552(B) 申请公布日期 2015.06.24
申请号 ZA20140004552 申请日期 2014.06.20
申请人 F. HOFFMANN-LA ROCHE AG 发明人 BLAQUIERE, NICOLE;DUDLEY, DANETTE;GOLDSMITH, RICHARD A.;HEFFRON, TIM;NDUBAKU, CHUDI;PRICE, STEPHEN;WEI, BINQING;DO, STEVEN;FOLKES, ADRIAN J.;HEALD, ROBERT;KOLESNIKOV, ALEKSANDR;OLIVERO, ALAN G.;STABEN, STEVEN
分类号 A61K;A61P;C07D 主分类号 A61K
代理机构 代理人
主权项
地址