发明申请
- 专利标题: BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
- 专利标题(中): 苯并吡喃PI3K抑制剂化合物及其使用方法
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申请号: US12890810申请日: 2010-09-27
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公开(公告)号: US20110076291A1公开(公告)日: 2011-03-31
- 发明人: Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
- 申请人: Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
- 主分类号: A61K31/429
- IPC分类号: A61K31/429 ; C07D513/04 ; C07D495/04 ; C07D495/14 ; A61K31/381 ; A61K31/4365 ; A61K31/4245 ; A61K31/454 ; A61K31/4439 ; A61K31/5377 ; A61K31/496 ; A61K39/00 ; A61P35/00 ; A61P35/02 ; A61P29/00 ; A61P9/00 ; A61P3/10 ; A61P31/12 ; A61P7/00 ; A61P1/16
摘要:
Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 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.
公开/授权文献
- US08263633B2 Benzoxepin PI3K inhibitor compounds and methods of use 公开/授权日:2012-09-11
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