发明公开
EP2435438A1 BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE
审中-公开
台达P110选择性双环嘧啶，其PI3K抑制化合物及使用方法
- 专利标题： BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE
- 专利标题（中）： 台达P110选择性双环嘧啶，其PI3K抑制化合物及使用方法
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申请号： EP10720979.3申请日： 2010-05-26
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公开(公告)号： EP2435438A1公开(公告)日： 2012-04-04
- 发明人: CASTANEDO, Georgette , CHAN, Bryan , GOLDSTEIN, David Michael , KONDRU, Rama K. , LUCAS, Matthew C. , PALMER, Wylie Solang , PRICE, Stephen , SAFINA, Brian , SAVY, Pascal Pierre Alexandre , SEWARD, Eileen Mary , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
- 申请人： Genentech, Inc. , F.Hoffmann-La Roche AG
- 申请人地址： 1 DNA Way South San Francisco, CA 94080 US
- 专利权人： Genentech, Inc.,F.Hoffmann-La Roche AG
- 当前专利权人： Genentech, Inc.,F.Hoffmann-La Roche AG
- 当前专利权人地址： 1 DNA Way South San Francisco, CA 94080 US
- 代理机构： Kiddle, Simon John
- 优先权： US181452P 20090527; US287607P 20091217
- 国际公布： WO2010138589 20101202
- 主分类号： C07D487/04
- IPC分类号： C07D487/04 ; C07D491/04 ; C07D513/04 ; A61K31/519 ; A61P35/00 ; A61P9/00 ; A61P29/00 ; A61P25/00
摘要：
Formula (I) ((Ia) and (Ib)) compounds wherein (i) X
1 is N and X
2 is S, (ii) X
1 is CR
7 and X
2 is S, (iii) X
1 is N and X
2 is NR
2 , or (iv) X
1 is CR
7 and X
2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. 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.
1 is N and X
2 is S, (ii) X
1 is CR
7 and X
2 is S, (iii) X
1 is N and X
2 is NR
2 , or (iv) X
1 is CR
7 and X
2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. 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.
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