发明公开
- 专利标题: PYRIMIDOTHIOPHENE COMPOUNDS
- 专利标题(中): 嘧啶并噻吩化合物
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申请号: EP04768197.8申请日: 2004-08-26
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公开(公告)号: EP1675861A1公开(公告)日: 2006-07-05
- 发明人: DYMOCK, Brian William, Evotec OAI Ltd , DRYSDALE, Martin James, Vernalis (Cambridge) Ltd , FROMONT, Christofe, Vernalis (Cambridge) Ltd , JORDAN, Allan, Vernalis (Cambridge) Limited , BARRIL-ALONSO, Xavier
- 申请人: Vernalis (Cambridge) Limited , Cancer Research Technology Limited , The Institute of Cancer Research
- 申请人地址: Granta Park Abington, Cambridge CB1 6GB GB
- 专利权人: Vernalis (Cambridge) Limited,Cancer Research Technology Limited,The Institute of Cancer Research
- 当前专利权人: Vernalis (Cambridge) Limited,Cancer Research Technology Limited,The Institute of Cancer Research
- 当前专利权人地址: Granta Park Abington, Cambridge CB1 6GB GB
- 代理机构: Walls, Alan James
- 优先权: GB0320300 20030829; GB0327924 20031202; GB0414467 20040629
- 国际公布: WO2005021552 20050310
- 主分类号: C07D495/04
- IPC分类号: C07D495/04 ; A61K31/00 ; A61P35/00
摘要:
Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula -(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk' and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=O)-, -(C=S)-, -S02-, -C(=O)O-, -C(=O) NR A- , -C(=S)NR A-, -S02NR A-, -NR AC(=O)_, -NR AS02- or-NR A-wherein R A is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.
公开/授权文献
- EP1675861B1 PYRIMIDOTHIOPHENE COMPOUNDS 公开/授权日:2015-12-23
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