发明申请
US20120101064A1 IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES
失效
咪唑衍生物及其作为细胞周期调节因子的调节剂
- 专利标题: IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES
- 专利标题(中): 咪唑衍生物及其作为细胞周期调节因子的调节剂
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申请号: US13266976申请日: 2010-04-30
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公开(公告)号: US20120101064A1公开(公告)日: 2012-04-26
- 发明人: Steven Howard , Paul Neil Mortenson , Steven Douglas Hiscock , Alison Jo-Anne Woolford , Andrew James Woodhead , Gianni Chessari , Marc O'reilly , Miles Stuart Congreve , Claudio Dagostin , Young Shin Cho , Fan Yang , Christine Hiu-Tung Chen , Christopher Thomas Brain , Bharat Lagu , Yaping Wang , Sunkyu Kim , John Grialdes , Michael Joseph Luzzio , Lawrence Blas Perez
- 申请人: Steven Howard , Paul Neil Mortenson , Steven Douglas Hiscock , Alison Jo-Anne Woolford , Andrew James Woodhead , Gianni Chessari , Marc O'reilly , Miles Stuart Congreve , Claudio Dagostin , Young Shin Cho , Fan Yang , Christine Hiu-Tung Chen , Christopher Thomas Brain , Bharat Lagu , Yaping Wang , Sunkyu Kim , John Grialdes , Michael Joseph Luzzio , Lawrence Blas Perez
- 申请人地址: GB Cambridge CH Basel
- 专利权人: Astex Therapeutics Limited,Novartis AG
- 当前专利权人: Astex Therapeutics Limited,Novartis AG
- 当前专利权人地址: GB Cambridge CH Basel
- 国际申请: PCT/GB2010/050725 WO 20100430
- 主分类号: A61K31/675
- IPC分类号: A61K31/675 ; A61K31/4439 ; A61K31/496 ; A61K31/4545 ; C07D413/06 ; A61K31/5377 ; C07D417/10 ; A61K31/427 ; C07D403/10 ; A61K31/4178 ; C07D409/10 ; C07D401/06 ; A61K31/4725 ; A61K31/551 ; C07D471/04 ; A61K31/437 ; C07F9/6561 ; A61P35/00 ; A61P35/02 ; C07D401/14
摘要:
The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O− or CR3; Y is N, N+—O− or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
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