发明申请
WO2006070192A1 THIAZOLE AND ISOTHIAZOLE DERIVATIVES THAT MODULATE THE ACIVITY OF CDK, GSK AND AURORA KYNASES
审中-公开
基本信息:
- 专利标题: THIAZOLE AND ISOTHIAZOLE DERIVATIVES THAT MODULATE THE ACIVITY OF CDK, GSK AND AURORA KYNASES
- 专利标题(中):调节CDK,GSK和AURORA KYNASES的活性的噻唑和异噻唑衍生物
- 申请号:PCT/GB2005/005089 申请日:2005-12-30
- 公开(公告)号:WO2006070192A1 公开(公告)日:2006-07-06
- 发明人: BERDINI, Valerio , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel , WYATT, Paul, Graham
- 申请人: ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel , WYATT, Paul, Graham
- 申请人地址: 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA GB
- 专利权人: ASTEX THERAPEUTICS LIMITED,BERDINI, Valerio,O'BRIEN, Michael, Alistair,PHILLIPS, Theresa, Rachel,WYATT, Paul, Graham
- 当前专利权人: ASTEX THERAPEUTICS LIMITED,BERDINI, Valerio,O'BRIEN, Michael, Alistair,PHILLIPS, Theresa, Rachel,WYATT, Paul, Graham
- 当前专利权人地址: 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA GB
- 代理机构: HUTCHINS, Michael, Richard
- 优先权: GB0428549.0 20041230; US60/640,509 20041230
- 主分类号: C07D417/04
- IPC分类号: C07D417/04 ; C07D417/14 ; A61K31/427 ; A61P35/00
摘要:
The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR 5 or N; each of Q 1 and Q 2 is a carbon atom; Q 3 is selected from S and CH; Q 4 is selected from CR 2 and S; provided that one of Q 3 and Q 4 is S and the other of Q 3 and Q 4 is not S; wherein when Q 3 is S, there is a double bond between Q 1 and Q 4 and a double bond between Q 2 and the adjacent ring nitrogen atom N; and when Q 4 is S, there is a double bond between Q 1 and Q 2 , and a double bond between Q 3 and the adjacent ring nitrogen atom N; A is a bond or -(CH 2 ) m -(B) n -; B is C=O, NR g (C=O) or O(C=O) wherein R 1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R ° is hydrogen or, together with NR g when present, forms a group -(CH 2 ) p - wherein p is 2 to 4; R 1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C 1-8 hydrocarbyl group; R 2 is hydrogen, halogen, methoxy, or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R 3 and R 4 together with the carbon atoms to which they are attached form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, 0 and S; and R 5 is hydrogen, a group R 2 or a group R 10 wherein R 10 is as defined in the claims.The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.
摘要(中):
本发明提供式(I)化合物或其盐,N-氧化物,互变异构体或溶剂合物,其中X为CR 5或N; Q 1和Q 2中的每一个是碳原子; Q 3和S 3选自S和CH; Q 4 SUP>选自CR 2和S; 只要Q 3和Q 4中的一个是S,Q 3和Q 4中的另一个不是 S; 其中当Q 3是S时,在Q 1和Q 2之间存在双键, / SUP>和相邻环氮原子N; 并且当Q 4是S时,Q 1和Q 2之间存在双键,并且Q 3 相邻环氮原子N; A是键或 - (CH 2)m - (B)n - B为C = O,NR(C = O)或O(C = O),其中R 1为氢或任选被羟基取代的C 1-4烃基或C
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D417/00 | 杂环化合物,含两个或更多个杂环、至少有1个环有氮原子和硫原子作为仅有的杂环原子,C07D415/00组不包含的 |
--------C07D417/02 | .含有两个杂环 |
----------C07D417/04 | ..被环原子—环原子的键直接连接的 |