发明公开
- 专利标题: SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY
- 专利标题(中): 蛋白激酶抑制效应取代的哌啶
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申请号: EP07848736.0申请日: 2007-12-20
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公开(公告)号: EP2125805A1公开(公告)日: 2009-12-02
- 发明人: WOODHEAD, Steven John , FREDERICKSON, Martyn , HAMLETT, Christopher , WOODHEAD, Andrew James , VERDONK, Marinus Leendert , SORE, Hannah Fiona , WALKER, David Winter , BLURTON, Peter , COLLINS, Ian , CHEUNG, Kwai Ming , CALDWELL, John , DA FONSECA McHARDY, Tatiana Faria , LUKE, Richard William Arthur , MATUSIAK, Zbigniew Stanley , LEACH, Andrew , MORRIS, Jeffrey James
- 申请人: Astex Therapeutics Limited , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
- 申请人地址: 436 Cambridge Science Park Milton Park Cambridge Cambridgeshire CB4 0QA GB
- 专利权人: Astex Therapeutics Limited,The Institute of Cancer Research: Royal Cancer Hospital,Cancer Research Technology Limited
- 当前专利权人: Astex Therapeutics Limited,The Institute of Cancer Research: Royal Cancer Hospital,Cancer Research Technology Limited
- 当前专利权人地址: 436 Cambridge Science Park Milton Park Cambridge Cambridgeshire CB4 0QA GB
- 代理机构: Brearley, Helen Rebecca
- 优先权: GB0625668 20061221; US871386P 20061221; US982633P 20071025
- 国际公布: WO2008075109 20080626
- 主分类号: C07D471/04
- IPC分类号: C07D471/04 ; C07D473/34 ; C07D487/04 ; C07D519/00 ; A61K31/437 ; A61K31/52 ; A61P35/00
摘要:
The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I); or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group CR5; J1-J2 is N=C(R6), (R7)C=N, (R8)N- C(O), (R8)2C-C(O), N=N or (R7)C=C(R6); Q3 is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR2R3, CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R1a and R1b are the same or different and each is hydrogen or a substituent R10; or R1a and R1b together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R10; and R2, R3, R4, R5, R7, R6, R8, and R10 are as defined in the claims.
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