发明公开
EP1883402A2 HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90
审中-公开
羟基苯甲酰胺衍生物及其作为HSP90抑制剂的用途
- 专利标题: HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90
- 专利标题(中): 羟基苯甲酰胺衍生物及其作为HSP90抑制剂的用途
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申请号: EP06726757.5申请日: 2006-04-13
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公开(公告)号: EP1883402A2公开(公告)日: 2008-02-06
- 发明人: CHESSARI, Gianni , CONGREVE, Miles Stuart , NAVARRO, Eva Figueroa , FREDERICKSON, Martyn , MURRAY, Christopher , WOOLFORD, Alison Jo-Anne , CARR, Maria Grazia , O'BRIEN,Michael Alistair , WOODHEAD, Andrew James
- 申请人: Astex Therapeutics Limited
- 申请人地址: 436 Cambridge Science Park Milton Road, Cambridge CB4 0QA GB
- 专利权人: Astex Therapeutics Limited
- 当前专利权人: Astex Therapeutics Limited
- 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: GB0507474 20050413; GB0604111 20060301; US670897P 20050413; US777989P 20060301
- 国际公布: WO2006109075 20061019
- 主分类号: A61K31/401
- IPC分类号: A61K31/401 ; A61K31/445 ; A61K31/5375 ; A61K31/166 ; C07C233/65 ; C07C233/66 ; C07D207/10 ; C07D211/34 ; C07D295/02 ; C07D309/14 ; C07D265/30 ; C07D295/18 ; C07D211/42 ; C07D211/22 ; C07D211/56
摘要:
The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy; wherein the C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy moieties are each optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; R4 is selected from hydrogen; a group -(O)n-R7 where n is 0 or 1 and R7 is an acyclic C 1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and mono- or di-C 1-5 hydrocarbyl-amino, wherein the acyclic Ci-5 hydrocarbyl group and the mono and di-C 1-5 hydrocarbylamino moieties in each instance are optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and R5 and R6 are as defined in the claims.
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