- 专利标题: 3,4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASE AND GLYCOGEN SYNTHASE KINASE-3 MODULATORS
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申请号: US11875470申请日: 2007-10-19
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公开(公告)号: US20080269207A1公开(公告)日: 2008-10-30
- 发明人: Valerio Berdini , Michael Alistair O'Brien , Maria Grazia Carr , Theresa Rachel Early , Adrian Liam Gill , Gary Trewartha , Alison Jo-Anne Woolford , Andrew James Woodhead , Paul Graham Wyatt
- 申请人: Valerio Berdini , Michael Alistair O'Brien , Maria Grazia Carr , Theresa Rachel Early , Adrian Liam Gill , Gary Trewartha , Alison Jo-Anne Woolford , Andrew James Woodhead , Paul Graham Wyatt
- 申请人地址: GB Cambridge
- 专利权人: ASTEX THERAPEUTICS, LTD.
- 当前专利权人: ASTEX THERAPEUTICS, LTD.
- 当前专利权人地址: GB Cambridge
- 优先权: GB0317127.9 20030722
- 主分类号: A61K31/541
- IPC分类号: A61K31/541 ; C07D231/38 ; A61K31/415 ; C07D401/12 ; A61K31/454 ; C07D413/12 ; A61K31/5377 ; C07D417/12
摘要:
The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).
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