发明名称 3, 4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASES (CDK) AND GLYCOGEN SYNTHASE KINASE-3 (GSK-3) MODULATORS
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. Formula (0). In formula (0): X is a group R<1>-A-NR<4>- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NR<g>(C=O) or O(C=O) wherein R<g> 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; R<1> 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 0, S, NH, SO, S02; R<2> 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); R<3> is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R<4> is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).
申请公布号 WO2005012256(A1) 申请公布日期 2005.02.10
申请号 WO2004GB03179 申请日期 2004.07.22
申请人 ASTEX TECHNOLOGY LIMITED;BERDINI, VALERIO;O'BRIEN, MICHAEL, ALISTAIR;CARR, MARIA, GRAZIA;EARLY, THERESA, RACHEL;NAVARRO, EVA, FIGUEROA;GILL, ADRIAN, LIAM;TREWARTHA, GARY;WOOLFORD, ALISON, JO-ANNE;WOODHEAD, ANDREW, JAMES;WYATT, PAUL, GRAHAM 发明人 BERDINI, VALERIO;O'BRIEN, MICHAEL, ALISTAIR;CARR, MARIA, GRAZIA;EARLY, THERESA, RACHEL;NAVARRO, EVA, FIGUEROA;GILL, ADRIAN, LIAM;TREWARTHA, GARY;WOOLFORD, ALISON, JO-ANNE;WOODHEAD, ANDREW, JAMES;WYATT, PAUL, GRAHAM
分类号 A61P25/28;A61P31/10;A61P31/12;A61P35/00;A61P37/00;C07D231/14;C07D231/38;C07D231/40;C07D401/12;C07D401/14;C07D403/04;C07D403/12;C07D405/12;C07D405/14;C07D409/12;C07D409/14;C07D413/12;C07D413/14;C07D453/02;C07D471/04 主分类号 A61P25/28
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