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 <p>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).</p>
申请公布号 SI2256106(T1) 申请公布日期 2015.10.30
申请号 SI20040032244T 申请日期 2004.07.22
申请人 ASTEX THERAPEUTICS LIMITED 发明人 BERDINI VALERIO;O'BRIEN MICHAEL ALISTAIR;CARR MARIA GRAZIA;EARLY THERESA RACHEL;GILL ADRIAN LIAM;TREWARTHA GARY;WOOLFORD ALISON JO-ANN;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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