发明名称 3,4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASE AND GLYCOGEN SYNTHASE KINASE-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. In formula (0): X is a group R<SUP>1</SUP>-A-NR<SUP>4</SUP>- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO<SUB>2</SUB>, C-O, NR<SUP>g</SUP>(C-O) or O(C-O) wherein R<SUP>g </SUP>is hydrogen or C<SUB>1-4 </SUB>hydrocarbyl optionally substituted by hydroxy or C<SUB>1-4 </SUB>alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R<SUP>1 </SUP>is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C<SUB>1-8 </SUB>hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C<SUB>1-4 </SUB>hydrocarbyloxy, amino, mono- or di-C<SUB>1-4 </SUB>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, SO<SUB>2</SUB>; R<SUP>2 </SUP>is hydrogen; halogen; C<SUB>1-4 </SUB>alkoxy (e.g. methoxy); or a C<SUB>1-4 </SUB>hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C<SUB>1-4 </SUB>alkoxy (e.g. methoxy); R<SUP>3 </SUP>is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R<SUP>4 </SUP>is hydrogen or a C<SUB>1-4 </SUB>hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C<SUB>1-4 </SUB>alkoxy (e.g. methoxy).
申请公布号 US2008269207(A1) 申请公布日期 2008.10.30
申请号 US20070875470 申请日期 2007.10.19
申请人 ASTEX THERAPEUTICS, LTD. 发明人 BERDINI VALERIO;O'BRIEN MICHAEL ALISTAIR;CARR MARIA GRAZIA;EARLY THERESA RACHEL;GILL ADRIAN LIAM;TREWARTHA GARY;WOOLFORD ALISON JO-ANNE;WOODHEAD ANDREW JAMES;WYATT PAUL GRAHAM
分类号 A61K31/541;A61K31/415;A61K31/454;A61K31/5377;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;C07D417/12;C07D453/02;C07D471/04 主分类号 A61K31/541
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