发明名称 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS
摘要 The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R<l >and NR<2>R<3> and a maximum chain length of 4 atoms extending between E and NR<2>R<3>, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the inker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR<2>R<3> group and provided that the oxo group when present is located at a carbon atom a with respect to the NR<2>R<3> group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R<l> is an aryl or heteroaryl group; and R<2>, R<3>, R<4> and R<5> are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
申请公布号 WO2005061463(A1) 申请公布日期 2005.07.07
申请号 WO2004GB05464 申请日期 2004.12.23
申请人 ASTEX TECHNOLOGY LIMITED;CANCER RESEARCH TECHNOLOGY LIMITED;THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL;BERDINI, VALERIO;SAXTY, GORDON;VERDONK, MARINUS, LEENDERT;WOODHEAD, STEVEN, JOHN;WYATT, PAUL, GRAHAM;BOYLE, ROBERT, GEORGE;SORE, HANNAH, FIONA;WALKER, DAVID, WINTER;COLLINS, IAN;DOWNHAM, ROBERT;CARR, ROBIN, ARTHUR, ELLIS 发明人 BERDINI, VALERIO;SAXTY, GORDON;VERDONK, MARINUS, LEENDERT;WOODHEAD, STEVEN, JOHN;WYATT, PAUL, GRAHAM;BOYLE, ROBERT, GEORGE;SORE, HANNAH, FIONA;WALKER, DAVID, WINTER;COLLINS, IAN;DOWNHAM, ROBERT;CARR, ROBIN, ARTHUR, ELLIS
分类号 A61K31/415;C07D231/12;C07D401/10;C07D413/10 主分类号 A61K31/415
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