摘要 |
Disclosed are pyrazole derivative 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 R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, 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 NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the specification. Also disclosed are pharmaceutical compositions containing these compounds, methods for preparing these compounds and their use as anticancer agents. |
申请人 |
ASTEX THERAPEUTICS LIMITED;CANCER RESEARCH TECHNOLOGY LIMITED;THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL |
发明人 |
BERDINI, VALERIO;SAXTY, GORDON;VERDONK, MARINUS LEENDERT;WOODHEAD, STEVEN JOHN;WYATT, PAUL GRAHAM;SORE, HANNAH FIONA;WALKER, DAVID WINTER;COLLINS, IAN;DOWNHAM, ROBERT;CARR, ROBIN ARTHUR ELLIS |