Astex Therapeutics Ltd;The Institute of Cancer Research: Royal Cancer Hospital;Cancer Research Technology Limited
发明人:
Valerio Berdini,Gordon Saxty,Marinus Leendert Verdonk,Steven John Woodhead,Paul Graham Wyatt,Robert George Boyle,Hannah Fiona Sore,David Winter Walker,Ian Collins,Robert Downham,Robin Arthur Ellis Car
申请号:
US14180440
公开号:
US09283226B2
申请日:
2014.02.14
申请国别(地区):
US
年份:
2016
代理人:
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 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 linker 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 α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR2R3 group;E is a monocyclic or bicyclic carbocyclic or heterocyclic group;R1 is an aryl or heteroaryl group; andR2, R3, R4 and R5 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.