The Institute of Cancer Research: Royal Cancer Hospital;CANCER RESEARCH TECHNOLOGY LIMITED;Astex Therapeutics Limited
发明人:
Berdini, Valerio,Boyle, Robert George,Saxty, Gordon,Woodhead, Steven John,Wyatt, Paul Graham,Caldwell, John,Collins, Ian,Da Fonseca , Tatiana Faria,Walker, David Winter,Donald, Alastair
申请号：
DK10184485
公开号：
DK2272517T4
申请日:
2005.10.25
申请国别(地区):
DK
年份:
2017
代理人:
摘要：
The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5 ； J 1 -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N-C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 )； E is a monocyclic carbocyclic or hctcrocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S； Q 1 is a bond or a saturated C 1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONR q or NR q CO where R q is hydrogen or methyl, or R q is a C 1-4 alkylene chain linked to R 1 or a carbon atom of Q 1 to form a cyclic moiety； and wherein the carbon atoms of the linker group Q 1 may optionally bear one or more substituents selected from fluorine and hydroxy； Q 2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, 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 may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom ± with respect to the G group； and provided that when E is aryl or heteroaryl, then Q 2 is other than a bond； G is hydrogen, NR 2 R 3 , OH or SH provided that when E is aryl or heteroaryl and Q 2 is a bond, then G is hydrogen； R 1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R 1 is hydrogen and G is NR 2 R 3 , then Q 2 is a bond； and R 2 , R 3 , R 4 , R 6 and R 8 are as defined in the claims.
