发明名称 ORTHO-CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E.G., PURINES) AS PROTEIN KINASES INHIBITORS
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 CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 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 CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 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 a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R is hydrogen and G is NR2R3, then Q is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims.
申请公布号 US2014303177(A1) 申请公布日期 2014.10.09
申请号 US201414310475 申请日期 2014.06.20
申请人 ASTEX THERAPEUTICS LIMITED ;THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL ;CANCER RESEARCH TECHNOLOGY LIMITED 发明人 BERDINI Valerio;BOYLE Robert George;SAXTY Gordon;WALKER David Winter;WOODHEAD Steven John;WYATT Paul Graham;DONALD Alastair;CALDWELL John;COLLINS Ian;DA FONSECA Tatiana Faria
分类号 C07D471/04;A61K31/52;A61K31/4545;C07D487/04;A61K31/519;C07D473/34;A61K31/522 主分类号 C07D471/04
代理机构 代理人
主权项
地址 Cambridge GB