公开(公告)号：EP2125805A1

公开(公告)日：2009-12-02

申请号：EP07848736.0

申请日：2007-12-20

申请人： Astex Therapeutics Limited ,  The Institute of Cancer Research: Royal Cancer Hospital ,  Cancer Research Technology Limited

发明人： WOODHEAD, Steven John ,  FREDERICKSON, Martyn ,  HAMLETT, Christopher ,  WOODHEAD, Andrew James ,  VERDONK, Marinus Leendert ,  SORE, Hannah Fiona ,  WALKER, David Winter ,  BLURTON, Peter ,  COLLINS, Ian ,  CHEUNG, Kwai Ming ,  CALDWELL, John ,  DA FONSECA McHARDY, Tatiana Faria ,  LUKE, Richard William Arthur ,  MATUSIAK, Zbigniew Stanley ,  LEACH, Andrew ,  MORRIS, Jeffrey James

IPC分类号： C07D471/04 ,  C07D473/34 ,  C07D487/04 ,  C07D519/00 ,  A61K31/437 ,  A61K31/52 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D473/34 ,  C07D519/00

摘要： The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I); or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group 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); Q3 is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR2R3, CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R1a and R1b are the same or different and each is hydrogen or a substituent R10; or R1a and R1b together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R10; and R2, R3, R4, R5, R7, R6, R8, and R10 are as defined in the claims.