SUBSTITUTED 2-ANILINOPYRIMIDINES USEFUL AS PROTEIN KINASE INHIBITORS
    2.
    发明公开
    SUBSTITUTED 2-ANILINOPYRIMIDINES USEFUL AS PROTEIN KINASE INHIBITORS 失效
    用作蛋白激酶抑制剂的取代的2-苯胺基嘧啶

    公开(公告)号:EP0862560A1

    公开(公告)日:1998-09-09

    申请号:EP96939171.0

    申请日:1996-11-20

    IPC分类号: C07D239 C07D401 C07D417

    摘要: Compounds of general formula (1) are described wherein R1 is a hydrogen or halogen atom or an optionally substitued straight or branched chain alkyl, alkenyl or alkynyl group or a group selected from hydroxyl (-OH), substituted hydroxyl, thiol (-SH), substituted thiol, amino (-NH¿2?), or substituted amino; R?2 and R3¿, which may be the same or different, is each an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R4 is a hydrogen atom or a straight or branched chain alkyl group; R5 is a hydrogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R6 is a hydrogen or halogen atom or an amino (-NH¿2?), substituted amino, nitro, carboxyl (-CO2H) or esterified carboxyl group or a group -X?1-R6a¿ where X1 is a direct bond or a linker atom or group and R6a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; X is a direct bond or a linker atom or group; R7 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein kinase inhibitors, particularly the kinases p56?lck, p59fyn¿, ZAP-70 and protein kinase C and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.