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    5-PHENYL-THIAZ0L-2-YL-UREA DERIVATIVES AND USE AS PI3 KINASE INHIBITORS
    8.
    发明公开
    5-PHENYL-THIAZ0L-2-YL-UREA DERIVATIVES AND USE AS PI3 KINASE INHIBITORS 审中-公开
    5-苯基THIAZ0L -2-基 - 脲衍生物及其作为PI3激酶抑制剂的

    公开(公告)号：EP2029562A1

    公开(公告)日：2009-03-04

    申请号：EP07764541.4

    申请日：2007-05-21

    申请人： Novartis AG

    发明人： BUDD, Emma ,  HAYLER, Judy, Fox ,  BRUCE, Ian ,  LEGRAND, Darren Mark ,  COX, Brian

    IPC分类号： C07D277/48 ,  C07D417/12 ,  A61K31/427 ,  A61P11/00

    CPC分类号： C07D277/48 ,  C07D417/12

    摘要： The present invention concerns a compound of formula Ia wherein: Ra * is hydrogen or C1-C4-alkyl; Rb* is -(C1-C4-alkylene)-Y-C1-C4-haloalkyl or -(C1-C4-alkylene)-Y-C1-C4-hydroxyalkyl; Y represents -CONH- or a five membered heteroaryl group. R2* is C1-C4-alkyl or halogen; R3* is halo, -SO2-CH3, -SO2-CF3, carboxy, -CO-NH2, -CO-di(C1-C8-alkyl)amino, or a 5- or 6- membered heterocyclic ring having one or more ring hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur, that ring being optionally substituted by halo, cyano, oxo, hydroxy, carboxy, nitro, C3-C8-cycloalkyl, C1-C8-alkylcarbonyl, C1-C8-alkoxy optionally substituted by aminocarbonyl, or C1-C8-alkyl optionally substituted by hydroxy, C1- C8-alkoxy, C1- C8-alkylamino or di(C1- C8-alkyl)amino; R4* is hydrogen, halo, -SO2-CH3, nitrile, C1- C8-haloalkyl, imidazolyl, C1- C8-alkyl, -NR8*R9*, or -SO2-NR8*R9*; and R5* is hydrogen, halogen or C1- C8-alkyl; R8* and R9* are independently hydrogen, amino, C1- C8-alkylamino, di(C1- C8-alkyl)amino, or CC1- C8-alkyl optionally substituted by hydroxyl; or a pharmaceutically acceptable salt, or solvate thereof, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.