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    • 7. 发明申请
    • 5-PHENYL-THIAZ0L-2-YL-UREA DERIVATIVES AND USE AS PI3 KINASE INHIBITORS
    • 5-PHENYL-THIAZ0L-2-YL-UREA衍生物和用作PI3激酶抑制剂
    • WO2007134827A1
    • 2007-11-29
    • PCT/EP2007/004500
    • 2007-05-21
    • NOVARTIS AGNOVARTIS PHARMA GMBHBUDD, EmmaFOX HAYLER, JudyIAN, BruceLEGRAND, DArren MArk Novartis Horsham Research CentreCOX, Brian
    • BUDD, EmmaFOX HAYLER, JudyIAN, BruceLEGRAND, DArren MArk Novartis Horsham Research CentreCOX, Brian
    • C07D277/48C07D417/12A61K31/427A61P11/00
    • C07D277/48C07D417/12
    • The present invention concerns a compound of formula Ia wherein: R a * is hydrogen or C 1 -C 4 -alkyl; R b* is -(C 1 -C 4 -alkylene)-Y-C 1 -C 4 -haloalkyl or -(C 1 -C 4 -alkylene)-Y-C 1 -C 4 -hydroxyalkyl; Y represents -CONH- or a five membered heteroaryl group. R 2* is C 1 -C 4 -alkyl or halogen; R 3* is halo, -SO 2 -CH 3 , -SO 2 -CF 3 , carboxy, -CO-NH 2 , -CO-di(C 1 -C 8 -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, C 3 -C 8 -cycloalkyl, C 1 -C 8 -alkylcarbonyl, C 1 -C 8 -alkoxy optionally substituted by aminocarbonyl, or C 1 -C 8 -alkyl optionally substituted by hydroxy, C 1 - C 8 -alkoxy, C 1 - C 8 -alkylamino or di(C 1 - C 8 -alkyl)amino; R 4* is hydrogen, halo, -SO 2 -CH 3 , nitrile, C 1 - C 8 -haloalkyl, imidazolyl, C 1 - C 8 -alkyl, -NR 8* R 9* , or -SO 2 -NR 8* R 9* ; and R 5* is hydrogen, halogen or C 1 - C 8 -alkyl; R 8* and R 9* are independently hydrogen, amino, C 1 - C 8 -alkylamino, di(C 1 - C 8 -alkyl)amino, or CC 1 - C 8 -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.
    • 本发明涉及式Ia化合物,其中:R a a *是氢或C 1 -C 4 - 烷基; R 1是 - (C 1 -C 4 - 亚烷基)-YC 1 -C 3 - 4 - 卤代烷基或 - (C 1 -C 4 - 亚烷基)-YC 1 -C 4 - SUB> - 羟基烷基; Y表示-CONH-或五元杂芳基。 R 2是C 1 -C 4 - 烷基或卤素; R 3是卤素,-SO 2 -CH 3,-SO 2 -CF 3 羧基,-CO-NH 2,-CO-二(C 1 -C 8 - 烷基)氨基,或 具有一个或多个选自氧,氮和硫的环杂原子的5-或6-元杂环,该环任选被卤素,氰基,氧代,羟基,羧基,硝基,C C 3 -C 8 - 环烷基,C 1 -C 8 - 烷基羰基,C 1〜 任选被氨基羰基取代的C 8 - 烷氧基或任选被羟基取代的C 1 -C 8 - 烷基,C 1〜 C 1 -C 8 - 烷氧基,C 1 -C 8 - 烷基氨基或二(C 1 -C 6 - 烷基) 8 - 烷基)氨基; R 4是氢,卤素,-SO 2 -CH 3,腈,C 1 -C 3烷基, 9个 - 卤代烷基,咪唑基,C 1 -C 8 - 烷基,-NR 8 * 9 或,或-SO 2 2 -NR 8 * 9 9 * 和R 5 *是氢,卤素或C 1 -C 8 - 烷基; R 8 *和R 9 *独立地是氢,氨基,C 1 -C 8 - 烷基氨基,二 (C 1 -C 8 - 烷基)氨基或任选被下述基团取代的C 1 -C 8 - 烷基 羟; 或其药学上可接受的盐或溶剂合物,用于治疗通过抑制磷脂酰肌醇3-激酶而变质的疾病的组合物和用途。