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    5-phenyl-thiazol-2-yl-urea derivatives and use as PI3 kinase inhibitors
    1.
    发明授权
    5-phenyl-thiazol-2-yl-urea derivatives and use as PI3 kinase inhibitors 失效
    5-苯基 - 噻唑-2-基 - 脲衍生物，用作PI3激酶抑制剂

    公开(公告)号：US07998990B2

    公开(公告)日：2011-08-16

    申请号：US12227315

    申请日：2007-05-21

    申请人： Emma Budd ,  Judy Fox Hayler ,  Ian Bruce ,  Darren Mark Legrand ,  Brian Cox

    发明人： Emma Budd ,  Judy Fox Hayler ,  Ian Bruce ,  Darren Mark Legrand ,  Brian Cox

    IPC分类号： A61K31/426 ,  C07D277/42

    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 ameliorated by inhibition of phosphatidylinositol 3-kinase.

    摘要翻译： 本发明涉及式Ia化合物，其中：Ra *是氢或C 1 -C 4 - 烷基; Rb *是 - （C1-C4-亚烷基）-Y-C1-C4-卤代烷基或 - （C1-C4-亚烷基）-Y-C1-C4-羟基烷基; Y表示-CONH-或五元杂芳基。 R2 *是C1-C4-烷基或卤素; R3 *是卤素，-SO2-CH3，-SO2-CF3，羧基，-CO-NH2，-CO-二（C1-C8-烷基）氨基或具有一个或多个环的5-或6-元杂环 氰基，氧代，羟基，羧基，硝基，C 3 -C 8 - 环烷基，C 1 -C 8 - 烷基羰基，任选地被C 1 -C 8 - 烷氧基取代的C 1 -C 8 - 烷氧基 被氨基羰基取代，或任选被羟基，C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷基氨基或二（C 1 -C 8 - 烷基）氨基取代的C 1 -C 8烷基; R4 *是氢，卤素，-SO2-CH3，腈，C1-C8-卤代烷基，咪唑基，C1-C8-烷基，-NR8 * R9 *或-SO2-NR8 * R9 * 和R5 *是氢，卤素或C1-C8-烷基; R 8 *和R 9 *独立地为氢，氨基，C 1 -C 8 - 烷基氨基，二（C 1 -C 8 - 烷基）氨基或任选被羟基取代的C 1 -C 8 - 烷基; 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-激酶而改善的疾病的组合物和用途。

    5-PHENYL-THIAZOL-2-YL-UREA DERIVATIVES AND USE AS PI3 KINASE INHIBITORS
    2.
    发明申请
    5-PHENYL-THIAZOL-2-YL-UREA DERIVATIVES AND USE AS PI3 KINASE INHIBITORS 失效
    5-苯基 - 噻唑-2-基-L-尿素衍生物，并用作PI3激酶抑制剂

    公开(公告)号：US20090234132A1

    公开(公告)日：2009-09-17

    申请号：US12227315

    申请日：2007-05-21

    申请人： Emma Budd ,  Judy Fox Hayler ,  Ian Bruce ,  Darren Mark Legrand ,  Brian Cox

    发明人： Emma Budd ,  Judy Fox Hayler ,  Ian Bruce ,  Darren Mark Legrand ,  Brian Cox

    IPC分类号： C07D277/46

    CPC分类号： C07D277/48 ,  C07D417/12

    摘要： The present invention concerns a compound of formula Ia wherein: Ra* is hydrogen or C1-4-alkyl; Rb* is —(C1-C4-alkylene)-Y—C1-4-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 ameliorated by inhibition of phosphatidylinositol 3-kinase.

    摘要翻译： 本发明涉及式Ia化合物，其中：R a *是氢或C 1-4 - 烷基; Rb *是 - （C 1 -C 4 - 亚烷基）-Y-C 1-4 - 卤代烷基或 - （C 1 -C 4亚烷基）-Y-C 1 -C 4 - 羟基烷基; Y表示-CONH-或五元杂芳基。 R2 *是C1-C4-烷基或卤素; R3 *是卤素，-SO2-CH3，-SO2-CF3，羧基，-CO-NH2，-CO-二（C1-C8-烷基）氨基或具有一个或多个环的5-或6-元杂环 氰基，氧代，羟基，羧基，硝基，C 3 -C 8 - 环烷基，C 1 -C 8 - 烷基羰基，任选地被C 1 -C 8 - 烷氧基取代的C 1 -C 8 - 烷氧基 被氨基羰基取代，或任选被羟基，C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷基氨基或二（C 1 -C 8 - 烷基）氨基取代的C 1 -C 8烷基; R4 *是氢，卤素，-SO2-CH3，腈，C1-C8-卤代烷基，咪唑基，C1-C8-烷基，-NR8 * R9 *或-SO2-NR8 * R9 * R5 *是氢，卤素或C1-C8-烷基; R 8 *和R 9 *独立地为氢，氨基，C 1 -C 8 - 烷基氨基，二（C 1 -C 8 - 烷基）氨基或任选被羟基取代的C 1 -C 8 - 烷基; 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-激酶而改善的疾病的组合物和用途。