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93 条记录 (耗时 0.031 秒)

    Substituted N-oxide pyrazine derivatives
    41.
    发明授权
    Substituted N-oxide pyrazine derivatives 有权
    取代的N-氧化吡嗪衍生物

    公开(公告)号：US08202874B2

    公开(公告)日：2012-06-19

    申请号：US12968958

    申请日：2010-12-15

    申请人： Alistair Lochead ,  Mourad Saady ,  Philippe Yaiche

    发明人： Alistair Lochead ,  Mourad Saady ,  Philippe Yaiche

    IPC分类号： A61K31/497

    CPC分类号： A61K31/497 ,  C07D241/52 ,  C07D401/04

    摘要： N-oxide pyrazine derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: R1, R2, R3, R4, and R5 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.

    摘要翻译： 式（I）表示的N-氧化吡嗪衍生物或其盐，或其溶剂合物或其水合物：其中：R1，R2，R3，R4和R5如本公开所定义。 还公开了制备式（I）化合物及其在治疗中的用途的方法。

    1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof
    45.
    发明授权
    1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof 有权
    1,4-二氮杂双环[3.2.2]壬烷甲酰胺衍生物，其制备和治疗用途

    公开(公告)号：US07456171B2

    公开(公告)日：2008-11-25

    申请号：US11098670

    申请日：2005-04-04

    申请人： Frederic Galli ,  Patrick Lardenois ,  Odile Leclerc ,  Alistair Lochead

    发明人： Frederic Galli ,  Patrick Lardenois ,  Odile Leclerc ,  Alistair Lochead

    IPC分类号： A61P25/00 ,  A61K31/55 ,  A61K31/551 ,  C07D487/08 ,  C07D519/00

    CPC分类号： C07D487/08

    摘要： The present invention discloses and claims compounds of general formula in which X represents a nitrogen atom or a group of formula C—R2, P represents a group of formula C—R3, Q represents a group of formula C—R4, R represents a group of formula C—R5, W represents a group of formula C—R6, or one of the symbols P, Q, R and W represents a nitrogen atom, R1 represents a hydrogen atom or an alkyl group, R2 represents a hydrogen atom or an alkyl group, R3, R4, R5 and R6 each represent a hydrogen or halogen atom, or an alkyl, alkoxy, nitro, amino, trifluoromethyl, cyano or amino group or other functional groups. The compounds of the invention are useful in a variety of therapeutic applications.

    摘要翻译： 本发明公开并要求通式的化合物，其中X表示氮原子或式CR 2的基团，P表示式CR 3的基团，Q表示 式CR 4的基团，R表示式CR 5的基团，W表示式CR 6的基团，或其中之一 符号P，Q，R和W表示氮原子，R 1表示氢原子或烷基，R 2表示氢原子或烷基，R R 3，R 4，R 5和R 6各自表示氢或卤素原子，或烷基， 烷氧基，硝基，氨基，三氟甲基，氰基或氨基或其它官能团。 本发明的化合物可用于各种治疗应用。

    Use of substituted 8-Perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives as therapeutic agents
    46.
    发明授权
    Use of substituted 8-Perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives as therapeutic agents 失效
    取代的8-全氟烷基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物作为治疗剂

    公开(公告)号：US07393853B2

    公开(公告)日：2008-07-01

    申请号：US11696256

    申请日：2007-04-04

    申请人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

    发明人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

    IPC分类号： A61K31/519

    CPC分类号： A61K31/519 ,  C07D487/04

    摘要： The invention relates to use of a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as described herein for treating a variety of disease states. More specifically, the invention relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of GSK3β, such as Pick's disease.

    摘要翻译： 本发明涉及由式（I）表示的取代嘧啶酮衍生物或其盐的用途：其中X，Y，R 1，R 2，R 3，R 4，R 5，n，p和q如本文所述用于处理多种 的疾病状态。 更具体地，本发明涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β的异常活性如皮克病引起的疾病。

    Substituted 2-(diaza-bicyclo-alkyl)-pyrimidone derivatives
    47.
    发明授权
    Substituted 2-(diaza-bicyclo-alkyl)-pyrimidone derivatives 失效

    公开(公告)号：US07211581B2

    公开(公告)日：2007-05-01

    申请号：US11219923

    申请日：2005-09-06

    申请人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

    发明人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

    IPC分类号： C07D401/14 ,  C07D403/14 ,  A61K31/506 ,  A61K31/444 ,  A61P3/10

    CPC分类号： A61K31/506 ,  C07D401/14 ,  C07D487/08

    摘要： The invention relates to a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): wherein: R1 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group optionally substituted by 1 to 4 substituents selected from a halogen atom, a hydroxyl group, a C1-4 alkoxy group; a C1-2 perhalogenated alkyl group, a benzyl group, a phenethyl group, a benzyloxycarbonyl group, a C1-4 alkoxy carbonyl group, a benzene ring, a naphthalene ring, a quinoline ring, a phthalazine ring, a 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a benzenesulfonyl group, a benzoyl group, a pyridazine ring, a furan ring and an imidazole ring; each of the benzyl group, the phenethyl group, the benzyloxycarbonyl group, the benzenesulfonyl group, the benzoyl group and the benzene, naphthalene, quinoline, phthalazine, 5,6,7,8-tetrehydronaphthalene, pyridine, indole, pyrrole and thiophene rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a benzene ring, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-4 alkoxy group, a nitro group, a cyano group, an amino group, a C1-6 monoalkylamino group and a C2-10 dialkylamino group; R3 represents a 2, 4 or 5-pyrimidine ring or a 2, 3 or 4-pyridine ring, the rings being optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R4 represents a C1-4 alkyl group optionally substituted by a hydroxyl group, a C1-4 alkoxy group or a halogen atom and n represents 1 or 2; or a salt thereof, or a solvate thereof or a hydrate thereof. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer's disease.