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93 条记录 (耗时 0.029 秒)

    Substituted N-oxide pyrazine derivatives
    23.
    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。

    Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl -6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
    28.
    发明授权
    Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl -6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives 失效
    杂芳基取代的2-吡啶基和2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物

    公开(公告)号：US07465737B2

    公开(公告)日：2008-12-16

    申请号：US11749349

    申请日：2007-05-16

    申请人： Alistair Lochead ,  Alain Nedelec ,  Mourad Saady ,  Philippe Yaiche

    发明人： Alistair Lochead ,  Alain Nedelec ,  Mourad Saady ,  Philippe Yaiche

    IPC分类号： A61K31/519

    CPC分类号： A61K31/519 ,  A01N43/90 ,  C07D487/04

    摘要： The invention relates to use of a pyrimidone derivative represented by formula (I)or a salt thereof wherein: X, Y, R1, R2, R3, R4, R5, m, n and p are as defined herein. In particular, 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 neurodegenerative disease caused by abnormal activity of GSK3β or GSK3β and cdk5/p25, such as Alzheimer disease.

    摘要翻译： 本发明涉及由式（I）表示的嘧啶酮衍生物或其盐，其中：X，Y，R 1，R 2，R 3，R 4，R 5，m，n和p如本文所定义。 特别地，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或GSK3β和cdk5 / p25的异常活性引起的神经变性疾病的预防和/或治疗，例如 阿尔茨海默病。

    Use of substituted 8-Perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives as therapeutic agents
    29.
    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
    30.
    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.