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    HETEROARYL SUBSTITUTED 2-PYRIDINYL AND 2-PYRIMIDINYL -6,7,8,9-TETRAHYDROPYRIMIDO[1,2-a] PYRIMIDIN-4-ONE DERIVATIVES
    2.
    发明申请
    HETEROARYL SUBSTITUTED 2-PYRIDINYL AND 2-PYRIMIDINYL -6,7,8,9-TETRAHYDROPYRIMIDO[1,2-a] PYRIMIDIN-4-ONE DERIVATIVES 失效
    异噻唑基取代的2-吡啶基和2-吡啶基-6,7,8,9-四氢吡啶并[1,2-a]嘧啶-4-酮衍生物

    公开(公告)号：US20070225300A1

    公开(公告)日：2007-09-27

    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 7-(PYRIMIDIN-4 YL)-IMIDAZO[1,2-a]PYRIMIDIN-5(1H)-ONES AS GSK-3BETA INHIBITORS
    6.
    发明申请
    USE OF 7-(PYRIMIDIN-4 YL)-IMIDAZO[1,2-a]PYRIMIDIN-5(1H)-ONES AS GSK-3BETA INHIBITORS 审中-公开
    用作GSK-3BETA抑制剂的7-（PYRIMIDIN-4YL）-IMIDAZO [1,2-a] PYRIMIDIN-5（1H） - 酮的用途

    公开(公告)号：US20080318980A1

    公开(公告)日：2008-12-25

    申请号：US12194899

    申请日：2008-08-20

    申请人： Alistair LOCHEAD ,  Mourad SAADY ,  Philippe YAICHE

    发明人： Alistair LOCHEAD ,  Mourad SAADY ,  Philippe YAICHE

    IPC分类号： A61K31/519 ,  A61P25/00 ,  A61P3/04

    CPC分类号： C07D487/04

    摘要： The invention relates to a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: X represents a bond, an ethenylene group, an ethynylene group, a methylene group optionally substituted; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted; R1 represents a 2, 4 or 5-pyrimidinyl optionally substituted; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a benzene ring, a naphthalene ring, 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted; and n represents 0 to 3. 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 disease.

    摘要翻译： 本发明涉及由式（I）表示的咪唑并[1,2-a]嘧啶酮衍生物或其盐：其中X表示键，亚乙烯基，亚乙炔基，任选取代的亚甲基; 羰基，氧原子，硫原子，磺酰基，亚砜基或任选取代的氮原子; R1表示任选取代的2,4或5-嘧啶基; R2表示C1-6烷基，C1-2全卤代烷基，C1-3卤代烷基，苄基，苯环，萘环，5,6,7,8-四氢萘环，吡啶 环，吲哚环，吡咯环，噻吩环，呋喃环或咪唑环，所述苄基和所述环任选被取代; 本发明还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GSK3beta异常活动引起的神经变性疾病，例如阿尔茨海默氏症 疾病。