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    SUBSTITUTED HETEROARYL PYRIDOPYRIMIDONE DERIVATIVES
    4.
    发明申请
    SUBSTITUTED HETEROARYL PYRIDOPYRIMIDONE DERIVATIVES 有权
    取代的杂芳基吡咯烷酮衍生物

    公开(公告)号：US20090306088A1

    公开(公告)日：2009-12-10

    申请号：US12487270

    申请日：2009-06-18

    申请人： Aude FAYOL ,  Thierry GALLET ,  Alistair LOCHEAD ,  Mourad SAADY ,  Corinne VERONIQUE ,  Philippe YAICHE

    发明人： Aude FAYOL ,  Thierry GALLET ,  Alistair LOCHEAD ,  Mourad SAADY ,  Corinne VERONIQUE ,  Philippe YAICHE

    IPC分类号： A61K31/519 ,  C07D471/04 ,  A61P25/00

    CPC分类号： A01N43/90 ,  C07D239/70

    摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof are disclosed and claimed. Wherein m, n, o, Y, Z, R1, R2, R3, R4, R5 R6 and R7 are as described herein. Also disclosed are the salts of compounds of formula (I). 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： 公开并要求保护由式（I）表示的嘧啶酮衍生物或其盐，或其溶剂合物或其水合物。 其中m，n，o，Y，Z，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所述。 还公开了式（I）化合物的盐。 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，所述活性成分用于预防和/或治疗由GSK3β如阿尔茨海默病异常活动引起的神经变性疾病。

    HETEROARYL SUBSTITUTED 2-PYRIDINYL AND 2-PYRIMIDINYL -6,7,8,9-TETRAHYDROPYRIMIDO[1,2-a] PYRIMIDIN-4-ONE DERIVATIVES
    5.
    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
    10.
    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。