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    USE OF 7-(PYRIMIDIN-4 YL)-IMIDAZO[1,2-a]PYRIMIDIN-5(1H)-ONES AS GSK-3BETA INHIBITORS
    5.
    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。

    SUBSTITUTED HETEROARYL PYRIDOPYRIMIDONE DERIVATIVES
    10.
    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。