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    Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders
    2.
    发明授权
    Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders 失效
    取代的2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮和7-嘧啶基-2,3-二氢咪唑并[1,2-a]嘧啶-5（1H） 神经变性疾病的衍生物

    公开(公告)号：US07388005B2

    公开(公告)日：2008-06-17

    申请号：US10490136

    申请日：2002-09-19

    申请人： Thierry Gallet ,  Patrick Lardenois ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

    发明人： Thierry Gallet ,  Patrick Lardenois ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

    IPC分类号： A61K31/551 ,  A61K31/519 ,  C07D487/04 ,  A61P25/28

    CPC分类号： A61K31/519 ,  A61K31/551 ,  C07D487/04

    摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; y represents a bond, an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a nitrogen atom being optionally; or a methylene group optionally substituted; R1 represents a pyrimidine group optionally substituted; R2 may represent a C1-6 alkyl group optionally substituted by a C6,10 aryloxy or a C6,10 arylamino group; a C3-6 cycloalkyl group, a C1-4 alkylthio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represents each independently a hydrogen atom, C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom. 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 GSK3β3 or GSK3β3 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表示两个氢原子，硫原子，氧原子或C 1-12烷基和氢 原子; y表示键，亚乙烯基，亚乙炔基，氧原子，硫原子，磺酰基，亚砜基，羰基，任选的氮原子; 或任选取代的亚甲基; R1表示任选取代的嘧啶基团; R 2可以表示任选被C 6,10芳氧基或C 6,10芳基氨基取代的C 1-6烷基; C 3-6环烷基，C 1-4烷硫基，C 1-4烷氧基，C 1 -C 4烷氧基， 1-2个全卤代烷基，C 1-3卤代烷基，苯硫基，苄基，苯环，茚满环，5,6,7， 8-四氢萘环，萘环，吡啶环，吡咯环，噻吩环，呋喃环或咪唑环; R 3和R 4各自独立地表示氢原子，C 1-6烷基，羟基，C 1-4烷氧基或卤素原子; R5表示氢原子，C 1-6烷基或卤素原子。 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GSK3β3或GSK3β3和cdk5 / p25的异常活性引起的神经变性疾病，例如阿尔茨海默病 。

    1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7pyridinyl-imidazo[1,2-alpha]pyrimidin-5(1H)-one derivatives
    3.
    发明授权
    1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7pyridinyl-imidazo[1,2-alpha]pyrimidin-5(1H)-one derivatives 失效

    公开(公告)号：US07067521B2

    公开(公告)日：2006-06-27

    申请号：US10362857

    申请日：2001-08-31

    申请人： Alistair Lochead ,  Séverine Marguerie ,  Mourad Saady ,  Philippe Yaiche

    发明人： Alistair Lochead ,  Séverine Marguerie ,  Mourad Saady ,  Philippe Yaiche

    IPC分类号： A61K31/519

    CPC分类号： A61K31/519 ,  C07D487/04

    摘要： The invention relates to an imidazo[1,2-a]pyrimidone derivative represented by formula (1) or a salt thereof, wherein: X represents a bond, an ethenylene group, and ethenylene group, a methylene group optionally substituted by one or two groups selected from a C1-6 alkyl group, a hydroxy group and a C1-4 alkoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a C1-6 alkyl group; R1 represents a 2,3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a phenyl ring, a naphthyl ring, 5,6,7,8-tetrahydronaphthyl ring, a pyridyl 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 by 1 to 4 substituents selected from a C1-6 alkyl group, a phenyl 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, a cyano, an amino, a C1-6 monoalkylamino group or a C2-10 dialkylamino group; 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.

    7-(Pyrimidin-4-yl)-Imidazo[1,2-a]Pyrimidin-5(1H)-ones as GSK3β inhibitors
    7.
    发明授权
    7-(Pyrimidin-4-yl)-Imidazo[1,2-a]Pyrimidin-5(1H)-ones as GSK3β inhibitors 失效
    7-（嘧啶-4-基） - 咪唑并[1,2-a]嘧啶-5（1H） - 酮作为GSK3beta抑制剂

    公开(公告)号：US07429663B2

    公开(公告)日：2008-09-30

    申请号：US10504679

    申请日：2003-02-26

    申请人： Alistair Lochead ,  Mourad Saady ,  Philippe Yaiche

    发明人： Alistair Lochead ,  Mourad Saady ,  Philippe Yaiche

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/04 ,  A61P3/10 ,  A61P25/28

    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: R1 wherein X represents a bond, an ethenylene group, an ethenylene 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：R 1其中X表示键，亚乙烯基，亚乙烯基， 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; R 1表示任选取代的2,4或5-嘧啶基; R 2表示C 1-6烷基，C 1-12全卤代烷基，C 1-3烷基， 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，呋喃环或呋喃环 咪唑环，苄基和环任选被取代; 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。

    Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
    8.
    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：US07232827B2

    公开(公告)日：2007-06-19

    申请号：US10504677

    申请日：2003-02-26

    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： A01N43/90 ,  A61K31/519 ,  C07D471/00 ,  C07D487/00

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

    摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (I) X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring optionally substituted; R2 represents a heterocyclic bicyclic rings, having 1–4 heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and having 5–9 carbon atoms, of formula (II) R3 represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-4 alkoxy group or a halogen atom. 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 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：（I）X表示两个氢原子，硫原子，氧原子或C 1-12烷基 和氢原子; Y表示键，亚乙烯基，亚乙炔基或任选取代的亚甲基; R1表示2,3或4-吡啶环或任选取代的2,4或5-嘧啶环; R 2表示具有1-4个选自氧原子，硫原子和氮原子并且具有5-9个碳原子的杂原子的式（II）的杂环双环，R 3表示氢原子，C 1 -C 1-6烷基，羟基，C 1-4烷氧基或卤素原子; R 4表示氢原子，C 1-6烷基，C 1-4烷氧基或卤素原子。 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GSK3β或GSK3β和cdk5 / p25的异常活性引起的神经变性疾病，例如阿尔茨海默病

    Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
    9.
    发明授权
    Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives 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

    公开(公告)号：US07217715B2

    公开(公告)日：2007-05-15

    申请号：US11224873

    申请日：2005-09-13

    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： C07D487/04 ,  A61K31/519

    CPC分类号： A61K31/519 ,  C07D487/04

    摘要： The invention relates to 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. 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）表示的取代嘧啶酮衍生物或其盐：其中X，Y，R 1，R 2，R 3，R 4，R 5，n，p和q如本文所述。 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。