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    SUBSTITUTED 8'-PYRI(MI)DINYL-DIHYDROSPIRO-[CYCLOALKYLAMINE]-PYRIMIDO[1,2-a]PYRIMIDIN-6-ONE DERIVATIVES
    52.
    发明申请
    SUBSTITUTED 8'-PYRI(MI)DINYL-DIHYDROSPIRO-[CYCLOALKYLAMINE]-PYRIMIDO[1,2-a]PYRIMIDIN-6-ONE DERIVATIVES 失效
    取代的8'-哌嗪（MI）十二烷基二 - [环己基] - 吡咯并[1,2-a]吡啶-6-酮衍生物

    公开(公告)号：US20080081820A1

    公开(公告)日：2008-04-03

    申请号：US11866687

    申请日：2007-10-03

    申请人： Nathalie CHEREZE ,  Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

    发明人： Nathalie CHEREZE ,  Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

    IPC分类号： A61K31/527 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P3/04

    CPC分类号： A61K31/527 ,  A61K31/397 ,  C07D487/04 ,  Y02P20/142

    摘要： The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom, a C1-4 alkoxy carbonyl group, a C1-5 alkyl group optionally substituted; o and m represent 1 to 2; n represents 0 to 3; p represents 0 to 2; and q represents 0 to 2. 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）表示的二氢螺环 - [环烷基胺] - 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 1-2 - 烷基和氢原子; Y表示键，羰基，任选取代的亚甲基; R1表示2,3或4-吡啶环或2,4或5-嘧啶环，该环任选被取代; R2表示苯环或萘环; 所述环任选被取代; R 3表示氢原子，C 1-6烷基或卤素原子; R4表示氢原子，C 1-4烷氧基羰基，任选取代的C 1-5烷基; o和m表示1〜2; n表示0〜3; p表示0〜2; 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 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
    54.
    发明申请
    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：US20060035910A1

    公开(公告)日：2006-02-16

    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： A61K31/519 ,  C07D487/04

    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。

    8-Substituted-6,7,8,9-tetrahydropyrimido [1,2-a] pyrimidin-4-one derivatives
    55.
    发明申请
    8-Substituted-6,7,8,9-tetrahydropyrimido [1,2-a] pyrimidin-4-one derivatives 失效
    8-取代的6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物

    公开(公告)号：US20060035885A1

    公开(公告)日：2006-02-16

    申请号：US11225218

    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： A61K31/55 ,  A61K31/519 ,  C07D487/04

    CPC分类号： A61K31/519 ,  C07D487/04

    摘要： The invention relates to substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined 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'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：其中X，Y，R 1，R 2，R 3，R 4，R 5，n，p和q如本文所定义。 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如阿尔茨海默病异常活动引起的神经变性疾病。

    Substituted 2-(diaza-bicyclo-alkyl)-pyrimidone derivatives
    56.
    发明申请
    Substituted 2-(diaza-bicyclo-alkyl)-pyrimidone derivatives 失效

    公开(公告)号：US20060025417A1

    公开(公告)日：2006-02-02

    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： A61K31/513 ,  C07D403/14

    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.

    Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
    57.
    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
    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：US20050222172A1

    公开(公告)日：2005-10-06

    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： A61K31/519 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P17/14 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P27/02 ,  A61P27/06 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04 ,  C07D519/00

    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: (1) 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：（1）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 。

    1-[alkyl 1-[heteroaryl )alkyl] and 1-[ aryl) alkyl]-7-( pyrimidin-4-yl) imadazo [1,2-a] pyrimidin-5(1h)-one derivatives
    58.
    发明申请
    1-[alkyl 1-[heteroaryl )alkyl] and 1-[ aryl) alkyl]-7-( pyrimidin-4-yl) imadazo [1,2-a] pyrimidin-5(1h)-one derivatives 失效
    1- [烷基1- [杂芳基]烷基]和1- [芳基]烷基] -7-（嘧啶-4-基）咪唑并[1,2-a]嘧啶-5（1h） - 酮衍生物

    公开(公告)号：US20050119280A1

    公开(公告)日：2005-06-02

    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： A61K31/437 ,  A61K31/519 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P17/14 ,  A61P25/02 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P27/06 ,  A61P35/00 ,  C07D487/04

    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: 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。