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    1,4-diazabicyclo[3.2.2]nonane-4-carboxylates and carboxamide derivates, production and use thereof in therapeutics
    1.
    发明授权
    1,4-diazabicyclo[3.2.2]nonane-4-carboxylates and carboxamide derivates, production and use thereof in therapeutics 有权
    1,4-二氮杂双环[3.2.2]壬烷-4-羧酸酯和羧酰胺衍生物，其在治疗中的生产和应用

    公开(公告)号：US06987106B1

    公开(公告)日：2006-01-17

    申请号：US09937045

    申请日：2000-03-21

    申请人： Thierry Gallet ,  Samir Jegham ,  Patrick Lardenois ,  Alistair Lochead ,  Alain Nedelec

    发明人： Thierry Gallet ,  Samir Jegham ,  Patrick Lardenois ,  Alistair Lochead ,  Alain Nedelec

    IPC分类号： A61P25/00 ,  A61K31/551 ,  C07D471/08

    CPC分类号： C07D471/08

    摘要： Compounds of general formula in which X represents an oxygen atom or a group of formula NZ in which Z represents a hydrogen atom or an alkyl group, n represents a number 0, 1 or 2, and R1, R2, R3, R4 and R5 each represent a hydrogen or halogen atom or a trifluoromethyl, trifluoromethoxy, cyano, hydroxyl, alkyl, alkoxy, phenoxy or phenyl group optionally substituted with a halogen atom or a trifluoromethyl, cyano, hydroxyl, alkyl or alkoxy group, or alternatively R2 and R3 together form a group of formula —OCH2O— or —CH2CH2CH2CH2—. Application in therapy.

    摘要翻译： 其中X表示氧原子或式NZ的基团的通式的化合物，其中Z表示氢原子或烷基，n表示数字0,1或2，R 1， R 2，R 3，R 4和R 5各自表示氢或卤素原子或三氟甲基， 三氟甲氧基，氰基，羟基，烷基，烷氧基，苯氧基或苯基，任选被卤素原子或三氟甲基，氰基，羟基，烷基或烷氧基取代，或者R 2和R 3 一起形成式-OCH 2 O或-CH 2 CH 2 CH 2 CH 2的基团 > CH 2 - 。 应用于治疗。

    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
    4.
    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 。

    Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido{1,2-a}pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo{1,2-a}pyrimidin-5(1h)one derivatives
    7.
    发明申请
    Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido{1,2-a}pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo{1,2-a}pyrimidin-5(1h)one derivatives 失效
    取代的2-吡啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮和7-吡啶基-2,3-二氢咪唑并[1,2-a]嘧啶-5（1h） 衍生品

    公开(公告)号：US20050049261A1

    公开(公告)日：2005-03-03

    申请号：US10490135

    申请日：2002-09-19

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

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

    IPC分类号： A61K31/519 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P17/14 ,  A61P25/00 ,  A61P25/02 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P27/02 ,  A61P27/06 ,  A61P35/00 ,  A61P43/00 ,  C07D213/50 ,  C07D213/60 ,  C07D487/04

    CPC分类号： A01N43/90 ,  C07D213/50 ,  C07D213/60 ,  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 sulfur 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 sulfur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a hydroxyiminomethylene group, a dioxolan group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring optionally substituted; R2 may represent a C1-6 alkyl group optionally; a C3-6 cycloalkyl group, a C1-4 alkythio 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 represent, each independently, a hydrogen atom, a 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; with the proviso that when R3 and R4 represent each a hydrogen atom then R5 is not a hydrogen 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，亚乙烯基，亚乙炔基，氧原子，硫原子，磺酰基，亚砜基，羰基，羟基亚氨基亚甲基，二氧戊环基，任选取代的氮原子; 或任选取代的亚甲基; 或任选取代的亚甲基; R1表示任选取代的2,3或4-吡啶环; R 2可以任选地表示C 1-6烷基; C 3-6环烷基，C 1-4链炔基，C 1-4烷氧基，C1-2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，C1-6烷基或卤素原子; 条件是当R 3和R 4各自表示氢原子时，R 5不是氢原子。 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GSK3beta以及cdk5 / p25例如阿尔茨海默病的异常活动引起的神经退行性疾病 疾病。

    1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof
    8.
    发明授权
    1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof 有权
    1,4-二氮杂双环[3.2.2]壬烷甲酰胺衍生物，其制备和治疗用途

    公开(公告)号：US07456171B2

    公开(公告)日：2008-11-25

    申请号：US11098670

    申请日：2005-04-04

    申请人： Frederic Galli ,  Patrick Lardenois ,  Odile Leclerc ,  Alistair Lochead

    发明人： Frederic Galli ,  Patrick Lardenois ,  Odile Leclerc ,  Alistair Lochead

    IPC分类号： A61P25/00 ,  A61K31/55 ,  A61K31/551 ,  C07D487/08 ,  C07D519/00

    CPC分类号： C07D487/08

    摘要： The present invention discloses and claims compounds of general formula in which X represents a nitrogen atom or a group of formula C—R2, P represents a group of formula C—R3, Q represents a group of formula C—R4, R represents a group of formula C—R5, W represents a group of formula C—R6, or one of the symbols P, Q, R and W represents a nitrogen atom, R1 represents a hydrogen atom or an alkyl group, R2 represents a hydrogen atom or an alkyl group, R3, R4, R5 and R6 each represent a hydrogen or halogen atom, or an alkyl, alkoxy, nitro, amino, trifluoromethyl, cyano or amino group or other functional groups. The compounds of the invention are useful in a variety of therapeutic applications.

    摘要翻译： 本发明公开并要求通式的化合物，其中X表示氮原子或式CR 2的基团，P表示式CR 3的基团，Q表示 式CR 4的基团，R表示式CR 5的基团，W表示式CR 6的基团，或其中之一 符号P，Q，R和W表示氮原子，R 1表示氢原子或烷基，R 2表示氢原子或烷基，R R 3，R 4，R 5和R 6各自表示氢或卤素原子，或烷基， 烷氧基，硝基，氨基，三氟甲基，氰基或氨基或其它官能团。 本发明的化合物可用于各种治疗应用。

    1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof
    9.
    发明申请
    1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof 有权
    1,4-二氮杂双环[3.2.2]壬烷甲酰胺衍生物，其制备和治疗用途

    公开(公告)号：US20050182062A1

    公开(公告)日：2005-08-18

    申请号：US11098670

    申请日：2005-04-04

    申请人： Frederic Galli ,  Patrick Lardenois ,  Odile Leclerc ,  Alistair Lochead

    发明人： Frederic Galli ,  Patrick Lardenois ,  Odile Leclerc ,  Alistair Lochead

    IPC分类号： A61K31/498 ,  A61K31/519 ,  C07D487/04 ,  C07D487/08 ,  C07D519/00

    CPC分类号： C07D487/08

    摘要： The present invention discloses and claims compounds of general formula in which X represents a nitrogen atom or a group of formula C—R2, P represents a group of formula C—R3, Q represents a group of formula C—R4, R represents a group of formula C—R5, W represents a group of formula C—R6, or one of the symbols P, Q, R and W represents a nitrogen atom, R1 represents a hydrogen atom or an alkyl group, R2 represents a hydrogen atom or an alkyl group, R3, R4, R5 and R6 each represent a hydrogen or halogen atom, or an alkyl, alkoxy, nitro, amino, trifluoromethyl, cyano or amino group or other functional groups. The compounds of the invention are useful in a variety of therapeutic applications.

    摘要翻译： 本发明公开并要求通式的化合物，其中X表示氮原子或式CR 2的基团，P表示式CR 3的基团，Q表示 式CR 4的基团，R表示式CR 5的基团，W表示式CR 6的基团，或其中之一 符号P，Q，R和W表示氮原子，R 1表示氢原子或烷基，R 2表示氢原子或烷基，R R 3，R 4，R 5和R 6各自表示氢或卤素原子，或烷基， 烷氧基，硝基，氨基，三氟甲基，氰基或氨基或其它官能团。 本发明的化合物可用于各种治疗应用。