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    6-pyrrolidin-2-ylpyrindine derivatives, their preparation and application in therapy
    11.
    发明授权
    6-pyrrolidin-2-ylpyrindine derivatives, their preparation and application in therapy 失效
    6-吡咯烷-2-基嘧啶衍生物，其制备和应用于治疗

    公开(公告)号：US06184229B2

    公开(公告)日：2001-02-06

    申请号：US09462352

    申请日：2000-01-07

    申请人： Alistair Lochead ,  Samir Jegham ,  Frédéric Galli

    发明人： Alistair Lochead ,  Samir Jegham ,  Frédéric Galli

    IPC分类号： A61K31435

    CPC分类号： C07D401/04 ,  A61K31/435

    摘要： Compound corresponding to the general formula (I) in which R1 represents a hydrogen atom, a (C1-C4)alkyl group or a phenyl(C1-C4)alkyl group, R2 represents a hydrogen atom or a (C1-C4) alkyl group, and R3, R4 and R5 each represent a hydrogen or halogen atom or a trifluoromethyl, cyano, hydroxyl, (C1-C6)alkyl or (C1-C6) alkoxy group.

    摘要翻译： 对应于通式（I）的化合物，其中R 1表示氢原子，（C 1 -C 4）烷基或苯基（C 1 -C 4）烷基，R 2表示氢原子或（C 1 -C 4）烷基 ，R 3，R 4和R 5各自表示氢或卤素原子或三氟甲基，氰基，羟基，（C 1 -C 6）烷基或（C 1 -C 6）烷氧基。

    5-phenyl-3-(piperidin-4-yl)-1,3,4-oxadiazol-2(3H)-one derivatives for use as 5-Ht4 or H3 receptor ligands
    12.
    发明授权
    5-phenyl-3-(piperidin-4-yl)-1,3,4-oxadiazol-2(3H)-one derivatives for use as 5-Ht4 or H3 receptor ligands 失效
    5-苯基-3-（哌啶-4-基）-1,3,4-恶二唑-2（3H） - 酮衍生物，用作5-Ht4或H3受体配体

    公开(公告)号：US5929089A

    公开(公告)日：1999-07-27

    申请号：US68390

    申请日：1998-05-08

    申请人： Samir Jegham ,  Alistair Lochead ,  Frederic Galli ,  Alain Nedelec ,  Axelle Solignac ,  Laurence De Cruz

    发明人： Samir Jegham ,  Alistair Lochead ,  Frederic Galli ,  Alain Nedelec ,  Axelle Solignac ,  Laurence De Cruz

    IPC分类号： A61K31/00 ,  A61K31/4245 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4523 ,  A61K31/454 ,  A61P43/00 ,  C07D413/04 ,  C07D413/14

    CPC分类号： C07D413/04 ,  C07D413/14

    摘要： Compounds corresponding to the general formula (I) ##STR1## in which R.sub.1 represents a (C.sub.1 -C.sub.4)alkyl or (C.sub.3 -C.sub.7)cycloalkylmethyl group, X.sub.1 represents a hydrogen or halogen atom or a (C.sub.1 -C.sub.4)alkoxy group or else OR.sub.1 and X.sub.1 together represent a group of formula -OCH.sub.2 O-, -O(CH.sub.2).sub.2 -, -O(CH.sub.2).sub.3 -, -O(CH.sub.2).sub.2 O- or -O(CH.sub.2).sub.3 O-, X.sub.2 represents a hydrogen atom or an amino group, X.sub.3 represents a hydrogen or halogen atom, and R.sub.2 represents either a hydrogen atom or an optionally substituted (C.sub.1 -C.sub.6) alkyl group or a phenyl (C.sub.1 -C.sub.4) alkyl group which is optionally substituted on the phenyl ring or a phenyl (C.sub.2 -C.sub.3) alkenyl group or a phenoxy (C.sub.2 -C.sub.4) alkyl group or a cyclo (C.sub.3 -C.sub.7) alkylmethyl group or a 2,3-dihydro-1H-inden-1-yl or 2,3-dihydro-1H-inden-2-yl group or a group of general formula -(CH.sub.2).sub.n CO-Z in which n represents a number from 1 to 6 and Z represents a piperidin-1-yl or 4-(dimethylamino)piperidin-1-yl group. Application in therapeutics.

    摘要翻译： PCT No.PCT / FR96 / 01730 Sec。 371日期1998年5月8日 102（e）日期1998年5月8日PCT 1996年11月5日PCT PCT。 公开号WO97 / 17345 日期：1997年5月15日对应于通式（I）的化合物，其中R1表示（C1-C4）烷基或（C3-C7）环烷基甲基，X1表示氢或卤素原子或（C1-C4）烷氧基或 其中OR 1和X 1一起表示式-OCH 2 O-，-O（CH 2）2 - ， - O（CH 2）3 - ， - O（CH 2）2 O-或-O（CH 2）3 O- - 的基团， 原子或氨基，X3表示氢或卤素原子，R2表示氢原子或任选取代的（C1-C6）烷基或在苯环上任意取代的苯基（C1-C4）烷基 或苯基（C 2 -C 3）烯基或苯氧基（C 2 -C 4）烷基或环（C 3 -C 7）烷基甲基或2,3-二氢-1H-茚-1-基或2,3-二氢-1H-茚-1-基， 二氢-1H-茚-2-基或通式 - （CH 2）n CO-Z的基团，其中n表示1至6的数，Z表示哌啶-1-基或4-（二甲基氨基）哌啶-1-基， 吡啶-1-基。 在治疗中的应用。

    2-Pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-A]pyrimidin-4-one and 7-pyridinyl-2,3-dihydoimidazo[1,2-A]pyrimidin-5(1H)one derivatives
    16.
    发明申请
    2-Pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-A]pyrimidin-4-one and 7-pyridinyl-2,3-dihydoimidazo[1,2-A]pyrimidin-5(1H)one derivatives 审中-公开

    公开(公告)号：US20060014762A1

    公开(公告)日：2006-01-19

    申请号：US11227007

    申请日：2005-09-15

    申请人： Antonio Almario Garcia ,  Thierry Gallet ,  Adrien Ll ,  Alistair Lochead ,  Severine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Philippe Yaiche

    发明人： Antonio Almario Garcia ,  Thierry Gallet ,  Adrien Ll ,  Alistair Lochead ,  Severine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Philippe Yaiche

    IPC分类号： A61K31/519 ,  C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/519

    摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents 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, a 1,2-cyclopropylene, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxyde group, a carbonyl group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridyl group optionally substituted by a C3-6 cycloalkyl group a C1-4 alkyl group, a C1-4 alkoxy group, a benzyl group or a halogen atom; when Y represents a bond, a methylene group optionally substituted or a carbonyl group then R2 represents a C1-6 alkyl 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 5,6,7,8-tetrahydronaphthyl ring, a naphthyl ring, a phenylthio group, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; when Y represents an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxyde group or a nitrogen atom being optionally substituted then R2 represents a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a naphthyl ring, a 5,6,7,8-tetrahydronaphthyl ring, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring. And 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 diseases caused by abnormal activity of GSK3β such as Alzheimer's disease.

    Derivatives of 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, the preparation thereof and the application of same in therapeutics
    19.
    发明授权
    Derivatives of 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, the preparation thereof and the application of same in therapeutics 有权
    5-（吡啶-3-基）-1-氮杂双环[3.2.1]辛烷的衍生物及其在治疗中的应用

    公开(公告)号：US07223750B2

    公开(公告)日：2007-05-29

    申请号：US10500015

    申请日：2003-01-03

    申请人： Frédéric Galli ,  Odile LeClerc ,  Alistair Lochead ,  Alain Nedelec

    发明人： Frédéric Galli ,  Odile LeClerc ,  Alistair Lochead ,  Alain Nedelec

    IPC分类号： A61K31/55

    CPC分类号： C07D471/08

    摘要： Compounds complying with the general formula (I) in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1–C6)alkyl, (C1–C6)alkoxy, nitro, amino, trifluoromethyl, cyano, hydroxy, acetyl or methylenedioxy groups, or represents a pyridinyl group, a thienyl group, an indolyl group, or a pyrimidinyl group optionally substituted by one or more (C1–C6)alkoxy groups, where, of the two carbon-carbon bonds represented by , one is single and the other may be single or double. Therapeutic application.

    摘要翻译： 符合通式（I）的化合物，其中R表示卤素原子或被一个或多个选自卤素原子和（C 1 -C 6）烷基的基团取代的苯基， 烷基，（C 1 -C 6 -C 6）烷氧基，硝基，氨基，三氟甲基，氰基，羟基，乙酰基或亚甲二氧基，或表示吡啶基， 噻吩基，吲哚基或任选被一个或多个（C 1 -C 6 -C 6）烷氧基取代的嘧啶基，其中两个碳 - 碳键 代表为，一个是单个，另一个可以是单个或双重。 治疗应用。

    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
    20.
    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 。