利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

93 条记录 (耗时 0.037 秒)

    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
    23.
    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。

    3-(Pyrrolidin-3-yl)-1,3,4-oxadiazol-2(3H)-one derivatives and their use as 5-HT4 ligands
    25.
    发明授权
    3-(Pyrrolidin-3-yl)-1,3,4-oxadiazol-2(3H)-one derivatives and their use as 5-HT4 ligands 失效
    3-（吡咯烷-3-基）-1,3,4-恶二唑-2（3H） - 酮衍生物及其作为5-HT 4配体的用途

    公开(公告)号：US06248757B1

    公开(公告)日：2001-06-19

    申请号：US09403779

    申请日：1999-11-04

    申请人： Alistair Lochead ,  Samir Jegham ,  Jean Jeunesse

    发明人： Alistair Lochead ,  Samir Jegham ,  Jean Jeunesse

    IPC分类号： A61K31445

    CPC分类号： C07D413/04 ,  C07D413/14

    摘要： Compounds corresponding to the general formula (I) in which R1 represents hydrogen or an alkyl or cycloalkylmethyl group, X1 represents hydrogen or a halogen or an alkoxy group, or alternatively OR1 and X1 together represent a group of formula —OCH2O—, —O(CH2)2—, —O(CH2)3—, —O(CH2)2O— or —O(CH2)3O—, X2 represents hydrogen, an amino group or a group of general formula —NHCO2R in which R represents an alkyl or phenylalkyl group, X3 represents hydrogen or a halogen, and R2 represents hydrogen or an alkyl, phenylalkyl or [(4-dimethylamino)piperid-1-ylcarbonyl]alkyl group. Therapeutic application.

    摘要翻译： 对应于通式（I）的化合物，其中R 1表示氢或烷基或环烷基甲基，X 1表示氢或卤素或烷氧基，或者OR 1和X 1一起表示式-OCH 2 O-，-O（ CH2）2-，-O（CH2）3-，-O（CH2）2O-或-O（CH2）3O-，X2表示氢，氨基或通式-NHCO2R基团，其中R表示烷基 或苯基烷基，X 3表示氢或卤素，R 2表示氢或烷基，苯基烷基或[（4-二甲基氨基）哌啶-1-基羰基]烷基。 治疗应用。

    Substituted heteroaryl pyridopyrimidone derivatives
    26.
    发明授权
    Substituted heteroaryl pyridopyrimidone derivatives 有权
    取代的杂芳基吡啶并嘧啶衍生物

    公开(公告)号：US08198287B2

    公开(公告)日：2012-06-12

    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： A01N43/90 ,  A61K31/519 ,  C07D239/70

    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，其用于预防和/或治疗由GSK3和bgr的异常活性如阿尔茨海默病引起的神经退行性疾病。

    Derivatives of 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, their preparation and their therapeutic application
    30.
    发明授权
    Derivatives of 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, their preparation and their therapeutic application 有权
    5-（吡啶-3-基）-1-氮杂双环[3.2.1]辛烷的衍生物及其制备方法及其治疗应用

    公开(公告)号：US07585974B2

    公开(公告)日：2009-09-08

    申请号：US11696993

    申请日：2007-04-05

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

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

    IPC分类号： C07D237/00 ,  C07D401/00 ,  C07D221/99

    CPC分类号： C07D471/08

    摘要： Compounds complying with the general formula 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. The compounds of this invention are useful as therapeutic agents.

    摘要翻译： 符合通式的化合物，其中R代表卤素原子或被一个或多个选自卤素原子和（C1-C6）烷基，（C1-C6）烷氧基，硝基，氨基，三氟甲基，氰基 ，羟基，乙酰基或亚甲二氧基，或代表任选被一个或多个（C 1 -C 6）烷氧基取代的吡啶基，噻吩基，吲哚基或嘧啶基，其中两个碳 - 碳键代表 “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”4.23mm“file =”US07585974-20090908-P00001.TIF“alt =”custom character“img-content =”character“img- format =“tif”/>，一个是单个，另一个可以是单个或双重。 本发明的化合物可用作治疗剂。