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93 条记录 (耗时 0.041 秒)

    7-(Pyrimidin-4-yl)-Imidazo[1,2-a]Pyrimidin-5(1H)-ones as GSK3β inhibitors
    61.
    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。

    Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
    62.
    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。

    1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof
    64.
    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。

    Benzothiazepin-4-one derivatives, their preparation and their application in therapy
    65.
    发明授权
    Benzothiazepin-4-one derivatives, their preparation and their application in therapy 失效
    苯并硫氮杂-4-酮衍生物，其制备及其在治疗中的应用

    公开(公告)号：US4914092A

    公开(公告)日：1990-04-03

    申请号：US339978

    申请日：1989-04-18

    申请人： Alistair Lochead ,  Jean C. Muller ,  Colombe Denys ,  Andre Dumas

    发明人： Alistair Lochead ,  Jean C. Muller ,  Colombe Denys ,  Andre Dumas

    IPC分类号： A61K31/55 ,  A61K31/554 ,  A61P3/00 ,  A61P3/14 ,  A61P9/08 ,  A61P25/02 ,  C07D281/10 ,  C07D417/12

    CPC分类号： C07D417/12 ,  C07D281/10

    摘要： A compound, in the form of a pure diastereoisomer or mixture thereof, which is a benzothiazepin-4-one derivative of formula (I): ##STR1## in which: R1 is hydrogen or a C.sub.2 -C.sub.4 alkanoyl group;R2 and R3 independently each is hydrogen, a linear or branched C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.5 cycloalkyl group, a phenyl group, a benzyl group or a phenethyl group, or R2 and R3 together form, with the nitrogen atom to which they are attached, a pyrrolidinyl, 2,2-dimethylpyrrolidinyl, piperidyl, 4-phenylpiperidyl, 4-(3-methoxyphenyl)piperidyl, 4-(4-fluorobenzoyl)piperidyl, 1,2,3,6-tetrahydropyridyl, perhydroazepinyl, perhydroazocinyl, 1,3-thiazolidinyl, thiomorpholinyl, morpholinyl, 2,3-dihydroindolyl, 1,2,3,4-tetrahydroisoquinolyl, 6-methoxy-1,2,3,4-tetrahydroisoquinolyl, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolyl or 2,3,4,5-tetrahydro-1H-benz[b]azepinyl group; andX is hydrogen or chlorine;or a pharmacologically acceptable acid addition salt thereof.

    摘要翻译： 化合物，其为纯的非对映异构体或其混合物，其为式（I）的苯并硫氮杂-4-酮衍生物：其中：R 1为氢或C 2 -C 4烷酰基; R 2和R 3各自独立地为氢，直链或支链C 1 -C 4烷基，C 3 -C 5环烷基，苯基，苄基或苯乙基，或R 2和R 3一起与其中的氮原子一起形成 吡咯烷基，2,2-二甲基吡咯烷基，哌啶基，4-苯基哌啶基，4-（3-甲氧基苯基）哌啶基，4-（4-氟苯甲酰基）哌啶基，1,2,3,6-四氢吡啶基，全氢化吖嗪基， ，1,3-噻唑烷二基，硫代吗啉基，吗啉基，2,3-二氢吲哚基，1,2,3,4-四氢异喹啉，6-甲氧基-1,2,3,4-四氢异喹啉，6,7-二甲氧基-1,2 3,4-四氢异喹啉基或2,3,4,5-四氢-1H-苯并[b]吖庚因基; X为氢或氯; 或其药理学上可接受的酸加成盐。