利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

93 条记录 (耗时 0.042 秒)

    Benzothiazepin-4-one derivatives, their preparation and their application in therapy
    71.
    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。

    Use of 8-substituted-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
    77.
    发明授权
    Use of 8-substituted-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives 失效
    8-取代-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物的用途

    公开(公告)号：US08093256B2

    公开(公告)日：2012-01-10

    申请号：US11764374

    申请日：2007-06-18

    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 use of 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. More specifically, the invention relates 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 disease caused by abnormal activity of GSK3β, such as Pick's disease among various other diseases as claimed herein.

    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的用途：其中X，Y，R 1，R 2，R 3，R 4，R 5，n，p和q如本文所定义。 更具体地，本发明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GSK3＆bgr异常活性引起的疾病，例如各种其他疾病中的皮克病 如本文所要求的。