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207 条记录 (耗时 0.025 秒)

    ISOQUINOLINE -1,3,4-TRIONE, THE SYNTHETIC METHOD AND THE USE THEREOF
    144.
    发明授权
    ISOQUINOLINE -1,3,4-TRIONE, THE SYNTHETIC METHOD AND THE USE THEREOF 有权
    异喹啉基-1,3,4- TRION，合成工艺及其用途

    公开(公告)号：EP1640367B1

    公开(公告)日：2011-02-09

    申请号：EP04738186.8

    申请日：2004-05-31

    申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

    发明人： NAN, Fajun ,  LI, Jia ,  CHEN, Yihua ,  ZHANG, Yahui ,  GU, Min ,  ZHANG, Huajie

    IPC分类号： C07D217/04 ,  A61P25/00 ,  A61P25/28

    CPC分类号： C07D417/04 ,  C07D217/24

    摘要： The invention relates to all types of substituted isoquinoline -1,3,4-trione, the synthetic method thereof and the use for treatding neurodegenerative diseases , especially as the medicine for Alzhermer's disease, appplexy and brain ischernic injuries, the compound is represented by the structure, Formula (I); Dihydroisoquinoline-1,3,4-trione) wherein substituents R, can be one , two or three groups optionally selected from the group consisting of H; alkyl; hydroxyl; alkyl substituted by the groups including halogen , alkoxyl, hydroxyl; alkyl or alkylamine substituted by the groups including halogen , alkoxyl, hydroxyl; C,-,alkenyl substituted by oxygen or amine; C, 6cycloalkyl; substituted aryl; benzyl; alkanoyl; alkanoyl substituted by the groups including halogen , alkoxyl, hydroxyl; C2-6enc,yl ; C,-,cycloalkanoyl; tert­butoxycarbonyl; benzoyl; benzoyl. substituted by one, two or three groups including alkylarnine; benzylacryl; benzylacryl. substituted by one, two or three groups including alkylamine; thienylfonnyl; admantyliForrnyl; mandeloyl; alkoxyl; alkylamine; cycloalkoxyl; cycloalkoxycarbonyl; alkanoylxy; alkanoylamine; cycloalkyanoylxy; cycloalkanoylarnine; ureido; urenylene; alkanoyl; nitro; carboxyl; R2 is H; alkyl; alkyl. or Cl-C4cycloalkyl which are substituted by the groups including halogen, alkoxyl, hydroxyl; C2-C,alkenyl; acryl; substituted acryl; X is H, CH2, N-H, 0, S; is CH, N.

    A METHOD FOR PREPARING 4-Ý9-(6-AMINOPURINE)¨-2-(S)-HYDROXYL-BUTYRIC ACID METHYL ESTER
    146.
    发明公开
    A METHOD FOR PREPARING 4-Ý9-(6-AMINOPURINE)¨-2-(S)-HYDROXYL-BUTYRIC ACID METHYL ESTER 审中-公开
    VERFAHREN ZUR HERSTELLUNG VON 4- [9-（6-氨基嘌呤）] - 2-（S） - 羟基丁酸乙酯

    公开(公告)号：EP2230239A1

    公开(公告)日：2010-09-22

    申请号：EP08864601.3

    申请日：2008-11-06

    申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

    发明人： NAN, Fajun ,  ZUO, Jianping ,  ZHANG, Yangming ,  GU, Min ,  TANG, Wei

    IPC分类号： C07D473/34 ,  C07D317/34

    CPC分类号： C07D473/34 ,  Y02P20/55

    摘要： The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2( S )-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2( S )-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product. Comparing with the prior preparation methods, the present method has advantages in low cost, mild conditions, high retention of the chiral center during the reaction, high productivity, great improvement in the quality and yield of the product and great decrease in cost, and thus is suitable for the production on a large scale.

    摘要翻译： 本发明公开了一种制备和纯化4-（6-氨基 - 嘌呤-9-基）-2（S） - 羟基 - 丁酸甲酯的新方法。 该制剂从便宜且容易获得的L-苹果酸开始，其在同时保护1-羧基和2-羟基的基团后转化为中间体I. 将中间体I选择性还原成中间体醇II，其中羟基进一步转化为容易离去的基团，得到中间体III。 中间体III被腺嘌呤亲核取代以得到中间体IV中间体IV在酸或碱的存在下在甲醇中同时脱甲基酯化，得到粗品4-（6-氨基 - 嘌呤-9-基） - 2（S） - 羟基 - 丁酸甲酯，通过重结晶纯化，得到纯化产物。 与现有的制备方法相比，本发明方法成本低，条件温和，反应中手性中心保留性高，生产效率高，产品质量和产量大幅提高，成本大幅降低， 适合大规模生产。

    13,13a-DIHYDROBERBERINE DERIVATIVES, THEIR PHARMACEUTICAL COMPOSITION AND USE
    148.
    发明公开
    13,13a-DIHYDROBERBERINE DERIVATIVES, THEIR PHARMACEUTICAL COMPOSITION AND USE 有权
    13,13A-DIHYDROBERBERINDERIVATE，IHRE PHARMAZEUTISCHEN ZUSAMMENSETZUNGEN UND VERWENDUNG

    公开(公告)号：EP2070926A1

    公开(公告)日：2009-06-17

    申请号：EP07816496.9

    申请日：2007-09-30

    申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

    发明人： HU, Lihong ,  YE, Jiming ,  LI, Jingya ,  JAMES, David, E ,  KRAEGEN, Edward, W ,  ZHANG, Hankun ,  CHENG, Zhe ,  LI, Jia

    IPC分类号： C07D455/03 ,  A61K31/4375 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10

    CPC分类号： C07D455/03

    摘要： The present invention provides 13,13a-dihydroberberine derivatives or their physiologically acceptable salts represented by the following formula, pharmaceutical compositions comprising the same, and uses thereof. The 13,13a-dihydroberberine derivatives have an activity of promoting glucose absorption in muscle cells, and the whole animal tests show that the present compounds have effects on improving glucose-tolerance and insulin-resistance, facilitating weight loss, relieving fatty liver and the like. Thus, the present compounds can be used in treating diabetes mellitus, adiposity, fatty liver and complications thereof induced by insulin resistance.

    摘要翻译： 本发明提供由下式表示的13,13a-二氢小檗碱衍生物或其生理学上可接受的盐，其包含其的药物组合物及其用途。 13,13a-二氢小檗碱衍生物具有促进肌肉细胞中葡萄糖吸收的活性，整个动物试验表明，本发明化合物具有改善葡萄糖耐量和胰岛素抵抗，促进体重减轻，缓解脂肪肝等作用 。 因此，本发明化合物可用于治疗由胰岛素抵抗引起的糖尿病，肥胖，脂肪肝及其并发症。