PROCESS FOR THE PREPARATION OF CLOPIDOGREL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
    1.
    发明申请
    PROCESS FOR THE PREPARATION OF CLOPIDOGREL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS 失效
    制备石蜡及其药物接受盐的方法

    公开(公告)号:US20100016594A1

    公开(公告)日:2010-01-21

    申请号:US12439642

    申请日:2007-09-04

    IPC分类号: C07D471/04

    CPC分类号: C07D495/04

    摘要: The present invention provides a process for the preparation of clopidogrel and its pharmaceutically acceptable salts thereof comprises the resolving racemic methyl alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorophenyl)-acetate by the salt formation of methyl alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorophenyl)-acetate with excess levorotatory camphor-10-sulfonic acid to get a maximum yield of camphor sulphonate salt of methyl S-(+)-alpha-5-(4,5,6,7-tetrahydro[3,2-e]thienopyridyl)(2-chlorophenyl)-acetate and transforming the camphor sulphonate salt to clopidogrel or its pharmaceutically acceptable salts thereof.

    摘要翻译: 本发明提供氯吡格雷及其药学上可接受的盐的制备方法,其包括拆分外消旋甲基α-5-(4,5,6,7-四氢[3,2-c]噻吩并吡啶基)(2-氯苯基) (4,5,6,7-四氢[3,2-c]噻吩并吡啶基)(2-氯苯基) - 乙酸甲酯与过量的左旋樟脑-10-磺酸形成盐,得到 甲基S - (+) - α-5-(4,5,6,7-四氢[3,2-e]噻吩并吡啶基)(2-氯苯基) - 乙酸酯的樟脑磺酸盐的最大产率,并转化樟脑磺酸盐 氯吡格雷或其药学上可接受的盐。

    PROCESS FOR THE PREPARATION OF CLOPIDOGREL HYDROGEN SULPHATE FORM I
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF CLOPIDOGREL HYDROGEN SULPHATE FORM I 审中-公开
    制备氯膦酸氢溴酸盐形式的方法I

    公开(公告)号:US20110263858A1

    公开(公告)日:2011-10-27

    申请号:US13125114

    申请日:2009-10-20

    IPC分类号: C07D495/04

    CPC分类号: C07D495/04

    摘要: The present invention relates to a process for the preparation of Form 1 of (+)-(S)-∞-(2-Chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester hydrogen sulphate commonly known as clopidogrel bisulphate. The present invention further relates to a process for reducing the residual amount of methyl isobutyl ketone and controlling the amount of mesityl oxide in clopidogrel hydrogen sulphate Form 1 by washing with ethyl acetate. Formula (I).

    摘要翻译: 本发明涉及制备(+) - (S)-∞-(2-氯苯基)-6,7-二氢噻吩并[3,2-c]吡啶-5(4H) - 乙酸 酸甲酯硫酸氢盐,俗称氯吡格雷硫酸氢盐。 本发明还涉及通过用乙酸乙酯洗涤来减少甲基异丁基酮的残留量并控制氯吡格雷硫酸氢盐形式1中的平均二氧化物的量的方法。 式(I)。

    Process for the preparation of clopidogrel and its pharmaceutically acceptable salts
    3.
    发明授权
    Process for the preparation of clopidogrel and its pharmaceutically acceptable salts 失效
    制备氯吡格雷及其药学上可接受的盐的方法

    公开(公告)号:US08247558B2

    公开(公告)日:2012-08-21

    申请号:US12439642

    申请日:2007-09-04

    IPC分类号: C07D495/04

    CPC分类号: C07D495/04

    摘要: The present invention provides a process for the preparation of clopidogrel and its pharmaceutically acceptable salts thereof comprises the resolving racemic methyl alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorophenyl)-acetate by the salt formation of methyl alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorophenyl)-acetate with excess levorotatory camphor-10-sulfonic acid to get a maximum yield of camphor sulphonate salt of methyl S-(+)-alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl) (2-chlorophenyl)-acetate and transforming the camphor sulphonate salt to clopidogrel or its pharmaceutically acceptable salts thereof.

    摘要翻译: 本发明提供氯吡格雷及其药学上可接受的盐的制备方法,其包括拆分外消旋甲基α-5-(4,5,6,7-四氢[3,2-c]噻吩并吡啶基)(2-氯苯基) (4,5,6,7-四氢[3,2-c]噻吩并吡啶基)(2-氯苯基) - 乙酸甲酯与过量的左旋樟脑-10-磺酸形成盐,得到 甲基S - (+) - α-5-(4,5,6,7-四氢[3,2-c]噻吩并吡啶基)(2-氯苯基) - 乙酸酯的樟脑磺酸盐的最大产率,并转化樟脑磺酸盐 氯吡格雷或其药学上可接受的盐。

    Tamsulosin derivative
    7.
    发明授权
    Tamsulosin derivative 失效
    坦索罗辛衍生物

    公开(公告)号:US07084301B2

    公开(公告)日:2006-08-01

    申请号:US11016264

    申请日:2004-12-17

    IPC分类号: A61K31/18 C07C303/40

    CPC分类号: C07C311/37 C07C303/40

    摘要: The optically active compound, R (−)-5-[2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl]-2-hydroxybenzenesulfonamide in good optical purity, a metabolite of the α1-adrenergic blocking agent tamsulosin, and methods for the preparation thereof. Pharmaceutical compositions including the optically active compound and methods of treatment comprising administration of an effective α1-adrenergic antagonistic amount of such compositions to mammals.

    摘要翻译: 具有良好光学纯度的旋光活性化合物R( - ) - 5- [2 - [[2-(2-乙氧基苯氧基)乙基]氨基]丙基] -2-羟基苯磺酰胺是α< SUB-肾上腺素能阻断剂坦洛新,及其制备方法。 包括光学活性化合物的药物组合物和治疗方法包括向哺乳动物施用有效的α1 - 肾上腺素能拮抗剂量的这种组合物。