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11 条记录 (耗时 0.021 秒)

    N-methylnaltrexone zwitterion
    5.
    发明授权
    N-methylnaltrexone zwitterion 有权
    N-甲基纳曲酮两性离子

    公开(公告)号：US08288547B2

    公开(公告)日：2012-10-16

    申请号：US12625649

    申请日：2009-11-25

    申请人： Alain Dlubala

    发明人： Alain Dlubala

    IPC分类号： C07D489/02

    CPC分类号： C07D489/08

    摘要： The invention discloses and claims N-Methylnaltrexone zwitterion, of formula (I), substantially in the anhydrous form or a hydrate thereof:

    摘要翻译： 本发明公开并要求式（I）的N-甲基纳曲酮两性离子基本上为无水形式或其水合物：

    Processs for preparing N-alkylnaltrexone halides
    6.
    发明授权
    Processs for preparing N-alkylnaltrexone halides 有权
    N-烷基纳曲酮卤化物的制备方法

    公开(公告)号：US07645880B2

    公开(公告)日：2010-01-12

    申请号：US12049607

    申请日：2008-03-17

    申请人： Alain Dlubala

    发明人： Alain Dlubala

    IPC分类号： C07D489/08

    CPC分类号： C07D489/08

    摘要： The invention relates to a novel process for preparing N-methylnaltrexone bromide, comprising at least the steps consisting in: (i) reacting N-methylnaltrexone methyl sulfate in aqueous solution with an alkaline agent chosen from the group constituted by sodium carbonate, potassium carbonate, calcium carbonate, magnesium carbonate, cesium carbonate, strontium carbonate and mixtures thereof, for a pH of the aqueous reaction medium of between 7 and 10, and then in (ii) reacting the product thus obtained with hydrobromic acid, which is added for a pH of the aqueous reaction medium of between 0.5 and 5, in order thus to obtain the N-methylnaltrexone bromide.

    摘要翻译： 本发明涉及一种制备N-甲基纳曲酮溴化物的新方法，其至少包括以下步骤：（i）使N-甲基纳曲酮甲基硫酸盐在水溶液中与碱性试剂反应，所述碱性试剂选自碳酸钠，碳酸钾， 碳酸钙，碳酸镁，碳酸铯，碳酸锶及其混合物，使反应介质的pH值在7至10之间，然后在（ii）将所得产物与氢溴酸反应，将其加入pH 的水性反应介质为0.5至5，以便得到N-甲基纳曲酮溴化物。

    PROCESS FOR PREPARING N-ALKYLNALTREXONE HALIDES
    8.
    发明申请
    PROCESS FOR PREPARING N-ALKYLNALTREXONE HALIDES 有权
    制备N-烷基胆碱酯的方法

    公开(公告)号：US20080214817A1

    公开(公告)日：2008-09-04

    申请号：US12049607

    申请日：2008-03-17

    申请人： Alain Dlubala

    发明人： Alain Dlubala

    IPC分类号： C07D491/08

    CPC分类号： C07D489/08

    摘要： The invention relates to a novel process for preparing N-methylnaltrexone bromide, comprising at least the steps consisting in: (i) reacting N-methylnaltrexone methyl sulfate in aqueous solution with an alkaline agent chosen from the group constituted by sodium carbonate, potassium carbonate, calcium carbonate, magnesium carbonate, cesium carbonate, strontium carbonate and mixtures thereof, for a pH of the aqueous reaction medium of between 7 and 10, and then in (ii) reacting the product thus obtained with hydrobromic acid, which is added for a pH of the aqueous reaction medium of between 0.5 and 5, in order thus to obtain the N-methylnaltrexone bromide.

    摘要翻译： 本发明涉及一种制备N-甲基纳曲酮溴化物的新方法，其至少包括以下步骤：（i）使N-甲基纳曲酮甲基硫酸盐在水溶液中与碱性试剂反应，所述碱性试剂选自碳酸钠，碳酸钾， 碳酸钙，碳酸镁，碳酸铯，碳酸锶及其混合物，使反应介质的pH值在7至10之间，然后在（ii）将所得产物与氢溴酸反应，将其加入pH 的水性反应介质为0.5至5，以便得到N-甲基纳曲酮溴化物。

    Method for the preparation of morphine compounds
    9.
    发明授权
    Method for the preparation of morphine compounds 有权
    吗啡化合物的制备方法

    公开(公告)号：US08455509B2

    公开(公告)日：2013-06-04

    申请号：US12774156

    申请日：2010-05-05

    申请人： Alain Dlubala

    发明人： Alain Dlubala

    IPC分类号： A61K31/485 ,  C07D489/08

    CPC分类号： C07D489/08 ,  C07B63/02 ,  C07D489/00

    摘要： The present invention relates to a method for the preparation of morphine compounds comprising a low content of α,β-unsaturated compounds, which comprises the steps of: (i) bringing the crude morphine compound into contact with a base, at a pH of greater than 13, under conditions which make possible the Michael addition reaction on the α,β-unsaturated compound(s) present; (ii) separating the morphine compound from the reaction mixture; and (iii) if appropriate, separating the addition product formed from the morphine compound. It also relates to a composition comprising at least 99% by dry weight of morphine compound or of a pharmaceutically acceptable salt thereof, and an α,β-unsaturated compound in a content of less than 100 ppm.

    摘要翻译： 本发明涉及一种制备包含低含量α，β-不饱和化合物的吗啡化合物的方法，其包括以下步骤：（i）将粗制吗啡化合物与碱接触，pH较大 在使得可能存在α，β-不饱和化合物上的迈克尔加成反应的条件下， （ii）从反应混合物中分离吗啡化合物; 和（iii）如果合适，分离由吗啡化合物形成的加成产物。 它还涉及包含至少99重量％的吗啡化合物或其药学上可接受的盐以及含量低于100ppm的α，β-不饱和化合物的组合物。

    Synthesis of morphine-6-glucuronide or one of the derivatives thereof
    10.
    发明授权
    Synthesis of morphine-6-glucuronide or one of the derivatives thereof 有权
    吗啡-6-葡糖醛酸苷的合成或其衍生物之一

    公开(公告)号：US08258298B2

    公开(公告)日：2012-09-04

    申请号：US13155646

    申请日：2011-06-08

    申请人： Alain Dlubala ,  Claire Trecant ,  Isabelle Ripoche

    发明人： Alain Dlubala ,  Claire Trecant ,  Isabelle Ripoche

    IPC分类号： C07D489/02

    CPC分类号： C07D489/02

    摘要： The disclosure relates to a method for preparing morphine-6-glucuronide or one of the deritives thereof comprising reacting a compound of formula (I): wherein R1 is as defined in the disclosure, with a glucuronic acid derivative of formula (II): wherein PG, X, and R4 are as defined in the disclosure, in the presence of an aromatic solvent and trimethylsilyl trifluoromethanesulfonate; (ii) reacting the product obtained in step (i) with a strong basic agent; and then (iii) recovering the product obtained in step (ii).

    摘要翻译： 本公开涉及制备吗啡-6-葡糖醛酸苷或其衍生物之一，其包括使式（I）化合物：其中R 1如本公开内容所定义的与式（II）的葡糖醛酸衍生物反应：其中 PG，X和R4如本发明中所定义，在芳族溶剂和三氟甲磺酸三甲基甲硅烷基酯的存在下; （ii）使步骤（i）中获得的产物与强碱性试剂反应; 然后（iii）回收步骤（ii）中获得的产物。