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120 条记录 (耗时 0.019 秒)

    A METHOD OF PREPARING MEMANTINE HYDROCHLORIDE
    31.
    发明公开
    A METHOD OF PREPARING MEMANTINE HYDROCHLORIDE 有权
    VERFAHREN ZUR HERSTELLUNG VON MEMANTINHYDROCHLORID

    公开(公告)号：EP1674446A1

    公开(公告)日：2006-06-28

    申请号：EP03785457.7

    申请日：2003-12-19

    申请人： Shanghai Institute of Pharmaceutical Industry ,  Zhejiang Kangyu Pharmaceutical Co., Ltd.

    发明人： ZHANG, Fuli ,  HU, Meng ,  ZHAO, Lizhi ,  GE, Mengya

    IPC分类号： C07C211/38 ,  C07C209/08 ,  A61P25/28

    CPC分类号： C07C209/08 ,  C07C211/38

    摘要： A new method of preparing memantine hydrochloride, comprises the following steps: reacting 1-bromo-3,5-dimethyl adamantane and urea/formic acid with formic acid also acting as the solvent; hydrolysising with aqueous inorganic acid; alkalifying, extracting and acidifying with hydrochloric acid; finally collecting target compound. The method uses cheaper raw materials and conducts in homogeneous phase under mild conditions. It can reach high yield and good product purity, and be suitable for macrochemistry. The purity of crude product is 99.0%, and reaches 99.98% after first recrystallization, yield: 69.5%, mp: 332 C (DSC).

    摘要翻译： 一种新的盐酸美金刚的方法，包括以下步骤：使1-溴-3,5-二甲基金刚烷与脲/甲酸与还可作为溶剂的甲酸反应; 用无机酸水溶液水解; 用盐酸碱化，提取和酸化; 最后收集目标化合物。 该方法使用较便宜的原料，并在温和条件下均匀进行。 它可以达到高产量和良好的产品纯度，适用于宏观化学。 粗产物纯度为99.0％，第一次重结晶后达到99.98％，产率为69.5％，mp：332℃（DSC）。

    Fluoro-substituted adamantane derivatives
    37.
    发明公开
    Fluoro-substituted adamantane derivatives 失效
    金刚烷衍生物

    公开(公告)号：EP0870757A2

    公开(公告)日：1998-10-14

    申请号：EP98302196.5

    申请日：1998-03-24

    申请人： PFIZER INC.

    发明人： Jasys, Vytautus John ,  Volkmann, Robert Alfred

    IPC分类号： C07C211/38 ,  C07C211/19 ,  C07C61/15 ,  C07C69/753 ,  C07C233/58 ,  A61K31/13 ,  A61K31/16 ,  A61K31/19

    CPC分类号： C07C69/00 ,  C07C61/15 ,  C07C211/38 ,  C07C271/24 ,  C07C2603/00 ,  C07C2603/74

    摘要： The invention relates to fluoro-substituted adamantane derivatives of the formula
    and to pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , and R 4 are as defined herein. The invention also relates to methods of treating neurological disorders, such as memory loss and Parkinson's disease, and bacterial and viral infections, through administration of a therapeutically effective amount of a compound of formula I. The invention also relates to a method of increasing the metabolic stability of an adamantane-containing pharmaceutical compound by incorporating a fluoro substituent on at least one bridge-head carbon of the adamantyl group of said adamantane-containing pharmaceutical compound.

    摘要翻译： 本发明涉及式的氟取代金刚烷衍生物及其药学上可接受的盐，其中R 1，R 2，R 3和R 4如本文所定义。 本发明还涉及通过施用治疗有效量的式I化合物来治疗神经障碍如记忆丧失和帕金森病以及细菌和病毒感染的方法。本发明还涉及增加代谢的方法 通过在所述含金刚烷的药物化合物的金刚烷基的至少一个桥头碳上引入氟取代基来制备含金刚烷的药物化合物的稳定性。