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    Processes for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants
    21.
    发明授权
    Processes for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants 失效
    制备大环内酯类免疫抑制剂水溶性聚乙二醇共轭物的方法

    公开(公告)号：US07605257B2

    公开(公告)日：2009-10-20

    申请号：US11713973

    申请日：2007-03-05

    申请人： Jianxin Gu ,  Mark Ruppen ,  Tianmin Zhu ,  Mahdi Fawzi

    发明人： Jianxin Gu ,  Mark Ruppen ,  Tianmin Zhu ,  Mahdi Fawzi

    IPC分类号： C07D498/18

    CPC分类号： C07D498/18 ,  A61K47/60

    摘要： Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol) derivative in the presence of a base. Also described are processes for preparing 32-pegylated tacrolimus and/or ascomycin using these steps.

    摘要翻译： 描述了制备42-聚乙二醇化雷帕霉素的方法，包括在脂肪酶存在下使雷帕霉素与酰化剂反应形成酰化雷帕霉素，并在酰基存在下使酰化雷帕霉素与甲氧基聚（乙二醇）衍生物反应。 还描述了使用这些步骤制备32-聚乙二醇化他克莫司和/或小霉素的方法。

    Vasopressin agonist formulation and process
    22.
    发明授权
    Vasopressin agonist formulation and process 失效
    加压素激动剂配方及方法

    公开(公告)号：US06831079B1

    公开(公告)日：2004-12-14

    申请号：US09669204

    申请日：2000-09-25

    申请人： Joseph K. Yoon ,  Richard W Saunders ,  Mahdi Fawzi

    发明人： Joseph K. Yoon ,  Richard W Saunders ,  Mahdi Fawzi

    IPC分类号： A61K3155

    CPC分类号： A61K9/4858 ,  A61K9/4866 ,  A61K31/55 ,  Y10S514/937

    摘要： This invention provides novel formulations for vasopressin agonist compounds, or a pharmaceutically acceptable salt thereof, having the general structure: and processes for making them, the formulations comprising from about 1% to about 20% of active ingredient, from about 1% to about 18% of a surfactant component, from about 50% to about 80% of a component of one or more polyethylene glycols, from about 1% to about 20% of a component of one or more sucrose fatty acid esters and/or polyvinylpyrrolidone and, optionally, one or more preservatives or antioxidants.

    摘要翻译： 本发明提供了具有一般结构的加压素激动剂化合物或其药学上可接受的盐的新型制剂及其制备方法，所述制剂包含约1％至约20％的活性成分，约1％至约18 ％的表面活性剂组分，约50％至约80％的一种或多种聚乙二醇的组分，约1％至约20％的一种或多种蔗糖脂肪酸酯和/或聚乙烯吡咯烷酮的组分，以及任选地 ，一种或多种防腐剂或抗氧化剂。

    Pharmaceutical carrier formulation
    26.
    发明授权
    Pharmaceutical carrier formulation 有权
    药物载体制剂

    公开(公告)号：US06437006B1

    公开(公告)日：2002-08-20

    申请号：US09668970

    申请日：2000-09-25

    申请人： Joseph K. Yoon ,  Richard W. Saunders ,  Mahdi Fawzi

    发明人： Joseph K. Yoon ,  Richard W. Saunders ,  Mahdi Fawzi

    IPC分类号： A61K4732

    CPC分类号： A61K9/4858 ,  A61K9/4866 ,  A61K47/44 ,  Y10S514/966

    摘要： This invention provides carrier systems useful in preparing pharmaceutical formulations, the systems comprising, by weight percentage, from about 1% to about 20%, preferably from about 5% to about 12%, of a surfactant component; from about 55% to about 93%, preferably from about 60% to about 85%, of a component of one or more polyethylene glycols (PEG); and from about 1% to about 25%, preferably from about 5% to about 15%, of one or more sucrose fatty acid esters or polyvinylpyrrolidone (PVP) with a K value between about 15 and about 90, preferably with a K value of from about 16 to about 18, most preferably about 17, as defined in USP/NF, or a combination of one or more sucrose fatty acid esters or PVP, and, optionally, one or more pharmaceutically acceptable preservatives or antioxidants, such as BHA, BHT, ascorbyl palmitate or benzyl alcohol.

    摘要翻译： 本发明提供了可用于制备药物制剂的载体系统，该系统按重量百分比计包含约1％至约20％，优选约5％至约12％的表面活性剂组分; 约55％至约93％，优选约60％至约85％的一种或多种聚乙二醇（PEG）的组分; 和约1％至约25％，优选约5％至约15％的一种或多种K值在约15至约90之间的蔗糖脂肪酸酯或聚乙烯吡咯烷酮（PVP），优选具有K值 约16至约18，最优选约17，如USP / NF中定义的，或一种或多种蔗糖脂肪酸酯或PVP的组合，以及任选的一种或多种药学上可接受的防腐剂或抗氧化剂，例如BHA， BHT，抗坏血酸棕榈酸酯或苯甲醇。

    Processes for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants
    27.
    发明申请
    Processes for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants 失效
    制备大环内酯类免疫抑制剂水溶性聚乙二醇共轭物的方法

    公开(公告)号：US20070212371A1

    公开(公告)日：2007-09-13

    申请号：US11713973

    申请日：2007-03-05

    申请人： Jianxin Gu ,  Mark Ruppen ,  Tianmin Zhu ,  Mahdi Fawzi

    发明人： Jianxin Gu ,  Mark Ruppen ,  Tianmin Zhu ,  Mahdi Fawzi

    IPC分类号： A61K31/395 ,  C07D273/01

    CPC分类号： C07D498/18 ,  A61K47/60

    摘要： Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol) derivative in the presence of a base. Also described are processes for preparing 32-pegylated tacrolimus and/or ascomycin using these steps.

    摘要翻译： 描述了制备42-聚乙二醇化雷帕霉素的方法，包括在脂肪酶存在下使雷帕霉素与酰化剂反应以形成酰化雷帕霉素，并在碱的存在下使酰化雷帕霉素与甲氧基聚（乙二醇）衍生物反应。 还描述了使用这些步骤制备32-聚乙二醇化他克莫司和/或子囊霉素的方法。