公开(公告)号：US06331547B1

公开(公告)日：2001-12-18

申请号：US09639610

申请日：2000-08-16

申请人： Tianmin Zhu ,  Syed M. Shah ,  Richard W. Saunders

发明人： Tianmin Zhu ,  Syed M. Shah ,  Richard W. Saunders

IPC分类号： C07D49816

CPC分类号： C07D498/18

摘要： This invention provides novel water soluble pegylated esters of rapamycin, having the general structure: wherein n is an integer from about 5 to about 450, as well as pharmaceutical compositions containing these compounds and methods for their use as immunosuppressive, anti-inflammatory, antifungal, antiproliferative and antitumor agents.

摘要翻译： 本发明提供新型的雷帕霉素的水溶性聚乙二醇化酯，其具有以下通用结构：其中n为约5至约450的整数，以及含有这些化合物的药物组合物及其用作免疫抑制，抗炎，抗真菌， 抗增殖剂和抗肿瘤剂。

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。

公开(公告)号：US06352718B1

公开(公告)日：2002-03-05

申请号：US09668883

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： A61K964

CPC分类号： A61K9/4866

摘要： This invention provides novel formulations for N-[4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)ylcarbonyl)-3-chlorophenyl]-5-fluoro-2-methyl-benzamide, or a pharmaceutically acceptable salt thereof, 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 pharmaceutically acceptable preservatives or antioxidants

摘要翻译： 本发明提供N- [4-（5H-吡咯并[2,1-c] [1,4]苯并二氮杂-10（11H）基羰基）-3-氯苯基] -5-氟-2-甲基 - 苯甲酰胺 ，或其药学上可接受的盐及其制备方法，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％ 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，和任选的一种或多种药学上可接受的防腐剂或抗氧化剂