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1. 发明申请

WO2008048298A2 POLYMER PARTICLES FOR DELIVERY OF MACROMOLECULES AND METHODS OF USE 审中-公开
标题翻译：用于输送大分子的聚合物颗粒和使用方法
公开(公告)号：WO2008048298A2
公开(公告)日：2008-04-24
申请号：PCT/US2006045268
申请日：2006-11-21
申请人： MEDIVAS LLC , GOMURASHVILI ZAZA D , LANDIS GEOFFREY C , LI HONG , TURNELL WILLIAM D , DEFIFE KRISTIN , VASSILEV VASSIL P , YUAN YUMIN NMN
发明人： GOMURASHVILI ZAZA D , LANDIS GEOFFREY C , LI HONG , TURNELL WILLIAM D , DEFIFE KRISTIN , VASSILEV VASSIL P , YUAN YUMIN NMN
IPC分类号： A61K48/00 , A61K9/14 , A61K38/28 , C08F20/00
CPC分类号： A61K9/167 , A61K9/1075 , A61K9/5146 , A61K38/28 , A61K47/59 , A61K47/593 , A61K47/595 , C08L77/12
摘要： The present invention provides biodegradable polymer particle delivery compositions for delivery of macromolecular biologies, for example in crystal form, based on polymers, such as polyester amide (PEA), polyester urethane (PEUR), and polyester urea (PEU) polymers, which contain amino acids in the polymer. The polymer particle delivery compositions can be formulated either as a liquid dispersion or a lyophilized powder of polymer particles containing bound water molecules with the macromolecular biologies, for example insulin, dispersed in the particles. Bioactive agents, such as drugs, polypeptides, and polynucleotides can also be delivered by using particles sized for local, oral, mucosal or circulatory delivery. Methods of delivering a macromolecular biologic with substantial native activity to a subject, for example orally, are also included.
摘要翻译：本发明提供了生物可降解聚合物颗粒递送组合物，其用于递送基于聚合物例如聚酯酰胺（PEA），聚酯氨基甲酸酯（PEUR）和聚酯脲（PEU）聚合物的大分子生物学，例如晶体形式，其含有氨基酸在聚合物中。聚合物颗粒递送组合物可以配制成液体分散体或含有结合水分子的聚合物颗粒与分散在颗粒中的大分子生物制剂（例如胰岛素）的冻干粉末。生物活性剂如药物，多肽和多核苷酸也可以通过使用大小适合局部，口服，粘膜或循环递送的颗粒来递送。也包括向受试者递送具有大量天然活性的大分子生物制剂的方法，例如口服。

2. 发明申请

WO2006083874A2 VACCINE DELIVERY COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：疫苗输送组合物及其使用方法
公开(公告)号：WO2006083874A2
公开(公告)日：2006-08-10
申请号：PCT/US2006003412
申请日：2006-01-31
申请人： MEDIVAS LLC , TUNELL WILLIAM G , VASSILEV VASSIL P , DEFIFE KRISTIN M , LI HONG , GOMURASHVILI ZAZA D , KATSARAVA RAMAZ
发明人： TUNELL WILLIAM G , VASSILEV VASSIL P , DEFIFE KRISTIN M , LI HONG , GOMURASHVILI ZAZA D , KATSARAVA RAMAZ
IPC分类号： A61K39/00
CPC分类号： A61K39/39 , A61K9/0019 , A61K47/593 , A61K47/595 , A61K2039/55511 , A61K2039/57
摘要： The present invention provides synthetic vaccine delivery compositions based on polyester amide (PEA), polyester urethane (PEUR), and polyester urea (PEU) polymers for stimulating an immune response to a variety of pathogenic organisms and tumor cells in humans and other mammals. The vaccine delivery compositions are formulated as a liquid dispersion of polymer particles or molecules including class I or class II antigen peptides derived from organism or tumor cell proteins, which are taken up by antigen presenting cells of the mammal to induce an immune response in the mammal. Methods of inducing an immune response to the pathogenic organism or tumor cells in the invention compositions are also included.
摘要翻译：本发明提供了基于聚酯酰胺（PEA），聚酯聚氨酯（PEUR）和聚酯尿素（PEU）聚合物的合成疫苗递送组合物，用于刺激人和其它哺乳动物中各种致病生物体和肿瘤细胞的免疫应答。疫苗递送组合物被配制为聚合物颗粒或分子的液体分散体，包括衍生自生物或肿瘤细胞蛋白的I类或II类抗原肽，其被哺乳动物的抗原呈递细胞吸收以在哺乳动物中诱导免疫应答。还包括诱导本发明组合物中致病生物或肿瘤细胞的免疫应答的方法。

3. 发明申请

WO2007133616A2 BIODEGRADABLE WATER SOLUBLE POLYMERS 审中-公开
标题翻译：可生物降解的水溶性聚合物
公开(公告)号：WO2007133616A2
公开(公告)日：2007-11-22
申请号：PCT/US2007011272
申请日：2007-05-09
申请人： MEDIVAS LLC , GOMURASHVILI ZAZA D , TURNELL WILLIAM D , VASSILEV VASSIL P , CHOWDARI NAIDU SREENIVASA
发明人： GOMURASHVILI ZAZA D , TURNELL WILLIAM D , VASSILEV VASSIL P , CHOWDARI NAIDU SREENIVASA
IPC分类号： C07D233/00
CPC分类号： C07D495/04 , C07D233/58
摘要： The invention provides biodegradable, water soluble PEA, PEUR and PEU carrier polymers, which can be used to conjugate, and thereby stabilize and/or solublize, bioactive agents via polar uncharged or charged groups and activated ester or amino groups contained in the building blocks that make up the backbone of the polymer. The bioactive agents are released at a controlled rate determined by biodegradation of the polymers. The highly versatile Active Polycondensation (APC) method, which is mainly carried out in solution at mild temperatures, readily allows synthesis of such polymers. The invention water soluble polymers can also be used as water solubilizing tethers to attach drugs, and biologies to the surface of such carrier constructs as liposomes, particles and micelles.
摘要翻译：本发明提供可生物降解的水溶性PEA，PEUR和PEU载体聚合物，其可用于通过极性不带电荷或带电基团和包含在构建块中的活化的酯或氨基来缀合并由此稳定和/或溶解生物活性剂，弥补聚合物的骨架。生物活性剂以通过聚合物的生物降解测定的受控速率释放。主要在温和温度下在溶液中进行的多功能活性缩聚（APC）方法容易合成这种聚合物。本发明的水溶性聚合物也可以用作水溶性绳索以附着药物，以及生物制品作为脂质体，颗粒和胶束等载体构建体的表面。

4. 发明申请

WO0048463A9 METHOD FOR PREPARATION OF PHARMACEUTICAL-GRADE DITHIOCARBAMATE 审中-公开
标题翻译：制备药物级二氢碳酸酯的方法
公开(公告)号：WO0048463A9
公开(公告)日：2001-11-01
申请号：PCT/US0003994
申请日：2000-02-16
申请人： MEDINOX INC , VASSILEV VASSIL P , LIAW WEI CHENG , LAI CHING SAN
发明人： VASSILEV VASSIL P , LIAW WEI-CHENG , LAI CHING-SAN
IPC分类号： A61K31/325 , C07C333/16 , A01N47/10 , C07C333/00
CPC分类号： C07C333/16
摘要： The present invention provides methods for producing pharmaceutical-grade particulate dithiocarbamates from secondary amines by vigorously contacting at least one secondary amine and a pharmaceutically acceptable diluent that is a solvent for the carbon disulfide, but not for the secondary amine in an inert gas atmosphere, cooling the mixture so as to precipitate the dithiocarbamate therefrom, and separating the precipitated dithiocarbamate from the cooled mixture. The preferred solvent contains absolute ethanol. In alternative embodiments, the invention further provides methods for purifying a dithiocarbamate to obtain a pharmaceutical-grade dithiocarbamate particulate from a dithiocarbamate feed and methods for producing a sterile pharmaceutical-grade dithiocarbamate from a dithiocarbamate feed.
摘要翻译：本发明提供了通过与惰性气体气氛中的至少一种仲胺和作为二硫化碳的溶剂而不是仲胺的药学上可接受的稀释剂剧烈接触来从仲胺生产药物级颗粒二硫代氨基甲酸盐的方法，冷却混合物以从其中沉淀二硫代氨基甲酸盐，并将沉淀的二硫代氨基甲酸盐与冷却的混合物分离。优选的溶剂含有无水乙醇。在替代实施方案中，本发明还提供了用于纯化二硫代氨基甲酸盐以从二硫代氨基甲酸盐进料获得药物级二硫代氨基甲酸盐颗粒的方法和从二硫代氨基甲酸盐进料生产无菌药用二硫代氨基甲酸盐的方法。

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