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1. 发明申请

US20090253651A1 DRUG DELIVERY SYSTEM BASED ON REGIOSELECTIVELY AMIDATED HYALURONIC ACID 审中-公开
标题翻译：药物递送系统基于静脉注射的羟丙酸
公开(公告)号：US20090253651A1
公开(公告)日：2009-10-08
申请号：US12375379
申请日：2007-07-27
申请人： Stefano Norbedo , Susanna Bosi , Massimo Bergamin , Riaz Ahmed Khan , Erminio Murano , Francesca Dinon
发明人： Stefano Norbedo , Susanna Bosi , Massimo Bergamin , Riaz Ahmed Khan , Erminio Murano , Francesca Dinon
IPC分类号： A61K31/728 , C07H5/06 , C07K2/00
CPC分类号： C08B37/0072 , A61K47/61
摘要： New drug delivery systems (DDS) are described containing hyaluronic acid and a therapeutic agent, wherein the therapeutic agent is linked, directly or via a linker, to 6-aminohyaluronic acid and where the linkage of the drug or linker with 6-aminohyaluronic acid is realised by an amide bond. Preferred therapeutic agents for use in the present DDS are anti-inflammatory, antibiotic, antitumor drugs. Preferred linkers are: succinic acid, succinic acid linked to aminoacids, succinic acid linked to peptides. The DDS are stable and free of undesired reaction by-products and impurities, and show a high level of pharmacological efficacy.
摘要翻译：描述了新的药物递送系统（DDS），其含有透明质酸和治疗剂，其中治疗剂直接或经由接头连接至6-氨基透明质酸，并且其中药物或接头与6-氨基透明质酸的连接是通过酰胺键实现。用于本DDS的优选治疗剂是抗炎，抗生素，抗肿瘤药物。优选的接头是：琥珀酸，与氨基酸连接的琥珀酸，与肽连接的琥珀酸。 DDS稳定，没有不希望的反应副产物和杂质，显示出高水平的药理功效。

2. 发明申请

US20090197797A1 USE OF HYALURONIC ACID AS A CARRIER MOLECULE FOR DIFFERENT CLASSES OF THERAPEUTIC ACTIVE AGENTS 审中-公开
标题翻译：用作不同类型治疗活性剂的载体分子的羟丙酸
公开(公告)号：US20090197797A1
公开(公告)日：2009-08-06
申请号：US12162337
申请日：2007-01-25
申请人： Stefano Norbedo , Susanna Bosi , Massimo Bergamin , Riaz Ahmed Khan , Erminio Murano
发明人： Stefano Norbedo , Susanna Bosi , Massimo Bergamin , Riaz Ahmed Khan , Erminio Murano
IPC分类号： A61K38/38 , C07H5/06 , A61K31/728
CPC分类号： A61K31/728 , A61K47/61
摘要： The present invention refers to a drug delivery system consisting of hyaluronic acid and a therapeutic active agent.
摘要翻译：本发明涉及由透明质酸和治疗活性剂组成的药物递送系统。

3. 发明授权

US4117224A Preparation of sucrose 6,6'-dichloro hexa-acetate 失效
标题翻译：蔗糖6,6“ - 二氯乙酸乙酯的制备
公开(公告)号：US4117224A
公开(公告)日：1978-09-26
申请号：US639780
申请日：1975-12-11
申请人： Riaz Ahmed Khan , Khizar Sultan Mufti , Kenneth John Parker
发明人： Riaz Ahmed Khan , Khizar Sultan Mufti , Kenneth John Parker
IPC分类号： C07H5/02 , C07H13/04
CPC分类号： C07H5/02 , C07H13/04
摘要： 6,6'-Dichloro-6,6'-dideoxysucrose is obtained directly in high yield by reacting sucrose with methanesulphonyl chloride in N,N-dimethylformamide. 1',6,6'-Trichloro-1',6,6'-trideoxysucrose is obtained as a by-product and its formation can be suppressed by starting the reaction at -40.degree. C to -15.degree. C. The dichlorodideoxy and trichloro-trideoxy compounds, which are useful as intermediates for preparing other sucrose derivates, are most conveniently isolated from the reaction mixture in the form of their hexa-acetate and penta-acetate respectively, which are then deacetylated to give the free compounds.

4. 发明授权

US4002609A Sucrose derivatives 失效
标题翻译：蔗糖衍生物
公开(公告)号：US4002609A
公开(公告)日：1977-01-11
申请号：US552205
申请日：1975-02-24
申请人： Riaz Ahmed Khan
发明人： Riaz Ahmed Khan
IPC分类号： C07H13/06 , C07H13/04 , C08B37/00
CPC分类号： C07H13/04
摘要： Two sucrose hepta-acetates, useful as synthetic intermediates in the preparation of functional sucrose derivatives, are obtained by tritylating sucrose, acetylating the resulting mixture of monotritylsucroses, and detritylating the resulting mixture of monotritylsucrose hepta-acetates. The previously known compound, 1',2,3,3',4,4',6-hepta-O-acetylsucrose, can be recovered by crystallization from the solution obtained in the detritylation step. When the remaining solution is subjected to retritylation and chromatography, it yields a new compound, 1',2,3,3',4',6,6'-hepta-O-acetylsucrose.
摘要翻译：在制备功能性蔗糖衍生物中可用作合成中间体的两种蔗糖七乙酸酯通过三苯甲基化蔗糖获得，乙酰化所得到的单重性蔗糖混合物，并使所得到的单甘油蔗糖七乙酸酯的混合物脱硝。先前已知的化合物1'，2,3,3'，4,4'，6-七-O-乙酰蔗糖可以通过从去离
子化步骤中得到的溶液中结晶回收。当剩余的溶液进行再溶剂和色谱法时，产生新的化合物1'，2,3,3'，4'，6,6'-七-O-乙酰基蔗糖。

5. 发明授权

US3996206A Process of making sucrose esters 失效
标题翻译：制备蔗糖酯的方法
公开(公告)号：US3996206A
公开(公告)日：1976-12-07
申请号：US448695
申请日：1974-03-06
申请人： Kenneth John Parker , Riaz Ahmed Khan , Khizar Sultan Mufti
发明人： Kenneth John Parker , Riaz Ahmed Khan , Khizar Sultan Mufti
IPC分类号： C07G3/00 , B01F17/34 , C07H13/06 , C11D1/00 , C11D1/68 , C08B37/00
CPC分类号： C07H13/06 , Y10S516/06
摘要： A surface active composition is prepared by reacting solid particulate sucrose with at least one triglyceride, in the presence of a basic transesterification catalyst, at a temperature of from 110.degree. to 140.degree. C, at atmospheric pressure and in the absence of any solvent. The preferred temperature range is 120.degree. to 130.degree. C, most preferably about 125.degree. C. The preferred catalyst is potassium carbonate. The reaction can be accelerated by adding a suitable emulsifier, such as a diglyceride, a monoglyceride or a surfactant product of the reaction, to the reaction mixture.
摘要翻译：在碱性酯交换催化剂的存在下，在大气压下和在不存在任何溶剂的条件下，使固体颗粒状蔗糖与至少一种甘油三酸酯在110-140℃的温度下反应制备表面活性组合物。优选的温度范围是120℃至130℃，最优选约125℃。优选的催化剂是碳酸钾。可以通过向反应混合物中加入合适的乳化剂，例如甘油二酯，单酸甘油酯或反应的表面活性剂产物来加速反应。

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