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1. 发明申请

WO2009074678A3 ANTICANCER CONJUGATES OF CAMPTOTHECIN TO HYALURONIC ACID 审中-公开
标题翻译：氨苄青霉素对羟丙酸的反应
公开(公告)号：WO2009074678A3
公开(公告)日：2009-08-13
申请号：PCT/EP2008067433
申请日：2008-12-12
申请人： EURAND PHARMACEUTICALS LTD , NORBEDO STEFANO , DINON FRANCESCA , BOSI SUSANNA , BERGAMIN MASSIMO , MURANO ERMINIO
发明人： NORBEDO STEFANO , DINON FRANCESCA , BOSI SUSANNA , BERGAMIN MASSIMO , MURANO ERMINIO
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： A61K47/61
摘要： New conjugates are described, containing camptothecin connected to hyaluronic acid via a linker, where the linker is bound to the hyaluronic acid by means of an ester bond. The ester bond involves on one side, a hydroxyl group of hyaluronic acid and, on the other side, a carboxyl group present on the linker; the linker is covalently bonded to camptothecin. Pharmaceutical compositions thereof, their use in the treatment of pathologies responsive to camptothecin, and a process to prepare said conjugates are also described.
摘要翻译：描述了新的缀合物，其含有通过接头与透明质酸连接的喜树碱，其中接头通过酯键与透明质酸结合。酯键在一侧涉及透明质酸的羟基，另一方面存在于接头上的羧基; 接头共价键合到喜树碱。还描述了其药物组合物，其用于治疗对喜树碱有反应的病理学的用途，以及制备所述缀合物的方法。

2. 发明申请

WO2007085629A3 USE OF HYALURONIC ACID AS A CARRIER MOLECULE FOR?DIFFERENT CLASSES OF THERAPEUTIC ACTIVE AGENTS 审中-公开
标题翻译：作为载体分子的羟丙酸的使用？不同类型的治疗活性剂
公开(公告)号：WO2007085629A3
公开(公告)日：2007-11-29
申请号：PCT/EP2007050726
申请日：2007-01-25
申请人： EURAND PHARMACEUTICALS LTD , NORBEDO STEFANO , BOSI SUSANNA , BERGAMIN MASSIMO , KHAN RIAZ AHMED , MURANO ERMINIO
发明人： NORBEDO STEFANO , BOSI SUSANNA , BERGAMIN MASSIMO , KHAN RIAZ AHMED , MURANO ERMINIO
IPC分类号： A61K31/728 , A61K47/48 , A61P29/00 , A61P31/00 , A61P35/00
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. 发明申请

WO2009074678A2 NEW ANTICANCER CONJUGATES 审中-公开
标题翻译：新的反对者联合
公开(公告)号：WO2009074678A2
公开(公告)日：2009-06-18
申请号：PCT/EP2008/067433
申请日：2008-12-12
申请人： EURAND PHARMACEUTICALS LIMITED , NORBEDO, Stefano , DINON, Francesca , BOSI, Susanna , BERGAMIN, Massimo , MURANO, Erminio
发明人： NORBEDO, Stefano , DINON, Francesca , BOSI, Susanna , BERGAMIN, Massimo , MURANO, Erminio
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： A61K47/61
摘要： New conjugates are described, containing camptothecin connected to hyaluronic acid via a linker, where the linker is bound to the hyaluronic acid by means of an ester bond. The ester bond involves on one side, a hydroxyl group of hyaluronic acid and, on the other side, a carboxyl group present on the linker; the linker is covalently bonded to camptothecin. Pharmaceutical compositions thereof, their use in the treatment of pathologies responsive to camptothecin, and a process to prepare said conjugates are also described.
摘要翻译：描述了新的缀合物，其含有通过接头与透明质酸连接的喜树碱，其中接头通过酯键与透明质酸结合。酯键在一侧涉及透明质酸的羟基，另一方面存在于接头上的羧基; 接头共价键合到喜树碱。还描述了其药物组合物，其用于治疗对喜树碱有反应的病理学的用途，以及制备所述缀合物的方法。

4. 发明申请

WO2006122954A2 NEW ANTIPROLIFERATIVE DRUG 审中-公开
标题翻译：新型抗增生药
公开(公告)号：WO2006122954A2
公开(公告)日：2006-11-23
申请号：PCT/EP2006062388
申请日：2006-05-17
申请人： EURAND PHARMACEUTICALS LTD , MURANO ERMINIO , FLAIBANI ANTONELLA , BERGAMIN MASSIMO , NORBEDO STEFANO , SORBI CLAUDIA , KHAN RIAZ AHMED
发明人： MURANO ERMINIO , FLAIBANI ANTONELLA , BERGAMIN MASSIMO , NORBEDO STEFANO , SORBI CLAUDIA , KHAN RIAZ AHMED
IPC分类号： A61K31/48 , A61K31/715 , A61P35/00
CPC分类号： A61K31/728 , A61K47/61
摘要： Object of the present invention are esterified conjugates of hyaluronic acid having anti-proliferative activity.
摘要翻译：本发明的目的是具有抗增殖活性的透明质酸的酯化缀合物。

5. 发明申请

WO2012053017A1 ENZYME-CATALYZED PROCESS FOR THE PREPARATION OF SUGAR 6 -E STERS 审中-公开
标题翻译：用于制备糖6 -E STERS的酶催化方法
公开(公告)号：WO2012053017A1
公开(公告)日：2012-04-26
申请号：PCT/IT2010/000420
申请日：2010-10-19
申请人： ISTITUTO DI RICERCA PROTOS , KHAN, Riaz, Ahmed , PERIN, Danilo , MURANO, Erminio , BERGAMIN, Massimo
发明人： KHAN, Riaz, Ahmed , PERIN, Danilo , MURANO, Erminio , BERGAMIN, Massimo
IPC分类号： C12P7/62 , C12P19/44
CPC分类号： C12P19/44 , C12Y301/01003
摘要： The present invention deals with a process for the enzyme-catalysed selective esterif ication of sugar molecules. Said process may comprise one phase in which a lipase enzyme is encapsulated into a biopolymer scaffold to catalyse the selective esterif ication of a sugar substrate with an acylating agent, e.g., an acyl donor fatty acid ester such as a vinyl alkanoate, mostly at a fixed position of the sugar moiety, e.g. at the C-6 position thereof; and one phase in which said reaction is carried out preferably in an alkyl hydroxylic solvent, being both the enzyme and the sugar substrate immobilized or encapsulated within the biopolymer scaffold. This process is particularly useful for producing biodegradable surfactants, like fatty acid esters of suitable sugars, and for producing intermediates for the production of useful sugar derivatives, e.g. 6-O-acyl-sucrose, which is a key intermediate in a route to the production of the high-intensity sweetener Sucralose®.
摘要翻译：本发明涉及糖分解酶催化选择性酯化的方法。所述方法可以包括一个阶段，其中将脂肪酶包封到生物聚合物支架中以催化糖底物与酰化剂（例如酰基供体脂肪酸酯如链烷酸乙烯酯）的选择性酯化，主要是固定的糖部分的位置，例如在C-6位置; 其中所述反应优选在烷基羟基溶剂中进行，所述反应是固定化或包封在生物聚合物支架内的酶和糖底物。该方法特别适用于生产可生物降解的表面活性剂，例如合适的糖的脂肪酸酯，以及制备用于生产有用的糖衍生物的中间体。 6-O-酰基蔗糖，其是生产高强度甜味剂Sucralose的途径中的关键中间体。

6. 发明申请

WO2008012365A2 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：WO2008012365A2
公开(公告)日：2008-01-31
申请号：PCT/EP2007057772
申请日：2007-07-27
申请人： EURAND PHARMACEUTICALS LTD , NORBEDO STEFANO , BOSI SUSANNA , BERGAMIN MASSIMO , KHAN RIAZ AHMED , MURANO ERMINIO , DINON FRANCESCA
发明人： NORBEDO STEFANO , BOSI SUSANNA , BERGAMIN MASSIMO , KHAN RIAZ AHMED , MURANO ERMINIO , DINON FRANCESCA
IPC分类号： A61K47/48
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。

7. 发明申请

WO2007085629A2 A NOVEL DRUG DELIVERY SYSTEM: USE OF HYALURONIC ACID AS A CARRIER MOLECULE FOR DIFFERENT CLASSES OF THERAPEUTIC ACTIVE AGENTS 审中-公开
标题翻译：一种新型药物递送系统：作为载体分子的羟丙酸作为不同类型的治疗活性剂
公开(公告)号：WO2007085629A2
公开(公告)日：2007-08-02
申请号：PCT/EP2007/050726
申请日：2007-01-25
申请人： EURAND PHARMACEUTICALS LTD. , NORBEDO, Stefano , BOSI, Susanna , BERGAMIN, Massimo , KHAN, Riaz Ahmed , MURANO, Erminio
发明人： NORBEDO, Stefano , BOSI, Susanna , BERGAMIN, Massimo , KHAN, Riaz Ahmed , MURANO, Erminio
IPC分类号： A61K31/728 , A61K47/48 , A61P29/00 , A61P31/00 , A61P35/00
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。

8. 发明申请

WO2008012365A3 DRUG DELIVERY SYSTEM BASED ON REGIOSELECTIVELY AMIDATED HYALURONIC ACID 审中-公开
公开(公告)号：WO2008012365A3
公开(公告)日：2008-01-31
申请号：PCT/EP2007/057772
申请日：2007-07-27
申请人： EURAND PHARMACEUTICALS LTD. , NORBEDO, Stefano , BOSI, Susanna , BERGAMIN, Massimo , KHAN, Riaz, Ahmed , MURANO, Erminio , DINON, Francesca
发明人： NORBEDO, Stefano , BOSI, Susanna , BERGAMIN, Massimo , KHAN, Riaz, Ahmed , MURANO, Erminio , DINON, Francesca
IPC分类号： A61K47/48 , A61P35/00
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.

9. 发明申请

WO2006122954A3 ANTIPROLIFERATIVE CONJUGATES COMPRISING HYALURONIC ACID AND N-DERIVATIVES OF GLUTAMIC ACID 审中-公开
公开(公告)号：WO2006122954A3
公开(公告)日：2006-11-23
申请号：PCT/EP2006/062388
申请日：2006-05-17
申请人： EURAND PHARMACEUTICALS LIMITED , MURANO, Erminio , FLAIBANI, Antonella , BERGAMIN, Massimo , NORBEDO, Stefano , SORBI, Claudia , KHAN, Riaz Ahmed
发明人： MURANO, Erminio , FLAIBANI, Antonella , BERGAMIN, Massimo , NORBEDO, Stefano , SORBI, Claudia , KHAN, Riaz Ahmed
IPC分类号： A61K31/48 , A61K31/728 , A61P35/00
摘要： Conjugates between hyaluronic acid and N-derivatives of glutamic acid, are further esterified on the residual primary hydroxyl groups of the hyaluronic acid with an aminoacid, a peptide, an aliphatic acid, an arilaliphatic acid and/or arylic acid a significant and unexpected increase in their antiproliferative activity and decrease in their toxicity is observed.

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