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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

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。

3. 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。

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. 发明专利

AU2007209366A1 Use of hyaluronic acid as a carrier molecule for different classes of therapeutic active agents 未知
公开(公告)号：AU2007209366A1
公开(公告)日：2007-08-02
申请号：AU2007209366
申请日：2007-01-25
申请人： EURAND PHARMACEUTICALS LTD
发明人： BERGAMIN MASSIMO , NORBEDO STEFANO , KHAN RIAZ AHMED , MURANO ERMINIO , BOSI SUSANNA
IPC分类号： A61K31/728 , A61K47/48 , A61P29/00 , A61P31/00 , A61P35/00
摘要： The present invention refers to a drug delivery system consisting of hyaluronic acid and a therapeutic active agent.

6. 发明专利

ES2337726T3 FARMACO ANTIPROLIFERATIVO. 未知
公开(公告)号：ES2337726T3
公开(公告)日：2010-04-28
申请号：ES06763171
申请日：2006-05-17
申请人： EURAND PHARMACEUTICALS LTD
发明人： MURANO ERMINIO , FLAIBANI ANTONELLA , BERGAMIN MASSIMO , NORBEDO STEFANO , SORBI CLAUDIA , KHAN RIAZ AHMED
IPC分类号： A61K47/48 , A61K31/728 , A61P35/00
摘要： Conjugados de ácido hialurónico, en forma tanto de ácido como de sal, en los que los grupos hidroxilo primarios de la unidad de N-acetil-D-glucosamina del ácido hialurónico se esterifican ambos con el grupo carboxílico de un compuesto A seleccionado de entre: (i): Un ácido alifático seleccionado de entre el grupo que consiste en el ácido acético, el ácido butírico, el ácido propiónico, el ácido retinoico, el ácido n-propilacético, el ácido succínico, el ácido ciclohexanocarboxílico, el ácido ciclohexanoacetílico y el ácido ciclopropanocarboxílico; (ii) un aminoácido seleccionado de entre el grupo que consiste en alanina, valina, leucina, isoleucina, metionina, glicina, serina, cisteína, asparagina, glutamina, ácido aspártico, ácido glutámico, prolina, histidina fenilalanina, triptófano y tirosina; (iii) Un ácido arilalifático seleccionado de entre el grupo que consiste en el ácido fenilacético, el ácido fenoxiacético, el ácido naftilacético, el ácido 2-(4-isobutilfenil) propiónico, el ácido 2-(6-metoxi-2-naftil) propiónico y el ácido cinámico; (iv) ácido benzoico sustituido o sin sustituir. y con **(Ver fórmula)** R2 y R4, independientemente entre sí representan: -NH2, -OH, -OCH3, un grupo alquilo C1 -C5, =O; X e Y representan: -C(R5)=, -CH(R5)-, -NH-, -N=, en la que R5 representa: -H, un grupo alquilo C1 - C5; Z representa: -CH(R10)-, -N(R10)-, -O-; R10 representa: -H, un grupo alquilo C1 - C5, un grupo alquenilo C1 - C5, un grupo alquinilo C1 - C5, un anillo heterocíclico con un número de miembros comprendido entre 5 y 6 con de 1 a 3 heteroátomos seleccionados de entre el grupo que consiste en nitrógeno, azufre y oxígeno; Ar representa: un grupo 1,4-fenilo, un grupo 1,4-fenilo condensado con uno o más anillos aromáticos con un número de miembros comprendido entre 5 y 6, un grupo 1,4-fenilo condensado con uno o más heterociclos con un número de miembros comprendido entre 5 y 6, en la que dichos grupos están posiblemente sustituidos con R2; los anillos A y B, independientemente entre sí, pueden ser aromáticos o no aromáticos.

7. 发明专利

AU2006248966A1 Antiproliferative conjugates comprising hyaluronic acid and N-derivatives of glutamic acid 未知
公开(公告)号：AU2006248966A1
公开(公告)日：2006-11-23
申请号：AU2006248966
申请日：2006-05-17
申请人： EURAND PHARMACEUTICALS LTD
发明人： NORBEDO STEFANO , BERGAMIN MASSIMO , KHAN RIAZ AHMED , SORBI CLAUDIA , MURANO ERMINIO , FLAIBANI ANTONELLA
IPC分类号： A61K31/48 , A61K31/715 , A61K31/728 , A61P35/00
摘要： Object of the present invention are esterified conjugates of hyaluronic acid having anti-proliferative activity.

8. 发明专利

IE20060565A1 Drug delivery system based on regioselectively amidated hyaluronic acid 未知
公开(公告)号：IE20060565A1
公开(公告)日：2008-02-06
申请号：IE20060565
申请日：2006-07-28
申请人： EURAND PHARMACEUTICALS LTD
发明人： NORBEDO STEFANO , BOSI SUSANNA , BERGAMIN MASSIMO , KHAN RIAZ , MURANO ERMINIO , DINON FRANCESCA
IPC分类号： A61K47/36 , A61K47/48
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 released 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. 发明专利

CA2658587A1 DRUG DELIVERY SYSTEM BASED ON REGIOSELECTIVELY AMIDATED HYALURONIC ACID 未知
公开(公告)号：CA2658587A1
公开(公告)日：2008-01-31
申请号：CA2658587
申请日：2007-07-27
申请人： EURAND PHARMACEUTICALS LTD
发明人： DINON FRANCESCA , MURANO ERMINIO , KHAN RIAZ AHMED , NORBEDO STEFANO , BERGAMIN MASSIMO , BOSI SUSANNA
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 o r 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. Preferre d therapeutic agents for use in the present DDS are anti-inflammatory, antib iotic, antitumor drugs. Preferred linkers are: succinic acid, succinic acid linked to aminoacids, succinic acid linked to peptides. The DDS are stable a nd free of undesired reaction by-products and impurities, and show a high le vel of pharmacological efficacy.

10. 发明专利

DE602006010852D1 未知
公开(公告)号：DE602006010852D1
公开(公告)日：2010-01-14
申请号：DE602006010852
申请日：2006-05-17
申请人： EURAND PHARMACEUTICALS LTD
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： Object of the present invention are esterified conjugates of hyaluronic acid having anti-proliferative activity.

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