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1. 发明授权

EP1411956B1 USE OF OVERSULFATED POLYSACCHARIDES AS INHIBITORS OF HIV 有权
标题翻译：过硫酸化多糖AS艾滋病病毒抑制剂的用途
公开(公告)号：EP1411956B1
公开(公告)日：2005-07-06
申请号：EP02749173.7
申请日：2002-07-26
申请人： FONDAZIONE CENTRO SAN RAFFAELE DEL MONTE TABOR , Zoppetti, Giorgio , Oreste, Pasqua Anna
发明人： ZOPPETTI, Giorgio , ORESTE, Pasqua, Anna , POLI, Guido , VICENZI, Elisa
IPC分类号： A61K31/737 , A61P31/18
CPC分类号： A61K31/737
摘要： The present invention relates to the use of N,O oversulfated K5 derivatives having a degree of sulfation higher than 3.2 or of their pharmaceutically acceptable salts for the preparation of pharmaceutical composition s for treating the infection and the consequent HIV/AIDS disease.

2. 发明公开

EP1411956A1 USE OF OVERSULFATED POLYSACCHARIDES AS INHIBITORS OF HIV 有权
标题翻译：过硫酸化多糖AS艾滋病病毒抑制剂的用途
公开(公告)号：EP1411956A1
公开(公告)日：2004-04-28
申请号：EP02749173.7
申请日：2002-07-26
申请人： FONDAZIONE CENTRO SAN RAFFAELE DEL MONTE TABOR , Zoppetti, Giorgio , Oreste, Pasqua Anna
发明人： ZOPPETTI, Giorgio , ORESTE, Pasqua, Anna , POLI, Guido , VICENZI, Elisa
IPC分类号： A61K31/737 , A61P31/18
CPC分类号： A61K31/737
摘要： The present invention relates to the use of N,O oversulfated K5 derivatives having a degree of sulfation higher than 3.2 or of their pharmaceutically acceptable salts for the preparation of pharmaceutical composition s for treating the infection and the consequent HIV/AIDS disease.

3. 发明申请

WO2003106505A1 PROCESS FOR THE MANUFACTURE OF N-ACYL-(EPI)K5-AMINE-O-SULFATE-DERIVATIVES AND PRODUCTS THUS OBTAINED 审中-公开
标题翻译：制备N-亚氨基 - （EPI）K5-氨基-O-硫酸酯衍生物和获得的产品的方法
公开(公告)号：WO2003106505A1
公开(公告)日：2003-12-24
申请号：PCT/IB2003/002339
申请日：2003-06-17
申请人： ORESTE, Pasqua, Anna , ZOPPETTI, Giorgio
发明人： ORESTE, Pasqua, Anna , ZOPPETTI, Giorgio
IPC分类号： C08B37/00
CPC分类号： A61K31/726 , A61K31/727 , A61K31/737 , C07H1/00 , C08B37/006 , C08B37/0075 , C08B37/0078
摘要： A new method is described for the oversulfation of (epi)KS-N-sulfates to obtain (epi)K5-amine-O-oversulfates at extremely high degree of sulfation and for the transformation of these intermediates into new Nacyl-(epi)K5-amine-O-oversulfates basically free of activity on the coagulation parameters and useful in the cosmetic or pharmaceutical field. Also described are pharmaceutical compositions containing, as one of their active ingredients, an (epi)K5-amine-O-oversulfate.
摘要翻译：描述了一种用于（epi）KS-N-硫酸盐过硫酸盐以获得（epi）极高硫酸化程度的（表面）K 5 - 胺 - O-硫酸盐和将这些中间体转化成新的Nacyl-（epi）K5的新方法 - 胺 - 过硫酸盐基本上没有凝血参数的活性，并且在化妆品或制药领域中有用。还描述了含有作为其活性成分之一的（epi）K5-胺-O-过硫酸盐的药物组合物。

4. 发明申请

WO2003106506A1 LOW MOLECULAR WEIGHT OVERSULFATED POLYSACCHARIDE 审中-公开
标题翻译：低分子量超声波多糖
公开(公告)号：WO2003106506A1
公开(公告)日：2003-12-24
申请号：PCT/IB2003/002347
申请日：2003-06-17
申请人： ORESTE, Pasqua, Anna , ZOPPETTI, Giorgio
发明人： ORESTE, Pasqua, Anna , ZOPPETTI, Giorgio
IPC分类号： C08B37/00
CPC分类号： A61K31/726 , A61K31/727 , A61K31/737 , C07H1/00 , C08B37/006 , C08B37/0075 , C08B37/0078
摘要： LMW-K5-N,O-oversulfates are described, having a sulfation degree of from 3.2 to 4 and a mean molecular weight of from about 3,000 to about 6,000, obtainable by depolymerization of corresponding K5-N,O-oversulfates or starting from LMW-K5-N-sulfates by O-oversulfation of a tertiary amine or quaternary ammonium salt thereof and subsequent N-resulfation of the K5-amine-O-oversulfate thus obtained. Furthermore, pharmaceutical compositions containing these LMW-K5-N,Ooversulfates having antiangiogenetic and antiviral, in particular anti-HIV-1 activity. Intermediate LMW-K5-N-sulfates are also described.
摘要翻译：描述了LMW-K5-N，过硫酸盐，其硫酸化度为3.2至4，平均分子量为约3,000至约6,000，可通过相应的K5-N，O-硫酸盐的解聚或从LMW开始获得 -K5-N-硫酸盐，其通过叔胺或其季铵盐的过氧化和随后的N-重硫化由此获得的K5-胺-O-硫酸盐。此外，含有具有抗血管发生和抗病毒药物的这些LMW-K5-N，过硫酸盐的药物组合物，特别是抗HIV-1活性。还描述了中间体LMW-K5-N-硫酸盐。

5. 发明申请

WO2002083155A1 USE OF SULFATED BACTERIAL POLYSACCHARIDES SUITABLE FOR THE INHIBITION OF ANGIOGENESIS 审中-公开
标题翻译：使用适合抑制血管生成的硫酸多糖
公开(公告)号：WO2002083155A1
公开(公告)日：2002-10-24
申请号：PCT/IB2002/001138
申请日：2002-04-10
申请人： UNIVERSITA' DEGLI STUDI DI BRESCIA , ZOPPETTI, Giorgio , ORESTE, Pasqua, Anna , PRESTA, Marco
发明人： ZOPPETTI, Giorgio , ORESTE, Pasqua, Anna , PRESTA, Marco
IPC分类号： A61K31/737
CPC分类号： A61K31/737
摘要： The present invention refers to the use of N,O sulfated K5 having a degree of sulfation of at least 2, and of their pharmaceutical acceptable salts for the preparation of medicaments for treating angiogenesis-dependent diseases.
摘要翻译：本发明涉及硫酸化程度至少为2的N，O硫酸化K5及其药学上可接受的盐在制备用于治疗血管发生依赖性疾病的药物中的应用。

6. 发明申请

WO2005058976A2 LOW MOLECULAR WEIGHT POLYSACCHARIDES HAVING ANTHROMBOTIC ACTIVITY 审中-公开
标题翻译：低分子量多糖具有抗氧化活性
公开(公告)号：WO2005058976A2
公开(公告)日：2005-06-30
申请号：PCT/IB2004/004128
申请日：2004-12-15
申请人： GLYCORES 2000 S.R.L. , ORESTE, Pasqua, Anna , ZOPPETTI, Giorgio
发明人： ORESTE, Pasqua, Anna , ZOPPETTI, Giorgio
IPC分类号： C08B37/00
CPC分类号： C08B37/0063
摘要： Novel depolymerized-LMWepiK5-N,O-sulfates obtainable starting from a LMW epiK5-N-sulfate prepared by nitrous depolymerization of an epiK5-N-sulfate or by C5-epimerization of a LMW-K5-N-sulfate obtained by nitrous depolymerization of a KS-N-sulfate. A process consists of submitting the starting depolymerized-LMW-epiK5-N-sulfate to four steps: a O-oversulfation, a partila 0-desulfation, a 6-0-sulfation and a N-sulfation. The new depolymerizedLMWepiK5-N,O-sulfates present a di- or trisulfated 2,5-anhydromannitol unit at the reducing end of the majority of its chains, have a content of iduronic acid of 40-60%, a sulfation degree of from 2.3 to 2.9 and a mean molecular weight of from about 1,500 to about 12,000. They exhibit a good antithrombotic activity with a low pro-hemorrhagic risk.
摘要翻译：新型解聚LMWepiK5-N，O-硫酸酯可从LMW＆shy开始获得; 通过epiK5-N-硫酸盐的亚硝基解聚反应制备的epiK5-N-硫酸酯或通过KS-N-硫酸酯的亚硝基解聚反应获得的LMW-K5-N-硫酸酯的C5-差向异构化制备。一种方法包括将起始解聚的LMW-epiK5-N-硫酸酯分成四个步骤：O-过硫酸盐，partila-脱硫酸盐，6-0-硫酸盐化和N-硫酸盐化。新的解聚＆害羞的; LMWepiK5-N，O-硫酸盐在其大部分链的还原端呈现二 - 或三硫酸化的2,5-脱水甘露糖醇单元，具有40-60％的艾杜糖醛酸含量，硫酸化度从2.3到2.9，平均分子量从约1,500到约12,000。它们表现出良好的抗血栓形成活性，具有低的出血前风险。

7. 发明申请

WO2003106504A1 EPIMERIZED DERIVATIVES OF K5 POLYSACCHARIDE WITH A VERY HIGH DEGREE OF SULFATION 审中-公开
标题翻译： K5多糖的异构衍生物具有非常高的硫化程度
公开(公告)号：WO2003106504A1
公开(公告)日：2003-12-24
申请号：PCT/IB2003/002338
申请日：2003-06-17
申请人： ORESTE, Pasqua, Anna , ZOPPETTI, Giorgio
发明人： ORESTE, Pasqua, Anna , ZOPPETTI, Giorgio
IPC分类号： C08B37/00
CPC分类号： A61K31/726 , A61K31/727 , A61K31/737 , C07H1/00 , C08B37/006 , C08B37/0075 , C08B37/0078
摘要： A new method is described for the oversulfation of epiK5-N-sulfate to obtain an epiK5-amine-O-oversulfate with very high sulfation degree which, by subsequent N-sulfation, provides new epiK5-N,O-oversulfate-derivatives with a sulfation degree of at least 4, basically free of activity on the coagulation parameters and useful in the cosmetic or pharmaceutical field. Also described are new low molecular weight epiK5-N-sulfates useful as intermediates in the preparation of the corresponding LMW-epiK5-N,O-oversulfate-derivatives.
摘要翻译：描述了一种用于过硫酸化epiK5-N-硫酸盐以获得具有非常高的硫酸化程度的epiK5-胺-O-硫酸盐的新方法，其通过随后的N-硫酸化，提供新的epiK5-N，O-过硫酸盐衍生物与硫酸化度至少为4，对凝结参数基本没有活性，可用于化妆品或制药领域。还描述了可用作制备相应的LMW-epiK5-N，过硫酸盐衍生物的中间体的新的低分子量epiK5-N-硫酸盐。

8. 发明申请

WO2003011307A1 USE OF OVERSULFATED POLYSACCHARIDES AS INHIBITORS OF HIV 审中-公开
标题翻译：使用作为艾滋病毒感染者的绝经多糖
公开(公告)号：WO2003011307A1
公开(公告)日：2003-02-13
申请号：PCT/IB2002/002909
申请日：2002-07-26
申请人： FONDAZIONE CENTRO SAN RAFFAELE DEL MONTE TABOR , ZOPPETTI, Giorgio , ORESTE, Pasqua, Anna , POLI, Guido , VICENZI, Elisa
发明人： ZOPPETTI, Giorgio , ORESTE, Pasqua, Anna , POLI, Guido , VICENZI, Elisa
IPC分类号： A61K31/737
CPC分类号： A61K31/737
摘要： The present invention relates to the use of N,O oversulfated K5 derivatives having a degree of sulfation higher than 3.2 or of their pharmaceutically acceptable salts for the preparation of pharmaceutical composition s for treating the infection and the consequent HIV/AIDS disease.
摘要翻译：本发明涉及硫酸化程度高于3.2的N，O过硫酸化K5衍生物或其药学上可接受的盐在制备用于治疗感染和随后的HIV / AIDS疾病的药物组合物中的用途。

9. 发明申请

WO2002068477A1 HIGHLY SULFATED DERIVATIVES OF K5 POLYSACCHARIDE AND THEIR PREPARATION 审中-公开
标题翻译： K5多糖的高度硫化衍生物及其制备
公开(公告)号：WO2002068477A1
公开(公告)日：2002-09-06
申请号：PCT/IB2002/000561
申请日：2002-02-26
申请人： ZOPPETTI, Giorgio , ORESTE, Pasqua, Anna
发明人： ZOPPETTI, Giorgio , ORESTE, Pasqua, Anna
IPC分类号： C08B37/00
CPC分类号： C07H3/00 , A61K31/737 , C08B37/0063 , C08B37/0075 , Y02A50/473
摘要： The purification of the E.coli K5 polysaccharide by treatment with isopropyl alcohol and elimination of lipophilic substances is described. The purified product can be used to prepare, after N-deacetylation, new N,O-sulfated polysaccharides with high degree of sulfation.
摘要翻译：描述了通过用异丙醇处理和消除亲脂性物质来纯化大肠杆菌K5多糖。纯化的产物可用于在N-脱乙酰化后制备具有高程度硫酸化的新的N，O-硫酸化多糖。

10. 发明申请

WO2006095026A2 NEW SOFT GELATIN CAPSULES 审中-公开
标题翻译：新软胶囊
公开(公告)号：WO2006095026A2
公开(公告)日：2006-09-14
申请号：PCT/EP2006/060649
申请日：2006-03-13
申请人： ALTERGON S.A. , ZOPPETTI, Giorgio , MARCHIORRI, Maurizio
发明人： ZOPPETTI, Giorgio , MARCHIORRI, Maurizio
CPC分类号： A61K9/4825 , A61K31/355 , A61K31/4415 , A61K31/51 , A61K31/525 , A61K31/57 , A61K31/593 , A61K31/616 , A61K31/714 , A61K33/04 , A61K33/08 , A61K33/10 , A61K33/18 , A61K33/30 , A61K47/40
摘要： The present invention relates to soft gelatin capsules characterized in that the shell includes a cyclodextrin and in that the filling material contains a liposoluble drug capable of forming a complex with said cyclodextrin for improving the solubility of the active ingredient upon disintegration of the soft gelatin capsule.
摘要翻译：本发明涉及软明胶胶囊，其特征在于该壳包括环糊精，并且填充材料含有能够与所述环糊精形成络合物的脂溶性药物，以改善活性成分在软明胶胶囊分解时的溶解度。

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