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1. 发明授权

US5648362A Fluoroalkylated amphiphilic ligands, their metallic complexes and their uses 失效
标题翻译：氟烷基化两亲配体，它们的金属络合物及其用途
公开(公告)号：US5648362A
公开(公告)日：1997-07-15
申请号：US377917
申请日：1995-01-25
申请人： Jean G. Riess , Pierre Vierling , Nathalie Garelli
发明人： Jean G. Riess , Pierre Vierling , Nathalie Garelli
IPC分类号： A61K31/44 , A61K31/4418 , A61P17/00 , C07C45/50 , C07D213/22 , C07D213/26 , C07D213/79 , C07D213/80 , C07D471/04 , C07F15/00 , A61K31/435
CPC分类号： C07D213/22 , C07D213/26 , C07D213/80 , C07D471/04 , C07F15/0053 , C07F15/0066 , C07F15/0093
摘要： Fluoroalkylated amphiphilic ligands are derived from aromatic amines of the bipyridine (I) or phenanthroline (II) types, and form complexes with platinum, palladium and ruthenium. ##STR1## In formulae (I) and (II), R.sup.1 and R.sup.2 are independently a hydrogen atom, or a fluoroalkylated or hydrocarbon chain, provided at least one of R.sup.1 and R.sup.2 is a fluoroalkylated chain, and W represents a methylene, ester, ether, carbonyl or amide group.Fluoroalkylated ligands (I or II) and their complexes can be included in preparations comprising emulsions, dispersions, gels, or microemulsions, particularly in preparations for therapeutic use.
摘要翻译：氟烷基化两亲配体衍生自联吡啶（I）或菲咯啉（II）类型的芳族胺，并与铂，钯和钌形成络合物。只要R1和R2中的至少一个为氟代烷基化链，W代表亚甲基，酯，醚，羰基或酰胺基，则其中R 1和R 2独立地为氢原子或氟代烷基化或烃链。氟烷基化配体（I或II）及其配合物可以包括在包含乳液，分散体，凝胶或微乳液的制剂中，特别是在用于治疗用途的制剂中。

2. 发明授权

US5399694A Fluoroalkylated amphiphilic ligands and their metallic complexes 失效
标题翻译：氟烷基化两亲配体及其金属络合物
公开(公告)号：US5399694A
公开(公告)日：1995-03-21
申请号：US955473
申请日：1992-10-02
申请人： Jean G. Riess , Pierre Vierling , Nathalie Garelli
发明人： Jean G. Riess , Pierre Vierling , Nathalie Garelli
IPC分类号： A61K31/44 , A61K31/4418 , A61P17/00 , C07C45/50 , C07D213/22 , C07D213/26 , C07D213/79 , C07D213/80 , C07D471/04 , C07F15/00 , C07F17/02 , C07D401/04 , C07F17/00
CPC分类号： C07D213/22 , C07D213/26 , C07D213/80 , C07D471/04 , C07F15/0053 , C07F15/0066 , C07F15/0093
摘要： Fluoroalkylated amphiphilic ligands of bipyridine (I) that form complexes with platinum and palladium are disclosed. ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom, or a fluoroalkylated or hydrocarbon chain, provided at least one of R.sup.1 and R.sup.2 is a fluoroalkylated chain, and W represents a methylene, ester, ether, carbonyl or amide group.
摘要翻译：公开了与铂和钯形成络合物的联吡啶（I）的氟烷基化两亲配体。其中R 1和R 2独立地为氢原子或氟代烷基化或烃链，其中R 1和R 2中的至少一个为氟代烷基化链，W表示亚甲基，酯，醚，羰基或酰胺基。

3. 发明授权

US5846516A Perfluoroalkylated amphiphilic phosphorus compounds: preparation and biomedical applications 失效
标题翻译：全氟烷基化两亲磷化合物：制备和生物医学应用
公开(公告)号：US5846516A
公开(公告)日：1998-12-08
申请号：US893227
申请日：1992-06-03
申请人： Jean G. Riess , Jacques Greiner , Alain Milius , Pierre Vierling , Frederic Guillod , Sylvie Gaentzler
发明人： Jean G. Riess , Jacques Greiner , Alain Milius , Pierre Vierling , Frederic Guillod , Sylvie Gaentzler
IPC分类号： A61K9/127 , B01F17/00 , C07F9/09 , C07F9/141 , C07H9/04 , C07H11/04 , A61K31/715 , A61K49/00 , B01J13/00 , C07F9/02
CPC分类号： C07H9/04 , A61K9/1272 , B01F17/0064 , C07F9/091 , C07F9/1411 , C07H11/04 , Y10S514/832 , Y10S514/938 , Y10S514/975 , Y10S516/01 , Y10S516/907 , Y10S516/908 , Y10T428/2984
摘要： Perfluoroalkylated amphiphilic phosphorus compounds, corresponding to the formulae: ##STR1## wherein V is O or S; R.sup.1, R.sup.2 and R.sup.3 are H or substituted or unsubstituted perfluoroalkylated or hydrocarbon radicals; provided that R.sup.1, R.sup.2 or R.sup.3 is a perfluoroalkylated radical; and Y and Z are radicals which can bear a part derived from a sugar, a polyol, or a hydrophilic polymer such as polyethyleneglycol, a perfluoroalkylated part or a part derived from a pharmaceutically active molecule, and method for their preparation and use. These compounds can be included in preparations, emulsions, dispersions, gels, microemulsions, notably for biomedical uses.
摘要翻译：全氟烷基化两亲磷化合物，其对应于下式：其中V是O或S; R1，R2和R3是H或取代或未取代的全氟烷基化或烃基; 条件是R1，R2或R3是全氟烷基化基团; 并且Y和Z是可以承载衍生自糖，多元醇或亲水性聚合物如聚乙二醇，全氟烷基化部分或衍生自药学活性分子的部分的部分的基团，及其制备和使用方法。这些化合物可以包括在制剂，乳剂，分散体，凝胶，微乳液中，特别是用于生物医学用途。

4. 发明授权

US5344930A Fluorine and phosphorous-containing amphiphilic molecules with surfactant properties 失效
标题翻译：含氟和含磷的两亲分子具有表面活性剂性质
公开(公告)号：US5344930A
公开(公告)日：1994-09-06
申请号：US149008
申请日：1993-11-08
申请人： Jean G. Riess , Francois Jeanneaux , Marie-Pierre Krafft , Catherine Santaella , Pierre Vierling
发明人： Jean G. Riess , Francois Jeanneaux , Marie-Pierre Krafft , Catherine Santaella , Pierre Vierling
IPC分类号： A61K8/55 , A61K8/06 , A61K8/14 , A61K8/49 , A61K8/58 , A61K8/92 , A61K9/00 , A61K9/127 , A61K31/675 , A61K47/24 , A61K49/00 , C07F9/09 , C07F9/10 , C07F9/14 , C07F9/24 , C07F9/6533 , C07F9/564 , C07F9/568 , C07F9/572 , C07F9/59
CPC分类号： A61K9/0026 , A61K47/24 , A61K49/0002 , A61K9/0019 , A61K9/1271 , A61K9/1272 , C07F9/091 , C07F9/10 , C07F9/6533
摘要： Compounds of the general formula: ##STR1## are useful as surfactants in the preparation of fluorocarbon emulsions, which can be used as oxygen-carrying blood substitutes, and for many other therapeutic and diagnostic applications. They are further useful in liposomal formulations which are themselves therapeutic agents or provide a vehicle for such agents.
摘要翻译：通用化合物：“IMAGE”可用作制备氟碳乳液的表面活性剂，可用作载氧血液代用品，也可用于许多其他治疗和诊断应用。它们在脂质体制剂中是进一步有用的，脂质体制剂本身是治疗剂或提供这种药剂的载体。

5. 发明授权

US5679459A Perfluorinated amphiphilic phosphorous compounds: liposomal compositions 失效
标题翻译：全氟化两亲磷化合物：脂质体组合物
公开(公告)号：US5679459A
公开(公告)日：1997-10-21
申请号：US467467
申请日：1995-06-06
申请人： Jean G. Riess , Jacques Greiner , Alain Milius , Pierre Vierling , Frederic Guillod , Sylvie Gaentzler
发明人： Jean G. Riess , Jacques Greiner , Alain Milius , Pierre Vierling , Frederic Guillod , Sylvie Gaentzler
IPC分类号： A61K9/127 , B01F17/00 , C07F9/09 , C07F9/141 , C07H9/04 , C07H11/04 , B01F17/14 , C07F9/02
CPC分类号： C07H9/04 , A61K9/1272 , B01F17/0064 , C07F9/091 , C07F9/1411 , C07H11/04 , Y10S514/832 , Y10S514/938 , Y10S514/975 , Y10S516/01 , Y10S516/907 , Y10S516/908 , Y10T428/2984
摘要： Perfluoroalkylated amphiphilic phosphorus compounds, corresponding to the formulae: ##STR1## wherein V is O or S; R.sup.1, R.sup.2 and R.sup.3 are H or substituted or unsubstituted perfluoroalkylated or hydrocarbon radicals; provided that R.sup.1, R.sup.2 or R.sup.3 is a perfluoroalkylated radical; and Y and Z are radicals which can bear a part derived from a sugar, a polyol, or a hydrophilic polymer such as polyethyleneglycol, a perfluoroalkylated part or a part derived from a pharmaceutically active molecule, and method for their preparation and use. These compounds can be included in preparations, emulsions, dispersions, gels, microemulsions, notably for biomedical uses.
摘要翻译：全氟烷基化两亲磷化合物，其对应于下式：其中V是O或S; R1，R2和R3是H或取代或未取代的全氟烷基化或烃基; 条件是R1，R2或R3是全氟烷基化基团; 并且Y和Z是可以承载衍生自糖，多元醇或亲水性聚合物如聚乙二醇，全氟烷基化部分或衍生自药学活性分子的部分的部分的基团，及其制备和使用方法。这些化合物可以包括在制剂，乳剂，分散体，凝胶，微乳液中，特别是用于生物医学用途。

6. 发明授权

US5904933A Stable reverse and multiple fluorocarbon emulsions 失效
标题翻译：稳定的反向和多氟碳乳液
公开(公告)号：US5904933A
公开(公告)日：1999-05-18
申请号：US478824
申请日：1995-06-07
申请人： Jean G. Riess , Marie-Pierre Krafft
发明人： Jean G. Riess , Marie-Pierre Krafft
IPC分类号： A61K9/107 , A61K9/00 , A61K9/113 , A61K47/06 , B01J13/00 , A61K9/127
CPC分类号： A61K9/0026 , A61K9/113 , B01F2003/0838 , Y10S514/832 , Y10S514/937 , Y10S514/938
摘要： Stable reverse water-in-fluorocarbon emulsions and water-in-fluorocarbon-in-water multiple emulsions comprising the reverse fluorocarbon emulsions. The reverse emulsions comprise a continuous phase which is a highly fluorinated or perfluorinated compound, a discontinuous aqueous phase and a fluorinated surfactant or mixture of surfactants. The multiple emulsions comprise an aqueous continuous phase and a discontinuous phase comprising globules formed of aqueous droplets dispersed into a highly fluorinated or perfluorinated compound. The emulsions can contain pharmacologically active agents, and are particularly suitable for pulmonary drug delivery.
摘要翻译：包含反向碳氟化合物乳液的稳定的反向含氟碳乳液和含氟碳水化合物的多重乳液。反向乳液包括连续相，其是高度氟化或全氟化合物，不连续水相和氟化表面活性剂或表面活性剂的混合物。多重乳液包含水性连续相和不连续相，其包含由分散在高度氟化或全氟化合物中的水性液滴形成的小球。乳剂可以含有药理活性剂，特别适用于肺部药物递送。

7. 发明授权

US5637564A Amphiphilic compounds derived from amino acids or peptides, their methods of synthesis and their application as drug delivery systems 失效
标题翻译：衍生自氨基酸或肽的两亲化合物，其合成方法及其作为药物递送系统的应用
公开(公告)号：US5637564A
公开(公告)日：1997-06-10
申请号：US470140
申请日：1995-06-06
申请人： Andre A. Pavia , Bernard Pucci , Jean G. Riess , Leila Zarif , Camille Guedj
发明人： Andre A. Pavia , Bernard Pucci , Jean G. Riess , Leila Zarif , Camille Guedj
IPC分类号： A61K9/107 , A61K9/00 , A61K9/127 , A61K47/26 , C07C237/22 , C07C323/60 , C07H15/04 , C07H15/06 , C07K1/107 , C07K1/113 , C07K5/04 , C07K7/04 , A61K38/00 , A61K38/02
CPC分类号： A61K9/0026 , A61K47/26 , A61K9/0019 , A61K9/1272 , B82Y5/00 , C07H15/04 , C07H15/06 , Y10S977/738 , Y10S977/895 , Y10S977/902 , Y10S977/907 , Y10S977/915
摘要： Amphiphilic derivatives of amino acids or peptides are provided, comprising a polyhydroxylated hydrophilic part derived from a sugar, from a polyol, from an aminopolyol or from an oligosaccharide, and at least one hydrophobic part derived from a hydrocarbon, fluorocarbon, or a mixed fluorocarbon/hydrocarbon, saturated or unsaturated, having from 5 to 20 carbon atoms, the hydrophobic part(s) being linked to the hydrophilic part by a junction bearing an amino acid or a peptide.
摘要翻译：提供氨基酸或肽的两亲性衍生物，其包含衍生自糖的多羟基化亲水部分，多元醇，氨基多元醇或寡糖，以及衍生自烃，碳氟化合物或混合碳氟化合物的至少一种疏水部分，具有5至20个碳原子的烃，饱和或不饱和的，疏水部分通过带有氨基酸或肽的连接物与亲水部分连接。

8. 发明授权

US5582813A Iodine-containing fluorocarbon contrast agents 失效
标题翻译：含碘碳氟造影剂
公开(公告)号：US5582813A
公开(公告)日：1996-12-10
申请号：US188396
申请日：1994-01-27
申请人： Jean G. Riess , Leila Zarif , Veronique Sanches , Jacques Greiner
发明人： Jean G. Riess , Leila Zarif , Veronique Sanches , Jacques Greiner
IPC分类号： A61K49/04 , A61K51/12 , B01J13/00
CPC分类号： A61K49/0461 , A61K2123/00 , Y10S514/938
摘要： The present invention relates to nonterminally iodinated fluorinated compositions. The compositions, including, dispersions, emulsions, microemulsions, and gels are useful for biomedical applications, particularly radiography and scintigraphy. The compounds used in the invention preferably have the following general formula:R.sub.F CH.dbd.CIR.sup.1wherein,R.sub.F is a linear, branched, or cyclic first fluorocarbon radical, having 2 to 12 carbon atoms in which 50 to 100% of the hydrogen atoms have been replaced by fluorine atoms; andR.sup.1 is selected from the group consisting of a second fluorocarbon radical and a hydrocarbon radical, wherein,the second fluorocarbon radical is linear, branched, or cyclic, having 2 to 12 carbon atoms in which 50 to 100% of the hydrogen atoms have been replaced by fluorine atoms; andthe hydrocarbon radical is linear, branched, or cyclic, having 2 to 14 carbon atoms.
摘要翻译：本发明涉及非最终碘化的氟化组合物。组合物，包括分散体，乳液，微乳液和凝胶可用于生物医学应用，特别是放射摄影和闪烁扫描。本发明中使用的化合物优选具有以下通式：RFCH = CIR1其中，RF是具有2至12个碳原子的直链，支链或环状的第一碳氟基，其中50至100％的氢原子已被氟原子; 并且R 1选自第二氟烃基和烃基，其中，第二氟烃基为直链，支链或环状，具有2至12个碳原子，其中50至100％的氢原子已经被被氟原子取代; 烃基是直链，支链或环状的，具有2至14个碳原子。

9. 发明授权

US5965258A Elongated microstructures from perfluoroalkylated amphiphiles 失效
标题翻译：来自全氟烷基化两亲物的细长微结构
公开(公告)号：US5965258A
公开(公告)日：1999-10-12
申请号：US214411
申请日：1994-03-16
申请人： Jean G. Riess , Francoise Giulieri , Marie-Pierre Krafft , Leila Zarif
发明人： Jean G. Riess , Francoise Giulieri , Marie-Pierre Krafft , Leila Zarif
IPC分类号： A61K9/127 , B01J13/02 , B32B1/00 , A61K9/00 , B01J13/00
CPC分类号： B01J13/02 , A61K9/1274 , Y10S428/903 , Y10S977/70 , Y10T428/2913 , Y10T428/2924 , Y10T428/2925 , Y10T428/2975
摘要： Microstructures formed from fluorinated amphiphiles and mixed fluorinated and non-fluorinated amphiphiles and having the geometry of tubules, helixes and fibers and methods for preparing them. Tubular forms are capable of encapsulating or incorporating bioactive agents or other useful substances for controlled release in vivo.
摘要翻译：由氟化两亲物和混合氟化和非氟化两亲物形成的微结构，并具有小管，螺旋和纤维的几何形状以及用于制备它们的方法。管状形式能够在体内包封或掺入生物活性剂或其它有用物质用于控制释放。

10. 发明授权

US5733526A Hydrocarbon oil/fluorochemical preparations and methods of use 失效
标题翻译：烃油/含氟化合物制剂及使用方法
公开(公告)号：US5733526A
公开(公告)日：1998-03-31
申请号：US572859
申请日：1995-12-14
申请人： Leo A. Trevino , Jean G. Riess , Luis A. Dellamary , Marie-Pierre Krafft , Thomas E. Tarara
发明人： Leo A. Trevino , Jean G. Riess , Luis A. Dellamary , Marie-Pierre Krafft , Thomas E. Tarara
IPC分类号： A61K9/00 , A61K9/113 , A61K49/04 , A61K31/03
CPC分类号： A61K9/0026 , A61K9/113 , Y10S514/937 , Y10S977/786 , Y10S977/795 , Y10S977/902 , Y10S977/904 , Y10S977/905 , Y10S977/915 , Y10S977/926 , Y10S977/927 , Y10S977/962
摘要： Novel hydrocarbon oil/fluorochemical preparations and methods for their use are provided. The preparations, which preferably comprise a fluorophilic dispersing agent, may be in the form of hydrocarbon oil-in-fluorochemical dispersions or in the form of a multiple emulsion comprising a polar liquid continuous phase and are particularly useful for administering bioactive agents. In particular the preparations of the present invention may be used to control the bioavailability and improve the efficacy of lipophilic bioactive agents having limited solubility in an aqueous physiological environment.
摘要翻译：提供新型烃油/含氟化合物制剂及其使用方法。优选包含嗜氟分散剂的制剂可以是烃油中的含氟化合物分散体的形式或者包含极性液体连续相的多重乳液的形式，并且特别可用于施用生物活性剂。特别地，本发明的制剂可用于控制生物利用度并改善在水性生理环境中溶解度有限的亲脂性生物活性剂的功效。

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