公开(公告)号：US08293255B2

公开(公告)日：2012-10-23

申请号：US12084368

申请日：2006-10-31

申请人： Olivier Soula ,  Rémi Soula ,  Olivier Breyne

发明人： Olivier Soula ,  Rémi Soula ,  Olivier Breyne

IPC分类号： A61K9/10 ,  A61K9/16 ,  A61K9/00 ,  A61K47/32 ,  A61K47/00

CPC分类号： C08G69/10 ,  A61K8/88 ,  A61K2800/57 ,  A61Q19/00 ,  C07K14/001

摘要： The invention relates to novel biodegradable materials based on modified polyamino acids and suitable, in particular, for vectoring active substance(s) (AS). Said invention also relates to novel pharmaceutical, cosmetic, dietary or plant protective compositions which are based on said polyamino acids.The aim of said invention is to provide a novel polymer raw material usable for vectoring the AS and capable to optimally meet all specification in this area: biocompatibility, biodegradability, ability to become easily associated with many active substances or to solubilize them and to release said active substances in vivo. The aim is attained to 30 carbon atoms.Said polyglutamates modified by histidine derivatives are soluble with pH lower than 5 and are easily and economically convertible into active substance vectorization particles which are able to form stable aqueous colloidal suspensions. On the contrary, said modified polyglutamates are insoluble in water with a physiological pH (7.4), and thereby have to be precipitated on an injection site in the case of a subcutaneous injection.

摘要翻译： 本发明涉及基于改性聚氨基酸的新型可生物降解材料，特别适用于载体活​​性物质（AS）。 所述发明还涉及基于所述聚氨基酸的新型药物，化妆品，膳食或植物保护性组合物。 本发明的目的是提供一种可用于载体AS的新型聚合物原料，能够最佳地满足该领域的所有规格：生物相容性，生物降解性，与许多活性物质容易相关的能力或使其溶解并释放所述 体内活性物质。 目标达到30个碳原子。 由组氨酸衍生物修饰的所述聚谷氨酸可溶于pH低于5，易于经济地转化成能形成稳定的水性胶体悬浮液的活性物质载体化颗粒。 相反，所述改性的聚谷氨酸不溶于具有生理pH（7.4）的水中，因此在皮下注射的情况下必须在注射部位沉淀。

公开(公告)号：US20070265192A1

公开(公告)日：2007-11-15

申请号：US10574475

申请日：2004-09-28

申请人： Rémi Soula ,  You-Ping Chan ,  Gerard Soula ,  Olivier Breyne

发明人： Rémi Soula ,  You-Ping Chan ,  Gerard Soula ,  Olivier Breyne

IPC分类号： A61K47/30 ,  A61K38/28 ,  A61P3/10 ,  C07C229/12

CPC分类号： A61K8/88 ,  A61K9/1075 ,  A61K9/5146 ,  A61K47/34 ,  A61K47/645 ,  A61Q19/00 ,  C08G69/10 ,  C08G73/028 ,  C08L79/02

摘要： The invention relates to novel materials based on biodegradable homopolyamino acids and which can be used for the vectorization of (an) active ingredient(s) (AI). The invention also relates to novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on said homopolyamino acids. The aim of the invention is to produce a novel polymer raw material which can be used for the vectorization of AI and which meets all specifications in an optimum manner: biocompatibility, biodegradability, the ability to become easily associated with a large number of active ingredients or to solubilize them and to release said ingredients in vivo. According to the present invention, which primarily relates to linear homopolyamino acids having aspartic or glutamic units and whose extremities include hydrophobic groups having 8-30 carbon atoms. Said homopolymers are amphiphilic and anionic and can easily be transformed at low cost into particles for the vectorization of active ingredients. Said particles can form stable aqueous colloidal suspensions.

摘要翻译： 本发明涉及基于可生物降解的均聚氨基酸的新型材料，其可用于（a）活性成分（AI）的向量化。 本发明还涉及基于所述均聚氨基酸的新型药物，化妆品，饮食或植物检疫组合物。 本发明的目的是生产一种新颖的聚合物原料，其可用于AI的载体化并且以最佳方式满足所有规格：生物相容性，生物降解性，与许多活性成分容易相关的能力或 以溶解它们并在体内释放所述成分。 根据本发明，其主要涉及具有天冬氨酸或谷氨酸单元的线性均聚氨基酸，其末端包括具有8-30个碳原子的疏水基团。 所述均聚物是两亲性的和阴离子的，并且可以容易地以低成本转化成用于活性成分载体化的颗粒。 所述颗粒可以形成稳定的水性胶体悬浮液。

公开(公告)号：US20120094902A1

公开(公告)日：2012-04-19

申请号：US13287793

申请日：2011-11-02

申请人： Olivier Soula ,  Rémi Soula ,  Gerard Soula

发明人： Olivier Soula ,  Rémi Soula ,  Gerard Soula

IPC分类号： A61K38/28 ,  C07K1/107 ,  A61P3/10 ,  C07K14/62

CPC分类号： A61K38/28 ,  A61K9/0019 ,  A61K47/61

摘要： A complex between an insulin and a polysaccharide comprising carboxyl functional groups is described, the polysaccharide being chosen from polysaccharides functionalized with at least one phenylalanine derivative, noted Phe, the phenylalanine derivative being chosen from phenylalanine and its alkali metal cation salts, phenylalaninol, phenylalaninamide and ethylbenzylamine or from phenylalanine esters, and the insulin being either a human insulin or an insulin analog. A pharmaceutical composition including at least one complex, especially in the form of an injectable solution, is also described.

摘要翻译： 描述了胰岛素和包含羧基官能团的多糖之间的复合物，所述多糖选自用至少一种苯丙氨酸衍生物官能化的多糖，注意到Phe，苯丙氨酸衍生物选自苯丙氨酸及其碱金属阳离子盐，苯丙氨醇，苯丙氨酰胺和 乙基苄胺或苯丙氨酸酯，胰岛素是人胰岛素或胰岛素类似物。 还描述了包含至少一种复合物，特别是可注射溶液形式的药物组合物。

公开(公告)号：US20110044930A1

公开(公告)日：2011-02-24

申请号：US11883223

申请日：2006-01-23

申请人： Rémi Soula ,  You-Ping Chan

发明人： Rémi Soula ,  You-Ping Chan

IPC分类号： A61K31/765 ,  C08G69/10

CPC分类号： A61K8/88 ,  A61K2800/57 ,  A61Q19/00 ,  C08G69/10 ,  C08G69/48 ,  C08L77/04

摘要： The invention relates to novel biodegradable materials which are based on modified polyamino acids and which can be used for the vectorisation of active principle(s) (AP). The invention also relates to novel pharmaceutical, cosmetic, dietary or phytosanitary compositions based on said polyamino acids. The aim of the invention is to provide a novel polymer raw material which can be used for the vectorisation of active principles and which can optimally fulfil all required specifications in said area, namely: biocompatibility, biodegradability and the ability to become easily associated with many active principles or to solubilise said principles and to release same in vivo. Said aim is achieved with novel copolyhydroxyalkylglutamines comprising glutamine units and optionally glutamate units and bearing hydrophobic groups containing between 8 and 30 carbon atoms. Said copolyhydroxyalkylglutamines are amphiphilic and can be easily and economically transformed into particles for the vectorisation of active principles, whereby said particles can form stable aqueous colloidal suspensions.

摘要翻译： 本发明涉及基于改性聚氨基酸并且可用于向量化活性成分（AP）的新型可生物降解材料。 本发明还涉及基于所述多氨基酸的新型药物，化妆品，膳食或植物检疫组合物。 本发明的目的是提供一种新颖的聚合物原料，其可用于活性成分的向量化，并且可以最佳地满足所述区域中的所有要求的规格，即：生物相容性，生物降解性和与许多活性成分容易相关的能力 原则或溶解所述原理并在体内释放它们。 所述目的通过包含谷氨酰胺单元和任选的谷氨酸单元的新型共聚羟烷基谷氨酰胺来实现，并带有含有8至30个碳原子的疏水基团。 所述共聚羟烷基谷氨酰胺是两亲性的，并且可以容易地和经济地转化成用于载体活​​性成分的颗粒，由此所述颗粒可以形成稳定的水性胶体悬浮液。

公开(公告)号：US07659365B2

公开(公告)日：2010-02-09

申请号：US10574475

申请日：2004-09-28

申请人： Rémi Soula ,  You-Ping Chan ,  Gérard Soula ,  Olivier Breyne

发明人： Rémi Soula ,  You-Ping Chan ,  Gérard Soula ,  Olivier Breyne

IPC分类号： C07K14/00

CPC分类号： A61K8/88 ,  A61K9/1075 ,  A61K9/5146 ,  A61K47/34 ,  A61K47/645 ,  A61Q19/00 ,  C08G69/10 ,  C08G73/028 ,  C08L79/02

摘要： The invention relates to novel materials based on biodegradable homopolyamino acids and which can be used for the vectorization of (an) active ingredient(s) (AI). The invention also relates to novel pharmaceutical, cosmetic, dietetic or phytosanitaty compositions based on homopolyamino acids. The invention can produce a novel polymer raw material which can be used for the vectoiization of Al that can optimally be: biocompatible, biodegradable, capable of becoming easily associated with a large number of active ingredients or solubilizing them and releasing the active ingredients in vivo. According to the present invention, which primarily relates to linear homopolyamino acids having aspartic or glutamic units and whose attachments can include hydrophobic groups having 8-30 carbon atoms. The homopolymers are amphiphilic and anionic and can easily be transformed at low cost into particles for the vectorization of active ingredients. The particles can form stable aqueous colloidal suspensions.

摘要翻译： 本发明涉及基于可生物降解的均聚氨基酸的新型材料，其可用于（a）活性成分（AI）的向量化。 本发明还涉及基于均聚氨基酸的新型药物，化妆品，饮食或植物营养成分。 本发明可以生产出一种新型的聚合物原料，它可以用于最佳的生物相容性，生物降解性，能够容易地与大量活性成分缔合或溶解它们并在体内释放活性成分的Al的促进作用。 根据本发明，其主要涉及具有天冬氨酸或谷氨酸单元的线性均聚氨基酸，并且其连接物可以包括具有8-30个碳原子的疏水基团。 均聚物是两亲性的和阴离子的，并且可以容易地以低成本转化成用于活性成分载体化的颗粒。 颗粒可以形成稳定的水性胶体悬浮液。

公开(公告)号：US07078363B2

公开(公告)日：2006-07-18

申请号：US10380698

申请日：2001-09-17

申请人： Jerôme Claverie ,  Rémi Soula ,  Roger Spitz

发明人： Jerôme Claverie ,  Rémi Soula ,  Roger Spitz

IPC分类号： B01J31/38 ,  C08F4/72

CPC分类号： C08F10/00 ,  C07F15/006 ,  C07F15/0086 ,  C07F15/04 ,  C08F4/80 ,  C08F4/26

摘要： The invention concerns a catalyst for olefin polymerisation, of formula (I) wherein: E is an oxygen or sulphur atom; X is a phosphorus, arsenic or antimony atom; M is a nickel, palladium or platinum atom comprising a non-attributed valency; a is 1 or 2; R1, R2, R3, identical or different can be selected among hydrogen, alkyl, cycloalkyl, aryl, alkylaryl, arylalkyl radicals, the hydroxyl radical, the alkoxide radicals (with 1 to 20 carbon atoms), the groups —C(O)OR′—, —SO3Y; and Z represents a hydrocarbon radical comprising 2 to 3 carbon atoms; R represents a hydrocarbon radical of valency a, provided that at least one of the radicals Z or R bears at least an electroattractive substituent

摘要翻译： 本发明涉及式（I）的烯烃聚合催化剂，其中：E是氧或硫原子; X是磷，砷或锑原子; M是包含非归属化合价的镍，钯或铂原子; a是1或2; R 1，R 2，R 3，相同或不同可以选自氢，烷基，环烷基，芳基，烷基芳基，芳基烷基， 羟基，烷氧基（具有1至20个碳原子），基团-C（O）OR'，-SO 3 Y; Z表示碳原子数2〜3的烃基。 R表示化合价a的烃基，条件是基团Z或R中的至少一个至少带有电吸引取代基

公开(公告)号：US08895063B2

公开(公告)日：2014-11-25

申请号：US11651577

申请日：2007-01-10

申请人： Florence Guimberteau ,  Frederic Dargelas ,  Gérard Soula ,  Rémi Soula

发明人： Florence Guimberteau ,  Frederic Dargelas ,  Gérard Soula ,  Rémi Soula

IPC分类号： A61K8/20 ,  A61K9/50 ,  A61K45/06 ,  A61K33/30 ,  A61K33/26 ,  A61K33/06 ,  A61K9/48

CPC分类号： A61K9/5047 ,  A61K9/4825 ,  A61K9/5078 ,  A61K9/5084 ,  A61K33/06 ,  A61K33/26 ,  A61K33/30 ,  A61K45/06 ,  A61K2300/00

摘要： An oral solid dosage form containing one or several active principle(s) having analgesic properties, the composition of said dosage form being such that it prevents the misuse of said dosage form through the liquid extraction of the active principle(s) contained therein, using commonly available solvents.Said oral solid dosage form containing at least one salt of at least one analgesic active principle, and an anti-misuse system comprising at least one quenching agent, said quenching agent being suitable for inducing complexation of said analgesic active principle salt when the analgesic active principle salt is improperly extracted, notably by a drug abuser, in vitro in solution from said oral solid dosage form.

摘要翻译： 含有一种或多种具有止痛特性的活性成分的口服固体剂型，所述剂型的组成使得其通过液体提取其中包含的活性成分来防止所述剂型的滥用，其使用 常用的溶剂。 所述口服固体剂型含有至少一种至少一种止痛活性成分的盐，以及包含至少一种猝灭剂的抗滥用系统，所述猝灭剂适合于诱导所述止痛活性成分盐在所述止痛活性成分 在所述口服固体剂型的溶液中，盐不适当地提取，特别是药物滥用者。

公开(公告)号：US20100034886A1

公开(公告)日：2010-02-11

申请号：US12084368

申请日：2006-10-31

申请人： Olivier Soula ,  Rémi Soula ,  Olivier Breyne

发明人： Olivier Soula ,  Rémi Soula ,  Olivier Breyne

IPC分类号： A61K9/14 ,  C07K5/00 ,  A61K38/07 ,  A61K38/16 ,  A61P35/00

CPC分类号： C08G69/10 ,  A61K8/88 ,  A61K2800/57 ,  A61Q19/00 ,  C07K14/001

摘要： The invention relates to novel biodegradable materials based on modified polyamino acids and suitable, in particular, for vectoring active substance(s) (AS). Said invention also relates to novel pharmaceutical, cosmetic, dietary or plant protective compositions which are based on said polyamino acids.The aim of said invention is to provide a novel polymer raw material usable for vectoring the AS and capable to optimally meet all specification in this area: biocompatibility, biodegradability, ability to become easily associated with many active substances or to solubilise them and to release said active substances in vivo. The aim is attained to 30 carbon atoms.Said polyglutamates modified by histidine derivatives are soluble with pH lower than 5 and are easily and economically convertible into active substance vectorization particles which are able to form stable aqueous colloidal suspensions. On the contrary, said modified polyglutamates are insoluble in water with a physiological pH (7.4), and thereby have to be precipitated on an injection site in the case of a subcutaneous injection.

摘要翻译： 本发明涉及基于改性聚氨基酸的新型可生物降解材料，特别适用于载体活​​性物质（AS）。 所述发明还涉及基于所述聚氨基酸的新型药物，化妆品，膳食或植物保护性组合物。 本发明的目的是提供一种可用于载体AS的新型聚合物原料，能够最佳地满足该领域的所有规格：生物相容性，生物降解性，与许多活性物质容易相关的能力或溶解它们并释放所述 体内活性物质。 目标达到30个碳原子。 由组氨酸衍生物修饰的所述聚谷氨酸可溶于pH低于5，易于经济地转化成能形成稳定的水性胶体悬浮液的活性物质载体化颗粒。 相反，所述改性聚谷氨酸不溶于具有生理pH（7.4）的水中，因此在皮下注射的情况下必须在注射部位沉淀。

公开(公告)号：US20100137456A1

公开(公告)日：2010-06-03

申请号：US12461326

申请日：2009-08-07

申请人： Rémi Soula ,  Gérard Soula ,  Olivier Soula

发明人： Rémi Soula ,  Gérard Soula ,  Olivier Soula

IPC分类号： A61K47/36 ,  C08B37/00 ,  A61P43/00

CPC分类号： C08B37/0018 ,  A61K47/36 ,  C08B37/00 ,  C08B37/0006 ,  C08B37/0009 ,  C08B37/0021 ,  C08B37/0024 ,  C08B37/0045 ,  C08B37/0054 ,  C08B37/0057 ,  C08B37/0072 ,  C08B37/0084

摘要： The present invention relates to novel polysaccharide derivatives, predominantly comprising glycosidic bonds of (1,4), (1,3) and/or (1,2) type, functionalized by at least one tryptophan derivative. It also relates to processes for the synthesis thereof, to their uses as pharmaceutical excipient and to the pharmaceutical compositions comprising them.

摘要翻译： 本发明涉及新的多糖衍生物，主要包含由至少一种色氨酸衍生物官能化的（1,4），（1,3）和/或（1,2）型的糖苷键。 它还涉及其合成方法，其作为药物赋形剂的用途以及包含它们的药物组合物。

公开(公告)号：US20090305948A1

公开(公告)日：2009-12-10

申请号：US11658875

申请日：2005-07-19

申请人： Rémi Soula ,  Gauthier Pouliquen ,  You-Ping Chan

发明人： Rémi Soula ,  Gauthier Pouliquen ,  You-Ping Chan

IPC分类号： A61K38/00 ,  C07K2/00 ,  A61K38/16 ,  A61K31/715 ,  A61K31/7088 ,  A61K8/64

CPC分类号： A61K8/88 ,  A61K47/34 ,  A61K47/645 ,  A61K2800/57 ,  A61Q19/00 ,  C08G69/10 ,  C08G69/48

摘要： The invention concerns novel materials based on biodegradable branched polyaminoacids particularly useful for transporting active principle(s). The invention also concerns novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on polyaminoacids. The invention aims at providing a novel polymeric material, capable of being used for transporting active principle(s) and enabling all the required relevant specifications to be optimally satisfied: biocompatibility, biodegradability, easy ability to be combined with a large number of active principles or to solubilize same, and to release said active principles in vivo. This is achieved by the present invention which firstly concerns branched polyaminoacids comprising aspartic acid units and or glutamic acid units, and which bear hydrophobic groups including 8 to 30 carbon atoms. Said branched polyaminoacids are amphiphilic and are capable of being easily and economically transformed into particles for transporting active principles, said particles being themselves capable of forming stable aqueous colloidal suspensions.

摘要翻译： 本发明涉及基于可生物降解的支化聚氨基酸的新型材料，其特别适用于输送活性成分。 本发明还涉及基于聚氨基酸的新型药物，化妆品，饮食或植物检疫组合物。 本发明旨在提供一种新型的聚合物材料，其能够用于输送活性成分，并使所有所需的相关规格得到最佳的满足：生物相容性，生物降解性，易于与许多活性成分组合的能力，或 使其溶解，并在体内释放所述活性成分。 这通过本发明实现，其首先涉及包含天冬氨酸单元和/或谷氨酸单元并且具有包含8至30个碳原子的疏水基团的支链聚氨基酸。 所述支化聚氨基酸是两亲性的，并且能够容易地和经济地转化成用于输送活性成分的颗粒，所述颗粒本身能够形成稳定的水性胶体悬浮液。