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1. 发明授权

US08206744B2 Branched polyamino acids functionalized with hydrophobic groups, and applications thereof particularly therapeutic applications 失效
标题翻译：用疏水基团官能化的支链聚氨基酸，及其应用特别是治疗应用
公开(公告)号：US08206744B2
公开(公告)日：2012-06-26
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： A61K9/00 , A61K47/42 , C08G83/00
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 the 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. The branched polyaminoacids are amphiphilic and are capable of being easily and economically transformed into particles for transporting active principles, the 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，或溶解相同，并在体内释放活性成分。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。支链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，颗粒本身能够形成稳定的水性胶态悬浮液。

2. 发明申请

US20090305948A1 Branched Polyamino Acids Functionalized with Hydrophobic Groups, and Applications Thereof Particularly Therapeutic Applications 失效
标题翻译：用疏水基功能化的支链聚氨基酸及其应用特别是治疗应用
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。

3. 发明申请

US20110044930A1 COPOLYHYDROXYALKYLGLUTAMINES FUNCTIONALISED WITH HYDROPHOBIC GROUPS, AND USES THEREOF, ESPECIALLY IN THERAPEUTICS 审中-公开
标题翻译：具有疏水性功能的共聚羟基谷氨酰胺及其用途，特别适用于治疗
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。

4. 发明授权

US07659365B2 Telechelic homopolyamino acids functionalized with hydrophobic groups, and their applications, especially therapeutic applications 失效
标题翻译：用疏水基团官能化的远端电泳多聚氨基酸及其应用，特别是治疗应用
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。

5. 发明申请

US20070265192A1 Telechelic Homopolyamino Acids Functionalized with Hydrophobic Groups, and Their Applications, Especially Therapeutic Applications 失效
标题翻译：用疏水基团功能化的远端肝氨基酸及其应用，特别是治疗应用
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。

6. 发明申请

US20100098656A1 Polyamino acids functionalized by hydrophobic grafts bearing an anionic charge and applications thereof, such as therapeutic applications 审中-公开
标题翻译：由具有阴离子电荷的疏水性接枝物官能化的聚氨基酸及其应用，例如治疗应用
公开(公告)号：US20100098656A1
公开(公告)日：2010-04-22
申请号：US11658803
申请日：2005-07-25
申请人： Olivier Breyne , Gauthier Pouliquen , You-Ping Chan
发明人： Olivier Breyne , Gauthier Pouliquen , You-Ping Chan
IPC分类号： A61K38/16 , C07K2/00 , A61K38/18 , A61K38/20 , A61K38/21
CPC分类号： C08G69/10 , A61K8/88 , A61K2800/57 , A61Q19/00 , C08G69/48
摘要： The present invention relates to novel materials based on biodegradable polyamino acids that are useful especially for the vectorization of active principle(s) (AP). The invention further relates to novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on these polyamino acids. The object of the invention is to provide a novel polymer starting material that is capable of being used for the vectorization of AP and makes it possible on the one hand to achieve high polymer/AP ratios, and on the other hand optimally to satisfy all the specifications required in the case in point: biocompatibility, biodegradability, ability to associate easily with numerous active principles or to solubilize them, and ability to release these active principles in vivo. This object is achieved by the present invention, which relates first and foremost to linear polyamino acids comprising aspartic units or glutamic units and having hydrophobic grafts comprising hydrophobic groups containing from 8 to 30 carbon atoms, at least one of these hydrophobic grafts having at least one anionic charge and/or one or more mutually identical or different ionizable groups each capable of giving rise to at least one anionic charge. These polymers are amphiphilic and anionic and are capable of being converted easily and economically to particles for the vectorization of active principles, these particles themselves being capable of forming stable aqueous colloidal suspensions.
摘要翻译：本发明涉及基于可生物降解的聚氨基酸的新型材料，其特别用于活性成分（AP）的向量化。本发明还涉及基于这些聚氨基酸的新型药物，化妆品，饮食或植物检疫组合物。本发明的目的是提供一种新的聚合物起始材料，其能够用于AP的向量化，并且一方面可以实现高聚合物/ AP比率，另一方面最佳地满足所有在这种情况下需要的规格：生物相容性，生物降解能力，容易与许多活性成分缔合或溶解它们的能力以及在体内释放这些活性成分的能力。该目的通过本发明来实现，本发明首先涉及包含天冬氨酸单元或谷氨酸单元并具有包含含有8至30个碳原子的疏水基团的疏水性接枝的线性聚氨基酸，这些疏水性移植物中的至少一种具有至少一个阴离子电荷和/或一个或多个相互相同或不同的可离子化基团，每个基团能够产生至少一种阴离子电荷。这些聚合物是两亲性和阴离子性的，并且能够容易地和经济地转化成用于活性成分载体化的颗粒，这些颗粒本身能够形成稳定的水性胶态悬浮液。

7. 发明授权

US10052289B2 Composition comprising an active agent with low aqueous solubility 有权
公开(公告)号：US10052289B2
公开(公告)日：2018-08-21
申请号：US12641773
申请日：2009-12-18
申请人： Rémi Meyrueix , Rafael Jorda , Gauthier Pouliquen , You-Ping Chan , Olivier Breyne
发明人： Rémi Meyrueix , Rafael Jorda , Gauthier Pouliquen , You-Ping Chan , Olivier Breyne
IPC分类号： A61K9/52 , A61K9/14 , A61K9/22 , A61K31/337 , A61K31/403 , A61K31/366 , A61K31/4418 , A61K31/496 , A61K38/13 , A61P35/00 , A61P37/00 , A61P31/10 , A61P9/12 , A61P3/06 , A61K9/50 , A61K9/51 , A61K47/34
CPC分类号： A61K9/5078 , A61K9/5015 , A61K9/5026 , A61K9/5146 , A61K47/34
摘要： The present invention relates to a composition comprising at least one active ingredient with low aqueous solubility, said active ingredient being present therein in a form noncovalently associated with nanoparticles formed by at least one POM polymer of formula (I), and in which said active ingredient is present in a proportion of at least 5 μmol/g of POM.It is also directed towards the use of such nanoparticles, noncovalently associated with an active ingredient, with a view to increasing the aqueous solubilization of said active ingredient.

8. 发明授权

US09272020B2 IFN-beta compositions, preparation methods and uses thereof 有权
标题翻译： IFN-β组合物，其制备方法和用途
公开(公告)号：US09272020B2
公开(公告)日：2016-03-01
申请号：US14118757
申请日：2012-05-16
申请人： Daniel Leblanc , Evert Nicolaas Lamme , Helen Gabriela Baldascini , Joel Richard , Frederic Checot , You-Ping Chan , Roger Kravtzoff , Gauthier Pouliquen
发明人： Daniel Leblanc , Evert Nicolaas Lamme , Helen Gabriela Baldascini , Joel Richard , Frederic Checot , You-Ping Chan , Roger Kravtzoff , Gauthier Pouliquen
IPC分类号： A61K38/21 , A61K9/00 , A61K47/34 , A61K47/36 , A61K9/20 , A61K9/19 , A61K47/42
CPC分类号： A61K38/215 , A61K9/0019 , A61K9/19 , A61K9/2018 , A61K47/34 , A61K47/42
摘要： The present invention pertains to interferon-beta (IFN-beta) compositions comprising interferon-beta and a grafted poly(glutamic acid) polymer having an average molecular weight between 26,000 and 40,000 g/mol, grafted with alpha-tocopherol substituents, the average molar grafting ratio being 4.5-5.5 moles %, the weight/weight ratio between said grafted poly(glutamic acid) polymer and IFN-beta being between 24 and 125. The present invention also pertains to the preparation methods of such compositions and their application to obtain therapeutic compositions in dosage unit form delivering IFN-beta over an extended period of time.
摘要翻译：本发明涉及包含干扰素-β和平均分子量为26,000至40,000g / mol的接枝聚（谷氨酸）聚合物的干扰素-β（IFN-β）组合物，用α-生育酚取代基接枝，平均摩尔接枝率为4.5-5.5摩尔％，所述接枝的聚（谷氨酸）聚合物与IFN-β之间的重量/重量比为24至125.本发明还涉及这些组合物的制备方法及其应用以获得剂量单位的治疗组合物在长时间内形成IFN-β。

9. 发明申请

US20120294832A1 COMPOSITION COMPRISING INTERFERON ALPHA 审中-公开
标题翻译：包含干扰素的组合物
公开(公告)号：US20120294832A1
公开(公告)日：2012-11-22
申请号：US13472675
申请日：2012-05-16
申请人： Gauthier Pouliquen , You-Ping Chan , Rémi Meyrueix , David Chognot , Roger Kravtzoff
发明人： Gauthier Pouliquen , You-Ping Chan , Rémi Meyrueix , David Chognot , Roger Kravtzoff
IPC分类号： A61K38/21
CPC分类号： A61K38/212 , A61K9/0019 , A61K9/19 , A61K47/34
摘要： The present invention relates to a novel solid composition, useful for treating hepatitis, in particular hepatitis C, comprising at least one interferon alpha and at least one grafted poly(glutamic acid) having an average molar mass ranging from 26,000 to 40,000 g/mol, preferably approximately 33,000 g/mol and carrying grafts of alpha-tocopherol at an average molar grafting rate ranging from 4.5 to 5.5%, preferably approximately 5%, the interferon alpha and said grafted poly(glutamic acid) being present in a grafted poly(glutamic acid)/interferon alpha weight ratio ranging from 21 to 125.It also relates to the use of such a solid composition for the preparation of a liquid composition by the addition of an aqueous liquid.
摘要翻译：本发明涉及一种用于治疗肝炎，特别是丙型肝炎的新型固体组合物，其包含至少一种干扰素α和至少一种平均摩尔质量范围为26,000至40,000g / mol的接枝聚（谷氨酸）优选约33,000g / mol，并且以干扰素α和所述接枝的聚（谷氨酸）存在于接枝的聚（谷氨酸）中的平均摩尔接枝率为4.5至5.5％，优选约5％的载体接种α-生育酚酸）/干扰素α重量比范围为21至125.还涉及使用这种固体组合物通过加入水性液体制备液体组合物。

10. 发明申请

US20100178337A1 Composition comprising an active agent with low aqueous solubility 审中-公开
标题翻译：组合物，其含有低溶解度的活性剂
公开(公告)号：US20100178337A1
公开(公告)日：2010-07-15
申请号：US12641773
申请日：2009-12-18
申请人： Rémi MEYRUEIX , Rafael Jorda , Gauthier Pouliquen , You-Ping Chan , Olivier Breyne
发明人： Rémi MEYRUEIX , Rafael Jorda , Gauthier Pouliquen , You-Ping Chan , Olivier Breyne
IPC分类号： A61K9/52 , A61K9/14 , A61K9/22 , A61K31/337 , A61K31/403 , A61K31/366 , A61K31/4418 , A61K31/496 , A61K38/13 , A61P35/00 , A61P37/00 , A61P31/10 , A61P9/12 , A61P3/06
CPC分类号： A61K9/5078 , A61K9/5015 , A61K9/5026 , A61K9/5146 , A61K47/34
摘要： The present invention relates to a composition comprising at least one active ingredient with low aqueous solubility, said active ingredient being present therein in a form noncovalently associated with nanoparticles formed by at least one POM polymer of formula (I), and in which said active ingredient is present in a proportion of at least 5 μmol/g of POM.It is also directed towards the use of such nanoparticles, noncovalently associated with an active ingredient, with a view to increasing the aqueous solubilization of said active ingredient.
摘要翻译：本发明涉及包含至少一种具有低溶解度的活性成分的组合物，所述活性成分以与式（I）的至少一种POM聚合物形成的纳米颗粒非共价结合的形式存在，其中所述活性成分以至少5μmol/ g的POM的比例存在。还涉及使用与活性成分非共价结合的这种纳米颗粒，以增加所述活性成分的水溶性。

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