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1. 发明授权

US07919572B2 Polyamino acids functionalised with at least one hydrophobic group and applications thereof particularly therapeutic applications 失效
标题翻译：用至少一个疏水基团官能化的聚氨基酸及其应用特别是治疗应用
公开(公告)号：US07919572B2
公开(公告)日：2011-04-05
申请号：US10558617
申请日：2004-05-28
申请人： Stéphanie Angot , Olivier Breyne , You-Ping Chan
发明人： Stéphanie Angot , Olivier Breyne , You-Ping Chan
IPC分类号： C08G69/10 , A01N25/00 , A61K47/00
CPC分类号： A61K8/88 , A61K47/645 , A61K2800/57 , A61Q19/00 , C08G69/10 , C08G69/48
摘要： The invention relates to novel materials based on biodegradable polyamino acids, particularly useful for the vectorisation of active principals (PA). The invention further relates to novel, pharmaceutical, cosmetic, dietary or phytosanitary compositions. The invention provides novel polymeric raw material, for use in the vectorisation of PA and with an optimal match for all the requirements of the type: biocompatibility, biodegradability, stability, ability to easily associate with numerous active principals or to solubilise the same and to liberate said active principals in vivo. Said aim is achieved with polyamino acids comprising aspartic and/or glutamate units, some of which carry at least one graft, characterised in that at least one of said grafts is bonded to an aspartic or glutamate unit by means of an amino acids spacer based on Leu, and/or Ileu, and/or Val, and/or Phe and a hydrophobic group with C6-C30 is connected by an ester bond to the spacer.
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，特别适用于活性成分（PA）的向量化。本发明进一步涉及新的，药物，化妆品，膳食或植物检疫组合物。本发明提供新颖的聚合物原料，用于PA的载体化和与所有类型的所有要求的最佳匹配：生物相容性，生物可降解性，稳定性，容易与许多活性成分相关联或溶解它并释放的能力活体检者在体内表示。所述目的通过包含天冬氨酸和/或谷氨酸单体的聚氨基酸实现，其中一些氨基酸携带至少一个接枝物，其特征在于至少一个所述移植物通过氨基酸间隔基与天冬氨酸或谷氨酸单元结合，基于 Leu和/或Ileu和/或Val，和/或Phe和具有C6-C30的疏水基团通过酯键连接到间隔物上。

2. 发明授权

US07683024B2 Polyaminoacids functionalized by alpha tocopherol and uses thereof, particular for therapeutic applications 有权
标题翻译：由α-生育酚功能化的聚氨基酸及其用途，特别用于治疗应用
公开(公告)号：US07683024B2
公开(公告)日：2010-03-23
申请号：US10516733
申请日：2003-06-03
申请人： You-Ping Chan , Stéphanie Angot , Olivier Breyne
发明人： You-Ping Chan , Stéphanie Angot , Olivier Breyne
IPC分类号： C07K38/02
CPC分类号： A61K8/88 , A61K8/678 , A61K9/5146 , A61K47/34 , A61K2800/57 , A61Q19/00 , C08G69/10 , C08G69/48
摘要： The invention concerns novel biodegradable polyaminoacid materials, useful in particular for vectoring active principle(s). The invention also concerns novel pharmaceutical, cosmetic dietetic or phytosanitary compositions based on said polyaminoacids. The invention aims at providing a novel polymer raw material, capable of being used for vectoring active principles and enabling optimal fulfillment of all specified requirements: biocompatibility, biodegradability, easy and inexpensive transformation into particles vectoring active principles, the particles being themselves capable of forming colloidal suspensions, of being easily associated with numerous active principles, and of releasing said active principles in vivo. Therefor, the present invention concerns first of all amphiphilic polyaminoacids comprising aspartic acid units and/or glutamic acid units, characterized in that at least part of said units carry grafts, including at least one alpha-tocopherol motif, for example (polyglutamate or polyaspartate grafted with alpha-tocopherol of synthetic or natural origin).
摘要翻译：本发明涉及新型可生物降解的聚氨基酸材料，特别适用于向量活性成分。本发明还涉及基于所述聚氨基酸的新型药物，美容饮食或植物检疫组合物。本发明旨在提供一种新颖的聚合物原料，能够用于向导活性原理，并能够最佳地实现所有特定的要求：生物相容性，生物降解性，易于和便宜地转化成粒子的载体活性成分，颗粒本身能够形成胶体悬浮液，易于与许多活性成分相关联，并且在体内释放所述活性成分。因此，本发明涉及包含天冬氨酸单元和/或谷氨酸单元的所有两亲性聚氨基酸的首要问题，其特征在于所述单元的至少一部分携带移植物，包括至少一种α-生育酚基序，例如（聚谷氨酸或聚天冬氨酸嫁接合成或天然来源的α-生育酚）。

3. 发明授权

US07678882B2 Polyamino acids functionalized by at least one hydrophobic group and the therapeutic application thereof 失效
标题翻译：由至少一个疏水基团官能化的聚氨基酸及其治疗应用
公开(公告)号：US07678882B2
公开(公告)日：2010-03-16
申请号：US11509783
申请日：2006-08-25
申请人： Stéphanie Angot , Olivier Breyne , You-Ping Chan , Gérard Soula
发明人： Stéphanie Angot , Olivier Breyne , You-Ping Chan , Gérard Soula
IPC分类号： C07K2/00
CPC分类号： A61Q19/00 , A61K8/88 , A61K47/34 , A61K47/645 , A61K47/65 , C08G69/10 , C08G69/48
摘要： The invention relates to novel materials based on biodegradable polyamino acids that are useful for vectorizing active principle(s)(AP). The aim of the invention is to supply a new polymeric raw material that is used for vectorizing AP and optimally fulfills all requirements concerning biocompatibility, biodegradability, the ability to be easily associated with numerous active principles or solubilize the active principles and to release the active principles in vivo. Such polymers can also be readily and economically transformed into particles vectorizing active principles according to the grafting rate of the hydrophobic groups, said particles being able to form stable aqueous colloidal suspensions. The aim of the invention is achieved by the inventive amphiphile polyamino acids comprising aspartic and/or glutamic units that carry grafts which encompass at least one hydrophobic unit and are linked to the aspartic and/or glutamic units via a rotula containing two amide functions, more particularly via a spacer of the lysine or ornithine type. The amide functions ensure better stability during hydrolysis than comparable products known in prior art. The invention also relates to new pharmaceutical, cosmetic, dietetic, or phytosanitary compositions based on the inventive polyamino acids.
摘要翻译：本发明涉及可用于向量化活性成分（AP）的可生物降解的聚氨基酸的新型材料。本发明的目的是提供一种新的聚合物原料，其用于向AP进行载体化，并且最佳地满足关于生物相容性，生物可降解性，易于与许多活性成分相关联或增溶活性成分的能力的所有要求，并释放活性成分体内。这样的聚合物也可以容易地和经济地转化成根据疏水基团的接枝速率向量化活性成分的颗粒，所述颗粒能够形成稳定的水性胶态悬浮液。本发明的目的是通过包含天冬氨酸和/或谷氨酸单元的本发明的两亲性聚氨基酸实现的，所述天然氨基酸和/或谷氨酸单元携带包含至少一个疏水单元的移植物，并通过含有两个酰胺官能团的转运体与天冬氨酸和/或谷氨酸单元连接特别是通过赖氨酸或鸟氨酸类型的间隔物。酰胺功能确保在水解期间比现有技术中已知的可比产品更好的稳定性。本发明还涉及基于本发明的聚氨基酸的新的药物，化妆品，饮食或植物检疫组合物。

4. 发明申请

US20100048735A1 POLYAMINOACIDS FUNCTIONALIZED WTIH ALPHA-TOCOPHEROL, AND USES THEREOF, ESPECIALLY THERAPEUTIC USES 审中-公开
标题翻译：聚氨基甲酸酯功能性维生素A和其用途，特别是治疗用途
公开(公告)号：US20100048735A1
公开(公告)日：2010-02-25
申请号：US12581644
申请日：2009-10-19
申请人： You-Ping Chan , Stéphanie Angot , Olivier Breyne
发明人： You-Ping Chan , Stéphanie Angot , Olivier Breyne
IPC分类号： A61K47/34 , C08G73/10 , A61P43/00
CPC分类号： A61K8/88 , A61K8/678 , A61K9/5146 , A61K47/34 , A61K2800/57 , A61Q19/00 , C08G69/10 , C08G69/48
摘要： The invention concerns novel biodegradable polyaminoacid materials, useful in particular for vectoring active principles(s). The invention also concerns novel pharmaceutical, cosmetic dietetic or phytosanitary compositions based on said polyaminoacids. The invention aims at providing a novel polymer raw material, capable of being used for vectoring active principles and enabling optimal fulfillment of all specified requirements: biocompatibility, biodegradability, easy and inexpensive transformation into particles vectoring active principles, said particles being themselves capable of forming colloidal suspensions, of being easily associated with numerous active principles, and of releasing said active principles in vivo. Therefor, the present invention concerns first of all amphiphilic polyaminoacids comprising aspartic acid units and/or glutamic acid units, characterized in that at least part of said units carry grafts, including at least one alphα-tocopherol motif, for example (polyglutamate or polyaspartate grafted with alphα-tocopherol of synthetic or natural origin).
摘要翻译：本发明涉及新颖的可生物降解的聚氨基酸材料，特别适用于载体活性成分。本发明还涉及基于所述聚氨基酸的新型药物，美容饮食或植物检疫组合物。本发明旨在提供一种新颖的聚合物原料，其能够用于向量活性成分的原理并且能够最佳地实现所有特定的要求：生物相容性，生物降解性，容易且便宜的转化成粒子的载体活性成分，所述颗粒本身能够形成胶体悬浮液，易于与许多活性成分相关联，并且在体内释放所述活性成分。因此，本发明涉及包含天冬氨酸单元和/或谷氨酸单元的所有两亲性聚氨基酸的首要问题，其特征在于至少部分所述单元携带移植物，包括至少一种α-α-生育酚基序，例如（聚谷氨酸或聚天冬氨酸酯接枝合成或天然来源的α-生育酚）。

5. 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。

6. 发明申请

US20070160568A1 Polyamino acids functionalized by at least one hydrophobic group and the therapeutic application thereof 失效
标题翻译：由至少一个疏水基团官能化的聚氨基酸及其治疗应用
公开(公告)号：US20070160568A1
公开(公告)日：2007-07-12
申请号：US11509783
申请日：2006-08-25
申请人： Stephanie Angot , Olivier Breyne , You-Ping Chan , Gerard Soula
发明人： Stephanie Angot , Olivier Breyne , You-Ping Chan , Gerard Soula
IPC分类号： A61K38/16 , A61K31/785 , C07K14/47
CPC分类号： A61Q19/00 , A61K8/88 , A61K47/34 , A61K47/645 , A61K47/65 , C08G69/10 , C08G69/48
摘要： The invention relates to novel materials based on biodegradable polyamino acids that are useful for vectorizing active principle/s (AP). The aim of the invention is to supply a new polymeric raw material that is used for vectorizing AP and optimally fulfills all requirements concerning biocompatibility, biodegradability, the ability to be easily associated with numerous active principles or solubilize said active principles and to release the active principles in vivo. Said polymers can also be readily and economically transformed into particles vectorizing active principles according to the grafting rate of the hydrophobic groups, said particles being able to form stable aqueous colloidal suspensions. Said aim is achieved by the inventive amphiphile polyamino acids comprising aspartic and/or glutamic units that carry grafts which encompass at least one hydrophobic unit and are linked to the aspartic and/or glutamic units via a rotula containing two amide functions, more particularly via a spacer of the lysine or ornithine type. Said amide functions ensure better stability during hydrolysis than comparable products known in prior art. The invention also relates to new pharmaceutical, cosmetic, dietetic, or phytosanitary compositions based on the inventive polyamino acids.
摘要翻译：本发明涉及可用于向量化活性成分（AP）的可生物降解的聚氨基酸的新型材料。本发明的目的是提供一种新的聚合物原料，其用于向AP进行载体化，并且最佳地满足关于生物相容性，生物可降解性，易于与许多活性成分相关联的能力或增溶所述活性成分并释放活性成分的所有要求体内。所述聚合物也可以容易地和经济地转化成根据疏水基团的接枝速率向量化活性成分的颗粒，所述颗粒能够形成稳定的水性胶体悬浮液。所述目的通过包含天冬氨酸和/或谷氨酸单元的本发明的两亲性聚氨基酸实现，所述天然氨基酸和/或谷氨酸单元携带包含至少一个疏水单元的移植物，并且通过含有两个酰胺官能团的转运体连接到天冬氨酸和/或谷氨酸单元，赖氨酸或鸟氨酸类型的间隔物。所述酰胺功能确保在水解期间比现有技术中已知的可比产品更好的稳定性。本发明还涉及基于本发明的聚氨基酸的新的药物，化妆品，饮食或植物检疫组合物。

7. 发明授权

US06426023B1 Benzopyrans annelated in C7-C8 with an aromatic heterocycle and compositions and (CO)polymer matrices containing them 失效
标题翻译：苯并吡喃在C7-C8中与芳族杂环和含有它们的组合物和（CO）聚合物基质结合
公开(公告)号：US06426023B1
公开(公告)日：2002-07-30
申请号：US09590000
申请日：2000-06-08
申请人： Olivier Breyne , You-Ping Chan , Patrick Jean
发明人： Olivier Breyne , You-Ping Chan , Patrick Jean
IPC分类号： G02B523
CPC分类号： C07D493/04 , C07D495/04 , C08F20/10 , G02B5/23
摘要： The invention relates to novel benzopyran-type compounds having an aromatic heterocycle annelated in position 7,8 and a carbocycle annelated in position 5,6. These compounds have the formula (I) given below: These compounds (I) have interesting photochromic properties. The invention also relates to their preparation, to their applications as photochromes, as well as to the compositions and (co)polymer matrices containing them.
摘要翻译：本发明涉及新的苯并吡喃型化合物，其具有在位置7,8上被取代的芳族杂环和在5,6位上被取代的碳环。这些化合物具有下面给出的式（I）：这些化合物（I）具有有趣的光致变色性质。本发明还涉及它们作为光致变色剂的应用以及含有它们的组合物和（共）聚合物基质）的制备。

8. 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。

9. 发明申请

US20090011028A1 Self-precipitating pharmaceutical formulations for the moified release of an active principle 失效
标题翻译：用于释放活性成分的自沉淀药物制剂
公开(公告)号：US20090011028A1
公开(公告)日：2009-01-08
申请号：US12149541
申请日：2008-05-05
申请人： Frederic Checot , Cecile Bonnet-Gonnet , You-Ping Chan , Olivier Breyne , Remi Meyrueix
发明人： Frederic Checot , Cecile Bonnet-Gonnet , You-Ping Chan , Olivier Breyne , Remi Meyrueix
IPC分类号： A61K47/42 , A61K9/10 , A61K38/20
CPC分类号： A61K9/0019 , A61K9/10 , A61K9/1641 , A61K38/02 , A61K47/645 , A61K48/00
摘要： The present invention relates to novel pharmaceutical formulations for the release of an active principle (AP) over a sustained period of time of several days, or even several weeks.The invention relates, in a first aspect, to a liquid formulation comprising at least one active principle (AP) and an aqueous suspension based on colloïdal particles of a polymer (PO), wherein said formulation satisfies the following four conditions:(a) the polymer (PO) is a polyamino acid comprising glutamic residues, wherein some glutamic residues each carry a pendant cationic group (CG), said cationic groups being identical or different from one another, and other glutamic residues each carry a pendent hydrophobic group (GH), said hydrophobic groups (GH) being identical or different from one another, (b) the pHf value of the pH of said formulation is between 3.0 and 6.5; (c) at the pHf value, the polymer (PO) forms a colloïdal solution which associates spontaneously and noncovalently with the active principle (AP); (d) 1 ml of said formulation precipitates during mixing with a volume of 1 ml of a test buffer solution Tp. The invention also relates to a process for the preparation of such formulations and to a process for the preparation of medicaments including such formulations.
摘要翻译：本发明涉及用于在持续的几天甚至几周的时间内释放活性成分（AP）的新型药物制剂。本发明在第一方面涉及包含至少一种活性成分（AP）和基于聚合物（PO）的胶体颗粒的水性悬浮液的液体制剂，其中所述制剂满足以下四个条件：（a）聚合物（PO）是包含谷氨酸残基的聚氨基酸，其中一些谷氨酸残基各自携带阳离子基团（CG），所述阳离子基团彼此相同或不同，并且其它谷氨酸残基各自携带悬垂疏水基团（GH），所述疏水基团（GH）彼此相同或不同，（b）所述制剂的pH值的pHf值为3.0至6.5; （c）在pHf值下，聚合物（PO）形成一种自发和非共价结合活性成分（AP）的胶体溶液; （d）1ml所述制剂在与1ml测试缓冲溶液Tp的体积混合期间沉淀。本发明还涉及一种制备这些制剂的方法以及制备包括这些制剂的药物的方法。

10. 发明授权

US07332260B2 Naphthopyrans annelated in C5-C6, their preparation and compositions and (CO)polymer matrices containing them 有权
标题翻译： Naphthopyrans在C5-C6中，它们的制备和组成以及含有它们的（CO）聚合物基质
公开(公告)号：US07332260B2
公开(公告)日：2008-02-19
申请号：US10196114
申请日：2002-07-16
申请人： Olivier Breyne , You-Ping Chan , Patrick Jean
发明人： Olivier Breyne , You-Ping Chan , Patrick Jean
IPC分类号： G11B7/24 , C07D311/78 , C07D311/94
CPC分类号： C07D311/92 , C07D311/78 , C07D311/94 , C07D409/04 , G02B5/23 , Y10S430/146
摘要： The present invention relates to novel compounds of the naphthopyran type which have an annelated carbocycle in position 5,6. These compounds are of formula (I) given below: in which A is an alicyclic ring which is optionally annelated with an aromatic ring and in which two adjacent R3 can together form at least one ring, for example a benzo group. These compounds (I) possess interesting photochromic properties. The invention also relates to the method of preparing these compounds (I), as well as their applications as photochromes and compositions and (co)polymer matrices comprising them.
摘要翻译：本发明涉及萘并吡喃类型的新化合物，其具有位置5,6上的环状碳环。这些化合物具有下面给出的式（I）：其中A是任选被芳环环化的脂环族环，其中两个相邻的R 3可以一起形成至少一个环，例如苯并基。这些化合物（I）具有有趣的光致变色性质。本发明还涉及制备这些化合物（I）的方法，以及它们作为光致变色剂和包含它们的组合物和（共））聚合物基质的应用。

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