公开(公告)号：US20110129540A1

公开(公告)日：2011-06-02

申请号：US12955076

申请日：2010-11-29

申请人： You-Ping CHAN ,  Olivier BREYNE ,  Alain CONSTANCIS

发明人： You-Ping CHAN ,  Olivier BREYNE ,  Alain CONSTANCIS

IPC分类号： A61K9/14 ,  C08F8/12 ,  C08F8/32 ,  A61K38/00 ,  B82Y5/00

CPC分类号： C08F220/58 ,  A61K8/8152 ,  A61K9/5138 ,  A61K31/00 ,  A61K47/32 ,  A61Q19/00 ,  C08F220/30

摘要： The present invention relates to a novel family of polymers of acrylic and/or methacrylic type, comprising alpha-tocopherol grafts, capable of forming nanoparticles in an aqueous medium at a neutral pH.It also relates to the use of such nanoparticles, non-covalently combined with an active ingredient, in particular an active ingredient of low or average aqueous solubility, for conveying, solubilizing and/or increasing the aqueous solubilization of said active ingredient.

摘要翻译： 本发明涉及一种丙烯酸和/或甲基丙烯酸类型的新型聚合物系列，其包含α-生育酚接枝物，能够在中性pH下在水性介质中形成纳米颗粒。 它还涉及与活性成分非共价组合的这种纳米颗粒的使用，特别是低或平均水溶性的活性成分，用于输送，增溶和/或增加所述活性成分的水溶性增溶。

公开(公告)号：US20090012028A1

公开(公告)日：2009-01-08

申请号：US12149542

申请日：2008-05-05

申请人： You-Ping Chan ,  Cecile Bonnet-Gonnet ,  Olivier Breyne

发明人： You-Ping Chan ,  Cecile Bonnet-Gonnet ,  Olivier Breyne

IPC分类号： A61K47/36 ,  A61K31/711 ,  A61K31/7105 ,  C08G63/685

CPC分类号： C08G69/10 ,  A61K9/10 ,  A61K47/34 ,  A61K47/645 ,  C08G69/48

摘要： The present invention relates to novel biodegradable materials based on modified polyamino acids that are useful in particular in the vectorization of active principle(s) (APs). The invention is also directed to novel pharmaceutical, cosmetic, health-food or plant-protection compositions based on these polyamino acids.The aim of the invention is to provide a novel polymeric starting material which can be used for AP vectorization and which satisfy all the requirements: biocompatibility, biodegradability, ability to easily associate with or dissolve numerous active principles and to release these active principles in vivo. This goal is achieved by the present invention, which relates to novel polyglutamates modified by cationic groups, which, if they can be deprotonated, exhibit a pKa equal to or greater than 7, and by hydrophobic groups comprising from 8 to 30 carbon atoms.These polyglutamates modified by cationic groups are easily and economically converted into particles for the vectorization of active principles, these particles being themselves capable of forming stable aqueous colloidal suspensions. These modified polyglutamates exhibit the advantage of being less viscous than other analogous polymers while retaining an ability to associate proteins, such as insulin. Some are soluble in water at acidic pH and become insoluble at physiological pH (7.4) and should thus, during subcutaneous injection, precipitate on the site of 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，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，保健食品或植物保护组合物。 本发明的目的是提供一种新颖的聚合起始材料，其可用于AP向量化，并且其满足所有要求：生物相容性，生物降解性，容易地与许多活性成分缔合或溶解的能力，并在体内释放这些活性成分。 该目的通过本发明来实现，本发明涉及由阳离子基团修饰的新的聚谷氨酸，如果它们可以去质子化，表现出等于或大于7的pKa，以及含有8至30个碳原子的疏水基团。 通过阳离子基团改性的这些聚谷氨酸可容易且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。 这些改性的聚谷氨酸显示出比其它类似聚合物粘稠度较低的优点，同时保留了使蛋白质如胰岛素相关联的能力。 一些在酸性pH下溶于水，在生理pH（7.4）下变得不溶，因此皮下注射时，在注射部位沉淀。

公开(公告)号：US07250120B2

公开(公告)日：2007-07-31

申请号：US10867201

申请日：2004-06-14

申请人： You-Ping Chan ,  Olivier Breyne

发明人： You-Ping Chan ,  Olivier Breyne

IPC分类号： G02B5/23 ,  C07D311/60 ,  C07D311/78 ,  C07D311/92

CPC分类号： C07D311/78 ,  C07D311/92 ,  C08K5/1545 ,  C09K9/02 ,  C09K2211/1088

摘要： Disclosed are novel benzo-, naphtho- and phenanthrochromenes substituted by carbamated or ureated phenyls having the following general formula (I): wherein R1 represents a group their preparation, photochromic compositions and articles containing them. This family of compounds have interesting and useful photochromic properties, especially in terms of absorption band and discoloration speed.

摘要翻译： 公开了由具有以下通式（I）的氨基甲酰化或脲化苯基取代的新型苯并，萘并菲和菲并苯系：其中R 1表示其制备物，光致变色组合物和含有它们的制品。 该化合物族具有有趣和有用的光致变色性质，特别是在吸收带和变色速度方面。

公开(公告)号：US20070010652A1

公开(公告)日：2007-01-11

申请号：US10558617

申请日：2004-05-28

申请人： Stephanie Angot ,  Olivier Breyne ,  You-Ping Chan

发明人： Stephanie Angot ,  Olivier Breyne ,  You-Ping Chan

IPC分类号： C08G69/10

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 based on said polyamino acids. The aim of the invention is to provide a 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. Said specific amino acid spacers guarantee an improved stability to hydrolysis and a higher association quotient with proteins when compared with conventional analogous products. Said polymers have the advantage of easily and economically being transformed into vectorisation particles for active principals said particles being themselves able to form 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，特别适用于活性成分（PA）的向量化。 本发明进一步涉及基于所述聚氨基酸的新型药物，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型的聚合物原料，用于PA的向量化，并具有与以下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的能力或 溶解相同并在体内释放所述活性成分。 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。 当与常规类似产物相比时，所述特异性氨基酸间隔物保证了水解的稳定性提高和与蛋白质的较高缔合商。 所述聚合物具有容易且经济地转化成用于活性原料的载体化颗粒的优点，所述颗粒本身能够形成稳定的水性胶体悬浮液。

公开(公告)号：US06506322B1

公开(公告)日：2003-01-14

申请号：US09712058

申请日：2000-11-14

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： C07D311/92 ,  C07D311/78 ,  C07D311/94

摘要： The present invention relates to novel naphthopyran-type compounds, annelated in position C5-C6 by an indene- or dihydronaphthalene-type carbocycle, which are of the formulae (I) and (II) given below: These compounds (I) and (II) 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： 本发明涉及由下式给出的式（I）和（II）的茚或二氢萘型碳环在C5-C6位置上取代的新型萘并吡喃型化合物：这些化合物（I）和（II ）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。

公开(公告)号：US08236353B2

公开(公告)日：2012-08-07

申请号：US12149541

申请日：2008-05-05

申请人： Frédéric Checot ,  Cecile Bonnet-Gonnet ,  You-Ping Chan ,  Olivier Breyne ,  Remi Meyrueix

发明人： Frédéric Checot ,  Cecile Bonnet-Gonnet ,  You-Ping Chan ,  Olivier Breyne ,  Remi Meyrueix

IPC分类号： A61K9/14 ,  A61K9/64 ,  A61K9/58 ,  A61K38/00 ,  A61K9/52

CPC分类号： A61K9/0019 ,  A61K9/10 ,  A61K9/1641 ,  A61K38/02 ,  A61K47/645 ,  A61K48/00

摘要： The present invention relates to pharmaceutical formulations for the release of an active principle (AP) over a sustained period of time. The invention relates to a liquid formulation comprising at least one active principle (AP) and an aqueous suspension based on colloidal particles of a polymer (PO), wherein said formulation satisfies the following four conditions: (a) the PO is a polyamino acid comprising glutamic residues, wherein some glutamic residues each carry a pendant cationic group (CG), said CG being identical or different from one another, and other glutamic residues each carry a pendent hydrophobic group (GH), said 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 PO forms a colloidal solution which associates spontaneously and noncovalently with the AP; (d) 1 ml of said formulation precipitates during mixing with a volume of 1 ml of a test buffer solution Tp.

摘要翻译： 本发明涉及用于在持续时间内释放活性成分（AP）的药物制剂。 本发明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）PO是聚氨基酸，其包含 谷氨酸残基，其中一些谷氨酸残基各自携带阳离子基团（CG），所述CG彼此相同或不同，其他谷氨酸残基各自携带悬垂疏水基团（GH），所述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，PO形成胶体溶液，其与AP自发地和非共价结合; （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。

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。

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）。

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。

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）。