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。

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。

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。

公开(公告)号：US06203729B1

公开(公告)日：2001-03-20

申请号：US09444477

申请日：1999-11-19

申请人： Olivier Breyne

发明人： Olivier Breyne

IPC分类号： G02B523

CPC分类号： C07D491/04 ,  C08K5/0041 ,  G02B5/23

摘要： Disclosed are naphthopyran-type compounds having a pyrrole group annelated in position 5.6, as well as compositions and particularly (co)polymer matrices containing them. These compounds, compositions, and matrices have photochromic properties. These [pyrrole]naphthopyran compounds have the general formula: Articles containing these photochromic compounds, such as ophthalmic and/or solar glasses, lenses, glazing, devices, and the like, are also disclosed.

摘要翻译： 公开了具有在位置5.6被取代的吡咯基团的萘并吡喃型化合物以及含有它们的组合物和特别是（共）聚合物基质）。 这些化合物，组合物和基质具有光致变色性质。 这些[吡咯]萘并吡喃化合物具有以下通式：还公开了含有这些光致变色化合物的制品，如眼科和/或太阳眼镜，透镜，玻璃，装置等。

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：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。

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。

公开(公告)号：US06392043B1

公开(公告)日：2002-05-21

申请号：US09530554

申请日：2000-08-24

申请人： Konstantine Bourchteine ,  Olivier Breyne

发明人： Konstantine Bourchteine ,  Olivier Breyne

IPC分类号： C07D49122

CPC分类号： C07D491/04 ,  C07D311/78 ,  C08G73/0672 ,  G02B5/23

摘要： The object of the present invention is novel photochromic [indole]naphthopyran compounds and their methods of preparation.

摘要翻译： 本发明的目的是新型光致变色[吲哚]萘并吡喃化合物及其制备方法。

公开(公告)号：US06379591B1

公开(公告)日：2002-04-30

申请号：US09590405

申请日：2000-06-08

申请人： Olivier Breyne

发明人： Olivier Breyne

IPC分类号： G02B523

CPC分类号： C07D491/04 ,  C07D221/18 ,  G02B5/23

摘要： The invention relates to novel naphthopyran-type compounds having a lactam-type 6-membered ring annelated in position C5-C6. 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： 本发明涉及具有在C5-C6位置被取代的内酰胺型6元环的新型萘并吡喃型化合物。 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。

公开(公告)号：US08481019B2

公开(公告)日：2013-07-09

申请号：US12149552

申请日：2008-05-05

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

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

IPC分类号： A61K31/74

CPC分类号： A61K9/5146 ,  A61K9/1641

摘要： The present invention relates to novel particles comprising polyelectrolyte polymers which are transporters of active principle (AP), in particular protein and peptide active principle, and to novel modified-release pharmaceutical formulations comprising said AP microparticles.These novel particles loaded with AP release the AP over a prolonged period of time of several days, or even several weeks.The invention relates, in a first aspect, to particles comprising: a) a first polyelectrolyte polymer (PE1) in a charged state, carrying side hydrophobic groups (GH), wherein said first polyelectrolyte polymer (PE1) can spontaneously form, in water, a colloidal solution of particles at least one pHm value of the pH of between 3 and 8; b) a second polyelectrolyte polymer (PE2) of opposite polarity to the first polyelectrolyte polymer (PE1), wherein said second polyelectrolyte polymer (PE2) forms, in water, a solution or a colloidal solution at said pHm value of the pH; and c) at least one active principle (AP) associated noncovalently with the particles of the colloidal solution of the first polyelectrolyte polymer (PE1); wherein said particles are obtained by mixing, at a pH equal to pHm, the first polyelectrolyte polymer (PE1), in the form of a colloidal solution of particles associated with the active principle (AP), with the second polyelectrolyte polymer (PE2), in the form of a solution or colloidal solution. The invention also relates to the process for the preparation of these particles, to a pharmaceutical formulation comprising such particles and to a process for the preparation of medicaments.