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11. 发明授权

US08481019B2 Modified-release particles of polyelectrolytes and pharmaceutical formulations thereof 失效
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.

12. 发明申请

US20090012028A1 Polyglutamic acids functionalized by cationic groups and hydrophobic groups and applications thereof, in particular therapeutic applications thereof 失效
标题翻译：由阳离子基团和疏水基团官能化的聚谷氨酸及其应用，特别是其治疗应用
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。

13. 发明授权

US07250120B2 Benzo-, naphtho- and phenanthrochromene substituted by carbamated or ureated phenyls, preparation thereof and compositions and articles containing them 有权
标题翻译：由氨基甲酸酯化或脲化苯基取代的苯并 - 萘并菲衍生物，其制备方法和含有它们的组合物和制品
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。

14. 发明申请

US20070010652A1 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：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。

15. 发明授权

US06506322B1 Naphthopyrans annelated in C5-C6 with an indene- or dihydronaphthalene-type carbocycle, and compositions and (co)polymer matrices containing them 有权
标题翻译： Naphthopyrans在C5-C6中用茚或二氢萘型碳环，和包含它们的组合物和（共）聚合物基质）
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。

16. 发明授权

US08236353B2 Self-precipitating pharmaceutical formulations for the modified release of an active principle 失效
标题翻译：用于改性释放活性成分的自沉淀药物制剂
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。

17. 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。

18. 发明申请

US20090011039A1 Modified-release particles of polyelectrolytes and pharmaceutical formulations thereof 失效
标题翻译：聚电解质的改性释放颗粒及其药物制剂
公开(公告)号：US20090011039A1
公开(公告)日：2009-01-08
申请号：US12149552
申请日：2008-05-05
申请人： Cecile Bonnet-Gonnet , Frederic Checot , You-Ping Chan , Olivier Breyne
发明人： Cecile Bonnet-Gonnet , Frederic Checot , You-Ping Chan , Olivier Breyne
IPC分类号： A61K47/30 , A61K9/14
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.
摘要翻译：本发明涉及包含聚电解质聚合物的新型颗粒，其为活性成分（AP）的转运体，特别是蛋白质和肽活性成分，以及包含所述AP微粒的新型改性释放药物制剂。装载AP的这些新型颗粒在几天甚至几周的较长时间内释放AP。本发明在第一方面涉及包含以下的颗粒：a）带电状态的第一聚电解质聚合物（PE1），其携带侧疏水基团（GH），其中所述第一聚电解质聚合物（PE1）可在水中自发形成，颗粒的胶体溶液，其pH值在3至8之间的至少一个pHm值; b）与第一聚电解质聚合物（PE1）相反极性的第二聚电解质聚合物（PE2），其中所述第二聚电解质聚合物（PE2）在水中以所述pHm的pH值在水中形成溶液或胶体溶液; 和c）与第一聚电解质聚合物（PE1）的胶体溶液的颗粒非共价结合的至少一种活性成分（AP）; 其中所述颗粒是通过在等于pHm的pH下，以与活性成分（AP）相关的颗粒的胶态溶液与第二聚电解质聚合物（PE2）的形式混合第一聚电解质聚合物（PE1）而获得的，以溶液或胶体溶液的形式存在。本发明还涉及制备这些颗粒的方法，包括这种颗粒的药物制剂和制备药物的方法。

19. 发明申请

US20050092972A1 Benzo-, naphtho- and phenanthrochromene substituted by carbamated or ureated phenyls, preparation thereof and compositions and articles containing them 有权
标题翻译：由氨基甲酸酯化或脲化苯基取代的苯并 - 萘并菲衍生物，其制备方法和含有它们的组合物和制品
公开(公告)号：US20050092972A1
公开(公告)日：2005-05-05
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： C07D311/78 , C07D311/92 , C08K5/00 , C08K5/15 , C08K5/1545 , C09K9/02 , G02B5/23
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。

20. 发明授权

US06506538B1 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，其制备和组成以及含有它们的（共）聚合物基质
公开(公告)号：US06506538B1
公开(公告)日：2003-01-14
申请号：US09393213
申请日：1999-09-09
申请人： Olivier Breyne , You-Ping Chan , Patrick Jean
发明人： Olivier Breyne , You-Ping Chan , Patrick Jean
IPC分类号： C07D31194
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，例如苯并基团。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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