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1.发明申请公开(公告)号：US20090011028A1
公开(公告)日：2009-01-08
申请号：US12149541
申请日：2008-05-05
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。
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2.发明授权公开(公告)号：US08716217B2
公开(公告)日：2014-05-06
申请号：US12149542
申请日：2008-05-05
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。
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公开(公告)号：US08481019B2
公开(公告)日：2013-07-09
申请号：US12149552
申请日：2008-05-05
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.
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4.发明申请公开(公告)号：US20090012028A1
公开(公告)日：2009-01-08
申请号：US12149542
申请日：2008-05-05
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。
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5.发明授权公开(公告)号：US08236353B2
公开(公告)日：2012-08-07
申请号：US12149541
申请日：2008-05-05
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。
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6.发明申请公开(公告)号：US20090011039A1
公开(公告)日：2009-01-08
申请号：US12149552
申请日：2008-05-05
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。
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7.发明授权Telechelic homopolyamino acids functionalized with hydrophobic groups, and their applications, especially therapeutic applications 失效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。
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8.发明授权Naphthopyrans annelated in C5-C6, their preparation and compositions and (CO)polymer matrices containing them 有权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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公开(公告)号：US20100178337A1
公开(公告)日：2010-07-15
申请号：US12641773
申请日：2009-12-18
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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10.发明申请Polyamino acids functionalized by at least one hydrophobic group and the therapeutic application thereof 失效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
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。
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