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    • 14. 发明申请
      US20110044930A1 COPOLYHYDROXYALKYLGLUTAMINES FUNCTIONALISED WITH HYDROPHOBIC GROUPS, AND USES THEREOF, ESPECIALLY IN THERAPEUTICS 审中-公开
    • COPOLYHYDROXYALKYLGLUTAMINES FUNCTIONALISED WITH HYDROPHOBIC GROUPS, AND USES THEREOF, ESPECIALLY IN THERAPEUTICS
    • 具有疏水性功能的共聚羟基谷氨酰胺及其用途，特别适用于治疗
    • US20110044930A1
    • 2011-02-24
    • US11883223
    • 2006-01-23
    • Rémi Soula , You-Ping Chan
    • Rémi Soula , You-Ping Chan
    • A61K31/765 , C08G69/10
    • A61K8/88 , A61K2800/57 , A61Q19/00 , C08G69/10 , C08G69/48 , C08L77/04
    • The invention relates to novel biodegradable materials which are based on modified polyamino acids and which can be used for the vectorisation of active principle(s) (AP). The invention also relates to novel pharmaceutical, cosmetic, dietary or phytosanitary compositions based on said polyamino acids. The aim of the invention is to provide a novel polymer raw material which can be used for the vectorisation of active principles and which can optimally fulfil all required specifications in said area, namely: biocompatibility, biodegradability and the ability to become easily associated with many active principles or to solubilise said principles and to release same in vivo. Said aim is achieved with novel copolyhydroxyalkylglutamines comprising glutamine units and optionally glutamate units and bearing hydrophobic groups containing between 8 and 30 carbon atoms. Said copolyhydroxyalkylglutamines are amphiphilic and can be easily and economically transformed into particles for the vectorisation of active principles, whereby said particles can form stable aqueous colloidal suspensions.
    • 本发明涉及基于改性聚氨基酸并且可用于向量化活性成分（AP）的新型可生物降解材料。 本发明还涉及基于所述多氨基酸的新型药物，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颖的聚合物原料，其可用于活性成分的向量化，并且可以最佳地满足所述区域中的所有要求的规格，即：生物相容性，生物降解性和与许多活性成分容易相关的能力 原则或溶解所述原理并在体内释放它们。 所述目的通过包含谷氨酰胺单元和任选的谷氨酸单元的新型共聚羟烷基谷氨酰胺来实现，并带有含有8至30个碳原子的疏水基团。 所述共聚羟烷基谷氨酰胺是两亲性的，并且可以容易地和经济地转化成用于载体活​​性成分的颗粒，由此所述颗粒可以形成稳定的水性胶体悬浮液。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 15. 发明授权
      US07659365B2 Telechelic homopolyamino acids functionalized with hydrophobic groups, and their applications, especially therapeutic applications 失效
    • Telechelic homopolyamino acids functionalized with hydrophobic groups, and their applications, especially therapeutic applications
    • 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
    • US07659365B2
    • 2010-02-09
    • US10574475
    • 2004-09-28
    • Rémi Soula , You-Ping Chan , Gérard Soula , Olivier Breyne
    • Rémi Soula , You-Ping Chan , Gérard Soula , Olivier Breyne
    • C07K14/00
    • A61K8/88 , A61K9/1075 , A61K9/5146 , A61K47/34 , A61K47/645 , A61Q19/00 , C08G69/10 , C08G73/028 , C08L79/02
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 16. 发明申请
      US20090011028A1 Self-precipitating pharmaceutical formulations for the moified release of an active principle 失效
    • Self-precipitating pharmaceutical formulations for the moified release of an active principle
    • 用于释放活性成分的自沉淀药物制剂
    • US20090011028A1
    • 2009-01-08
    • US12149541
    • 2008-05-05
    • Frederic Checot , Cecile Bonnet-Gonnet , You-Ping Chan , Olivier Breyne , Remi Meyrueix
    • Frederic Checot , Cecile Bonnet-Gonnet , You-Ping Chan , Olivier Breyne , Remi Meyrueix
    • A61K47/42 , A61K9/10 , A61K38/20
    • A61K9/0019 , A61K9/10 , A61K9/1641 , A61K38/02 , A61K47/645 , A61K48/00
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 17. 发明申请
      US20080102128A1 Modified-release microparticles based on amphiphilic copolymer and on active principles(s) and pharmaceutical formulations comprising them 审中-公开
    • Modified-release microparticles based on amphiphilic copolymer and on active principles(s) and pharmaceutical formulations comprising them
    • 基于两亲性共聚物的改性释放微粒和包含它们的活性成分和药物制剂
    • US20080102128A1
    • 2008-05-01
    • US11878947
    • 2007-07-27
    • Alain Constancis , You-Ping Chan
    • Alain Constancis , You-Ping Chan
    • A61K38/16 , A61K9/14 , A61P43/00 , C08G63/44
    • A61K47/42 , A61K9/0019 , A61K9/0075 , A61K9/1658 , A61K9/19 , A61K38/2013 , A61K38/212 , A61K38/27 , A61K38/28
    • The present invention relates to novel microparticles formed of amphiphilic polyamino acids which transport active principle(s), AP(s), in particular protein and peptide active principle(s), and to novel modified-release pharmaceutical formulations comprising said AP microparticles. The aim of the invention is to develop novel microparticles, charged with AP, obtained by aggregation of nanoparticles of amphiphilic polyamino acids and having improved properties, in particular in the dry solid form, with regard to their ability to be dispersed and, concerning the reconstituted suspension, its stability and its ability to be easily handled and injected. The invention relates firstly to microparticles of amphiphilic polyamino acid (PO) comprising at least one AP (associated noncovalently) which spontaneously form a colloidal suspension of nanoparticles in water, at pH 7.0, under isotonic conditions; which microparticles a. are obtained by atomization of a solution or colloidal suspension of PO comprising at least one AP, b. have a size of between 0.5 and 100 microns, c. and are dispersible in colloidal suspension. The invention also relates to the process for the preparation of these microparticles, to a liquid formulation comprising a suspension of these PO/AP microparticles, to a reconstitution process and kit for this formulation and to a dry form of this formulation.
    • 本发明涉及由两亲多聚氨基酸形成的新型微粒，其中所述两亲性聚氨基酸输送活性成分，特别是蛋白质和肽活性成分的AP，以及包含所述AP微粒的新型改性释放药物制剂。 本发明的目的是开发新的带有AP的微粒，其通过聚集两亲性聚氨基酸的纳米颗粒而获得，并且具有改进的性质，特别是以干固体形式，关于其分散能力，以及关于重构的 悬浮液，其稳定性及其易于处理和注入的能力。 本发明首先涉及在等渗条件下包含至少一种AP（非共价相关的）的自亲形成纳米颗粒在水中的胶体悬浮液（pH 7.0）的两亲性聚氨基酸（PO）的微粒; 哪个微粒a。 通过雾化包含至少一种AP的PO的溶液或胶态悬浮液获得，b。 具有0.5至100微米的尺寸，c。 并且可分散在胶体悬浮液中。 本发明还涉及制备这些微粒的方法，包括这些PO / AP微粒的悬浮液的液体制剂，用于该制剂的重构方法和试剂盒以及该制剂的干燥形式。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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