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    COPOLYHYDROXYALKYLGLUTAMINES FUNCTIONALISED WITH HYDROPHOBIC GROUPS, AND USES THEREOF, ESPECIALLY IN THERAPEUTICS
    1.
    发明申请
    COPOLYHYDROXYALKYLGLUTAMINES FUNCTIONALISED WITH HYDROPHOBIC GROUPS, AND USES THEREOF, ESPECIALLY IN THERAPEUTICS 审中-公开
    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

    公开(公告)号：US20110044930A1

    公开(公告)日：2011-02-24

    申请号：US11883223

    申请日：2006-01-23

    申请人： Rémi Soula ,  You-Ping Chan

    发明人： Rémi Soula ,  You-Ping Chan

    IPC分类号： A61K31/765 ,  C08G69/10

    CPC分类号： A61K8/88 ,  A61K2800/57 ,  A61Q19/00 ,  C08G69/10 ,  C08G69/48 ,  C08L77/04

    摘要： 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.

    摘要翻译： 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。

    Telechelic homopolyamino acids functionalized with hydrophobic groups, and their applications, especially therapeutic applications
    2.
    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。

    Self-precipitating pharmaceutical formulations for the moified release of an active principle
    3.
    发明申请
    Self-precipitating pharmaceutical formulations for the moified release of an active principle 失效
    用于释放活性成分的自沉淀药物制剂

    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。

    Modified-release microparticles based on amphiphilic copolymer and on active principles(s) and pharmaceutical formulations comprising them
    4.
    发明申请
    Modified-release microparticles based on amphiphilic copolymer and on active principles(s) and pharmaceutical formulations comprising them 审中-公开
    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

    公开(公告)号：US20080102128A1

    公开(公告)日：2008-05-01

    申请号：US11878947

    申请日：2007-07-27

    申请人： Alain Constancis ,  You-Ping Chan

    发明人： Alain Constancis ,  You-Ping Chan

    IPC分类号： A61K38/16 ,  A61K9/14 ,  A61P43/00 ,  C08G63/44

    CPC分类号： A61K47/42 ,  A61K9/0019 ,  A61K9/0075 ,  A61K9/1658 ,  A61K9/19 ,  A61K38/2013 ,  A61K38/212 ,  A61K38/27 ,  A61K38/28

    摘要： 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.

    摘要翻译： 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。

    Naphthopyrans annelated in C5-C6, their preparation and compositions and (CO)polymer matrices containing them
    5.
    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。

    Photochromic spiroxazines, compositions and articles containing them
    7.
    发明授权
    Photochromic spiroxazines, compositions and articles containing them 失效
    光致变色螺噻嗪，组合物和含有它们的物品

    公开(公告)号：US06030555A

    公开(公告)日：2000-02-29

    申请号：US370

    申请日：1998-01-28

    申请人： You-Ping Chan

    发明人： You-Ping Chan

    IPC分类号： C07D265/00 ,  G02B5/23

    CPC分类号： C07D498/10 ,  C03C14/008 ,  C03C2214/17

    摘要： The invention concerns photochromic compounds having a formula (I), where R.sup.1 is a polycyclo group formed by at least one alicyclic group linked to, bridged or condensed, with at least one other aliphatic or aromatic ring. ##STR1##

    摘要翻译： PCT No.PCT / US96 / 12083 Sec。 371日期1998年1月28日 102（e）日期1998年1月28日PCT提交1996年7月22日PCT公布。 公开号WO97 / 08573 日期1997年3月6日本发明涉及具有式（I）的光致变色化合物，其中R1是通过至少一个与至少一个其它脂肪族或芳香环连接的桥连或缩合的脂环族基团形成的多环基团。

    COMPOSITION COMPRISING INTERFERON ALPHA
    8.
    发明申请
    COMPOSITION COMPRISING INTERFERON ALPHA 审中-公开
    包含干扰素的组合物

    公开(公告)号：US20120294832A1

    公开(公告)日：2012-11-22

    申请号：US13472675

    申请日：2012-05-16

    申请人： Gauthier Pouliquen ,  You-Ping Chan ,  Rémi Meyrueix ,  David Chognot ,  Roger Kravtzoff

    发明人： Gauthier Pouliquen ,  You-Ping Chan ,  Rémi Meyrueix ,  David Chognot ,  Roger Kravtzoff

    IPC分类号： A61K38/21

    CPC分类号： A61K38/212 ,  A61K9/0019 ,  A61K9/19 ,  A61K47/34

    摘要： The present invention relates to a novel solid composition, useful for treating hepatitis, in particular hepatitis C, comprising at least one interferon alpha and at least one grafted poly(glutamic acid) having an average molar mass ranging from 26,000 to 40,000 g/mol, preferably approximately 33,000 g/mol and carrying grafts of alpha-tocopherol at an average molar grafting rate ranging from 4.5 to 5.5%, preferably approximately 5%, the interferon alpha and said grafted poly(glutamic acid) being present in a grafted poly(glutamic acid)/interferon alpha weight ratio ranging from 21 to 125.It also relates to the use of such a solid composition for the preparation of a liquid composition by the addition of an aqueous liquid.

    摘要翻译： 本发明涉及一种用于治疗肝炎，特别是丙型肝炎的新型固体组合物，其包含至少一种干扰素α和至少一种平均摩尔质量范围为26,000至40,000g / mol的接枝聚（谷氨酸） 优选约33,000g / mol，并且以干扰素α和所述接枝的聚（谷氨酸）存在于接枝的聚（谷氨酸）中的平均摩尔接枝率为4.5至5.5％，优选约5％的载体接种α-生育酚 酸）/干扰素α重量比范围为21至125.还涉及使用这种固体组合物通过加入水性液体制备液体组合物。

    Branched Polyamino Acids Functionalized with Hydrophobic Groups, and Applications Thereof Particularly Therapeutic Applications
    10.
    发明申请
    Branched Polyamino Acids Functionalized with Hydrophobic Groups, and Applications Thereof Particularly Therapeutic Applications 失效
    用疏水基功能化的支链聚氨基酸及其应用特别是治疗应用

    公开(公告)号：US20090305948A1

    公开(公告)日：2009-12-10

    申请号：US11658875

    申请日：2005-07-19

    申请人： Rémi Soula ,  Gauthier Pouliquen ,  You-Ping Chan

    发明人： Rémi Soula ,  Gauthier Pouliquen ,  You-Ping Chan

    IPC分类号： A61K38/00 ,  C07K2/00 ,  A61K38/16 ,  A61K31/715 ,  A61K31/7088 ,  A61K8/64

    CPC分类号： A61K8/88 ,  A61K47/34 ,  A61K47/645 ,  A61K2800/57 ,  A61Q19/00 ,  C08G69/10 ,  C08G69/48

    摘要： The invention concerns novel materials based on biodegradable branched polyaminoacids particularly useful for transporting active principle(s). The invention also concerns novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on polyaminoacids. The invention aims at providing a novel polymeric material, capable of being used for transporting active principle(s) and enabling all the required relevant specifications to be optimally satisfied: biocompatibility, biodegradability, easy ability to be combined with a large number of active principles or to solubilize same, and to release said active principles in vivo. This is achieved by the present invention which firstly concerns branched polyaminoacids comprising aspartic acid units and or glutamic acid units, and which bear hydrophobic groups including 8 to 30 carbon atoms. Said branched polyaminoacids are amphiphilic and are capable of being easily and economically transformed into particles for transporting active principles, said particles being themselves capable of forming stable aqueous colloidal suspensions.

    摘要翻译： 本发明涉及基于可生物降解的支化聚氨基酸的新型材料，其特别适用于输送活性成分。 本发明还涉及基于聚氨基酸的新型药物，化妆品，饮食或植物检疫组合物。 本发明旨在提供一种新型的聚合物材料，其能够用于输送活性成分，并使所有所需的相关规格得到最佳的满足：生物相容性，生物降解性，易于与许多活性成分组合的能力，或 使其溶解，并在体内释放所述活性成分。 这通过本发明实现，其首先涉及包含天冬氨酸单元和/或谷氨酸单元并且具有包含8至30个碳原子的疏水基团的支链聚氨基酸。 所述支化聚氨基酸是两亲性的，并且能够容易地和经济地转化成用于输送活性成分的颗粒，所述颗粒本身能够形成稳定的水性胶体悬浮液。