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1. 发明申请

WO2011098962A2 ANIONIC POLYSACCHARIDES FUNCTIONALISED BY AT LEAST TWO HYDROPHOBIC GROUPS SUPPORTED BY AN AT LEAST TRIVALENT SPACER 审中-公开
标题翻译：由至少两个间隔层支持的至少两个疏水组功能的绝对多糖
公开(公告)号：WO2011098962A2
公开(公告)日：2011-08-18
申请号：PCT/IB2011050554
申请日：2011-02-09
申请人： ADOCIA , CHARVET RICHARD , SOULA REMI , SOULA OLIVIER
发明人： CHARVET RICHARD , SOULA REMI , SOULA OLIVIER
IPC分类号： A61K31/70 , A61K38/00 , A61K38/18 , A61K47/36 , A61K47/48 , A61P19/00 , C07K14/51 , C08B11/12 , C08B15/00 , C08B37/00 , C08B37/02
CPC分类号： A61K47/36 , C08B11/12 , C08B11/14 , C08B37/0018 , C08B37/0021 , C08B37/0045 , C08B37/0072 , C08B37/0084
摘要： The present invention relates to novel anionic polysaccharide derivatives partially functionalised by at least two vicinal hydrophobic groups, said identical or different hydrophobic groups being supported by an at least trivalent radical or spacer. The invention also relates to methods for synthesising same. The invention further relates to the use of functionalised polysaccharides according to the invention for preparing pharmaceutical compositions including one of the polysaccharides according to the invention and at least one active principle.
摘要翻译：本发明涉及由至少两个邻位疏水基团部分官能化的新型阴离子多糖衍生物，所述相同或不同的疏水基团由至少三价基团或间隔基负载。本发明还涉及其合成方法。本发明还涉及根据本发明的官能化多糖用于制备包含根据本发明的多糖和至少一种活性成分之一的药物组合物的用途。

2. 发明申请

WO2010122385A1 FAST-ACTING INSULIN FORMULATION 审中-公开
标题翻译：速效胰岛素制剂
公开(公告)号：WO2010122385A1
公开(公告)日：2010-10-28
申请号：PCT/IB2010000711
申请日：2010-03-29
申请人： ADOCIA , SOULA GERARD , SOULA OLIVIER , SOULA REMI
发明人： SOULA GERARD , SOULA OLIVIER , SOULA REMI
IPC分类号： A61K38/28 , A61K47/36 , A61K47/48 , A61P5/50
CPC分类号： A61K38/28 , A61K9/0019
摘要： The invention relates to a complex of insulin and a polysaccharide comprising carboxylic functional groups, said polysaccharide being selected from among the polysaccharides functionalized by at least one phenylalanine derivative, in particular said phenylalanine derivative being selected from the group consisting of phenylalanine and the alkaline cation salts thereof, phenylalanine, phenylalaninamide, amine ethyl benzyl or from among the esters of phenylalanine and said insulin being either a human insulin or equivalent insulin. The invention also relates to a pharmaceutical composition including at least one complex according to the invention, particularly in the form of an injectable solution.
摘要翻译：本发明涉及胰岛素和含有羧基官能团的多糖的复合物，所述多糖选自由至少一种苯丙氨酸衍生物官能化的多糖，特别是所述苯丙氨酸衍生物选自苯丙氨酸和碱性阳离子盐其苯丙氨酸，苯丙氨酸酰胺，胺乙基苄基或苯丙氨酸的酯中，并且所述胰岛素是人胰岛素或等同的胰岛素。本发明还涉及包含至少一种根据本发明的复合物的药物组合物，特别是以可注射溶液的形式。

3. 发明申请

WO2010041138A2 COMPLEX BETWEEN HUMAN INSULIN AND AN AMPHIPHILIC POLYMER, AND USE OF SAID COMPLEX FOR PREPARING A QUICK HUMAN INSULIN FORMULATION 审中-公开
标题翻译：人胰岛素和人血浆聚合物之间的复合物，以及使用复合物制备快速人胰岛素制剂
公开(公告)号：WO2010041138A2
公开(公告)日：2010-04-15
申请号：PCT/IB2009007106
申请日：2009-10-12
申请人： ADOCIA , SOULA OLIVIER , SOULA REMI , SOULA GERARD
发明人： SOULA OLIVIER , SOULA REMI , SOULA GERARD
IPC分类号： A61K47/48 , A61K31/721 , A61K38/28 , A61K47/36 , A61P3/10 , C07K14/62 , C08B37/00
CPC分类号： C08L89/00 , A61K31/721 , A61K38/28 , A61K47/61 , C08B37/0021 , C08K3/20 , C08K3/32 , C08K5/13 , C08K5/15 , C08K5/175 , C08L5/02 , A61K2300/00
摘要： The invention relates to a complex between human insulin and an amphiphilic polymer containing carboxyl functional groups, said amphiphilic polymer being selected from among the functionalised polysaccharides mostly made up of glycosidic monomers bonded by (1,6) glycosidic bonds functionalised by at least one tryptophan derivative. The invention also relates to a pharmaceutical composition including at least one complex according to the invention, said formulation capable of being in the form of an injectable solution. The invention relates, more particularly, to the use of a complex according to the invention for the preparation of a formulation of human insulin with a concentration of around 600 µM (100 UI/mL), with the onset of action being in less than 30 minutes, preferably in less than 20 minutes, and more preferably in less than 15 minutes and/or with the glycaemic nadir being in less than 120 minutes, preferably in less than 105 minutes, and more preferably in less than 90 minutes.
摘要翻译：本发明涉及人胰岛素与含有羧基官能团的两亲聚合物之间的复合物，所述两亲性聚合物选自主要由通过至少一种色氨酸衍生物官能化的（1,6）糖苷键结合的糖苷单体组成的官能化多糖中。本发明还涉及包含至少一种根据本发明的复合物的药物组合物，所述制剂能够以可注射溶液的形式存在。本发明更具体地涉及根据本发明的复合物用于制备浓度为约600μM（100 UI / mL）的人胰岛素制剂的用途，起始作用小于30 分钟，优选小于20分钟，更优选小于15分钟，和/或血糖最低点在小于120分钟内，优选小于105分钟，更优选小于90分钟。

4. 发明申请

WO2009144577A2 ANIONIC POLYAMIDE FUNCTIONALIZED BY A TRYPTOPHAN UNIT 审中-公开
标题翻译：由TRYPTOPHAN UNIT功能化的阴离子聚酰胺
公开(公告)号：WO2009144577A2
公开(公告)日：2009-12-03
申请号：PCT/IB2009005798
申请日：2009-06-01
申请人： ADOCIA , SOULA REMI
发明人： SOULA REMI
IPC分类号： C08G69/10 , A61K38/00 , A61K47/34 , A61K47/48 , A61P43/00 , C08G69/08 , C08G69/48 , C08G73/10
CPC分类号： C08G69/48 , A61K47/645 , C08G69/10
摘要： The invention relates to an anionic polyamide functionalized by at least one tryptophan unit, -Trp, said tryptophan unit being bonded to the polyamide by an amide function separated from the backbone by a linker arm L, the polyamide being a chain selected from the group consisting of the following polymers: Formulas (I), (II), (III), L being selected from the group consisting of a simple link, a -CH2- group, or a -CH2CH2- group, -Trp being a tryptophan residue, L and/or D, produced by the coupling of the amino of the tryptophan or a tryptophan derivative, selected from the group consisting of tryptophanol, tryptophanamide, and the alkaline cation salts thereof, and an acid carried by the polyamide. The present invention also relates to a pharmaceutical composition containing one of the polyamides according to the invention.
摘要翻译：本发明涉及由至少一个色氨酸单元-Trp功能化的阴离子聚酰胺，所述色氨酸单元通过由主链与连接臂L分离的酰胺官能团键合到聚酰胺上，所述聚酰胺是选自以下的链：的以下聚合物：式（I），（II），（III），L选自简单连接基团，-CH 2 - 基团或-CH 2 CH 2 - 基团，-Trp是色氨酸残基，通过色氨酸的氨基或选自色氨酸，色氨酰胺及其碱性阳离子盐的色氨酸衍生物的偶联产生的L和/或D和由聚酰胺携带的酸。本发明还涉及含有本发明的聚酰胺之一的药物组合物。

5. 发明申请

WO2008120085A3 ANGIOGENIC COMPOSITION 审中-公开
标题翻译：生物成分
公开(公告)号：WO2008120085A3
公开(公告)日：2009-09-11
申请号：PCT/IB2008000762
申请日：2008-03-31
申请人： ADOCIA , SOULA OLIVIER , SOULA GERARD , SOULA REMI , ELOY ROSY
发明人： SOULA OLIVIER , SOULA GERARD , SOULA REMI , ELOY ROSY
IPC分类号： A61K47/48 , A61K9/00 , A61K38/18 , A61P9/10
CPC分类号： A61K9/0014 , A61K38/1858 , A61K47/61
摘要： The invention relates to the use of an amphiphilic polymer for the preparation of a therapeutic composition that is intended to promote angiogenesis at the administration site thereof, comprising a complex between a polymer and a platelet-derived growth factors (PDGF), characterised in that the polymer is amphiphilic. In one embodiment of the invention, the PDGF is selected from the PDGF group and the amphiphilic polymer is selected from the group comprising amphiphilic polymers formed by a hydrophilic polymer backbone functionalised with hydrophobic substituents and hydrophilic groups having general formula (I). The invention also relates to the use of same in accordance with these claims, characterised in that the therapeutic composition takes the form of a gel, cream, solution, spray, paste, patch or bandage.
摘要翻译：本发明涉及两亲性聚合物在制备治疗组合物中的用途，所述治疗组合物旨在促进其施用部位的血管发生，其包含聚合物与血小板衍生生长因子（PDGF）之间的复合物，其特征在于，聚合物是两亲性的。在本发明的一个实施方案中，PDGF选自PDGF基团，两亲性聚合物选自由疏水取代基官能化的亲水性聚合物骨架和具有通式（I）的亲水基团形成的两亲聚合物。本发明还涉及根据权利要求的用途，其特征在于治疗组合物采取凝胶，霜剂，溶液，喷雾剂，糊剂，贴剂或绷带的形式。

6. 发明申请

WO2007051923A3 POLYGLUTAMIC ACIDS FUNCTIONALISED BY HISTIDINE DERIVATIVES AND HYDROPHOBIC GROUPS AND THE USES THEREOF IN PARTICULAR FOR THERAPEUTIC PURPOSES 审中-公开
标题翻译：西地丁衍生物和疏水基团作用的多聚谷氨酸及其用途，特别是用于治疗目的的用途
公开(公告)号：WO2007051923A3
公开(公告)日：2007-06-28
申请号：PCT/FR2006002443
申请日：2006-10-31
申请人： FLAMEL TECH SA , SOULA OLIVIER , SOULA REMI , BREYNE OLIVIER
发明人： SOULA OLIVIER , SOULA REMI , BREYNE OLIVIER
IPC分类号： C07K2/00 , A61K47/48 , C08G69/10
CPC分类号： C08G69/10 , A61K8/88 , A61K2800/57 , A61Q19/00 , C07K14/001
摘要： The invention relates to novel biodegradable materials based on modified polyomino acids and suitable, in particular, for vectoring active substance(s) (AS). Said invention also relates to novel pharmaceutical, cosmetic, dietary or plant protective compositions which are based on said polyamino acids. The aim of said invention is to provide a novel polymer raw material usable for vectoring the AS and capable to optimally meet all specification in this area: biocompatibility, biodegradability, ability to become easily associated with many active substances or to solubilise them and to release said active substances in vivo. The aim is attained by the invention which relates to novel polyglutomates modified by histidine derivatives and hydrophobic groups containing from 8 to 30 carbon atoms. Said polyglutomates modified by histidine derivatives are soluble with pH lower than 5 and are easily and economically convertible into active substance vectorisation particles which are able to form stable aqueous colloidal suspensions. On the contrary, said modified polyglutamates are insoluble in water with a physiological pH (7, 4), and thereby have to be precipitated on an injection site in the case of a subcutaneous injection.
摘要翻译：本发明涉及基于改性的多酚酸的新型生物可降解材料，并且特别适用于载体活性物质（AS）。本发明还涉及基于所述聚氨基酸的新型药物，化妆品，膳食或植物保护组合物。本发明的目的是提供一种新型聚合物原料，其可用于载体AS并能最佳地满足该领域的所有规格：生物相容性，生物降解性，易与许多活性物质结合或溶解它们并释放所述物质体内活性物质。本发明通过涉及由组氨酸衍生物和含有8至30个碳原子的疏水基团修饰的新型多聚谷氨酸盐的发明达到目的。所述由组氨酸衍生物修饰的多聚谷氨酸盐在pH低于5时是可溶的，并且容易且经济地转化为能够形成稳定的含水胶态悬浮液的活性物质载体化颗粒。相反，所述改性聚谷氨酸盐不溶于具有生理pH（7,4）的水中，因此在皮下注射的情况下必须在注射部位沉淀。

7. 发明申请

WO2006134018A3 ORAL DOSAGE FORM COMPRISING AN ANTIMISUSE SYSTEM 审中-公开
标题翻译：口服剂型包含抗体系统
公开(公告)号：WO2006134018A3
公开(公告)日：2007-03-08
申请号：PCT/EP2006062625
申请日：2006-05-24
申请人： FLAMEL TECH SA , GUIMBERTEAU FLORENCE , DARGELAS FREDERIC , SOULA GERARD , SOULA REMI
发明人： GUIMBERTEAU FLORENCE , DARGELAS FREDERIC , SOULA GERARD , SOULA REMI
IPC分类号： A61K9/51 , A61K9/62
CPC分类号： A61K9/5047 , A61K9/4825 , A61K9/5078 , A61K9/5084 , A61K33/06 , A61K33/26 , A61K33/30 , A61K45/06 , A61K2300/00
摘要： An oral solid dosage form containing one or several active principle(s) having analgesic properties, the composition of said dosage form being such that it prevents the misuse of said dosage form through the liquid extraction of the active principle(s) contained therein, using commonly available solvents. Said oral so lid dosage form containing at least one salt of at least one analgesic active principle, and an anti-misuse system comprising at least one quenching agent, said quenching agent being suitable for inducing complexation of said analgesic active principle salt when the analgesic active principle salt is improperly extracted, notably by a drug abuser, in vitro in solution from said oral solid dosage form.
摘要翻译：含有一种或多种具有镇痛特性的活性成分的口服固体剂型，所述剂型的组成使得其通过液体提取其中包含的活性成分来防止所述剂型的滥用，其使用常用的溶剂。所述含有至少一种至少一种止痛活性成分的盐的口服所述盖剂型和包含至少一种猝灭剂的防误用系统，所述猝灭剂适合于当所述止痛活性成分主要盐在体外在所述口服固体剂型的溶液中被不正确地提取，特别是由药物滥用者提取。

8. 发明申请

WO2005033181A3 TELECHELIC HOMOPOLYAMINO ACIDS FUNCTIONALIZED BY HYDROPHOBIC GROUPS AND USES, PARTICULARLY THERAPEUTIC, THEREOF 审中-公开
标题翻译：通过疏水性组合和用途进行功能化的电化学共聚酰胺酸，特别是其治疗方法
公开(公告)号：WO2005033181A3
公开(公告)日：2005-06-09
申请号：PCT/FR2004050465
申请日：2004-09-28
申请人： FLAMEL TECH SA , SOULA REMI , CHAN YOU-PING , SOULA GERARD , BREYNE OLIVIER
发明人： SOULA REMI , CHAN YOU-PING , SOULA GERARD , BREYNE OLIVIER
IPC分类号： A61K8/88 , A61K9/51 , A61K47/48 , A61Q19/00 , C08G69/10 , C08G69/48 , C08G73/02 , C08L77/04 , C08L79/02 , A61K9/20
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 phytosanitary compositions based on said homopolyamino acids. The aim of the invention is to produce a novel polymer raw material which can be used for the vectorization of AI and which meets all specifications in an optimum manner: biocompatibility, biodegradability, the ability to become easily associated with a large number of active ingredients or to solubilize them and to release said ingredients in vivo. According to the present invention, which primarily relates to linear homopolyamino acids having aspartic or glutamic units and whose extremities include hydrophobic groups having 8-30 carbon atoms. Said homopolymers are amphiphilic and anionic and can easily be transformed at low cost into particles for the vectorization of active ingredients. Said 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。本发明还涉及基于所述均聚氨基酸的新型药物，化妆品，饮食或植物检疫组合物。本发明的目的是生产一种新颖的聚合物原料，可用于AI的载体化，并以最佳方式满足所有规格：生物相容性，生物降解性，易于与大量活性成分缔合的能力或以溶解它们并在体内释放所述成分。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，其末端包括具有8-30个碳原子的疏水基团。所述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。所述颗粒可以形成稳定的水性胶体悬浮液。

9. 发明申请

WO2012153071A3 FUNCTIONALIZED POLYSACCHARIDES 审中-公开
标题翻译：功能多糖
公开(公告)号：WO2012153071A3
公开(公告)日：2013-01-24
申请号：PCT/FR2012051040
申请日：2012-05-10
申请人： ADOCIA , CHARVET RICHARD , MORA GUILHEM , SOULA REMI
发明人： CHARVET RICHARD , MORA GUILHEM , SOULA REMI
IPC分类号： C08B37/00 , A61K31/715 , A61K31/721 , A61K47/36 , C08G18/64 , C08G18/71 , C08L5/02 , C08L5/04 , C08L5/08
CPC分类号： C08B37/0021 , C08B37/0045 , C08B37/0072 , C08B37/0084 , C08G18/6484 , C08G18/711 , C08L5/02 , C08L5/04 , C08L5/08
摘要： The invention relates to an anionic polysaccharide characterized in that the same is selected from among the polysaccharides comprising carboxylic acid functions of formula (I), where the polysaccharide is selected from among the group consisting of natural, artificial, or modified dextran, alginate, hyaluronan, and galacturonan; i represents the degree of functionalization of the hydroxyls contained in each saccharide unit, where 0
摘要翻译：本发明涉及一种阴离子多糖，其特征在于其选自包含式（I）的羧酸官能团的多糖，其中多糖选自天然，人造或修饰的葡聚糖，藻酸盐，透明质酸，和半乳糖聚糖; i表示每个糖单元中包含的羟基的官能化程度，其中0≤3; j表示每个糖单元中含有的羟基的官能化程度，其中0 = j = 1和0 2-; L和Q彼此不同，并且代表任选地包含一个或多个杂原子如O，N和/和/或任选地包含一个或多个饱和的不饱和的，包含1至15个任选支链和/或不饱和的碳的链，或芳族环或杂环，F是选自氨基甲酸酯官能团，与基团Q连接的羰基，酯官能团，与基团Q连接的羰基，酰胺官能团，羰基连接到基团Q或羧酸酯官能团; Grp选自单价或二价阳离子，包含任选包含一个或多个杂原子如O，N和/和/或S的4至50个任选支链和/或不饱和碳的链，特别是在选自由任选包含一个或多个饱和，不饱和或芳族环或羧基的羧酸，醇或硫醇官能团组成的组的形式; 并且如果羧酸官能团是游离的，它是盐的形式; 并且羧酸官能团是一价或二价阳离子羧酸盐的形式。

10. 发明申请

WO2007034320A3 PDGF AMPHIPHILIC POLYMER COMPLEX 审中-公开
公开(公告)号：WO2007034320A3
公开(公告)日：2007-10-04
申请号：PCT/IB2006002666
申请日：2006-09-26
申请人： PROTEINS & PEPTIDES MAN , DUBREUCQ GUY , DAHRI-CORREIA LATIFA , CORREIA JOSE , DURACHER DAVID , SOULA REMI , SOULA OLIVIER , SOULA GERARD
发明人： DUBREUCQ GUY , DAHRI-CORREIA LATIFA , CORREIA JOSE , DURACHER DAVID , SOULA REMI , SOULA OLIVIER , SOULA GERARD
IPC分类号： A61K38/18 , A61K47/36 , A61P17/02
CPC分类号： A61K47/36 , A61K38/1858
摘要： The invention concerns novel platelet-derived growth factor (PDGF) complexes associated with amphiphilic polymers for enhancing the physical and chemical in vitro and in vivo stability of the therapeutic protein for pharmaceutical applications. The invention also concerns a method for preparing the PDGF-amphiphilic polymer complex characterized in that it consists in preparing said polymer/PDGF-BB complex in an aqueous medium and in the absence of organic solvent likely to cause denaturation of the protein and the use of said PDGF-amphiphilic polymer complex for preparing a therapeutic wound-healing composition for topically treating ulcers.
摘要翻译：本发明涉及与两亲聚合物相关的新型血小板衍生生长因子（PDGF）复合物，用于增强用于药物应用的治疗性蛋白质的物理和化学体外和体内稳定性。本发明还涉及一种制备PDGF-两亲性聚合物复合物的方法，其特征在于其包括在水性介质中制备所述聚合物/ PDGF-BB复合物，并且在不存在可能引起蛋白质变性的有机溶剂的情况下以及使用所述PDGF-两亲性聚合物复合物用于制备用于局部治疗溃疡的治疗性伤口愈合组合物。

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