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    • 1. 发明申请
    • DEXTRAN FUNCTIONALIZED BY HYDROPHOBIC AMINO ACIDS
    • 由疏水性氨基酸功能化的地西泮
    • US20120041079A1
    • 2012-02-16
    • US13250803
    • 2011-09-30
    • Gerard SOULAOlivier SoulaRemi SoulaRichard Charvet
    • Gerard SOULAOlivier SoulaRemi SoulaRichard Charvet
    • A61K47/36C07H15/18C07H15/04C07H17/02
    • A61K31/721A61K47/36C08B37/0021
    • Dextran of the following general formula I: is described, wherein R represents a chain containing from 1 to 15 carbon atoms and having at least one acid functional group prior to attachment to AA, the chain optionally being branched and/or unsaturated and containing one or more heteroatoms, such as O, N or/and S, F represents an ester, a carbamate or an ether, AA represents a hydrophobic amino acid radical, L or D, derived from a coupling between an amine of an amino acid and at least one acid functional group of R; the amino acid, prior to attachment to R, being selected from the group consisting of tryptophan, phenylalanine, leucine, isoleucine, alanine and valine, and alcohol, amide or decarboxylated derivatives thereof, and alkaline cation salts thereof, i represents the molar fraction of substituent F—R-[AA]n per glycosidic unit and is from 0.1 to 2, n represents the molar fraction of R groups substituted by AA and is from 0.05 to 1, and wherein for R groups not substituted by AA, the acid(s) of the group R are alkaline cation carboxylates such as Na or K.
    • 描述了以下通式I的葡聚糖,其中R表示含有1至15个碳原子并且在与AA连接之前具有至少一个酸官能团的链,该链任选是支链和/或不饱和的,并且含有一个或 更多的杂原子,例如O,N或/和S,F代表酯,氨基甲酸酯或醚,AA代表疏水性氨基酸基团,L或D衍生自氨基酸的胺与至少 一个酸官能团的R; 氨基酸在与R连接之前选自色氨酸,苯丙氨酸,亮氨酸,异亮氨酸,丙氨酸和缬氨酸,以及其醇,酰胺或其脱羧基衍生物及其碱性阳离子盐,i表示 取代基F-R- [AA] n,为0.1〜2,n表示被AA取代的R基的摩尔分数,为0.05〜1,对于不被AA取代的R基,酸( 的基团R是碱性阳离子羧酸盐,例如Na或K.
    • 8. 发明申请
    • Telechelic Homopolyamino Acids Functionalized with Hydrophobic Groups, and Their Applications, Especially Therapeutic Applications
    • 用疏水基团功能化的远端肝氨基酸及其应用,特别是治疗应用
    • US20070265192A1
    • 2007-11-15
    • US10574475
    • 2004-09-28
    • Rémi SoulaYou-Ping ChanGerard SoulaOlivier Breyne
    • Rémi SoulaYou-Ping ChanGerard SoulaOlivier Breyne
    • A61K47/30A61K38/28A61P3/10C07C229/12
    • A61K8/88A61K9/1075A61K9/5146A61K47/34A61K47/645A61Q19/00C08G69/10C08G73/028C08L79/02
    • 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 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.
    • 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,其可用于AI的载体化并且以最佳方式满足所有规格:生物相容性,生物降解性,与许多活性成分容易相关的能力或 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。