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    • 5. 发明申请
    • NANOPARTICLES BASED ON A GAG AND A SQUALENE
    • 基于GAG和SQUALENE的纳米颗粒
    • WO2014091436A1
    • 2014-06-19
    • PCT/IB2013/060842
    • 2013-12-12
    • CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEUNIVERSITE PARIS-SUD 11
    • RALAY-RANAIVO, BettinaCOUVREUR, PatrickDESMAELE, DidierBIANCHINI, ElsaBORGEL, DelphineGREF, Ruxandra
    • A61K47/48A61K31/727A61P7/02
    • A61K9/19A61K9/4891A61K9/5123A61K31/727A61K45/06A61K47/541A61K47/6907
    • The present invention relates to nanoparticles comprising at least one negatively charged glycosaminoglycan-type macromolecule or a derivative thereof, non-covalently coupled to at least one molecule of a cationic hydrocarbon-based radical of squalene nature represented by the formula (I) which follows: (I) wherein: A, B, C, D, E and F are a hydrogen atom or a methyl group; Z and Y represent a radical (formula (II)), an ethyltrialkylammonium radical, an ethylguanidium radical or a 1-[ethylideneamino]guanidinium radical with the proviso that at least one of Z and Y is different from (formula (II)), the symbol * showing the position of the attachment of the radical to the structure; and n is equal to 1 or 2. The present invention also relates to a method for preparing said nanoparticles, and to a lyophilisate, a solid dosage form and pharmaceutical or dermatological compositions comprising said nanoparticles. Said nanoparticles are useful as medicines and more particularly as anticoagulant agents.
    • 本发明涉及包含至少一种带负电荷的糖胺聚糖型大分子或其衍生物的纳米颗粒,所述至少一种带负电荷的糖胺聚糖型大分子或其衍生物与由下式(I)表示的角鲨烯性质的基于阳离子烃的基团的至少一个分子非共价偶联: (I)其中:A,B,C,D,E和F是氢原子或甲基; Z和Y代表一个基团(式(II)),乙基三烷基铵基,乙基胍基或1- [亚乙基氨基]胍基,条件是Z和Y中的至少一个不同于(式(II)), 符号*表示激进组织对结构的附着位置; 并且n等于1或2.本发明还涉及制备所述纳米颗粒的方法,还涉及冻干物,固体剂型和包含所述纳米颗粒的药物或皮肤病学组合物。 所述纳米颗粒可用作药物,更特别地可用作抗凝血剂。