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Lipids and complexes of cationic lipids and active substances, in particular for the transfection of cells.

机译:阳离子脂质和活性物质的脂质和复合物,特别用于细胞转染。

摘要

The invention relates to new lipid compounds of formula:paragraph lvl="0"in-line-formulaR-HN-[-(CH2)m-NR-]n-1-(CH2)m-NH-R I/in-line-formulain which: the R residues are, independently of each other, a hydrogen atom or a group of formula II: for which: R1 and R2 are, independently of each other, C6-C23 alkyl or alkenyl radicals, which are linear or branched, or radicals -C(=O)-(C6-C23) alkyl or -C(=O)-(C6-C23) alkenyl, which are linear or branched, aryl radicals, cycloalkyl radicals, fluoroalkyl radicals, polyethylene glycol groups, oxyethylene or oxymethylene groups which are optionally repeated, linear or branched, optionally substituted, p is a positive integer from 1 to 4, n is a positive integer from 1 to 6, m is a positive integer from 1 to 6 which may be different for each motif -(CH2)m, and more particularly for each motif -(CH2)m-NR- when n1, the number of R groups of formula II being between 1 and 4 said compounds being optionally in a cationic form and being combined with one or more biologically acceptable anions. It also relates to new complexes comprising at least one said cationic compound and an active substance comprising negative charges allowing the introduction of said active substances into cells. It relates in particular to new complexes, in which the active substance consists of one or more nucleic acids, useful for transfecting cells.
机译:本发明涉及下式的新脂质化合物:<式lvl =“ 0”> <在线式> R-HN-[-((CH2)m-NR-] n-1-(CH2)m-NH-式中,R 1:R残基彼此独立地是氢原子或式II的基团:其中:R 1和R 2彼此独立地为C 6 -C 23烷基或直链或支链的烯基,或直链或支链的-C(= O)-(C6-C23)烷基或-C(= O)-(C6-C23)烯基,芳基,环烷基任选地重复,直链或支链,任选地被取代的基团,氟代烷基,聚乙二醇基团,氧乙烯基或氧亚甲基,p是1至4的正整数,n是1至6的正整数,m是正整数从1至6,对于每个基序-(CH 2)m可以不同,并且更特别地对于每个基序-(CH 2)m-NR-当n> 1时,式II的R基团的数目在1至4之间,化合物可选地呈阳离子形式并结合与一种或多种生物学上可接受的阴离子。本发明还涉及包含至少一种所述阳离子化合物和包含允许将所述活性物质引入细胞的负电荷的活性物质的新的复合物。它尤其涉及新的复合物,其中活性物质由一种或多种核酸组成,可用于转染细胞。

著录项

  • 公开/公告号FR2760193B1

    专利类型

  • 公开/公告日1999-05-28

    原文格式PDF

  • 申请/专利权人 TRANSGENE SA;

    申请/专利号FR19970002420

  • 申请日1997-02-28

  • 分类号A61K47/48;

  • 国家 FR

  • 入库时间 2022-08-22 02:10:39

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