LIPOPOLYAMINES AS TRANSFECTION AGENTS AND PHARMACEUTICAL USES THEREOF

摘要

Lipopolyamines of formula (I), wherein each of R1, R2 and R3, which are the same or different, is a hydrogen atom or a -(CH2)q-NRR' grouping, where q is independently 1, 2, 3, 4, 5 or 6 for each of the groupings R1, R2 and R3; each of m, n and p, which are the same or different, is an integer from 0 to 6; and R4 is a grouping of general formula (II), wherein each of R6 and R7, which are the same or different, is a hydrogen atom or a saturated or unsaturated C10-22 aliphatic radical, with the proviso that at least one of the two groupings is not hydrogen, u is an integer from 0 to 10, X is an oxygen or sulphur atom or an optionally monoalkylated amine grouping, Y is a carbonyl or methylene grouping, R5 is a hydrogen atom or an optionally substituted natural amino acid side chain, and r is an integer from 1 to 10, with the proviso that when r is 1, R5 is an optionally substituted natural amino acid side chain, and when r is more than 1, R5 is a hydrogen atom, are disclosed. Pharmaceutical compositions containing said lipopolyamines, and the use thereof for in vitro or in vivo nucleic acid transfection in cells, are also disclosed.