Lipid complexes for transferring at least a therapeutically active substance, in particular a polynucleotide into a target cell and use in gene therapy

US6291423A · kind A · utility

Assignee

• TRANSGENE SA · FR

Inventors

• Rainer Bischoff
• Danis Heissler · Eckbolsheim, FR
• Abdesslame Nazih · Strasbourg, FR

Key dates

• Filing date: Feb 12, 1999
• Grant date: Sep 18, 2001
• Expiry date: Feb 12, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D295/15
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention concerns a complex comprising at least a lipid and at least a therapeutically active substance useful for transferring said substance into a target cell, characterised in that said lipid is of formula (I): in which: n.sub.1, n.sub.2, identical or different are whole numbers between 0 and 1; R.sub.1, R.sub.2, identical or different are: a) selected among the group consisting of a hydrogen atom and alkyl radicals with 1 to 6 carbon atoms optionally substituted, independently of one another, by a hydroxyl radical; or b) in one particular case for which n.sub.1 =n.sub.2 =1, R.sub.1 and R.sub.2 can form together a divalent alkylene chain of 2 to 3 carbon atoms (C.sub.2 -C.sub.3); R.sub.3, R.sub.4, identical or different are alkyl radicals of 1 to 6 carbon atoms or can together form a divalent alkylene chain of 2 to 3 carbon atoms (C.sub.2 -C.sub.3); m, p, identical or different are whole numbers between 1 and 10; R.sub.5, R.sub.6, identical or different are selected in the group consisting of radicals of formula: 1) R.sub.7 C(.dbd.O)--X-- in which: X=NH, O, S; R.sub.7 is an alkyl or alkenyl radical of 6 to 23 carbon atoms (C.sub.6 -C.sub.23), linear or branched; 2) R.sub.8…