Lipopolyamines as transfection agents and pharamaceutical uses thereof

US6107286A · kind A · utility

Assignee

• RHONE-POULENC RORER S.A. · FR

Inventors

• Gerardo Byk · Créteil, FR
• Daniel Scherman · Paris, FR
• Catherine Dubertret · Chalon-sur-Saône, FR

Key dates

• Filing date: Jun 4, 1997
• Grant date: Aug 22, 2000
• Expiry date: Jun 4, 2017

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K48/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Cationic lipids of general formula (I), wherein m is an integer from 2 to 6 inclusive; n is an integer from 1 to 9 inclusive, preferably 1-5, where, when n is 2-9, a single R grouping other than hydrogen is present in the general formula, and m has variable or identical values within the groupings (a) or --(CH.sub.2).sub.m ; R is a hydrogen atom or a radical of general formula (II), wherein X or X.sup.1, which are the same or different, are an oxygen atom, a methylene grouping --(CH.sub.2).sub.q -- where q is 0, 1, 2 or 3, or an amino grouping --NH-- or NR.sup.1 --, where R is a C.sub.1-4 alkyl grouping; Y and Y.sup.1, which are the same or different, are a hydrogen atom or an optionally substituted C.sub.1-4 alkyl radical, and p is 0-5; and R.sub.6 is a cholesterol derivative or an alkylamino grouping --NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are, independently of each other, a straight or branched, saturated or unsaturated C.sub.12-22 aliphatic radical. Pharmaceutical compositions containing said lipids, and their uses for transfecting nucleic acids whether in vitro or in vivo in cells, are also disclosed.