US 7,915,450 B2 · Transfection reagents

Abstract

Disclosed are cationic lipid compounds and compositions of lipid aggregates for delivery of macromolecules and other compounds into cells. The compounds can be used alone or in combination with other compounds lo prepare liposomes and other lipid aggregates suitable for iransfcclion or delivery of compounds to target cells, cither in vitro or in vivo. The compounds are preferably polycationic and preferably form highly stable complexes with various anionic macromolecules. particularly polyanions such as nucleic acids. These compounds have the properly, when dispersed in water, of forming lipid aggregates which associate strongly, via their cationic portion, with polyanions. Also disclosed are intermediates for preparing the compound and compositions of the invention and methods of using the compounds to introduce other compounds into cells.

Claims19

Dependent claims

A compound or polycation having the formula:

wherein
m, n, q, r, s, u, and y are 1;
v and w are 0;
Q is N;
L is (CH2)1, where 1 is an integer from 1 to 4;
R1 and R4 are H;
R2, R3, R5 and R6, independently of one another, are H, or an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an amino alcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkyltio, a urea, a thiourea, a guanidyl, and a carbamoyl group;
at least one of R3 and R6 is a straight-chain alkyl group;
and R3 and R6 are covalently linked with each other to form a cyclic moiety;
X is a physiologically acceptable anion;
and
a is the number of positive charges divided by the valence of the anion.

9 more elements

Dependencies are inferred from the claim text.

Transfection reagents

Life of this patent

Transfection reagents

Life of this patent

Abstract

Claims19