Cationic lipids

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

C12N 15/88 (2006.01) A61K 9/127 (2006.01) C07C 217/28 (2006.01) C07C 237/10 (2006.01) C07C 323/25 (2006.01)

Patent

CA 2141334

The present invention discloses cationic lipids useful for making lipid aggregates for delivery of macromolecules especially for DNA and other compounds into cells. Lipids of this invention have the following general structure: (see formula I) wherein R1 and R2 can be C1-23alkyl or alkenyl, or -CO-C1-23 alkyl or alkenyl, Z1 and Z2can be H or unbranched alkyl C1-6, q is 1 to 6, and X can be: - (CH2 n Br, (CH2)n Cl, (CH2)n F or (CH2)n I, where n=0-6; - (CH2)n NH2, where n =0-6; -NH-(CH2)m-NH2, where m =2-6; -NH-(CH2)3-NH-(CH2)4-NH2; -NH- (CH2)3-NH- (CH2 4-NH (CH2)3-NH2: (see formula II) where p is 2-5, Y is H or other groups attached by amide or alkyl amino groups; a polyamine; a reporter molecule; a polysaccharide or substituted polysaccharide;a protein; an antibody; an amine or halide reactive group; -(CH2)r-SH where r is 0-6; or -(CH2)s-S- S-(CH2)t-NH2 where s is 0-6 and t is 2-6 .

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