Low molecular weight cationic lipids for oligonucleotide delivery
AssigneeSirna Therapeutics, Inc.
InventorsMatthew G. Stanton, Brian W. Budzik, Gregory L. Beutner, Hongbiao Liao
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Abstract
The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
Claims7
A cationic lipid of Formula A:
- wherein:
- R1 and R2 are each methyl;
- R3 is H;
- n is 2;
- L1 is C12-C24 alkenyl;
- and
- L2 is selected from C3-C9 alkyl and C3-C9 alkenyl;
- or any pharmaceutically acceptable salt or stereoisomer thereof.
Dependencies are inferred from the claim text.