Cationic lipids for intracellular delivery of biologically...

C - Chemistry – Metallurgy – 12 – N

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C12N 15/87 (2006.01) A61K 9/127 (2006.01) A61K 47/18 (2006.01) A61K 47/24 (2006.01) A61K 47/44 (2006.01) A61K 47/48 (2006.01) A61K 48/00 (2006.01) C12N 15/88 (2006.01)

Patent

CA 2079814

Disclosed are cationic lipids capable of facilitating transport of biologically active agents into cells, including the transfection of cells by therapeutic polynucleotides, the delivery of antiviral drugs, and the introduction of immunogenic peptides. The cationic lipids, comprising an ammonium group, have general structure (I). Also disclosed are adducts of these compounds comprising additional cationic sites that enhance the transfective or transport activity. Structure-activity correlations provide for the selection of preferred compounds to be synthesized for this purpose. Compositions disclosed for use of these cationic lipids include formulations for in vitro transfection and pharmaceutical formulations for parenteral and topical administration of therapeutic agents.

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