Cationic lipids
AssigneeGilead Sciences, Inc.
InventorsKuei-Ying Lin, Jason G. Lewis, Mark D. Matteucci, Richard W. Wagner
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Abstract
The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two arginine, lysine or ornithine residues linked to a lipophilic moiety. The lipids form a composition when mixed with polyanions such as nucleic acids. The compositions permit efficient transfer of polyanions into cells without significant toxicity to the cells.
Claims20
A composition comprising nucleopolymer and a lipid having the structure A ##STR19## or a salt or solvate thereof wherein each R.sup.1 is alkyl (12-22 C) or mono unsaturated alkenyl (12-22 C);
- R.sup.4 is H;
- R.sup.5 is H, CH.sub.3, CH(CH.sub.3).sub.2, CH.sub.2 CH(CH.sub.3).sub.2, CH(CH.sub.3)CH.sub.2 CH.sub.3, CH.sub.2 C.sub.6 H.sub.5, CH.sub.2 C.sub.6 H.sub.4 OH, CH.sub.2 OH, CH(OH)CH.sub.3, (CH.sub.2).sub.4 NHR.sup.4, (CH.sub.2).sub.3 NHR.sup.4 or (CH.sub.2).sub.3 NR.sup.4 C(NH)NHR.sup.4 ;
- and
- R.sup.6 is NHR.sup.4, CH.sub.2 NHR.sup.4 or NR.sup.4 C(NH)NHR.sup.4.
A compound having the structure ##STR20## or a salt or solvate thereof wherein each R.sup.1 independently is alkyl (12-22 C) or mono unsaturated alkenyl (12-22 C);
- R.sup.4 is H or a protecting group;
- R.sup.5 is H, CH.sub.3, CH(CH.sub.3).sub.2, CH.sub.2 CH(CH.sub.3).sub.2, CH(CH.sub.3)CH.sub.2 CH.sub.3, CH.sub.2 C.sub.6 H.sub.5, CH.sub.2 C.sub.6 H.sub.4 OH, CH.sub.2 OH, CH(OH)CH.sub.3, (CH.sub.2).sub.4 NHR.sup.4, (CH.sub.2).sub.3 NHR.sup.4 or (CH.sub.2).sub.3 NR.sup.4 C(NH)NHR.sup.4 ;
- and
- R.sup.6 is NHR.sup.4, CH.sub.2 NHR.sup.4 or NR.sup.4 C(NH)NHR.sup.4.
Dependencies are inferred from the claim text.