Perfluorinated esters of alkanoyl L-carnitine for the preparation of cationic lipids for the intracellular delivery of pharmacologically active compounds
AssigneeSigma-Tau Industrie Farmaceutiche Riunite S.p.A.
InventorsMosè Santaniello, Lucia Critelli, Nazareno Scafetta, Maria Grazia Cima, Maria Ornella Tinti, Claudio Pisano, Andrea Pucci
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Abstract
Perfluorinated esters of alkanoyl-L-carnitine of the formula (I): are useful as cationic lipids for the intracellular delivery of pharmacologically active compounds.
Claims18
A perfluorinated ester of alkanoyl-L-carnitine of the formula (I):
- where:
- R1 is alkanoyl, linear or branched, with 2-20 carbon atoms optionally perfluorinated, in which at least 40% of the hydrogen atoms are replaced by fluorine atoms or polyfluorinated;
- R2 is perfluorinated alkyl, linear or branched, with 4-20 carbon atoms;
- and
- X is the anion of a pharmacologically acceptable acid.
A liposome containing a perfluorinated ester of alkanoyl carnitine with formula (I):
- where
- R1 is alkanoyl, linear or branched, with 2-20 carbon atoms, optionally perfluorinated in which at least 40% of the hydrogen atoms are replaced by fluorine atoms;
- R2 is polyfluorinated alkyl, linear or branched, with 4-20 carbon atoms;
- and
- X is the anion of a pharmacologically acceptable acid.
Undecanoyl-L-carnitine chloride 1,1H-2,2H-heptadecafluorodecyl ester.
Lauroyl-L-carnitine chloride, 1,1H-2,2H-tridecafluoro-octyl ester.
Lauroyl-L-carnitine chloride 1,1H-2,2H-3,3H-pentafluoropentyl ester.
Undecanoyl-L-chloride 1,1H-2,2H-nonafluorohexyl ester.
Isovaleryl-L-carnitine chloride 1,1H-2,2H-3,3H-4,4H-5,5H-6,6H nonafluoro-decyl ester.
Undecanoyl-L-carnitine chloride 1,1H-2,2H-3,3H-4,4H-5,5H-6,6H nonafluoro-decyl ester.
Dependencies are inferred from the claim text.