Use of a cationic amphipathic compound as a transfection agent, vaccine additive or drug

摘要

Cationic amphipathic cpds of formula (I) for use as a medicament, are new. A = a single bond, NHR', or NHCOR'; R' = 1-22C opt. substd., opt. unsatd. aliphatic group which is opt. interrupted by O, N, and/or S, and/or by one or more carbocyclic or heterocyclic, opt. unsatd. or aromatic, gps.; R1, R2, R3 = higher alkyl or acyl; R7, R8, R9 = (CH2)n; n = 1-6; R4, R5, R6 = H or opt. substd. 1-22C alkyl, alkenyl, alkynyl, or acyl, all opt. interrupted by O, N, and/or S, or by one or more carbocyclic or heterocyclic, satd, unsatd, or aromatic groups; or at least two of R4, R5 and R6 together with the attached N atom may form quinuclidino, piperidino, pyrrolidino, or morpholino; and X = a non-toxic anion, esp. bromide. Also claimed are: (1) compsns in which (I) is associated with a neutral lipid, esp. di-oleoyl phosphatidyl ethanolamine, in the molar ratio 1:9 - 9:1, optionally as aqueous or lyophilised liposomes; and (2) a method of transfecting eucaryote cells by mixing a transfection agent with at least one plasmid or polynucleotide and contacting with the cells to be transfected.