Amphiphilic nucleosidephosphate analogues

摘要

PCT No. PCT/EP93/00346 Sec. 371 Date Jan. 27, 1995 Sec. 102(e) Date Jan. 27, 1995 PCT Filed Feb. 12, 1993 PCT Pub. No. WO93/16093 PCT Pub. Date Aug. 19, 1993Amphiphilic nucleoside phosphate analogues of formula I <IMAGE> (I) wherein R1 denotes a hydroxyl or amino group or an acylated or alkylated or polyoxyethylene-substituted amino group, the acyl or alkyl group of which is straight-chained or branched, has 1 to 24 carbon atoms and up to 2 double bonds and may be substituted by an aromatic group; R2 denotes H, F, a 2-bromo vinyl group or a straight-chained or branched C1-24-alkyl group; R3 and R4 are identical or different and denote H, hydroxyl, halogen and azido; R5 denotes a nucleoside group of formula II <IMAGE> (II) wherein R6 denotes a hydroxyl or amino group or an acylated or alkalized amino group, the acyl or alkyl group of which is straight-chained or branched, contains 1 to 24 carbon atoms and up to 2 double bonds and may be substituted by an aromatic group, whilst R6 and R1 are different and one of the groups denotes acylamino or alkylamino groups having 12 to 24 carbon atoms, R1, R2, R6 and R7 are selected so that, together, they impart an amphiphilic nature to a dinucleotide phosphate analogue; and the corresponding salts of the acid forms of these compounds.