Patent ID: 6153594
Filing Date: 2000-11-28
Classification: A61P,C07H

Abstract:
A monoester compound of formula I:Nu--O--Fawherein O is oxygen, Nu is a nucleoside analogue, Fa is an acyl group of a mono-unsaturated C18 or C20 .omega.-9 fatty acid, which fatty acid is esterified with a hydroxyl group in the 5'-position of the sugar moiety of the nucleoside analogue or with a terminal hydroxyl group on the non-cyclic group of the nucleoside analogue, and wherein Nu is represented by the formula II:B--Swherein S is either a mono-saccharide-derivative selected from: 1-.beta.-D-ribofuranose, 1-.beta.-D-arabinofuranose, 2-deoxy-1-.beta.-D-ribofuranose, 2,3-dideoxy-1-.beta.-D-ribofuranose, 2,3-didehydro-2,3-dideoxy-1-.beta.-D-ribofuranose, 2-deoxy-2-fluoro-1-.beta.-D-arabinofuranose, 2,2-dideoxy-3-azido-1-.beta.-D-ribofuranose or 4-hydroxymethyl-2-cyclopenten-1-yl, or selected from the group of 2-hydroxy-ethoxy-methyl, 4-hydroxy-3-(hydroxymethyl-butyl, 2-hydroxyl-1-(hydroxymethyl)-ethoxy-methyl, 2,3-dihydroxy-propoxy or 2,3-dihydroxy-propyl; and B is a heterocyclic ring system selected from the following formulas: ##STR10## wherein X=O, S, NH and R.sub.1 =NH.sub.2, CH.sub.3, CH.sub.3 O and A=NH, S, Se, CH.sub.2, O,or ##STR11## wherein X=NH, S, O and Y=H, OH, F, Cl, Br, I, NH.sub.2, CH.sub.2 CN, C.dbd.CHor ##STR12## wherein R.sub.4 =H, NH.sub.2, NHOH, NHCOCH.sub.3, NHCH.sub.3, NHNH.sub.2 and R.sub.5 =H, F, Cl, Br, I, CH.sub.3, CF.sub.3 and R.sub.6 =CH.sub.3, I, CH.dbd.CHBr, CH.sub.2 OH, CH.sub.2 NH.sub.2, C.dbd.CCH.sub.3or ##STR13## wherein R.sub.2 =OH, SH, H, Cl and R.sub.3 =H, OH, Cl, SH, NH.sub.2 ; with the proviso that when S is 1-.beta.-D-arabinofuranose, 2,3-dideoxy-3-azido-1-.beta.-D-ribofuranose, 2-hydroxy-ethoxy-methyl, 4-hydroxy-3-(hydroxymethyl)-butyl, 2-hydroxy-1-(hydroxymethyl)-ethoxy-methyl or 2,3-di-hydroxy-propoxy, then B cannot be ##STR14##