Patent ID: 6191266
Filing Date: 2001-02-20
Classification: A61P,C07H

Abstract:
A nucleoside having the structure: ##STR6##wherein:R.sub.2 is selected from the group consisting of H, OH, alkoxy, aralkoxy and aryloxy;R.sub.3 and R.sub.5 are independently selected from the group consisting of OH, OCEPA and a hydroxyl blocking group;X is selected from the group consisting of O and CH.sub.2 ;B is a nucleoside base;when X is CH.sub.2,R.sub.1 ', R.sub.3 ', R.sub.4 ' and R.sub.5 ' are independently selected from the group consisting of H, CN,N.sub.3, NO.sub.2, CF.sub.3, alky, substituted alkyl, aralkyl, substituted aralkyl, aryl, and substituted aryl, provided that R.sub.1 ', R.sub.3 ', R.sub.4 ' and R.sub.5 ' cannot all be H at the same time and R.sub.4 ' is not a label;when X is O,R.sub.4 ' and R.sub.5 ' are H, andR.sub.1 ' is selected from the group consisting of N.sub.3, NO.sub.2, CF.sub.3, alky, substituted alkyl, aralkyl, substituted aralkyl, aryl, and substituted aryl, where the substituted portion of at least one of the substituted alkyl substituted aralkyl and substituted aryl is selected from the group consisting of NO.sub.2, N.sub.3, CF.sub.3, SH, SR, COOH, COOR, SO.sub.3 H SO.sub.3 R, F, Cl, Br, I, Ts, Ac, CF.sub.3 CO, acyl, where R is selected from lower alkyl aralkyl and aryl; andR.sub.3 ' is selected from the group consisting of CN, N.sub.3, NO.sub.2, CF.sub.3, alkyl, substituted alkyl, aralkyl, substituted aralkyl, aryl, and substituted aryl, where the substituted portion of at least one of the substituted akl, substituted aralkyl and substituted aryl is selected from the group consisting of CN, NO.sub.2, N.sub.3, CF.sub.3, NH.sub.2, NR.sub.2, OR, SH, SR, COOH, COOR, SO.sub.3 R, F, Cl, Br, I Ts, Ac, CF.sub.3 CO, acyl, where R is selected from lower alkyl, aralkyl and aryl; andwhereinany alkyl portion of R.sub.1 ', R.sub.3 ', R.sub.4 ' and R.sub.5 ' is C1 to C10, linear, branched, saturated or unsaturated.