Patent ID: 6147200
Filing Date: 2000-11-14
Classification: A61P,C07H

Abstract:
A compound having the formula: ##STR7## wherein: Bx is an optionally protected heterocyclic base moiety;each T.sub.1 and T.sub.2 is, independently, OH, a protected hydroxyl;or one of T.sub.1 and T.sub.2 is OH or a protected hydroxyl and the other of T.sub.1 and T.sub.2 is a solid support or an activated phosphorus-containing substituent group;each E.sub.1 and E.sub.2 is, independently, C.sub.1 -C.sub.10 alkyl, or one of E.sub.1 and E.sub.2 is H and the other of E.sub.1 and E.sub.2 is --CH.sub.3 ;or each E.sub.1 and E.sub.2 is, independently, H, --(CH.sub.2).sub.m --S--R.sub.4 where m is from 1 to 10, --{(CH.sub.2).sub.nn --N(H)}.sub.nnn --(CH.sub.2).sub.nn NH.sub.2 where each nn is from 2 to 4 and nnn is from 2 to 10, a polypeptide having from 2 to 10 peptide linked amino acids, a folic acid moiety optionally bearing a linking group attaching said folic acid moiety from the .alpha. or .gamma. carboxyl group to the 2'-substituent wherein said linking group is --N(H)--(CH.sub.2).sub.6 --, or a cholesterol moiety optionally bearing a linking group attaching said cholesterol moiety from the hydroxyl group to the 2'-substituent, wherein said linking group is --C(.dbd.O)--N(H)--(CH.sub.2).sub.6 --, provided that only one of E.sub.1 and E.sub.2 is H; andR.sub.4 is H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.6 -C.sub.14 aryl or a thio protecting group.