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Abstract

Disclosed are oligonucleoside boranophosphates, or salts thereof, comprising a chain of natural or modified ribonucleotides or deoxyribonucleotides, containing at least one boronated internucleotide phospodiester linkage of the formula: ##STR1## W is selected from the group consisting of .dbd.O, .dbd.S, --OPr, and --SPr where Pr is a base-labile protecting group. X is selected from the group consisting of --BH.sub.3, --BH.sub.2 R.sub.1, --BHR.sub.1 R.sub.2 and --BR.sub.1 R.sub.2 R.sub.3. R.sub.1 is selected from the group consisting of --R.sub.4, --COOH, --COOR.sub.4, --CONHR.sub.4, --CON(R.sub.4).sub.2, --CN.sup.+ R.sub.4 Z.sup.-, wherein Z.sup.- is an anion, --CN, carboxycholesteryl and carboxybenzyl, wherein R.sub.4 is C1 to C18 alkyl. R.sub.2 is selected from the group consisting of --R.sub.5, --COOH, --COOR.sub.5, --CONHR.sub.5, --CON(R.sub.5).sub.2, --CN.sup.+ R.sub.5 Z.sup.-, wherein Z.sup.- is an anion, --CN, carboxy- cholesteryl and carboxybenzyl, wherein R.sub.5 is C1 to C18 alkyl. R.sub.3 is selected from the group consisting of C1 to C3 alkyl. Most preferably, X is --BH.sub.3 and W is =0. Compounds of Formula (III) are useful as antisense agents and probes in molecular biology, and have pharmacological activities including anti-inflammatory, antihyperlipidemic, and antineoplastic activity.

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First Claim