Non-nucleoside linkers for convenient attachment of labels to oligonucleotides using standard synthetic methods

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United States of America Patent

PATENT NO 5414077
SERIAL NO

08237233

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Abstract

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Pseudonucleosides and pseudonucleotides are useful in the synthesis of oligomers which contain these components as a means to derivatize the resulting oligonucleotide to useful substituents such as chelators, intercalators, or lipophilic compounds. In general, these pseudonucleotide components are of the formula: ##STR1## wherein each Y is independently O or S; each X is independently H, PO.sub.3.sup.-2, an activated nucleotide synthesis coupling moiety, a protecting group, a nucleoside, a nucleotide or a nucleotide sequence, or comprises a solid support; F is a functional group capable of linking an additional moiety or said group already reacted to effect the binding of said additional moiety; .quadrature. is an organic backbone which does not contain additional F or Y-X substituents and which is either achiral even when the Y-X substituents are different, or is a single enantiomer of a chiral compound; with the proviso that at least one X is a nucleoside, nucleotide, nucleotide sequence, an activated nucleotide synthesis coupling moiety, or comprises a solid support, or F represents said functional group already reacted with an additional group. Oligonucleotides having the pseudonucleoside at the 3' terminus are particularly stable in vivo.

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Patent Owner(s)

Patent OwnerAddress
ISIS PHARMACEUTICALS INC2280 FARADAY AVENUE CARLSBAD CA 92008 UNITED STATES OF AMERICA

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Lin, Kuei-Ying Fremont, CA 46 3168
Matteucci, Mark Burlingame, CA 55 6077

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