Modified oligonucleotides and intermediates useful in...

C - Chemistry – Metallurgy – 07 – H

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C07H 21/00 (2006.01) C07H 19/06 (2006.01) C07H 19/16 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2186250

The present invention provides nuclease resistant 3'-carbon modified oligonucleotides that can be wed in the field of nucleic acid therapeutics and diagnostics. The modified oligonulceotides of the present invention have at least one modified internucleotide linkage wherein the divalent oxygen moiety at the 3'-position of the internucleotide linkage is replaced by a tetravalent carbon moiety. The 3'- carbon modified internucleotide linkage is preferably a 3'-methylene or 3'-hydroxymethylene linkage. Also provided are a method and monomeric nucleoside and nucleotide intermediates for making the modified oligonucleotides of the present invention.

L'invention porte sur des oligonucléotides modifiés par C en position 3' d'une liaison internucléotidique, résistant à la nucléase et pouvant servir dans le domaine des thérapies et des diagnostics recourant à l'acide nucléique. Ces nucléotides présentent au moins une liaison internucléotidique modifiée, la fraction d'oxygène bivalent en position 3' de ladite liaison étant remplacée par une fraction de carbone tétravalent. La liaison internucléotidique modifiée par C en position 3' est de préférence une liaison du type 3'-méthylène ou 3'-hydroxyméthylène. L'invention porte également sur un procédé, un nucléoside monomère et des intermédiaires de nucléotides servant à produire les oligonucléotides selon l'invention.

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