Thiono triester modified antisense oligodeoxynucleotide...

C - Chemistry – Metallurgy – 07 – H

Patent

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C07H 21/00 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2216284

Antisense oligonucleotides having improved cellular uptake, increased nuclease resistance, and thermodynamically more stable target-binding capacity are disclosed. These novel oligonucleotides are characterized by having from 1 to 10 thiono-triester phosphorothioate internucleoside linkages bearing lipophilic moieties.

Cette invention concerne des oligonucléotides anti-sens possédant des qualités d'absorption cellulaire accrues, une meilleure résistance à la nucléase, et des qualités de liaison à une cible plus stables sur le plan thermodynamique. Ces nouveaux oligonucléotides se caractérisent par le fait qu'ils possèdent de 1 à 10 liaisons d'internucléosides de phosphorothioate de thiono-triester ayant des moitiés lipophiles.

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