Oligonucleotide prodrugs

Details Oligonucleotide prodrugs Oligonucleotide prodrugs

C - Chemistry, Metallurgy

07

H

C07H 21/00 (2006.01) A61K 31/70 (2006.01) C07J 43/00 (2006.01) C12N 15/11 (2006.01)

Patent

CA 2199464

Disclosed is an oligonucleotide prodrug comprising at least six covalently linked nucleotides, at least one of which is derivatized with a lipophilic chemical group reversibly and covalently attached to the nucleotide at a 5' phosphate, a 3' phosphate, or an internucleotidic phosphate linkage. The prodrug is reactive with a cellular or tissue enzyme which cleaves the lipophilic group from the derivatized nucleotide, thereby regenerating the parent oligonucleotide.

L'invention concerne un promédicament oligonucléotidique comprenant au moins six nucléotides à liaison covalente, dont au moins un est dérivé avec un groupe chimique lipophile fixé de manière réversible et covalente au nucléotide au niveau d'un phosphate 5', d'un phosphate 3', ou d'une liaison phosphate internucléotidique. Le promédicament réagit avec une enzyme cellulaire ou tissulaire qui clive le groupe lipophile du nucléotide dérivé, ce qui régénère l'oligonucléotide parent.

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