Sugar-modified gapped oligonucleotides

C - Chemistry – Metallurgy – 07 – H

Patent

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C07H 21/00 (2006.01)

Patent

CA 2246229

Oligonucleotides are provided which have increased nuclease resistance, substituent groups for increasing binding affinity to complementary nucleic acid strand, and subsequences of 2'-deoxy-erythro-pentofuranosyl nucleosides that activate RNase H. Such oligonucleotides are useful for diagnostics and other research purposes, for modulating the expression of a protein in organisms, and for the diagnosis, detection and treatment of other conditions susceptible to oligonucleotide therapeutics.

Cette invention concerne la synthèse et l'utilisation d'oligonucléotides afin de déclencher l'activité de RNase H en vue du clivage d'un brin dans un brin opposé. Cette invention concerne également des oligonucléotides dans lesquels quelques-unes au moins des unités nucléosides des oligonucléotides sont fonctionnalisées de manière à résister à la nucléase, quelques-unes au moins des unités nucléosides des oligonucléotides comprennent un substituant qui favorise l'hybridation de l'oligonucléotide à un brin complémentaire d'acide nucléique, et quelques-unes au moins des unités nucléosides des oligonucléotides comprennent des fragments de sucre 2'-désoxy-érythro-pentofuranosyle.

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