Xylo-lna analogues

C - Chemistry – Metallurgy – 07 – H

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C07H 19/06 (2006.01) C07H 19/10 (2006.01) C07H 21/00 (2006.01)

Patent

CA 2368135

A bicyclic nucleoside derivative, wherein an intranucleoside ring locks the ring conformation of the nucleoside, is termed an LNA - a Locked Nucleic Acid. LNAs of the xylo-configuration, considered useful as therapeutic agents, diagnostic agents and useful for the formation of oligonucleotides, have been prepared. These oligonucleotides are also useful as a therapeutic and in diagnostic fields. Furthermore, oligonucleotides comprising LNAs of the xylo-configuration are useful for high-affinity targeting of complementary single stranded and double stranded DNA and RNA and have interesting activity with regards to specificity and affinity to oligonucleotides.

Un dérivé nucléosidique bicyclique, dans lequel un cycle intranucléosidique bloque la conformation cyclique du nucléoside, est appelé LNA acide nucléique bloqué. Des LNA de configuration xylo, considérés utiles en tant qu'agents thérapeutiques, agents diagnostiques et pour la formation d'oligonucléotides, ont été préparés. Ces oligonucléotides sont également utiles en tant qu'agents thérapeutiques et dans les domaines diagnostiques. Par ailleurs, des oligonucléotides comprenant les LNA de configuration xylo sont utiles pour le ciblage à affinité élevée d'ADN et d'ARN simple et double brin et possèdent une activité intéressante pour ce qui concerne la spécificité et l'affinité par rapport aux oligonucléotides.

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