6-disubstituted bicyclic nucleic acid analogs

Details 6-disubstituted bicyclic nucleic acid analogs 6-disubstituted bicyclic nucleic acid analogs

C - Chemistry, Metallurgy

07

H

C07H 21/00 (2006.01) C07H 19/04 (2006.01)

Patent

CA 2692579

The present disclosure describes 6-disubstituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the 6- disubstituted bicyclic nucleosides each comprise a 2'-O- C(Ri)(R2)-4' or 2'-O- C=(R3)(R.4)-4' bridge wherein each R is, independently a substituent group and Ri and R2 include H. The 6-disubstituted bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.

La présente invention concerne des nucléosides bicycliques disubstitués en position 6, des composés oligomériques préparés à partir de ceux-ci et des procédés d'utilisation des composés oligomériques. Plus particulièrement, la présente invention concerne des nucléosides bicycliques disubstitués en position 6 comportant un pont de formule 2'-O-C(Ri)(R2)-4' or 2'-O- C=(R3)(R.4)-4' dans laquelle chaque R est indépendamment un groupe substituant et Ri et R2 comporte H. Les nucléosides bicycliques disubstitués en position 6 sont utiles pour l'amélioration de propriétés de composés oligomériques comportant une résistance à la nucléase. Selon certains modes de réalisation, les composés oligomériques selon l'invention s'hybrident à une partie d'un ARN cible entraînant la perte d'une fonction normale de l'ARN cible.

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