Rna amidates and thioamidates for rnai

Details Rna amidates and thioamidates for rnai Rna amidates and thioamidates for rnai

C - Chemistry, Metallurgy

12

N

C12N 15/11 (2006.01) A61K 31/7125 (2006.01) A61P 31/12 (2006.01) C07H 21/00 (2006.01)

Patent

CA 2544349

The present disclosure relates to RNA amidates and thioamidates useful for RNA interference applications. The RNA amidates and thioamidates contain at least one internucleoside linkage chosen from ribo-N3'.fwdarw.P5' phosphoramidate (NP) and ribo-N3'.fwdarw.P5' thiophosphoramidate (NPS) linkages, and optionally further containing at least one covalently conjugated lipid moiety. Compositions comprising the amidates and thioamidates are disclosed, as are methods for their use in modulating gene expression.

La présente invention se rapporte à des amidates et des thioamidates utiles pour des applications d'interférence ARN. Ces amidates et thioamidates ARN contiennent au moins une liaison internucléoside sélectionnée parmi des liaisons ribo-N3'?P5' phosphoramidate (NP) et ribo-N3'?P5' thiophosphoramidate (NPS), contenant en outre éventuellement au moins une fraction lipidique conjuguée de manière covalente. L'invention se rapporte à des compositions comportant ces amidates et thioamidates, ainsi qu'à des procédés permettant leur utilisation pour la modulation d'une expression génique.

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