Antisense agents combining strongly bound base - modified...

C - Chemistry – Metallurgy – 12 – N

Patent

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C12N 15/11 (2006.01) A61K 31/7115 (2006.01)

Patent

CA 2651031

The present invention provides compounds having a chelating moiety and an oligonucleotide sequence wherein the oligonucleotide includes one or more modified nucleobases, such as hydroxynucleobases. The disclosed compounds are suitable for antisense therapy. The chelating moiety can be complexed to an ion of a lanthanide metal. These compounds are efficient translation inhibitors of nucleic acids and have increased binding affinity for target nucleic acids. The invention also includes compositions and methods of using these compositions as antisense therapy.

La présente invention concerne des composés ayant un fragment chélatant et une séquence oligonucléotidique, l'oligonucléotide comprenant une ou plusieurs nucléobases modifiées, par exemple des hydroxynucléobases. Les composés présentés sont adéquats pour la thérapie antisens. Le fragment chélatant peut être complexé à un ion de lanthanide. Ces composés sont des inhibiteurs efficaces de la traduction des acides nucléiques et ils ont une affinité de liaison augmentée pour les acides nucléiques cibles. L'invention concerne également des compositions et des procédés d'utilisation de ces compositions pour la thérapie antisens.

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