Bi- and tri-cyclic nucleoside, nucleotide and...

C - Chemistry – Metallurgy – 07 – H

Patent

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C07H 21/00 (2006.01)

Patent

CA 2303299

The present invention relates to novel bicyclic and tricyclic nucleoside and nucleotide analogues of formula (I) as well as to oligonucleotides comprising such elements. The nucleotide analogues, LNAs (<u>L</u>ocked <u>N</u>ucleoside <u>A</u>nalogues), are able to provide valuable improvements to oligonucleotides with respect to affinity and specificity towards complementary RNA and DNA oligomers. The novel type of LNA modified oligonucleotides, as well as the LNAs as such, are useful in a wide range of diagnostic applications as well as therapeutic applications. Among these can be mentionned antisense applications, PCR applications, strand displacement oligomers, as substrates for nucleic acid polymerases, as nucleotide based drugs, etc. The present invention also relates to such applications.

L'invention concerne de nouveaux analogues de nucléosides et de nucléotides bicycliques et tricycliques, ainsi que des oligonucléotides renfermant de tels éléments. Les analogues de nucléotides, LNA (analogues de nucléosides verrouillés), sont capables d'apporter des améliorations précieuses aux oligonucléotides en ce qui concerne leur affinité et leur spécificité à l'égard d'oligomères d'ADN et d'ARN complémentaires. Le nouveau type d'oligonucléotides transformés en LNA, ainsi que les LNA à proprement parler, sont utiles dans une large gamme d'applications diagnostiques et thérapeutiques, notamment les applications antisens, les applications ACP, les oligomères à déplacement de brins en tant que substrats pour polymérases d'acide nucléique, en tant que médicaments à base de nucléotide, etc. L'invention concerne aussi de telles applications.

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