Oligonucleotide analogs with novel linkages

C - Chemistry – Metallurgy – 07 – H

Patent

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Details

C07H 21/00 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01) C07H 19/06 (2006.01) C07H 19/16 (2006.01) C07H 23/00 (2006.01) C12Q 1/68 (2006.01)

Patent

CA 2071483

The instant invention is directed to oligonucleotide compounds wherein on or more phosphodiester linkages between adjacent nucleotides are replaced by a formacetal/ketal type linkage. The nucleotides of the present invention are resistant to nucleases and do not need to exhibit the diastereomerism characteristic of many other oligonucleotide compounds and thus are capable of strong hybridization to target RNA or DNA. These oligonucleotide compounds are useful in therapies which modulate gene expression using antisense or other specifically binding oligomers.

L'invention concerne des composés d'oligonucléotides dans lesquels une ou plusieurs liaisons phosphodiesters entre des nucléotides adjacents sont remplacées par une liaison de type formacétal/cétal. Les nucléotides de la présente invention sont résistants aux nucléases et n'ont pas besoin de présenter la caractéristique de diastéréomérisme de nombreux autres composés d'oligonucléotides et, par conséquent, sont capables d'une hybridation forte sur l'ARN ou l'ADN cibles. Ces composés d'oligonucléotides sont utiles dans des thérapies qui modulent l'expression des gènes en utilisant des oligomères non codants ou autres oligomères de liaisons spécifiques.

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