Oligonucleotide-dendrimer conjugates

C - Chemistry – Metallurgy – 07 – H

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C07H 21/00 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01) C12Q 1/68 (2006.01)

Patent

CA 2206915

Oligonucleotide-dendrimer conjugates, wherein dendrimer is the monovalent residue of a dendrimer of the first to tenth generation and oligonucleotide is a natural, modified or synthetic sequence which is composed of natural, modified or synthetic deoxynucleosides or peptide nucleic acid building blocks which are linked via internucleotide bridges and which encompasses a region which is complementary, preferably completely complementary, to a target nucleic acid (target RNA or target DNA), with the dendrimer being bonded to an internucleotide bridge, a nucleic acid base or a sugar of the oligonucleotide, and the salts thereof.

La présente invention concerne des conjugués oligonucléotide-dendrimère et leurs sels. Dans ces conjugués, le dendrimère est le reste monovalent d'un dendrimère de la première à la dixième génération, et l'oligonucléotide est une séquence synthétique, modifiée ou naturelle composée de désoxynucléosides synthétiques, naturels ou modifiés ou de motifs structuraux d'acide nucléique peptidique. Des ponts internucléotidique relient ces motifs structuraux et entourent une région complémentaire, de préférence totalement complémentaire, d'un acide nucléique cible (ARN cible ou ADN cible). Le dendrimère est lié à un pont internucléotide, une base d'acide nucléique ou un sucre de l'oligonucléotidique.

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