Derivatized oligonucleotides having improved uptake and...

C - Chemistry – Metallurgy – 12 – N

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C12N 11/10 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01) A61K 48/00 (2006.01) C07H 21/00 (2006.01) C07H 23/00 (2006.01) C07J 43/00 (2006.01) C07J 51/00 (2006.01) C07K 9/00 (2006.01) C07K 14/00 (2006.01)

Patent

CA 2122030

Linked nudeosides having at least one functionalized nucleoside that bears a substituent such as a steroid molecule, a re- porter molecule, a non-aromatic lipophilic molecule, a reporter enzyme, a peptide, a protein, a water soluble vitamin, a lipid solu- ble vitamin, an RNA cleaving complex, a metal chelator, a porphyrin, an alkylator, a pyrene, a hybrid photonuclease/intercala- tor, or an aryl azide photo-crosslinking agent exhibit increased cellular uptake and other properties. The substituent can be attached at the 2'-position of the functionalized nucleoside via a linking group. If at least a portion of the remaining linked nucle- osides are 2'-deoxy-2'-fluoro, 2'-O-methoxy, 2'-O-ethoxy, 2'-O-propoxy, 2'-O-aminoalkoxy or 2'-O-allyloxy nucleosides, the sub- stituent can be attached via a linking group at any of the 3' or the 5' positions of the nncleoside or on the heterocyclic base of the nucleoside or on the inter-nucleotide linkage linking the nucleoside to an adjacent nucleoside.

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