Bifunctional nucleosides, oligomers thereof, and methods of...

C - Chemistry – Metallurgy – 07 – H

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C07H 21/00 (2006.01) A61K 31/70 (2006.01) A61K 48/00 (2006.01) C07H 19/04 (2006.01) C07H 19/06 (2006.01) C07H 19/16 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2159628

Disclosed are novel bifunctional nucleoside analogs and oligonucleosides of 3 - 4 bases (trimers and tetramers) and longer containing at least two consecutive internucleodide linkages of two carbon-one nitrogen atom or two carbon-one oxygen atom (3'-NCC-5', 3'-CNC- 5', 3'-OCC-5') internucleoside linkages. The bifunctional nucleosides are useful for preparing the trimers and tetramers, which, in turn, are useful, together with the nucleosides, in preparing oligonucleosides as well as chimeric oligonucleotide analogs, preferably antisense oligonucleosides and oligonucleosides analogs, of 6 to about 60 bases having at least two consecutive internucleoside linkages of two carbon atoms and one nitrogen atom or 2 carbon atoms and one oxygen atom in the oligonucleoside backbone.

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