Novel 5'-substituted nucleosides and oligomers produced...

C - Chemistry – Metallurgy – 07 – H

Patent

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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 19/10 (2006.01) C07H 19/16 (2006.01) C07H 19/20 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2159632

Disclosed are novel 5'-substituted nucleosides and oligonucleotide analog compounds prepared therefrom having from 2 to about 60 bases and having an internucleoside backbone containing one or more 3'-O-PO2H-O-5'-CR1R2- internucleoside linkages instead of the naturally occurring backbone of phosphodiester internucleoside linkages. The present invention also discloses a method of synthesizing oligonucleotide compounds having from 2 to about 60 bases and having an internucleoside backbone containing one or more 3'-O-PO2H- O-5'-CR1R2 internucleoside linkages instead of the naturally occurring backbone of phosphodiester internucleoside linkages, this process comprising preparation of 5'-substituted nucleoside compounds, for example, as illustrated in Figure 1, and utilizing them as synthons in automated DNA synthesizers. Oligonucleotide analogs of the present invention are useful as nuclease resistant, sequence specific antisense compounds.

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