Sugar modified nucleosides and oligonucleotides

Details Sugar modified nucleosides and oligonucleotides Sugar modified nucleosides and oligonucleotides

1994-11-02

1997-10-28

Marschel, Ardin H.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 231, 536 253, 514 44, C07H 1900, C07H 2102, C07H 2100, A01N 4304

Patent

active

056819404

ABSTRACT:
A number of modified nucleosides are disclosed composed of modified sugar moieties which contain substituents at C1 and C4 positions, or branched substituents at C3 and C5 positions of deoxyribose or ribose. Each nucleoside is converted to or properly protected and then converted to the corresponding phosphoramidites. These phosphoramidites are used to assemble oligonucleotides in which there is at least one forenoted nucleosides. These sugar modified oligonucleotides have the potential to be used as antisense therapies since they are expected to enhance nuclease resistance and cellular uptake while they maintain sequence-specificity and affinity to nucleic acid targets in vitro or in vivo.

REFERENCES:
patent: 5446137 (1995-08-01), Maag et al.
Rabow L. and Stubbe, J., "Identification of the Alkaline-Labile Product Accompanying Cytosine Release during Bleomycin-Mediated Degradation of d(CGCGCG)", J. Am. Chem. Soc. 1986, 108, 7130-7131 (dated 1986).

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