Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1996-02-22
1999-01-12
LeGuyader, John L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
135 6, 135 911, 135375, 536 231, A61K 4800, C12Q 168, C07H 2101
Patent
active
058589880
ABSTRACT:
In accordance with the present invention, antisense oligonucleotides are provided with enhanced membrane permeability and stability. This is accomplished in accordance with the invention through conjugating oligoribonucleotides with a hydrophobic carrier agent at the 2'-O position of the oligonucleotides. The hydrophobic carrier agent comprises a compound of the following general structure: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are independently H, NO.sub.2, halide, linear or branched alkyl, linear or branched acyl, linear or branched alkylene, linear or branched O-alkyl, linear or branched amido, linear or branched S-alkyl, mono or disubstituted amine, linear or branched thioamido, phosphothionate, or phosphothioate.
In a preferred embodiment, R.sup.1 and R.sup.3 are NO.sub.2. In such embodiment, it will be appreciated that when R.sup.2, R.sup.4, and R.sup.5 are H, the compound is DNP and when R.sup.4 is F, the compound is FDNP.
REFERENCES:
patent: 5466786 (1995-11-01), Buhr et al.
patent: 5496546 (1996-03-01), Wang et al.
patent: 5514577 (1996-05-01), Draper et al.
E. Lesnik et al. Biochem. 32: 7837-8 1993.
J Grzybowski et al. Nucl. Acids Res. 21(8): 1705-12 1993.
Steward, David L., et al., "Influence of 2'O-acetylation on the antiviral activity of polyribonucleotides", Biochim. Biophys. Acta, 262, 227-232, (1972).
Chuan, Hua, et al., "3'O-(5-Fluro-2,4-dinitrphenyl)ADP Ether and ATP Ether", The Journal of Biological Chemistry, vol. 263, No. 26, 13003-13006, Sep. 15, 1988..
Kang Insug, et al., "Design of Structure-based Reverse Transcriptase Inhibitors", The Journal of Biological Chemistry, vol. 269, No. 16, 12024-12031, Apr. 22, 1994.
Steward, et al., Chem. Ab., 77 77: 1242G.
William, Chem. Ab., 87 (23) 177597, (1977).
Chem. Ab., 83:158731 (1975).
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