Phosphotriester type biologically active compounds

Details Phosphotriester type biologically active compounds Phosphotriester type biologically active compounds

1998-06-22

2000-02-01

Wilson, James O.

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

Organic compounds

Carbohydrates or derivatives

536 2671, 536 2672, 536 2674, 536 268, 536 269, 544243, 544264, C07H 100, C07H 1900

Patent

active

060204826

ABSTRACT:
Phosphotriester compound of general formula (I); ##STR1## wherein R is a radical --(CH.sub.2).sub.n --S--X in which X is a radical (a) or --S--U, Z being O or S, and Y and U denote an alkyl, aryl or osidic radical, optionally substituted in particular by an OH, SH or NH.sub.2 group, and n is from 1 to 4, preferably 1 or 2, and Nu is a radical consisting of a biologically active compound residue or the dephosphorylated residue of a compound that is biologically active when it carries a phosphate or phosphonate group.

REFERENCES:
patent: 5430136 (1995-07-01), Urdea et al.
patent: 5430138 (1995-07-01), Urdea et al.
patent: 5770725 (1998-06-01), Gosselin et al.
Hao, Z. et al., "Potent DNA Chain Termination Activity and Selective Inhibition of Human Immunodeficiency Virus Reverse Transcriptase by 2',3'-Dideoxyuridine-5'-triphosphate", Molec. Pharmacol., 1989, 37, 157-163.
Hao, Z. et al., "2',3'-Dideoxyuridine Triphosphate: A Potent Inhinitor of HIV Reverse Transcriptase", Proc. AACR, 1988, 29, 348, Abstract 1386.
Matthes, E. et al., "Inhibition of HIV-Associated Reverse Transcriptase by Sugar-Modified Derivatives of Thymidine 5'-Triphosphate in Comparison to Cellular DNA Polymerases .alpha. and .beta.", Biochem. & Biophys. Res. Comm., 1987, 148(1), 78-85.
Rosenberg, I. et al., "Synthesis of Potential Prodrugs and Metabolites of 9-(S)-(3-Hydroxy-2-Phosphonylmethoxypropyl) Adenine", Coll. Czech. Chem. Commun., 1987, 52, 2792-2800.

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