Aryl phosphate derivatives of d4T having anti-HIV activity

Details Aryl phosphate derivatives of d4T having anti-HIV activity Aryl phosphate derivatives of d4T having anti-HIV activity

1998-06-30

2000-02-29

Wilson, James O.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 49, 514 50, 514885, 536 261, 536 268, 536 282, C07H 19073, A61K 3170, A61K 3117

Patent

active

060309571

ABSTRACT:
Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.

REFERENCES:
patent: 5659023 (1997-08-01), Alexander et al.
patent: 5672698 (1997-09-01), Chen et al.
patent: 5750729 (1998-05-01), Alexander et al.
Vig et al., Antiviral Chem. Chemother., vol. 9(5), pp. 445-448, 1998.
Alexander et al., "Synthesis and Antiviral Activity of Pyranosylphosphonic Acid Nuceotide Analogues", J. Med. Chem., 39:1321-1330, 1996.
M.M. Mansuri et al., J. of Med. Chem., vol. 32(2), pp. 461-466, 1989.
McGuigane et al.,, J. Med. Chem., vol. 39, p. 1748, 1996.

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