3'-azido-2', 3'-dideoxyuridine anti-retroviral composition

Details 3'-azido-2', 3'-dideoxyuridine anti-retroviral composition 3'-azido-2', 3'-dideoxyuridine anti-retroviral composition

A - Human Necessities

61

K

167/218

A61K 31/70 (2006.01) C07H 19/06 (2006.01) C07H 19/10 (2006.01)

Patent

CA 1313498

3'-AZIDO-2',3'-DIDEOXYURIDINE ANTI-RETROVIRAL COMPOSITION Abstract Compositions for the treatment of AIDS and ARC having the following compound as an active ingredient: Image where R1 is OH, monophosphate, diphosphate, or triphosphate; or a pharmacologically acceptable salt thereof. The primary advantage of this compound is its highly selective anti-retroviral activity, i.e., it significantly decreases viral replication as measured as reverse transcriptase activity while demonstrating orders of magnitude less cytotoxicity than other anti- viral compounds such as AZT. In a preferred embodiment, the compound is present in an amount sufficient to inhibit the HIV reverse transcriptase activity but not significantly inhibit human DNA polymerase activity. Also included within the scope of this invention are 3'-azido-2',3'- dideoxyuridine 5'-mono-, di-, and triphosphate and compositions containing these compounds as the active agent.

557486

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