Benzoxazinones utilisées comme inhibiteurs de transcriptase inverse de HIV

Benzoxazinones as inhibitors of HIV reverse transcriptase

Benzoxazinone als Inhibitoren von reverser Trans-Kriptase von HIV

Abstract

Certain benzoxazinones of the formula: wherein:    X is halo,    X¹ is trihalomethy, or pentahaloethyl;    Z is O; are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

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Patent Citations (2)

    Publication numberPublication dateAssigneeTitle
    EP-0093922-A2November 16, 1983Dr. Karl Thomae GmbHBenzoxazin-2-ones, their preparation and therapeutic agents containing these compounds
    US-3526621-ASeptember 01, 1970Farmaceutical Italia SocSubstituted 3,1-benzoxazin-2-one

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