Merck + Co., Inc.

Harri G Ramjit

Steven M Pitzenberger

Suresh K Balani

Jiunn H Lin

Edgar H Ulm

Byron H Arison

Michael S Schwartz

Anthony D Theoharides

Laura R Kauffman

Anthony Y Lu

Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation product the compound 3-[2-(benzoxazol-2-yl)ethyl]-5-(1-hydroxyethyl)-6-methyl-2-(1H)-pyridinone . This product is useful in the prevention or treatment of infection by HIV and the treatment of AIDS.

Preparation of

Novel dipeptide isosteres are the biotransformed products after incubation with rat liver slices. They inhibit HIV protease, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts (when appropriate), pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Method of preparing HIV protease inhibitors

Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation products the 6-hydroxymethyl and 5-(1-hydroxy)ethyl anologs. These products are useful in the prevention or treatment of infection by HIV and the treatment of AIDS.

Method of hydroxylating substituted 3-aminopyridinones using mammalian

A metabolite of the known anxiolytic agent, 7-chloro-5,6-dihydro-3-(5-isopropyl-1,2,4-oxadiazol-3-yl)-5-methyl-6-oxo-4 H-i midazo[1,5a][1,4]benzodiazepine is a 1,2-dihydroxy derivative of the isopropyl moiety and is itself an anxiolytic agent of greater activity than its substrate.

7-chloro-5,6-di

A metabolite of the known anxiolytic agent, 7-chloro-5,6-dihydro-3-(5-isopropyl-1,2,4-oxadiazol-3-yl)-5-methyl-6-oxo-4 H- imidazo[1,5a][1,4]benzodiazepine is a 2-hydroxy derivative of the isopropyl moiety and is itself an anxiolytic agent.

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Lansdale, PA, United States of America

Harri G Ramjit