Merck + Co., Inc.

Randall R Miller

Shieh-Shung T Chen

Byron H Arison

Ali Shafiee

George M Garrity

Brian Heimbuch

Ralph A Stearns

Biotransformation products of a fermentation with culture MA7074 are potent HIV protease inhibitors. These products are useful in the prevention or treatment of infection by HIV and in 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.

Streptomyces sp. MA 7074 (ATCC 55605) used for microbial synthesis of

Microbial transformation of a macrolide immunosuppressant by the microorganism Streptomyces sp., (Merck Culture Collection MA 6960) ATCC No. 55387 yields a compound of the structural formula (I): ##STR1## This compound is an immunosuppressant useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

Microbial transformation product having immunosuppressive activity

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Piscataway, NJ, United States of America

Randall R Miller