Synthesis of protease inhibitor

Chemistry: molecular biology and microbiology – Micro-organism – tissue cell culture or enzyme using process...

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435 711, 435120, 4352535, 544 60, C12P 100, C12P 2104

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active

051926687

ABSTRACT:
A dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a 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.

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Ser. No. 07/595,894 filed Oct. 11, 1990 by Chen (Merck 18208).
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Pearl, L. H. et al., "A structural model for retroviral proteases," Nature 329, 351 (1987).
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Ratner, L. et al., "Complete Nucleotide Sequence in AIDS Virus, HTLV-III," Nature 313, 277 (1985).
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