Inhibitors of HIV protease

Details Inhibitors of HIV protease Inhibitors of HIV protease

1992-09-25

1993-10-05

Brust, Joseph Paul

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548437, 435119, A61K 3140, C07D20956

Patent

active

052505634

ABSTRACT:
Novel cytochalasins are the biotransformed products after incubation with a substrate in a culture of the microorganism Kibdelosporangium sp. (Merck Culture Collection MA 6559), ATCC No. 53771. The compounds of the present invention inhibit HIV protease and are 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.

REFERENCES:
patent: 3849437 (1974-11-01), Ousby et al.
patent: 5183826 (1993-02-01), Bills et al.
Kohl, N. E. et al., "Active HIV Protease is required for viral infectivity," Proc. Natl. Acad. Sci., 85, 4686 (1988).
Ratner, L. et al., "Complete Nucleotide Sequence of the AIDS Virus, HTLV-III, " Nature 313, 277 (1985).
Toh, H. et al., "Close Structural Resemblance . . . ," EMBO J. 4, 1267 (1985).
Power, M. D. et al., "Nucleotide Sequence of SRV-1 . . . ," Science 231, 1567 (1986)
Pearl, L. H. et al., "A structural model for the retroviral proteases," Nature 329, 351 (1987).

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