HIV protease inhibitors useful for the treatment of AIDS

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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544362, 544363, 544373, 544374, 544376, 544377, 544387, 544388, 546114, 546115, 549 62, 549517, 549527, 549552, 514 43, 514 49, 514220, 5142305, 514252, A61K 31495, C07D40914

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active

056504128

ABSTRACT:
Compounds of formula ##STR1## are HIV protease inhibitors. These compounds 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.

REFERENCES:
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Caron, et al., "Radioselective Azide Opening of 2,3-Epoxy Alcohols by [Ti(O-i-Pr)2(N3)2]: Synthesis . . . ", J. Org., Chem., 53, pp. 5185-5187, 1988.
Cohen, et al., "Characterization of the Binding Site for Nevirapine (BI-RG-587), a Nonnucleoside Inhibitor . . . ", J. Biol. Chem., vol. 266, No. 22, pp. 14670-14674, 1991.
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Gao, et al., "Catalytic Asymmetric Epoxidation and Kinetic Resolution: Modified Procedures Including in Situ Derivatization", J. Am. Chen. Soc., 109, pp. 5765-5780, 1987.
Hargrave, et al., "Novel Non-Nucleoside InhibitorsIV-1 Reverse Transcriptase. 1. Tricyclic Pyridobenzo-- and Dipyridodiazepinones", J. Med. Chem., vol. 34, pp. 2231-2241, 1991.
Klunder, et al., "Novel Non-Nucleotide Inhibitors of HIV-1 Reverse Transcriptase. 2. Tricyclic Pyridobenzoxazapinones and Dibenzaxazapinones", J. Chem., vol.34, pp. 2231-2241, 1991.
Winslow et al, AIDS, 8 pp. 753-756 (1994).
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