Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-01-17
1996-11-26
Higel, Floyd D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514311, 514397, 514400, 514475, 546175, 5462817, 546256, 5483111, 5483657, 549553, A61K 3147, A61K 31415, A61K 31335, C07D21538, C07D30336, C07D30308
Patent
active
055786081
ABSTRACT:
An HIV protease inhibiting compound of formula I ##STR1## wherein: R is C.sub.1 -C.sub.6 alkyl, cycloalkyl, heterocycle, unsaturated heterocycle, aryl, cycloalkyl (C.sub.1 -C.sub.4)alkyl, heterocycle(C.sub.1 -C.sub.4)alkyl, unsaturated heterocycle (C.sub.1 -C.sub.4)alkyl, aryl(C.sub.1 -C.sub.4)alkyl, or --A--(CH.sub.2).sub.q --R.sup.0, where A is --O--, --NH-- or --S--; q is 0, 1, 2 or 3; and R.sup.0 is cycloalkyl, aryl, heterocycle or unsaturated heterocycle; ##STR2## where R.sup.1 is aryl, cycloalkyl, heterocycle or unsaturated heterocycle; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.3 is an amino acid side chain, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.3, --CH.sub.2 (CH.sub.2).sub.2 CH.sub.3, --C(CH.sub.3).sub.3, cyano(C.sub.1 -C.sub.4)alkyl, unsaturated heterocycle (C.sub.1 -C.sub.4)alkyl, aryl(C.sub.1 -C.sub.4)alkyl, --(CH.sub.2).sub.s --A.sup.0 --(CH.sub.2).sub.r --R.sup.4, or --CH.sub.2 --C(O)--NR.sup.2 --(CH.sub.2).sub.r --R.sup.5, where s is 1, 2, 3 or 4; r is 0, 1, 2 or 3; A.sup.0 is --O--, --NH-- or --S--; R.sup.4 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, aryl, heterocycle or unsaturated heterocycle; R.sup.5 is cycloalkyl, aryl, heterocycle or unsaturated heterocycle; j is 0, 1, 2, 3 or 4; k is 0 or 1; and Y is --O--, --N(R.sup.2)-- or --S--; or a pharmaceutically acceptable salt thereof.
REFERENCES:
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"Synthetic Non-peptide Inhibitors of HIV Protease", Blumenstein, J. J., et al., Biochem. and Biophys. Res. Comm. 163(2), pp. 980-987 (1989).
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"In Vitro Inhibition of HIV-1 Proteinase by Cerulenin", Moelling, K., et al., FEBS Letters (1990), pp. 373-377.
"Peptidyl Expoxides as Potent, Active Site-directed Irreversible Inhibitors of HIV-1 Protease", Moore, M. L. et al., Peptides Chemistry and Biology, Proceedings of the Twelfth American Peptide Symposium, Jun. 16-21, 1991, edited by John A. Smith and Jean E. Rivier, pp. 781-782 (1992).
"Design, Synthesis and Characterization of an Irreversible Inhibitor of HIV-1 Protease", Kaldor, S. W. et al., Abstr. No. 178, 203rd ACS National Meeting (Apr. 5-10, 1992).
"Human Immunodeficiency Virus 1 Protease Expressed in Escherichia coli behaves as a Dimeric Aspartic Protease", Meek, T. D. et al., Proc. Natl. Acad. Sci. USA, 86, pp. 1841-1845 (1989).
Hornback William J.
Munroe John E.
Eli Lilly and Company
Higel Floyd D.
McClain Janet T.
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