Enzyme inhibitors

Details Enzyme inhibitors Enzyme inhibitors

1989-06-06

1993-05-18

Russel, Jeffrey E.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 18, 530330, 530331, A61K 3743, C07K 510, C07K 706

Patent

active

052121577

ABSTRACT:
Disclosed herein are peptide derivatives which inhibit the activity of human immunodeficiency virus (HIV) protease. The peptide derivatives can be represented by general formula R.sup.1 --R.sup.2 --Y--R.sup.3 --R.sup.4 wherein R.sup.1 is an optionally substituted 3-(1,2,3,4-tetrahydroisoquinolyl)carbonyl residue, R.sup.2 and R.sup.3 are amino acid or analogous amino acid residues (R.sup.3 may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R.sup.4 is [--NR.sup.17 CH(R.sup.18)C(O)].sub.p --Z wherein R.sup.17 is hydrogen or lower alkyl, R.sup.18 is an amino acid or analogous amino acid side chain, p is zero or 1 and Z is a terminal group (e.g. hydroxy or amino), or R.sup.4 is --NR.sup.17 CR.sup.18 (R.sup.21)CH.sub.2 --OH wherein R.sup.17 and R.sup.18 are as noted hereinabove and R.sup.21 is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives also inhibit renin activity. Accordingly, the derivatives can be used for combating HIV infections or for treating hypertension or congestive heart failure.

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patent: 4894437 (1990-01-01), TenBrink
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Gopalakrishnan et al, "The Regulation of Receptors, Ion Channels, and G. Proteins . . . ". Cardovascular Drug Reviews vol. 8, No. 3, 1990. p. 255.
Chemical Abstracts: CA 111:209687j: Gros et al. "Protection of atrial natriuretic factor against . . . " (1989).
Plattner, "Renin Inhibitors", J. Med. Chem. 1988, 31, 2277-2288.
Moore et al, "Peptide Substrates and Inhibitors of HIV-1 Protease" Biochem. Biophys, Res. Com. 159 (2), 420-425 (1989).
Richards et al, "Effective Blocking of HIV-1 Proteinase Activity by Characteristic Inhibitors of Aspartic Proteinases", FEBS Letters 247 (1), 113-116 (1989).
Seelmeier et al, "Human Immunodeficiency Virus has an Aspartic-Type Protease that can be inhibited by Pepstatin A", PNAS 85, 6612-6616 (1988).

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