The Upjohn Co.

University Patents, Inc.

Tomi K Sawyer

Victor J Hruby

Mac E Hadley

Jackson B Hester, Jr

Ronald B Gammill

Ruth Elizabeth TenBrink

Suvit Thaisrivongs

Heinrich Josef Schostarez

Christopher B Heward

Hossain H Saneii

Donald T Pals

The present invention provides novel peptides of the formula X-A.sub.6 -B.sub.7 -C.sub.8 -D.sub.9 -E.sub.10 -F.sub.11 containing a novel (1-amino-2-hydroxy-2-heterocyclic) ethyl moiety of the formula XL.sub.2c at the E.sub.10 -F.sub.11 -position, X is a terminal group, and the remaining variables are amino acid residues. The present invention also provides novel intermediate compounds. These peptides are useful as renin inhibitors and as inhibitors of retroviral proteases. Renin inhibitors are useful for the diagnosis and control of renin-dependent hyperaldosterism, other renin-dependent cardiovascular disorders and ocular disorders. Inhibitors of retroviral proteases, such as the HIV-I protease, are useful for treating diseases caused by retroviruses, such as human acquired immunodificiency disease syndrome (AIDS). ##STR1##

Peptides containing a (1-amino-2-hydroxy-2-heterocyclic)ethyl moiety

The present invention provides novel renin-inhibiting peptides and novel processes and intermediates for the preparation of both novel and known renin-inhibiting peptide analogs. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension.

Renin inhibitory peptides containing an N-alkyl-histidine moiety

Cyclic analogues of the tridecapeptide hormone, .alpha.-melanotropin. (.alpha.-melanocyte stimulating hormone, .alpha.-MSH), wherein a physiologically stable intramolecular interaction exists (1) between the amino acid residue at position 4 and an amino acid residue at position 10 or 11, and/or (2) between the amino acid residue at position 5 and an amino acid residue at position 10 or 11. Preferred analogues, e.g., [half-Cys.sup.4, half-Cys.sup.10 ]-.alpha.-MSH display greatly increased in vitro potency, prolongation, and resistance to enzymatic degradation.

Synthetic analogues of .alpha.-melanotropin

Analogues of the tridecapeptide hormone, .alpha.-melanotropin (a-melanocyte stimulating hormone, .alpha.-MSH) of the formula:

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Kalamazoo, MI, United States of America

Tomi K Sawyer