Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substitute

Details Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substitute Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substitute

1987-02-05

1988-07-19

Schwartz, Richard A.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514 18, 530331, 548344, A61K 3764, C07K 508

Patent

active

047585846

ABSTRACT:
Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulphinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

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Evans, B., et al., J. Org. Chem 50: 4615-4625 (1983).
Holladay, M., et al., Tetrahedron Letters vol. 24, No. 41, pp. 4401-4404 (1983).
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Rich, et al., Peptides, Structure and Function, Proceedings of the Eight American Peptide Symposium, pp. 511-520.
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