Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substitute

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

1989-09-08

1990-04-03

Schwartz, Richard A.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

514 18, 530331, 564153, A61K 31165, C07C14705

Patent

active

049141295

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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B. Evans et al., J. Org. Chem., vol. 50, pp. 4615-4625 (1985).
D. Rich et al., Peptides: "Structure and Function", 8th American Peptide Sympsium, pp. 511-520 (1983).
M. Szelke et al., "Peptides: Structure and Function", Proceedings of the 8th American Peptide Symposium, pp. 579-582 (1983).
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