Substituted 5-amino-4-hydroxyvaleryl derivatives

Details Substituted 5-amino-4-hydroxyvaleryl derivatives Substituted 5-amino-4-hydroxyvaleryl derivatives

1984-11-14

1986-09-23

Phillips, Delbert R.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

560125, 560170, 562444, 562507, 562567, C07C10130, C07C 6974, C07C10172, C07C 6108

Patent

active

046136762

ABSTRACT:
Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl- lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, 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.

REFERENCES:
patent: 4198398 (1980-04-01), Hudson et al.
patent: 4304715 (1981-12-01), Hudson et al.
patent: 4424207 (1984-01-01), Szelke et al.
Chem. Abstr. vol. 101, (1984) 125684m.
Tetrahedron Letters, vol. 23, No. 25, pp. 2533-2534 (1982).
M. Szelke et al., "Peptides: Structure and Function", Proceedings of the 8th American Peptide Symposium 579-582 (1983).
M. W. Holladay and D. H. Rich, Tetrahedron Letters 24, 4401-4404 (1983).

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