Substituted 5-amino-4-hydroxyvaleryl derivatives

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

1986-06-02

1988-01-12

Phillips, Delbert R.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Tripeptides, e.g., tripeptide thyroliberin , etc.

564197, 564198, 564157, 562564, 560170, 548204, 548495, 548344, 548550, 546336, C07K 508, C07C10334, C07C10312, C07C10320, C07C10130, C07D27720, C07D20918, C07D23364, C07D20712, C07D21170

Patent

active

047192887

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: 4372974 (1983-02-01), Fish et al.
patent: 4424207 (1984-01-01), Szelke et al.
patent: 4470971 (1984-09-01), Boger et al.
patent: 4478826 (1984-10-01), Veber et al.
patent: 4479941 (1984-10-01), Veber et al.
patent: 4609643 (1986-09-01), Szelke et al.
PCT/WO84/03044, (Aug. 16, 1984).
Tetrahedron Letters, vol. 24, 4401-4404, (1983).
Journal of Medicinal Chemistry, vol. 28, No. 3, (1985), 263-273.
J. Org. Chem., (1985), 4615-4625, vol. 50.
Rich, et al., Peptides: Structure & Function: Proceedings of the 8th American Peptide Symposium pp. 511-520, (1983).

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