Functionalized peptidyl aminodiols and -triols

Details Functionalized peptidyl aminodiols and -triols Functionalized peptidyl aminodiols and -triols

1988-05-09

1989-06-06

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 19, 530331, A61K 3743, C07K 508

Patent

active

048372048

ABSTRACT:
The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; aryalkyl; OR.sub.8 or SR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or aminoalkyl; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.11 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected)-(alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, .alpha.-methylbenzyl, .alpha.,.alpha.-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)-methyl, (2-naphthyl)methyl, (4-imidazolyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R.sub.1 is henoxy, thiophenoxy or anilino, B is CH.sub.2 or CHOH or A is hydrogen; R.sub.3 is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R.sub.4 is loweralkyl, cycloalkyl- methyl or benzyl; R.sub.2, R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl; X is O, NH or S; R.sub.7 is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl ##STR3## wherein R.sub.12 and R.sub.13 are independently hydrogen or loweralkyl, n is 0-2 and R.sub.14 is substituted or unsubstituted phenyl or heterocyclic; or XR.sub.7 together are loweralkylsulfonyl, N.sub.3 or Cl, and pharmaceutically acceptable salts thereof.

REFERENCES:
patent: 4548926 (1985-10-01), Matsueda et al.
patent: 4645759 (1987-02-01), Luly et al.
patent: 4652551 (1987-03-01), Luly et al.
patent: 4657931 (1987-04-01), Baran et al.
T. Kokubu et al., Hypertension, Supp. I, I-8, I-11 (1985), "Highly Potent and Specific Inhibitors of Human Renin".
R. Matsueda et al., Chemistry Letters 1041-1044 (1985), "Short Chain Peptide Inhibitors of Human Renin".
G. Hanson et al., Biochem. Biophys. Res. Commun. 132 155-161 (1985), "Dipeptide Glycols: A New Class of Renin Inhibitors".

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