Functionalized peptidyl aminodiols and -triols 4-amino-5-cyclohexyl-3-hydroxy-1,2-oxopentane and derivatives thereof

Abstract

Abstract The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; OR 8 or SR 8 wherein R 8 is hydrogen, loweralkyl or aminoalkyl; NR 9 R 10 wherein R 9 and R 10 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH 2 or CHOH and R 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 1 is loweralkyl, cycloalkylmethyl, benzyl, α-methylbenzyl, α, α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)-methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R 1 is phenoxy, thiophenoxy or anilino, B is CH 2 or CHOH or A is hydrogen; R 3 is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R 4 is lower-alkyl, cycloalkyl- methyl or benzyl; R 2 , R 5 and R 6 are independently hydrogen or loweralkyl; X is O, NH or S; R 7 is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl ##STR3## wherein R 12 and R 13 are independently hydrogen or loweralkyl, n is 0-2 and R 14 is substituted or unsubstituted phenyl or heterocyclic; or XR 7 together are loweralkylsulfonyl, N 3 or Cl, and pharmaceutically acceptable salts thereof.

Inventors

• 👤 Saul H. Rosenberg
• 👤 Jay R. Luly
• 👤 Jacob J. Plattner

Bibliographic Details