摘要 |
<p>The invention relates to renin inhibiting compounds of the formula <CHEM> wherein A is hydrogen; loweralkyl; arylalkyl; OR8 or SR8 wherein R8 is hydrogen, loweralkyl or aminoalkyl; NR9R10 wherein R9 and R10 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; <CHEM> wherein B is NH, alkylamino, S, O, CH2 or CHOH and R11 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; R1 is loweralkyl, cycloalkylmethyl, benzyl, alpha -methylbenzyl, alpha , alpha -dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R1 is phenoxy, thiophenoxy or anilino, B is CH2 or CHOH or A is hydrogen; R3 is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R4 is loweralkyl, cycloalkyl- methyl or benzyl; R2, R5 and R6 are independently hydrogen or loweralkyl; X is O, NH or S; R7 is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl. <CHEM> wherein R12 and R13 are independently hydrogen or loweralkyl, n is 0-2 and R14 is substituted or unsubstituted penyl or heterocyclic; or XR7 together are loweralkylsulfonyl, N3 or Cl, and pharmaceutically acceptable salts thereof.</p> |