| abstract |
Non-peptidyl compounds characterized generally as aminoalkylaminocarbonyl aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are of the formulan wherein X is selected from oxygen atom and methylene; wherein each of R 1 and R 9 is independently selected from hydrido, methyl, ethyl, t-butyloxycarbonyl; and methoxymethylcarbonyl; wherein R 2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R 3 is selected from benzyl, phenethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R 4 and R 6 is independently selected from hydrido and methyl; wherein R 7 is cyclohexylmethyl; wherein R 8 is isobutyl; wherein each of R 11 and R 12 is hydrido; wherein m is zero or one and n is a number selected from zero through five; or a pharmaceutically-acceptable salt thereof; with the proviso that where m is zero, then R s is selected from imidazolemethyl, thiazolemethyl and isobutyl; and with the further proviso that when m is one, then R s is methyl or ethyl. |