Ethynyl-alanine-amino-diol compounds for treatment of hypertension.

摘要

Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I <CHEM> wherein A is selected from CO and SO<6> wherein X is selected from oxygen atom and methylene; wherein each of R<5> and R¦ is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R<5> and R¦ are attached may be combined with oxygen to form an N-oxide; wherein R<6> is selected from hydrido, methyl, ethyl and isopropyl; wherein R<7> is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R psi is propargyl or a propargyl-containing moiety; wherein R1/2 is cyclohexylmethyl; wherein each of R<8> and R1/4 is independently selected from hydrido and methyl; wherein R3/4 is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R<5><5> and R<5><6> is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.