Ethynyl-alanine aryl/alkylsulfonyl-terminated amino-diol compounds for treatment of hypertension

A pharmaceutical composition comprising a therapeutically-effective amount of a renin-inhibiting compound and a pharmaceutically-acceptable carrier or diluent, said renin-inhibiting compound selected from a family of compounds of Formula I:

• ##STR52## wherein R.sup.1 is selected from the group consisting of alkyl, trifluoromethyl, cycloalkyl, cycloalkylalkyl, aryl, haloaryl, aralkyl and haloaralkyl;
• wherein x is a number selected from the group consisting of zero, one and two;
• wherein R.sup.2 is selected from hydrido and alkyl;
• wherein R.sup.3 is selected from the group consisting of hydrido, cycloalkylalkyl, aralkyl and haloaralkyl;
• wherein each of R.sup.4 and R.sup.6 is independently selected from the group consisting of hydrido and methyl;
• wherein R.sup.5 is propargyl or a propargyl-containing moiety;
• wherein R.sup.7 is selected from the group consisting of alkyl, cycloalkylalkyl and aralkyl;
• wherein R.sup.8 is selected from the group consisting of hydrido, alkyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkenyl and haloalkenyl;
• and wherein any one of said R.sup.1 through R.sup.8 groups having a substitutable position may be substituted with one or more groups selected from alkyl, hydroxy, alkoxy and alkenyl.

A therapeutic method for treating hypertension, said method comprising administering to a hypertensive patient a therapeutically-effective amount of a compound of Formula I:

• ##STR54## wherein R.sup.1 is selected from the group consisting of alkyl, trifluoromethyl, cycloalkyl, cycloalkylalkyl, aryl, haloaryl, aralkyl and haloaralkyl;
• wherein x is a number selected from the group consisting of zero, one and two;
• wherein R.sup.2 is selected from the group consisting of hydrido and alkyl;
• wherein R.sup.3 is selected from the group consisting of hydrido, cycloalkylalkyl, aralkyl and haloaralkyl;
• wherein each of R.sup.4 and R.sup.6 is independently selected from the group consisting of hydrido and methyl;
• wherein R.sup.5 is propargyl or a propargyl-containing moiety;
• wherein R.sup.7 is selected from the group consisting of alkyl, cycloalkylalkyl and aralkyl;
• wherein R.sup.8 is selected from the group consisting of hydrido, alkyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkenyl and haloalkenyl;
• and wherein any one of said R.sup.1 through R.sup.8 groups having a substitutable position may be substituted with one or more groups selected from alkyl, hydroxy, alkoxy and alkenyl.