Benzothiophenyl benzothiophenylalkyl-N-terminal amino hydroxy .beta.-amino acid derivatives
AssigneeG. D. Searle & Co.
InventorsGunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
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AssigneeG. D. Searle & Co.
InventorsGunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
Estimating the term…
Non-peptidyl compounds characterized generally as benzothiophenyl/benzothiophenylalkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein X is sulfur atom; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; and wherein R.sub.7 is isobutyl or ethyl; or a pharmaceutically-acceptable salt thereof.
Compound of the formula ##STR27## wherein R.sub.1 is selected from heteroaryl and heteroaralkyl groups represented by ##STR28## wherein each of Y and Z is independently selected from hydrido, lower alkyl, hydroxy, halo, alkoxy, carboxy, amino, alkylamino, dialkylamino, aryl, sulfhydryl and thioalkyl;
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 the formula ##STR29## wherein R.sub.1 is selected from heteroaryl and heteroaralkyl groups represented by ##STR30## wherein each of Y and Z is independently selected from hydrido, lower alkyl, hydroxy, halo, alkoxy, carboxy, amino, alkylamino, dialkylamino, aryl, sulfhydryl and thioalkyl;
A therapeutic method for treating hypertension, said method comprising administering to a hypertensive patient a therapeutically-effective amount of a compound of the formula ##STR31## wherein R.sub.1 is selected from heteroaryl and heteroaralkyl groups represented by ##STR32## wherein each of Y and Z is independently selected from hydrido, lower alkyl, hydroxy, halo, alkoxy, carboxy, amino, alkylamino, dialkylamino, aryl, sulfhydryl and thioalkyl;
Dependencies are inferred from the claim text.