Quinoxalinyl/quinoxalinylakyl-N- terminal cycloalkoxy-C- terminal amino hydroxy .beta.-amino acid derivatives
AssigneeG. D. Searle & Co.
InventorGunnar J. Hanson
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AssigneeG. D. Searle & Co.
InventorGunnar J. Hanson
Estimating the term…
Non-peptidyl compounds characterized generally as quinoxalinyl/quinoxalinylalkyl-N-terminal cycloalkoxy-C-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 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 and R.sub.7 are taken together to form a partially saturated or fully saturated heterocyclic ring containing five to eight ring members with one or two ring members being oxygen atoms and the remaining ring members being carbon atoms, and which heterocyclic ring may be optionally substituted with lower alkyl; or a pharmaceutically-acceptable salt thereof.
Compound of the formula ##STR28## wherein R.sub.1 is selected from heteroaryl and heteroaralkyl groups represented by ##STR29## 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 ##STR30## wherein R.sub.1 is selected from heteroaryl and heteroaralkyl groups represented by ##STR31## 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 ##STR32## wherein R.sub.1 is selected from heteroaryl and heteroaralkyl groups represented by ##STR33## 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.