Cycloalkyl/cycloalkylalkyl-N-terminal cycloalkoxy-C-terminal ami

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514451, 514452, 514467, 514471, 549346, 549347, 549372, 549375, 549378, 549379, 549416, 549417, 549419, 549425, 549426, 549449, 549450, 549452, 549474, 549475, 549476, 549478, 549479, 549492, 549493, A61K 3134, A61K 3135, C07D32110, C07D32112

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active

052179915

ABSTRACT:
Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylalkyl-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 cycloalkyl and cycloalkylalkyl groups, wherein said cycloalkyl group contains three to about eight carbon atoms and the acyclic alkyl portion of said cycloalkylalkyl group contains one to about eight carbon atoms; 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.

REFERENCES:
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Hanson et al, Biochem. Biophys. Res. Commun., 132, 155-161 (1985) and 146, 959-963 (1987).

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