Imidazolyl/imidazolylalkyl-N-terminal cycloalkoxy-C-terminal ami

Details Imidazolyl/imidazolylalkyl-N-terminal cycloalkoxy-C-terminal ami Imidazolyl/imidazolylalkyl-N-terminal cycloalkoxy-C-terminal ami

1992-05-28

1993-07-27

Brust, Joseph Paul

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

5483111, 5483154, A61K 31415, C07D40712

Patent

active

052311112

ABSTRACT:
Non-peptidyl compounds characterized generally as imidazolyl/imidazolylalkyl-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 imidazolyl or imidazolylmethyl; 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.

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Castro et al, FEBS Lett., 167, 273 (1984).
Hanson et al, Biochm. Biophys. Res. Comm., 132:155-161 (1985), 146:959-963 (1987).

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