Benothiophenyl/benzothiophenylalkyl-N-terminal cycloalkoxy-C-ter

Details Benothiophenyl/benzothiophenylalkyl-N-terminal cycloalkoxy-C-ter Benothiophenyl/benzothiophenylalkyl-N-terminal cycloalkoxy-C-ter

1992-07-16

1993-06-08

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

549 51, 549 57, 549 58, A61K 3138, C07D33352, C07D33372

Patent

active

052179893

ABSTRACT:
Non-peptidyl compounds characterized generally as benzothiophenyl/benzothiophenylalkyl-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 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 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:
patent: 5145845 (1992-08-01), Johnson et al.
Umezawa et al, J. Antibiot. (Tokyo), 23, 259-262 (1970).
Gross et al, Science, 175, 656 (1971).
Boger et al, Nature, 303, 81-84 (1983).
Kokubu et al, Biochem. Biophys. Res. Commun., 118, 929-933 (1984).
Castro et al, FEBS Lett., 167, 273 (1984).
Hanson et al, Biochem. Biophys. Res. Commun., 132, 155-161 (1985) and 146, 959-963 (1987).

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