Benzothiophenyl benzothiophenylalkyl-N-terminal amino hydroxy .b

Details Benzothiophenyl benzothiophenylalkyl-N-terminal amino hydroxy .b Benzothiophenyl benzothiophenylalkyl-N-terminal amino hydroxy .b

1991-08-02

1993-05-18

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

549 57, 549 58, A61K 3138, C07D33356

Patent

active

052121755

ABSTRACT:
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.

REFERENCES:
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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