Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1991-07-29
1992-12-15
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514469, 549466, 549467, A61K 3134, C07D30778
Patent
active
051717514
ABSTRACT:
Non-peptidyl compounds characterized generally as benzofuran/benzofuranalkyl-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 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).
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Baran John S.
Hanson Gunnar J.
Russell Mark
Weissing Dave
G. D. Searle & Co.
Keane J. Timothy
Matukaitis Paul D.
Richter Johann
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