Aralkyl-N-terminal amino hydroxy

Details Aralkyl-N-terminal amino hydroxy Aralkyl-N-terminal amino hydroxy

1991-07-29

1993-01-19

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

514 19, 514535, 514539, 514542, 514521, 514522, 560 9, 560 13, 560 17, 560 39, 560 41, 560 43, 564154, 564155, 564157, 564158, 558393, 558408, 558409, 558412, 558414, 558415, 558416, A61K 3117, C07C23303, C07C23304, C07C23307

Patent

active

051807440

ABSTRACT:
Non-peptidyl compounds characterized generally as aralkyl-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; wherein R.sub.7 is isobutyl or ethyl; and wherein each of R.sub.8 and R.sub.9 is hydrido; or a pharmaceutically-acceptable salt thereof. g

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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