Aralkyl-N-terminal cycloalkoxy-C terminal amino hydroxy .beta.-a

Details Aralkyl-N-terminal cycloalkoxy-C terminal amino hydroxy .beta.-a Aralkyl-N-terminal cycloalkoxy-C terminal amino hydroxy .beta.-a

1992-07-16

1993-06-01

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514451, 514452, 514467, 514471, 549346, 549347, 549372, 549375, 549378, 549379, 549416, 549417, 549419, 549425, 549426, 549449, 549450, 549452, 549474, 549475, 549476, 549478, 549479, 549492, 549493, A61K 3134, A61K 3135, C07D32110, C07D32112

Patent

active

052160130

ABSTRACT:
Non-peptidyl compounds characterized generally as heterocyclic acyl aminodiol .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are compounds of the formula ##STR1## wherein R.sub.1 is selected from aryl and aralkyl groups represented by ##STR2## and wherein R.sub.1 may be further selected from heteroaryl and heteroaralkyl represented by ##STR3## wherein each of T and A is independently selected from N and CH; wherein n is a number selected from zero through five, inclusive; wherein X is selected from oxygen atom, methylamino and NH; wherein each of Y and Z is independently selected from chloro, fluoro, methoxy and dimethylamino; wherein Q is oxygen atom; and wherein each of T and A is independently selected from N and CH; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is selected from methyl and ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; wherein R.sub.7 is selected from isobutyl and ethyl; wherein each of R.sub.8 and R.sub.9 is independently selected from hydrido, methyl and isopropyl; or a pharmaceutically-acceptable salt thereof;

REFERENCES:
patent: 5145845 (1992-09-01), 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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