Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
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...
546122, 546123, A61K 31435, C07D47104
Patent
active
052159965
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 form hydrido, methyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
REFERENCES:
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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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