Azachromonyl/azachromonylalkyl-N-terminal cycloalkoxy-C-terminal

Details Azachromonyl/azachromonylalkyl-N-terminal cycloalkoxy-C-terminal Azachromonyl/azachromonylalkyl-N-terminal cycloalkoxy-C-terminal

1992-07-16

1994-03-01

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

546116, A61K 3135, C07D47104

Patent

active

052907872

ABSTRACT:
Non-peptidyl compounds characterized generally as azachromonyl/azachromonylalkyl-N-terminal cycloalkoxy-C-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 and R.sub.7 are taken together to form a partially saturated or fully saturated heterocyclic ring containing five to eight ring members with one or two ring members being oxygen atoms and the remaining ring members being carbon atoms, and which heterocyclic ring may be optionally substituted with lower alkyl; 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, 173 (1984).
Hanson et al, Biochem. Biophys. Res. Commun., 132, 155-161 (1985) and 146, 959-963 (1987).

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