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
1993-06-08
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514414, 548467, 548492, 548495, A61K 31405, C07D20912, C07D20914
Patent
active
052179885
ABSTRACT:
Non-peptidyl compounds characterized generally as indolyl/indolylalkyl-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 X is selected from ##STR3## 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:
patent: 5145845 (1992-09-01), Johnson et al.
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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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G. D. Searle & Co.
Keane J. Timothy
Matukaitis Paul D.
Richter Johann
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