Quinolonyl/quinolonylalkyl-N-terminal cycloalkoxy-C-terminal ami

Details Quinolonyl/quinolonylalkyl-N-terminal cycloalkoxy-C-terminal ami Quinolonyl/quinolonylalkyl-N-terminal cycloalkoxy-C-terminal ami

1992-05-28

1993-06-29

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

546153, 546156, A61K 3147, C07D21536

Patent

active

052235122

ABSTRACT:
Non-peptidyl compounds characterized generally as quinolonyl/quinolonylalkyl-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:
Lazar et al., Biochem. Pharma., 23: 2776-2778 (1974).
Miller et al., Biochem. Pharma., 21: 2941-2944 (1972).
Haber, Clinical Science, 59: 7s-19s (1980).
Rich et al., J. Org. Chem., 43: 3624 (1978).
Rich et al., J. Med. Chem., 23: 27 (1980).
Haber, Clin. and Exper. Hyper., A5 (7&8), 1193 (1983).

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