Quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal ami

Details Quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal ami Quinolinyl/quinolinylalkyl-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...

546169, 546171, 546175, A61K 3147, C07D21538

Patent

active

052235149

ABSTRACT:
Non-peptidyl compounds characterized generally as quinolinyl/quinolinylalkyl-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., in 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).
Marshall, Federation Proc., 35: 2494-2501 (1976).
Burton, et al., Proc. Natl. Acad. Sci. USA, 77: 5476-5479 (1980).
Suketa et al., Biochemistry, 14: 3188 (1975).
Swales, Pharmac. Ther., 7: 173-201 (1979).
Kokubu et al., Nature, 217: 456-457 (1968).
Matsushita et al., J. Antibiotics, 28: 1016-1018 (1975).
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).

Affiliated with

Also associated with

Rating

Quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal ami does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal ami, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal ami will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1755682