Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-08-14
1994-03-29
Bernhardt, Emily
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514249, 544349, 544383, 544384, 544385, 544386, 544387, 544388, 544400, 560 29, 560115, 564453, A61K 31495, C07D29518, C07D295145, C07D48708
Patent
active
052985059
ABSTRACT:
Compounds characterized generally as ethynyl alanine amino diol compounds having a piperazinyl-terminated or a piperazinyl-alkylamino-terminated group and derivatives thereof are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein G is a piperazinyl group or is a piperazinyl-containing group of Formula II: ##STR2## wherein B is a piperazinyl group or a alkylene-bridged-piperazinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR3## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
REFERENCES:
patent: 4902706 (1990-02-01), Hanson et al.
patent: 5032577 (1991-07-01), Fung et al.
patent: 5036053 (1991-07-01), Himmelsbach et al.
patent: 5223535 (1993-06-01), Hanson et al.
patent: 5227401 (1993-07-01), Hanson et al.
Hanson et al, Biochm. Biophys. Res. Comm., 132, pp. 155-161 (1985).
Hanson et al, Biochm. Biophys. Res. Comm., 146, pp. 959-963 (1987).
Umezawa et al, in J. Antibiot. (Tokyo), 23, 259-262 (1970).
Gross et al, Science, 175, 656 (1971).
Boger et al, Nature, 303, 81 (1983).
Kokubu et al, Biochm. Biophys. Res. Commun., 118, 929 (1984).
Castro et al, FEBS Lett., 167, 273 (1984).
Bernhardt Emily
G. D. Searle & Co.
Keane J. Timothy
LandOfFree
Ethynyl alanine amino diol compounds having a piperazinyl-termin does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Ethynyl alanine amino diol compounds having a piperazinyl-termin, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Ethynyl alanine amino diol compounds having a piperazinyl-termin will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-792022