.alpha.-phosphonosulfinic squalene synthetase inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

514 76, 514 89, 514100, 546 22, 549220, 558177, 562 23, A61K 3166, C07F 938, C07F 940

Patent

active

054479223

ABSTRACT:
.alpha.-Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is alkyl, arylalkyl or aryl; R.sup.4 is H or pharmaceutically acceptable cation;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts.

REFERENCES:
patent: 2965665 (1960-12-01), Gaertner et al.
patent: 3595880 (1971-07-01), Firestone
patent: 3657282 (1972-04-01), Christensen et al.
patent: 4032521 (1977-06-01), Christensen et al.
patent: 4254215 (1981-03-01), Kramp et al.
patent: 4696693 (1987-09-01), Swerdloff et al.
patent: 4795815 (1989-01-01), Ternansky
patent: 5011938 (1991-04-01), Barnett et al.
Burton, D. J., J. Am. Chem. Soc. 1989, 111, 1773-1776.
Su, D. et al, Can. J. Chem. 1989, 67, 1795-1799.
Farrington, G. K., et al, J. Med. Chem. 1985, 28, 1668-1673.
Musicki, B. et al, T. S. Tetrahedron Lett. 1991, 32, 1267-1270.
Carretero, J. C. et al, Tetrahedron 1987, 43, 5125-5134.
Callahan, L. et al, Analytical biochemistry 1989, 177, 67-71.
Amin, Dilip et al, "Bisphosphonates used for the treatment of bone disorders inhibit squalene sythase and cholesterol biosynthesis", Journal of Lipid Research, vol. 33, 1993, pp. 1657-1663.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

.alpha.-phosphonosulfinic squalene synthetase inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with .alpha.-phosphonosulfinic squalene synthetase inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and .alpha.-phosphonosulfinic squalene synthetase inhibitors will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-472856

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.