.alpha.-phosphonosulfonate squalene synthetase inhibitors and me

Organic compounds -- part of the class 532-570 series – Organic compounds – Phosphorus acids or salts thereof

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

544232, 544243, 544244, 546 22, 546 23, 548112, 548113, 549218, 549220, C07F 938

Patent

active

055678416

ABSTRACT:
.alpha.-Phosphonosulfonate 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 H, alkyl, arylalkyl or aryl; R.sup.4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, 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 and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.

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

Rate now

     

Profile ID: LFUS-PAI-O-2359645

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