2-(3,5-di-tert-butyl-4-hydroxy-phenyl)-oxazoles as anti-atherosc

Details 2-(3,5-di-tert-butyl-4-hydroxy-phenyl)-oxazoles as anti-atherosc 2-(3,5-di-tert-butyl-4-hydroxy-phenyl)-oxazoles as anti-atherosc

1994-08-30

1996-02-13

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

548235, A61K 3142

Patent

active

054911591

ABSTRACT:
The earliest lesion of atherosclerosis is development of the fatty streak lesions which contain lipid-laden macrophages and lipid-laden smooth muscle cells. Macrophages do not take up native low density lipoprotein (LDL) but do take up modified, i.e., acetylated LDL or oxidized LDL via acetyl-LDL or "scavenger" receptors to form the foam cells of atherosclerotic plaque. Arterial smooth muscle cells generate superoxide and oxidize LDL in the presence of micromolar concentrations of Cu.sup.+2 or Fe.sup.+2. The way LDL can be modified by endothelial cells can be mimicked in vitro by incubation of the lipoprotein in the presence of CuCl.sub.2. The compounds of this invention inhibit copper mediated oxidation of LDL in vitro and are thus useful in the prophylaxis and treatment of clinical conditions for which inhibition of the oxidative modification of lipids is indicated, for example, atherosclerosis. The compounds of this invention are represented by the formula 1 below ##STR1## wherein: R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or naphthyl;

REFERENCES:
patent: 4636516 (1987-01-01), Kubo et al.
patent: 5344925 (1994-09-01), Goulet
patent: 5428048 (1995-06-01), Malamas et al.
Steinberg, American Journal of Cardiology 57, 16H-21H (Jun. 27, 1986).
Reaven et al., Arteriosclerosis and Thrombosis 12(3), 318-324 (1992).
Carew et al., Proc. Natl. Acad. Sci. USA 84, 7725-7729 (1987).

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