Cyclic diamine compound and pharmaceutical containing the same

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C544S368000

Reexamination Certificate

active

10763241

ABSTRACT:
The present invention relates to 2-[4-[2-(7-trifluoromethylbenzoxazol-2-ylthio)ethyl]piperazin-1-yl]-N-[4-hydroxy-2,6-bis(trifluoromethyl)phenyl]acetamide or salt thereof, and an intermediate for the preparation thereof.The above-described compound has both an inhibitory action on ACAT in the artery wall and remarkably high metabolic resistance in human liver microsomes, and exhibits excellent effects for suppressing lipids depression in aorta in vivo so that it is useful as a highly effective preventive or remedy for hyperlipidemia and arteriosclerosis with less side effects.

REFERENCES:
patent: WO 98/54153 (1998-12-01), None
patent: WO 03/018564 (2003-03-01), None
Kawaguchi et al. Chemical Abstracts, vol. 123, No. 222345 (1995) (Abstract for JP 07167862 (Jul. 4, 1995).
Vippagunta et al Advanced Drug Delivery Reviews, vol. 48, pp. 3-26 (2001).
P. J. Gillies, et al., Experimental and Molecular Pathology, vol. 44, pp. 329-339, “Regulation of Acyl-CoA: Cholesterol Acyltransferase Activity in Normal and Atherosclerotic Rabbit Aortas: Role of a Cholesterol Substrate Pool”, 1996.
L. Li, et al., Biochimica and Biophysica Acta, vol. 1530, pp. 111-122, “Effects of High-Density Lipoprotein2 on Cholesterol Transport and Acyl-Coenzyme A: Cholesterol Acyltransferase Activity in P388D1 Macrophages”, 2001.

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