Pyripyropene derivatives having an acat2-inhibiting activity

Details Pyripyropene derivatives having an acat2-inhibiting activity Pyripyropene derivatives having an acat2-inhibiting activity

C - Chemistry, Metallurgy

07

D

C07D 493/04 (2006.01) A61K 31/4433 (2006.01) A61K 31/695 (2006.01) A61P 9/10 (2006.01) A61P 43/00 (2006.01) C07D 493/14 (2006.01) C07F 7/18 (2006.01)

Patent

CA 2710791

The present invention is a compound having the general formula (I), (II), or (III) or a pharmacologically acceptable salt, solvate, or hydrate thereof, and a pharmaceutical composition containing such a compound, or its pharmacologically acceptable ester, or other pharmacologically acceptable derivative thereof as an active ingredient. The compound has an excellent ACAT 2-inihibiting activity by a mechanism different from that of a statin drug and is useful as a therapeutic or prophylactic agent for obesity, adiposis, hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, and arteriosclerosis, as well as obesity-derived hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, arteriosclerosis, and hypertension. 1 1

L'invention porte sur un composé représenté par la formule générale (I), (II) ou (III), ou sur un sel, solvate ou hydrate acceptable, du point de vue pharmacologique, de celui-ci ; et sur une composition pharmaceutique comportant le composé ou le sel, solvate ou hydrate acceptable, du point de vue pharmacologique, de celui-ci comme ingrédient actif. Le composé présente une excellente activité inhibitrice d'ACAT2 et le mécanisme d'action du composé est différent de celui d'un agent pharmaceutique contenant de la statine. Par conséquent, le composé peut être utilisé comme agent thérapeutique ou prophylactique pour l'obésité ; l'adipose ; l'hyperlipémie ; l'hypercholestérolémie ; la dyslipidémie métabolique ; l'artériosclérose ; l'hyperlipémie, l'hypercholestérolémie, la dyslipidémie métabolique, l'artériosclérose ou l'hypertension induites par l'obésité ou autre.

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