Biphenyl derivatives

Details Biphenyl derivatives Biphenyl derivatives

C - Chemistry, Metallurgy

07

C

C07C 275/30 (2006.01) A61K 31/166 (2006.01) A61K 31/167 (2006.01) A61K 31/17 (2006.01) A61K 31/18 (2006.01) A61K 31/41 (2006.01) A61K 31/54 (2006.01) A61P 3/06 (2006.01) A61P 9/10 (2006.01) A61P 43/00 (2006.01) C07C 311/09 (2006.01) C07C 311/60 (2006.01) C07D 257/04 (2006.01)

Patent

CA 2434228

Biphenyl derivatives represented by the following formula (1): (see formula 1) wherein R1 represents a C5-7 alkyl group, R2 represents a substituted or unsubstituted aromatic hydrocarbon, or cycloalkyl group, R3 represents a tetrazolyl group, -NHCOCF3, -NHSO2CF3 or -SO2NHCONHR4 in which R4 represents a substituted or unsubstituted aromatic hydrocarbon group, and Z represents a single bond, a C1-4 alkylene group or --SO2NH-, and salts thereof; and ACAT inhibitors and medicines containing them as active ingredients. The compounds according to the present invention possess excellent ACAT inhibitory activities, and are useful as preventives and/or therapeutics for diseases cased by the enhancement of ACAT activity, for example, hypercholesterolemia, atherosclerosis and the like.

L'invention concerne des dérivés de biphényle représentés par la formule générale (1) ou leurs sels, ainsi que des inhibiteurs ou médicaments ACAT les contenant en tant qu'ingrédient actif. [R<1> représente C5-7 alkyle; R<2> représente éventuellement un hydrocarbyle ou cycloalkyle aromatique substitué; R3 représente tétrazolyle, -NHCOCF3, -NHSO2CF3, ou SO2NHCONHR<4> (R<4> représentant éventuellement un hydrocarbyle aromatique substitué); et Z représente une liaison simple, C1-4 alkylène, ou SO2NH-]. Ces dérivés et sels, qui présentent une excellente activité inhibitrice, sont utilisés comme médicaments de prévention et/ou thérapeutiques contre des maladies dues à l'augmentation de l'activité ACAT, par exemple l'hypercholestérolémie et l'athérosclérose.

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