Ester compound and medical use thereof

Details Ester compound and medical use thereof Ester compound and medical use thereof

C - Chemistry, Metallurgy

07

C

C07C 69/732 (2006.01) A61K 31/215 (2006.01) A61K 31/216 (2006.01) A61K 31/235 (2006.01) A61K 31/24 (2006.01) A61K 31/245 (2006.01) A61K 31/277 (2006.01) A61K 31/381 (2006.01) A61K 31/397 (2006.01) A61K 31/40 (2006.01) A61K 31/4015 (2006.01) A61K 31/404 (2006.01) A61K 31/4184 (2006.01) A61K 31/423 (2006.01) A61K 31/426 (2006.01) A61K 31/4402 (2006.01) A61K 31/4406 (2006.01) A61K 31/4418 (2006.01) A61K 31/4453 (2006.01) A61K 31/4468 (2006.01) A61K 31/5375 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P

Patent

CA 2460682

A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1") (see formula 1") (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is -COO- or -CON(R10)-; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R8 and R9 are each independently hydrogen atom, C1-C6 alkyl, -CON(R18)(R19) or -COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

L'invention porte sur un nouvel agent thérapeutique antikyperlipémie, composé d'esters, de formule générale (1"): [dans laquelle: R?1¿ et R?2¿ sont chacun hydrogène, aryle facultativement substitué, etc.; X est -COO- ou -CON(R?10¿)-; R?3¿ et R?4¿ sont chacun hydrogène, C¿1-6? alkyle, C¿1-6? alkoxy, etc.; R?5¿, R?6¿, et R?7¿ sont chacun hydrogène, C¿1-6? alkyle, C¿1-6? alkoxy, etc.; R?8¿ et R?9¿ sont identiques ou différents et chacun hydrogène, C¿1-6? alkyle, -CON(R?18¿)(R?19¿), -COO(R?20¿), etc.; les cycles A, B, et C sont identiques ou différents et chacun aryle, un résidue hétérocyclique, etc.; Alk?1¿ et Alk?2¿ sont identiques ou différents et chacun alkanediyle, etc.; et l et m sont chacun un entier de 0 à 3]. L'invention porte en outre sur un promédicament de composés d'esters ou ses sels pharmacocompatibles. Ledit agent thérapeutique inhibe sélectivement la MTP dans l'intestin grèle sans présenter d'effets secondaires tels que la stéatose hépatique.

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