Benzimidazole derivatives and medical uses thereof

Details Benzimidazole derivatives and medical uses thereof Benzimidazole derivatives and medical uses thereof

C - Chemistry, Metallurgy

07

H

C07H 19/052 (2006.01) A61K 31/7056 (2006.01) A61P 13/12 (2006.01) A61P 19/06 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2550441

The invention provides benzimidazole derivatives represented by the general formula (I) or pharmacologically acceptable salts or prodrugs thereof which exhibit inhibitory activities against sodium-dependent nucleoside transporter 2 and are efficacious against diseases caused by abnormality in plasma uric acid level: (I) (wherein n is 1 or 2; R1 and R2 are each H, halogeno, cyano, optionally substituted alkyl, optionally substituted aryl, or the like; R3 is H, halogeno, optionally substituted alkyl, or the like; R4 and R5 are each H, halogeno, OH, or the like; R6 and RX are each H or OH; and RY is F or OH). The compounds are useful in the prevention or treatment of gout, hyperuricemia, urolithiasis, hyperuricemic nephropathy, and so on.

La présente invention concerne des dérivés benzimidazole représentés par la formule générale (I), ou certains de leurs sels ou promédicaments pharmaceutiquement admis. Présentant des acitivités inhibitrices contre le transporteur nucléoside 2 sodium-dépendant, ils sont efficaces contre des maladies imputables à une anomalie du niveau d'acide urique du plasma. Dans cette formule (I), n vaut 1 ou 2; R?1¿ et R?2¿ sont chacun H, halogéno, cyano, alkyle éventuellement substitué, aryle éventuellement substitué, ou analogue; R?3¿ est H, halogéno, alkyle éventuellement substitué, ou analogue; R?4¿ et R?5¿ sont chacun H, halogéno, OH, ou analogue; R?6¿ et R<SP>X</SP> sont chacun H ou OH; enfin R<SP>Y</SP> est F ou OH. Ces composés conviennent particulièrement pour la prévention ou le traitement de la goutte, de l'hyperuricémie, de l'urolithiase, de la néphropathie hyperuricémique, etc.

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