Glucopyranosyloxybenzylbenzene derivatives and medicinal...

C - Chemistry – Metallurgy – 07 – H

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C07H 15/203 (2006.01) A61K 31/7034 (2006.01) A61P 3/04 (2006.01) A61P 3/10 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2423568

The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: (see formula I) wherein P represents a group forming a prodrug; and R represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group or a lower alkoxy--substituted (lower alkylthio) group, which have an improved oral absorption and can exert an excellent inhibitory activity in human SGLT2 in vivo and which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutical compositions comprising the same.

L'invention concerne des dérivés de glucopyranosiloxybenzylbenzène représentés par la formule générale (I). Ces composés présentent une absorbabilité orale améliorée et exercent une action inhibitrice marquée de l'activité SGLT2 humaine <i>in vivo</i>. Par conséquent, ils sont utiles comme agents prophylactiques ou thérapeutiques destinés aux maladies causées par l'hyperglycémie, telles que le diabète, les complications du diabète et l'obésité. Dans la formule (I), P représente un groupe constituant un promédicament, et R représente alkyle inférieur, alcoxy inférieur, alkylthio inférieur, alcoxy inférieur alkyle inférieur, alcoxy inférieur alcoxy inférieur ou alcoxy inférieur alkylthio inférieur.

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