Glucopyranosyloxybenzylbenzene derivatives and medicinal use...

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 3/06 (2006.01) A61P 3/10 (2006.01) A61P 7/10 (2006.01) A61P 9/02 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01) A61P 19/06 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2437240

The present invention provides glucopyranosyloxybenzyl- benzene derivatives represented by the general formula: (see formula I) wherein P represents a hydrogen atom or a group forming a prodrug; R1 represents a hydrogen atom, an optionally substituted amino group, a carbamoyl group, an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkylthio group, etc., which have an improved oral absorption, and exert an inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, or pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

L'invention concerne des dérivés glucopyranosyloxybenzylbenzène représentés par la formule générale suivante (I) et des sels de ceux-ci pharmaceutiquement acceptables que l'on peut utiliser comme agents prophylactiques ou remèdes contre des maladies provoquées par l'hyperglycémie, par exemple les diabètes, les complications diabétiques et l'obésité du fait qu'ils présentent une meilleure absorbabilité orale et exercent une excellente action inhibitrice de l'activité SGLT2 humaine in vivo. P représente hydrogène ou un groupe formant un promédicament; R?1¿ représente hydrogène, amino éventuellement substitué, carbamoyle, alkyle inférieur éventuellement substitué, alcoxy inférieur éventuellement substitué, etc.; R?2¿ représente hydrogène ou alkyle inférieur; et R?3¿ représente alkyle inférieur éventuellement substitué, alcoxy inférieur éventuellement substitué, alkylthio éventuellement substitué, etc.

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