The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: ##STR00001## wherein R.sup.1 represents a hydrogen atom or a hydroxy(lower alkyl) group; and R.sup.2 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a hydroxy(lower alkyl) group, a hydroxy(lower alkoxy) group, a hydroxy(lower alkylthio) group etc., and salts thereof, which have an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, obesity etc., and intermediates thereof.