SPIROKETAL DERIVATIVES AND USE THEREOF AS MEDICINAL AGENT AGAINST DIABETES Russian patent published in 2011 - IPC C07H19/01 A61K31/7048 A61K31/706 A61P3/10 

FIELD: chemistry.

SUBSTANCE: invention relates to a group of compounds of general formula (I) (where substitute Q-A is on a ring atom, which is separated by two atoms from the ring atom directly bonded to the substituted glucitol group), where R¹, R², R³ and R⁴ are each independently selected from hydrogen, -C(=O)Rx and alkyl, which can be substituted with one or more Ra, where Ra is phenyl and Rx is alkyl; Ar¹ is a benzene ring which can be substituted with alkyl or halogen, a thiophene ring or pyrazine ring; Q is -(CH₂)_m-(L)_p-; m is an integer from 0 to 2, n is equal to 1 or 2, p is equal to 0 or 1; L is -O-, A is a phenyl which can be substituted with one or more Rb, naphthyl or a 5-10-member aromatic heterocyclic group containing a nitrogen or sulphur atom; Rb is independently selected from alkenyl, alkynyl, halogen, hydroxyl, cyano group, carboxyl group, alkoxy group, which can be substituted with one or more Rc, phenyl, alkylthio group, alkylsulphonyl group, -NRfRg, alkylcarbonyl group, alkoxycarbonyl group, alkylenedioxy group, pyrazolyl group and tetrahydrofuranyloxy group; Re is independently selected from halogen, hydroxyl and phenyl; Rf is hydrogen and Rg is alkylcarbonyl, or pharmaceutically acceptable salts thereof. The invention also relates to a group of specific compounds having general formula (I). The invention also pertains to a group of intermediate compounds of compounds of general formula (Ib), which are used in synthesis of compounds of formula (Ia) (special case of formula I). The invention also relates to pharmaceutical compositions based on compounds of formula (I) for use as an inhibitor or Na⁺-glucose II cotransporter, as well as for use in preventing or treating diabetes, hyperglycemia, caused by hyperglycemia of diabetic complications, or obesity. The invention also relates to a method of preventing or treating diabetes caused by hyperglycemia of diabetic complications or obesity by administering a therapeutically effective amount of the compound of formula (I) to a patient.

EFFECT: high effectiveness of the compounds.

15 cl, 10 tbl, 48 ex