C-ARYLGLUCOSIDE INHIBITORS OF SGLT-2 Russian patent published in 2005 - IPC

FIELD: organic chemistry, biochemistry, medicine.

SUBSTANCE: invention proposes compounds inhibiting activity of enzyme SGLT-2 of the formula (I)

wherein R¹, R² and R^2a mean independently hydrogen atom, hydroxyl (OH), OR⁵, alkyl, CF₃, -OCHF₂, -OCF₃, CR⁵ⁱ or halogen atom, or two radicals among R¹, R² and R^2a in common with adjacent carbon atoms can form annelated 5-membered heterocycle; R³ and R⁴ mean independently hydrogen atom, OH, OR⁵, O-aryl, OCH₂-aryl, alkyl, cycloalkyl, CF₃, -OCHF₂, -OCF₃, halogen atom, -CN, -CO₂R^5b, - CO₂H, -CONR⁶R^6a, -NHCOR^5c, -NHSO₂R_5d, -NHSO₂-aryl, aryl, -SR^5c, -SOR^5f, -SO₂R^5g, -SO₂-aryl, or 5-, 6- or 7-membered carbocycle or heterocycle; R⁵, R^5a, R^5b, R^5c, R^5d, R^5e, R^5f, RR^5g, R^5h and R⁵ⁱ means independently alkyl; R⁶, R^6a, R^6b, R^6c and R^6d mean independently hydrogen atom, alkyl, aryl, alkylaryl or cycloalkyl, or R⁶ and R^6a in common with adjacent nitrogen atoms form annelated 5-, 6- or 7-membered heterocycle; A means oxygen (O), sulfur (S) atom, NH or (CH₂)_n wherein n = 0-3. Also, invention proposes a method for treatment of diabetes mellitus and related diseases by using the above described compound in doses inhibiting activity of SGLT-2 taken as a single substance or in combination with other therapeutic agents.

EFFECT: valuable medicinal and biochemical properties of inhibitors.

19 cl, 2 tbl, 82 ex