DERIVATIVES OF CHINOLINESULPHONAMIDES AND THEIR APPLICATION FOR MODULATION OF PKM2 ACTIVITY Russian patent published in 2015 - IPC C07D401/12 C07D401/14 C07D403/12 C07D403/14 C07D405/14 C07D409/14 C07D417/14 A61K31/47 A61K31/4709 A61K31/496 A61P35/00 A61P3/10 A61P9/00 

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to heterocyclic compounds of general formula (I) and to their pharmaceutically acceptable salts, where each W, X, Y and Z represents CH; each W, X and Y represents CH and Z represents N or each W, X and Z represents CH and Y represents N; D and D¹ are independently selected from bond or NR^b; A represents chinolinyl; L is bond, -C(O)-, -(CR^cR^c)_m-, -OC(O)-, -(CR^cR^c)_m-OC(O)-, -(CR^cR^c)_m-C(O)-, -NR^bC(S)- or -NR^bC(O)- (where point of binding to R¹ is on the left side); R¹ is selected from C₁-C₆ alkyl, C₃-C₆ cycloalkyl, aryl (where aryl represents phenyl or naphthyl), heteroaryl (where heteroaryl represents 5-10-membered mono- or bicyclic aromatic ring with 1-3 heteroatoms, selected from nitrogen and sulphur) and heterocyclyl (where heterocyclyl represents tetrahydrofuranyl or azetidinyl) each of which is substituted with 0-5 substituents R^d; each R³ is independently selected from halo-C₁-alkyl, C₁-C₆ alkyl, hydroxyl and -OR^a; each R^a is independently selected from C₁-C₆ alkyl and acyl (where acyl represents -C(O)CH₃), hydroxy-C₁-C₂ alkyl; each R^b is independently selected from hydrogen and C₁-C₆ alkyl; each R^c is independently selected from hydrogen, C₁-C₆ alkyl or two R^c, taken together with atoms of carbon, which they are bound to, form C₃-cycloalkyl; each R^d is independently selected from halo-C₁-alkyl, halo-C₁-alkoxy, C₁-C₆ alkyl, C₂-C₆ alkinyl, cyano, hydroxyl, -C(O)R^a, -OC(O)R^a, -C(O)OR^a, -SR^a, -NR^aR^b and -OR^a; n equals 0 or 1; m equals 1, 2 or 3; h equals 1 or 2 and g equals 1. Invention also relates to particular compounds, pharmaceutical composition, based on formula (I) compound and method of modulating PKM2 activity.

EFFECT: novel heterocyclic compounds, useful for modulating PKM2 activity, have been obtained.

46 cl, 1 dwg, 2 tbl, 2 ex