1-THIO-D-GLUCITOL DERIVATIVES Russian patent published in 2010 - IPC C07D335/02 C07D409/04 C07D409/10 C07D409/12 C07D409/14 C07D417/10 C07D495/04 A61K31/382 A61K31/404 A61K31/428 A61K31/4436 A61K31/497 A61K31/506 A61P3/10 

FIELD: chemistry.

SUBSTANCE: invention relates to novel 1-thio-D-glucitol compounds of formula I or to pharmaceutically acceptable salts thereof or hydrates of the compound or salts: , [where R¹, R², R³ and R⁴ are identical or different, and each is a hydrogen atom, C₁-C₆-alkyl group), A is -(CH₂)_n-, -CONH(CH₂)_n-, -O- or -(CH₂)_nCH=CH- (where n is an integer from 0 to 3, Ar¹ is an arylene group, heteroarylene group, which is an unsaturated 5-9-member mono- or bicyclic group, containing 1-2 heteroatoms, selected from S and N, Ar² is an aryl group or heteroaryl group which is an unsaturated 5-9-member mono- or bicyclic group containing 1-2 heteroatoms selected from O, S and N, and R⁵, R⁶, R⁷, R⁸, R⁹ and R¹⁰ are identical or different, and each is (i) a hydrogen atom, (ii) a halogen atom, (iii) a hydroxyl group, (iv) C_1-8-alkyl group, optionally substituted with hydroxyl group(s), (v) -(CH₂)m-Q {where m is an integer from 0 to 4, and Q is -CO₂H, -OR^c1, -CO₂R^a3, -SR^e1, -NHR^a6 or -NR^a7R^a7 (where each of R^a3, R^a6 and R^a7 is a C_1-6-alkyl group, R^c1 is a C_1-6-alkyl group, and R^c1 is a C_1-6-alkyl group)}, (vi) -O-(CH₂)m'-Q' {where m' is an integer from 1 to 4, and Q' is a hydroxyl group,-CO₂H, -CO₂R^a8, -CONR^a10R^a10, -NR^a12R^a12 (where each of R^a8, R^a10 and R^a12 is a C_1-6-alkyl group)}, (vii) -OR^f {where R^f is C_3-7-cycloalkyl group or tetrahydropyranyl group)}, (viii) morpholine group, (ix) phenyl group, (x) pyridyl group]. The invention also relates to 1-thio-D-glucitol compounds of formulae IA, II, III, IV, to a pharmaceutical agent, to methods of obtaining 1-thio-D-glucitol compounds, as well as to compounds of formulae XIII, XIV.

EFFECT: obtaining novel biologically active compounds which are inhibitors of sodium-dependent co-transporter-2-glucose.

25 cl, 140 ex, 3 tbl