DERIVATIVES OF OXAZOLIDINE ANTIBIOTICS Russian patent published in 2014 - IPC C07D471/04 C07D413/14 C07D417/14 A61K31/4375 A61K31/5415 A61K31/4709 A61K31/498 A61P31/04 

FIELD: chemistry.

SUBSTANCE: invention relates to compound of formula I in which R¹ represents halogen, methoxy group or cyano group; each of Y¹ and Y² represents CH, and one or two from U, V, W and X represent N, and each remaining one represents CH, or in case X, cam also represent CR^a, or R^a represents halogen; A represents CH₂CH(OH), CH₂CH(NH₂), CH(OH)CH(NH₂) or CH(NH₂)CH₂, B represents CH₂CH₂, CH₂NH or CONH, and D represents CH₂, or A represents CH(OH)CH₂, and B represents CH₂NH, N(R²)CO or CONH, and D represents CH₂, or B represents N(R^2a)CH₂, and D represents CH(OH), or A represents CH(OH)CH(OH), B represents CH₂NH or CONH and D represents CH₂, or A represents CH₂CH₂, and B represents CH₂CH₂, CH₂NR³, NHCO, CONR⁴, CH₂O, COCH₂ or CH₂CH₂NH, and D represents CH₂, or B represents CH₂NH, and D represents CO, or A also represents CH₂CH₂, B represents NR^4bCH₂ and D represents CH(OH), or A represents CH=CH, B represents CH₂NR⁵ or CONR⁶, and D represents CH₂, or A represents C≡C, B represents CH₂NH and D represents CO, or A represents COCH₂, B represents CONH and D represents CH₂, or A represents CH₂N(R⁷), and B represents CH₂CH₂, a D represents CH₂, or B represents CH₂CH(OH), a D represents CH(OH), or A represents NHCH₂, and B represents CH₂NH, a D represents CH₂, or B represents CH₂NH, a D represents CO, or A represents NHCO, B represents CH(R⁸)NH or CH₂CH₂, and D represents CH₂, or A represents OCH₂, B represents CH=CH or CONH, and D represents CH₂; R² represents (C₁-C₄)alkyl; R^2a represents hydrogen; R³ represents hydrogen, CO-(CH₂)_p-COOR^3', (CH₂)_p-COOR³, (C₂-C₅)acyl or amino(C₁-C₄)alkyl, or also R³ represents (C₁-C₄₎alkyl, which can be one or two times substituted with hydroxygroup, p stands for integer number from 1 to 4, and R³ represents hydrogen or (C₁-C₄)alkyl; R⁴ represents hydrogen or (C₁-C₄)alkyl; R^4b represents hydrogen; R⁵ represents hydrogen or (C₂-C₅)acyl; R⁶ represents hydrogen or (C₁-C₄)alkyl; R⁷ represents hydrogen or (C₁-C₄)alkyl, which can be one or two times substituted with group, independently selected from hydroxygroup and aminogroup, R⁸ represents hydrogen or (C₁-C₄)alkyl; E represents one of the following groups (a-a1) where Z represents CH or N, and Q represents O or S, or E represents phenyl group, which is one or two times substituted in meta- and/or para-position with substituents, each of which is independently selected from group, including halogen, (C₁-C₃)alkyl and trifluoromethyl; or pharmaceutically acceptable salt of such compound. Formula I compound or its pharmaceutically acceptable salt is applied for obtaining medication or pharmaceutical composition for prevention or treatment of bacterial infection.

EFFECT: derivatives of oxazolidine antibiotics for obtaining medication for treatment of bacterial infections.

15 cl, 2 tbl, 214 ex