Substituted oxazolidinone and their use as antibacterial medicine

摘要

Substituted oxazolidinone compounds of formula (I) and their salts are new. A = 6-membered aromatic heterocycle (containing at least one N and which is linked via C), a 6-membered, bi- or tricyclic aromatic heterocycle (containing at least one N and which is linked via C), beta -carbolin-3-yl, indolizinyl (linked via the 6-membered ring), or a 5-membered aromatic heterocycle (containing up to 3 N, O and/or S, which may also be fused to a benzene or naphthalene ring, and which is linked via C), all of these cyclic groups being optionally substituted by (a) 1-3 COOH, halo, CN, mercapto, CHO, pyridyl, phenyl, CF3, NO2, TO, T', TS or Ac, or (b) T or 2-6C alkenyl (themselves optionally substituted by phenyl); or a group of formula (i)-(iv): R<3>-R<7> = H, COOH, halo, CN, CHO, CF3, NO2, T or CONR<13>R<14>; R<13>, R<14> = H, 1-4C alkyl or phenyl; R<2>, R<8>-R<12> = H, 3-6C cycloalkylcarbonyl, 3-6C cycloalkyl, T', or 1-10C alkyl (optionally substituted by CN, CF3, halo, phenyl, OH, COOH, T', 6-10C aryl, 3-6C cycloalkyl, (CO)cNR<15>R<16>, R<17>-NH-SO2-R<18>, R<19>R<20>NSO2 or R<21>S(O)d); c = 0 or 1; R<15>-R<17> = H, 1-4C alkyl or phenyl; or together with the nitrogen atom, these groups form a 5-6 membered saturated heterocycle which optionally contains a further N, O or S heteroatom, and which is optionally substituted on C or N by 1-3C alkyl or 1-3C acyl; R<19>, R<20> = H, 1-4C alkyl or phenyl; d = 0-2; R<18>, R<21> = 1-4C alkyl, benzyl, phenyl, tolyl, or 1-6C acyl (optionally substituted by CF3, CCl3 or OR<22>); R<22> = H, T (optionally substituted by aryl containing up to 10C), or (CO)eNR<23>R<24>, NR<25>-SO2R<26>, R<27>R<28>NSO2 or R<29>-S(O)f; e = 0 or 1; R<23>-R<25> = as R<15>-R<17>; R<27>, R<28> = H, 1-4C alkyl or phenyl; f = 0-2; R<26>, R<29> = as R<18>, R<21>; D = O or S(O)g; g = 0-2; E, L = O or S; G, M, T, Q = O, S or NR<30>; R<30> = H or 1-5C alkyl; a, b = 1 or 2; R<1> = C(=S)R<31>, C(=NR<32>)R<33>, C(=O)-(CH2)hOR<34>, CN, a group Q or C(R<36>)=C(R<35>)NO2: R<31> = 1-7C alkyl, 3-6C cycloalkyl, phenyl or NR<38>R<39>; R<38>, R<39> = H, 1-4C alkyl or phenyl; R<32> = H, CN, 3-6C cycloalkyl, phenyl or 1-7C alkyl; R<33> = H, 1-7C alkyl, phenyl, 3-6C cycloalkyl, or NR<40>R<41>; R<40>, R<41> = H, 1-4C alkyl or phenyl; h = 1-4; R<34> = T or benzyl; R<35>, R<36> = H or T; Q = a 5-7 membered, saturated, partially unsaturated, or unsaturated heterocycle, containing up to 3 heteroatoms (selected from N, O and/or S) and which is optionally substituted on C or N by benzyl, halo or 1-5C alkyl; T =1-6C alkyl; T' = 1-6C alkoxycarbonyl; and Ac = 1-6C acyl.