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    • 6. 发明专利
    • BENZOXAZOLYLOXAZOLIDINONES AND BENZOTHIAZOLYLOXAZOLIDINONES, PROCESS OF THEIR PREPARATION AND USE FOR PREPARING MEDICAMENTS
    • CZ198895A3
    • 1996-02-14
    • CZ198895
    • 1995-08-02
    • BAYER AG
    • HABICH DIETER DRRIEDL BERND DRRUPPELT MARTIN DRSTOLLE ANDERAS DRWILD HANNO DRENDERMANN RAINER DRBREMM KLAUS DIETER DRKROLL HEIN PETER DRLABISCHINSKI HARALD PROF DRSCHALLER KLAUS DRWERLING HANS OTTO DR
    • C07D491/113A61K31/42A61K31/423A61K31/425A61K31/44A61K31/445A61K31/495A61K31/496A61K31/505A61K31/535A61K31/5377A61K31/55A61P31/04C07D247/02C07D263/38C07D263/56C07D263/58C07D413/04C07D417/04C07D417/12C07D417/14C07D419/12C07D491/10
    • Benzoxazolyl and benzothiazolyloxazolidinone derivs. of formula (I) and their salts are new. A = O or S(O)a; a = 0-2; R = azido or OSO2R or NR R ; R = H, formyl, carboxy, opt. branched ≤ 6C alkoxy-carbonyl; or is alkenyl or alkenyl of ≤ 8C (which are opt. substd. by OH, halo, or by alkoxy, acyl, alkylthio or alkoxycarbonyl each of ≤ 6C or phenyl which in turn may be substd by halo), 6-10C aryl (opt. substd. with carboxy, halogen, CN, formyl, CF3, NO2, 1-6C alkoxy, 1-6C alkoxycarbonyl, 1-6C alkylthio, 1-6C acyl or 1-6C alkyl), or is NR R , OR , S(O)cR , morpholino or a gp. of formula (a)-(h). R = 1-4C alkyl or Ph (opt. substd. with 1-4C alkyl); R and R = each 3-6C cycloalkyl, H, Ph, 1-8C alkyl or an amino protecting gp; or R or R = COR ; R = 3-6C cycloalkyl, 1-8C alkyl, 1-8C alkoxy, Ph or H; G, L and M = each H, COOH, halogen, CN, formyl, CF3, NO2, 1-6C alkoxy, 1-6C alkoxy-carbonyl, 1-6C alkylthio, 1-6C acyl, 1-6C alkyl (this last opt. substd. with OH , 1-5C alkoxy, 1-5C acyl or NR R ), NR 'R ', 2-8C alkyl phenyl, Ph or a 5-6 membered opt. satd. heterocycle contg. up to 3 heteroatoms chosen from S, N and/or O and opt. itself substd. with CONR R , NR R , NR SO2R , R R N-SO2 or R S(O)b; and/or G, L and M are opt. mono- or di- substd. with carboxy, halogen, CN, formly, CF3, NO2 Ph 1-6C alkoxy, 1-6C alkoxycarbonyl, 1-6C alkylthio, 1-6C acyl, 1-6C alkyl (this last itself opt. substd. with OH, 1-5C alkoxy, 1-5C acyl or NR R ); R and R = each H, 1-4C alkyl or Ph or together with the N to which they are attached form a 5-6 membered satd. heterocycle contg. a further heteroatom chosen from N, S and/or O and opt. substd. on one of the further N with 1-3C alkyl or acyl and/or R and R = NR 'R ', R ' and R ' = as defined for R and R . b = 0-2; R , R , R , R and R = each H, 1-6C alkyl or Ph; R , R 2, R and R = each as defined for R and R ; R and R = each as defined for R ; R = 3-6C cycloalkyl, Ph, 1-6C acyl, 1-8C alkyl (opt. substd. with OH, alkoxy or OH-substd. 1-6C alkoxy, a 5-6 membered aromatic heterocycle contg up to 3 heteroatoms chosen from S, N and/or O or with Ph (itself opt. substd. with OH, CF3, halogen, NO2 or 1-4C alkyl) or alkyl opt. substd. with NR R or a gp. of formula (i)) R = a gp of formula (j) R = OH, 1-4C alkoxy or NR R R and R = each H, 1-5C alkyl, 3-6C cycloalkyl or Ph; R = H 1-7C alkyl (opt. substd. with indolyl, OH, SH, imidazolyl, methylthio, amino, Ph, OH-substd. Ph, CONH2 CO2H or C(NH2)=NH; d = 0-6; T = O, CH2 or NR ; R = H, Ph, 1-6C alkyl (opt. substd. with OH); R = as defined for R or H; R = 1-8C alkyl (opt. substd. with 1-6C alkoxy or OH- or 1-6C alkoxy-substd. 1-6C alkoxy, 3-6C cycloalkyl or a 6-membered aromatic, opt. benzo condensed heterocycle contg. up to 4 N whichis itself opt. mono- or di-substd. with NO2, CF3, halogen, CN, OH, 1-5C alkyl, 1-5C alkoxy or 1-5C acyl; R = a gp of formula (l), Ph or pyridyl; e = as defined for (d) W = as defined for T; C = 0-2; R = 1-16C alkyl or alkenyl (opt. substd. with 1-6C alkoxycarbonyl, Ph or a 5-7 membered aromatic heterocycle contg 1-3 heteroatoms chosen from S, N and O) or 6-10C aryl or 1 5-7 membered aromatic heterocycle contg 1-3 heteroatoms chosen from S, N and O (these cycles being opt. mono or di-substd. with carboxy, halogen, CN, formyl, CF3, NO2, 1-6C alkoxy, 1-6C alkoxy-carbonyl, 1-6C alkylthio, 1-6C acyl or 1-6C alkyl); R and R = as defined for R and R ; R and R together form O or R and R = each H, OH or 1-6C alkyl / opt. substd. with NR R ; f = 0-1; g = 0-6; R = 6-10C acyl or a 5-6 membered aromatic opt. benzo-condensed heterocycle contg. up to 3 heteroatoms chosen from S, N and O (all ring system being opt. mono-, di- or tri-substd. with NO2, CN, OH, Ph, halogen, CF3, 1-5C alkyl, 1-5C alkoxy or 1-5C acetyl (sic)) or morpholino, OH, 1-6C alkoxy, NR R , COR or a gp. of formula (l); R and R = each as defined for R and R ; R = morpholino, OH or 1-6C alkoxy; R and R = each H, Ph, 1-6C alkyl or benzyl; R , R and R = as defined for R ; l = 1-2.