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    • 6. 发明专利
    • DE19544106A1
    • 1996-10-24
    • DE19544106
    • 1995-11-27
    • BAYER AG
    • STOLLE ANDREAS DRHAEBICH DIETER DRBARTEL STEPHAN DRRIEDL BERND DRRUPPELT MARTIN DRWILD HANNO DRENDERMANN RAINER DRBREMM KLAUS-DIETER DRKROLL HEIN-PETER DRLABISCHINSKI HARALD PROFSCHALLER KLAUS DRWERLING HANS-OTTO DR
    • A61K31/425C07D263/58C07D413/04C07D413/06C07D413/14C07D417/04C07D417/14C07D419/04C07F9/6558C07F9/6584C07D291/08C07F9/6581C07F9/6564C07F9/6539A61K31/42
    • A compound of formula (I) and its interchangeable isomeric form, isomer and salts thereof: wherein R1 represents triazo, hydroxyl, or formula-OR2, O-SO2R3 or -NR4R5 groups, in which R2 represents straight or branched acyl having no more than 8 carbon atoms, or hydroxyl protected groups, R3 represents straight or branched alkyl having no more than 4 carbon atoms, or phenyl substitutable by straight or branched alkyl having no more than 4 carbon atoms, R4 and R5 are the same or different from each other and represent cycloalkyl having 3-6 carbon atoms, hydrogen, phenyl, straight or branched alkyl having no more than 8 carbon atoms or alkoxy or amino protected group, or R4 or R5 represents -CO-R6, P(O)(OR7)(OR8) or -SO2-R9 group, in which R6 represents cycloalkyl having 3-6 carbon atoms or halogen-substituted cycloalkyl; trifluoromethyl, straight or branched alkoxy having no more than 8 carbon atoms, phenyl, benzyloxy or hydrogen, or R6 represents straight or branched alkyl or alkenyl having no more than 8 carbon atoms, randomly substituted by cyano, halogen or trifluoromethyl, or represents under each condition thioalkyl or acyl having no more than 6 carbon atoms, or -NR10R11 group, in which R10 and R11 are the same or different and represent hydrogen, phenyl or straight or branched alkyl having no more than 6 carbon atoms, or R6 represents 5-member aryl heteroring having no more than 3 heteroatoms selected from S, N and/or O, randomly substituted by straight or branched alkyl having no more than 3 carbon atoms; R7 and R8 are the same or different and represent hydrogen or straight or branched alkyl having no more than 4 carbon atoms; R9 represents straight or branched alkyl or phenyl having no more than 4 carbon atoms. A represents the following group: in which G, L, and M are the same or different, and represent hydrogen, halogen, cyano, trifluoromethyl, straight or branched alkyl having no more than 6 atoms, or -CO-NR17R18 group, in which R17 and R18 are the same or different and represent hydrogen, straight or branched alkyl having no more than 4 carbon atoms, or phenyl, R12 represents hydrogen, cycloalkylcarbonyl or cycloalkyl having 3-6 carbon atoms or straight or branched oxo-carbonyl having no more than 6 carbon atoms, or straight or branched alkyl or alkenyl having no more than 10 carbon atoms, which can be randomly substituted by the following groups: cyano, azido, trifluoromethyl, pyridyl, halogen, hydroxyl, carboxyl, straight or branched carbonyl having no more than 6 atoms, benzyloxycarbonyl, aryl having no more than 6-10 carbon atoms, cycloalkyl having 3-6 carbon atoms and/or group R25-S(O)d, in which d denotes number 0 or 2, R25 represents straight or branched alkyl having no more than 4 carbon atoms, benzyl, phenyl or methylphenyl, or R12 represents the following groups, or represents -COOCl3 or straight or branched acyl having no more than 6 carbon atoms and randomly substituted by the following groups: trifluoromethyl, trichloromethyl or -OR26 group, in which R26 represents hydrogen or straight or branched alkyl having no more than 6 carbon atoms which can be randomly substituted by aryl having no more than 10 carbon atoms or R12 represents groups of formula -(CO)c-NR27R28, -NR29-SO2R30, R31R32-N-SO2- or R33-S(O)f, in which is number 0 or 1, R27, R28 and R29 are defined the same as R17 and R18 above and can be the same or different, or form together with nitrogen atom 5-6 member saturated hetero ring containing other heteroatoms randomly selected from N, S and/or O, and can be randomly substituted by straight or branched alkyl or acyl having no more than 3 carbon atoms, which even substitutes other nitrogen atom, R31 and R32 are defined the same as R17 and R18 and can be the same or different, R30 and R33 under all circumstances are defined the same as R25 above and can be the same or different, D represents O or S, E represents O or S or -NH, T represents O or -NH, R13 and R 14 are defined the same as R12 above and can be the same or different, or T represents S, in the proviso: R13 and R14 are defined the same as R12 above, but do not represent hydrogen, or under the condition where R12, R13 and R14 do not represent hydrogen, E and/or T represent -NR34, in which R34 is defined the same as R12 above except for hydrogen and can be the same or different, or R34 represents cyano or -CO2R35, in which R35 represents benzyl or phenyl and is randomly substitutable by nitro or halogen, and W are defined the same as D above or represents N-R14 above and can the same or different, a denotes number 1 or 2, b denotes number 0 or 1, R15 and R16 are defined the same as R12 above and the same as or different from R12.
    • 8. 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.