PYRIDO[1,2,3-D,E][1,3,4]BENZOXADIAZINE DERIVATIVES

• Main Authors: SCHENKE, THOMAS, WETZSTEIN, HEINZ-GEORG, MIELKE, BURKHARD, PHILIPPS, THOMAS, SCHEER, MARTIN, JAETSCH, THOMAS, ENDERMANN, RAINER, PETERSEN, UWE, BREMM, KLAUS DIETER, STEGEMANN, MICHAEL, METZGER, KARL GEORG
• Format: Patent
• Language: English; French
• Published: 13.06.2006
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to novel pyrido[1, 2, 3- d,e][1,3.4]benzoxadiazine derivatives of the formula (I) (see formula I) in which R1 is hydrogen or C1-C4-alkyl optionally substituted by hydroxyl or halogen, R2 independently of R1 is hydrogen or methyl, R3 is hydrogen or C1-C4-alkyl. R4 is hydrogen, C1-C4-alkyl optionally substituted by hydroxyl, methoxy, amino, methylamino or dimethyl- amino, or (5-methyl-2-oxo-1, 3-dioxol-4-yl) -methyl, X1 ~is hydrogen or halogen and Z~is a radical of the structure (see formula I, II, III) in which R7 ~is hydrogen. hydroxyl, -NR10R11, hydroxymethyl, -CH2- NR10R11, carboxyl, methoxycarbonyl or ethoxycarbonyl, R10 being hydrogen, C1-C3-alkyl optionally substituted by hydroxyl, alkoxycarbonyl having 1 to 4 C atoms in the alkoxy moiety, or C1-C3-acyl, and R11 being hydrogen or methyl, R8 ~is hydrogen. linear or branched C1-C3-alkyl or cyclo-~ propyl, R9 ~is hydrogen or methyl, R6 ~is hydrogen or methyl, R5 ~is hydrogen, methyl or a radical of the structure -CH=CH-CO2R5', -CH2-CH2-CO2R5', -CH2-CO-CH3 or -CH2-CH-2-CN, R5' ~being methyl or ethyl, and B ~is -CH2-. O or a direct bond, to their preparation and to their use for the therapy or prophylaxis of bacterial infections.