Bicyclic nitroimidazoles covalently linked to substituted...

C - Chemistry – Metallurgy – 07 – D

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C07D 498/04 (2006.01) A61K 31/5365 (2006.01) A61P 31/04 (2006.01) A61P 31/06 (2006.01)

Patent

CA 2712613

The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bi-cyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild- type and resistant strains of pathogens, and are there-fore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.

Cette invention concerne une série de nitroimidazoles bicycliques-phényl- oxazolidinones substituées, le pharmacophore nitroimidazole bicyclique étant lié par covalence à la phényloxazolidinone, leurs compositions pharmaceutiques, et un procédé d'utilisation des compositions pour prévenir et traiter les infections bactériennes. Les nitroimidazoles bicycliques-phényloxazolidinones substituées possèdent une surprenante activité antibactérienne contre des souches de type sauvage et résistantes de pathogènes, et sont, par conséquent, utiles pour prévenir, maîtriser et traiter un certain nombre d'infections bactériennes humaines et vétérinaires provoquées par ces pathogènes, tels que Mycobacterium tuberculosis.

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