Oxazolidinone compounds and compositions and methods related...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 413/00 (2006.01) A61K 31/541 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2574668

The invention provides new oxazolidinones of formula (I), where R1, R2, R3 and R4 are independently selected from hydrogen, F and Cl; A is selected from certain heterocycles optionally substituted; X is selected from O, S, NRs and CR8Rg; Y is selected from O, S, SO, SO2, NO, NR11 and CR11R12; and n is selected from 0 and 1. The invention also provides different processes for the preparation of such compounds. Oxazolidinone compounds of formula (I) are active against Gram-positive and some Gram-negative human and veterinary pathogens with a weak monoamine oxidase (MAO) inhibitory activity. They are useful for the treatment of bacterial infections.

L'invention concerne de nouveaux oxazolidinones représentés par la formule (I), dans laquelle R1, R2, R3 et R4 sont indépendamment choisis dans le groupe hydrogène, F et Cl ; A est choisi parmi certains hétérocycles éventuellement substitués ; X est choisi dans le groupe O, S, NRs et CR8Rg ; Y est choisi dans le groupe constitué de O, S, SO, SO2, NO, NR11 et CR11R12 ; et n est choisi dans le groupe constitué de 0 et 1. L'invention concerne également différents procédés de préparation de ces composés. Les composés oxazolidinone représentés par la formule (I) sont actifs contre des pathogènes humains et vétérinaires gram-positifs et, pour certains, gram-négatifs présentant une faible activité inhibitrice de la monoamine oxydase (MAO). Les composés selon l'invention sont utiles pour le traitement d'infections bactériennes.

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