5-hydroxymethyl-oxazolidin-2-one antibacterials

Details 5-hydroxymethyl-oxazolidin-2-one antibacterials 5-hydroxymethyl-oxazolidin-2-one antibacterials

C - Chemistry, Metallurgy

07

D

C07D 498/14 (2006.01) A61K 31/5383 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2668369

The invention relates to novel chimeric antibiotics of formula (I) wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen; R4 is H, (C1-C3) alkyl, or cycloalkyl; R5 represents piperidin-4-yl or R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; n is O or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula (I). These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).

L'invention concerne des antibiotiques chimères inédits de formule (I), où R1 représente OH, OPO3H2 ou OCOR5; R2 représente H, OH ou OPO3H2; R3 représente H ou un halogène; R4 représente H, un groupe cycloalkyle ou un groupe alkyle en C1-C3 ; R5 représente un groupe pipéridin-4-yle ou R5 est le résidu d'un acide aminé naturel, de l'énantiomère d'un acide aminé naturel ou de la diméthylaminoglycine; n est égal à 0 ou 1; ainsi que des sels (en particulier des sels acceptables sur le plan pharmaceutique) de composés de formule (I). Ces composés chimères sont utilisables dans le cadre de la fabrication de médicaments destinés au traitement des infections (par exemple d'infections bactériennes).

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