5-hydroxymethyl-oxazolidin-2-one derivatives

Details 5-hydroxymethyl-oxazolidin-2-one derivatives 5-hydroxymethyl-oxazolidin-2-one derivatives

C - Chemistry, Metallurgy

07

D

C07D 413/14 (2006.01) A61K 31/4375 (2006.01) A61K 31/4709 (2006.01) A61P 31/00 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2668280

The invention relates to novel chimeric antibiotics of formula (I) wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; R3 represents H or fluorine; R4 is H, (C1-C3) alkyl, or cycloalkyl; R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; R6 represents H, alkoxy or halogen; and 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 porte sur de nouveaux antibiotiques chimériques de formule I, dans laquelle R1 représente OH, OPO3H2 ou OCOR5; R2 représente H, OH ou OPO3H2; A représente N ou CR6; R3représente H ou fluor; R4 représente H, alkyle C1-C3 ou cycloalkyle; R5 est le reste d'un acide aminé se trouvant dans la nature, de l'énantiomère d'un acide aminé se trouvant dans la nature ou de diméthylaminoglycine; R6 représente H, alcoxy ou halogène; et n est 0 ou 1; et sur les sels (en particulier les sels pharmaceutiquement acceptables) des composés de formule I. Ces composés chimériques sont utiles dans la fabrication de médicaments destinés au traitement d'infections (par exemple d'infections bactériennes).

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