Pleuromutilin derivatives as antimicrobials

摘要

The compounds of formula (IA) or (IB) where: R1 is vinyl or ethyl R2 is an optionally substituted non-aromatic monocyclic group containing one or two basic nitrogen atoms and attached through a ring carbon atom each of n and m is independently 0,1 or 2 and X is selected from -O-, -S(O)-, -SO2-, -CO.O-, -NH-, -CONH-, -NHCONH- and a bond or n is 1 or 2 and m is 2 and X is -S- Or R2 is an optionally substituted non-aromatic bicyclic group containing one or two basic nitrogen atoms an d attached through a ring carbon atom each of n and m is independently 0,1 or 2 and X is selected from -O-, -S-, -S(O)-, -SO2-, -CO.O-, -NH-, -CONH-, -NHCONH- R3 is H or OH or The moiety R2(CH2)mX(CH2)nCH2COO at position 14 of (IA) or (IB) is replaced by RaRbC=CHCOO in which one of Ra and Rb is hydrogen and the other R2 or Ra and Rb together form R2. Or a pharmaceutically acceptable salt thereof. Also described is a process to prepare the compounds of formula (IA) or (IB). The compounds of formula (IA) or (IB) are useful for administration to the nasal cavity for reducing or eliminating the nasal carriage of pathogenic organism and for the prophylaxis or recurrent otitis media or recurrent acute bacterial sinusitis.