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US 5,684,023 AGranted
Benzofuranyl -and benzothienyloxazolidinones
AssigneeBayer Aktiengesellschaft
InventorsBernd Riedl, Dieter Habich, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus Dieter Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
Life of this patent
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Abstract
The present invention relates to benzofuranyl- and benzothienyloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.
Claims11
An oxazolidinone of the formula ##STR73## in which R.sup.1 represents azido, hydroxyl or a group of the formula --OR.sup.2, --O--SO.sub.2 R.sup.3 or --NR.sup.4 R.sup.5,
- wherein
- R.sup.2 denotes a straight-chain or branched acyl having up to 6 carbon atoms or benzyl,
- R.sup.3 denotes straight-chain or branched alkyl having up to 4 carbon atoms or phenyl which is optionally substituted by straight-chain or branched alkyl having up to 4 carbon atoms,
- R.sup.4 and R.sup.5 are identical or different and denote cycloalkyl having 3 to 6 carbon atoms, hydrogen, phenyl, straight-chain or branched alkyl or alkoxy having up to 8 carbon atoms, tert-butoxycarbonyl or benzyloxycarbonyl,
- or
- R.sup.4 and R.sup.5 denotes a group of the formula --CO--R.sup.6,
- wherein
- R.sup.6 denotes cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or straight-chain or branched alkyl or alkoxy in each case having up to 6 carbon atoms, hydrogen or phenyl,
- A represents an oxygen or sulphur atom,
- D, E, G, L and M are identical or different and represent hydrogen, carboxyl, fluorine, chlorine, bromine, cyano, formyl, trifluoromethyl, straight-chain or branched alkoxy, alkoxycarbonyl or acyl in each case having up to 6 carbon atoms or straight-chain or branched alkyl having up to 6 carbon atoms, which for its parts is optionally substituted by hydroxy, by straight-chain or branched alkoxy or acyl having up to 5 carbon atoms, by a radical of the formula ##STR74## or by a group of the formula --NR.sup.7 R.sup.8, wherein
- R.sup.7 and R.sup.8 are identical or different and denote hydrogen, straight-chain or branched alkyl having up to 3 carbon atoms or phenyl,
- and/or D, E, G, L and/or M
- optionally represent a group of the formula --NR.sup.7 'R.sup.8',
- wherein
- R.sup.7' and R.sup.8' have the meaning of R.sup.7 and R.sup.8 indicated above and are identical to or different from this and/or one of D, E, G, L and M optionally represents iodine and/or one of D, E, G, L and M optionally represents nitro,
- and/or D, E, G, L or M
- optionally represent (C.sub.2 -C.sub.4)-alkenylphenyl, phenyl, pyridyl or thienyl which for their parts are optionally substituted by a group of the formula --CO--NR.sup.9 R.sup.10, --N.sup.11 R.sup.12,
- wherein
- R.sup.9 and R.sup.10 are identical or different and denote hydrogen straight-chain or branched alkyl having up to 4 carbon atoms or phenyl,
- R.sup.11 and R.sup.12 are identical or different and have the meaning of R.sup.7 and R.sup.8 indicated above and are identical or different from them,
- which said (C.sub.2 -C.sub.4)-alkenylphenyl, phenyl, pyridyl or thienyl for their parts are optionally substituted up to 2 times by identical or different substituents from the group consisting of carboxyl, fluorine, chlorine, bromine, iodine, cyano, mercapto, formyl, trifluoromethyl, nitro, phenyl, or straight-chain or branched alkoxy, alkoxycarbonyl, alkylthio and acyl in each case having up to 4 carbon atoms or straight-chain or branched alkyl having up to 4 carbon atoms, which for its part can optionally be substituted by hydroxyl, by straight-chain or branched alkoxy or acyl having up to 4 carbon atoms or by a group of the formula --NR.sup.18 R.sup.19,
- wherein
- R.sup.18 and R.sup.19 have the meaning of R.sup.7 and R.sup.8 indicated above and are identical to or different from this,
- or a salt or S-oxide thereof.
21 more elements
Dependencies are inferred from the claim text.