2-Oxo-and 2-thio-1,2-dihydroquinolinyl-oxazolidinones

• Main Authors: WALTER GUARNIERI, BERND RIEDL, STEPHAN BARTEL, ANDREAS STOLLE, MARTIN RUPPELT, DIETER HABICH, RAINER ENDERMANN, HEIN-PETER KROLL
• Format: Patent
• Language: English
• Published: 17.07.1997
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

2-(Oxo or thio)-1,2-dihydroquinolinyl-oxazolidinones (I) and their isomers and salts are new: A = O or S; D = H; 3-6C cycloalkyl; alkoxycarbonyl with up to 4C; alkyl or alkenyl with up to 9C optionally substituted by CN, CF3, halo, OH, pyridyl, Ph, COOH, CONH2, alkoxycarbonyl with up to 5C, naphthyl, 3-6C cycloalkyl and/or -(CO)a-NR R , -N(R )-SO2-R , -SO2-N-R R or -S(O)b-R ; acyl with up to 5C optionally substituted by CF3, CCl3 or OR ; -(CT)d-NR R ; -(CO)e-NR -CO-NR R ; -NR -SO2R R R -N-SO2-; R -S(O)f; or -CO-R ; E, L = H; COOH; halo; CN; CHO; CF3; NO2; or 1-4C alkyl; R = N3; OH; OR ; OSO2R ; or NR R ; a, d, e = 0 or 1; f, b = 0-2; R -R , R , R = H; 1-5C alkyl; or Ph; or NR R = morpholinyl, thiomorpholino, pyrrolidinyl, piperazinyl or piperidyl optionally substituted on a free N atom by alkyl or acyl with up to 4C; R , R = 1-6C alkyl, Ph; benzyl; or tolyl; R = H or 1-5C alkyl optionally substituted by Ph or naphthyl; T = O or S; R -R , R , R = as R -R ; R , R = = R and R ; R = 6-10C aryl optionally substituted by halo; R = acyl with up to 6C or a OH protecting group; R = 1-5C alkyl; Ph; or toluoyl; R , R = H; 3-6C cycloalkyl; Ph; 1-6C alkoxy; t-Boc; Fmoc; benzyloxycarbonyl; 1-6C alkyl optionally substituted by CN or alkoxycarbonyl with up to 4C; -CT-R ; P(O)(OR )(OR ) or -SO2-R ; R = H; 3-6C cycloalkyl; CF3; 1-6C alkoxy; Ph; Ph-CH2O; 1-6C alkyl optionally substituted by alkoxycarbonyl with up to 5C, CN, F, Cl, Br or CF3; thioalkyl or acyl with up to 5C; or -NR R ; R , R = H or 1-4C alkyl; R = 1-4C alkyl or Ph; and R , R = H; Ph; or 1-4C alkyl.