5-MEMBERED HETEROARYL-OXAZOLIDINONES

3-Heteroaryl-2-oxazolidinone derivs. of formula (I) and their salts and S-oxides are new: R1 = azido, OH, OR2, OSO2R3 or NR4R5; R2 = 1-8C acyl or a protecting gp.; R3 = 1-4C alkyl, phenyl or (1-4C alkyl)phenyl; R4, R5 = H, 1-8C alkyl, 3-6C cycloalkyl, phenyl or amino protecting gp., or one of R4, R5...

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Main Authors HANNO WILD, BERND RIEDL, KLAUS SCHALLER, ANDREAS STOLLE, HANS-OTTO WERLING KROLL, DIETER HAEBICH, HARALD LABISCHINSKI, KLAUS DIETER BREMM, HEIN-PETER KROLL, REINER ENDERMANN
Format Patent
LanguageEnglish
Published 30.06.1997
Edition6
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
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Summary:3-Heteroaryl-2-oxazolidinone derivs. of formula (I) and their salts and S-oxides are new: R1 = azido, OH, OR2, OSO2R3 or NR4R5; R2 = 1-8C acyl or a protecting gp.; R3 = 1-4C alkyl, phenyl or (1-4C alkyl)phenyl; R4, R5 = H, 1-8C alkyl, 3-6C cycloalkyl, phenyl or amino protecting gp., or one of R4, R5 = COR6; R6 = H, 1-8C alkyl, 3-6C cycloalkyl or phenyl; A = C-bonded 5-membered heteroaryl contg. 1-3 of S, N and/or O and opt. benzo- or naphtho-fused, the rings being opt. substd. by 1-3 of COOH, halo, CN, SH, CHO, CF3, NO2, 1-6C alkoxy, 2-6C alkoxycarbonyl, 1-6C alkylthio, 1-6C acyl and 1-6C alkyl, where alkyl is opt. substd. by OH, 1-5C alkoxy, 1-5C acyl or NR7R8; and/or NR7'R8'; and/or phenyl, (2-8C alkenyl)phenyl or 5- or 6-membered heterocyclyl contg. 1-3 of S, N and/or O, where these gps. are opt. substd. by CONR9R10, NR11R12, NR13SO2R14, SO2NR15R16, or S(O)aR17; and/or by 1-2 of COOH, halo, CN, SH, CHO, CF3, NO2, phenyl, 1-6C alkoxy, 2-6C alkoxycarbonyl, 1-6C alkylthio, 1-6C acyl and 1-6C alkyl, where alkyl is opt. substd. by OH, 1-5C alkoxy, 1-5C acyl or NR18R19; and/or 5-7C 3-oxo-1-cycloalkenyl; a =0-2; R7, R8 = H, 1-4C alkyl or phenyl; or NR7R8 = a satd. 5- or 6-membered ring opt. contg. another heteroatom selected from N, S and/or O and opt. substd. by 1-3C alkyl or acyl; R7', R8', R11, R12, R18, R19 = as R7 and R8; R9, R10, R13, R15, R16 = H, 1-6C alkyl or phenyl; R14, R17 = as R3. (I) are antimicrobial agents active against Gram-positive bacteria and bacterium-like microorganisms, e.g. Mycoplasma spp. (I) are useful for treating local or systemic infections in humans and animals.
Bibliography:Application Number: HR1995P000391