Oxa(thia)zolidine derivative and anti-inflammatory drug

A medicinal composition characterized by comprising as the active ingredient either a compound represented by a general formula (1) or a pharmaceutically acceptable composite thereof;

• 59
• wherein X represents oxygen or sulfur,
• R1 represents hydrogen, C1-4 alkyl or C1-4 haloalkyl,
• R2 represents phenyl optionally substituted by A1, naphthyl optionally substituted by A1, 5 to 6-membered heterocyclic group optionally substituted by A1 containing at least one heteroatom selected from a group consisting of oxygen, sulfur and nitrogen, quinolyl optionally substituted by A1, or a group represented by a formula
• 60
• wherein Q represents —(CH2)3—, —(CH2)4— or —OCH2O—,
• R3 represents hydrogen, C1-4 alkyl optionally substituted by A2, C1-4 alkoxy optionally substituted by A2, C1-4 alkylcarbonyl optionally substituted by A2, C1-4 alkoxycarbonyl optionally substituted by A2, C2-4 alkenylcarbonyl optionally substituted by A2, phenyliminomethyl optionally substituted by A3, phenyl optionally substituted by A3, anilino optionally substituted by A3, or a group represented by the following formulae;
• 61
• wherein Y represents oxygen or sulfur, R4 represents hydrogen or C1-4 alkyl, R5 represents C1-6 alkyl optionally substituted by A2, C2-6 alkenyl optionally substituted by A2, C2-6 alkynyl optionally substituted by A2, C1-6 alkoxy optionally substituted by A2, C2-6 alkenyloxy optionally substituted by A2, mono- or di-(C1-6 alkyl)amino optionally substituted by A2, C3-7 cycloalkyl optionally substituted by A4, C5-7 cycloalkenyl optionally substituted by A4, phenyl optionally substituted by A3, benzoyl optionally substituted by A3, anilino optionally substituted by A3, C1-6 alkoxycarbonyl optionally substituted by A2, phenylsulfonyl optionally substituted by A3, C1-6 alkoxysulfonyl optionally substituted by A2, mono- or di-(C1-6 alkyl)aminosulfonyl optionally substituted by A2, or 5- to 7-membered heterocyclic group optionally substituted by A4 containing at least one atom selected from a group consisting of oxygen, sulfur and nitrogen as a heteroatom, and n represents 0, 1 or 2,
• R represents oxygen, sulfur or a group represented by a formula of N—G, wherein G represents hydrogen, nitro, cyano, C1-4 alkyl optionally substituted by A2, C1-4 alkoxy, C1-4 alkylcarbonyl, phenyl optionally substituted by A3, benzoyl optionally substituted by A3, anilino optionally substituted by A3, a group represented by a formula of NHCOR6, wherein R6 represents C1-4 alkyl or phenyl optionally substituted by A3, or a group represented by the following formula;
• 62
• wherein Z represents oxygen or sulfur, R7 represents C1-4 alkyl, C3-7 cycloalkyl optionally substituted by A4, phenyl optionally substituted by A3, benzoyl optionally substituted by A3, or optionally substituted 5- to 7-membered heterocyclic group,
• A1 represents halogeno, amino, nitro, cyano, C1-12 alkyl, C2-6 alkenyl, C1-4 haloalkyl, C3-7 cycloalkyl, phenyl optionally substituted by halogeno, C1-4 alkyl or C1-4 haloalkyl, pyridyl, thienyl, C1-4 alkoxy, methylenedioxy, C1-4 alkylthio, C1-4 alkylsulfenyl, C1-4 alkylsulfonyl, mono- or di-(C1-4 alkyl)amino, C1-4 haloalkoxy, benzyl, phenetyl, phenoxy, phenylthio, C1-4 alkoxycarbonyl, C1-4 haloalkoxycarbonyl, C1-4 alkylcarbonyloxy, carbamoyl, or mono- or di-(C1-4 alkyl)carbamoyl,
• A2 represents halogeno, C1-4 alkoxy, C1-4 alkoxy C1-4 alkoxy, amino, mono- or di-(C1-4 alkyl)amino, C1-4 alkylcarbonyloxy, C1-4 alkoxycarbonyl, halo C1-4 alkoxycarbonyl, C1-4 alkylcarbamoyl, di-(C1-4 alkyl)carbonylamino, morpholino, phenyl, or pyridyl optionally substituted by halogeno,
• A3 represents halogeno, hydroxy, oxo, mercapto, nitro, amino, cyano, C1-4 alkyl, C1-4 haloalkyl, pyridyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylsulfenyl, C1-4 alkylsulfonyl, mono- or di-(C1-4 alkyl)amino, C1-4 haloalkoxy, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, C1-4 haloalkoxycarbonyl, carbamoyl, mono- or di-(C1-4 alkyl)carbamoyl, or C1-4 alkoxycarbonyl C1-4 alkylthio, and
• A4 represents halogeno, hydroxy, oxo, C1-4 alkyl, halo C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, halo C1-4 alkoxy, halo C1-4 alkylthio, C1-4 alkoxy C1-4 alkoxy, C1-4 alkylsulfonyl, C1-4 alkoxycarbonyl, or C1-4 haloalkoxycarbonyl,
• provided that R is oxygen or sulfur, R3 represents a group represented by the following formula;
• 63
• wherein Y, R4 and R5 are as defined above.