| 摘要 |
A thioamide derivative or pharmaceutically acceptable salts and esters thereof has the formula (I) wherein: X is a group of the formula (X-1), (X-2) or (X-3); Y is a group of formula (Y-1), (Y-2), (Y-3); R15 is halogen, nitro, alkyl sulphonyl, cyano, alkyl, alkoxy, alkoxycarbonyl, carboxy, alkyl aminosulphonyl, perfluoroalkyl, alkylthio, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, alkylsulphinyl, alkanoyl, aroyl, aryl or aryloxy; R16 is hydrogen, halogen, nitro, cyano, alkyl, OH, perfluoro alkyl, or alkylthio; Het is a 5-or 6-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms selected from N, O, and S or a 9-or 10- membered bicyclic heteroaromatic ring containing 1, 2, 3 or 4 heteroatoms selected from O, S, and N; R30 is hydrogen or alkyl; p is 0 or 1; R18 is aryl, heteroaryl, arylalkyl, or heteroarylalkyl R19 is optionally substituted alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl; R20 is optionally substituted alkanoyl or aroyl; R22 and R23 are independently hydrogen, alkyl, alkoxy, cycloalkyl, aryl, arylalkyl, nitro, cyano, alkylthio, alkylsulphinyl, alkylsulphonyl, alkanoyl, halogen, or perfluoroalkyl provided that at least one of R22 and R23 is other than hydrogen; R24 is hydrogen, alkyl, alkoxy, aryl, nitro, cyano, alkylsulphonyl, or halogen; or Y-2 is a group of the formula: Het' is a five or six membered heteroaromatic ring bonded via a carbon atom containing one, two or three heteroatoms selected from the group consisting of, O and S; R30' and R31 are independently hydrogen, alkyl, cycloalkyl, halogen, cyano, perfluoroalkyl, or aryl provided at least one of R30' and R31 is adjacent to the point of attachment; R25 is alkyl, alkenyl, fluoroalkenyl, or a group of formula R26-(CH2)e-, Q is -(CH2)fO-, -(CH2)fS-, -(CH2)fN(R27)-, -(CH2)f or a bond; R26 and R27 are as defined in the specification; e is 0 to 4, f is 1 to 3, and the dotted bond is optionally hydrogenated. The compounds are useful for the treatment or prophylaxis of rheumatoid arthritis, multiple sclerosis, inflammatory bowel disease and asthma.
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