摘要 |
An anilide derivative, its N-oxides, prodrugs or pharmaceutically acceptable salts and solvates thereof has the formula (I) wherein: R1 is hydrogen, halogen, hydroxy, alkyl or alkoxy; X1, X2 and X6 independently are N or CR10 and one of X3, X4 and X5 is CR11 and the others independently are N or CR10; R10 is hydrogen, amino, halogen, hydroxy, alkyl, alkoxy, alkylthio, alkylsulphinyl, nitro, alkylsulphonyl or trifluoromethyl; R11 is a group -L1-Ar1-L2-Y and L1 is a-R2-R3-linkage; R2 is alkylene, alkenylene, or alkynylene and R3 is a bond, cycloalkylene, heteroaryldiyl, heterocycloalkylene, arylene, -C (=Z)-NR4-, -NR4-C(=Z)-, -Z1-, -C(=O)-, -C (=NOR4)-, -NR4-C(=Z)-NR4-, -SO2-NR4-, -NR4-SO2-, -O-C(=O)-, -C(=O)-O-, -NR4-C(=O)-O- or -O-C(=O)-NR4- but excluding compounds where an oxygen, nitrogen or sulphur atom in R3 is attached directly to a carbon to carbon multiple bond in R2; R4 is hydrogen or alkyl and n is 0 to 2; Z is O or S and Z1 is O, S(O)n or NR4; Ar1 is arylene or heteroaryldiyl and L2 represents: a bond; optionally substituted alkylene, alkenylene, alkynylene, cycloalkenyl, cycloalkylene, heteroaryldiyl, heterocycloalkylene or arylene or -[C(=O)-N(R6)-C(R4) (R7)]p-, -Z2-R9-, -C(=O)-CH2-C(=O)-, R9-Z2-R9- or -C(R4)(R8)-[C(=O)-N(R6)-C(R4)(R7)]p-; Z2 is O, S(O)n, NR4, SONR4, C(=O)NR4 or C(=O); and p is 0 to 4; Y is carboxy (or an acid bioisostere) or-C(=O)-NY1Y2 and R5 to R9, Y1 and Y2 are as defined in the specification limited by the exclusions and provisos as listed in the specification. A pharmaceutical composition thereof is useful for treating an inflammatory disease such as asthma.
|
申请人 |
AVENTIS PHARMA LIMITED |
发明人 |
ASTLES, PETER CHARLES;CLARK, DAVID EDWARD;COLLIS, ALAN JOHN;COX, PAUL JOSEPH;EASTWOOD, PAUL JOSEPH;HARRIS, NEIL VICTOR;LAI, JUSTINE YEUN QUAI;MORLEY, ANDREW DAVID;PORTER, BARRY |