| 摘要 |
<p>Compounds of formula (I), or a pharmaceutically acceptable salt, quaternised derivative, N-oxide or solvate thereof: R1-Ar-(CH2)a-X-(CH2)b-NH-Het (I) wherein: R1 is hydrogen, halogen, hydroxy, C1-4 alkyl, C1-4 alkoxy, or amino or guanidino, the or any amino moiety being optionally substituted by one or two C1-4 alkyl optionally substituted by halogen, or an aminomethylene group of formula (a), <CHEM> in which R2 and R3 are the same or different and are hydrogen, C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-4 alkyl or phenyl C1-4 alkyl, or R2 and R3 together with the nitrogen atom to which they are attached are morpholino, pyrrolidino or piperidino; Ar is furandiyl, thiophendiyl, phenylene, pyridinediyl, pyrimidinediyl, thiazolediyl, thiadiazolediyl or imidazolediyl; a is 0 or an integer 1 or 2; X is -S-, -O-, -CH2-, -@- or -NH-; b is an integer from 2 to 5; and Het is a bicyclic heteroaryl group of formula (b) or (c), <CHEM> in which R4 and R5 are the same or different and are hydrogen, halogen, C1-6 alkyl, trifluoromethyl, nitro, cyano, hydroxy, C1-6 alkoxy, C1-6 alkylthio, carboxy, amino, aminocarbonyl, aminocarbonylamino, amino-thiocarbonylamino, aminosulphonyl, C1-6 alkylsulphonyl, C1-6 alkylsulphinyl, C1-6 alkylsulphonylamino, C1-6 alkyluslphinylamino, phenylsulphonyl, phenylsulphinyl or are a group of formula (d) or (e), R9-CY- (d) R9-CY-Z- (e) in which R9 is hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, phenyl, phenoxy or phenylthio, Y is oxygen or sulphur and Z is oxygen, sulphur or N-R10, R10 being hydrogen or C1-6 alkyl, the C1-6 alkyl group or the C1-6 alkyl moiety of any of the foregoing C1-6 alkyl-containing groups for R4 and R5 being optionally substituted by phenyl, the amino group or the amino moiety of any of the foregoing amino-containing groups for R4 and R5 being optionally substituted by one or two C1-6 alkyl, phenyl or phenyl-C1-4 alkyl or optionally N-disubstituted by C4-5 polymethylene, and the phenyl moity of any of the foregoing phenyl-containing groups for R4 and R5 being optionally substituted by C1-6 alkyl, C1-6 alkoxy, halogen, nitro or trifluoromethyl, one of R6 and R8 is hydrogen, C1-6 alkyl, C1-6 alkanoyl, C1-6 alkylsulphonyl, C1-6 alkoxycarbonyl or phenoxycarbonyl, benzyloxycarbonyl, phenyl, phenylsulphonyl or phenyl C1-4 alkyl, the phenyl moiety being optionally substituted by benzoyl, C1-6 alkyl, C1-4 alkoxy, halogen, nitro or trifluoromethyl, and the other of R6 and R8 together with R7 is a bond, and n is O or an integer 1 or 2.</p> |
