| 摘要 |
Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV. Formula (I) Wherein: - R1 represents C1-6 alkyl, aryl or heteroaryl; - R2 represents hydrogen or C1- 6 alkyl; - each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, -CO2RI, -CONRIR II, -NH-CO-RI, -S(O)RI, -S(O) 2RI, -NH-S(O)2RI, -S(O) NRIRII or -S(O)2NRIRII wherein each RI and R II is the same or different and represents hydrogen or C1- 6 alkyl; - n is from 0 to 3; R4 represents hydrogen or C 1-6 alkyl; - R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)-C(O)-, heteroaryl-C(O)-C(O) -, carbocyclyl-C(O)-C(O)-, heterocyclyl-C(O)-C(O)- or, -XR6; - X represents -CO-, -S(O)- or -S(0)2-; and - R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1- 6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1- 6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C 1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl- (C1-6hydroxyalkyl)-, heterocyclyl-(C 1-6 hydroxyalkyl)-, aryl-(C 1-6alkyl)-O-, heteroaryl-(C 1-6alkyl)-O-, carbocyclyl-(C1-6 alkyl)-O-, heterocyclyl-(C1-6 alkyl)- O- or -NRIRIIwherein each RI and RII is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl- (C1-6 alkyl)-, heteroaryl-(C1-6 alkyl) -, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.
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