申请人:BEECHAM GROUP PLC
公开号:EP0151962A2
公开(公告)日:1985-08-21
Compound of formula (I) and pharmaceutically acceptable salts thereof:
wherein:
R, is hydrogen, C, alkyl or phenyl optionally substituted by halogen, CF3, C1-4 alkoxy or C1-4 alkyl;
R2 is hydrogen or C1-6 alkyl;
R3 is hydroxy, nitro, cyano. C2-10 acyloxy, NR6R7 wherein R8 and R7 are independently selected from hydrogen, C1-6 alkyl, C2-7 alkanoyl or C1-6 alkylsulphonyl: or CORe wherein R8 is hydroxy, C1-8 alkoxy or NR9R10 wherein R9 and R10 are independently selected from hydrogen or C1-6 alkyl;
R. is hydrogen, halogen, CF3, C1-4 alkoxy, C1-4 alkyl or any of the groups listed for R3; and
R5 is hydrogen, C1-4 alkyl or benzyl optionally substituted in the phenyl ring by halogen, CF3, C1-4 alkoxy or C1-4 alkyl and is attached at nitrogen atom 1 or 2, having anti-inflammatory and/or anti-allergy activity, a process for their preparation and their use as pharmaceuticals.
式(I)化合物及其药学上可接受的盐类:
其中
R,是氢、C、烷基或任选被卤素、CF3、C1-4 烷氧基或 C1-4 烷基取代的苯基;
R2 是氢或 C1-6 烷基;
R3 是羟基、硝基、氰基。或 CORe,其中 R8 是羟基、C1-8 烷氧基或 NR9R10,其中 R9 和 R10 独立地选自氢或 C1-6 烷基;
R. 是氢、卤素、CF3、C1-4 烷氧基、C1-4 烷基或 R3 所列的任何基团;以及
R5是氢、C1-4烷基或在苯基环上任选被卤素、CF3、C1-4烷氧基或C1-4烷基取代并连接在氮原子1或2上的苄基,具有抗炎和/或抗过敏活性,其制备方法及其作为药物的用途。