申请人:SHIONOGI & CO., LTD.
公开号:EP0676397A1
公开(公告)日:1995-10-11
An oxopyridinylquinoxaline derivative represented by the following Formula I or pharmaceutically acceptable salts thereof:
wherein R¹ is hydrogen, halogen, nitro, or trihalomethyl; R² is hydrogen, halogen, nitro, cyano, trihalomethyl, carbamoyl, carbamoyl substituted with lower alkyl, sulfamoyl, or sulfamoyl substituted with lower alkyl; R³ is hydrogen, nitro, or halogen; R⁴ is hydrogen, lower alkyl, substituted lower alkyl, lower cycloalkyl, or substituted lower cycloalkyl; R5's are substituents independently selected from the group consisting of halogen, nitro, cyano, lower alkyl, carbamoyl, and carbamoyl substituted with lower alkyl; and n is an integer of 0 to 4. The derivative works as an antagonistic agent against both the NMDA receptors and the AMPA receptors, so that it is effective as a therapeutic agent for neurological disorders caused by excitatory amino acids binding to the receptors.
下式 I 所代表的氧吡啶基喹喔啉衍生物或其药学上可接受的盐类:
其中R¹是氢、卤素、硝基或三卤甲基;R²是氢、卤素、硝基、氰基、三卤甲基、氨基甲酰基、被低级烷基取代的氨基甲酰基、氨基磺酰基或被低级烷基取代的氨基磺酰基;R³是氢、硝基或卤素;R⁴ 是氢、低级烷基、取代的低级烷基、低级环烷基或取代的低级环烷基;R5 是独立选自卤素、硝基、氰基、低级烷基、氨基甲酰基和被低级烷基取代的氨基甲酰基组成的取代基;以及 n 是 0 至 4 的整数。该衍生物对 NMDA 受体和 AMPA 受体均有拮抗作用,因此可有效治疗由兴奋性氨基酸与受体结合引起的神经紊乱。