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    • 1. 发明授权
    • Oxopyridinylquinoxaline derivative
    • 氧吡嗪基喹喔啉衍生物
    • US5677305A
    • 1997-10-14
    • US418196
    • 1995-04-07
    • Susumu TakadaNobuo ChomeiMakoto AdachiMasami EigyoKazuo Kawasaki
    • Susumu TakadaNobuo ChomeiMakoto AdachiMasami EigyoKazuo Kawasaki
    • C07D401/04C07D241/36A01N43/60C07D241/38
    • C07D401/04
    • An oxopyridinylquinoxaline derivative represented by the following Formula I or pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1 is hydrogen, halogen, nitro, or trihalomethyl; R.sup.2 is hydrogen, halogen, nitro, cyano, trihalomethyl, carbamoyl, carbamoyl substituted with lower alkyl, sulfamoyl, or sulfamoyl substituted with lower alkyl; R.sup.3 is hydrogen, nitro, or halogen; R.sup.4 is hydrogen, lower alkyl, substituted lower alkyl, lower cycloalkyl, or substituted lower cycloalkyl; R.sup.5 '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.
    • 由下式I表示的氧代吡啶基喹喔啉衍生物或其药学上可接受的盐:其中R 1是氢,卤素,硝基或三卤代甲基; 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,氨磺酰基或被低级烷基取代的氨磺酰基; 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; R 5是独立地选自卤素,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的取代基。 并且n为0至4的整数。该衍生物作为对NMDA受体和AMPA受体的拮抗剂起作用,因此其作为由与受体结合的兴奋性氨基酸引起的神经障碍的治疗剂是有效的。