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    • 49. 发明公开
    • HETEROCYCLIC COMPOUNDS AND THEIR PREPARATION AND USE
    • 杂环化合物和其生产和使用
    • EP0743945A1
    • 1996-11-27
    • EP95909651.0
    • 1995-01-30
    • NOVO NORDISK A/S
    • JEPPESEN, Lone
    • A61K31A61P1A61P3A61P25A61P29C07D487
    • C07D487/04
    • Imidazol[1,2-a]quinoxalinone derivatives of general formula (I) wherein R?1, R2, R3¿ are the same or independently are H, alkyl, alkoxy, halogen, NO¿2?, NH2, CF3, CN, SO2CH3, SO2CF3, SO2NR'R' or a 5- or 6- membered N-containing heterocyclic ring, optionally substituted, and R', R' are independently H or alkyl; and R?4¿ is H or CH¿2?-R?6; and R6¿ is H, halogen, POR'''R'''', NR7R8 or a 5- or 6-membered N-containing heterocyclic ring optionally substituted, and R''', R'''' are independently hydroxy or alkoxy; and R7, R8 are the same or independently are H, (a) or alkyl optionally substituted; and n is 1, 2, or 3; (b), CH¿2?OH, CHNOH, CN, (c) or (d) and R?9¿ is OH, alkoxy, H or NR?10R11; and R10, R11¿ are the same or independently are H, NH¿2? or OH; and X is O or S; and Y is O, S or NH2, and pharmaceutically acceptable salts thereof, have affinity for the AMPA receptors and are antagonists in connection with this type of receptor which makes them useful in the treatment of CNS ailments, especially in the treatment of any of the numerous indications caused by hyperactivity of excitatory amino acids.