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    QUINOXALINEDIONE DERIVATIVES AS EAA ANTAGONISTS
    1.
    发明授权
    QUINOXALINEDIONE DERIVATIVES AS EAA ANTAGONISTS 失效
    喹喔啉AS EAA拮抗剂

    公开(公告)号：EP0664807B1

    公开(公告)日：1997-09-10

    申请号：EP93922849.0

    申请日：1993-10-08

    申请人： WARNER-LAMBERT COMPANY

    发明人： BIGGE, Christopher, Franklin ,  MALONE, Thomas, Charles ,  WÄTJEN, Frank

    IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/495 ,  A61K31/55 ,  C07F9/6561 ,  A61K31/675 ,  C07D215/40 ,  C07D215/38 ,  C07D217/02 ,  C07D217/04 ,  C07D209/48

    CPC分类号： C07D471/04 ,  C07D217/04 ,  C07D487/04 ,  C07F9/6561

    摘要： A compound having formula (I) or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or hydroxy; R1 is hydrogen, alkyl, arylalkyl, (CH¿2?)nOH or (CH2)nNR?7R8; R5 and R6¿ are each independently hydrogen, halogen, NO¿2?, CN, CF3, SO2NR?7R8, PO¿3R9R10, alkyl, alkenyl, alkynyl, (CH¿2?)nCONR?7R8, (CH¿2)nCO2R?10, NHCOR11¿, wherein R?7 and R8¿ are each independently hydrogen or alkyl or together R?7 and R8¿ form a ring of from three to seven atoms, R9 is hydrogen or alkyl, R10 is hydrogen or alkyl, R11 is hydrogen or alkyl, and n is an integer of from zero to four; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b, and formed by the following bivalent radicals: a-NR?12-CHR13-CHR14¿-b, a-CHR?13-CHR14-NR12¿-b, a-CHR?13-NR12-CHR14¿-b, a-CHR14-CH2-NR?12-CHR13¿-b, a-CHR?13-NR12-CH¿2-CHR14-b, a-CH¿2?-CH2-CHR?13-NR12¿-b, a-NR?12-CHR13-CH¿2-CH2-b, a-CH2-CH2-NR12-CH2-CH2-b, a-CH2-CH2-CH2-NR12-CH2-b, a-CH2-NR12-CH2-CH2-CH2-b, a-CH2-CH2-CH2-CH2-NR12-b, a-NR12-CH2-CH2-CH2-CH2-b, wherein R12 is hydrogen, CH¿2?CH2OH, or alkyl, and R?13 and R14¿ are each independently hydrogen, CN, CONH¿2?, CH2NH2, CH2OH, alkyl, arylalkyl, alkenyl or CO2R?15¿, wherein R15 is hydrogen or alkyl. The compounds are useful in the treatment of disorders of mammals, responsive to the blockade of glutamic and aspartic acid receptors. Processes for preparing the compounds and novel intermediate useful in the processes are also included.