QUINOXALINEDIONE DERIVATIVES AS EAA ANTAGONISTS

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.