SPIRO HETEROCYCLE-IMIDAZO(1,2-a]INDENO(1,2-e]PYRAZINE]-4'-ONES, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT
    8.
    发明公开
    SPIRO HETEROCYCLE-IMIDAZO(1,2-a]INDENO(1,2-e]PYRAZINE]-4'-ONES, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT 失效
    螺[HETEROZYCLISCHE咪唑并[1,2-α]茚并[1,2-e]吡嗪将)-4'- ONE,它们的生产和药物含有它们

    公开(公告)号:EP0789699A1

    公开(公告)日:1997-08-20

    申请号:EP95936624.0

    申请日:1995-10-30

    CPC分类号: C07D471/20 C07D487/20

    摘要: Compounds of formula (I), wherein R3 and R4, taken together with the carbon atom to which they are attached, form (a) a 2- or 3-pyrrolidine ring, a 2- or 4-piperidine ring or a 2-azacycloheptane ring, said rings being optionally substituted at the nitrogen atom by an alkyl radical, -CHO, -COOR11, -CO-alk-COOR6, -CO-alk-NR6R12, -CO-alk-CONR6R8, -CO-COOR6, -CO-CH2-O-CH2-COOR6, -CO-CH2-S-CH2-COOR6, -CO-CH=CH-COOR6, -CO-alk, -CO-Ar'. -CO-alk-Ar', -CO-NH-Ar', -CO-NH-alk-Ar', -CO-Het, -CO-alk-Het, -CO-NH-Het, -CO-NH-alk-Het, -CO-NH2, -CO-NH-alk, -CO-N(alk)alk', -CS-NH2, -CS-NH-alk, -CS-NH-Ar', -CS-NH-Het, -alk-Het, -alk-NR6R8, -alk-COOR6, -alk-CO-NR6R8, -alk-Ar', -SO2-alk, -SO2-Ar or -CO-cycloalkyl, where the cycloalkyl is optionally 2-substituted by a carboxy radical; or (b) a 2-pyrrolidine-5-one ring. The compounds of formula (I) have useful pharmacological properties and are α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and especially NMDA receptor glycine modulation site ligands.