Spiro�heterocycle-imidazo�1,2-a!indeno�1,2-e!pyrazine!-4'-ones,
preparation thereof and drugs containing same
    24.
    发明授权
    Spiro�heterocycle-imidazo�1,2-a!indeno�1,2-e!pyrazine!-4'-ones, preparation thereof and drugs containing same 失效
    螺[杂环咪唑并[1,2-a]茚并[1,2-e]吡嗪] -4'-酮,其制备方法和含有它们的药物

    公开(公告)号:US5777114A

    公开(公告)日:1998-07-07

    申请号:US836410

    申请日:1997-06-30

    CPC分类号: C07D471/20 C07D487/20

    摘要: Compounds of formula (I): ##STR1## wherein R.sub.3 and R.sub.4, 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, --CHO, --COOR.sub.11, --CO--alk--COOR.sub.6, --CO--alk--NR.sub.6 R.sub.12, --CO--alk--CONR.sub.6 R.sub.8, --CO--COOR.sub.6, --CO--CH.sub.2 --O--CH.sub.2 --COOR.sub.6, --CO--CH.sub.2 --S--CH.sub.2 --COOR.sub.6, --CO--CH.dbd.CH--COOR.sub.6, 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--NH.sub.2, --CO--NH--alk, --CO--N(alk)alk', --CS--NH.sub.2, --CS--NH--alk, --CS--NH--Ar", --CS--NH--Het, --alk--Het, --alk--NR.sub.6 R.sub.8, --alk--COOR.sub.6, --alk--CO--NR.sub.6 R.sub.8, --alk--Ar", --SO.sub.2 --alk or --SO.sub.2 --Ar radical, or a --CO-cycloalkyl radical where the cycloalkyl is optionally 2-substituted by a carboxyl radical; or (b) a 2-pyrrolidin-5-one ring. The compounds of formula (I) have useful pharmacological properties and are .alpha.-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.

    摘要翻译: PCT No.PCT / FR95 / 01430 Sec。 371日期:1997年6月30日 102(e)日期1997年6月30日PCT 1995年10月30日PCT PCT。 WO96 / 14318 PCT公开号 日期:1996年5月17日式(I)化合物:其中R 3和R 4与它们所连接的碳原子一起形成(a)2-或3-吡咯烷环, 或4-哌啶环或2-氮杂环庚烷环,所述环任选在氮原子上被烷基,-CHO,-COOR11,-CO-烷基-COOR6,-CO-alk-NR6R12,-CO- CONR6R8,-CO-COOR6,-CO-CH2-O-CH2-COOR6,-CO-CH2-S-CH2-COOR6,-CO-CH = CH-COOR6,-CO-烷基,-CO-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或-SO2-Ar基,或-CO - 环烷基,其中环烷基任选被羧基任意地2-取代; 或(b)2-吡咯烷-5-酮环。 式(I)化合物具有有用的药理学性质,并且是α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体拮抗剂,所述受体也称为quisqualate受体。 此外,式(I)化合物是非竞争性N-甲基-D-天冬氨酸(NMDA)受体拮抗剂,特别是NMDA受体甘氨酸调节位点配体。