5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives,
preparation thereof, intermediates thereof and drugs containing the same
    6.
    发明授权
    5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives, preparation thereof, intermediates thereof and drugs containing the same 失效
    5H,10H-咪唑并[1,2-a]茚并[1,2-e]吡嗪-4-酮衍生物,其制备方法,其中间体和含有它们的药物

    公开(公告)号:US5990108A

    公开(公告)日:1999-11-23

    申请号:US101428

    申请日:1998-07-09

    CPC分类号: C07D487/04 C07F9/6561

    摘要: Compounds of formula (I), wherein R is a hydrogen atom or a --COOH, -alk-COOH, --PO.sub.3 H.sub.2, --CH.sub.2 --PO.sub.3 H.sub.2, or --CH.dbd.CH--COOH radical, or a phenyl radical substituted by a carboxy radical, R.sub.1 is an alk-CN, -alk-COOH, -alk-Het, alk-PO.sub.3 H.sub.2 or -alk-CO--NH--SO.sub.2 R.sub.2 radical, R.sub.2 is an alkyl or phenyl radical, alk is an alkyl radical, Het is a saturated or unsaturated mono- or polycyclic heterocyclic ring containing 1-9 carbon atoms and one or more heteroatoms selected from O, S and N, said heterocyclic ring optionally being substituted by one or more alkyl, phenyl or phenylalkyl radicals, with the proviso that when R is a hydrogen atom or a --COOH or --PO.sub.3 H.sub.2 radical, R.sub.1 cannot be -alk-COOH, isomers, racemic mixtures, enantiomers and diastereoisomers thereof, salts thereof, the preparation thereof, intermediates thereof and drugs containing said compounds, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor, and specifically ligands for NMDA receptor glycine modulator sites. ##STR1##

    摘要翻译: PCT No.PCT / FR97 / 00019 Sec。 371日期:1998年7月9日 102(e)日期1998年7月9日PCT 1997年1月6日PCT PCT。 出版物WO97 / 25328 日期:1997年7月17日式(I)化合物其中R为氢原子或-COOH,-alk-COOH,-PO3H2,-CH2-PO3H2或-CH = CH-COOH基,或苯基取代 通过羧基,R 1是烷基-C CN,-alk-COOH,-alk-Het,alk-PO 3 H 2或-alk -CO-NH-SO 2 R 2基团,R 2是烷基或苯基, Het是含有1-9个碳原子和一个或多个选自O,S和N的杂原子的饱和或不饱和单环或多环杂环,所述杂环任选被一个或多个烷基,苯基或苯基烷基取代,其中 条件是当R是氢原子或-COOH或-PO 3 H 2基团时,R 1不能是-alk COOH,其异构体,外消旋混合物,对映异构体和非对映异构体,其盐,其制备,其中间体和含有所述化合物的药物, 被披露。 式(I)化合物具有有价值的药理学性质,也是也称为quisqualate受体的α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体的拮抗剂。 此外,式(I)化合物是N-甲基-D-天冬氨酸(NMDA)受体的非竞争性拮抗剂,特别是NMDA受体甘氨酸调节剂位点的配体。