Polycyclic alcaloid-derivatives as NMDA-receptor antagonists
    6.
    发明授权
    Polycyclic alcaloid-derivatives as NMDA-receptor antagonists 失效
    多环类别衍生物作为NMDA-受体拮抗剂

    公开(公告)号:US5990104A

    公开(公告)日:1999-11-23

    申请号:US981935

    申请日:1998-03-25

    摘要: Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor. ##STR1##

    摘要翻译: PCT No.CPC / CA96 / 00468 Sec。 371日期:1998年3月25日 102(e)1998年3月25日PCT PCT 1996年7月12日PCT公布。 公开号WO97 / 03929 日期:1997年2月6日式(I)的多环生物碱,其中R 1为H,C 1-6烷基或任选被极性基团取代的C 6-12芳基; R2和R3独立地是H,OH,C1-6烷基,-C(NH)-NH2,带正电荷的基团或任选被NH 2,OH,C 1-6烷基或卤素取代的C 7-13芳烷基; 或R 2和R 3一起形成任选地加入杂原子的5至6元环; R4是H,C1-6烷基,OR6,SR6或N(R6)2,其中每个R6独立地是H,C1-3烷基; X ix O,S,SO,SO 2或N-R 5,其中每个R 5独立地为H,C 1-6烷基或任选被一个或多个杂原子间断的C 7-13芳烷基; n为0〜2的整数; m是0-3的整数。这些化合物在离子型NMDA(N-甲基 - (D) - 天冬氨酸)受体上起拮抗剂的作用。