INDOLE-2-CARBOXAMIDINE DERIVATIVES AS NMDA RECEPTOR ANTAGONISTS
    8.
    发明授权
    INDOLE-2-CARBOXAMIDINE DERIVATIVES AS NMDA RECEPTOR ANTAGONISTS 有权
    吲哚-2-甲脒衍生物作为NMDA受体拮抗剂

    公开(公告)号:EP1773770B1

    公开(公告)日:2009-04-01

    申请号:EP05764412.2

    申请日:2005-07-21

    摘要: The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I) - wherein the meaning of X is hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl group, Y, V and Z independently are hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, trifluoromethyl, trifluoromethoxy, C1-C4 alkyl, C1-C4 alkoxy group, or the neighboring V and Z groups in given case together with one or more identical or different additional hetero atom and -CH= and/or -CH2- groups can form an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably benzene, dioxolane ring, A, B and C independently are substituted carbon atom or one of them is nitrogen atom, and the salts thereof. Further objects of the invention are the processes for producing indole-2-carboxamidine derivatives of formula (I), and the pharmaceutical manufacture of medicaments containing these compounds, as well as the process of treatments with these compounds, which means administering to a mammal to be treated - including human - effective amount/amounts of indole-2-carboxamidine derivatives of formula (I) of the present invention as such or as medicament. The new indole-2-carboxamidine derivatives of formula (I) of the present invention are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.