发明名称 INDOLE-2-CARBOXAMIDINE DERIVATIVES AS NMDA RECEPTOR ANTAGONISTS
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, C-Calkyl, C-Calkoxy, trifluoromethyl group, Y, V and Z independently are hydrogen or halogen atom, hydroxy, cyano, C-Calkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C-Calkanoylamido optionally substituted by a halogen atom or halogen atoms, trifluoromethyl, trifluoromethoxy, C-Calkyl, C-Calkoxy 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 –CH- groups can form an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably benzene, dioxolane ring, A, B and C independently are a 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 pharmaceutical manufacture of medicaments containing these compounds as well as processes for the treatments with these compounds, which means administering 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 antagonists of NR2B subtype of NMDA receptor.
申请公布号 EA009981(B1) 申请公布日期 2008.04.28
申请号 EA20070000365 申请日期 2005.07.21
申请人 RICHTER GEDEON VEGYESZETI GYAR RT. 发明人 BORZA ISTVAV;HORVATH CSILLA;FARKAS SANDOR;NAGY JOSEF;KOLOK SANDOR
分类号 C07D209/42;A61K31/405;A61P25/00;C07D401/12;C07D405/12 主分类号 C07D209/42
代理机构 代理人
主权项
地址