利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

6 条记录 (耗时 0.014 秒)

    Improvements in or relating to excitatory amino acid receptor antagonists
    1.
    发明公开
    Improvements in or relating to excitatory amino acid receptor antagonists 失效
    在Bezug auf exzitatorischeAminosäurenrezeptorantagonisten的Verbesserungen von oder。

    公开(公告)号：EP0518530A2

    公开(公告)日：1992-12-16

    申请号：EP92304887.0

    申请日：1992-05-29

    申请人： ELI LILLY AND COMPANY

    发明人： McQuaid, Loretta Ames ,  Mitch, Charles Howard ,  Ornstein, Paul Leslie ,  Schoepp, Darryle Darwin ,  Smith, Edward C. R.

    IPC分类号： A61K31/50 ,  A61K31/505

    CPC分类号： C07D487/04 ,  A61K31/495 ,  A61K31/505

    摘要： Excitatory amino acid receptor antagonists and methods for the use thereof are disclosed. The antagonists include compounds having the preferred formula :

    or

    in which : each of A 1 , A 2 and A3 is independently either C or N, except that at least one of A 1 , A 2 and A3 is N ; one of A4 and A 5 is C and the other is N ; each R 1 and R 2 is independently hydrogen, halogen, CN, NO2, alkyl, aromatic, azido or CF 3 ; and R 3 is hydrogen, alkyl, aromatic or CF 3 . Also included are the tautomers thereof, and the pharmaceutically acceptable salts of (III) and (IV) and the tautomers thereof. These compounds are useful as EAA antagonists for blocking one or more EAA receptors, for reducing EAA phosphoinositide hydrolysis, as neuroprotective agents, and in the treatment of various neurological disorders associated with EAA receptors.

    摘要翻译： 公开了兴奋性氨基酸受体拮抗剂及其使用方法。 拮抗剂包括具有以下优选的化合物：或，其中：A1，A2和A3各自独立地为C或N，除了A1，A2和A3中的至少一个为N; A4和A5之一是C，另一个是N; 每个R 1和R 2独立地是氢，卤素，CN，NO 2，烷基，芳族，叠氮基或CF 3; 并且R 3是氢，烷基，芳族或CF 3。 还包括其互变异构体和（III）和（IV）的药学上可接受的盐及其互变异构体。 这些化合物可用作阻断一种或多种EAA受体，用于减少EAA磷酸肌醇水解作为神经保护剂的EAA拮抗剂，以及用于治疗与EAA受体相关的各种神经障碍。

    Improvements in or relating to excitatory amino acid receptor antagonists
    3.
    发明公开
    Improvements in or relating to excitatory amino acid receptor antagonists 失效
    改善或相关于激素氨基酸受体拮抗剂

    公开(公告)号：EP0518530A3

    公开(公告)日：1993-01-20

    申请号：EP92304887.0

    申请日：1992-05-29

    申请人： ELI LILLY AND COMPANY

    发明人： McQuaid, Loretta Ames ,  Mitch, Charles Howard ,  Ornstein, Paul Leslie ,  Schoepp, Darryle Darwin ,  Smith, Edward C. R.

    IPC分类号： A61K31/50 ,  A61K31/505

    CPC分类号： C07D487/04 ,  A61K31/495 ,  A61K31/505

    摘要： Excitatory amino acid receptor antagonists and methods for the use thereof are disclosed. The antagonists include compounds having the preferred formula :

    or

    in which : each of A 1 , A 2 and A3 is independently either C or N, except that at least one of A 1 , A 2 and A3 is N ; one of A4 and A 5 is C and the other is N ; each R 1 and R 2 is independently hydrogen, halogen, CN, NO2, alkyl, aromatic, azido or CF 3 ; and R 3 is hydrogen, alkyl, aromatic or CF 3 . Also included are the tautomers thereof, and the pharmaceutically acceptable salts of (III) and (IV) and the tautomers thereof. These compounds are useful as EAA antagonists for blocking one or more EAA receptors, for reducing EAA phosphoinositide hydrolysis, as neuroprotective agents, and in the treatment of various neurological disorders associated with EAA receptors.