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    Excitatory amino acid receptor antagonists in methods for the use thereof
    6.
    发明授权
    Excitatory amino acid receptor antagonists in methods for the use thereof 失效
    兴奋性氨基酸受体拮抗剂在使用方法中

    公开(公告)号：US5196421A

    公开(公告)日：1993-03-23

    申请号：US904358

    申请日：1992-06-25

    申请人： Loretta A. McQuaid ,  Charles H. Mitch ,  Paul L. Ornstein ,  Darryle D. Schoepp ,  Edward C. R. Smith

    发明人： Loretta A. McQuaid ,  Charles H. Mitch ,  Paul L. Ornstein ,  Darryle D. Schoepp ,  Edward C. R. Smith

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

    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: ##STR1## in which: each of A.sub.1, A.sub.2 and A.sub.3 is independently either C or N, except that at least one of A.sub.1, A.sub.2 and A.sub.3 is N; one of A.sub.4 and A.sub.5 is C and the other is N; each R.sub.1 and R.sub.2 is independently hydrogen, halogen, CN, NO.sub.2, alkyl, aromatic, azido or CF.sub.3 ; and R.sub.3 is hydrogen, alkyl, aromatic or CF.sub.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, 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结构式的化合物：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 是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受体的EAA拮抗剂，作为神经保护剂，以及治疗与EAA受体相关的各种神经障碍。