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    Imidazo�1,2-a! Pyridinyldiacid compounds for cognitive enhancement and for treatment of cognitive disorders and neurotoxic injury
    10.
    发明授权
    Imidazo�1,2-a! Pyridinyldiacid compounds for cognitive enhancement and for treatment of cognitive disorders and neurotoxic injury 失效
    咪唑并[1,2-a]吡啶基二酸化合物用于认知增强和治疗认知障碍和神经毒性损伤

    公开(公告)号：US5721223A

    公开(公告)日：1998-02-24

    申请号：US538525

    申请日：1995-10-03

    申请人： Donald W. Hansen, Jr. ,  Karen B. Peterson ,  Joseph B. Monahan

    发明人： Donald W. Hansen, Jr. ,  Karen B. Peterson ,  Joseph B. Monahan

    IPC分类号： C07D471/04 ,  A61K31/44 ,  C07F9/58

    CPC分类号： C07D471/04

    摘要： A class of imidazo�1,2-a!pyridinyldiacid compounds is described for cognitive enhancement and for treatment of cognitive disorders and which have activity as a cognitive enhancer. Such compounds are also useful to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an agonist or partial agonist to modulate, or as an antagonist to inhibit, excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein each R.sup.20 is independently selected from hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Y.sub.m and Y.sub.n is a spacer group selected from methylene and ethylene radicals; wherein m is an integer of one or two; wherein n is an integer of from zero to two; wherein X is one or more groups independently selected from hydrogen, alkyl, cycloalkyl, halo, haloalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl and alkanoyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类咪唑并[1,2-a]吡啶基二酸化合物用于认知增强和治疗认知障碍，并且具有作为认知增强剂的活性。 这些化合物也可用于减少与缺氧或缺血相关的神经毒性损伤，其通常在中风，心脏骤停或围产期窒息之后。 治疗包括单独施用该类化合物或以有效量的作为调节剂的激动剂或部分激动剂的量的组合物施用，或作为抑制主要神经元兴奋性氨基酸受体位点的兴奋性毒性作用的拮抗剂。 最感兴趣的化合物是下式的化合物：其中每个R 20独立地选自氢，甲基，乙基，正丙基，异丙基，正丁基，异丁基，仲丁基，叔丁基，环丙基，环丁基， 环戊基，环己基和环庚基 其中Ym和Yn各自为选自亚甲基和亚乙基的间隔基; 其中m是1或2的整数; 其中n为0至2的整数; 其中X是一个或多个独立地选自氢，烷基，环烷基，卤素，卤代烷基，羟基，羟烷基，烷氧基，烷氧基烷基和烷酰基的基团。 或其药学上可接受的盐。