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    Phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compounds for treatment of neurotoxic injury
    10.
    发明授权
    Phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compounds for treatment of neurotoxic injury 失效
    膦酰基甲基 - 咪唑并[1,2-a]嘧啶-2-羧酸化合物，用于治疗神经毒性损伤

    公开(公告)号：US5302586A

    公开(公告)日：1994-04-12

    申请号：US982819

    申请日：1992-11-30

    申请人： Alexis A. Cordi ,  Eric T. Sun

    发明人： Alexis A. Cordi ,  Eric T. Sun

    IPC分类号： C07F9/6561 ,  A61K31/505 ,  C07F9/09

    CPC分类号： C07F9/6561

    摘要： A class of phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest, hypoglycemia or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective 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 of R.sup.1, R.sup.2 and R.sup.6 is independently selected from hydrido, alkyl, allyl, cycloalkyl, cycloalkylalkyl, phenyl and benzyl; wherein Y.sub.m is --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --; where m is one; wherein x is one or more groups attachable at one or more of the 5-, 6- and 7-ring positions of the imidazo[1,2-a]pyrimidine ring system; wherein each x and T is independently selected from hydrido, halo, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkenyl, alkynyl, phenyl, benzyl, hydroxy, hydroxyalkyl, alkoxy, phenoxy, alkoxyalkyl, benzyloxy, cyano, alkanoyl, alkylthio, arylthio and amino; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类膦酰基甲基 - 咪唑并[1,2-a]嘧啶-2-羧酸化合物用于治疗，以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，低血糖或围产期窒息之后。 治疗包括单独施用该类化合物或以有效作为拮抗剂的量的组合物施用以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。 最感兴趣的化合物是下式的化合物：其中R 1，R 2和R 6各自独立地选自氢，烷基，烯丙基，环烷基，环烷基烷基，苯基和苄基; 其中Ym是-CH 2 - 或-CH 2 -CH 2 - ; 哪里是一个; 其中x是在咪唑并[1,2-a]嘧啶环系统的一个或多个5-，6-和7-环位置可连接的一个或多个基团; 其中每个x和T独立地选自氢，卤素，烷基，环烷基，环烷基烷基，卤代烷基，烯基，炔基，苯基，苄基，羟基，羟烷基，烷氧基，苯氧基，烷氧基烷基，苄氧基，氰基，烷酰基，烷硫基，芳硫基和氨基 ; 或其药学上可接受的盐。