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    Imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds for treatment of neurotoxic injury
    8.
    发明授权
    Imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds for treatment of neurotoxic injury 失效
    咪唑并[1,2-a]吡啶基烷基膦酸化合物，用于治疗神经毒性损伤

    公开(公告)号：US5633237A

    公开(公告)日：1997-05-27

    申请号：US271395

    申请日：1994-07-06

    申请人： Donald W. Hansen, Jr. ,  Gilbert W. Adelstein ,  Karen B. Peterson ,  Sofya Tsymbalov

    发明人： Donald W. Hansen, Jr. ,  Gilbert W. Adelstein ,  Karen B. Peterson ,  Sofya Tsymbalov

    IPC分类号： C07D471/04 ,  C07F9/6561 ,  A61K31/44

    CPC分类号： C07D471/04 ,  C07F9/6561

    摘要： A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds is described for treatment 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 antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## and the carboxylic and phosphonic alkyl esters and salts thereof; wherein R.sup.9 is selected from hydrido, 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 independently selected methylene and ethylene radicals which may be unsubstituted and from methylene radicals which may be substituted with a group selected from halo, hydroxy and oxo;wherein each of m and n is a number independently selected from zero to two, inclusive; wherein each X and T is one or more groups independently selected from hydrido, alkyl, cycloalkyl, halo, haloalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl and alkanoyl; or a pharmaceutically-acceptable acid addition salt thereof.

    摘要翻译： 描述了一类咪唑并[1,2-a]吡啶基烷基膦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：其中羧酸和膦酸烷基酯及其盐; 其中R 9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各自是间隔基团，独立地选择亚甲基和亚乙基，其可以是未取代的，可以被可以被选自卤素，羟基和氧代的基团取代的亚甲基; 其中m和n各自独立地选自0至2，包括0和2; 其中每个X和T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，羟基烷基，烷氧基，烷氧基烷基和烷酰基的基团。 或其药学上可接受的酸加成盐。