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    Substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-Hydroxy-1H-Pyrrole-2,5-diones, their analogs and their salts
    3.
    发明公开
    Substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-Hydroxy-1H-Pyrrole-2,5-diones, their analogs and their salts 失效
    取代3-（2,3-二氢-1H-茚-5-基）-4-羟基-1H-吡咯-2,5-二酮，分析和分析。

    公开(公告)号：EP0160891A1

    公开(公告)日：1985-11-13

    申请号：EP85105005.4

    申请日：1985-04-25

    申请人： Merck & Co., Inc.

    发明人： Cragoe, Edward J., Jr. ,  Woltersdorf, Otto W., Jr.

    IPC分类号： C07D207/456 ,  C07D409/10 ,  C07D409/12 ,  A61K31/40

    CPC分类号： C07D207/456 ,  C07D409/10

    摘要： The invention relates to novel compounds of the formula:
    in which R and R' are different entities and wherein

    A is a bond, -0- or -0-(CH 2 )q;
    q is 1 to 5;
    z is 0 or H and OH;
    R is cycloalkyl, cycloalkyl-lower alkyl, aryl selected from phenyl, halophenyl, methoxyphenyl, hydroxyphenyl, heterocyclic including thienyl, aralkyl selected from benzyl and phenethyl, lower alkyl, lower alkenyl or lower alkynyl;
    R' is lower alkyl, lower alkenyl; or lower alkynyl;

    and X and Y are selected from halo and methyl provided that when A is a bond or when A is -O- and z is H and OH, R is not cycloalkyl or alkyl when R' is lower alkyl and both X and Y are chloro when the compounds are racemic.
    The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke, arrested breathing, cardiac arrest, Reye's syndrom, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.

    摘要翻译： 本发明涉及下式的新化合物：其中R和R min是不同的实体，其中A是键，-O-或-O-（CH 2）q; q为1〜5; z是O或H和OH; R是环烷基，环烷基 - 低级烷基，选自苯基，卤代苯基，甲氧基苯基，羟基苯基，包括噻吩基的杂环基，选自苄基和苯乙基，低级烷基，低级烯基或低级炔基的芳烷基。 R min为低级烷基，低级烯基; 或低级炔基; 并且X和Y选自卤素和甲基，条件是当A为键或当A为-O-且z为H且OH时，当R min为低级烷基且X和Y都为氯时，R不为环烷基或烷基 当化合物是外消旋的。 这些化合物可用于治疗和预防脑部损伤以及头部创伤，中风，呼吸停止，心脏骤停，Reye综合征，脑血栓形成，脑栓塞，脑出血，脑肿瘤，脑脊髓炎，脊髓损伤 脑积水，术后脑损伤创伤，脑部感染引起的水肿和各种脑震荡。