Derivatives of 2-carboxyindoles having pharmaceutical activity
    2.
    发明授权
    Derivatives of 2-carboxyindoles having pharmaceutical activity 失效
    具有药物活性的2-羧基吲哚衍生物

    公开(公告)号:US5284862A

    公开(公告)日:1994-02-08

    申请号:US839109

    申请日:1992-02-27

    CPC分类号: C07D209/42

    摘要: The present invention relates to novel 3-substituted-2-carboxyindoles; including as 3-substituents amides of hydroxamic acids and derivatives thereof or urea and carbonyl, carboxyl or phosphonic acids or ester amides, or 2-acylsulfonamides thereof; and including also as 3-substituents unsaturated acids and their further ester and amide derivatives. These 2-carboxyindoles are useful as pharmaceutical agents, therefore, the present invention is also pharmaceutical compositions and pharmaceutical methods of treatment therefor. The compounds of the present invention are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders.

    摘要翻译: 本发明涉及新的3-取代-2-羧基吲哚; 包括异羟肟酸及其衍生物或脲的3-取代基酰胺和羰基,羧基或膦酸或酯酰胺或其2-酰基磺酰胺; 并且还包括3-取代基不饱和酸及其另外的酯和酰胺衍生物。 这些2-羧基吲哚可用作药物,因此,本发明也是药物组合物及其治疗方法。 本发明的化合物可用于治疗神经变性疾病,包括脑血管障碍。

    N-substituted .alpha.-amino acids and derivatives thereof having
pharmaceutical activity
    6.
    发明授权
    N-substituted .alpha.-amino acids and derivatives thereof having pharmaceutical activity 失效
    具有药物活性的N-取代的α-氨基酸及其衍生物

    公开(公告)号:US5179085A

    公开(公告)日:1993-01-12

    申请号:US689726

    申请日:1991-04-22

    IPC分类号: C07F9/38 C07F9/40

    摘要: N-substituted .alpha.-amino acids and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in selectively blocking the N-methyl-D-aspartate (NMDA) excitatory amino acid receptors in mammals and also are useful in treating cerebrovascular disorders such as cerebral ischemia or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasm, hypoglycemia, cardiac arrest, status epilepticus and cerebral trauma as well as for treating schizophrenia, epilepsy, neurodegenerative disorders, Alzheimer's disease or Huntington's disease and also additionally useful as anesthetics in surgical procedures where a finite risk of cerebrovascular damage exists.

    摘要翻译: 描述了N-取代的α-氨基酸及其衍生物,以及其制备方法及其药物组合物,其可用于选择性阻断哺乳动物中的N-甲基-D-天冬氨酸(NMDA)兴奋性氨基酸受体,以及 也可用于治疗由血栓栓塞或出血性脑卒中,脑血管痉挛,低血糖症,心脏骤停,癫痫持续状态和脑损伤引起的脑缺血或脑梗死,以及用于治疗精神分裂症,癫痫,神经退行性疾病,阿尔茨海默病或亨廷顿舞蹈症的脑血管疾病 疾病,另外作为麻醉剂在脑血管损伤存在有限风险的外科手术中也是有用的。