Alkyl, azido, alkoxy, and fluoro-substituted and fused quinoxalinediones and the use thereof as glycine receptor antagonist
    81.
    发明授权
    Alkyl, azido, alkoxy, and fluoro-substituted and fused quinoxalinediones and the use thereof as glycine receptor antagonist 有权
    烷基,叠氮基,烷氧基和氟取代和稠合的喹喔啉并且其作为甘氨酸受体拮抗剂的用途

    公开(公告)号:US06251903B1

    公开(公告)日:2001-06-26

    申请号:US09661475

    申请日:2000-09-13

    IPC分类号: A61K31495

    摘要: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia, and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, and inducing anesthesia are disclosed by administering to an animal in need of such treatment an alkyl or azido-substituted 1,4-dihydroquinoxaline-2,3-dione or pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.

    摘要翻译: 治疗或预防与中风,局部缺血,CNS创伤,低血糖症和手术相关的神经元损失的方法,以及治疗神经变性疾病,包括阿尔茨海默病,肌萎缩性侧索硬化,亨廷顿病和唐氏综合征,治疗或预防不良后果 通过向需要这种治疗的动物施用烷基或叠氮基取代的1,4-二氢喹喔啉-2,3-二酮来公开兴奋性氨基酸的多动症以及治疗焦虑症,慢性疼痛,抽搐和诱导麻醉 或其药学上可接受的盐,其与甘氨酸受体具有高结合性。

    Azepine compounds
    85.
    发明授权
    Azepine compounds 失效
    Azepine化合物

    公开(公告)号:US5708168A

    公开(公告)日:1998-01-13

    申请号:US544107

    申请日:1995-10-17

    摘要: Disclosed are methods of preparing azepines by a multistep synthesis including a Diels-Alder reaction. Also disclosed are methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment an azepine which has high binding to the NMDA glycine site.

    摘要翻译: 公开了通过包括Diels-Alder反应的多步合成来制备氮杂的方法。 还公开了治疗或预防与中风,缺血,CNS创伤,低血糖和手术相关的神经元损失以及治疗神经变性疾病包括阿尔茨海默病,肌萎缩性侧索硬化,亨廷顿病和唐氏综合征的治疗或预防方法,治疗或预防不良后果 兴奋性氨基酸的多动症以及治疗焦虑症,慢性疼痛,抽搐,诱导麻醉和治疗或预防阿片剂耐受性的公开通过向需要这种治疗的动物施用与NMDA甘氨酸位点具有高结合性的吖庚因 。

    1,2,3,4-tetrahydroquinoline 2,3,4-trione-3 or 4-oximes
    86.
    发明授权
    1,2,3,4-tetrahydroquinoline 2,3,4-trione-3 or 4-oximes 失效
    1,2,3,4-四氢喹啉2,3,4-三酮-3或4-肟

    公开(公告)号:US5652368A

    公开(公告)日:1997-07-29

    申请号:US536937

    申请日:1995-09-29

    摘要: Disclosed herein are substituted or unsubstituted 1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes or pharmaceutically acceptable salts thereof that have high binding to the glycine receptor and are usefully administered to animals for the treatment or prevention of the adverse consequences of the hyperactivity of the excitatory amino acids, or neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, for the treatment of anxiety, chronic pain, convulsions, and neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome; and for the inducement of anesthesia.

    摘要翻译: 本文公开了与甘氨酸受体具有高结合性的取代或未取代的1,2,3,4-四氢喹啉-2,3,4-三酮-3或4-肟或其药学上可接受的盐,并有用于动物给予 治疗或预防兴奋性氨基酸多动症或与中风,缺血,CNS创伤,低血糖和手术相关的神经元损失的不良后果,用于治疗焦虑,慢性疼痛,抽搐和神经变性疾病,包括阿尔茨海默病, 肌萎缩性侧索硬化,亨廷顿氏病和唐氏综合征; 并诱导麻醉。