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88 条记录 (耗时 0.031 秒)

    1,2,3,4-tetrahydroquinoline 2,3,4-trione-3 or 4-oximes
    83.
    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

    申请人： Sui Xiong Cai ,  John F. W. Keana ,  Eckard Weber

    发明人： Sui Xiong Cai ,  John F. W. Keana ,  Eckard Weber

    IPC分类号： A61K31/47 ,  A61K51/04 ,  A61P9/10 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  C07D215/38 ,  C07D215/42 ,  C07D215/22 ,  C07D215/44 ,  C07D215/46

    CPC分类号： C07D215/42 ,  A61K31/47 ,  A61K51/0455 ,  C07D215/38 ,  A61K2121/00

    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。

    Glycine receptor antagonists and the use thereof
    84.
    发明授权
    Glycine receptor antagonists and the use thereof 失效
    甘氨酸受体拮抗剂及其用途

    公开(公告)号：US5620979A

    公开(公告)日：1997-04-15

    申请号：US405708

    申请日：1995-03-17

    申请人： Eckard Weber ,  John F. W. Keana

    发明人： Eckard Weber ,  John F. W. Keana

    IPC分类号： C07D241/44 ,  A61K20060101 ,  A61K31/495 ,  A61K31/498 ,  A61K45/00 ,  A61K51/04 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  C07D241/38 ,  C07D241/52 ,  C07D241/54 ,  C07D487/04 ,  C07D491/04

    CPC分类号： C07D491/04 ,  A61K31/495 ,  A61K51/0459 ,  C07D241/38 ,  C07D241/44 ,  C07D241/52 ,  C07D241/54 ,  C07D487/04

    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, inducing anesthesia and treating psychosis are disclosed by administering to an animal in need of such treatment a compound having high affinity for the glycine binding site, lacking PCP side effects and which crosses the blood brain barrier of the animal.Also disclosed are novel 1,4-dihydroquinoxaline-2,3-diones, and pharmaceutical compositions thereof. Also disclosed are highly soluble ammonium salts of 1,4-dihydroquinoxaline-2,3-diones.

    摘要翻译： 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，治疗或预防多动症的不良后果 通过向需要这种治疗的动物施用兴奋性氨基酸以及治疗焦虑症，慢性疼痛，惊厥，诱导麻醉和治疗精神病，通过向甘氨酸结合位点具有高亲和力的化合物，缺乏PCP副作用和哪些 穿过动物的血脑屏障。 还公开了新的1,4-二氢喹喔啉-2,3-二酮及其药物组合物。 还公开了1,4-二氢喹喔啉-2,3-二酮的高度可溶性铵盐。

    N,N'-disubstituted guanidines and their use as excitatory amino acid antagonists
    86.
    发明授权
    N,N'-disubstituted guanidines and their use as excitatory amino acid antagonists 失效
    N，N'-二取代胍及其作为兴奋性氨基酸拮抗剂的用途

    公开(公告)号：US5190976A

    公开(公告)日：1993-03-02

    申请号：US844498

    申请日：1992-03-02

    申请人： Eckard Weber ,  John F. W. Keana

    发明人： Eckard Weber ,  John F. W. Keana

    IPC分类号： C07D215/40 ,  A01N37/52 ,  A61K31/155 ,  A61K31/365 ,  A61K31/37 ,  A61K31/47 ,  A61P25/00 ,  A61P25/28 ,  C07C279/18 ,  C07D311/18

    CPC分类号： C07C279/18 ,  A61K31/155 ,  A61K31/365 ,  A61K31/47

    摘要： N,N'-disubstituted guanidines exhibiting a high binding affinity to phencyclidine (PCP) receptors are disclosed. These N,N'-disubstituted guanidine derivatives act as non-competitive inhibitors or glutamate-induced responses generated via the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert a neuroprotective property and are useful in the therapeutic treatment of neuronal loss in hypoxia, brain or spinal cord ischemia, brain or spinal cord trauma, as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

    摘要翻译： 公开了对苯环利定（PCP）受体表现出高结合亲和力的N，N'-二取代的胍。 这些N，N'-二取代的胍衍生物作为非竞争性抑制剂或通过NMDA受体产生的谷氨酸盐诱导的反应，作为NMDA受体 - 离子通道复合物的离子通道的阻断剂。 因此，这些化合物发挥神经保护性质，并且可用于治疗缺氧，脑或脊髓缺血，脑或脊髓创伤中的神经元丧失，以及用于治疗癫痫，阿尔茨海默病，肌萎缩性侧索硬化， 亨廷顿氏病，唐氏综合征，柯萨科夫病和其他神经退行性疾病。