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    Tri-and tetra-substituted guanidines and their use as excitatory amino acid antagonists
    31.
    发明授权
    Tri-and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
    三取代和四取代的胍和它们作为兴奋性氨基酸拮抗剂的用途

    公开(公告)号：US5767162A

    公开(公告)日：1998-06-16

    申请号：US470345

    申请日：1995-06-06

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

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

    IPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18 ,  A61K31/37 ,  A61K31/655

    CPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18

    摘要： Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

    摘要翻译： 表现出对苯环利定（PCP）受体的高结合亲和力，更优选对大脑σ受体的低亲和力的三取代和四取代胍基。 这些胍衍生物通过作为NMDA受体 - 离子通道复合物的离子通道的阻断剂，作为NMDA受体的谷氨酸诱导反应的非竞争性抑制剂。 因此，这些化合物发挥神经保护活性，并且可用于治疗缺氧，低血糖，脑或脊髓缺血以及脑或脊髓创伤中的神经元损失，以及用于治疗癫痫，阿尔茨海默病，肌萎缩性侧索硬化症 ，帕金森病，亨廷顿舞蹈病，唐氏综合征，柯萨科夫病和其他神经退行性疾病。

    4-hydroxy-3-nitro-1,2-dihydroquinolin-2-ones and the use thereof as excitatory amino acid and glycine receptor antagonists
    32.
    发明授权
    4-hydroxy-3-nitro-1,2-dihydroquinolin-2-ones and the use thereof as excitatory amino acid and glycine receptor antagonists 失效
    4-羟基-3-硝基-1,2-二氢喹啉-2-酮及其作为兴奋性氨基酸和甘氨酸受体拮抗剂的用途

    公开(公告)号：US5622965A

    公开(公告)日：1997-04-22

    申请号：US101244

    申请日：1993-08-02

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

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

    IPC分类号： A61K31/47 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  C07D215/22 ,  C07D215/38

    CPC分类号： C07D215/22 ,  A61K31/47

    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 a substituted or unsubstituted 4-hydroxy-3-nitro-1,2-dihydroquinolin-2-one 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取代或未取代的4-羟基-3-硝基-1,2-二氢喹啉-2-酮，通过给予兴奋性氨基酸以及治疗焦虑症，慢性疼痛，抽搐和诱导麻醉， 其与甘氨酸受体具有高结合性的一种或其药学上可接受的盐。

    1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes and the use thereof
    34.
    发明授权
    1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes and the use thereof 失效
    1,2,3,4-四氢喹啉-2,3,4-三酮-3或4-肟及其用途

    公开(公告)号：US5475007A

    公开(公告)日：1995-12-12

    申请号：US69005

    申请日：1993-05-28

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

    发明人： Sui X. 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

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

    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 a substituted or unsubstituted 1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oxime 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，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取代或未取代的1,2,3,4-四氢喹啉-2,3,4-四氢喹啉， 与甘氨酸受体具有高结合性的三酮-3或4-肟或其药学上可接受的盐。

    Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists
    35.
    发明授权
    Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
    三取代和四取代的胍和它们作为兴奋性氨基酸拮抗剂的用途

    公开(公告)号：US5559154A

    公开(公告)日：1996-09-24

    申请号：US105456

    申请日：1993-08-11

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

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

    IPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18

    CPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18

    摘要： Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

    摘要翻译： 表现出对苯环利定（PCP）受体的高结合亲和力，更优选对大脑σ受体的低亲和力的三取代和四取代胍基。 这些胍衍生物通过作为NMDA受体 - 离子通道复合物的离子通道的阻断剂，作为NMDA受体的谷氨酸诱导反应的非竞争性抑制剂。 因此，这些化合物发挥神经保护活性，并且可用于治疗缺氧，低血糖，脑或脊髓缺血以及脑或脊髓创伤中的神经元损失，以及用于治疗癫痫，阿尔茨海默病，肌萎缩性侧索硬化症 ，帕金森病，亨廷顿舞蹈病，唐氏综合征，柯萨科夫病和其他神经退行性疾病。

    Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists
    37.
    发明授权
    Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
    三取代和四取代的胍和它们作为兴奋性氨基酸拮抗剂的用途

    公开(公告)号：US5336689A

    公开(公告)日：1994-08-09

    申请号：US105458

    申请日：1993-08-11

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

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

    IPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18 ,  C07C279/00 ,  A61K31/13 ,  A61K31/135 ,  C07C311/02

    CPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18

    摘要： Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

    摘要翻译： 表现出对苯环利定（PCP）受体的高结合亲和力，更优选对大脑σ受体的低亲和力的三取代和四取代胍基。 这些胍衍生物通过作为NMDA受体 - 离子通道复合物的离子通道的阻断剂，作为NMDA受体的谷氨酸诱导反应的非竞争性抑制剂。 因此，这些化合物发挥神经保护活性，并且可用于治疗缺氧，低血糖，脑或脊髓缺血以及脑或脊髓创伤中的神经元损失，以及用于治疗癫痫，阿尔茨海默病，肌萎缩性侧索硬化症 ，帕金森病，亨廷顿舞蹈病，唐氏综合征，柯萨科夫病和其他神经退行性疾病。

    Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists
    39.
    发明授权
    Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
    三取代和四取代的胍和它们作为兴奋性氨基酸拮抗剂的用途

    公开(公告)号：US5262568A

    公开(公告)日：1993-11-16

    申请号：US663134

    申请日：1991-03-04

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

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

    IPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18 ,  C07C279/00 ,  A61K31/13 ,  A61K31/135 ,  C07D311/02

    CPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18

    摘要： Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

    摘要翻译： 表现出对苯环利定（PCP）受体的高结合亲和力，更优选对大脑σ受体的低亲和力的三取代和四取代胍基。 这些胍衍生物通过作为NMDA受体 - 离子通道复合物的离子通道的阻断剂，作为NMDA受体的谷氨酸诱导反应的非竞争性抑制剂。 因此，这些化合物发挥神经保护活性，并且可用于治疗缺氧，低血糖，脑或脊髓缺血以及脑或脊髓创伤中的神经元损失，以及用于治疗癫痫，阿尔茨海默病，肌萎缩性侧索硬化症 ，帕金森病，亨廷顿舞蹈病，唐氏综合征，柯萨科夫病和其他神经退行性疾病。

    N,N'-disubstituted guanidines and their use as excitatory amino acid antagonists
    40.
    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：US5093525A

    公开(公告)日：1992-03-03

    申请号：US487033

    申请日：1990-03-02

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

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

    IPC分类号： A61K31/155 ,  A61K31/00 ,  A61P25/00 ,  C07C279/00 ,  C07C279/18

    CPC分类号： C07C279/18

    摘要： Disubstituted guanidines, e.g., bis-1,3-(o-isopropylphenyl)guanidine, bis-1,3-(m-isopropylphenyl)guanidine, bis-1,3-(1-naphthyl)guanidine, bis-1,3-(m-methoxyphenyl)guanidine, N-(1-naphthyl)-N'-(o-iodophenyl)-guanidine, N-(1-naphthyl)-N'-(m-ethylphenyl)guanidine, and N-(1-napthyl)-N'-(o-isoproylphenyl) guanidine, exhibit a high binding affinity to phencyclidine (PCP) receptors. These N,N'-disubstituted guanidine derivatives act as non-competitive inhibitors of 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, hypoglycemia, brain or spinal chord ischemia, brain or spinal cord trauma, as well as being useful for the treatmnet of epilepsy, Alzheimer's disease, Amyotrophic Laterla Scherosis, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

    摘要翻译： 二取代的胍，例如双-1,3-（邻异丙基苯基）胍，双-1,3-（间 - 异丙基苯基）胍，双-1,3-（1-萘基）胍，双-1,3- （间 - 甲苯基）胍，N-（1-萘基）-N' - （邻碘苯基） - 胍，N-（1-萘基）-N' - （间乙基苯基）胍和N- 萘基）-N' - （邻 - 异丙酰苯基）胍显示出对苯环利定（PCP）受体的高结合亲和力。 这些N，N'-二取代的胍衍生物通过NMDA受体 - 离子通道复合物的离子通道作为阻断剂，作为通过NMDA受体产生的谷氨酸诱导的应答的非竞争性抑制剂。 因此，这些化合物发挥神经保护作用，可用于治疗缺氧，低血糖，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Laterla Scherosis，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。