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31. 发明授权

US5514680A Glycine receptor antagonists and the use thereof 失效
标题翻译：甘氨酸受体拮抗剂及其用途
公开(公告)号：US5514680A
公开(公告)日：1996-05-07
申请号：US148259
申请日：1993-11-05
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。

32. 发明授权

US5767162A Tri-and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
标题翻译：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。

33. 发明授权

US5622965A 4-hydroxy-3-nitro-1,2-dihydroquinolin-2-ones and the use thereof as excitatory amino acid and glycine receptor antagonists 失效
标题翻译： 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。

34. 发明授权

US5604228A Substituted guanidines having high binding to the sigma receptor and the use thereof 失效
标题翻译：与σ受体结合度高的取代胍类及其用途
公开(公告)号：US5604228A
公开(公告)日：1997-02-18
申请号：US226770
申请日：1994-04-12
申请人： John F. W. Keana , Eckard Weber
发明人： John F. W. Keana , Eckard Weber
IPC分类号： A61K31/155 , C07B59/00 , C07C279/04 , C07C279/16 , C07C279/18 , C07C331/12 , C07D233/50 , C07D311/14 , C07D311/18 , A61K31/495 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/505
CPC分类号： A61K31/155 , C07B59/001 , C07C279/04 , C07C279/16 , C07C279/18 , C07C331/12 , C07D233/50 , C07D311/14 , C07D311/18 , C07C2101/14 , C07C2102/08 , C07C2102/28 , C07C2103/64 , C07C2103/74
摘要： N,N-disubstituted-guanidines, e.g., of the formula ##STR1## wherein R and R' are substituted or unsubstituted hydrocarbon groups. Methods are provided for the treatment of psychosis and hypertension by administering an effective amount of an N,N'-disubstituted guanidine which, preferably, has a high affinity for the sigma receptor.
摘要翻译： N，N-二取代 - 胍，例如下式其中R和R'是取代或未取代的烃基。提供了通过施用有效量的N，N'-二取代的胍治疗精神病和高血压的方法，其优选地具有对σ受体的高亲和力。

35. 发明授权

US5475007A 1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes and the use thereof 失效
标题翻译： 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。

36. 发明授权

US5559154A Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
标题翻译：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。

37. 发明授权

US5478863A Substituted guanidines having high binding to the sigma receptor and the use thereof 失效
标题翻译：与σ受体结合度高的取代胍类及其用途
公开(公告)号：US5478863A
公开(公告)日：1995-12-26
申请号：US21247
申请日：1993-02-23
申请人： John F. W. Keana , Eckard Weber
发明人： John F. W. Keana , Eckard Weber
IPC分类号： A61K31/155 , C07B59/00 , C07C279/04 , C07C279/16 , C07C279/18 , C07C331/12 , C07D233/50 , C07D311/14 , C07D311/18
CPC分类号： C07C331/12 , A61K31/155 , C07B59/001 , C07C279/04 , C07C279/16 , C07C279/18 , C07D233/50 , C07D311/14 , C07D311/18 , C07C2101/14 , C07C2102/08 , C07C2102/28 , C07C2103/64 , C07C2103/74
摘要： N,N-disubstituted-guanidines, e.g., of the formula ##STR1## wherein R and R' are substituted or unsubstituted hydrocarbon groups. Methods are provided for the treatment of psychosis and hypertension by administering an effective amount of an N,N'-disubstituted guanidine which, preferably, has a high affinity for the sigma receptor.
摘要翻译： N，N-二取代 - 胍，例如下式其中R和R'是取代或未取代的烃基。提供了通过施用有效量的N，N'-二取代的胍治疗精神病和高血压的方法，其优选地具有对σ受体的高亲和力。

38. 发明授权

US5336689A Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
标题翻译：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。

39. 发明授权

US5308869A Substituted amidines having high binding to the sigma receptor and the use thereof 失效
标题翻译：具有与σ受体结合高的取代脒基及其用途
公开(公告)号：US5308869A
公开(公告)日：1994-05-03
申请号：US860571
申请日：1992-03-30
申请人： John F. W. Keana , Eckard Weber
发明人： John F. W. Keana , Eckard Weber
IPC分类号： A61K51/04 , C07C257/14 , C07C257/16 , C07C257/18 , A01N37/52
CPC分类号： C07C257/14 , A61K51/0406 , A61K2121/00 , C07B2200/05 , C07C2101/14 , C07C2102/42 , C07C2103/74
摘要： N,N'-disubstituted-amidines, e.g., of the formula ##STR1## wherein R, R' and R" are substituted or unsubstituted hydrocarbon and/or heterocyclic groups.Methods are provided for the treatment or prophylaxis of anxiety in an animal, for treating psychosis, and for treating hypertension by administering an effective amount of an N,N'-disubstituted amidine which, preferably, has a high affinity for the sigma receptor.
摘要翻译： N，N'-二取代的脒，例如下式：其中R，R'和R“是取代或未取代的烃和/或杂环基团。提供了用于治疗或预防动物焦虑症，用于治疗精神病和通过施用有效量的N，N'-二取代的脒来治疗高血压的方法，其优选地具有对σ受体的高亲和力。

40. 发明授权

US5262568A Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
标题翻译：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。

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