首页> 外国专利> Compound, use of a compound, pharmaceutical composition, and methods for treating a disease or disorder associated with pathogenic agonism, inverted agonism or gabaa receptor antagonism, to localize gabaa receptors, to inhibit binding of a benzodiazepine to a gabaa receptor, and to alter the signal transduction activity of gabaa receptors

Compound, use of a compound, pharmaceutical composition, and methods for treating a disease or disorder associated with pathogenic agonism, inverted agonism or gabaa receptor antagonism, to localize gabaa receptors, to inhibit binding of a benzodiazepine to a gabaa receptor, and to alter the signal transduction activity of gabaa receptors

机译：化合物，化合物的用途，药物组合物和用于治疗与病原性激动，反向激动或gabaa受体拮抗作用有关的疾病或病症的方法，以定位gabaa受体，抑制苯二氮卓与gabaa受体的结合，并改变受体的信号转导活性

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摘要

"COMPOUND, USE OF A COMPOUND, PHARMACEUTICAL COMPOSITION, AND METHODS FOR TREATMENT OF A DISEASE OR DISORDER ASSOCIATED WITH PATHOGENIC AGONISM, INVERTED AGONISM OR ANTAGONISM OF THE GABA ~ A ~ RECEPTOR TO RECEIVER INHIBIT THE CONNECTION OF A BENZODIAZEPIN COMPOUND TO A GABA ~ A ~ RECEIVER, AND TO ALTER THE GABA ~ A ~ RECEIVER SIGNAL TRANSDUCTION ACTIVITY ". Substituted pyrrolcarboxamide compounds are shown. These compounds are highly selective GABA-A ~ brain receptor agonists, antagonists or inverted agonists or prodrugs of GABA-A ~ brain receptor agonists, antagonists or inverted agonists and are therefore useful in the diagnosis and treatment. anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and memory enhancement. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. The compounds of the invention are also useful as probes for localization of GABA-Aβ receptors in tissue samples.

机译：“化合物，化合物的使用，药物组合物，以及与致病性肌无力症，转化性肌无力症或拮抗症相关的疾病或疾病的治疗方法，GABA〜受体能够阻止苯并二氮杂PIN与化合物的连接〜接收器，并更改GABA〜〜〜接收器信号转换活动”。显示了取代的吡咯甲酰胺化合物。这些化合物是高选择性的GABA-A〜脑受体激动剂，拮抗剂或反向激动剂或GABA-A〜脑受体激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗。焦虑，抑郁，阿尔茨海默氏症，睡眠和癫痫发作，苯二氮卓类药物过量和记忆力增强。还提供了药物组合物，包括包装的药物组合物。本发明的化合物还可用作在组织样品中定位GABA-Aβ受体的探针。

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公开/公告号BR0013664A

专利类型
公开/公告日2002-05-14

原文格式PDF
申请/专利权人 NEUROGEN CORPORATION;
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申请/专利号BR20000013664
发明设计人 PAMELA ALBAUGH;KENNETH SHAW;ALAN HUTCHISON;
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申请日2000-08-30
分类号C07D209/42;C07D209/52;C07D405/12;C07D401/12;C07D403/12;C07D401/14;C07D471/04;C07D417/14;A61K31/40;
国家 BR
入库时间 2022-08-22 00:46:10

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