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

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

机译:化合物,药物组合物,化合物的用途以及用于治疗与gabaa受体的致病性激动,反向激动或拮抗有关的疾病或病症的方法,以在组织样品中定位gabaa受体,以抑制苯二氮卓类化合物与gabaa受体和改变gabaa受体的信号转导活性的方法,以及包装好的药物组合物

摘要

"COMPOUND, PHARMACEUTICAL COMPOSITION, USE OF A COMPOUND, AND, METHODS FOR THE TREATMENT OF A DISEASE OR DISORDER ASSOCIATED WITH PATHOGENIC AGONISM, REVERSE AGONISM OR ANTAGONISM OF THE GABA ~ ~ ~ RECOMMENDER, TO LOCATE A RECOVERY OF GABA ~ ~ ~ IN A RECOVERY LOCATION. TISSUE SAMPLE, TO INHIBIT THE CONNECTION OF A BENZODIAZEPINE COMPOUND TO A GABA ~ A ~ RECEIVER AND TO CHANGE THE SIGNAL TRANSDUCTION ACTIVITY OF GABA ~ A ~, AND, PACKED PHARMACEUTICAL COMPOSITION ". The compounds of formula (I) or their pharmaceutically acceptable salts are disclosed where R ~ 1 ~, R ~ 2 ~ and W are defined herein. These compounds are highly selective agonists, antagonists or inverse antagonists for brain GABAa receptors or prominences of agonists, antagonists or inverse agonists for brain GABAa receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down, sleep and seizure disorders, overdose with benzodiazepine medications and memory enhancement. Pharmaceutical compositions that include packaged pharmaceutical compositions are also provided. The compounds of the invention are also useful as probes for locating GABA-A ~ receptors in tissue samples.
机译:“化合物,药物成分,化合物的使用以及与GABA的致病性机能障碍,逆向机能障碍或拮抗症有关的疾病或病症的治疗方法〜〜〜推荐人,以找到GABA的回收方法〜〜〜在A中恢复的位置。组织样本,以防止将苯二氮杂INE化合物与GABA〜A〜接收物连接,并改变GABA〜A〜以及包装好的药物成分的信号传递活性。公开了式(I)的化合物或其药学上可接受的盐,其中在本文中定义了R 1〜,R 2〜和W。这些化合物是脑GABAa受体的高度选择性激动剂,拮抗剂或反向拮抗剂,或者是脑GABAa受体的激动剂,拮抗剂或反向激动剂的突出物,因此可用于诊断和治疗焦虑症,抑郁症,唐突,睡眠和癫痫发作,用药过量与苯二氮卓类药物并增强记忆力。还提供了包括包装的药物组合物的药物组合物。本发明的化合物也可用作在组织样品中定位GABA-Aβ受体的探针。

著录项

  • 公开/公告号BR0010308A

    专利类型

  • 公开/公告日2002-01-08

    原文格式PDF

  • 申请/专利权人 NEUROGEN CORPORATION;

    申请/专利号BR20000010308

  • 申请日2000-05-05

  • 分类号C07D215/56;C07D405/12;C07D409/12;C07D401/12;C07D413/12;C07D413/04;C07D487/04;A61K31/47;

  • 国家 BR

  • 入库时间 2022-08-22 00:46:14

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