首页> 外国专利> Compound, pharmaceutical composition, packaging, methods for altering the signal transducing activity of a gaba receptor, to treat anxiety, depression, a sleep disorder, schizophrenia, attention deficit hyperactivity disorder or memory, to demonstrate the presence of a gabaa receptor on a cell or tissue sample and on a tissue section using a compound, and process for preparing a compound

Compound, pharmaceutical composition, packaging, methods for altering the signal transducing activity of a gaba receptor, to treat anxiety, depression, a sleep disorder, schizophrenia, attention deficit hyperactivity disorder or memory, to demonstrate the presence of a gabaa receptor on a cell or tissue sample and on a tissue section using a compound, and process for preparing a compound

机译:化合物,药物组合物,包装,用于改变gaba受体的信号转导活性,治疗焦虑症,抑郁症,睡眠障碍,精神分裂症,注意力不足过动症或记忆力的方法,以证明gabaa受体存在于细胞或组织样品和使用化合物的组织切片上的制备方法

摘要

"COMPOUND, PHARMACEUTICAL COMPOSITION, PACKAGING, METHODS TO CHANGE SIGNAL TRANSDUCTIVE ACTIVITY OF A GABA ~ A ~ RECEIVER, TO TREAT ANXIETY, DEPRESSION, SLEEP DISTURBY, DISTURAL DIFFERENCE HYDROPHYRIUM OR DIFFERENCE DIFFERENCE TO DEMONSTRATE THE PRESENCE OF A GABA ~ RECEIVER ON A CELL OR TISSUE SAMPLE AND ON A TISSUE SECTION, USE OF A COMPOUND, AND PROCESS TO PREPARE A COMPOUND. " This invention relates to benzimidazoles, pyridimidazoles and related heteroaryl bicyclic compounds, all of which may be described by Formula (I). The invention is particularly related to such compounds which bind with high selectivity and high affinity to the benzodiazepine site of GABA-Aβ receptors. This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of certain central nervous system (CNS) diseases. New processes for preparing the compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related heteroaryl bicyclic compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally, this invention relates to the use of such compounds as probes for locating GABA-Aβ receptors in tissue sections.
机译:“化合物,药物成分,包装,改变GABA〜A〜受体信号传递活性,治疗焦虑症,抑郁症,睡眠性Disturby,干扰性水文细菌或差异性差异的方法,以证明差异组织样品和组织部分上,化合物的使用,以及制备化合物的方法“本发明涉及苯并咪唑,吡啶并咪唑和相关的杂芳基双环化合物,所有这些都可以用式(I)描述。本发明特别涉及以高选择性和高亲和力结合于GABA-Aβ受体的苯并二氮杂位的化合物。本发明还涉及包含此类化合物的药物组合物,以及此类化​​合物在治疗某些中枢神经系统(CNS)疾病中的用途。公开了制备式I化合物的新方法。本发明还涉及苯并咪唑,吡啶并咪唑和相关的式I的杂芳基双环化合物与一种或多种其他CNS试剂的组合用于增强另一种CNS试剂的作用的用途。另外,本发明涉及这类化合物作为在组织切片中定位GABA-Aβ受体的探针的用途。

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