embedded image;The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed. ;This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II 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 such compounds as probes for the localization of GABAA receptors in tissue sections."/> Heteroaryl substituted fused bicyclic heteroaryl compounds as GABAA receptor ligands
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Heteroaryl substituted fused bicyclic heteroaryl compounds as GABAA receptor ligands

机译:杂芳基取代的稠合双环杂芳基化合物作为GABAA受体配体

摘要

This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: embedded image;The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed. ;This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II 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 such compounds as probes for the localization of GABAA receptors in tissue sections.
机译:本发明涉及杂芳基取代的稠合双环杂芳基化合物,例如杂芳基取代的咪唑并吡啶,咪唑并吡嗪,咪唑并吡啶并咪唑并嘧啶和咪唑并噻唑,它们可以用式I或式II描述: <图像alt =“嵌入式图像” file =“ US20060014746A1-20060119-C00001.GIF” he =“ 60.11mm” imgContent =“ chem” imgFormat =“ GIF” wi =“ 65.28mm” /> 本发明特别涉及这样的化合物,其与GABA A 受体的苯并二氮杂位点具有高选择性和高亲和力。本发明还涉及包含这样的化合物的药物组合物,并且涉及这样的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和式II化合物的方法。本发明还涉及式I或式II的苯并咪唑,吡啶并咪唑和相关的双环杂芳基化合物与一种或多种其他CNS试剂的组合用于增强其他CNS试剂的作用的用途。另外,本发明涉及这类化合物作为探针在组织切片中定位GABA A 受体的用途。

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