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1. 发明授权

US06420365B1 Imidazopyridines and related derivatives as selective modulators of bradykinin B2 receptors 失效
标题翻译：咪唑并吡啶类和相关衍生物作为缓激肽B2受体的选择性调节剂
公开(公告)号：US06420365B1
公开(公告)日：2002-07-16
申请号：US09765159
申请日：2001-01-17
申请人： John M. Peterson , Alan Hutchison , Kenneth Shaw , Kevin Hodgetts , George D. Maynard , Richard Lew
发明人： John M. Peterson , Alan Hutchison , Kenneth Shaw , Kevin Hodgetts , George D. Maynard , Richard Lew
IPC分类号： A61K31435
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein A, B, C, D, Y, R1, R3, R4, R5, and R6 are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒性盐，其中A，B，C，D，Y，R 1，R 3，R 4，R 5和R 6是本文定义的变量，该化合物是缓激肽B2受体的调节剂。这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛，经皮腔内冠状动脉血管成形术，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症，青光眼，疼痛，哮喘和鼻炎的再狭窄，以及增加血脑屏障或血脑屏障的渗透性，肿瘤屏障。

2. 发明授权

US06358949B1 Aryl and hetroaryl fused aminoalkyl-imidazole derivatives: selective modulators of bradykinin B2 receptors 失效
标题翻译：芳基和杂芳基稠合氨基烷基 - 咪唑衍生物：缓激肽B2受体的选择性调节剂
公开(公告)号：US06358949B1
公开(公告)日：2002-03-19
申请号：US09540580
申请日：2000-03-31
申请人： Robert W. DeSimone , Alan Hutchison , Kenneth Shaw , George D. Maynard , John M. Peterson , Richard Lew , Harry L. Brielmann
发明人： Robert W. DeSimone , Alan Hutchison , Kenneth Shaw , George D. Maynard , John M. Peterson , Richard Lew , Harry L. Brielmann
IPC分类号： A61K315377
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: A, B, C and D are N or CH; X is a bond or (un)substituted CH2; R1 is lower alkenyl or (un)substituted lower alkyl; R3 is lower alkyl; and R2, R4, R5, and R6 are variables defined herein; which compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatroy disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility or glaucoma, or for the increase of permeability of blood-brain barrier, pain, asthma, and rhinitis.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中：A，B，C和D是N或CH; X是一个或（un）取代的CH 2; R 1是低级烯基或（取代）低级烷基; R3是低级烷基; 和R2，R4，R5和R6是本文定义的变量;这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛，经皮腔内冠状动脉成形术后再狭窄，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症或青光眼，或增加血脑屏障通透性，疼痛，哮喘和鼻炎。

3. 发明授权

US06509366B2 Substituted imidazoles as selective modulators of Bradykinin B2 receptors 失效
标题翻译：取代的咪唑作为缓激肽B2受体的选择性调节剂
公开(公告)号：US06509366B2
公开(公告)日：2003-01-21
申请号：US09764805
申请日：2001-01-17
申请人： Stanislaw Rachwal , Alan Hutchison , Kenneth Shaw , George D. Maynard , Xiao-shu He , Robert DeSimone , Kevin Hodgetts
发明人： Stanislaw Rachwal , Alan Hutchison , Kenneth Shaw , George D. Maynard , Xiao-shu He , Robert DeSimone , Kevin Hodgetts
IPC分类号： A61K314174
CPC分类号： C07D233/64 , C07D233/68 , C07D401/06
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein Y, R1, R2, R3, R4, R5, R6, R7 R7′ are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are therefore useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis, and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中Y，R 1，R 2，R 3，R 4，R 5，R 6，R 7 R 7'是本文定义的变量，该化合物是缓激肽B2受体的调节剂。因此，这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛经皮腔内冠状动脉血管成形术，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症，青光眼，疼痛，哮喘和鼻炎的再狭窄，以及增加血脑屏障或血液 - 脑肿瘤屏障。

4. 发明授权

US06916819B2 Benzimidazole and pyridylimidazole derivatives 失效
标题翻译：苯并咪唑和吡啶基咪唑衍生物
公开(公告)号：US06916819B2
公开(公告)日：2005-07-12
申请号：US10038069
申请日：2001-12-21
申请人： Guiying Li , John M. Peterson , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , Vinod Singh , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu
发明人： Guiying Li , John M. Peterson , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , Vinod Singh , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/435 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D233/20 , C07D233/54 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10 , C07D491/113 , C07D403/12
CPC分类号： C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I 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. Novel processes for preparing compounds of Formula I are disclosed.This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl 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 such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译：本发明涉及苯并咪唑，吡啶基咪唑和相关双环杂芳基化合物，所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A的苯并二氮杂部位的化合物， / SUB>受体。本发明还涉及包含这些化合物的药物组合物以及这些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。本发明还涉及式I的苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。此外，本发明涉及使用这些化合物作为组织切片中GABA A A受体定位的探针。

5. 发明授权

US06894044B2 2-aminoquinolinecarboxamides: neurokinin receptor ligands 失效
标题翻译： 2-氨基喹啉甲酰胺：神经激肽受体配体
公开(公告)号：US06894044B2
公开(公告)日：2005-05-17
申请号：US10115409
申请日：2002-04-03
申请人： Jun Yuan , George D. Maynard , Alan Hutchison
发明人： Jun Yuan , George D. Maynard , Alan Hutchison
IPC分类号： A61K31/47 , A61P25/00 , A61P25/28 , C07D215/50 , C07D401/04 , C07D453/06 , C07D491/10 , A61K31/4709
CPC分类号： A61K31/47 , C07D215/50 , C07D401/04 , C07D453/06 , C07D491/10 , Y10S206/828
摘要： Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或药学上可接受的溶剂化物，其中R 1，R 2，R 3，X，本文定义Q 1和Q 2 2，这些化合物是神经激肽受体特别是NK-3受体的配体，并且可用于治疗广泛范围的疾病或病症，包括但不限于抑郁症，焦虑症，精神病，肥胖症，疼痛，帕金森病，阿尔茨海默病，神经变性疾病，运动障碍，呼吸系统疾病，炎性疾病，神经病，免疫疾病，偏头痛，胆汁功能异常和皮炎。

6. 发明授权

US07915288B2 1-aryl-4-substituted isoquinolines 失效
标题翻译： 1-芳基-4-取代的异喹啉
公开(公告)号：US07915288B2
公开(公告)日：2011-03-29
申请号：US11587906
申请日：2005-05-06
申请人： Kyungae Lee , Jun Yuan , George D. Maynard , Alan Hutchison , Scott Mitchell
发明人： Kyungae Lee , Jun Yuan , George D. Maynard , Alan Hutchison , Scott Mitchell
IPC分类号： C07D217/02 , A61K31/47
CPC分类号： C07D405/12 , A61K31/47 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/14 , C07D413/14
摘要： 1-aryl-4-substituted isoquinoline or 1-aryl-3,4-disubstituted isoquinoline analogues of Formula I and Formula II, as follows: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 1-aryl-4-substituted isoquinolines or 1-aryl-3,4-disubstituted isoquinolines, which are useful as probes for the localization of C5a receptors.
摘要翻译：式I和式II的1-芳基-4-取代的异喹啉或1-芳基-3,4-二取代的异喹啉类似物如下：其中R1，R2，R3，R8，R9，A和Ar如本文所定义。这些化合物是C5a受体的配体。优选的式I和II化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供标记的1-芳基-4-取代的异喹啉或1-芳基-3,4-二取代的异喹啉，其可用作C5a受体定位的探针。

7. 发明授权

US07642267B2 Benzimidazole and pyridylimidazole derivatives 失效
标题翻译：苯并咪唑和吡啶基咪唑衍生物
公开(公告)号：US07642267B2
公开(公告)日：2010-01-05
申请号：US11942480
申请日：2007-11-19
申请人： Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
发明人： Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I. 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. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl 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 such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译：本发明涉及苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物，所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A受体的苯并二氮杂位点的化合物。本发明还涉及包含这些化合物的药物组合物以及这些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。本发明还涉及式I的苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。此外，本发明涉及使用这些化合物作为组织切片中GABA A受体定位的探针。

8. 发明授权

US07300945B2 Benzimidazole and pyridylimidazole derivatives 失效
标题翻译：苯并咪唑和吡啶基咪唑衍生物
公开(公告)号：US07300945B2
公开(公告)日：2007-11-27
申请号：US11179458
申请日：2005-07-12
申请人： Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
发明人： Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I 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. Novel processes for preparing compounds of Formula I are disclosed.This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl 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 such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译：本发明涉及苯并咪唑，吡啶基咪唑和相关双环杂芳基化合物，所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A的苯并二氮杂部位的化合物， / SUB>受体。本发明还涉及包含这些化合物的药物组合物以及这些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。本发明还涉及式I的苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。此外，本发明涉及使用这些化合物作为组织切片中GABA A A受体定位的探针。

9. 发明授权

US06413982B1 4-substituted quinoline derivatives 失效
标题翻译： 4-取代喹啉衍生物
公开(公告)号：US06413982B1
公开(公告)日：2002-07-02
申请号：US09536922
申请日：2000-03-28
申请人： Jun Yuan , George D. Maynard , Alan Hutchison , Stanislaw Rachwal
发明人： Jun Yuan , George D. Maynard , Alan Hutchison , Stanislaw Rachwal
IPC分类号： A61L3147
CPC分类号： C07D401/04 , C07D401/14 , C07D413/04 , C07D487/04 , G01N33/9426 , G01N2333/70571
摘要： Disclosed are compounds of the Formula where R1, R2, R3, R4, X, Y1, and Y2 are defined herein. These compounds bind with high affinity to NK-3 receptors and/or GABAA receptors. Also provided are pharmaceutical compositions comprising these compounds, and methods of treating patients suffering from various central nervous system and peripheral diseases or disorders with these pharmaceutical compositions. This invention also relates to the use of such compounds in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. The compounds of this invention are also useful as probes for the localization of NK-3 receptors and GABAA receptors.
摘要翻译：公开了本文定义的化学式R 1，R 2，R 3，R 4，X，Y 1和Y 2的化合物。这些化合物以高亲和力结合NK-3受体和/或GABA A受体。还提供了包含这些化合物的药物组合物，以及用这些药物组合物治疗患有各种中枢神经系统和外周疾病或病症的患者的方法。本发明还涉及这样的化合物与一种或多种其它CNS剂组合用于增强其它CNS剂的作用的用途。本发明的化合物也可用作NK-3受体和GABA A受体定位的探针。

10. 发明申请

US20100267698A1 Benzimidazole and Pyridylimidazole Derivatives 审中-公开
标题翻译：苯并咪唑和吡啶基咪唑衍生物
公开(公告)号：US20100267698A1
公开(公告)日：2010-10-21
申请号：US12652435
申请日：2010-01-05
申请人： Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
发明人： Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
IPC分类号： A61K31/55 , C07D401/14 , A61K31/4439 , C07D403/06 , A61K31/4184 , A61K31/4196 , A61K31/41 , C07D413/14 , A61K31/4245 , C07D471/04 , A61K31/437 , C07D417/14 , A61K31/427 , C07D473/00 , A61K31/52 , C07D403/14 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P25/22 , A61P25/24 , A61P25/18 , A61P25/00 , C12N5/079 , C12Q1/02
CPC分类号： C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I 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. Novel processes for preparing compounds of Formula I are disclosed.This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl 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 such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译：本发明涉及苯并咪唑，吡啶基咪唑和相关双环杂芳基化合物，所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A受体的苯并二氮杂位点的化合物。本发明还涉及包含这些化合物的药物组合物以及这些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。本发明还涉及式I的苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。此外，本发明涉及使用这些化合物作为组织切片中GABA A受体定位的探针。

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