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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。
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公开(公告)号：US07521464B2
公开(公告)日：2009-04-21
申请号：US11772702
申请日：2007-07-02
IPC分类号： A61K31/41 , C07D231/02
CPC分类号： C07D401/06 , C07D231/40 , C07D401/12 , C07D403/06 , C07D405/04 , C07D409/04 , C07D409/12 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The invention provides compounds of Formula I: wherein R1, R2, R3, R4, R6, R7, R8 and A are as defined. Compounds of formula I have activity inhibiting production of Aβ-peptide. The invention also provides pharmaceutical compositions and methods for treating diseases, for example Alzheimer's disease, in mammals comprising compounds of Formula I.
摘要翻译： 本发明提供式I化合物：其中R 1，R 2，R 3，R 4，R 6，R 7，R 8和A如上所定义。 式I化合物具有抑制Abeta肽生产的活性。 本发明还提供用于在包含式I化合物的哺乳动物中治疗疾病例如阿尔茨海默氏病的药物组合物和方法。
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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。
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公开(公告)号：US20060025425A1
公开(公告)日：2006-02-02
申请号：US11179458
申请日：2005-07-12
申请人： Guiying Li , Pamela Albaugh , Kevin Currie , Guolin Cai , Linda Gustavson , Kyungae Lee , Alan Hutchison , George Maynard , Jun Yuan , Ling Xie , Manuka Ghosh , Nian Liu , George Luke , Scott Mitchell , Martin Allen , Spiros Liras
发明人： Guiying Li , Pamela Albaugh , Kevin Currie , Guolin Cai , Linda Gustavson , Kyungae Lee , Alan Hutchison , George Maynard , Jun Yuan , Ling Xie , Manuka Ghosh , Nian Liu , George Luke , Scott Mitchell , Martin Allen , Spiros Liras
IPC分类号： A61K31/506 , A61K31/4745 , A61K31/427 , A61K31/4184 , C07D471/02 , C07D403/02 , C07D417/02 , C07D413/02
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。
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公开(公告)号：US20050182079A1
公开(公告)日：2005-08-18
申请号：US11062133
申请日：2005-02-18
申请人： Martin Allen , Thomas Chappie , John Humphrey , Spiros Liras
发明人： Martin Allen , Thomas Chappie , John Humphrey , Spiros Liras
IPC分类号： C07D401/04 , C07D491/04 , A61K31/517 , C07D43/02
CPC分类号： C07D401/04 , C07D491/04
摘要： The invention pertains to substituted quinazoline and isoquinoline compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE-10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.
摘要翻译： 本发明涉及用作有效磷酸二酯酶（PDE）抑制剂的取代喹唑啉和异喹啉化合物。 特别地，本发明涉及作为PDE-10的选择性抑制剂的所述化合物。 本发明还涉及制备所述化合物的中间体; 包含所述化合物的药物组合物; 以及所述化合物在治疗某些中枢神经系统（CNS）或其它疾病的方法中的用途。
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