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11. 发明申请

US20060217384A1 Bicyclic and tricyclic heteroaromatic compounds 失效
标题翻译：双环和三环杂芳族化合物
公开(公告)号：US20060217384A1
公开(公告)日：2006-09-28
申请号：US11442812
申请日：2006-05-30
申请人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
发明人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
IPC分类号： C07D487/04 , A61K31/503 , A61K31/4745
CPC分类号： C07D217/26 , C07D237/30 , C07D471/04 , C07D487/04 , C07D519/00 , G01N2333/70571
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。这些化合物以高选择性和/或高亲和力结合GABA A A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和用作GABA < 组织样品中的受体。还公开了可用于制备这些化合物的中间体。

12. 发明授权

US07053093B2 Bicyclic and tricyclic hetroaromatic compounds 失效
标题翻译：双环和三环杂芳族化合物
公开(公告)号：US07053093B2
公开(公告)日：2006-05-30
申请号：US10352519
申请日：2003-01-28
申请人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
发明人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
IPC分类号： C07D471/04 , A61K31/437 , A61K25/24 , A61P25/22
CPC分类号： C07D217/26 , C07D237/30 , C07D471/04 , C07D487/04 , C07D519/00 , G01N2333/70571
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。这些化合物以高选择性和/或高亲和力结合GABA A A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和用作GABA < 组织样品中的受体。还公开了可用于制备这些化合物的中间体。

13. 发明申请

US20060025425A1 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：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。

14. 发明申请

US20060014746A1 Heteroaryl substituted fused bicyclic heteroaryl compounds as GABAA receptor ligands 审中-公开
标题翻译：杂芳基取代的稠合双环杂芳基化合物作为GABA A受体配体
公开(公告)号：US20060014746A1
公开(公告)日：2006-01-19
申请号：US11214345
申请日：2005-08-29
申请人： Alan Hutchison , George Maynard , Pamela Albaugh , Linghong Xie , Jun Yuan , Scott Mitchell , Vinod Singh , Manuka Ghosh , Guiying Li , Nian Liu
发明人： Alan Hutchison , George Maynard , Pamela Albaugh , Linghong Xie , Jun Yuan , Scott Mitchell , Vinod Singh , Manuka Ghosh , Guiying Li , Nian Liu
IPC分类号： C07D487/04 , C07D471/02 , A61K31/519 , A61K31/503 , A61K31/4745
CPC分类号： C07D487/04 , C07D471/04 , C07D513/04
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: 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.
摘要翻译：本发明涉及可以由式I或式II描述的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，咪唑并嘧啶和咪唑并噻唑。本发明特别涉及以高选择性结合的这些化合物并且对GABA A A受体的苯并二氮杂位点具有高亲和力。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，吡啶基咪唑和相关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。

15. 发明授权

US06515133B1 Pharmaceutical compositions containing certain diarylimidazole derivatives 失效
标题翻译：含有某些二芳基咪唑衍生物的药物组合物
公开(公告)号：US06515133B1
公开(公告)日：2003-02-04
申请号：US09523328
申请日：2000-03-10
申请人： Andrew Thurkauf , Jun Yuan , Alan Hutchison , Charles A. Blum , Richard L. Elliott , Marlys Hammond
发明人： Andrew Thurkauf , Jun Yuan , Alan Hutchison , Charles A. Blum , Richard L. Elliott , Marlys Hammond
IPC分类号： C07D40104
CPC分类号： C07D233/64 , C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D417/04
摘要： Certain diaryl imidazoles act as partial agonists or antagonists for NPY receptors, in particular NPY 5 receptors. They are of use, for example in treating loss of appetite. Such compounds bear aryl groups in the 2 position. Many of the compounds are novel.
摘要翻译：某些二芳基咪唑作为NPY受体特别是NPY 5受体的部分激动剂或拮抗剂。它们是有用的，例如用于治疗食欲不振。这种化合物在2位上带有芳基。许多化合物是新颖的。

16. 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。

17. 发明授权

US6156751A Certain tricyclic substituted diazabicyclo (3.2.1) octane derivatives 失效
标题翻译：某些三环取代的二氮杂双环（3.2.1）辛烷衍生物
公开(公告)号：US6156751A
公开(公告)日：2000-12-05
申请号：US393789
申请日：1999-09-10
申请人： Alan Hutchison , Jun Yuan , Raymond F. Horvath
发明人： Alan Hutchison , Jun Yuan , Raymond F. Horvath
IPC分类号： C07D487/08 , A61K31/495 , C07D247/00
CPC分类号： C07D487/08
摘要： This invention encompasses compounds of the formula: ##STR1## where either R.sub.1 or R.sub.2 represents ##STR2## and the other represents hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; andX is oxygen, methylene, or NH;Y is represents various inorganic and organic substituents;Z is hydrogen, amino or NHR.sub.6 where R.sub.6 is lowere alkyl having 1-6 carbon atoms;T is hydrogen, halogen, hydroxy, or lower alkoxy having 1-6 carbon atoms; andA is methylene, carbonyl or CHOH.These compounds are selective partial agonists or antagonists at brain monoamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neurolepticagents. These compounds show unexpectedly atypical antipsychotic profiles (clozapine-like) in the animal models described in this patent.
摘要翻译：本发明包括下式的化合物：其中R 1或R 2表示，另一个表示氢或具有1-6个碳原子的直链或支链低级烷基; X为氧，亚甲基或NH; Y代表各种无机和有机取代基; Z是氢，氨基或NHR 6，其中R6是具有1-6个碳原子的低级烷基; T是氢，卤素，羟基或具有1-6个碳原子的低级烷氧基; A是亚甲基，羰基或CHOH。这些化合物是脑单胺受体亚型或其前药的选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。这些化合物在本专利描述的动物模型中显示出意想不到的非典型抗精神病药谱（氯氮平样）。

18. 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。

19. 发明申请

US20080227793A1 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：US20080227793A1
公开(公告)日：2008-09-18
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： A61K31/496 , C07D403/06 , A61K31/4184 , C07D471/04 , G01N33/566 , A61P25/18 , A61P25/24 , C12N5/06 , A61K31/437 , C07D403/14
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。

20. 发明授权

US06936617B2 Heteroaryl substituted fused bicyclic heteroaryl compound as GABAA receptor ligands 失效
标题翻译：杂芳基取代的稠合双环杂芳基化合物作为GABA A受体配体
公开(公告)号：US06936617B2
公开(公告)日：2005-08-30
申请号：US10194852
申请日：2002-07-12
申请人： Alan Hutchison , George Maynard , Pamela Albaugh , Linghong Xie , Jun Yuan , Scott Mitchell , Vinod Singh , Manuka Ghosh , Guiying Li , Nian Liu
发明人： Alan Hutchison , George Maynard , Pamela Albaugh , Linghong Xie , Jun Yuan , Scott Mitchell , Vinod Singh , Manuka Ghosh , Guiying Li , Nian Liu
IPC分类号： G01N33/48 , A61K31/4355 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K31/519 , A61P25/00 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D471/04 , C07D487/04 , C07D513/04 , C12N15/09 , C12Q1/02 , G01N33/58 , G01N33/60 , A61K31/437
CPC分类号： C07D487/04 , C07D471/04 , C07D513/04
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: 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.
摘要翻译：本发明涉及可以由式I或式II描述的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，咪唑并嘧啶和咪唑并噻唑。本发明特别涉及以高选择性结合的这些化合物并且对GABA A A受体的苯并二氮杂位点具有高亲和力。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，吡啶基咪唑和相关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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