专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US08119665B2 Aryl imidazoles and related compounds as C5a receptor modulators 失效
标题翻译：芳基咪唑和相关化合物作为C5a受体调节剂
公开(公告)号：US08119665B2
公开(公告)日：2012-02-21
申请号：US11680865
申请日：2007-03-01
申请人： George P. Luke , George D. Maynard , Scott Mitchell , Andrew Thurkauf , Linghong Xie , LuYan Zhang , Suoming Zhang , He Zhao , Bertrand L. Chenard , Yang Gao , Bingsong Han , Xiao Shu He
发明人： George P. Luke , George D. Maynard , Scott Mitchell , Andrew Thurkauf , Linghong Xie , LuYan Zhang , Suoming Zhang , He Zhao , Bertrand L. Chenard , Yang Gao , Bingsong Han , Xiao Shu He
IPC分类号： A61K31/4439 , A61K31/4164 , A61K31/4178
CPC分类号： C07D233/64 , A61K31/4164 , C07D233/68 , C07D235/02 , C07D235/30 , C07D237/12 , C07D401/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides packaged pharmaceutical preparations of Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula where the variables are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.
摘要翻译：本发明提供了芳基取代的咪唑，吡唑，吡啶并且其中变量在本文中定义的相关化合物的包装药物制剂。这些化合物是C5a受体的配体。本发明优选的化合物作用以高亲和力结合C5a受体，在C5a受体上表现出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。它还涉及这些化合物在治疗各种炎性和免疫系统疾病中的应用。

2. 发明授权

US07186734B2 Aryl imidazoles and related compounds as C5a receptor modulators 失效
标题翻译：芳基咪唑和相关化合物作为C5a受体调节剂
公开(公告)号：US07186734B2
公开(公告)日：2007-03-06
申请号：US10405989
申请日：2003-03-28
申请人： George D. Maynard , Andrew Thurkauf , He Zhao , Bertrand L. Chenard , Yang Gao
发明人： George D. Maynard , Andrew Thurkauf , He Zhao , Bertrand L. Chenard , Yang Gao
IPC分类号： A61K31/4439 , A61K31/4164 , A61K31/4178 , C07D401/04 , C07D233/61 , C07D233/54
CPC分类号： C07D233/64 , A61K31/4164 , C07D233/68 , C07D235/02 , C07D235/30 , C07D237/12 , C07D401/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula where the variables are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptos. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.
摘要翻译：本发明提供芳基取代的咪唑，吡唑，吡啶并且其中变量在本文中定义的相关化合物。这些化合物是C5a受体的配体。本发明优选的化合物作用以高亲和力结合C5a受体，并在C5a受体上表现出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。它还涉及这些化合物在治疗各种炎性和免疫系统疾病中的应用。

3. 发明授权

US07122546B2 Imidazol-1-ylmethyl pyridazine derivatives 失效
标题翻译：咪唑-1-基甲基哒嗪衍生物
公开(公告)号：US07122546B2
公开(公告)日：2006-10-17
申请号：US10680351
申请日：2003-10-07
申请人： Linghong Xie , Bingsong Han , Yuelian Xu , George D. Maynard
发明人： Linghong Xie , Bingsong Han , Yuelian Xu , George D. Maynard
IPC分类号： C07D403/06 , C07D403/14 , A61K31/501 , A61P25/22 , A61P25/24
CPC分类号： C07D409/14 , C07D401/14 , C07D403/06 , C07D417/14
摘要： The invention provides imidazol-1-ylmethyl pyridazine derivatives of the formula: that bind to GABAA receptors. In the above formula, R1, R2 R3, R4, R5, R6 and Ar are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
摘要翻译：本发明提供下式的咪唑-1-基甲基哒嗪衍生物：其结合GABA A A受体。在上式中，R 1，R 2，R 3，R 4，R 5， / SUB，R 6和Ar如本文所定义。这样的化合物可用于在体内或体外调节配体与GABA A A受体的结合，并且特别可用于治疗人类中的各种中枢神经系统（CNS）紊乱，驯养伴侣动物，和牲畜。本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用，以增强其它CNS剂的作用。还提供了用于治疗这种病症的药物组合物和方法，以及使用这种配体检测GABA A受体的方法（例如，受体定位研究）。

4. 发明申请

US20090023737A1 Imidazo-Pyridazines, Triazolo-Pyridazines and Related Benzodiazepine Receptor Ligands 审中-公开
标题翻译：咪唑 - 哒嗪，三唑并哒嗪和相关苯并二氮杂受体配体
公开(公告)号：US20090023737A1
公开(公告)日：2009-01-22
申请号：US10589095
申请日：2005-02-09
申请人： Yuelian Xu , Bingsong Han , Linghong Xie , George D. Maynard
发明人： Yuelian Xu , Bingsong Han , Linghong Xie , George D. Maynard
IPC分类号： A61K31/5025 , C07D487/04 , A61P25/24 , A61P25/22
CPC分类号： C07D487/04 , A61K31/502 , A61K31/5025 , A61K31/53
摘要： Compounds of the Formula: are provided, as are methods for their preparation. The variables Z1, Z2, R3, Z4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
摘要翻译：提供式的化合物：其制备方法。上述式中的变量Z1，Z2，R3，Z4，R5，R6，R7，R8和Ar定义如下。这样的化合物可用于在体内或体外调节配体与GABA A受体的结合，并且特别可用于治疗人，驯养的伴侣动物和家畜中的各种中枢神经系统（CNS）障碍。本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用，以增强其它CNS剂的作用。还提供了用于治疗这种病症的药物组合物和方法，以及使用这种配体检测GABA A受体的方法（例如受体定位研究）。

5. 发明授权

US06951864B2 4-imidazol-1-ylmethyl-pyrimidine derivatives 失效
标题翻译： 4-咪唑-1-基甲基 - 嘧啶衍生物
公开(公告)号：US06951864B2
公开(公告)日：2005-10-04
申请号：US10702629
申请日：2003-11-06
申请人： Linghong Xie , Bingsong Han , Yuelian Xu , George D. Maynard
发明人： Linghong Xie , Bingsong Han , Yuelian Xu , George D. Maynard
IPC分类号： A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D401/14 , C07D403/06 , C07D417/14 , A61K31/4178
CPC分类号： C07D401/14 , C07D403/06 , C07D417/14
摘要： The invention provides 4-imidazol-1-ylmethyl pyrimidine of the formula that bind to GABAA receptors. In the above formula, R1, R2 R3, R4, R5, R6 and Ar are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
摘要翻译：本发明提供了结合GABA A A受体的下式的4-咪唑-1-基甲基嘧啶。在上式中，R 1，R 2，R 3，R 4，R 5， / SUB，R 6和Ar如本文所定义。这样的化合物可用于在体内或体外调节配体与GABA A A受体的结合，并且特别可用于治疗人类中的各种中枢神经系统（CNS）紊乱，驯养伴侣动物，和牲畜。本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用，以增强其它CNS剂的作用。还提供了用于治疗这种病症的药物组合物和方法，以及使用这种配体检测GABA A受体的方法（例如，受体定位研究）。

6. 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。

7. 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。

8. 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。

9. 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。

10. 发明授权

US07482350B2 4,5-disubstituted-2-aryl pyrimidines 失效
标题翻译： 4,5-二取代-2-芳基嘧啶
公开(公告)号：US07482350B2
公开(公告)日：2009-01-27
申请号：US11123755
申请日：2005-05-06
申请人： George D. Maynard , Manuka Ghosh , Jun Yuan , Kevin S. Currie , Scott Mitchell , Qin Guo , He Zhao
发明人： George D. Maynard , Manuka Ghosh , Jun Yuan , Kevin S. Currie , Scott Mitchell , Qin Guo , He Zhao
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04 , C07D403/00
CPC分类号： A61K31/505 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04
摘要： 4,5-disubstituted-2-arylpyrimidines of Formula I and Formula II are provided: 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 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式I和式II的4,5-二取代-2-芳基嘧啶：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4,5-二取代-2-芳基嘧啶，其可用作C5a受体定位的探针。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式