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1. 发明申请

US20110281837A1 3-SUBSTITUTED-6-ARYL PYRIDINES 审中-公开
标题翻译： 3-取代的6-芳基吡啶
公开(公告)号：US20110281837A1
公开(公告)日：2011-11-17
申请号：US12983661
申请日：2011-01-03
申请人： Alan J. Hutchinson , Jun Yuan , Kyungae Lee , George D. Maynard , Bertrand L. Chenard , Nian Liu , Qin Guo , Zihong Guo , Peter Hrnciar
发明人： Alan J. Hutchinson , Jun Yuan , Kyungae Lee , George D. Maynard , Bertrand L. Chenard , Nian Liu , Qin Guo , Zihong Guo , Peter Hrnciar
IPC分类号： A61K31/397 , A61K31/5377 , A61K31/4439 , A61K31/4709 , C12N5/078 , A61P19/02 , A61P17/06 , A61P9/00 , A61P11/06 , C12N5/071 , A61K31/4418 , A61K31/4545
CPC分类号： C07D213/30 , C07B2200/05 , C07D213/38 , C07D213/42 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/84 , C07D213/89 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C40B40/00
摘要： 3-substituted-6-aryl pyridines of Formula I 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 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 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式I的3-取代-6-芳基吡啶：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3-取代-6-芳基吡啶，其可用作C5a受体定位的探针。

2. 发明授权

US07863454B2 3-substituted-6-aryl pyridines 失效
标题翻译： 3-取代-6-芳基吡啶
公开(公告)号：US07863454B2
公开(公告)日：2011-01-04
申请号：US12041038
申请日：2008-03-03
申请人： Alan J. Hutchison , Jun Yuan , Kyungae Lee , George D. Maynard , Bertrand L. Chenard , Nian Liu , Qin Guo , Zihong Guo , Peter Hrnciar
发明人： Alan J. Hutchison , Jun Yuan , Kyungae Lee , George D. Maynard , Bertrand L. Chenard , Nian Liu , Qin Guo , Zihong Guo , Peter Hrnciar
IPC分类号： C07D401/04
CPC分类号： C07D213/30 , C07B2200/05 , C07D213/38 , C07D213/42 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/84 , C07D213/89 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C40B40/00
摘要： 3-substituted-6-aryl pyridines of Formula I 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 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 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式I的3-取代-6-芳基吡啶：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3-取代-6-芳基吡啶，其可用作C5a受体定位的探针。

3. 发明授权

US07342115B2 3-substituted-6-aryl pyridines 失效
标题翻译： 3-取代-6-芳基吡啶
公开(公告)号：US07342115B2
公开(公告)日：2008-03-11
申请号：US10704364
申请日：2003-11-07
申请人： Alan J. Hutchison , Jun Yuan , Kyungae Lee , George D. Maynard , Bertrand L. Chenard , Nian Liu , Qin Guo , Zihong Guo , Peter Hrnciar
发明人： Alan J. Hutchison , Jun Yuan , Kyungae Lee , George D. Maynard , Bertrand L. Chenard , Nian Liu , Qin Guo , Zihong Guo , Peter Hrnciar
IPC分类号： C07D213/61 , C07D213/62 , C07D213/72 , C07D213/73 , C07D213/84
CPC分类号： C07D213/30 , C07B2200/05 , C07D213/38 , C07D213/42 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/84 , C07D213/89 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C40B40/00
摘要： 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I 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 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式I的3-取代-6-芳基吡啶：其中R 1，R 2，R 3，R 8 R 9，R 9，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3-取代-6-芳基吡啶，其可用作C5a受体定位的探针。

4. 发明申请

US20090176980A1 3-Substituted-6-Aryl Pyridines 失效
标题翻译： 3-取代的6-芳基吡啶类
公开(公告)号：US20090176980A1
公开(公告)日：2009-07-09
申请号：US12041038
申请日：2008-03-03
申请人： Alan J. Hutchison , Jun Yuan , Kyungae Lee , George D. Maynard , Bertrand L. Chenard , Nian Liu , Qin Guo , Zhihong Guo , Peter Hrnciar
发明人： Alan J. Hutchison , Jun Yuan , Kyungae Lee , George D. Maynard , Bertrand L. Chenard , Nian Liu , Qin Guo , Zhihong Guo , Peter Hrnciar
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14
CPC分类号： C07D213/30 , C07B2200/05 , C07D213/38 , C07D213/42 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/84 , C07D213/89 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C40B40/00
摘要： 3-substituted-6-aryl pyridines of Formula I 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 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 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式I的3-取代-6-芳基吡啶：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3-取代-6-芳基吡啶，其可用作C5a受体定位的探针。

5. 发明授权

US08633193B2 Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds 失效
标题翻译：吡咯并吡啶，吡咯并嘧啶和相关的杂环化合物
公开(公告)号：US08633193B2
公开(公告)日：2014-01-21
申请号：US13014066
申请日：2011-01-26
申请人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
发明人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
IPC分类号： A61K31/519 , C07D487/04 , A61P37/00 , A61P37/06 , A61P11/06 , A61P17/06
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention 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 pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R 2，R 5，E，Z 1，Z 3，Z 4和Ar如本文所定义。这些化合物是C5a受体的配体。本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合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，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，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

6. 发明授权

US07906528B2 Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds 失效
标题翻译：吡咯并吡啶，吡咯并嘧啶和相关的杂环化合物
公开(公告)号：US07906528B2
公开(公告)日：2011-03-15
申请号：US11664565
申请日：2005-10-05
申请人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
发明人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
IPC分类号： C07D221/02 , C07D471/02 , C07D491/02 , C07D498/02 , A01N43/42 , A61K31/44
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention 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 pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R 2，R 5，E，Z 1，Z 3，Z 4和Ar如本文所定义。这些化合物是C5a受体的配体。本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合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，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，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

7. 发明申请

US20110118273A1 PYRROLO-PYRIDINE, PYRROLO-PYRIMIDINE AND RELATED HETEROCYCLIC COMPOUNDS 失效
标题翻译：吡咯并吡啶，吡咯并吡啶和相关的杂环化合物
公开(公告)号：US20110118273A1
公开(公告)日：2011-05-19
申请号：US13014066
申请日：2011-01-26
申请人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
发明人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
IPC分类号： A61K31/519 , C07D487/04 , A61P29/00 , A61P37/00 , A61P37/06 , A61P11/06 , A61P17/06 , A61P25/28 , A61P25/00 , A61P11/00 , A61P9/10 , A61P13/12 , A61P27/02 , A61P31/18
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention 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 pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R 2，R 5，E，Z 1，Z 3，Z 4和Ar如本文所定义。这些化合物是C5a受体的配体。本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合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，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，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

8. 发明申请

US20110160187A1 3-aryl-5,6-disubstituted pyridazines 失效
标题翻译： 3-芳基-5,6-二取代的哒嗪
公开(公告)号：US20110160187A1
公开(公告)日：2011-06-30
申请号：US11587737
申请日：2005-05-06
申请人： Taeyoung Yoon , Jun Yuan , Kyungae Lee , George D. Maynard , Nian Liu
发明人： Taeyoung Yoon , Jun Yuan , Kyungae Lee , George D. Maynard , Nian Liu
IPC分类号： A61K31/55 , C07D237/20 , C07D405/12 , C07D237/34 , C07D405/14 , C07D401/04 , C07D403/04 , C07D237/32 , C07D401/14 , C07D403/12 , C07D413/04 , A61K31/50 , A61K31/502 , C12N5/071 , A61K31/5377 , A61P29/00 , A61P17/06 , A61P9/00 , A61P11/06 , A61P25/00 , A61P9/10 , A61P11/00
CPC分类号： C07D237/20 , C07D237/34 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/04
摘要： The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.
摘要翻译：本发明提供式（I）或（II）的盐形式或前药的化合物，其中变量在本文中定义，其是金属蛋白酶例如基质金属蛋白酶（MMP）和ADAM的调节剂。本文所述的化合物或组合物可用于治疗与金属蛋白酶活性相关的疾病，包括例如关节炎，癌症，心血管疾病，皮肤病症，炎症或过敏性疾病。

9. 发明申请

US20080267887A1 Pyrrolo-Pyridine, Pyrrolo-Pyrimidine and Related Heterocyclic Compounds 失效
标题翻译：吡咯并 - 吡啶，吡咯并嘧啶和相关杂环化合物
公开(公告)号：US20080267887A1
公开(公告)日：2008-10-30
申请号：US11664565
申请日：2005-10-05
申请人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
发明人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
IPC分类号： A61K9/12 , C07D471/04 , A61K31/437 , C07K14/705 , A61P9/10 , C12Q1/02 , C12N5/06 , A61K31/506
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention 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 pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其分子式如下：其中R 1，R 2，R 5，E，Z 1， Z 3，Z 4和Ar如本文所定义。这些化合物是C5a受体的配体。本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合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，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，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a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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