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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

US07148225B2 Substituted biaryl amides as C5A receptor modulators 失效
标题翻译：取代的联芳酰胺作为C5A受体调节剂
公开(公告)号：US07148225B2
公开(公告)日：2006-12-12
申请号：US10994224
申请日：2004-11-19
申请人： Yang Gao , Alan J. Hutchinson , Wallace C. Pringle , Taeyoung Yoon , He Zhao
发明人： Yang Gao , Alan J. Hutchinson , Wallace C. Pringle , Taeyoung Yoon , He Zhao
IPC分类号： A61K31/34 , A61K31/40 , A61K31/495 , C07D207/10 , C07D241/04
CPC分类号： C07D209/08 , C07C233/65 , C07C233/66 , C07C233/73 , C07C235/62 , C07C237/30 , C07C2602/08 , C07D207/325 , C07D231/56 , C07D317/58 , C07D333/24 , C07D405/12
摘要： Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies
摘要翻译：提供式I的取代的联芳酰胺。这些化合物是可用于在体内或体外调节C5a受体活性的配体，并且特别可用于治疗与人类，驯养的伴侣动物和家畜中的病理性C5a受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法

3. 发明授权

US5182386A Certain imidazoquinoxalinones; a new class of gaba brain receptor ligands 失效
标题翻译：某些咪唑并喹喔啉酮; 一类新的gaba脑受体配体
公开(公告)号：US5182386A
公开(公告)日：1993-01-26
申请号：US750522
申请日：1991-08-27
申请人： Pamela Albaugh , Alan J. Hutchinson
发明人： Pamela Albaugh , Alan J. Hutchinson
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 are variables;X and Y represent hydrogen, halogen, hydroxy or amino substituents, with the proviso that when Y is a hydrogen, halogen, or amino substituent, X is hydroxy; andW represent aryl groups unsubstituted or substituted with halogen, hydroxy, alkyl, alkoxy or amino groups.These compounds or prodrugs thereof are highly selective agonists, antagonists or inverse agonists or GaBAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorder, overdose with benzodiazepine drugs, and enchancement of memory.
摘要翻译：本发明包括下式的化合物：其中R 1，R 2，R 3，R 4是可变的; X和Y代表氢，卤素，羟基或氨基取代基，条件是当Y是氢，卤素或氨基取代基时，X是羟基; W表示未被取代或被卤素，羟基，烷基，烷氧基或氨基取代的芳基。这些化合物或其前药是高度选择性的激动剂，拮抗剂或反向激动剂或GaBAa脑受体或其前体药物，并且可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量使用，记忆功能增强。

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