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1. 发明申请

US20100216763A1 Heteroaryl Amide Derivatives 失效
标题翻译：杂芳基酰胺衍生物
公开(公告)号：US20100216763A1
公开(公告)日：2010-08-26
申请号：US12516480
申请日：2007-11-27
申请人： Alan J. Hutchison , Hongbin Li , Jianmin Mao , David J. Wustrow , Jun Yuan , He Zhao
发明人： Alan J. Hutchison , Hongbin Li , Jianmin Mao , David J. Wustrow , Jun Yuan , He Zhao
IPC分类号： A61K31/397 , C07D471/04 , A61K31/437 , C07D403/14 , A61K31/496 , C07D413/14 , A61K31/5377 , C07D223/04 , A61K31/55 , C07D221/20 , A61K31/438 , C07D295/15 , A61K31/4995 , C07D243/08 , A61K31/551 , C07D221/22 , A61K31/439 , C07D417/14 , A61K31/541 , C07D281/06 , A61K31/553 , A61P29/00 , A61P25/24 , A61P25/22 , A61P25/18
CPC分类号： C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/113 , C07D519/00
摘要： Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供了以下分子式的杂芳酰胺衍生物：其中变量如本文所述。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了使用这些化合物治疗这种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。

2. 发明授权

US08431593B2 Heteroaryl amide derivatives 失效
标题翻译：杂芳酰胺衍生物
公开(公告)号：US08431593B2
公开(公告)日：2013-04-30
申请号：US12516480
申请日：2007-11-27
申请人： Alan J. Hutchison , Hongbin Li , Jianmin Mao , David J. Wustrow , Jun Yuan , He Zhao
发明人： Alan J. Hutchison , Hongbin Li , Jianmin Mao , David J. Wustrow , Jun Yuan , He Zhao
IPC分类号： A61K31/44 , A01N43/42 , C07D221/02
CPC分类号： C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/113 , C07D519/00
摘要： Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供了以下分子式的杂芳酰胺衍生物：其中变量如本文所述。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了使用这些化合物治疗这种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. 发明申请

US20070078135A1 Substituted heteroaryl CB1 antagonists 审中-公开
标题翻译：取代的杂芳基CB1拮抗剂
公开(公告)号：US20070078135A1
公开(公告)日：2007-04-05
申请号：US11406532
申请日：2006-04-18
申请人： Jun Yuan , Qin Guo , He Zhao , Shaojing Hu , Darren Whitehouse , Wallace Pringle , Jianmin Mao , George Maynard , Jack Hammer , David Wustrow , Hongbin Li
发明人： Jun Yuan , Qin Guo , He Zhao , Shaojing Hu , Darren Whitehouse , Wallace Pringle , Jianmin Mao , George Maynard , Jack Hammer , David Wustrow , Hongbin Li
IPC分类号： A61K31/53 , A61K31/497 , A61K31/4965 , C07D403/02
CPC分类号： C07D403/14 , C07D213/28 , C07D213/61 , C07D213/74 , C07D239/42 , C07D239/54 , C07D241/12 , C07D241/20 , C07D241/24 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.
摘要翻译：提供式I化合物。其中变量如本文所述。这种化合物可用于体内或体外调节CB1活性，并且特别可用于治疗对人类，家养伴侣动物和家畜中的CB1调节有反应的病症，包括食欲障碍，肥胖症和成瘾性疾病。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和各种体外测定的方法。

4. 发明授权

US06858637B2 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：US06858637B2
公开(公告)日：2005-02-22
申请号：US10401270
申请日：2003-03-27
申请人： Yang Gao , Alan J. Hutchison , Wallace C. Pringle , Andrew Thurkauf , Taeyoung Yoon , He Zhao
发明人： Yang Gao , Alan J. Hutchison , Wallace C. Pringle , Andrew Thurkauf , Taeyoung Yoon , He Zhao
IPC分类号： A61K31/165 , A61K31/341 , A61K31/355 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4164 , A61K31/4178 , C07D207/32 , C07D233/56 , C07D307/40
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。

5. 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。

6. 发明授权

US08129395B2 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：US08129395B2
公开(公告)日：2012-03-06
申请号：US12320539
申请日：2009-01-26
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-arypyrimidines 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-丙嘧啶：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。

7. 发明申请

US20050277654A1 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：US20050277654A1
公开(公告)日：2005-12-15
申请号：US11123755
申请日：2005-05-06
申请人： George Maynard , Manuka Ghosh , Jun Yuan , Kevin Currie , Scott Mitchell , Qin Guo , He Zhao
发明人： George Maynard , Manuka Ghosh , Jun Yuan , Kevin Currie , Scott Mitchell , Qin Guo , He Zhao
IPC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
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R 1，R 2，R 3，R 本文定义了R 8，R 9，A和Ar。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。

8. 发明授权

US11304338B1 System, method, and apparatus for a high-efficiency heat riser 有权
公开(公告)号：US11304338B1
公开(公告)日：2022-04-12
申请号：US17108808
申请日：2020-12-01
申请人： Nan Chen , He Zhao , Yunshui Chen
发明人： Nan Chen , He Zhao , Yunshui Chen
IPC分类号： H05K7/20
摘要： A system, method, and apparatus for a heat riser having stackable blocks of thermally conductive material that include an upper block and a lower block, wherein the lower block has a lower surface that is configured to be engaged in thermal communication with a heat source. The lower block also having an inclined upper surface, that is configured to be in thermal communication with a block directly above, having a complemental inclined surface, wherein the blocks are elastically coupled with elastic components. The upper block may slide along the lower block allowing for vertical and horizontal axial elastic adjustment while providing consistent pressure to both the heat source and a cooling source to provide for heat dispersion along a thermal pathway from the heating source through the lower block, upper block and to a cooling source.

9. 发明申请

US20150203374A1 METHOD AND REACTOR FOR REMOVING ORGANIC MATTERS BY IMMOBILIZED-ENZYMATIC ELECTRODE COUPLED ELECTRO-COAGULATION 有权
标题翻译：通过固定电极电耦合电凝聚来去除有机物的方法与反应器
公开(公告)号：US20150203374A1
公开(公告)日：2015-07-23
申请号：US14395653
申请日：2012-06-20
申请人： Hongbin Cao , He Zhao , Yuping Li , Haitao Li , Yi Zhang
发明人： Hongbin Cao , He Zhao , Yuping Li , Haitao Li , Yi Zhang
IPC分类号： C02F1/463 , C02F1/461
CPC分类号： C02F1/463 , C02F1/46109 , C02F3/005 , C02F3/342 , C02F2001/46133 , C02F2001/46138 , C02F2001/46142 , C02F2201/46115
摘要： The present invention provides a method and a reactor for removing organic matters by immobilized-enzymatic electrode coupled electro-coagulation. In the method, in a single electrochemical system, an enzyme-modified electrode is combined with electro-coagulation to synergistically remove organic matters from water. Certain electrochemical parameters are controlled such that a polymerization reaction is performed between hydrogen peroxide generated by a cathode reaction and organic matters catalyzed by the immobilized-enzymatic electrode. After the polymerization reaction, the organic product enters an anode chamber through a pump. The organic product is precipitated and removed by performing a reaction between the organic product and different hydrolysis products from the electro-coagulation through a coagulating/flocculating effect of compression of a double electric layer, adsorption and electric neutralization as well as precipitation capture. Ultimately, the object of removing the organic matters synergistically through the enzymatic catalyzed polymerization at the cathode and the electro-coagulation at the anode is achieved. The present invention has a strong selectivity for low-concentration toxic organic pollutants and a good effect in removing small-molecular hydrophilic organic matters, the addition amount of enzyme is low, the cathode and the anode are fully used, the cost is reduced, the operation is simple, and the applicable is wide, therefore, the present invention is applicable to a variety of water and wastewater containing organic matters, and the contaminated water.
摘要翻译：本发明提供了通过固定化酶电极偶联电凝法除去有机物的方法和反应器。在该方法中，在单个电化学系统中，将酶修饰的电极与电凝结合以协同地从水中去除有机物质。控制某些电化学参数，使得在由阴极反应产生的过氧化氢和由固定化酶电极催化的有机物之间进行聚合反应。在聚合反应之后，有机产物通过泵进入阳极室。通过双电层压缩，吸附和电中和以及析出捕获的凝结/絮凝效应，通过进行有机产物与不同水解产物之间的反应从电凝中沉淀和除去有机产物。最终，通过在阴极处的酶催化聚合和阳极处的电凝而协同地去除有机物质的目的。本发明对低浓度有毒有机污染物具有很强的选择性，对小分子亲水有机物质的去除效果好，酶的添加量低，阴极和阳极得到充分利用，成本降低，操作简单，适用范围广，因此本发明适用于各种含有有机物的水和废水，以及污染的水。

10. 发明申请

US20070208048A1 New Aryl Imidazoles and Related Compounds as C5a Receptor Modulators 失效
标题翻译：新的芳基咪唑和相关化合物作为C5a受体调节剂
公开(公告)号：US20070208048A1
公开(公告)日：2007-09-06
申请号：US11680865
申请日：2007-03-01
申请人： George Luke , George Maynard , Scott Mitchell , Andrew Thurkauf , Linghong Xie , LuYan Zhang , Suoming Zhang , He Zhao , Bertrand Chenard , Yang Gao , Bingsong Han , Xiao He
发明人： George Luke , George Maynard , Scott Mitchell , Andrew Thurkauf , Linghong Xie , LuYan Zhang , Suoming Zhang , He Zhao , Bertrand Chenard , Yang Gao , Bingsong Han , Xiao He
IPC分类号： A61K31/505 , A61K31/415 , A61K31/44 , A61K31/50
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 ring system represented by is a 5 membered heteroaryl ring system, in which x is 0, A is chosen from carbon and heteroatoms nitrogen, oxygen, and sulfur, and E and G are independently carbon or nitrogen provided that the 5 membered heteroaryl ring system does not contain more than 3 heteroatoms or more than 1 oxygen or sulfur atom, or a 6 membered heteroaryl ring system, in which x is 1, A, B, E, and G are independently chosen from carbon and nitrogen, provided that the 6 membered heteroaryl ring system does not contain more than 3 nitrogen atoms. The remaining variables, Ar1, Ar2, R, R1, R2, R3, R4, R5, R6, y and z 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：本发明提供芳基取代的咪唑，吡唑，吡啶并且其中由其表示的环系是5元杂芳基环系的相关化合物，其中x为0，A选自碳和杂原子氮，氧和硫，并且E和G独立地为碳或氮，条件是5元杂芳基环系不包含多于3个杂原子或多于1个氧或硫原子，或6元杂芳基环系，其中x为1，A，B E和G独立地选自碳和氮，条件是6元杂芳基环系不含3个以上的氮原子。其余的变量Ar 1，R 2，R 1，R 1，R 2，R 2， 3，R 4，R 5，R 6，y和z在本文中定义。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。

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