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91. 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。

92. 发明授权

US06916827B2 Substituted ring-fused imidazole derivative: GABAA receptors ligands 失效
标题翻译：取代的环稠合咪唑衍生物：GABA A受体配体
公开(公告)号：US06916827B2
公开(公告)日：2005-07-12
申请号：US10438496
申请日：2003-05-15
申请人： George D. Maynard , Jun Yuan , George P. Luke , Kevin Currie
发明人： George D. Maynard , Jun Yuan , George P. Luke , Kevin Currie
IPC分类号： A61P25/00 , C07D471/04 , A61K31/437 , A61K31/4184 , A61K31/506 , C07D403/06
CPC分类号： C07D471/04
摘要： Substituted ring-fused imidazole derivatives that bind to GABAA receptors are provided. 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：提供了与GABA A A受体结合的取代的环稠合咪唑衍生物。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）。

93. 发明授权

US06916819B2 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：US06916819B2
公开(公告)日：2005-07-12
申请号：US10038069
申请日：2001-12-21
申请人： Guiying Li , John M. Peterson , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , Vinod Singh , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu
发明人： Guiying Li , John M. Peterson , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , Vinod Singh , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/435 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D233/20 , C07D233/54 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10 , C07D491/113 , C07D403/12
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。

94. 发明申请

US20050015496A1 Virtual connnectivity with local connection translation 有权
标题翻译：虚拟连接与本地连接转换
公开(公告)号：US20050015496A1
公开(公告)日：2005-01-20
申请号：US10619330
申请日：2003-07-14
申请人： Chuanxiong Guo , Jun Yuan , Qian Zhang , Wenwu Zhu
发明人： Chuanxiong Guo , Jun Yuan , Qian Zhang , Wenwu Zhu
IPC分类号： G06F15/00 , H04L12/28 , H04L12/56 , H04L29/06 , H04L29/08 , H04L29/12 , G06F15/16
CPC分类号： H04L63/12 , H04L29/06 , H04L29/12009 , H04L29/12518 , H04L61/2571 , H04L69/32 , H04W8/14 , H04W36/0011 , H04W80/04
摘要： A middle layer network protocol enhancement, virtual connectivity (VC) makes the network attachment point changes of local and remote peers transparent to applications that use network services. A virtual connectivity module local to each peer translates communication connection parameters from apparent to real and vice versa, as well as sending and receiving secure connection updates directly to and from peers. Unlike Mobile IP, no routing infrastructure modifications are required. A subscribe-notify service provides connection update notifications when direct peer-to-peer connection updates are not possible, for example, when two communicating peers move simultaneously or when the moving peer is communicating with a peer behind network address translation (NAT). Methods for detecting these conditions are disclosed, as is a virtual connectivity protocol and virtual connectivity module architecture.
摘要翻译：中间层网络协议增强，虚拟连接（VC）使本地和远程对等体的网络连接点更改对使用网络服务的应用程序透明化。每个对等体本地的虚拟连接模块将通信连接参数从明显转换为实际，反之亦然，以及直接向对方发送和接收安全连接更新。与移动IP不同，不需要进行路由基础架构修改。当直接对等连接更新不可行时，例如当两个通信对等体同时移动或当移动对等体与网络地址转换（NAT）之后的对等体通信时，订阅通知服务提供连接更新通知。公开了用于检测这些条件的方法，以及虚拟连接协议和虚拟连接模块架构。

95. 发明授权

US06820073B1 System and method for multiple pass cooperative processing 有权
标题翻译：多通道协同处理系统和方法
公开(公告)号：US06820073B1
公开(公告)日：2004-11-16
申请号：US10101488
申请日：2002-03-20
申请人： Jeffrey A. Bedell , William Hurwood , Benjamin Z. Li , Sadanand Sahasrabudhe , Xinyi Wang , Jun Yuan
发明人： Jeffrey A. Bedell , William Hurwood , Benjamin Z. Li , Sadanand Sahasrabudhe , Xinyi Wang , Jun Yuan
IPC分类号： G06F1730
CPC分类号： G06F17/30286 , Y10S707/954 , Y10S707/99932 , Y10S707/99933 , Y10S707/99934
摘要： A system for collaborative processing, comprising a controlling module with access to at least one relational database capable of performing a first set of functions on the data in the database and at least one external analytical engine, the external analytical engine being external to the relational database and being capable of a second set of functions on the data in the database. The controlling module is capable of iteratively processing a multi-step calculation including generating SQL statements to the relational database, passing preliminary results to an external analytical engine and saving data back into the relational database for further processing until the multi-step calculation is performed.
摘要翻译：一种用于协同处理的系统，包括控制模块，该控制模块可访问至少一个能够对数据库中的数据执行第一组功能的关系数据库和至少一个外部分析引擎，所述外部分析引擎在关系数据库外部并且能够对数据库中的数据进行第二组功能。控制模块能够迭代处理多步计算，包括生成SQL语句到关系数据库，将初步结果传递给外部分析引擎，并将数据保存回关系数据库进行进一步处理，直到执行多步计算。

96. 发明授权

US06624175B2 4-Substituted quinoline derivatives 失效
标题翻译： 4-取代的喹啉衍生物
公开(公告)号：US06624175B2
公开(公告)日：2003-09-23
申请号：US10140693
申请日：2002-05-07
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： A61K3147
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。

97. 发明授权

US06564199B1 Kaolin clay pigments, their preparation and use 有权
标题翻译：高岭土颜料，其制备及用途
公开(公告)号：US06564199B1
公开(公告)日：2003-05-13
申请号：US09937671
申请日：2001-12-20
申请人： Robert J. Pruett , Jun Yuan , Harry Vincent Brown, Jr. , David O. Cummings
发明人： Robert J. Pruett , Jun Yuan , Harry Vincent Brown, Jr. , David O. Cummings
IPC分类号： C04B1404
CPC分类号： C09C1/42 , C01P2004/51 , C01P2004/54 , C01P2004/61 , C01P2004/62 , D21H19/40
摘要： A paper coating pigment manufactured from kaolin crude containing minor amounts of minerals is used in lightweight coated and ultra-lightweight coated applications. The pigments comprise a phyllosilicate assemblage of minerals that yield a final pigment MgO content ranging between 0.04 to 0.3 weight percent and a K2O content ranging between 0.12 and 0.8 weight percent based on the dry weight of the kaolin crude. The mica in the pigment product is 1.0% to 6.7% by weight, and smectite is 1.2% to 9.1% by weight of the kaolin. The presence of these weight percentages can be identified by a shape factor of 15 or greater. The viscous clay content of the feed to produce the pigment product is between 70 and 100 weight percent based on the dry weight of the kaolin clay. The pigment has a shape factor ranging between 35 and 60 or greater, and greater than 80% by weight of the particle are less than 2 microns, and greater than 12% are less than 0.25 microns.
摘要翻译：由含有少量矿物质的高岭土原料制成的纸涂颜料用于轻质涂层和超轻质涂层应用。颜料包括矿物的页硅酸盐组合物，其基于高岭土原油的干重，产生0.04-0.3重量％的最终颜料MgO含量和范围在0.12至0.8重量％之间的K 2 O含量。颜料中的云母为1.0〜6.7重量％，绿土为高岭土的1.2〜9.1重量％。这些重量百分比的存在可以通过15或更大的形状因子来识别。用于生产颜料产品的进料的粘性粘土含量基于高岭土的干重为70-100重量％。颜料具有35至60或更大的形状因子，并且大于80重量％的颗粒小于2微米，并且大于12重量％小于0.25微米。

98. 发明授权

US06514333B1 Preparation and use of high brightness kaolin pigments 失效
标题翻译：高亮度高岭土颜料的制备和使用
公开(公告)号：US06514333B1
公开(公告)日：2003-02-04
申请号：US09700027
申请日：2000-11-09
申请人： Jun Yuan , Vince H. Brown , Robert J. Pruett , William L. Garforth
发明人： Jun Yuan , Vince H. Brown , Robert J. Pruett , William L. Garforth
IPC分类号： C04B1404
CPC分类号： C09C1/42 , C01P2004/51 , C01P2004/61 , C01P2004/62 , C01P2006/12 , C01P2006/22 , C01P2006/60 , D21H19/40
摘要： A novel clay pigment, the manufacture thereof and the use of the pigment in the coating of lightweight groundwood paper are disclosed. The kaolin clay particles initially have a shape factor between less than 10 and a particle size distribution where between 30 to 60% by weight is less than 2 microns and 20% by weight is less than 0.25 micron e.s.d. This clay is subjected to attrition grinding to produce clay particles having a shape factor between 13 and 18 and then classified to produce a particle size distribution where 80 to 90% by weight are less than 2 microns and 20% by weight are less than 0.25 micron. These pigments have a G.E. brightness ranging from 88 to 92; are deficient in ultra-fine particles; are fluid at a high solids concentration greater than 70%, and have a low shear Brookfield viscosity below 500 cps and a high shear Hercules viscosity of 18 dyne-cm above 200 rpm when using an “A” bob.
摘要翻译：公开了一种新型粘土颜料，其制造方法以及颜料在轻质磨木纸涂料中的应用。高岭土最初具有小于10的形状因子和30至60重量％小于2微米的粒度分布，20重量％小于0.25微米e.s.d。对该粘土进行磨磨研磨以产生形状因子为13至18的粘土颗粒，然后分级以产生其中80至90重量％小于2微米的颗粒尺寸分布，并且20重量％小于0.25微米。这些颜料具有G.E. 亮度从88到92; 缺乏超细颗粒; 是高固体浓度大于70％的流体，并且当使用“A”鲍勃时，具有低于500cps的低剪切布鲁克菲尔德粘度和高于200rpm的18dyne-cm的高剪切赫氏体粘度。

99. 发明授权

US06476051B2 Antipsychotic heterocycle compounds 有权
标题翻译：抗精神病药物杂环化合物
公开(公告)号：US06476051B2
公开(公告)日：2002-11-05
申请号：US09735384
申请日：2000-12-12
申请人： Ronald J. Mattson , Joseph P. Yevich , Jun Yuan , Arlene S. Eison , Derek Denhart
发明人： Ronald J. Mattson , Joseph P. Yevich , Jun Yuan , Arlene S. Eison , Derek Denhart
IPC分类号： A61K314439
CPC分类号： C07D417/14 , A61K31/454 , C07D401/04 , C07D417/12
摘要： Compounds of Formula I: wherein Ar, Y, m, and Z are as defined in the specification, are useful antipsychotic and antidepressant agents demonstrating potent inhibition of 5-HT reuptake and dopamine D2 receptor antagonism.
摘要翻译：式I化合物：其中Ar，Y，m和Z如说明书中所定义，是有效的抗精神病药和抗抑郁药，其表现出5-HT再摄取和多巴胺D2受体拮抗作用的有效抑制。

100. 发明授权

US06369053B1 2-Aminoquinolinecarboxamides: neurokinin receptor ligands 失效
标题翻译： 2-氨基喹啉甲酰胺：神经激肽受体配体
公开(公告)号：US06369053B1
公开(公告)日：2002-04-09
申请号：US09560160
申请日：2000-04-28
申请人： Jun Yuan , George D. Maynard , Alan Hutchison
发明人： Jun Yuan , George D. Maynard , Alan Hutchison
IPC分类号： C07D21550
CPC分类号： A61K31/47 , C07D215/50 , C07D401/04 , C07D453/06 , C07D491/10 , Y10S206/828
摘要： Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或药学上可接受的溶剂化物，其中R1，R2，R3，X，Q1和Q2如本文所定义，哪些化合物是神经激肽受体，特别是NK-3受体的配体，用于治疗广泛的疾病或病症，包括但不限于抑郁症，焦虑症，精神病，肥胖症，疼痛，帕金森病，阿尔茨海默病，神经变性疾病，运动障碍，呼吸系统疾病，炎性疾病，神经病，免疫疾病，偏头痛，胆汁功能不全和皮炎。

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