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1. 发明申请

US20050148601A1 Neurokinin-3 receptor modulators: diaryl imidazole derivatives 审中-公开
标题翻译：神经激肽-3受体调节剂：二芳基咪唑衍生物
公开(公告)号：US20050148601A1
公开(公告)日：2005-07-07
申请号：US11007652
申请日：2004-12-07
申请人： George Maynard , Stanislaw Rachwal , Wallace Pringle , Jun Yuan , Linghong Xie , Yuelian Xu , Bingsong Han
发明人： George Maynard , Stanislaw Rachwal , Wallace Pringle , Jun Yuan , Linghong Xie , Yuelian Xu , Bingsong Han
IPC分类号： A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/498 , A61K31/506 , A61K31/538 , C07D233/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/12 , C07D413/02 , C07D413/04 , C07D417/02 , C07D417/04 , C07D43/02
CPC分类号： C07D233/90 , C07D233/64 , C07D405/04
摘要： The invention relates to compounds of general Formula I: wherein the variables are as defined herein. Also provided are pharmaceutical compositions comprising such compounds, and methods for treating patients suffering from a disorder responsive to neurokinin-3 receptor modulation. NK-3 receptor modulators provided herein are also useful as probes for the localization of NK-3 receptors.
摘要翻译：本发明涉及通式I的化合物：其中变量如本文所定义。还提供了包含这些化合物的药物组合物，以及用于治疗患有对神经激肽-3受体调节有响应的病症的患者的方法。本文提供的NK-3受体调节剂也可用作NK-3受体定位的探针。

2. 发明授权

US07271170B2 Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands 有权
标题翻译：咪唑并 - 嘧啶和三唑并嘧啶：苯并二氮杂受体配体
公开(公告)号：US07271170B2
公开(公告)日：2007-09-18
申请号：US10898690
申请日：2004-07-23
申请人： Linghong Xie , Bingsong Han , Yuelian Xu , George Maynard , Bertrand L. Chenard , Kenneth Shaw , Yang Gao
发明人： Linghong Xie , Bingsong Han , Yuelian Xu , George Maynard , Bertrand L. Chenard , Kenneth Shaw , Yang Gao
IPC分类号： C07D487/04 , A61K31/519 , A61P25/24 , A61P25/22 , A61P25/20
CPC分类号： C07D487/04
摘要： Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, 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：提供了式I化合物，以及其制备方法。变量Z 1，Z 2，Z 3，R 4，R 5，/或 >，R 6，R 7，R 8和Ar如上所定义。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）。

3. 发明申请

US20080139580A1 IMIDAZO-PYRIMIDINES AND TRIAZOLO-PYRIMIDINES: BENZODIAZEPINE RECEPTOR LIGANDS 审中-公开
标题翻译：咪唑并吡啶和三唑并嘧啶：苯并咪唑受体配体
公开(公告)号：US20080139580A1
公开(公告)日：2008-06-12
申请号：US11855386
申请日：2007-09-14
申请人： Linghong Xie , Bingsong Han , Yuelian Xu , George Maynard , Bertrand L. Chenard , Kenneth Shaw , Yang Gao
发明人： Linghong Xie , Bingsong Han , Yuelian Xu , George Maynard , Bertrand L. Chenard , Kenneth Shaw , Yang Gao
IPC分类号： A61K31/437 , C12N5/06 , C07K14/705 , A61P25/00 , A61P25/24
CPC分类号： C07D487/04
摘要： Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, 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：提供了式I化合物，以及其制备方法。变量Z 1，Z 2，Z 3，R 4，R 5，/或 >，R 6，R 7，R 8和Ar如上所定义。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

US20080004269A1 Pyrazolylmethy Heteroaryl Derivatives 审中-公开
标题翻译：吡唑基甲基杂芳基衍生物
公开(公告)号：US20080004269A1
公开(公告)日：2008-01-03
申请号：US11718528
申请日：2005-11-01
申请人： Yuelian Xu , Linghong Xie , Yang Gao , Bingsong Han , George Maynard , Bertrand Chenard , Jiong Lan
发明人： Yuelian Xu , Linghong Xie , Yang Gao , Bingsong Han , George Maynard , Bertrand Chenard , Jiong Lan
IPC分类号： A61K31/506 , A61K31/444 , A61K31/519 , A61P25/22 , A61P25/28 , C07D403/14 , C07D487/04 , C07D413/14 , C07D239/34 , A61P25/24 , A61K31/5377 , A61K31/497
CPC分类号： G01N33/9426 , C07D401/14 , C07D417/14 , C07D487/04
摘要： Compounds of Formula (I) are provided, as are methods for their preparation. The variables W, X, Y, Z, R5, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptorsin 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（I）的化合物，以及它们的制备方法。上式定义了上式中的变量W，X，Y，Z，R 5，R 8和Ar。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）障碍，驯养的伴侣动物和牲畜。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）。

5. 发明申请

US20050038043A1 Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands 有权
标题翻译：咪唑并 - 嘧啶和三唑并嘧啶：苯并二氮杂受体配体
公开(公告)号：US20050038043A1
公开(公告)日：2005-02-17
申请号：US10898690
申请日：2004-07-23
申请人： Linghong Xie , Bingsong Han , Yuelian Xu , George Maynard , Bertrand Chenard , Kenneth Shaw , Yang Gao
发明人： Linghong Xie , Bingsong Han , Yuelian Xu , George Maynard , Bertrand Chenard , Kenneth Shaw , Yang Gao
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, 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：提供了式I化合物，以及其制备方法。上述式中的变量Z1，Z2，Z3，R4，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）。

6. 发明授权

US07351826B2 Aryl acid pyrimidinyl methyl amides, pyridazinyl methyl amides and related compounds 失效
标题翻译：芳基嘧啶基甲基酰胺，哒嗪基甲基酰胺和相关化合物
公开(公告)号：US07351826B2
公开(公告)日：2008-04-01
申请号：US10544882
申请日：2004-02-16
申请人： Linghong Xie , Bingsong Han , Yuelian Xu
发明人： Linghong Xie , Bingsong Han , Yuelian Xu
IPC分类号： C07D487/00 , A61K31/519
CPC分类号： C07D213/69 , C07D213/81 , C07D237/08 , C07D237/12 , C07D237/16 , C07D239/26 , C07D239/30 , C07D239/34 , C07D401/12 , C07D487/04
摘要： The invention provides compounds of Formula (I) that bind to GABAA receptors. In the above formula, variables 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：本发明提供结合GABA A A受体的式（I）化合物。在上述公式中，变量在本文中定义。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。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）

7. 发明申请

US20070049571A1 Dipiperazinyl ketones and related analogues 有权
标题翻译：二哌嗪酮和相关的类似物
公开(公告)号：US20070049571A1
公开(公告)日：2007-03-01
申请号：US11495986
申请日：2006-07-28
申请人： Linghong Xie , Joseph Ochterski , Yang Gao , Bingsong Han , Timothy Caldwell , Yuelian Xu , John Peterson , Ping Ge , Robert Ohliger
发明人： Linghong Xie , Joseph Ochterski , Yang Gao , Bingsong Han , Timothy Caldwell , Yuelian Xu , John Peterson , Ping Ge , Robert Ohliger
IPC分类号： A61K31/551 , A61K31/55 , A61K31/497 , A61K31/496 , A61K31/4545 , A61K31/454 , C07D403/02
CPC分类号： C07D403/06 , C07D207/09 , C07D207/14 , C07D211/14 , C07D211/34 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/72 , C07D213/74 , C07D213/82 , C07D215/48 , C07D217/02 , C07D237/20 , C07D237/22 , C07D237/24 , C07D239/47 , C07D241/08 , C07D241/20 , C07D243/08 , C07D263/32 , C07D271/06 , C07D277/56 , C07D277/82 , C07D295/033 , C07D295/185 , C07D295/192 , C07D295/215 , C07D333/70 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/14 , C07D405/04 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/10 , C07D491/107
摘要： Dipiperazinyl ketones and related analogues are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
摘要翻译：提供了二吡嗪基酮和相关的类似物，以及它们的制备和使用方法。这样的化合物通常可用于在体内或体外调节配体与组胺H3受体的结合，并且特别可用于治疗人类，驯养的伴侣动物和家畜中的各种疾病。提供药物组合物和治疗方法，以及使用这种配体检测组胺H3受体的方法（例如，受体定位研究）。

8. 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）。

9. 发明申请

US20110082130A1 PIPERAZINYL OXOALKYL TETRAHYDROISOQUINOLINES AND RELATED ANALOGUES 审中-公开
标题翻译：哌嗪二甲氧基四氢喹啉和相关的类似物
公开(公告)号：US20110082130A1
公开(公告)日：2011-04-07
申请号：US12861504
申请日：2010-08-23
申请人： Yang Gao , Bingsong Han , Yuelian Xu , Timothy M Caldwell , Linghong Xie
发明人： Yang Gao , Bingsong Han , Yuelian Xu , Timothy M Caldwell , Linghong Xie
IPC分类号： A61K31/496 , C07D401/06 , C07D403/06 , C07D401/14 , C07D471/04 , C07D487/04 , A61K31/55 , A61K31/501 , A61K31/5377 , A61K31/4985 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/06 , A61P25/08 , A61P25/16 , A61P3/04 , A61P3/10
CPC分类号： C07D217/04 , C07D217/14 , C07D223/16 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/14 , C07D413/04 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/04 , C07D495/04 , C07D497/04 , C07D513/04
摘要： Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other 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 histamine H3 receptors (e.g., receptor localization studies).
摘要翻译：哌嗪基氧基烷基四氢异喹啉及其相关的类似物，其中变量如本文所述。这样的化合物可用于在体内或体外调节配体与组胺H3受体的结合，并且特别可用于治疗人，家养伴侣动物和家畜中的各种中枢神经系统（CNS）和其他疾病。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。提供了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组胺H3受体的方法（例如，受体定位研究）。

10. 发明授权

US07851474B2 Dipiperazinyl ketones and related analogues 有权
标题翻译：二哌嗪酮和相关的类似物
公开(公告)号：US07851474B2
公开(公告)日：2010-12-14
申请号：US11495986
申请日：2006-07-28
申请人： Linghong Xie , Joseph W. Ochterski , Yang Gao , Bingsong Han , Timothy M. Caldwell , Yuelian Xu , John M. Peterson , Ping Ge , Robert Ohliger
发明人： Linghong Xie , Joseph W. Ochterski , Yang Gao , Bingsong Han , Timothy M. Caldwell , Yuelian Xu , John M. Peterson , Ping Ge , Robert Ohliger
IPC分类号： A61K31/497 , C07D241/04 , C07D295/00
CPC分类号： C07D403/06 , C07D207/09 , C07D207/14 , C07D211/14 , C07D211/34 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/72 , C07D213/74 , C07D213/82 , C07D215/48 , C07D217/02 , C07D237/20 , C07D237/22 , C07D237/24 , C07D239/47 , C07D241/08 , C07D241/20 , C07D243/08 , C07D263/32 , C07D271/06 , C07D277/56 , C07D277/82 , C07D295/033 , C07D295/185 , C07D295/192 , C07D295/215 , C07D333/70 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/14 , C07D405/04 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/10 , C07D491/107
摘要： Dipiperazinyl ketones and related analogues are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
摘要翻译：提供了二吡嗪基酮和相关的类似物，以及它们的制备和使用方法。这样的化合物通常可用于在体内或体外调节配体与组胺H3受体的结合，并且特别可用于治疗人类，驯养的伴侣动物和家畜中的各种疾病。提供药物组合物和治疗方法，以及使用这种配体检测组胺H3受体的方法（例如，受体定位研究）。

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