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1. 发明公开

EP1713784A1 IMIDAZO-PYRIDAZINES, TRIAZOLO-PYRIDAZINES AND RELATED BENZODIAZEPINE RECEPTOR LIGANDS 审中-公开
标题翻译：咪唑并哒嗪，三唑并哒嗪和有关苯二氮卓受体配体
公开(公告)号：EP1713784A1
公开(公告)日：2006-10-25
申请号：EP05722901.5
申请日：2005-02-09
申请人： NEUROGEN CORPORATION , Xu, Yuelian , Han, Bingsong , Xie, Linghong , Maynard, George
发明人： XU, Yuelian , HAN, Bingsong , XIE, Linghong , MAYNARD, George
IPC分类号： C07D253/08 , C07D237/26 , C07D237/28 , C07D237/30 , A61K31/502 , A61K31/5025 , A61K31/53 , A61P25/28
CPC分类号： C07D487/04 , A61K31/502 , A61K31/5025 , A61K31/53
摘要： Compounds of the Formula are provided, as are methods for their preparation. The variables Z1, Z2, R3, Z4, 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).

2. 发明公开

EP1619948A4 SUSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS 审中-公开
标题翻译：取代的咪唑并吡嗪和三氮唑衍生物：GABAA受体配体
公开(公告)号：EP1619948A4
公开(公告)日：2007-02-14
申请号：EP04751255
申请日：2004-05-03
申请人： NEUROGEN CORP , XU YUELIAN , HAN BINGSONG , XIE LINGHONG
发明人： XU YUELIAN , HAN BINGSONG , XIE LINGHONG
IPC分类号： C07D487/00 , A61K31/50 , A61P25/00 , C07D471/00 , C07D487/04 , C07D491/00 , C07D495/00 , C07D497/00 , C07D519/00 , G01N33/566
CPC分类号： C07D487/04 , G01N33/566

3. 发明公开

EP1619948A1 SUSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS 审中-公开
标题翻译：悬浮咪唑并吡嗪和三唑并吡嗪衍生物：GABAA受体配体
公开(公告)号：EP1619948A1
公开(公告)日：2006-02-01
申请号：EP04751255.3
申请日：2004-05-03
申请人： NEUROGEN CORPORATION , Xu, Yuelian , Han, Bingsong , Xie, Linghong
发明人： XU, Yuelian , HAN, Bingsong , XIE, Linghong
IPC分类号： A01N43/58 , A01N43/60 , A61K31/495 , A61K31/50 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00
CPC分类号： C07D487/04 , G01N33/566
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：提供式（I）化合物，以及它们的制备方法。上式中的变量Z1，Z2，Z3，R4，R5，R6，R7，R8和Ar在本文中定义。此类化合物可用于在体内或体外调节配体与GABAA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）疾病。本文提供的化合物可以单独施用或与一种或多种其他CNS试剂组合施用以增强其他CNS试剂的作用。提供了用于治疗此类病症的药物组合物和方法，以及使用这些配体用于检测GABAA受体（例如受体定位研究）的方法。

4. 发明申请

WO2006093911A2 THIAZOLYLMETHYL AND OXAZOLYLMETHYL HETEROARYL DERIVATIVES 审中-公开
标题翻译：三唑基甲基和氧代甲基苯乙烯衍生物
公开(公告)号：WO2006093911A2
公开(公告)日：2006-09-08
申请号：PCT/US2006006937
申请日：2006-02-28
申请人： NEUROGEN CORP , XU YUELIAN , XIE LINGHONG
发明人： XU YUELIAN , XIE LINGHONG
CPC分类号： C07D487/04 , C07D413/14 , C07D417/14
摘要： Compounds of Formula: (I) are provided, as are methods for their preparation. The variables in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABA A 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 GABA A 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。上述公式中的变量在此定义。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）障碍，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（例如受体定位研究）的方法。

5. 发明申请

WO2005066137A1 2,5-DIARYL-1H-IMIDAZOLE-4-CARBOXAMIDES AS NEUROKININ-3 RECEPTOR MODULATORS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM AND PERIPHERAL DISEASES 审中-公开
标题翻译：作为治疗中枢神经系统和外周疾病的神经营养因子-3受体调节剂的2,5-DIARYL-1H-咪唑-4-羧酰胺
公开(公告)号：WO2005066137A1
公开(公告)日：2005-07-21
申请号：PCT/US2004/041097
申请日：2004-12-07
申请人： NEUROGEN CORPORATION , MAYNARD, George , RACHWAL, Stanislaw , PRINGLE, Wallace, C. , YUAN, Jun , XIE, Linghong , XU, Yuelian , HAN, Bingsong
发明人： MAYNARD, George , RACHWAL, Stanislaw , PRINGLE, Wallace, C. , YUAN, Jun , XIE, Linghong , XU, Yuelian , HAN, Bingsong
IPC分类号： C07D233/54
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。

6. 发明申请

WO2007146122A3 TETRAHYDROPYRIDO[3,4-D]PYRIMIDINES AND RELATED ANALOGUES 审中-公开
标题翻译：四氢吡咯并[3,4-D]吡嗪和相关的类似物
公开(公告)号：WO2007146122A3
公开(公告)日：2008-12-04
申请号：PCT/US2007013506
申请日：2007-06-08
申请人： NEUROGEN CORP , XU YUELIAN , GAO YANG , XIE LINGHONG
发明人： XU YUELIAN , GAO YANG , XIE LINGHONG
IPC分类号： C07D471/02 , A61K31/54 , C07D265/30 , C07D417/14
CPC分类号： A61K31/496 , A61K31/55 , C07D471/04 , C07D487/04
摘要： Tetrahydropyrido[3,4-d]pyrimidines and related analogues are provided, of the formula (I) in which variables are as described herein, 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：提供四氢吡啶并[3,4-d]嘧啶和相关的类似物，其中变量如本文所述，其式（I）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）。

7. 发明申请

WO2006052546A2 PYRAZOLYLMETHYL HETEROARYL DERIVATIVES 审中-公开
标题翻译：吡唑啉衍生物衍生物（PYRAZOLYLMETHYL HETEROARYL DERIVATIVES）
公开(公告)号：WO2006052546A2
公开(公告)日：2006-05-18
申请号：PCT/US2005/039488
申请日：2005-11-01
申请人： NEUROGEN CORPORATION , XU, Yuelian , XIE, Linghong , GAO, Yang , HAN, Bingsong , MAYNARD, George, D. , CHENARD, Bertrand, L. , LAN, Jiong
发明人： XU, Yuelian , XIE, Linghong , GAO, Yang , HAN, Bingsong , MAYNARD, George, D. , CHENARD, Bertrand, L. , LAN, Jiong
IPC分类号： A61K31/506
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, R 5 , R 8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABA A 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 GABA A 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 Aα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）。

8. 发明申请

WO2004107863A1 SUSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS 审中-公开
标题翻译：不溶性咪唑并吡嗪和三唑并吡啶衍生物：GABAA受体配体
公开(公告)号：WO2004107863A1
公开(公告)日：2004-12-16
申请号：PCT/US2004/013778
申请日：2004-05-03
申请人： NEUROGEN CORPORATION , XU, Yuelian , HAN, Bingsong , XIE, Linghong
发明人： XU, Yuelian , HAN, Bingsong , XIE, Linghong
IPC分类号： A01N43/58
CPC分类号： C07D487/04 , G01N33/566
摘要： Compounds of Formula (I) are provided, as are methods for their preparation. The variables Z 1 , Z 2 , Z 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and Ar in the above Formula are defined herein. Such compounds may be used to modulate ligand binding to GABA A 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 GABA A 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。上述式中的变量Z1，Z2，Z3，R4，R5，R6，R7，R8和Ar如本文所定义。此类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，家养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）。

9. 发明申请

WO2004074259A1 ARYL ACID PYRIMIDINYL METHYL AMIDES, PYRIDAZINYL METHYL AMIDES AND RELATED COMPOUNDS 审中-公开
标题翻译：芳基酰亚胺基甲基酰胺，吡咯烷基甲基和相关化合物
公开(公告)号：WO2004074259A1
公开(公告)日：2004-09-02
申请号：PCT/IB2004/000009
申请日：2004-02-16
申请人： NEUROGEN CORPORATION , XIE, Linghong , HAN, Bingsong , XU, Yuelian
发明人： XIE, Linghong , HAN, Bingsong , XU, Yuelian
IPC分类号： C07D237/16
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 GABA A receptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABA A 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 GABA A receptors (e.g., receptor localization studies).
摘要翻译：本发明提供结合GABA A受体的式（I）化合物。在上述公式中，变量在本文中定义。此类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，家养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）。

10. 发明申请

WO2009039431A3 SUBSTITUTED ARYL-FUSED SPIROCYCLIC AMINES 审中-公开
标题翻译：取代的ARYL-FUSED螺旋烯胺
公开(公告)号：WO2009039431A3
公开(公告)日：2010-07-01
申请号：PCT/US2008077103
申请日：2008-09-19
申请人： NEUROGEN CORP , XU YUELIAN , XIE LINGHONG
发明人： XU YUELIAN , XIE LINGHONG
IPC分类号： C07D403/14 , C07D403/12
CPC分类号： C07D405/14 , C07D401/14 , C07D471/10
摘要： Substituted Aryl-fused Spirocyclic Amines of the formula (I): 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：提供式（I）的取代的芳基稠合的四环胺：其制备和使用方法。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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