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1. 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

2. 发明申请

WO2006052546A3 PYRAZOLYLMETHYL 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：WO2006052546A3
公开(公告)日：2006-07-20
申请号：PCT/US2005039488
申请日：2005-11-01
申请人： NEUROGEN CORP , 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： C07D401/14 , A61K31/4155 , C07D231/28 , C07D403/14
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 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 GABA A 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W，X，Y，Z，R 5，R 8，Ar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GABA受体的结合，并且特别可用于治疗人类，家养伴侣动物中的多种中枢神经系统（CNS）病症和家畜动物。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GABA受体（例如受体定位研究）的方法。

3. 发明申请

WO2009097405A3 COMPOUNDS AND METHODS FOR PREPARING DIAZASPIRO DERIVATIVES 审中-公开
标题翻译：制备二氮杂衍生物的化合物和方法
公开(公告)号：WO2009097405A3
公开(公告)日：2009-10-15
申请号：PCT/US2009032400
申请日：2009-01-29
申请人： NEUROGEN CORP , XU YUELIAN , XIE LINGHONG , HAN BINGSONG , MAYNARD GEORGE D , CHENARD BERTRAND L , STAAB ANDREW J
发明人： XU YUELIAN , XIE LINGHONG , HAN BINGSONG , MAYNARD GEORGE D , CHENARD BERTRAND L , STAAB ANDREW J
IPC分类号： C07D487/04 , C07D487/02
CPC分类号： C07D471/10 , C07D471/20
摘要： Compounds and methods are provided for the synthesis of diazaspiro derivatives of the Formula: wherein R is as described herein. Such compounds are useful, for example, as intermediates in the synthesis of biologically active compounds.
摘要翻译：提供了用于合成下式的二氮杂螺衍生物的化合物和方法：其中R如本文所述。这样的化合物例如可用作合成生物活性化合物的中间体。

4. 发明申请

WO2007106349A3 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：WO2007106349A3
公开(公告)日：2007-11-29
申请号：PCT/US2007005762
申请日：2007-03-08
申请人： NEUROGEN CORP , GAO YANG , HAN BINGSONG , XU YUELIAN , CALDWELL TIMOTHY M , XIE LINGHONG
发明人： GAO YANG , HAN BINGSONG , XU YUELIAN , CALDWELL TIMOTHY M , XIE LINGHONG
IPC分类号： A01N55/02 , A61K31/555
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）。

5. 发明申请

WO2007016496A2 DIPIPERAZINYL KETONES AND RELATED ANALOGUES 审中-公开
标题翻译：二苯乙酮酮和相关的类似物
公开(公告)号：WO2007016496A2
公开(公告)日：2007-02-08
申请号：PCT/US2006029761
申请日：2006-07-28
申请人： NEUROGEN CORP , XIE LINGHONG , OCHTERSKI JOSEPH W , GAO YANG , HAN BINGSONG , CALDWELL TIMOTHY M , XU YUELIAN , PETERSON JOHN M , GE PING , OHLIGER ROBERT
发明人： XIE LINGHONG , OCHTERSKI JOSEPH W , GAO YANG , HAN BINGSONG , CALDWELL TIMOTHY M , XU YUELIAN , PETERSON JOHN M , GE PING , OHLIGER ROBERT
IPC分类号： A61K31/551 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/55 , 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）。

6. 发明申请

WO2005012306A2 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：WO2005012306A2
公开(公告)日：2005-02-10
申请号：PCT/US2004023794
申请日：2004-07-23
申请人： NEUROGEN CORP , XIE LINGHONG , HAN BINGSONG , XU YUELIAN , MAYNARD GEORGE , CHENARD BERTRAND L , SHAW KENNETH , GAO YANG
发明人： XIE LINGHONG , HAN BINGSONG , XU YUELIAN , MAYNARD GEORGE , CHENARD BERTRAND L , SHAW KENNETH , GAO YANG
IPC分类号： C07D487/04 , C07D487/00
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，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）。

7. 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）。

8. 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。

9. 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）。

10. 发明申请

WO2006078891A3 IMIDAZOLYLMETHYL AND PYRAZOLYLMETHYL HETEROARYL DERIVATIVES 审中-公开
标题翻译：咪唑基甲基和吡唑基甲基杂芳基衍生物
公开(公告)号：WO2006078891A3
公开(公告)日：2006-08-24
申请号：PCT/US2006002017
申请日：2006-01-19
申请人： NEUROGEN CORP , HAN BINGSONG , GAO YANG , XIE LINGHONG
发明人： HAN BINGSONG , GAO YANG , XIE LINGHONG
IPC分类号： A01N43/58 , A01N43/42 , A01N43/60 , A01N43/90 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/519 , C07D237/26 , C07D237/28 , C07D471/00 , C07D471/02 , C07D487/00 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02
CPC分类号： C07D487/04 , C07D471/04 , C07D513/04
摘要： Compounds of Formula I and Formula II are provided, as are methods for their preparation. The variables Y, 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和式II的化合物，以及它们的制备方法。变量Y，Z _{1，SUB <2>，SUB <3>，_{4，_{在此定义上式中的R 6，R 7，R 8，R 8和Ar。此类化合物可用于在体内或体外调节配体与GABA受体的结合，并特别用于治疗人类，家养伴侣动物中的多种中枢神经系统（CNS）疾病和家畜。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GABA受体（例如受体定位研究）的方法。}}}

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