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).

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。

公开(公告)号：EP1909797A2

公开(公告)日：2008-04-16

申请号：EP06788999.8

申请日：2006-07-28

申请人： NEUROGEN CORPORATION

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 ,  A61K31/55 ,  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).

公开(公告)号：EP1838152A2

公开(公告)日：2007-10-03

申请号：EP06718998.5

申请日：2006-01-19

申请人： NEUROGEN CORPORATION

发明人： HAN, Bingsong ,  GAO, Yang ,  XIE, Linghong

IPC分类号： A01N43/58 ,  A01N43/60 ,  A01N43/90 ,  A01N43/42 ,  A61K31/50 ,  A61K31/495 ,  A61K31/519 ,  A61K31/44 ,  C07D237/26 ,  C07D237/28 ,  C07D487/00 ,  C07D471/00 ,  C07D471/02 ,  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, 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).

公开(公告)号：EP1807417A2

公开(公告)日：2007-07-18

申请号：EP05825135.6

申请日：2005-11-01

申请人： NEUROGEN CORPORATION

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 ,  C07D403/14 ,  C07D231/28

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 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).

公开(公告)号：EP1648899A2

公开(公告)日：2006-04-26

申请号：EP04779031.6

申请日：2004-07-23

申请人： NEUROGEN CORPORATION

发明人： XIE, Linghong ,  HAN, Bingsong ,  XU, Yuelian ,  MAYNARD, George ,  CHENARD, Bertrand, L. ,  SHAW, Kenneth ,  GAO, Yang

IPC分类号： C07D487/04

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).

公开(公告)号：EP1594848A1

公开(公告)日：2005-11-16

申请号：EP04711415.2

申请日：2004-02-16

申请人： NEUROGEN CORPORATION

发明人： XIE, Linghong ,  HAN, Bingsong ,  XU, Yuelian

IPC分类号： C07D237/16 ,  C07D487/04 ,  C07D237/08 ,  C07D213/69 ,  C07D239/26 ,  C07D401/12 ,  A61K31/50 ,  A61P25/00

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： 本发明提供了结合GABAA受体的式（I）化合物。 在上面的公式中，变量是在这里定义的。 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。

公开(公告)号：EP1490343A1

公开(公告)日：2004-12-29

申请号：EP03726169.0

申请日：2003-03-28

申请人： Neurogen Corporation

发明人： LUKE, George, P. ,  MAYNARD, George ,  MITCHELL, Scott ,  THURKAUF, Andrew ,  XIE, Linghong ,  ZHANG, LuYan ,  ZHANG, Suoming ,  ZHAO, He ,  CHENARD, Bertrand, L. ,  GAO, Yang ,  HAN, Bingsong ,  HE, Xiao, Shu

IPC分类号： C07D233/54 ,  A61K31/4164

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 (I) where the ring system represented by Formula (A) 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.

公开(公告)号：EP1998620B1

公开(公告)日：2011-01-12

申请号：EP07752458.5

申请日：2007-03-08

申请人： Neurogen Corporation

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).

公开(公告)号：EP1648899B1

公开(公告)日：2007-01-03

申请号：EP04779031.6

申请日：2004-07-23

申请人： NEUROGEN CORPORATION

发明人： XIE, Linghong ,  HAN, Bingsong ,  XU, Yuelian ,  MAYNARD, George ,  CHENARD, Bertrand, L. ,  SHAW, Kenneth ,  GAO, Yang

IPC分类号： C07D487/04

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).