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1. 发明申请

WO2008024433A3 HALOALKYL-SUBSTITUTED PYRIMIDINONE DERIVATIVES 审中-公开
公开(公告)号：WO2008024433A3
公开(公告)日：2008-02-28
申请号：PCT/US2007/018635
申请日：2007-08-22
申请人： NEUROGEN CORPORATION , BLUM, Charles, A. , ZHENG, Xiaozhang , MARTINEZ, Isamir , CHENARD, Bertrand, L.
发明人： BLUM, Charles, A. , ZHENG, Xiaozhang , MARTINEZ, Isamir , CHENARD, Bertrand, L.
IPC分类号： C07D487/04 , C07D471/04 , C07D473/30 , C07D513/04 , C07D495/04 , A61K31/522 , A61K31/519 , A61P23/00 , A61P11/14 , A61P13/10 , A61P17/04
摘要： Haloalkyl-substituted pyrimidinone derivatives are provided, of the Formula (I): wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

2. 发明申请

WO2006093911A3 THIAZOLYLMETHYL AND OXAZOLYLMETHYL HETEROARYL DERIVATIVES 审中-公开
公开(公告)号：WO2006093911A3
公开(公告)日：2006-09-08
申请号：PCT/US2006/006937
申请日：2006-02-28
申请人： NEUROGEN CORPORATION , XU, Yuelian , XIE, Linghong
发明人： XU, Yuelian , XIE, Linghong
IPC分类号： C07D417/08 , C07D413/08 , C07D487/04 , A61K51/04 , C07D419/08
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).

3. 发明申请

WO2007133820A3 DIARYL TRIAZOLONES AS CB1 ANTAGONISTS 审中-公开
公开(公告)号：WO2007133820A3
公开(公告)日：2007-11-22
申请号：PCT/US2007/060599
申请日：2007-01-17
申请人： NEUROGEN CORPORATION , HUTCHISON, Alan, J. , MAO, Jianmin , MAYNARD, George D. , PRINGLE, Wallace, C. , ZHAO, He , WUSTROW, David, J.
发明人： HUTCHISON, Alan, J. , MAO, Jianmin , MAYNARD, George D. , PRINGLE, Wallace, C. , ZHAO, He , WUSTROW, David, J.
IPC分类号： A61K31/41 , C07D249/08
摘要： Diaryl triazolones of Formula I are provided, in which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using diaryl traizolones of Formula I to treat such disorders are provided, as are methods for using such compounds as ligands for receptor localization studies and various in vitro assays.

4. 发明申请

WO2007016496A3 DIPIPERAZINYL KETONES AND RELATED ANALOGUES 审中-公开
公开(公告)号：WO2007016496A3
公开(公告)日：2007-02-08
申请号：PCT/US2006/029761
申请日：2006-07-28
申请人： NEUROGEN CORPORATION , 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： C07D241/04 , C07D295/00
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).

5. 发明申请

WO2006089076A3 THIAZOLE AMIDES, IMIDAZOLE AMIDES AND RELATED ANALOGUES 审中-公开
公开(公告)号：WO2006089076A3
公开(公告)日：2006-08-24
申请号：PCT/US2006/005562
申请日：2006-02-16
申请人： NEUROGEN CORPORATION , PRINGLE, Wallace C. , PETERSON, John M. , XIE, Linghong , GE, Ping , GAO, Yang , OCHTERSKI, Joseph W. , LAN, Jiong
发明人： PRINGLE, Wallace C. , PETERSON, John M. , XIE, Linghong , GE, Ping , GAO, Yang , OCHTERSKI, Joseph W. , LAN, Jiong
IPC分类号： A61K31/426 , C07D277/24 , C07D277/28
摘要： Thiazole amides, imidazole amides 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).

6. 发明申请

WO2006078891A2 IMIDAZOLYLMETHYL AND PYRAZOLYLMETHYL HETEROARYL DERIVATIVES 审中-公开
标题翻译：咪唑并咪唑衍生物和吡唑并咪唑衍生物
公开(公告)号：WO2006078891A2
公开(公告)日：2006-07-27
申请号：PCT/US2006/002017
申请日：2006-01-19
申请人： NEUROGEN CORPORATION , HAN, Bingsong , GAO, Yang , XIE, Linghong
发明人： HAN, Bingsong , GAO, Yang , XIE, Linghong
IPC分类号： A61K31/503
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，以及其制备方法。变量Y，Z 1，Z 2，Z 3，R 4，R 5，上述式中R 6，R 6，R 7，R 8和Ar定义如上。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。

7. 发明申请

WO2006052542A3 ARYLALKYL UREAS AS CB1 ANTAGONISTS 审中-公开
公开(公告)号：WO2006052542A3
公开(公告)日：2006-05-18
申请号：PCT/US2005/039474
申请日：2005-11-01
申请人： NEUROGEN CORPORATION , HUTCHISON, Alan, J. , YUAN, Jun
发明人： HUTCHISON, Alan, J. , YUAN, Jun
IPC分类号： C07C273/00 , C07C275/00
摘要： CB1 antagonists are provided. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 receptor modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.

8. 发明申请

WO2006049941A2 DIARYL UREAS AS CB1 ANTAGONISTS 审中-公开
标题翻译： DIARYL UREAS作为CB1 ANTAGONISTS
公开(公告)号：WO2006049941A2
公开(公告)日：2006-05-11
申请号：PCT/US2005/038316
申请日：2005-10-24
申请人： NEUROGEN CORPORATION , HUTCHISON, Alan J. , YUAN, Jun
发明人： HUTCHISON, Alan J. , YUAN, Jun
IPC分类号： A61K31/17
CPC分类号： A61K31/17 , C07C275/34 , C07C275/42 , C07C311/05 , C07C2602/08 , C07D213/64 , C07D213/75 , C07D231/12 , C07D239/26 , C07D239/42 , C07D241/12 , C07D261/08 , C07D263/32 , C07D265/30 , C07D277/28 , C07D295/135
摘要： Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.
摘要翻译：提供式I化合物。其中变量如本文所述。这些化合物可用于体内或体外调节CB1活性，并且特别可用于治疗对人，家养伴侣动物和家畜中的CB1调节有反应的病症，包括食欲障碍，肥胖症和成瘾性疾病。还提供了用于治疗这些疾病的药物组合物和方法，以及使用这些配体进行受体定位研究和各种体外测定的方法。

9. 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）。

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