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1. 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。

2. 发明申请

WO2003066634A1 SUBSTITUTED FUSED PYRAZOLECARBOXYLIC ACID ARYLAMIDES AND RELATED COMPOUNDS 审中-公开
标题翻译：取代的共聚吡咯并苯甲酸和相关化合物
公开(公告)号：WO2003066634A1
公开(公告)日：2003-08-14
申请号：PCT/US2003/003872
申请日：2003-02-07
申请人： NEUROGEN CORPORATION , MAYNARD, George , YUAN, Jun , RACHWAL, Stanislaw
发明人： MAYNARD, George , YUAN, Jun , RACHWAL, Stanislaw
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07B2200/05 , C07D487/04
摘要： Heterocyclic compounds such as 3,4,5,6-tetrahydro-2,3,10-triaza-benzo[e]azulene-1-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinoline-9-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinazoline-9-carboxylic acid arylamides, 2,4,5,6-Tetrahydro-1,2,6,7-tetraaza-as-indacene-8-carboxylic acid arylamides and related compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABA A brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABA A brain receptors and are therefore useful in the treatment of anxiety, depression, sleep and seizure disorders, overdose with benzodiazepine drugs, Alzheimer's dementia, and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Intermediates useful for the synthesis of pyrazolecarboxylic acid arylamides are also provided. Compounds of the invention are also useful as probes for the localization of GABA A receptors in tissue samples.
摘要翻译：杂环化合物如3,4,5,6-四氢-2,3,10-三氮杂 - 苯并[e]薁-1-羧酸芳基酰胺，5,7-二氢-6H-吡唑并[3,4-h] 喹啉-9-羧酸芳基酰胺，5,7-二氢-6H-吡唑并[3,4-h]喹唑啉-9-羧酸芳基酰胺，2,4,5,6-四氢-1,2,6,7- 四氮杂 - 引嗪并] -8-羧酸芳基酰胺和相关化合物。这些化合物是用于GABAA脑受体的G选择性激动剂，拮抗剂或反向激动剂或GABAA脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于治疗焦虑，抑郁，睡眠和癫痫发作，用苯二氮卓类药物过量服用，阿尔茨海默病的痴呆，并增强记忆力。还提供药物组合物，包括包装的药物组合物。还提供了可用于合成吡唑甲酰芳基酰胺的中间体。本发明的化合物也可用作组织样品中GABA A受体定位的探针。

3. 发明申请

WO2000058303A1 4-SUBSTITUTED QUINOLINE DERIVATIVES AS NK-3 AND/OR GABA(A) RECEPTOR LIGANDS 审中-公开
标题翻译： 4-取代的喹啉衍生物作为NK-3和/或GABA（A）受体配体
公开(公告)号：WO2000058303A1
公开(公告)日：2000-10-05
申请号：PCT/US2000/008205
申请日：2000-03-28
申请人： NEUROGEN CORPORATION , YUAN, Jun , MAYNARD, George, D. , HUTCHISON, Alan , RACHWAL, Stanislaw
发明人： YUAN, Jun , MAYNARD, George, D. , HUTCHISON, Alan , RACHWAL, Stanislaw
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D413/04 , C07D487/04 , G01N33/9426 , G01N2333/70571
摘要： The invention relates to certain novel compounds of general Formula (I) where R 1 , R 2 , R 3 , R 4 , X, Y 1 , and Y 2 are defined herein. These compounds bind with high affinity to NK-3 receptors and/or GABA A receptors. Also provided are pharmaceutical compositions comprising them, and methods of treating patients suffering from certain central nervous system and peripheral diseases or disorders with these pharmaceutical compositions. This invention also relates to the use of such compounds in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. The compounds of this invention are also useful as probes for the localization of NK-3 receptors and GABA A receptors.
摘要翻译：本发明涉及通式（I）的某些新化合物，其中R 1，R 2，R 3，R 4，X，Y 1和Y 2在本文中定义。这些化合物以高亲和力结合NK-3受体和/或GABA A受体。还提供了包含它们的药物组合物，以及用这些药物组合物治疗患有某些中枢神经系统和外周疾病或病症的患者的方法。本发明还涉及这样的化合物与一种或多种其它CNS剂组合用于增强其它CNS剂的作用的用途。本发明的化合物也可用作NK-3受体和GABA A受体定位的探针。

4. 发明申请

WO2003006471A1 HETEROARYL SUBSTITUTED FUSED BICYCLIC HETEROARYL COMPOUNDS AS GABAA RECEPTOR LIGANDS 审中-公开
标题翻译：作为GABAA受体配体的HETEROARYL取代的双熔体杂环化合物
公开(公告)号：WO2003006471A1
公开(公告)日：2003-01-23
申请号：PCT/US2002/022130
申请日：2002-07-12
申请人： NEUROGEN CORPORATION , HUTCHISON, Alan , MAYNARD, George , ALBAUGH, Pamela , XIE, Linghong , YUAN, Jun , MITCHELL, Scott , SINGH, Vinod , GHOSH, Manuka , LI, Guiying , LIU, Nian
发明人： HUTCHISON, Alan , MAYNARD, George , ALBAUGH, Pamela , XIE, Linghong , YUAN, Jun , MITCHELL, Scott , SINGH, Vinod , GHOSH, Manuka , LI, Guiying , LIU, Nian
IPC分类号： C07D513/04
CPC分类号： C07D487/04 , C07D471/04 , C07D513/04
摘要： This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: The invention is particularly relates to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABA A receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABA A receptors in tissue sections.
摘要翻译：本发明涉及可以由式I或式II描述的杂芳基取代的稠合双环杂芳基化合物，例如杂芳基取代的咪唑并吡啶，咪唑并吡嗪，咪唑并吡啶，咪唑并吡啶和咪唑并噻唑。本发明特别涉及以高选择性结合的这类化合物并且对GABA A受体的苯并二氮杂位点具有高亲和力。本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统（CNS）疾病中的用途。公开了制备式I和式II化合物的方法。本发明还涉及式I或式II的苯并咪唑，吡啶基咪唑和相关双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。此外，本发明涉及使用这些化合物作为组织切片中GABA A受体定位的探针。

5. 发明申请

WO2003097643A1 SUBSTITUTED RING-FUSED IMIDAZOLE DERIVATES: GABAA RECEPTOR LIGANDS 审中-公开
标题翻译：取代环状咪唑衍生物：GABAA受体配体
公开(公告)号：WO2003097643A1
公开(公告)日：2003-11-27
申请号：PCT/US2003/015578
申请日：2003-05-15
申请人： NEUROGEN CORPORATION , MAYNARD, George, D. , YUAN, Jun , LUKE, George, P. , CURRIE, Kevin
发明人： MAYNARD, George, D. , YUAN, Jun , LUKE, George, P. , CURRIE, Kevin
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： (Formula I). Substituted ring-fused imidazole derivatives that bind to GABA A receptors are provided. 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：（式I）。提供了与GABA A受体结合的取代的环稠合的咪唑衍生物。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）。

6. 发明申请

WO2006113704A2 SUBTITUTED HETEROARYL CB1 ANTAGONISTS 审中-公开
标题翻译：受体异常CB1拮抗剂
公开(公告)号：WO2006113704A2
公开(公告)日：2006-10-26
申请号：PCT/US2006/014548
申请日：2006-04-18
申请人： NEUROGEN CORPORATION , YUAN, Jun , GUO, Qin , ZHAO, He , HU, Shaojing , WHITEHOUSE, Darren , FRINGLE, Wallace , MAO, Jianmin , MAYNARD, George , HAMMER, Jack , WUSTROW, David , LI, Hongbin
发明人： YUAN, Jun , GUO, Qin , ZHAO, He , HU, Shaojing , WHITEHOUSE, Darren , FRINGLE, Wallace , MAO, Jianmin , MAYNARD, George , HAMMER, Jack , WUSTROW, David , LI, Hongbin
IPC分类号： C07D401/04 , C07D403/04 , C07D401/14 , C07D417/14 , C07D403/14 , C07D413/14 , C07D405/12 , C07D401/12 , C07D403/12 , C07D417/04 , A61K31/497 , A61K31/53
CPC分类号： C07D403/14 , C07D213/28 , C07D213/61 , C07D213/74 , C07D239/42 , C07D239/54 , C07D241/12 , C07D241/20 , C07D241/24 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CBl activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CBl 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 Iigands 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。这种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类，家养伴侣动物和家畜动物中的CB1调节有反应的病症，包括食欲障碍，肥胖症和成瘾性疾病。还提供了使用它们治疗这种病症的药物组合物和方法，以及使用这些液体用于受体定位研究和各种体外测定的方法。

7. 发明申请

WO2004043925A2 3-SUBSTITUTED-6-ARYL PYRIDINES 审中-公开
标题翻译： 3-取代的6-芳基吡啶
公开(公告)号：WO2004043925A2
公开(公告)日：2004-05-27
申请号：PCT/US2003/035694
申请日：2003-11-07
申请人： NEUROGEN CORPORATION , HUTCHISON, Alan , YUAN, Jun , LEE, Kyungae , MAYNARD, George , CHENARD, Bertrand, L. , LIU, Nian , GUO, Qin , GUO, Zihong , HRNCIAR, Peter
发明人： HUTCHISON, Alan , YUAN, Jun , LEE, Kyungae , MAYNARD, George , CHENARD, Bertrand, L. , LIU, Nian , GUO, Qin , GUO, Zihong , HRNCIAR, Peter
IPC分类号： C07D213/00
CPC分类号： C07D213/30 , C07B2200/05 , C07D213/38 , C07D213/42 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/84 , C07D213/89 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C40B40/00
摘要： 3-substituted-6-aryl pyridines of Formula (I) are provided: Formula (I) wherein R 1 , R 2 , R 3 , R 8 , R 9 , A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula (I) bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式（I）的3-取代-6-芳基吡啶：式（I）其中R 1，R 2，R 3，R 8，R 9，A和Ar如本文所定义。这些化合物是C5a受体的配体。优选的式（I）化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供标记的3-取代-6-芳基吡啶，其可用作C5a受体定位的探针。

8. 发明申请

WO2002050062A3 BENZIMIDAZOLE AND PYRIDYLIMIDAZOLE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
公开(公告)号：WO2002050062A3
公开(公告)日：2002-06-27
申请号：PCT/US2001/050038
申请日：2001-12-21
申请人： NEUROGEN CORPORATION , PFIZER INC. , LI, Guiying , PETERSON, John, M. , ALBAUGH, Pamela , CURRIE, Kevin, S. , CAI, Guolin , GUSTAVSON, Linda, M. , LEE, Kyungae , HUTCHISON, Alan , SINGH, Vinod , MAYNARD, George, D. , YUAN, Jun , LING HONG, Xie , GHOSH, Manuka , LIU, Nian , LUKE, George, P. , MITCHELL, Scott , ALLEN, Martin, Patrick , LIRAS, Spiros
发明人： LI, Guiying , PETERSON, John, M. , ALBAUGH, Pamela , CURRIE, Kevin, S. , CAI, Guolin , GUSTAVSON, Linda, M. , LEE, Kyungae , HUTCHISON, Alan , SINGH, Vinod , MAYNARD, George, D. , YUAN, Jun , LING HONG, Xie , GHOSH, Manuka , LIU, Nian , LUKE, George, P. , MITCHELL, Scott , ALLEN, Martin, Patrick , LIRAS, Spiros
IPC分类号： C07D401/14
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula (I). The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABA A receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABA A receptors in tissue sections.

9. 发明申请

WO2006042102A2 PYRROLO-PYRIDINE, PYRROLO-PYRIMIDINE AND RELATED HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：吡咯并吡啶，吡咯并吡啶和相关杂环化合物
公开(公告)号：WO2006042102A2
公开(公告)日：2006-04-20
申请号：PCT/US2005/036126
申请日：2005-10-05
申请人： NEUROGEN CORPORATION , YUAN, Jun , HRNCIAR, Peter , GUO, Qin , MAYNARD, George, D.
发明人： YUAN, Jun , HRNCIAR, Peter , GUO, Qin , MAYNARD, George, D.
IPC分类号： A61K31/519 , A61K31/4745
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R 2 , R 5 , E, Z 1 , Z 3 , Z 4 , and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R'

10. 发明申请

WO2005110991A1 1-ARYL-4-SUBSTITUTED ISOQUINOLINES 审中-公开
标题翻译： 1-ARYL-4取代的异喹啉
公开(公告)号：WO2005110991A1
公开(公告)日：2005-11-24
申请号：PCT/US2005/015959
申请日：2005-05-06
申请人： NEUROGEN CORPORATION , LEE, Kyungae , YUAN, Jun , MAYNARD, George, D. , HUTCHISON, Alan , MITCHELL, Scott
发明人： LEE, Kyungae , YUAN, Jun , MAYNARD, George, D. , HUTCHISON, Alan , MITCHELL, Scott
IPC分类号： C07D217/02
CPC分类号： C07D405/12 , A61K31/47 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/14 , C07D413/14
摘要： 1-Aryl-4-substituted isoquinolines analogues of Formula (I) and Formula (II) are provided, as follows : wherein R 1 , R 2 , R 3 , R 8 , R 9 , A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula (I) and (II) bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 1-aryl-4-substituted isoquinolines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式（I）和式（II）的1-芳基-4-取代的异喹啉类似物，如下所述：其中R1，R2，R3，R8，R9，A和Ar如本文所定义。这些化合物是C5a受体的配体。式（I）和（II）的优选化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供标记的1-芳基-4-取代的异喹啉，其可用作C5a受体定位的探针。

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