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1. 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。

2. 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。

3. 发明申请

WO2004041809A2 SUBSTITUTED IMIDAZOLYLMETHYL PYRIDINE AND PYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS 审中-公开
标题翻译：取代的咪唑基甲基吡啶和吡嗪衍生物：GABAA受体配体
公开(公告)号：WO2004041809A2
公开(公告)日：2004-05-21
申请号：PCT/US2003/014348
申请日：2003-05-07
申请人： NEUROGEN CORPORATION , XIE, Linghong , GHOSH, Manuka , MAYNARD, George
发明人： XIE, Linghong , GHOSH, Manuka , MAYNARD, George
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K45/06 , C07D403/14 , C07D417/14 , A61K2300/00
摘要： Substituted imidazolylmethyl pyridine and pyrazine 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：提供了与GABA> A <受体结合的取代的咪唑甲基吡啶和吡嗪衍生物。这样的化合物可用于调节配体结合GABA> A <受体在体内或体外，并且特别可用于治疗人类，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。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。

4. 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。

5. 发明申请

WO2003082829A1 NEW ARYL IMIDAZOLES AND RELATED COMPOUNDS AS C5A RECEPTOR MODULATORS 审中-公开
标题翻译：作为C5A受体调节剂的新ARYL咪唑和相关化合物
公开(公告)号：WO2003082829A1
公开(公告)日：2003-10-09
申请号：PCT/US2003/009938
申请日：2003-03-28
申请人： NEUROGEN CORPORATION , 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
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
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, Ar 1 , Ar 2 , R, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , 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.
摘要翻译：本发明提供了式（I）的芳基取代的咪唑，吡唑，吡啶和相关化合物，其中由式（A）表示的环系是5元杂芳基环系，其中x是0，A选自碳和杂原子氮，氧和硫，并且E和G独立地为碳或氮，条件是5元杂芳基环系不包含多于3个杂原子或多于1个氧或硫原子或6元杂芳基环系，其中x为1，A，B，E和G独立地选自碳和氮，条件是6元杂芳基环系不含3个以上的氮原子。剩余的变量Ar1，Ar2，R，R1，R2，R3，R4，R5，R6，y和z在本文中定义。这些化合物是C5a受体的配体。本发明优选的化合物作用以高亲和力结合C5a受体，在C5a受体上表现出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。它还涉及这些化合物在治疗各种炎性和免疫系统疾病中的应用。

6. 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).

7. 发明申请

WO2005080355A1 IMIDAZO-PYRIDAZINES, TRIAZOLO-PYRIDAZINES AND RELATED BENZODIAZEPINE RECEPTOR LIGANDS 审中-公开
标题翻译：咪唑并吡啶，三唑并吡啶和相关的苯二甲酸受体配体
公开(公告)号：WO2005080355A1
公开(公告)日：2005-09-01
申请号：PCT/US2005/004194
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
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 Z 1 , Z 2 , R 3 , Z 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：提供式的化合物，以及它们的制备方法。上述式中的变量Z1，Z2，R3，Z4，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）。

8. 发明申请

WO2005012306A3 IMIDAZO-PYRIMIDINES AND TRIAZOLO-PYRIMIDINES: BENZODIAZEPINE RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2005012306A3
公开(公告)日：2005-02-10
申请号：PCT/US2004/023794
申请日：2004-07-23
申请人： NEUROGEN CORPORATION , 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
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).

9. 发明申请

WO2004041808A1 4-IMIDAZOL-1-YLMETHYL-PYRIMIDINE DERIVATIVES_AS LIGANDS FOR GABAA RECEPTORS 审中-公开
标题翻译： 4-IMIDAZOL-1-YLMETHYL-PYRIMININE DERIVATIVES_AS GABAA受体配体
公开(公告)号：WO2004041808A1
公开(公告)日：2004-05-21
申请号：PCT/IB2003/004978
申请日：2003-11-04
申请人： NEUROGEN CORPORATION , XIE, Linghong , HAN, Bingsong , XU, Yuelian , MAYNARD, George
发明人： XIE, Linghong , HAN, Bingsong , XU, Yuelian , MAYNARD, George
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D403/06 , C07D417/14
摘要： The invention provides 4-imidazol-1-ylmethyl pyrimidine of the formula (I) that bind to GABA A receptors. In the above formula, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and Ar 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 composition 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）的4-咪唑-1-基甲基嘧啶。在上式中，R 1，R 2，R 3，R 4，R 5，R 6和Ar定义如下。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

WO2004031174A1 DERIVES DE IMIDAZOL-1-YLMETHYL PYRIDAZINE 审中-公开
标题翻译：衍生物咪唑-1-基甲基吡咯烷酮
公开(公告)号：WO2004031174A1
公开(公告)日：2004-04-15
申请号：PCT/IB2003/004382
申请日：2003-10-06
申请人： NEUROGEN CORPORATION , XIE, Linghong , HAN, Bingson , XU, Yuelian , MAYNARD, George
发明人： XIE, Linghong , HAN, Bingson , XU, Yuelian , MAYNARD, George
IPC分类号： C07D401/14
CPC分类号： C07D409/14 , C07D401/14 , C07D403/06 , C07D417/14
摘要： The invention provides imidazol-l-ylmethyl pyridazine derivatives of the Formula (I), that bind to GABA A receptors. In the above formula, R 1 , R 2 R 3 , R 4 , R 5 , R 6 and Ar 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）的咪唑-1-基甲基哒嗪衍生物。在上式中，R1，R2 R3，R4，R5，R6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）。

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