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1. 发明申请

WO2007101007A3 ARYL SULFONYL HETEROCYCLES 审中-公开
公开(公告)号：WO2007101007A3
公开(公告)日：2008-10-16
申请号：PCT/US2007062406
申请日：2007-02-20
申请人： NEUROGEN CORP , PETERSON JOHN M , LI GUIYING , IHLE DAVID C , HODGETTS KEVIN J , GUO QIN , GE PING , HUTCHISON ALAN J
发明人： PETERSON JOHN M , LI GUIYING , IHLE DAVID C , HODGETTS KEVIN J , GUO QIN , GE PING , HUTCHISON ALAN J
IPC分类号： A61K31/54 , A61K31/50 , C07D279/10 , C07D295/00
CPC分类号： C07D265/30 , C07D205/04 , C07D207/48 , C07D241/04 , C07D267/10 , C07D267/22 , C07D279/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04
摘要： Compounds of Formula (I) are provided in which the variables are as described herein. Such compounds may be used to modulate bradykinin receptor activity in vivo or in
摘要翻译：提供式（I）的化合物，其中变量如本文所述。这样的化合物可用于调节体内或体内的缓激肽受体活性

2. 发明申请

WO2006089076A9 THIAZOLE AMIDES, IMIDAZOLE AMIDES AND RELATED ANALOGUES 审中-公开
标题翻译：噻唑类，咪唑类和相关的类似物
公开(公告)号：WO2006089076A9
公开(公告)日：2007-04-26
申请号：PCT/US2006005562
申请日：2006-02-16
申请人： NEUROGEN CORP , 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
CPC分类号： C07D231/14 , C07D233/64 , C07D233/90 , C07D277/28 , C07D277/30 , C07D401/06 , C07D403/06 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D451/04 , C07D471/04
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).
摘要翻译：提供了噻唑酰胺，咪唑酰胺和式的相关类似物：其中变量如本文所述。这些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类，驯养的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组胺H3受体的方法（例如，受体定位研究）。

3. 发明申请

WO2005042498A3 4-AMINO (AZA) QUINOLINE DERIVATIVES AS CAPSAICIN RECEPTOR AGONISTS 审中-公开
标题翻译：作为CAPSAICIN受体激动剂的4-氨基（AZA）喹啉衍生物
公开(公告)号：WO2005042498A3
公开(公告)日：2005-07-07
申请号：PCT/US2004036295
申请日：2004-10-28
申请人： NEUROGEN CORP , BAKTHAVATCHALAM RAJAGOPAL , BLUM CHARLES A , BRIELMANN HARRY , CALDWELL TIMOTHY M , CORTRIGHT DANIEL N , HODGETTS KEVIN J , PETERSON JOHN M , ZHENG XIAOZHANG
发明人： BAKTHAVATCHALAM RAJAGOPAL , BLUM CHARLES A , BRIELMANN HARRY , CALDWELL TIMOTHY M , CORTRIGHT DANIEL N , HODGETTS KEVIN J , PETERSON JOHN M , ZHENG XIAOZHANG
IPC分类号： C07D213/56 , C07D215/44 , C07D235/14 , C07D239/94 , C07D401/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D475/04 , C07D475/06 , A61K31/4375 , A61K31/4706 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/519
CPC分类号： C04B35/632 , C07D215/44 , C07D239/94 , C07D401/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D475/06
摘要： Capsaicin receptor agonists are provided. Such compounds are ligands that may be used to modulate VRl activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to capsaicin receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供辣椒素受体激动剂。这些化合物是可用于在体内或体外调节VR1活性的配体，并且特别可用于治疗对人，驯养的伴侣动物和家畜中的辣椒素受体活化有反应的病症。还提供了用于治疗这些病症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的方法。

4. 发明申请

WO2005042498A2 CAPSAICIN RECEPTOR AGONISTS 审中-公开
标题翻译： CAPSAICIN受体激素
公开(公告)号：WO2005042498A2
公开(公告)日：2005-05-12
申请号：PCT/US2004/036295
申请日：2004-10-28
申请人： NEUROGEN CORPORATION , BAKTHAVATCHALAM, Rajagopal , BLUM, Charles, A. , BRIELMANN, Harry , CALDWELL, Timothy, M. , CORTRIGHT, Daniel, N. , HODGETTS, Kevin, J. , PETERSON, John, M. , ZHENG, Xiaozhang
发明人： BAKTHAVATCHALAM, Rajagopal , BLUM, Charles, A. , BRIELMANN, Harry , CALDWELL, Timothy, M. , CORTRIGHT, Daniel, N. , HODGETTS, Kevin, J. , PETERSON, John, M. , ZHENG, Xiaozhang
IPC分类号： C07D239/00
CPC分类号： C04B35/632 , C07D215/44 , C07D239/94 , C07D401/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D475/06
摘要： Capsaicin receptor agonists are provided. Such compounds are ligands that may be used to modulate VRl activity in vivo or in vitro , and are particularly useful in the treatment of conditions responsive to capsaicin receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供辣椒素受体激动剂。这些化合物是可用于在体内或体外调节VR1活性的配体，并且特别可用于治疗对人，驯养的伴侣动物和家畜中的辣椒素受体活化有反应的病症。还提供了用于治疗这些病症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的方法。

5. 发明申请

WO2005007087A2 SUBSTITUTED (HETEROCYCLOALKYL)METHYL AZOLE DERIVATIVES AS C5A RECEPTOR MODULATORS 审中-公开
标题翻译：作为C5A受体调节剂的取代（杂环烷基）甲基偶氮衍生物
公开(公告)号：WO2005007087A2
公开(公告)日：2005-01-27
申请号：PCT/US2004/021191
申请日：2004-06-30
申请人： NEUROGEN CORPORATION , ZHANG, Suoming , HE, Zhao , GAO, Yang , THURKAUF, Andrew , MAYNARD, George , BERTRAND, Chenard , OHLIGER, Robert , PETERSON, John, M.
发明人： ZHANG, Suoming , HE, Zhao , GAO, Yang , THURKAUF, Andrew , MAYNARD, George , BERTRAND, Chenard , OHLIGER, Robert , PETERSON, John, M.
IPC分类号： A61K
CPC分类号： C07D405/14 , C07D233/68 , C07D401/06 , C07D401/14 , C07D403/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： (Heterocycloalkyl)methyl azole derivatives of Formula (I) are provided: Formula I wherein A is oxygen, sulfur, or NR; J and K and each L are independently oxygen, sulfur, NH, or CH 2 ; and the remaining variables are defined herein. Such compounds are modulators of C5a receptors, and preferably bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. Also provided herein are pharmaceutical compositions comprising such compounds, as well as methods for using such compounds in treating a variety of inflammatory and immune system disorders.
摘要翻译：（I）的（杂环烷基）甲基唑衍生物：式I其中A是氧，硫或NR; J和K各自独立地为氧，硫，NH或CH 2; 并且其余的变量在本文中定义。这些化合物是C5a受体的调节剂，优选以高亲和力结合C5a受体，并在C5a受体上显示中性拮抗剂或反向激动剂活性。本文还提供了包含这些化合物的药物组合物，以及使用这些化合物治疗各种炎性和免疫系统疾病的方法。

6. 发明申请

WO0153298A9 IMIDAZOPYRIDINES AND RELATED AZACYCLIC DERIVATIVES AS SELECTIVE MODULATORS OF BRADYKININ B2 RECEPTORS 审中-公开
标题翻译：作为BRADYKININ B2受体的选择性调节剂的咪唑并吡啶类和相关的ZACYCLIC衍生物
公开(公告)号：WO0153298A9
公开(公告)日：2002-10-17
申请号：PCT/US0101601
申请日：2001-01-17
申请人： NEUROGEN CORP , PETERSON JOHN M , HUTCHISON ALAN , SHAW KENNETH , HODGETTS KEVIN J , MAYNARD GEORGE D , LEW RICHARD
发明人： PETERSON JOHN M , HUTCHISON ALAN , SHAW KENNETH , HODGETTS KEVIN J , MAYNARD GEORGE D , LEW RICHARD
IPC分类号： C07D471/04 , A61K31/50 , A61P29/00
CPC分类号： C07D471/04
摘要： Disclosed are compounds of formula (I) or the pharmaceutically acceptable non-toxic salts thereof wherein A, B, C, D, Y, R1, R3, R4, R5, and R6 are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthema, and rhinitis and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要翻译：公开了式（I）化合物或其药学上可接受的无毒性盐，其中A，B，C，D，Y，R 1，R 3，R 4，R 5和R 6是本文定义的变量，该化合物是缓激肽B2 受体。这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛，经皮腔内冠状动脉血管成形术，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症，青光眼，疼痛，哮喘和鼻炎的再狭窄，以及增加血脑屏障或血脑屏障的渗透性，肿瘤屏障。

7. 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.

8. 发明申请

WO0250062A2 BACKGROUND OF THE INVENTION 审中-公开
标题翻译：背景技术
公开(公告)号：WO0250062A2
公开(公告)日：2002-06-27
申请号：PCT/US0150038
申请日：2001-12-21
申请人： NEUROGEN CORP , PFIZER , 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： A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/435 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D233/20 , C07D233/54 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10 , C07D491/113
CPC分类号： C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
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 GABAA 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 GABAA receptors in tissue sections.
摘要翻译：本发明涉及苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物，所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A受体的苯并二氮杂位点的化合物。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化合物的新方法。本发明还涉及式I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。

9. 发明申请

WO1996040660A1 CERTAIN SUBSTITUTED BENZYLAMINE DERIVATIVES: A NEW CLASS OF NEUROPEPTIDE Y1 SPECIFIC LIGANDS 审中-公开
标题翻译：某些替代的苯甲酰胺衍生物：新一代神经元Y1特异性配体
公开(公告)号：WO1996040660A1
公开(公告)日：1996-12-19
申请号：PCT/US1996005843
申请日：1996-04-26
申请人： PFIZER INC. , PETERSON, John, M. , BLUM, Charles, A. , CAI, Guolin , HUTCHISON, Alan
发明人： PFIZER INC.
IPC分类号： C07D295/08
CPC分类号： C07D295/096 , C07D213/38 , C07D239/42 , C07D309/14 , C07D317/58 , C07D335/02
摘要： This invention encompasses compounds of formula (I) and the pharmaceutically acceptable salts thereof wherein Ar is an aryl group preferably selected from the group consisting of phenyl, 2-, 3-, or 4-pyridyl, 2- or 3-thienyl, 2-, 4- or 5-pyrimidyl, each of which is optionally mono- or disubstituted with halogen, hydroxy, lower alkoxy, or lower alkyl; B is sulfur, oxygen, N(R5) or C(R5)(R6); or B represents a group of formula (II) optionally substituted with halogen, hydroxy, lower alkyl or lower alkoxy; n is 1, 2, or 3; m is 2, 3, or 4; W, X, Y, and T are the same or different and represent hydrogen, halogen, hydroxy, lower alkoxy, or lower alkoxy alkoxy; R1 and R2 are the same or different and represent hydrogen, or lower alkyl; R3 and R4 are the same or different and represent hydrogen, lower alkyl, or lower alkoxy; R5 represents lower alkyl, phenyl, 2-, 3-, or 4-pyridyl, phenyl, lower alkyl, or 2-, 3-, or 4-pyridyl, lower alkyl; and A and R6 are the same or different and represent hydrogen, hydroxyl, amino, lower alkyl, lower alkoxy, phenyl, optionally substituted benzyloxy, 2-, 3-, or 4-pyridyl, phenoxy, 2-, 3-, or 4-pyridyloxy, or -(CH2)p-A'-(CH2)q-B' where p is 0-5, q is 1-5, and A' is a direct bond, oxygen or sulfur, and B' is hydrogen, lower alkyl, lower alkoxy, phenyl, 2-, 3-, or 4-pyridyl, phenoxy, 2-, 3-, or 4-pyridyloxy, carboxyl, carboalkoxy, carboxamido, mono- or dialkylcarboxamido, amino, or mono- or dialkylamino.
摘要翻译：本发明包括式（I）化合物及其药学上可接受的盐，其中Ar是优选选自苯基，2-，3-或4-吡啶基，2-或3-噻吩基，，4-或5-嘧啶基，其各自任选被卤素，羟基，低级烷氧基或低级烷基单取代或二取代; B是硫，氧，N（R 5）或C（R 5）（R 6）; 或B表示任选被卤素，羟基，低级烷基或低级烷氧基取代的式（II）的基团; n为1,2或3; m为2,3或4; W，X，Y和T相同或不同，表示氢，卤素，羟基，低级烷氧基或低级烷氧基烷氧基; R1和R2相同或不同，代表氢或低级烷基; R3和R4相同或不同，代表氢，低级烷基或低级烷氧基; R 5表示低级烷基，苯基，2-，3-或4-吡啶基，苯基，低级烷基或2-，3-或4-吡啶基低级烷基; 并且A和R6相同或不同，代表氢，羟基，氨基，低级烷基，低级烷氧基，苯基，任选取代的苄氧基，2-，3-或4-吡啶基，苯氧基，2-，3-或4- - （CH 2）p -A' - （CH 2）q B'，其中p为0-5，q为1-5，A'为直接键，氧或硫，B'为氢，低级烷基，低级烷氧基，苯基，2-，3-或4-吡啶基，苯氧基，2-，3-或4-吡啶氧基，羧基，烷氧羰基，甲酰胺基，单或二烷基羧酰胺基，氨基或单或二烷基氨基。

10. 发明申请

WO2008070014A2 BIARYL KETONE-SUBSTITUTED PIPERIDINES 审中-公开
标题翻译：二胺酮取代的哌啶
公开(公告)号：WO2008070014A2
公开(公告)日：2008-06-12
申请号：PCT/US2007/024717
申请日：2007-11-28
申请人： NEUROGEN CORPORATION , BAKTHAVATCHALM, Rajagopal , CHENARD, Bertrand, L. , CAPITOSTI, Scott, M. , HUTCHISON, Alan, J. , OHLIGER, Robert , PETERSON, John, M.
发明人： BAKTHAVATCHALM, Rajagopal , CHENARD, Bertrand, L. , CAPITOSTI, Scott, M. , HUTCHISON, Alan, J. , OHLIGER, Robert , PETERSON, John, M.
IPC分类号： A01N43/40
CPC分类号： C07D401/14 , C07D417/14 , C07D471/04 , C07D471/10
摘要： Biaryl ketone-substituted piperidines of the following Formulas are provided:, and in which the variables are as described herein. Such compounds may be used to modulate calcitonin gene-related peptide (CGRP) receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CGRP modulation in humans, domesticated companion animals and livestock animals, including headache such as migraine. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such compounds for receptor localization studies and various in vitro assays.
摘要翻译：提供以下公式的二芳基酮取代的哌啶，其中变量如本文所述。这些化合物可用于在体内或体外调节降钙素基因相关肽（CGRP）受体活性，并且特别可用于治疗对人，驯养伴侣动物和家畜的CGRP调节有反应的病症，包括头痛如偏头痛。还提供了用于治疗这些疾病的药物组合物和方法，以及使用这些化合物用于受体定位研究和各种体外测定的方法。

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