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公开(公告)号：US20070027155A1
公开(公告)日：2007-02-01
申请号：US10893799
申请日：2004-07-16
申请人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Bertrand Chenard , Stephane De Lombaert , Kevin Hodgetts , Alan Hutchison , Taeyoung Yoon , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Bertrand Chenard , Stephane De Lombaert , Kevin Hodgetts , Alan Hutchison , Taeyoung Yoon , Xiaozhang Zheng
IPC分类号： A61K31/53 , A61K31/506 , C07D43/14
CPC分类号： C04B35/632 , A61K31/496 , A61K31/506 , A61K31/53 , A61K31/5377 , C07D251/48 , C07D401/12 , C07D401/14 , C07D403/14 , C07D413/14
摘要： Biaryl piperazinyl-pyridine analogues are provided, of the Formula: 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.
摘要翻译： 提供了下式的双芳基哌嗪基 - 吡啶类似物：其中变量如本文所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种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。
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公开(公告)号：US20060194805A1
公开(公告)日：2006-08-31
申请号：US11412526
申请日：2006-04-26
申请人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Timothy Caldwell , Daniel Cortright , Kevin Hodgetts , John Peterson , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Timothy Caldwell , Daniel Cortright , Kevin Hodgetts , John Peterson , Xiaozhang Zheng
IPC分类号： A61K31/525 , A61K31/517 , A61K31/519 , A61K31/498 , C07D475/10 , C07D487/02
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 VR1 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。 这样的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激活有反应的病症。 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。
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![Spiro[isobenzofuran-1,4'-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4'-piperidines](/abs-image/US/2006/02/23/US20060040964A1/abs.jpg.150x150.jpg)
23.发明申请公开(公告)号：US20060040964A1
公开(公告)日：2006-02-23
申请号：US11183615
申请日：2005-07-18
申请人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , James Darrow , Stephane De Lombaert , Alan Hutchison , Jennifer Tran , Xiaozhang Zheng , Richard Elliott , Marlys Hammond
发明人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , James Darrow , Stephane De Lombaert , Alan Hutchison , Jennifer Tran , Xiaozhang Zheng , Richard Elliott , Marlys Hammond
IPC分类号： A61K31/519 , A61K31/4747 , C07D491/10
CPC分类号： C07D487/04 , C07D491/10
摘要： Substituted spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines capable of modulating NPY5 receptor activity are provided. Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.
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24.发明授权Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone(CRH) antagonists, useful for treating CNS and stress-related disorders 有权杂环取代的环稠合吡啶和嘧啶作为促肾上腺皮质激素释放激素（CRH）拮抗剂，用于治疗CNS和应激相关疾病公开(公告)号：US06245769B1
公开(公告)日：2001-06-12
申请号：US09145231
申请日：1998-09-01
IPC分类号： A61K314192
CPC分类号： C07D471/04 , C07D487/04
摘要： Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
摘要翻译： 式（I）的促肾上腺皮质激素释放因子（CRF）拮抗剂及其用于治疗精神疾病和神经系统疾病，焦虑相关疾病，创伤后应激障碍，核上性麻痹和进食障碍以及免疫学，心血管或心脏的治疗 与哺乳动物精神病理障碍和压力相关的疾病和结肠超敏反应。
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25.发明申请Use of capsaicin receptor antagonists to treat symptoms of tear gas exposure 审中-公开使用辣椒素受体拮抗剂治疗催泪瓦斯暴露症状公开(公告)号：US20090082362A1
公开(公告)日：2009-03-26
申请号：US12057808
申请日：2008-03-28
申请人： Rajagopal Bakthavatchalam , Alan Hutchison , Robert W. DeSimone , Kevin J. Hodgetts , James E. Krause , Geoffrey G. White
发明人： Rajagopal Bakthavatchalam , Alan Hutchison , Robert W. DeSimone , Kevin J. Hodgetts , James E. Krause , Geoffrey G. White
IPC分类号： A61K31/496 , A61P29/00 , A61P11/00
CPC分类号： C07D213/74 , C07D213/75 , C07D217/22 , C07D241/20 , C07D405/12 , C07D417/12
摘要： Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.
摘要翻译： 公开了二芳基哌嗪和相关化合物。 这些化合物是辣椒素受体的选择性调节剂，包括人类辣椒素受体，因此可用于治疗慢性和急性疼痛病症，瘙痒和尿失禁。 还提供了治疗这种疾病以及包装的药物组合物的方法。 本发明的化合物也可用作辣椒素受体定位的探针，也可用作辣椒素受体结合和辣椒素受体介导的阳离子电导测定中的标准。 给出了在受体定位研究中使用化合物的方法。
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26.发明授权Carboxylic acid, phosphate or phosphonate substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators 失效羧酸，磷酸酯或膦酸酯取代的喹唑啉-4-基胺类似物作为辣椒素受体调节剂公开(公告)号：US07432275B2
公开(公告)日：2008-10-07
申请号：US10539031
申请日：2003-12-12
申请人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry Brielmann , Timothy M. Caldwell , Stéphane DeLombaert , Kevin J. Hodgetts , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry Brielmann , Timothy M. Caldwell , Stéphane DeLombaert , Kevin J. Hodgetts , Xiaozhang Zheng
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72
CPC分类号： C07D417/14 , C07D239/94 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D491/10 , C07F9/65128 , C07F9/65583 , C07F9/6561
摘要： Acid-substituted quinazolin-4-ylamine analogues are provided. 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译： 提供了酸取代的喹唑啉-4-基胺类似物。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 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。
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27.发明授权Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues 失效取代的（7-吡啶基-4-苯基氨基 - 喹唑啉-2-基） - 甲醇类似物公开(公告)号：US07329664B2
公开(公告)日：2008-02-12
申请号：US10892741
申请日：2004-07-16
申请人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry Brielmann , Stéphane De Lombaert , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry Brielmann , Stéphane De Lombaert , Xiaozhang Zheng
IPC分类号： A61K31/517 , A61K31/519 , C07D401/04 , C07D405/14 , C07D487/04
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14
摘要： Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies
摘要翻译： 提供了取代的（7-吡啶基-4-苯基氨基 - 喹唑啉-2-基） - 甲醇类似物。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 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
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公开(公告)号：US20080015183A1
公开(公告)日：2008-01-17
申请号：US11864987
申请日：2007-09-29
申请人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Timothy Caldwell , Stephane De Lombaert , Kevin Hodgetts , Xiaozhang Zheng , James Krause , Uri Herzberg , Taeyoung Yoon
发明人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Timothy Caldwell , Stephane De Lombaert , Kevin Hodgetts , Xiaozhang Zheng , James Krause , Uri Herzberg , Taeyoung Yoon
IPC分类号： A61K31/517 , A61K31/47 , A61K31/519 , A61K31/541 , A61P11/14 , A61P17/02 , C07D215/58 , C07D237/30 , C07D279/12 , C07D471/04 , C07D417/12 , C07D413/14 , C07D413/10 , C07D401/14 , C07D401/10 , C07D239/84 , C07D223/04 , A61P25/04 , A61P11/16 , A61K31/55 , A61K31/5377 , A61K31/502
CPC分类号： C07D401/04 , C07D215/42 , C07D215/44 , C07D237/34 , C07D239/94 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , C07D419/14 , C07D471/04
摘要： Substituted quinazolin-4-ylamine analogues are provided. 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译： 提供了取代的喹唑啉-4-基胺类似物。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 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。
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公开(公告)号：US07304059B2
公开(公告)日：2007-12-04
申请号：US11345926
申请日：2006-02-01
申请人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry Brielmann , Timothy M. Caldwell , Stéphane De Lombaert , Kevin J. Hodgetts , Xiaozhang Zheng , Taeyoung Yoon
发明人： Rajagopal Bakthavatchalam , Charles A. Blum , Harry Brielmann , Timothy M. Caldwell , Stéphane De Lombaert , Kevin J. Hodgetts , Xiaozhang Zheng , Taeyoung Yoon
IPC分类号： C07D403/12 , C07D403/14 , A61K31/517
CPC分类号： C07D401/04 , C07D215/42 , C07D215/44 , C07D237/34 , C07D239/94 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , C07D419/14 , C07D471/04
摘要： Substituted quinazolin-4-ylamine analogues are provided. 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译： 提供了取代的喹唑啉-4-基胺类似物。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 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。
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30.发明申请Carboxylic acid, phosphate or phosphonate substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators 失效羧酸，磷酸酯或膦酸酯取代的喹唑啉-4-基胺类似物作为辣椒素受体调节剂公开(公告)号：US20060089354A1
公开(公告)日：2006-04-27
申请号：US10539031
申请日：2003-12-12
申请人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Timothy Caldwell , Stephane DeLombaert , Kevin Hodgetts , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Timothy Caldwell , Stephane DeLombaert , Kevin Hodgetts , Xiaozhang Zheng
IPC分类号： A61K31/5377 , A61K31/519 , A61K31/4745 , A61K31/4709 , C07D487/02 , C07D413/02 , C07D401/02 , C07D471/02
CPC分类号： C07D417/14 , C07D239/94 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D491/10 , C07F9/65128 , C07F9/65583 , C07F9/6561
摘要： Acid-substituted quinazolin-4-ylamine analogues are provided. 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 them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译： 提供了酸取代的喹唑啉-4-基胺类似物。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 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。
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