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公开(公告)号：US20120208829A1
公开(公告)日：2012-08-16
申请号：US13215195
申请日：2011-08-22
申请人： Rajagopal Bakthavatchalam , Scott M. Capitosti , Jianjun Xu , Bertrand L. Chenard , Manuka Ghosh , Charles A. Blum
发明人： Rajagopal Bakthavatchalam , Scott M. Capitosti , Jianjun Xu , Bertrand L. Chenard , Manuka Ghosh , Charles A. Blum
IPC分类号： A61K31/522 , C07D471/04 , C07D513/04 , C07D495/04 , A61K31/519 , A61P11/14 , A61P17/04 , A61P11/00 , A61P15/12 , A61P13/00 , A61P13/10 , C07D473/04 , A61P29/00
CPC分类号： C07D473/30 , C07D471/04 , C07D513/04
摘要： 2-Phenoxy pyrimidinone 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2-苯氧基嘧啶酮类似物，其具有如下所述的变体： 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：US20090286767A1
公开(公告)日：2009-11-19
申请号：US12368302
申请日：2009-02-09
申请人： Rajagopal Bakthavatchalam , Timothy M. Caldwell , Bertrand L. Chenard , Stéphane De Lombaert , Kevin J. Hodgetts
发明人： Rajagopal Bakthavatchalam , Timothy M. Caldwell , Bertrand L. Chenard , Stéphane De Lombaert , Kevin J. Hodgetts
IPC分类号： A61K31/397 , C12N5/00 , A61K31/5377 , A61K31/501 , A61K31/497 , A61K31/506 , A61K31/4375 , A61K31/4709 , C07D413/14 , C07D405/14 , C07D401/14 , C07D401/10 , A61P3/04 , A61P29/00
CPC分类号： C07D401/04 , C07D215/44 , C07D471/04 , C07D491/14
摘要： Substituted quinolin-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： 提供取代的喹啉-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：US07488740B2
公开(公告)日：2009-02-10
申请号：US10891832
申请日：2004-07-14
申请人： Rajagopal Bakthavatchalam , Timothy M. Caldwell , Bertrand L. Chenard , Stéphane De Lombaert , Kevin J. Hodgetts
发明人： Rajagopal Bakthavatchalam , Timothy M. Caldwell , Bertrand L. Chenard , Stéphane De Lombaert , Kevin J. Hodgetts
IPC分类号： A61K31/47 , C07D215/38
CPC分类号： C07D401/04 , C07D215/44 , C07D471/04 , C07D491/14
摘要： Substituted quinolin-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： 提供取代的喹啉-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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4.发明授权Melanin concentrating hormone receptor ligands: substituted benzoimidazole analogues 失效黑色素浓缩激素受体配体：取代的苯并咪唑类似物公开(公告)号：US06906075B2
公开(公告)日：2005-06-14
申请号：US10339111
申请日：2003-01-09
申请人： Robert W. DeSimone , Cheryl Steenstra , Linda Gustavson , Rajagopal Bakthavatchalam , Alan Hutchison
发明人： Robert W. DeSimone , Cheryl Steenstra , Linda Gustavson , Rajagopal Bakthavatchalam , Alan Hutchison
IPC分类号： A61K31/4184 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/55 , A61P1/14 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P15/00 , A61P43/00 , C07D235/10 , C07D235/14 , C07D401/04 , C07D403/04 , C07D403/10 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04 , C07D513/04 , C07D521/00 , C07D401/10 , A61K31/445 , A61K31/495
CPC分类号： C07D231/12 , C07D233/56 , C07D235/14 , C07D249/08 , C07D401/04 , C07D403/04 , C07D403/10 , C07D409/12 , C07D409/14 , C07D417/12 , C07D513/04
摘要： Melanin concentrating hormone receptor ligands (especially substituted benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要翻译： 提供能够调节MCH受体活性的黑色素浓缩激素受体配体（特别是取代的苯并咪唑类似物）。 这样的配体可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗人，驯养的伴侣动物和家畜中的各种代谢，喂养和性障碍。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。
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公开(公告)号：US06569861B2
公开(公告)日：2003-05-27
申请号：US09900679
申请日：2001-07-06
IPC分类号： A61K31495
CPC分类号： C07D295/096
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.
摘要翻译： 公开了下式的化合物及其药学上可接受的盐，其中Q，X，Y，Z和R 1 R 9和R 12 -R 19如本文所定义。这些化合物是MCH 1受体的选择性调节剂，因此其可用于 治疗各种代谢，喂养和性功能障碍。 还公开了治疗这种病症以及包装的药物组合物的方法。
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6.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，可用于治疗cns和应激相关疾病公开(公告)号：US06525056B2
公开(公告)日：2003-02-25
申请号：US09789673
申请日：2001-02-21
IPC分类号： C07D47104
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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公开(公告)号：US08759361B2
公开(公告)日：2014-06-24
申请号：US13215195
申请日：2011-08-22
申请人： Rajagopal Bakthavatchalam , Scott M. Capitosti , Jianjun Xu , Bertrand L. Chenard , Manuka Ghosh , Charles A. Blum
发明人： Rajagopal Bakthavatchalam , Scott M. Capitosti , Jianjun Xu , Bertrand L. Chenard , Manuka Ghosh , Charles A. Blum
IPC分类号： A61K31/522 , A61P25/04 , A61P17/04 , A61P13/10 , C07D473/04 , C07D495/04 , C07D487/04 , A61K31/519
CPC分类号： C07D473/30 , C07D471/04 , C07D513/04
摘要： 2-Phenoxy pyrimidinone 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2-苯氧基嘧啶酮类似物，其具有如下所述的变体： 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：US20120190680A1
公开(公告)日：2012-07-26
申请号：US12672413
申请日：2008-08-11
IPC分类号： A61K31/506 , C07D401/14 , C07D413/14 , C07D209/42 , C07D403/06 , A61K31/4439 , A61K31/5377 , A61K31/404 , A61K31/497 , A61K31/444 , A61K31/4178 , A61P29/00 , A61P25/00 , A61P9/00 , A61P27/02 , A61P19/02 , A61P9/10 , A61P1/00 , A61P25/28 , A61P11/06 , A61P11/00 , A61P25/24 , A61P25/22 , A61P25/18 , A61P25/08 , C07D403/04
摘要： Compounds, pharmaceutical compositions, and methods of use are disclosed for heteroaryl amide analogues of formula Ia and/or Ib: In certain embodiments, the heteroaryl amide analogues are agonists and/or ligands of dopamine receptors and may be useful, inter alia, for the treatment of a condition responsive to P2X7 receptor modulation, for example, pain, inflammation, a neurological or neurodegenerative disorder, a cardiovascular disorder, an ocular disorder or an immune system disorder.
摘要翻译： 公开了式Ia和/或Ib的杂芳基酰胺类似物的化合物，药物组合物和使用方法：在某些实施方案中，杂芳基酰胺类似物是多巴胺受体的激动剂和/或配体，并且特别可用于 治疗响应于P2X7受体调节的病症，例如疼痛，炎症，神经性或神经变性疾病，心血管疾病，眼病或免疫系统疾病。
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公开(公告)号：US20100292236A1
公开(公告)日：2010-11-18
申请号：US12669308
申请日：2008-07-21
申请人： Hongbin Li , Jun Yuan , Rajagopal Bakthavatchalam , Kevin J. Hodgetts , Scott M. Capitosti , Jianmin Mao , David J. Wustrow , Qin Guo
发明人： Hongbin Li , Jun Yuan , Rajagopal Bakthavatchalam , Kevin J. Hodgetts , Scott M. Capitosti , Jianmin Mao , David J. Wustrow , Qin Guo
IPC分类号： A61K31/5377
CPC分类号： C07D487/04 , C07D231/14 , C07D277/56 , C07D333/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/04 , C07D417/04 , C07D417/14
摘要： 5-Membered heterocyclic amides and related compounds 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5-组杂环酰胺和相关化合物，其具有如下所述的变体： 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：US07566712B2
公开(公告)日：2009-07-28
申请号：US10893799
申请日：2004-07-16
申请人： Rajagopal Bakthavatchalam , Charles A. Blum , Stéphane De Lombaert , Taeyoung Yoon , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Charles A. Blum , Stéphane De Lombaert , Taeyoung Yoon , Xiaozhang Zheng
IPC分类号： C07D401/14 , C07D403/14 , A61K31/53 , A61K31/506 , A61P19/02
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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