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1. 发明授权

US06476038B1 Amino substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines 失效
标题翻译：氨基取代的吡唑并[1,5-a] -1,5-嘧啶和吡唑并[1,5-a] -1,3,5-三嗪
公开(公告)号：US06476038B1
公开(公告)日：2002-11-05
申请号：US09676972
申请日：2000-09-29
申请人： James W. Darrow , Stéphane De Lombaert , Charles Blum , Jennifer Tran , Mark Giangiordano , David Andrew Griffith , Philip Albert Carpino
发明人： James W. Darrow , Stéphane De Lombaert , Charles Blum , Jennifer Tran , Mark Giangiordano , David Andrew Griffith , Philip Albert Carpino
IPC分类号： C07D48704
CPC分类号： C07D487/04 , G01N2333/5755 , G01N2333/70571
摘要： Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. 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 NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：公开了下式的化合物：其中R1，R2，R3，R4，R5，R6和X如本文所定义。这些化合物是NPY1受体的选择性调节剂。这些化合物可用于治疗许多CNS疾病，代谢紊乱和外周疾病，特别是进食障碍和高血压。还提供了治疗这种病症以及包装的药物组合物的方法。本发明的化合物也可用作NPY1受体定位的探针和作为NPY1受体结合测定中的标准物的探针。给出了在受体定位研究中使用化合物的方法。

2. 发明授权

US06372743B1 Certain alkylene diamine-substituted pyrazlo (1,5-a)-1,5-pyrimidines and pyrazolo (1,5-a) 1,3,5-triazines 失效
标题翻译：某些亚烷基二胺取代的吡唑（1,5-a）-1,5-嘧啶和吡唑并（1,5-a）1,3,5-三嗪
公开(公告)号：US06372743B1
公开(公告)日：2002-04-16
申请号：US09676970
申请日：2000-09-29
申请人： James W. Darrow , Stephane De Lombaert , Charles Blum , Jennifer Tran , Mark Giangiordano , David Andrew Griffith , Philip Albert Carpino
发明人： James W. Darrow , Stephane De Lombaert , Charles Blum , Jennifer Tran , Mark Giangiordano , David Andrew Griffith , Philip Albert Carpino
IPC分类号： A61K3153
CPC分类号： C07D487/04 , G01N2333/5755 , G01N2333/70571
摘要： Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. 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 NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：公开了下式的化合物：其中R1，R2，R3，R4，R5，R6和X如本文所定义。这些化合物是NPY1受体的选择性调节剂。这些化合物可用于治疗许多CNS疾病，代谢紊乱和外周疾病，特别是进食障碍和高血压。还提供了治疗这种病症以及包装的药物组合物的方法。本发明的化合物也可用作NPY1受体定位的探针和作为NPY1受体结合测定中的标准物的探针。给出了在受体定位研究中使用化合物的方法。

3. 发明申请

US20050033048A1 Spiro[isobenzofuran-1,4'-piperidin]-3-ones and 3h-spiroisobenzofuran-1,4'-piperidines 审中-公开
标题翻译：螺[异苯并呋喃-1,4'-哌啶] -3-酮和3h-螺二苯并呋喃-1,4'-哌啶
公开(公告)号：US20050033048A1
公开(公告)日：2005-02-10
申请号：US10415457
申请日：2001-12-11
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： C07D491/107 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/519 , A61K51/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P25/00 , A61P25/18 , A61P25/24 , A61P43/00 , C07D487/04 , C07D487/10 , C07D491/10 , C07D519/00
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 method for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.
摘要翻译：提供了能够调节NPY5受体活性的取代螺[异苯并呋喃-1,4'-哌啶] -3-酮和3H-螺异苯并呋喃-1,4'-哌啶。这样的化合物可用于在体内或体外调节配体与NPY5受体的结合，并且特别可用于治疗多种疾病（例如，进食障碍，例如肥胖或贪食症，精神疾病，糖尿病和心血管疾病，例如高血压），驯养的伴侣动物和家畜。还提供了用于治疗这种病症的药物组合物和方法，以及使用这些化合物检测NPY5受体的方法。

4. 发明申请

US20060040964A1 Spiro[isobenzofuran-1,4'-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4'-piperidines 审中-公开
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.

5. 发明授权

US5668283A Certain aryl substituted pyrrolopyrazines; a new class of GABA brain receptor ligands 失效
标题翻译：某些芳基取代的吡咯并吡嗪; 一类新的GABA脑受体配体
公开(公告)号：US5668283A
公开(公告)日：1997-09-16
申请号：US486595
申请日：1995-06-07
申请人： Charles Blum , Alan Hutchison
发明人： Charles Blum , Alan Hutchison
IPC分类号： C07D487/04 , A61K31/495 , A61K31/50 , C07D471/14
CPC分类号： C07D487/04
摘要： This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## represents: ##STR3## where n is 0, 1, or 2; R.sub.1 and R.sub.2 are hydrogen or straight or branched chain alkyl groups;Y represents various organic and inorganic substituents;W represents an aromatic group substituted with various organic and inorganic substituents;A is CH or N;B is a substituted or unsubstituted carbon or N; andE is hydrogen or straight or branched alkyl groupsThese compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.
摘要翻译：本发明包括下式的化合物：其中药物可接受的无毒盐，其中：其中n为0,1或2; R1和R2是氢或直链或支链烷基; Y代表各种有机和无机取代基; W表示被各种有机和无机取代基取代的芳族基团; A是CH或N; B是取代或未取代的碳或N; 并且E是氢或直链或支链烷基这些化合物是用于GABAa脑受体或前药的高选择性激动剂，拮抗剂或反向激动剂，并且可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量，并提高警觉性。

6. 发明授权

US5286860A Certain aryl substituted pyrrolopyrazines; a new class of GABA brain receptor ligands 失效
标题翻译：某些芳基取代的吡咯并吡嗪; 一类新的GABA脑受体配体
公开(公告)号：US5286860A
公开(公告)日：1994-02-15
申请号：US975409
申请日：1992-11-12
申请人： Charles Blum , Alan Hutchison
发明人： Charles Blum , Alan Hutchison
IPC分类号： C07D487/04 , C07D491/20 , C07D487/10 , C07D487/14 , C07D487/20
CPC分类号： C07D487/04
摘要： This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## represents: ##STR3## where n is 0, 1, or 2; R.sub.1 and R.sub.2 are hydrogen or straight or branched chain alkyl groups;Y represents various organic and inorganic substituents;W represents an aromatic group substituted with various organic and inorganic substituents;A is CH or N;B is a substituted or unsubstituted carbon or N; andE is hydrogen or straight or branched alkyl groupsThese compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.
摘要翻译：本发明包括下式的化合物：其中药物可接受的无毒盐，其中：其中n为0,1或2; R1和R2是氢或直链或支链烷基; Y代表各种有机和无机取代基; W表示被各种有机和无机取代基取代的芳族基团; A是CH或N; B是取代或未取代的碳或N; 并且E是氢或直链或支链烷基这些化合物是用于GABAa脑受体或前药的高选择性激动剂，拮抗剂或反向激动剂，并且可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量，并提高警觉性。

7. 发明授权

US09556201B2 Bicyclic pyridines and analogs as sirtuin modulators 有权
标题翻译：双环吡啶和类似物作为沉默调节剂
公开(公告)号：US09556201B2
公开(公告)日：2017-01-31
申请号：US13504134
申请日：2010-10-29
申请人： Pui Yee Ng , Charles Blum , Lauren McPherson , Robert B. Perni , Chi B. Vu , Mohammed Mahmood Ahmed , Jeremy S. Disch
发明人： Pui Yee Ng , Charles Blum , Lauren McPherson , Robert B. Perni , Chi B. Vu , Mohammed Mahmood Ahmed , Jeremy S. Disch
IPC分类号： A61K31/55 , A61K31/551 , A61K31/553 , A61K31/4375 , A61K31/437 , A61K31/5365 , A61K31/4985 , C07D471/04 , C07D487/04 , C07D519/00 , C07D498/04
CPC分类号： C07D498/04 , C07D471/04
摘要： Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本文提供了新的沉默调节蛋白的调节化合物及其使用方法。沉默调节蛋白的调节化合物可用于增加细胞的寿命，以及治疗和/或预防各种各样的疾病和病症，包括例如与老化或紧张相关的疾病或病症，糖尿病，肥胖症，神经变性疾病，心血管疾病，血液凝固障碍，炎症，癌症和/或潮红以及将受益于增加的线粒体活性的疾病或病症。还提供了包含与另一种治疗剂组合的沉默调节蛋白的调节化合物的组合物。

8. 发明申请

US20120252780A1 BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS 有权
标题翻译：双相PYRIDINES和模拟物作为SIRTUIN调节剂
公开(公告)号：US20120252780A1
公开(公告)日：2012-10-04
申请号：US13504134
申请日：2010-10-29
申请人： Pui Yee Ng , Charles Blum , Lauren McPherson , Robert B. Perni , Chi B. Vu , Mohammed Mahmood Ahmed , Jeremy S. Disch
发明人： Pui Yee Ng , Charles Blum , Lauren McPherson , Robert B. Perni , Chi B. Vu , Mohammed Mahmood Ahmed , Jeremy S. Disch
IPC分类号： A61K31/4375 , A61K31/5383 , C07D519/00 , C07D471/04 , A61P3/10 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/444 , A61P3/04 , C07D498/04 , A61K31/4985
CPC分类号： C07D498/04 , C07D471/04
摘要： Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本文提供了新的沉默调节蛋白的调节化合物及其使用方法。沉默调节蛋白的调节化合物可用于增加细胞的寿命，以及治疗和/或预防各种各样的疾病和病症，包括例如与老化或紧张相关的疾病或病症，糖尿病，肥胖症，神经变性疾病，心血管疾病，血液凝固障碍，炎症，癌症和/或潮红以及将受益于增加的线粒体活性的疾病或病症。还提供了包含与另一种治疗剂组合的沉默调节蛋白的调节化合物的组合物。

9. 发明申请

US20060100245A1 Substituted biphenyl-4-carboxylic acid arylamide analogues 审中-公开
标题翻译：取代的联苯-4-羧酸芳酰胺类似物
公开(公告)号：US20060100245A1
公开(公告)日：2006-05-11
申请号：US10539860
申请日：2003-12-19
申请人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , James Darrow , Stephane DeLombaert , Taeyoung Yoon , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , James Darrow , Stephane DeLombaert , Taeyoung Yoon , Xiaozhang Zheng
IPC分类号： A61K31/444 , A61K31/4433 , A61K31/4415 , C07D405/02 , C07D401/02
CPC分类号： C07D213/76 , C07C233/65 , C07C233/66 , C07C233/75 , C07C235/64 , C07D211/34 , C07D213/26 , C07D213/48 , C07D213/61 , C07D213/73 , C07D213/82 , C07D213/85 , C07D241/16 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D417/12
摘要： Substituted biphenyl-4-carboxylic acid arylamide analogues capable of modulating receptor activity, are provided. Such ligands may be used to modulate receptor activity in vivo or in vitro, and are particularly useful in the treatment of pain and other conditions associated with receptor activation 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 receptor localization studies.
摘要翻译：提供能调节受体活性的取代的联苯-4-羧酸芳酰胺类似物。这样的配体可以用于体内或体外调节受体活性，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的受体活化相关的疼痛和其它病症。还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

10. 发明申请

US20070105865A1 Substituted bicyclic quinazolin-4-ylamine derivatives 审中-公开
标题翻译：取代的双环喹唑啉-4-基胺衍生物
公开(公告)号：US20070105865A1
公开(公告)日：2007-05-10
申请号：US10571203
申请日：2004-09-09
申请人： Rajagopal Bakthavatchalam , Charles Blum , Bertrand Chenard
发明人： Rajagopal Bakthavatchalam , Charles Blum , Bertrand Chenard
IPC分类号： A61K31/519 , A61K31/525 , C07D487/02 , C07D475/02
CPC分类号： C07D401/12 , C04B35/632 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： Substituted bicyclic quinazolin-4-ylamine derivatives 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：提供了取代的双环喹唑啉-4-基胺衍生物。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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