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11. 发明申请

US20060122394A1 Substituted biaryl piperazinyl-pyridine analogues 有权
标题翻译：取代的联芳基哌嗪基 - 吡啶类似物
公开(公告)号：US20060122394A1
公开(公告)日：2006-06-08
申请号：US11204202
申请日：2005-08-13
申请人： Charles Blum , Harry Brielmann , Bertrand Chenard , Xiaozhang Zheng
发明人： Charles Blum , Harry Brielmann , Bertrand Chenard , Xiaozhang Zheng
IPC分类号： C07D403/14
CPC分类号： C07D405/14 , C07D239/42 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14
摘要： Substituted 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 receptors 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：提供了下式的取代的联芳基哌嗪基 - 吡啶类似物：其中变量如本文所述。这样的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，驯养的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。

12. 发明申请

US20060229308A1 Substituted pyrirmidin-4-ylamine analogues as vanilloid receptor ligands 审中-公开
标题翻译：取代的嘧啶-4-基胺类似物作为香草素受体配体
公开(公告)号：US20060229308A1
公开(公告)日：2006-10-12
申请号：US10564583
申请日：2004-07-15
申请人： Charles Blum , Harry Brielmann , Kevin Hodgetts
发明人： Charles Blum , Harry Brielmann , Kevin Hodgetts
IPC分类号： A61K31/5377 , A61K31/53 , A61K31/505 , C07D413/02
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D251/42 , C07D401/04
摘要： Substituted pyrimidyl-4-ylamine analogues are provided, of the Formula: (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate Vanilloid 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：提供了取代的嘧啶-4-基胺类似物，其具有如下所述的变体：式（I）。这样的化合物是可用于在体内或体外调节香草素受体活性的配体，并且特别可用于治疗与人，驯养的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。

13. 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。

14. 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。

15. 发明申请

US20080090845A1 Haloalkyl-substituted pyrimidinone derivatives 审中-公开
标题翻译：卤代烷基取代的嘧啶酮衍生物
公开(公告)号：US20080090845A1
公开(公告)日：2008-04-17
申请号：US11895266
申请日：2007-08-22
申请人： Charles Blum , Xiaozhang Zheng , Isamir Martinez , Bertrand Chenard
发明人： Charles Blum , Xiaozhang Zheng , Isamir Martinez , Bertrand Chenard
IPC分类号： A61K31/522 , A61K31/519 , A61P11/06 , A61P11/14 , A61P13/00 , A61P29/00 , A61P5/00 , C07D409/02 , C07D417/04 , C07D471/04 , C07D473/30 , C07K14/435 , C12N5/06
CPC分类号： C07D473/30 , C07D471/04 , C07D495/04 , C07D513/04
摘要： Haloalkyl-substituted pyrimidinone derivatives 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：提供了下式的卤代烷基取代的嘧啶酮衍生物：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。

16. 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。

17. 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。

18. 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。

19. 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。

20. 发明授权

US5910590A 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：US5910590A
公开(公告)日：1999-06-08
申请号：US931648
申请日：1997-09-16
申请人： Charles Blum , Alan Hutchison
发明人： Charles Blum , Alan Hutchison
IPC分类号： C07D487/04 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00
CPC分类号： C07D487/04
摘要： Compounds of the formula ##STR1## wherein R' and R" are independently hydrogen or lower alkoxy having 1-6 carbon atoms; and R'" is halogen are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors 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：下式的化合物其中R'和R“独立地是氢或具有1-6个碳原子的低级烷氧基; 并且R“'是卤素。这些化合物是GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂，可用于诊断和治疗焦虑症，睡眠和癫痫发作，用苯二氮卓类药物过量，提高警觉性。

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