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公开(公告)号：US07569679B2
公开(公告)日：2009-08-04
申请号：US11201696
申请日：2005-08-11
摘要： A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.
摘要翻译： 提供了一种生成其十八烷衍生物的合成代谢物的方法。 提供这些化合物和使用这些衍生物检测样品中的tanaproget代谢物的方法。
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2.发明申请Metabolites of 5-fluoro-8- quinoline and methods of preparation and uses thereof 审中-公开5-氟-8-喹啉代谢物及其制备方法及用途公开(公告)号：US20080262228A1
公开(公告)日：2008-10-23
申请号：US11986895
申请日：2007-11-27
申请人： Jianyao Wang , Alana Upthagrove , Lin Deng , Wayne Everett Childers , Zhongqi Shen , William Demaio , Robin D. Moore , Zeen Tong , Li Shen , Pixu Li , Michael K. May
发明人： Jianyao Wang , Alana Upthagrove , Lin Deng , Wayne Everett Childers , Zhongqi Shen , William Demaio , Robin D. Moore , Zeen Tong , Li Shen , Pixu Li , Michael K. May
IPC分类号： A61K31/496 , C07D401/14 , A61P25/00
CPC分类号： C07D401/14
摘要： The present invention relates to novel metabolites of 5-Fluoro-8-{4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl}quinoline, which can be useful in treating CNS disorders. The present invention further relates to processes for their preparation, to pharmaceutical compositions comprising them, and to methods of using them.
摘要翻译： 本发明涉及5-氟-8- {4- [4-（6-甲氧基喹啉-8-基）哌嗪-1-基]哌啶-1-基}喹啉的新代谢物，其可用于治疗CNS 疾病 本发明还涉及其制备方法，包含它们的药物组合物以及使用它们的方法。
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3.发明申请Isolated hydroxy and n-oxide metabolites and derivatives of O-desmethylvenlafaxine and methods of treatment 审中-公开分离的羟基和N-氧化物代谢物及其衍生物的O-去甲基文拉法辛及其治疗方法公开(公告)号：US20080261895A1
公开(公告)日：2008-10-23
申请号：US11976413
申请日：2007-10-24
申请人： Matthew J. Hoffmann , William DeMaio , Jim Wang , John W. Ullrich
发明人： Matthew J. Hoffmann , William DeMaio , Jim Wang , John W. Ullrich
IPC分类号： A61K31/7032 , A61K31/138 , C07C215/46 , A61K31/14 , C07C211/63 , C07H15/20
CPC分类号： C07C215/64 , C07C291/04 , C07C2601/14
摘要： The present invention provides novel isolated compounds characterized as metabolites or derivatives of desmethylvenlafaxine including hydroxy-DV metabolites, hydroxy-DV-glucuronide metabolites, N-oxide-DV metabolites, and benzyl-hydroxy-DV metabolites. The invention includes pharmaceutical compositions comprising any of the metabolites or derivatives of the invention in combination with a pharmaceutically acceptable carrier or excipient. The invention also includes a method of treating at least one central nervous system disorder in a mammal comprising providing to a mammal in need thereof an effective amount of the compounds of the invention.
摘要翻译： 本发明提供了新型分离的化合物，其特征在于代谢物或脱甲基蓝法的衍生物，包括羟基-DV代谢物，羟基-DV-葡糖苷酸代谢物，N-氧化物-DL代谢物和苄基羟基-DV代谢物。 本发明包括药物组合物，其包含本发明的任何代谢物或衍生物与药学上可接受的载体或赋形剂的组合。 本发明还包括治疗哺乳动物中的至少一种中枢神经系统病症的方法，其包括向有需要的哺乳动物提供有效量的本发明化合物。
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公开(公告)号：US07402687B2
公开(公告)日：2008-07-22
申请号：US11409479
申请日：2006-04-21
申请人： Gary Paul Stack , Jianyao Wang , William Demaio , Ronald Jordan , John Chuck Lem Erve , Rasmy Elsayed Talaat , Matthew John Hoffmann
发明人： Gary Paul Stack , Jianyao Wang , William Demaio , Ronald Jordan , John Chuck Lem Erve , Rasmy Elsayed Talaat , Matthew John Hoffmann
IPC分类号： C07D407/12
CPC分类号： C07D407/12 , C07D307/81 , C07D307/85
摘要： Compounds of formula I are described herein which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. or pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3, R4, Rx, Ry, and n are as defined herein. Such compounds, and compositions thereof, are useful for treating a variety of central nervous system disorders such as schizophrenia.
摘要翻译： 本文描述了式I化合物，其是脑5-羟色胺受体的2C亚型的激动剂或部分激动剂。 或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 4， R 1，R 2，和n如本文所定义。 这些化合物及其组合物可用于治疗各种中枢神经系统疾病如精神分裂症。
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![Metabolites of certain [1,4]diazepino[6,7,1-ij]quinoline derivatives and methods of preparation and use thereof](/abs-image/US/2006/05/25/US20060111305A1/abs.jpg.150x150.jpg)
5.发明申请Metabolites of certain [1,4]diazepino[6,7,1-ij]quinoline derivatives and methods of preparation and use thereof 审中-公开某些[1,4]二氮杂[6,7,1-ij]喹啉衍生物的代谢物及其制备方法及用途公开(公告)号：US20060111305A1
公开(公告)日：2006-05-25
申请号：US11267765
申请日：2005-11-04
申请人： Zeen Tong , Jim Wang , William DeMaio , Alvin Bach , Ronald Jordan , Youchu Wang , P. Sivaramakrishnan Ramamoorthy , Gary Stack
发明人： Zeen Tong , Jim Wang , William DeMaio , Alvin Bach , Ronald Jordan , Youchu Wang , P. Sivaramakrishnan Ramamoorthy , Gary Stack
IPC分类号： A61K31/7052 , C07H19/00 , C07H19/22 , C07H17/02
CPC分类号： C07D471/06 , C07H15/26 , C07H17/02 , C07H19/00 , C07H19/22
摘要： The invention relates to metabolites of certain [1,4]diazepino[6,7,1-ij]quinoline derivatives and methods of preparation and use thereof. Specifically, the invention relates to compounds of formula I wherein the various substituents are defined herein. The invention also provides pharmaceutical compositions including compounds of formula I, methods of making such compounds, and methods of using such compounds.
摘要翻译： 本发明涉及某些[1,4]二氮杂[6,7,1-ij]喹啉衍生物的代谢物及其制备及应用方法。 具体地，本发明涉及式I化合物，其中各种取代基在本文中定义。 本发明还提供药物组合物，包括式I化合物，制备此类化合物的方法，以及使用这些化合物的方法。
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公开(公告)号：US20060035843A1
公开(公告)日：2006-02-16
申请号：US11201696
申请日：2005-08-11
IPC分类号： A61K31/7052 , C07H17/02
摘要： A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.
摘要翻译： 提供了一种生成其十八烷衍生物的合成代谢物的方法。 提供这些化合物和使用这些衍生物检测样品中的tanaproget代谢物的方法。
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公开(公告)号：US08389698B2
公开(公告)日：2013-03-05
申请号：US12492229
申请日：2009-06-26
IPC分类号： C07H17/00 , C07H1/00 , C07H1/06 , C07D265/20 , C07D413/04 , A61K31/7042 , A61K31/536
摘要： A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.
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公开(公告)号：US20090306000A1
公开(公告)日：2009-12-10
申请号：US12492229
申请日：2009-06-26
IPC分类号： A61K31/706 , C07H19/24 , C07H17/00 , C12Q1/02 , C07K16/00 , G01N33/566
摘要： A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.
摘要翻译： 提供了一种生成其十八烷衍生物的合成代谢物的方法。 提供这些化合物和使用这些衍生物检测样品中的tanaproget代谢物的方法。
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公开(公告)号：US20060241176A1
公开(公告)日：2006-10-26
申请号：US11409479
申请日：2006-04-21
申请人： Gary Stack , Christine Huselton , Jianyao Wang , William Demaio , Ronald Jordan , John Erve , Rasmy Talaat , Matthew Hoffmann
发明人： Gary Stack , Christine Huselton , Jianyao Wang , William Demaio , Ronald Jordan , John Erve , Rasmy Talaat , Matthew Hoffmann
IPC分类号： A61K31/34 , A61K31/343 , C07D307/02
CPC分类号： C07D407/12 , C07D307/81 , C07D307/85
摘要： Compounds of formula I are described herein which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. or pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3, R4, Rx, Ry, and n are as defined herein. Such compounds, and compositions thereof, are useful for treating a variety of central nervous system disorders such as schizophrenia.
摘要翻译： 本文描述了式I化合物，其是脑5-羟色胺受体的2C亚型的激动剂或部分激动剂。 或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 4， R 1，R 2，和n如本文所定义。 这些化合物及其组合物可用于治疗各种中枢神经系统疾病如精神分裂症。
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公开(公告)号：US20060128950A1
公开(公告)日：2006-06-15
申请号：US11265790
申请日：2005-11-02
申请人： Ronald Jordan , William DeMaio , Matthew Hoffmann
发明人： Ronald Jordan , William DeMaio , Matthew Hoffmann
IPC分类号： C07J17/00
CPC分类号： C07J17/00
摘要： A glucuronide metabolite of tigecycline, and its corresponding epimer, have been identified in humans treated with tigecycline. Mass spectral data have been used to identify these structures.
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