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公开(公告)号：US08008296B2
公开(公告)日：2011-08-30
申请号：US11917941
申请日：2006-06-28
申请人： Lisa Selsam Beavers , Don Richard Finley , Robert Alan Gadski , Philip Arthur Hipskind , William Joseph Hornback , Cynthia Darshini Jesudason , Richard Todd Pickard , Takako Takakuwa , Grant Mathews Vaught
发明人： Lisa Selsam Beavers , Don Richard Finley , Robert Alan Gadski , Philip Arthur Hipskind , William Joseph Hornback , Cynthia Darshini Jesudason , Richard Todd Pickard , Takako Takakuwa , Grant Mathews Vaught
IPC分类号： A61K31/535 , A61K31/497 , A61K31/445 , C07D413/00 , C07D409/00 , C07D207/00
CPC分类号： C07D207/09 , C07D401/12 , C07D403/12
摘要： The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. (Formula I).
摘要翻译： 本发明公开了具有组胺-3H受体拮抗剂或反向激动剂活性的式I化合物或其药学上可接受的盐以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物以及使用它们治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法。 （式I）。
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公开(公告)号：US20100160319A1
公开(公告)日：2010-06-24
申请号：US11917941
申请日：2006-06-28
申请人： Lisa Selsam Beavers , Don Richard Finley , Robert Alan Gadski , Philip Arthur Hipskind , William Joseph Hornback , Cynthia Darshini Jesudason , Richard Todd Pickard , Takako Takakuwa , Grant Mathews Vaught
发明人： Lisa Selsam Beavers , Don Richard Finley , Robert Alan Gadski , Philip Arthur Hipskind , William Joseph Hornback , Cynthia Darshini Jesudason , Richard Todd Pickard , Takako Takakuwa , Grant Mathews Vaught
IPC分类号： A61K31/5377 , C07D207/04 , C07D401/14 , C07D403/14 , C07D413/14 , A61K31/4025 , A61K31/454 , A61K31/497 , A61K31/4439 , A61P25/00
CPC分类号： C07D207/09 , C07D401/12 , C07D403/12
摘要： The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. (Formula I)
摘要翻译： 本发明公开了具有组胺-3H受体拮抗剂或反向激动剂活性的式I化合物或其药学上可接受的盐以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物以及使用它们治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法。 （式I）
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公开(公告)号：US08008301B2
公开(公告)日：2011-08-30
申请号：US12610954
申请日：2009-11-02
申请人： Lisa Selsam Beavers , Don Richard Finley , Terry Patrick Finn , Robert Alan Gadski , Philip Arthur Hipskind , William Joseph Hornback , Cynthia Darshini Jesudason , Richard Todd Pickard , Takako Takakuwa , Grant Mathews Vaught
发明人： Lisa Selsam Beavers , Don Richard Finley , Terry Patrick Finn , Robert Alan Gadski , Philip Arthur Hipskind , William Joseph Hornback , Cynthia Darshini Jesudason , Richard Todd Pickard , Takako Takakuwa , Grant Mathews Vaught
IPC分类号： A61K31/501 , A61K31/4439 , A61K31/4245 , A61K31/4025 , C07D403/06 , C07D413/14 , C07D401/14
CPC分类号： C07D207/09 , C07D401/10 , C07D403/10 , C07D405/10 , C07D413/10 , C07D471/04
摘要： The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine—H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor—related diseases
摘要翻译： 本发明公开了具有组胺H3受体拮抗剂或反向激动剂活性的式（I）的新化合物或其药学上可接受的盐，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法
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公开(公告)号：US20100048580A1
公开(公告)日：2010-02-25
申请号：US12610954
申请日：2009-11-02
申请人： Lisa Selsam Beavers , Don Richard Finley , Terry Patrick Finn , Robert Alan Gadski , Philip Arthur Hipskind , Wiliam Joseph Hornback , Cynthia Darshini Jesudason , Richard Todd Pickard , Takako Takakuwa , Grant Mathews Vaught
发明人： Lisa Selsam Beavers , Don Richard Finley , Terry Patrick Finn , Robert Alan Gadski , Philip Arthur Hipskind , Wiliam Joseph Hornback , Cynthia Darshini Jesudason , Richard Todd Pickard , Takako Takakuwa , Grant Mathews Vaught
IPC分类号： A61K31/501 , C07D403/06 , C07D413/14 , C07D403/14 , C07D401/14 , A61K31/506 , A61K31/4439 , A61K31/4245 , A61K31/4025
CPC分类号： C07D207/09 , C07D401/10 , C07D403/10 , C07D405/10 , C07D413/10 , C07D471/04
摘要： The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases
摘要翻译： 本发明公开了具有组胺H3受体拮抗剂或反向激动剂活性的式（I）的新化合物或其药学上可接受的盐，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法
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公开(公告)号：US07951826B2
公开(公告)日：2011-05-31
申请号：US11908501
申请日：2006-03-13
申请人： Lisa Selsam Beavers , Don Richard Finley , Robert Alan Gadski , Philip Arthur Hipskind , Cynthia Darshini Jesudason , Richard Todd Pickard , Freddie Craig Stevens , Takako Takakuwa
发明人： Lisa Selsam Beavers , Don Richard Finley , Robert Alan Gadski , Philip Arthur Hipskind , Cynthia Darshini Jesudason , Richard Todd Pickard , Freddie Craig Stevens , Takako Takakuwa
IPC分类号： A61K31/4439 , A61K31/4025 , C07D401/14 , C07D403/06
CPC分类号： C07D207/09 , C07D401/14
摘要： The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
摘要翻译： 本发明公开了具有组胺H3受体拮抗剂或反向激动剂活性的式（I）的新化合物或其药学上可接受的盐，以及制备这些化合物的方法和中间体。 在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法。
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公开(公告)号：US20080207732A1
公开(公告)日：2008-08-28
申请号：US11908501
申请日：2006-03-13
申请人： Lisa Selsam Beavers , Don Richard Finley , Robert Alan Gadski , Philip Arthur Hipskind , Cynthia Darshini Jesudason , Richard Todd Pickard , Freddie Craig Stevens , Takako Takakuwa
发明人： Lisa Selsam Beavers , Don Richard Finley , Robert Alan Gadski , Philip Arthur Hipskind , Cynthia Darshini Jesudason , Richard Todd Pickard , Freddie Craig Stevens , Takako Takakuwa
IPC分类号： A61K31/4025 , C07D403/06
CPC分类号： C07D207/09 , C07D401/14
摘要： The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
摘要翻译： 本发明公开了具有组胺H3受体拮抗剂或反向激动剂活性的式（I）的新化合物或其药学上可接受的盐，以及制备这些化合物的方法和中间体。 在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法。
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公开(公告)号：US07705025B2
公开(公告)日：2010-04-27
申请号：US11574044
申请日：2005-08-15
申请人： Don Richard Finley , Terry Patrick Finn , Philip Arthur Hipskind , William Joseph Hornback , Cynthia Darshini Jesudason , Takako Takakuwa
发明人： Don Richard Finley , Terry Patrick Finn , Philip Arthur Hipskind , William Joseph Hornback , Cynthia Darshini Jesudason , Takako Takakuwa
IPC分类号： A61K31/427 , C07D277/20
CPC分类号： C07D207/327 , C07D401/14 , C07D403/10 , C07D405/10 , C07D409/10 , C07D409/14 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
摘要翻译： 本发明提供了具有组胺H3受体拮抗剂或反向激动剂活性的新型式（I）化合物或其药学上可接受的盐以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及用于治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法。
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公开(公告)号：US20090048225A1
公开(公告)日：2009-02-19
申请号：US11574044
申请日：2005-08-15
申请人： Don Richard Finley , Terry Patrick Finn , Philip Arthur Hipskind , William Joseph Hornback , Cynthia Darshini Jesudason , Takako Takakuwa
发明人： Don Richard Finley , Terry Patrick Finn , Philip Arthur Hipskind , William Joseph Hornback , Cynthia Darshini Jesudason , Takako Takakuwa
IPC分类号： A61K31/397 , C07D409/14 , A61K31/4025 , A61P25/00 , A61P3/04 , A61K31/422 , C07D413/14 , C07D401/14 , A61K31/4439 , A61K31/4178 , A61K31/454 , A61K31/427 , C07D417/14 , A61K31/404 , C07D403/14 , A61K31/4155 , A61K31/433 , A61K31/4184
CPC分类号： C07D207/327 , C07D401/14 , C07D403/10 , C07D405/10 , C07D409/10 , C07D409/14 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
摘要翻译： 本发明提供了具有组胺H3受体拮抗剂或反向激动剂活性的新型式（I）化合物或其药学上可接受的盐以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及用于治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法。
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9.发明授权2-oxo-benzimidazolyl substituted ethanolamine derivatives and their use as β3 agonists 失效2-氧代 - 苯并咪唑基取代的乙醇胺衍生物及其作为β3激动剂的用途公开(公告)号：US07009060B2
公开(公告)日：2006-03-07
申请号：US10498261
申请日：2002-12-24
IPC分类号： C07D235/24
CPC分类号： C07D213/82 , C07C235/46 , C07C2601/02 , C07C2601/08 , C07D235/26 , C07D401/12
摘要： The present invention relates to a β3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.
摘要翻译： 本发明涉及式I的β3 N 3肾上腺素能受体激动剂：或其药用盐; 其能够增加细胞中的脂肪分解和能量消耗，因此可用于治疗2型糖尿病和/或肥胖症。
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公开(公告)号：US07208505B2
公开(公告)日：2007-04-24
申请号：US10486867
申请日：2002-08-06
申请人： Daniel Jon Sall , Jolie Anne Bastian , Rushad Eruch Karanjawala , Cynthia Darshini Jesudason , Theo Schotten , Britta Evers , Gerd Reuhter , Don Richard Finley , Freddie Craig Stevens , Vincent Patrick Rocco , Patrick Gianpietro Spinazze , John Xiaoqiang He , John Arnold Werner , William George Trankle , Andrew Michael Ratz
发明人： Daniel Jon Sall , Jolie Anne Bastian , Rushad Eruch Karanjawala , Cynthia Darshini Jesudason , Theo Schotten , Britta Evers , Gerd Reuhter , Don Richard Finley , Freddie Craig Stevens , Vincent Patrick Rocco , Patrick Gianpietro Spinazze , John Xiaoqiang He , John Arnold Werner , William George Trankle , Andrew Michael Ratz
IPC分类号： C07D209/14 , C07D213/64 , A61K31/404 , A61K31/422 , A61K31/444
CPC分类号： C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g., for treating Type 2 diabetes and/or obesity
摘要翻译： 本发明涉及式（I）的β3肾上腺素能受体激动剂; 或其药学盐; 其能够增加细胞中的脂肪分解和能量消耗，因此可用于例如治疗2型糖尿病和/或肥胖症
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