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公开(公告)号：US20120142967A1
公开(公告)日：2012-06-07
申请号：US13378797
申请日：2010-06-17
申请人： John A. DeMattei , Marlon Carlos , Ryan O. Castro , Tsung-Hsun Chuang , Mark Allen Hadd , Xiao-Xiong Lu , Mark Macias , Stephen M. Shaw
发明人： John A. DeMattei , Marlon Carlos , Ryan O. Castro , Tsung-Hsun Chuang , Mark Allen Hadd , Xiao-Xiong Lu , Mark Macias , Stephen M. Shaw
IPC分类号： C07C209/08 , C07C209/74 , C07C211/29 , C07C213/02 , C07C17/16
CPC分类号： C07C209/74 , C07C17/04 , C07C17/16 , C07C209/08 , C07C211/29 , C07C213/00 , C07C213/08 , C07C215/08
摘要： The present invention relates to processes and intermediates useful in the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (lorcaserin), a serotonin (5-HT) receptor modulator that is useful in the treatment of, for example, central nervous system disorders, such as obesity.
摘要翻译： 本发明涉及可用于制备（R）-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并吖庚因（氯卡色林），5-羟色胺（5-HT）的方法和中间体 ）受体调节剂，其可用于治疗例如中枢神经系统疾病，例如肥胖症。
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公开(公告)号：US20150210625A1
公开(公告)日：2015-07-30
申请号：US14580399
申请日：2014-12-23
申请人： John A. DeMattei , Carlos Marlon , Ryan O. Castro , Tsung-Hsun Chuang , Mark Allen Hadd , Xiao-Xiong Lu , Mark Macias , Stephen M. Shaw
发明人： John A. DeMattei , Carlos Marlon , Ryan O. Castro , Tsung-Hsun Chuang , Mark Allen Hadd , Xiao-Xiong Lu , Mark Macias , Stephen M. Shaw
IPC分类号： C07C209/74 , C07C213/00 , C07C211/29 , C07C17/04
CPC分类号： C07C209/74 , C07C17/04 , C07C17/16 , C07C209/08 , C07C211/29 , C07C213/00 , C07C213/08 , C07C215/08
摘要： The present invention relates to processes and intermediates useful in the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (lorcaserin), a serotonin (5-HT) receptor modulator that is useful in the treatment of, for example, central nervous system disorders, such as obesity.
摘要翻译： 本发明涉及可用于制备（R）-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并吖庚因（氯卡色林），5-羟色胺（5-HT）的方法和中间体 ）受体调节剂，其可用于治疗例如中枢神经系统疾病，例如肥胖症。
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公开(公告)号：US08952197B2
公开(公告)日：2015-02-10
申请号：US13378797
申请日：2010-06-17
申请人： John A. DeMattei , Carlos Marlon , Ryan O. Castro , Tsung-Hsun Chuang , Mark Allen Hadd , Xiao-Xiong Lu , Mark Macias , Stephen M. Shaw
发明人： John A. DeMattei , Carlos Marlon , Ryan O. Castro , Tsung-Hsun Chuang , Mark Allen Hadd , Xiao-Xiong Lu , Mark Macias , Stephen M. Shaw
IPC分类号： C07C209/00 , C07C213/08 , C07C17/16 , C07C209/08 , C07C209/74 , C07C211/29
CPC分类号： C07C209/74 , C07C17/04 , C07C17/16 , C07C209/08 , C07C211/29 , C07C213/00 , C07C213/08 , C07C215/08
摘要： The present invention relates to processes and intermediates useful in the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (lorcaserin), a serotonin (5-HT) receptor modulator that is useful in the treatment of for example, central nervous system disorders, such as obesity.
摘要翻译： 本发明涉及可用于制备（R）-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并吖庚因（氯卡色林），5-羟色胺（5-HT）的方法和中间体 ）受体调节剂，其可用于治疗例如中枢神经系统疾病，例如肥胖症。
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![Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto](/abs-image/US/2015/09/08/US09126946B2/abs.jpg.150x150.jpg)
4.发明授权Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto 有权可用于制备1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基 - 苯基] -3-（2,4-二氟 - 苯基）脲和结晶 与之相关的形式公开(公告)号：US09126946B2
公开(公告)日：2015-09-08
申请号：US13126563
申请日：2009-10-27
IPC分类号： A61K31/415 , C07C231/16 , C07D231/16
CPC分类号： A61K31/415 , C07D231/12 , C07D231/16
摘要： The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.
摘要翻译： 本发明涉及可用于制备1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基 - 苯基] -3-（2,4 - 二氟 - 苯基） - 脲（化合物I），其结晶形式和溶剂合物形式; 和包含1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基 - 苯基] -3-（2,4-二氟 - 苯基） - 脲的结晶的组合物， 其通过如本文所述的方法制备的溶剂合物形式。
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![PROCESSES USEFUL FOR THE PREPARATION OF 1-[3-(4-BROMO-2-METHYL-2H-PYRAZOL-3-YL)-4-METHOXY-PHENYL]-3-(2,4-DIFLUORO-PHENYL)UREA AND CRYSTALLINE FORMS RELATED THERETO](/abs-image/US/2011/08/25/US20110207790A1/abs.jpg.150x150.jpg)
5.发明申请PROCESSES USEFUL FOR THE PREPARATION OF 1-[3-(4-BROMO-2-METHYL-2H-PYRAZOL-3-YL)-4-METHOXY-PHENYL]-3-(2,4-DIFLUORO-PHENYL)UREA AND CRYSTALLINE FORMS RELATED THERETO 有权用于制备1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基] -3-（2,4-二氟苯基）脲和结晶的方法 表格相关公开(公告)号：US20110207790A1
公开(公告)日：2011-08-25
申请号：US13126563
申请日：2009-10-27
IPC分类号： A61K31/415 , C07D231/10 , A61P25/00
CPC分类号： A61K31/415 , C07D231/12 , C07D231/16
摘要： The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.
摘要翻译： 本发明涉及可用于制备1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基 - 苯基] -3-（2,4 - 二氟 - 苯基） - 脲（化合物I），其结晶形式和溶剂合物形式; 和包含1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基 - 苯基] -3-（2,4-二氟 - 苯基） - 脲的结晶的组合物， 其通过如本文所述的方法制备的溶剂合物形式。
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6.发明申请CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF PHENYL-PYRAZOLES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR 有权用于制备作为5-HT2A丝氨酸受体的调节剂的苯基吡唑的晶体形式和方法公开(公告)号：US20100234380A1
公开(公告)日：2010-09-16
申请号：US12301212
申请日：2007-05-17
申请人： Tawfik Gharbaoui , Dipanjan Sengupta , Ashwin M. Krishnan , Nainesh Shah , Ryan M. Hart , Mark Macias
发明人： Tawfik Gharbaoui , Dipanjan Sengupta , Ashwin M. Krishnan , Nainesh Shah , Ryan M. Hart , Mark Macias
IPC分类号： A61K31/5377 , C07D413/12 , C07D403/12 , C07D231/12 , A61K31/496 , A61K31/415 , A61P7/00 , A61P25/00 , A61P25/18 , A61P9/00
CPC分类号： C07D231/12
摘要： The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT2A serotonin receptor modulators, compositions thereof and methods of using the same.
摘要翻译： 本发明涉及制备式（I）的苯基 - 吡唑的方法及其盐及其药物组合物，其可用作5-HT2A 5-羟色胺受体活性的调节剂。 本发明还涉及用于该方法及其制备的中间体。 本发明还涉及5-HT2A 5-羟色胺受体调节剂的结晶形式，其组合物及其使用方法。
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公开(公告)号：US08481535B2
公开(公告)日：2013-07-09
申请号：US12301212
申请日：2007-05-17
申请人： Tawfik Gharbaoui , Dipanjan Sengupta , Ashwin M. Krishnan , Nainesh Shah , Ryan M. Hart , Mark Macias , Edward A. Lally , Jonathan Duffield
发明人： Tawfik Gharbaoui , Dipanjan Sengupta , Ashwin M. Krishnan , Nainesh Shah , Ryan M. Hart , Mark Macias , Edward A. Lally , Jonathan Duffield
IPC分类号： A61K31/5377 , A61K31/496 , C07D295/185 , C07D403/12
CPC分类号： C07D231/12
摘要： The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT2A serotonin receptor modulators, compositions thereof and methods of using the same.
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