公开(公告)号：US10005743B2

公开(公告)日：2018-06-26

申请号：US15192098

申请日：2016-06-24

申请人： Supernus Pharmaceuticals, Inc.

发明人： Likan Liang ,  Padmanabh P. Bhatt ,  David Dain ,  Jean-Philippe Taquet ,  Aleksandr Pechenov ,  Alexei Tchesnokov ,  Reynold Mariaux

IPC分类号： C07D265/30 ,  C07D265/32 ,  C07C215/08 ,  C07C217/34

CPC分类号： C07D265/30 ,  C07C215/08 ,  C07C217/34 ,  C07D265/32

摘要： Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.

公开(公告)号：US10160733B2

公开(公告)日：2018-12-25

申请号：US15988190

申请日：2018-05-24

申请人： Supernus Pharmaceuticals, Inc.

发明人： Likan Liang ,  Padmanabh P. Bhatt ,  David Dain ,  Jean-Philippe Taquet ,  Aleksandr Pechenov ,  Alexei Tchesnokov ,  Reynold Mariaux

IPC分类号： C07D265/30 ,  C07D265/32 ,  C07C215/08 ,  C07C217/34

摘要： Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.

公开(公告)号：US09434703B2

公开(公告)日：2016-09-06

申请号：US14577380

申请日：2014-12-19

申请人： Supernus Pharmaceuticals, Inc.

发明人： Likan Liang ,  Padmanabh P. Bhatt ,  David Dain ,  Jean-Philippe Taquet ,  Aleksandr Pechenov ,  Alexei Tchesnokov ,  Reynold Mariaux

IPC分类号： C07C215/08 ,  C07D265/30 ,  C07C217/34 ,  C07D265/32 ,  A61P25/00 ,  A61P25/24 ,  A61K31/535

CPC分类号： C07D265/30 ,  C07C215/08 ,  C07C217/34 ,  C07D265/32

摘要： Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.

摘要翻译： 本文提供了维罗他嗪及其各种盐的制备方法，以及与维甲内酯相关的化合物，例如新的中间体反应产物及其多晶型物。 特别地，该方法提供基本上纯的维罗他嗪HCl的API，同时避免不期望的杂质。 该方法进一步提供了分离，鉴定和表征viloxazine的新型多晶型物。 还提供了用于合成和鉴定和描述维罗他嗪的新型中间体的方法，以及一些重要的代谢产物和维罗他嗪代谢物的前体。