公开(公告)号：EP3226907A1

公开(公告)日：2017-10-11

申请号：EP15816302.2

申请日：2015-12-02

申请人： Kempharm, Inc.

发明人： MICKLE, Travis ,  GUENTHER, Sven ,  BERA, Sanjib ,  KANSKI, Jaroslaw ,  MARTIN, Andrea

IPC分类号： A61K47/50 ,  C07D221/28

CPC分类号： A61K31/485 ,  A61K47/48038 ,  A61K47/48061 ,  A61K47/481 ,  A61K47/542 ,  A61K47/545 ,  A61K47/55 ,  C07D221/28 ,  C07D489/08

摘要： The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxymorphone (4,5-α-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxymorphone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxymorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

摘要翻译： 目前描述的技术提供包含芳基羧酸和例如NSAID的组合物，其与羟吗啡酮（4,5-α-环氧-3,14-二羟基-17-甲基吗啡喃-6-酮）化学缀合以形成新的前药/组合物 羟吗啡酮，包括苯甲酸盐，水杨酸盐，丙酸盐，芬那酸盐和乙酸盐，它们具有降低的羟吗啡酮滥用可能性。 本技术还提供了治疗患者的方法，药物试剂盒和本技术的缀合物的合成方法。