公开(公告)号：US20220096463A1

公开(公告)日：2022-03-31

申请号：US17550328

申请日：2021-12-14

申请人： KEMPHARM, INC.

发明人： Travis Mickle ,  Sven Guenther ,  Sanjib Bera

IPC分类号： A61K31/485 ,  A61K47/54

摘要： The presently described technology provides compositions of one or more of oxoacids, amino acids, polyethylene glycols, and/or vitamin compounds chemically conjugated to levorphanol ((−)-17-methylmorphinan-3-ol) to form novel prodrugs and compositions of levorphanol.

公开(公告)号：US11136295B2

公开(公告)日：2021-10-05

申请号：US16667804

申请日：2019-10-29

申请人： KemPharm, Inc.

发明人： Sven Guenther ,  Guochen Chi ,  Travis Mickle

IPC分类号： C07D213/56 ,  A61K31/4425 ,  C07D213/79 ,  C07D213/81 ,  C07D413/06 ,  A61K31/4458 ,  C07D401/06 ,  A61K47/55 ,  A61K9/00 ,  A61K31/4545 ,  C07D213/80 ,  A61K9/02

摘要： Disclosed are d-amphetamine compounds and compositions comprising at least one organic acid covalently bound to d-amphetamine, a salt thereof, a derivative thereof, or a combination thereof. Methods of making and using the same are also disclosed.

公开(公告)号：US11021459B2

公开(公告)日：2021-06-01

申请号：US16577876

申请日：2019-09-20

申请人： KemPharm, Inc.

发明人： Travis Mickle ,  Sven Guenther ,  Guochen Chi

IPC分类号： A61K9/00 ,  A61K31/4545 ,  A61K47/54 ,  A61K31/4458 ,  C07D401/12 ,  C07D211/34

摘要： The present technology is directed to d-threo-methylphenidate conjugates and a composition comprising d-threomethylphenidate conjugated to nicotinoyl-L-serine, or salt thereof. The present technology also relates to a composition comprising at least one conjugate of d-methylphenidate having at least two or more chiral centers. The composition is optically active. The present technology additionally relates to oral formulations and pharmaceutical kits comprising at least one d-threo-methylphenidate conjugate.
The pharmaceutical kit may comprise a specified amount of individual doses in a package. Each individual dose in the package may contain a pharmaceutically effective amount of a conjugate of d-threo methylphenidate.

公开(公告)号：US10463660B2

公开(公告)日：2019-11-05

申请号：US16054578

申请日：2018-08-03

申请人： KemPharm, Inc.

发明人： Travis Mickle ,  Sven Guenther ,  Sanjib Bera ,  Jaroslaw Kanski ,  Andrea Martin

IPC分类号： A61K31/485 ,  C07D489/08 ,  A61K47/54 ,  A61K47/55 ,  C07D221/28

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.

公开(公告)号：US10231960B2

公开(公告)日：2019-03-19

申请号：US15249088

申请日：2016-08-26

申请人： KemPharm, Inc.

发明人： Sven Guenther ,  Guochen Chi ,  Bindu Bera ,  Travis Mickle ,  Sanjib Bera

IPC分类号： C07D211/68 ,  C07D211/60 ,  A61K31/4458 ,  C07F9/59 ,  C07D211/34 ,  C07K5/02 ,  C07K5/062 ,  C07D401/12 ,  A61K9/00 ,  A61K47/60 ,  A61K47/54 ,  A61K47/64

摘要： The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.

公开(公告)号：US10144740B2

公开(公告)日：2018-12-04

申请号：US15812730

申请日：2017-11-14

申请人： KemPharm, Inc

发明人： Travis Mickle ,  Sven Guenther ,  Sanjib Bera ,  Bindu Bera ,  Jaroslaw Kanski ,  Andrea Martin

IPC分类号： C07D489/04 ,  C07D498/08 ,  A61P25/36

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

公开(公告)号：US10071091B2

公开(公告)日：2018-09-11

申请号：US15589158

申请日：2017-05-08

申请人： KemPharm, Inc.

发明人： Travis Mickle ,  Sven Guenther ,  Sanjib Bera ,  Jaroslaw Kanski ,  Andrea Martin

IPC分类号： A61K31/44 ,  A61K31/485 ,  A61K47/48 ,  C07D489/08 ,  C07D221/28

CPC分类号： A61K31/485 ,  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.

公开(公告)号：US09682076B2

公开(公告)日：2017-06-20

申请号：US14956642

申请日：2015-12-02

申请人： KemPharm, Inc.

发明人： Travis Mickle ,  Sven Guenther ,  Sanjib Bera ,  Jaroslaw Kanski ,  Andrea Martin

IPC分类号： A61K31/44 ,  A61K31/485 ,  A61K47/48 ,  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.

公开(公告)号：US09125947B2

公开(公告)日：2015-09-08

申请号：US14493611

申请日：2014-09-23

申请人： KemPharm, Inc.

发明人： Travis Mickle ,  Sven Guenther ,  Christal Mickle

IPC分类号： A61K31/44 ,  A61K31/19 ,  A61K47/48 ,  A61K31/485

CPC分类号： A61K47/48038 ,  A61K31/44 ,  A61K31/485 ,  A61K47/542

摘要： The presently described technology provides phenylethanoic acid, phenylpropanoic acid, phenylpropenoic acid, a salt thereof, a derivative thereof or a combination thereof chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs or compositions of hydrocodone which have a decreased potential for abuse of hydrocodone. 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苯基乙酸，苯基丙酸，苯基丙酸，其盐，其衍生物或其化合物与氢可酮（吗啡喃-6-酮，4,5-α-环氧-3-甲氧基-17- 甲基）以形成氢可酮的新药前体药物或组合物，其潜在滥用氢可酮的可能性降低。 本技术还提供了治疗患者的方法，药物试剂盒和本技术合成缀合物的方法。

公开(公告)号：US08871780B2

公开(公告)日：2014-10-28

申请号：US12828456

申请日：2010-07-01

申请人： Travis Mickle ,  Sven Guenther ,  Christal Mickle ,  Guochen Chi ,  Jaroslaw Kanski ,  Andrea K. Martin ,  Bindu Bera

发明人： Travis Mickle ,  Sven Guenther ,  Christal Mickle ,  Guochen Chi ,  Jaroslaw Kanski ,  Andrea K. Martin ,  Bindu Bera

IPC分类号： A61K31/485 ,  A61K45/06 ,  A61K47/48

CPC分类号： A61K47/48038 ,  A61K31/44 ,  A61K31/485 ,  A61K47/542

摘要： The presently described technology provides phenylethanoic acid, phenylpropanoic acid, phenylpropenoic acid, a salt thereof, a derivative thereof or a combination thereof chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs or compositions of hydrocodone which have a decreased potential for abuse of hydrocodone. 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苯基乙酸，苯基丙酸，苯基丙酸，其盐，其衍生物或其化合物与氢可酮（吗啡喃-6-酮，4,5-α-环氧-3-甲氧基-17- 甲基）以形成氢可酮的新药前体药物或组合物，其潜在滥用氢可酮的可能性降低。 本技术还提供了治疗患者的方法，药物试剂盒和本技术合成缀合物的方法。