公开(公告)号：US10010615B2

公开(公告)日：2018-07-03

申请号：US15595374

申请日：2017-05-15

申请人： KemPharm, Inc.

发明人： Travis Mickle ,  Sven Guenther ,  Sanjib Bera

IPC分类号： A61K31/554 ,  A61K47/48

CPC分类号： A61K47/542 ,  A61K9/0053 ,  A61K31/553 ,  A61K31/554 ,  A61K45/06 ,  C07D267/18

摘要： The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.

公开(公告)号：US09872915B2

公开(公告)日：2018-01-23

申请号：US14816915

申请日：2015-08-03

申请人： KemPharm, Inc.

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

IPC分类号： A61K31/485 ,  A61K31/167 ,  A61K47/48 ,  C07D491/08 ,  C07D489/04 ,  A61K45/06 ,  A61K9/20

CPC分类号： A61K47/545 ,  A61K9/0019 ,  A61K9/20 ,  A61K9/2054 ,  A61K31/167 ,  A61K31/485 ,  A61K45/06 ,  A61K47/542 ,  A61K47/55 ,  A61K47/556 ,  A61P25/30 ,  C07D489/02 ,  C07D489/04 ,  C07D491/08 ,  A61K2300/00

摘要： The presently described technology provides methods of treating a patient having moderate to severe pain, narcotic or opioid abuse or narcotic or opioid withdrawal. The presently described methods are carried out by comprising administering to the patient a pharmaceutically effective amount of a composition comprising acetaminophen and benzoate-hydrocodone hydrochloride. The composition has reduced side effects when compared with unconjugated hydrocodone.

公开(公告)号：US09650387B2

公开(公告)日：2017-05-16

申请号：US15076586

申请日：2016-03-21

申请人： KemPharm, Inc.

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

IPC分类号： C07D489/04 ,  A61K31/485 ,  A61K31/167 ,  A61K45/06 ,  C07D489/02 ,  C07D491/08 ,  A61K9/00 ,  A61K47/48

CPC分类号： A61K47/545 ,  A61K9/0019 ,  A61K9/20 ,  A61K9/2054 ,  A61K31/167 ,  A61K31/485 ,  A61K45/06 ,  A61K47/542 ,  A61K47/55 ,  A61K47/556 ,  A61P25/30 ,  C07D489/02 ,  C07D489/04 ,  C07D491/08 ,  A61K2300/00

摘要： The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, 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.

公开(公告)号：US09566343B2

公开(公告)日：2017-02-14

申请号：US14336549

申请日：2014-07-21

申请人： KemPharm, Inc.

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

IPC分类号： A61K47/48 ,  A61K31/485 ,  A61K31/616 ,  A61K31/185 ,  C07D489/02

CPC分类号： A61K47/55 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0053 ,  A61K31/185 ,  A61K31/485 ,  A61K31/616 ,  A61K47/542

摘要： The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. 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与氢吗啡酮（4,5-α-环氧-3-羟基-17-甲基吗啡喃-6-酮）化学偶联的芳基羧酸的组合物，以形成氢吗啡酮的新型前药/组合物。 与未缀合的氢吗啡酮相比，本技术的氢吗啡酮前药具有降低的副作用和降低的滥用潜力。 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：US08927716B2

公开(公告)日：2015-01-06

申请号：US13888587

申请日：2013-05-07

申请人： KemPharm, Inc.

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

IPC分类号： C07D491/08 ,  A61K31/485 ,  C07D489/04 ,  A61K45/06 ,  A61K47/48

CPC分类号： A61K47/545 ,  A61K9/0019 ,  A61K9/20 ,  A61K9/2054 ,  A61K31/167 ,  A61K31/485 ,  A61K45/06 ,  A61K47/542 ,  A61K47/55 ,  A61K47/556 ,  A61P25/30 ,  C07D489/02 ,  C07D489/04 ,  C07D491/08 ,  A61K2300/00

摘要： The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, 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.

公开(公告)号：US08816083B2

公开(公告)日：2014-08-26

申请号：US13660112

申请日：2012-10-25

申请人： KemPharm, Inc.

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

IPC分类号： C07D489/02 ,  A61K31/625

CPC分类号： A61K47/55 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0053 ,  A61K31/185 ,  A61K31/485 ,  A61K31/616 ,  A61K47/542

摘要： The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. 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与氢吗啡酮（4,5-α-环氧-3-羟基-17-甲基吗啡喃-6-酮）化学偶联的芳基羧酸的组合物，以形成氢吗啡酮的新型前药/组合物。 与未缀合的氢吗啡酮相比，本技术的氢吗啡酮前药具有降低的副作用和降低的滥用潜力。 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：US08748413B2

公开(公告)日：2014-06-10

申请号：US13888578

申请日：2013-05-07

申请人： KemPharm, Inc.

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

IPC分类号： A61K45/06 ,  A61K31/485

CPC分类号： A61K47/545 ,  A61K9/0019 ,  A61K9/20 ,  A61K9/2054 ,  A61K31/167 ,  A61K31/485 ,  A61K45/06 ,  A61K47/542 ,  A61K47/55 ,  A61K47/556 ,  A61P25/30 ,  C07D489/02 ,  C07D489/04 ,  C07D491/08 ,  A61K2300/00

摘要： The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, 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.

公开(公告)号：US08715699B2

公开(公告)日：2014-05-06

申请号：US13518981

申请日：2010-12-22

申请人： Travis Mickle ,  Sven Guenther ,  Sanjib Bera

发明人： Travis Mickle ,  Sven Guenther ,  Sanjib Bera

IPC分类号： A61K31/554 ,  A61K9/00 ,  A61K33/00 ,  C07D417/04 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22

CPC分类号： A61K47/542 ,  A61K9/0053 ,  A61K31/553 ,  A61K31/554 ,  A61K45/06 ,  C07D267/18

摘要： The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.

摘要翻译： 目前描述的技术提供了可以通过将氨基酸与喹硫平化学偶联来合成的新一类喹硫平前药。 本技术还提供了治疗患者的方法，药物组合物和本技术合成缀合物的方法。

公开(公告)号：US20220064116A1

公开(公告)日：2022-03-03

申请号：US17500680

申请日：2021-10-13

申请人： KemPharm, Inc.

发明人： Sven Guenther ,  Guochen Chi ,  Travis Mickle

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

摘要： Disclosed are d-amphetamine compounds and compositions comprising at least one organic acid covalently bound to d-amphetamine, having the structure of 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：US11021460B2

公开(公告)日：2021-06-01

申请号：US16577946

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 ,  C07D401/12 ,  C07D211/34 ,  A61K31/4458

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.