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公开(公告)号：US20180338968A1
公开(公告)日：2018-11-29
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 , C07D221/28 , A61K47/54 , C07D489/08 , A61K47/55
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.
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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.
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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.
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公开(公告)号：US20170247368A1
公开(公告)日：2017-08-31
申请号：US15595358
申请日：2017-05-15
申请人： KemPharm, Inc.
发明人： Travis Mickle , Sven Guenther , Sanjib Bera
IPC分类号： C07D417/14 , C07D285/36 , A61K9/00 , C07D417/04 , A61K31/554 , A61K45/06
CPC分类号： A61K45/06 , A61K9/0053 , A61K31/554 , A61K39/39 , A61K47/542 , A61K47/543 , C07D285/36 , C07D417/04 , C07D417/14
摘要： The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating fatty acids to quetiapine. Pharmaceutical compositions and methods of synthesizing conjugates of the present technology are also provided. Methods of treating patients with the compositions of the present technology are also provided.
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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.
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16.发明申请FATTY ACID CONJUGATES OF QUETIAPINE, PROCESS FOR MAKING AND USING THE SAME 审中-公开脂肪酸与昆虫的结合，制备和使用它的方法公开(公告)号：US20170042906A1
公开(公告)日：2017-02-16
申请号：US15340533
申请日：2016-11-01
申请人： KemPharm, Inc.
发明人： Travis Mickle , Sven Guenther , Sanjib Bera
IPC分类号： A61K31/554 , A61K9/00 , A61K45/06 , A61K47/48
CPC分类号： A61K45/06 , A61K9/0053 , A61K31/554 , A61K39/39 , A61K47/542 , A61K47/543 , A61P25/18 , C07D285/36 , C07D417/04 , C07D417/14
摘要： The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating fatty acids to quetiapine. Pharmaceutical compositions and methods of synthesizing conjugates of the present technology are also provided. Methods of treating patients with the compositions of the present technology are also provided.
摘要翻译： 目前描述的技术提供了可以通过将脂肪酸与喹硫平化学偶联来合成的新一类喹硫平前药。 还提供了本技术合成缀合物的药物组合物和方法。 还提供了用本技术组合物治疗患者的方法。
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17.发明授权Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof 有权苯甲酸，苯甲酸衍生物和氢吗啡酮的杂芳基羧酸共轭物，前药，其制备方法和用途公开(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。
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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.
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19.发明授权Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof 有权苯甲酸，苯甲酸衍生物和氢吗啡酮的杂芳基羧酸共轭物，前药，其制备方法和用途公开(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。
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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.
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