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公开(公告)号：US08461137B2
公开(公告)日：2013-06-11
申请号：US12828381
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： A61K45/06 , A61K31/485 , A61K47/48038
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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2.发明申请Phenylethanoic Acid, Phenylpropanoic Acid and Phenylpropenoic Acid Conjugates and Prodrugs of Hydrocodone, Methods of Making and Use Thereof 审中-公开苯乙酸，苯丙酸和苯丙酸接头物和氢可酮的前药，其制备和使用方法公开(公告)号：US20120142720A1
公开(公告)日：2012-06-07
申请号：US13378857
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 , A61P25/04 , A61P25/36 , C07D489/04
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。
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3.发明授权Phenylethanoic acid, phenylpropanoic acid and phenylpropenoic acid conjugates and prodrugs of hydrocodone, method of making and use thereof 有权苯基乙酸，苯基丙酸和苯基丙酸共轭物和氢可酮的前体药物，其制备方法和用途公开(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。
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4.发明申请PHENYLETHANOIC ACID, PHENYLPROPANOIC ACID AND PHENYLPROPENOIC ACID CONJUGATES AND PRODRUGS OF HYDROCODONE, METHOD OF MAKING AND USE THEREOF 有权苯乙酸，苯甲酸，苯丙酸和苯并三唑酸的共聚物及其制备方法及其应用公开(公告)号：US20110002991A1
公开(公告)日：2011-01-06
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： A61K9/28 , C07D489/04 , A61K31/485 , A61P29/00 , A61P25/36 , A61P25/30
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。
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公开(公告)号：US08759368B2
公开(公告)日：2014-06-24
申请号：US13378800
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
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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6.发明申请BENZOIC ACID, BENZOIC ACID DERIVATIVES AND HETEROARYL CARBOXYLIC ACID CONJUGATES OF HYDROCODONE, PRODRUGS, METHODS OF MAKING AND USE THEREOF 有权苯甲酸，苯甲酸衍生物和羟基苯甲酸羧酸共聚物，制备方法及其制备方法及用途公开(公告)号：US20110002990A1
公开(公告)日：2011-01-06
申请号：US12828381
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： A61K9/28 , C07D489/04 , A61K31/485 , A61K31/60 , A61K31/609 , A61K31/616 , A61P25/36 , A61P29/00 , A61P25/30
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.
摘要翻译： 目前描述的技术提供包含与氢可酮（吗啡喃-6-酮，4,5-α-环氧-3-甲氧基-17-甲基）化学偶联的芳基羧酸的组合物，以形成新的前药/氢可酮组合物，包括苯甲酸酯和杂芳基 羧酸，其潜在的潜在滥用氢可酮。 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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7.发明申请Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof 有权苯酮，苯甲酸衍生物和氢可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：US20120142719A1
公开(公告)日：2012-06-07
申请号：US13378800
申请日：2010-07-01
申请人： Travis Mickle , Sven Guenther , Christal Mickle , Guochen Chi , Jaroslaw Kansi , Andrea K. Martin , Bindu Bera
发明人： Travis Mickle , Sven Guenther , Christal Mickle , Guochen Chi , Jaroslaw Kansi , Andrea K. Martin , Bindu Bera
IPC分类号： A61K31/485 , A61P25/36 , A61P25/00 , C07D489/00
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.
摘要翻译： 目前描述的技术提供包含与氢可酮（吗啡喃-6-酮，4,5-α-环氧-3-甲氧基-17-甲基）化学偶联的芳基羧酸的组合物，以形成新的前药/氢可酮组合物，包括苯甲酸酯和杂芳基 羧酸，其潜在的潜在滥用氢可酮。 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：US20190142815A1
公开(公告)日：2019-05-16
申请号：US16244460
申请日：2019-01-10
申请人： Sven Guenther , Guochen Chi , Bindu Bera , Travis Mickle , Sanjib Bera
发明人： Sven Guenther , Guochen Chi , Bindu Bera , Travis Mickle , Sanjib Bera
IPC分类号： A61K31/4458 , C07F9/59 , A61K47/64 , A61K47/54 , C07D211/34 , A61K9/00 , C07K5/062 , C07K5/02 , C07D401/12 , A61K47/60
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.
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9.发明授权Methylphenidate-oxoacid conjugates, processes of making and using the same 有权哌甲酯 - 含氧酸共轭物，制备和使用它们的方法公开(公告)号：US09079928B2
公开(公告)日：2015-07-14
申请号：US14234440
申请日：2012-07-27
申请人： Sven Guenther , Guochen Chi , Bindu Bera , Travis Mickle , Sanjib Bera
发明人： Sven Guenther , Guochen Chi , Bindu Bera , Travis Mickle , Sanjib Bera
IPC分类号： C07D211/68 , C07D211/60 , C07F9/59 , A61K47/48 , C07D211/34 , C07K5/02 , C07K5/062 , C07D401/12
CPC分类号： A61K31/4458 , A61K9/0053 , A61K47/542 , A61K47/545 , A61K47/548 , A61K47/60 , A61K47/64 , C07D211/34 , C07D401/12 , C07F9/59 , C07K5/0202 , C07K5/06026
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.
摘要翻译： 本技术涉及用于治疗与至少一种醇，胺，含氧酸，硫醇或其衍生物缀合的哌甲酯或哌甲酯衍生物的各种疾病和/或病症的前药和组合物。 在一些实施方案中，缀合物还包括至少一个接头。 本技术还涉及与至少一种醇，胺，含氧酸，硫醇或其衍生物或其组合缀合的哌甲酯或哌甲酯衍生物的合成。
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10.发明申请METHYLPHENIDATE-OXOACID CONJUGATES, PROCESSES OF MAKING AND USING THE SAME 有权亚甲基 - 氧化物偶联物，制备和使用它们的方法公开(公告)号：US20140243291A1
公开(公告)日：2014-08-28
申请号：US14234440
申请日：2012-07-27
申请人： Sven Guenther , Guochen Chi , Bindu Bera , Travis Mickle
发明人： Sven Guenther , Guochen Chi , Bindu Bera , Travis Mickle
IPC分类号： C07F9/59 , C07D211/34 , C07D401/12
CPC分类号： A61K31/4458 , A61K9/0053 , A61K47/542 , A61K47/545 , A61K47/548 , A61K47/60 , A61K47/64 , C07D211/34 , C07D401/12 , C07F9/59 , C07K5/0202 , C07K5/06026
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.
摘要翻译： 本技术涉及用于治疗与至少一种醇，胺，含氧酸，硫醇或其衍生物缀合的哌甲酯或哌甲酯衍生物的各种疾病和/或病症的前药和组合物。 在一些实施方案中，缀合物还包括至少一个接头。 本技术还涉及与至少一种醇，胺，含氧酸，硫醇或其衍生物或其组合缀合的哌甲酯或哌甲酯衍生物的合成。
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