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1.发明申请Compositions Comprising Enzyme-Cleavable Phenol-Modified Tapentadol Prodrug 有权组合物包含酶 - 可裂解酚改性的他喷他多前药公开(公告)号：US20130090379A1
公开(公告)日：2013-04-11
申请号：US13634530
申请日：2010-10-14
IPC分类号： A61K31/27 , C07C271/52
CPC分类号： A61K31/27 , A61K31/137 , A61K31/195 , C07C271/52 , C07C279/14 , A61K2300/00
摘要： A method of providing a patient with controlled release of tapentadol using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing tapentadol is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of tapentadol from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.
摘要翻译： 公开了一种使用能够在酶活化和分子内环化作用释放他喷他多的前药的患者给予他喷他多的控制释放的方法。 本公开还提供了这样的前药化合物和包含这些化合物的药物组合物。 这样的药物组合物可以任选地包括与酶相互作用的酶抑制剂，以介导来自该前药的酶促释放的他喷他多，以便修饰前药的酶裂解。 还包括使用这些化合物和药物组合物的方法。
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2.发明申请Compositions Comprising Enzyme-Cleavable Amphetamine Prodrugs and Inhibitors Thereof 审中-公开组合物，其中包括可酶切的安非他明前药及其抑制剂公开(公告)号：US20130059914A1
公开(公告)日：2013-03-07
申请号：US13634524
申请日：2011-04-08
IPC分类号： A61K31/197 , C07C279/14 , C12Q1/02 , C07C237/22 , A61K31/165
CPC分类号： A61K31/165 , A61K9/0019 , A61K9/0053 , A61K31/16 , A61K31/24 , A61K45/06 , A61K47/542 , A61K47/543 , C07C237/22 , C07C279/14 , A61K2300/00
摘要： Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an amphetamine prodrug that provides enzymatically-controlled release of amphetamine or an amphetamine analog. The composition can further comprise an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of amphetamine or the amphetamine analog from the amphetamine prodrug so as to attenuate enzymatic cleavage of the amphetamine prodrug.
摘要翻译： 提供药物组合物及其使用方法，其中药物组合物包含提供苯丙胺或苯丙胺类似物的酶控释放的安非他明前药。 该组合物可以进一步包含酶介导酶，其介导苯丙胺或苯丙胺类似物从苯丙胺前药的酶控释放，从而减弱苯丙胺前药的酶裂解。
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3.发明申请Compositions Comprising Enzyme-Cleavable Ketone-Modified Opioid Prodrugs and Optional Inhibitors Thereof 有权包含酶可克解酮改性阿片类前体药物及其任选的抑制剂的组合物公开(公告)号：US20120230916A1
公开(公告)日：2012-09-13
申请号：US13393470
申请日：2010-04-21
IPC分类号： A61K49/00 , C12Q1/37 , A61K31/495 , A61P25/00 , C07D489/08 , A61K31/485
CPC分类号： A61K31/485 , A61K31/445 , A61K31/495 , A61K38/05 , A61K47/54 , A61K47/542 , C07D489/02 , C07D489/08
摘要： A method of providing a patient with controlled release of ketone-containing opioid using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing the ketone-containing opioid is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of the ketone-containing opioid from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.
摘要翻译： 公开了一种使用能够在酶活化和分子内环化释放含酮阿片样物质的前体药物给予含酮类阿片样物质的受控释放的患者的方法。 本公开还提供了这样的前药化合物和包含这些化合物的药物组合物。 这样的药物组合物可以任选地包括与酶相互作用的酶抑制剂，以介导来自前体药物的含酮阿片样物质的酶控释放，从而修饰前药的酶裂解。 还包括使用这些化合物和药物组合物的方法。
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公开(公告)号：US20110281886A1
公开(公告)日：2011-11-17
申请号：US13121335
申请日：2009-10-16
IPC分类号： A61K31/485 , A61K31/496 , A61P29/00 , A61K31/495
CPC分类号： C07K5/06121 , A61K31/135 , A61K31/155 , A61K31/195 , A61K31/439 , A61K31/445 , A61K31/451 , A61K31/485 , A61K31/495 , A61K31/55 , A61K38/05 , A61K47/50 , A61K47/54 , A61K47/543 , A61K47/56 , C07C215/64 , C07C257/18 , C07C279/18 , C07C2603/80 , C07D211/66 , C07D217/04 , C07D221/26 , C07D223/04 , C07D295/185 , C07D491/08
摘要： Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
摘要翻译： 提供了药物组合物及其使用方法，其中药物组合物包含提供酚类阿片样物质的酶控释放的酚类阿片样物质前药，以及与介导酶促控制释放的酶相互作用的酶抑制剂 来自前药的酚类阿片样物质，以减轻前药的酶裂解。
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5.发明授权Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof 有权包含可酶切的酮修饰的阿片类前体药物及其任选的抑制剂的组合物公开(公告)号：US09493477B2
公开(公告)日：2016-11-15
申请号：US13393470
申请日：2010-04-21
IPC分类号： A01N43/42 , A61K31/44 , C07D489/02 , C07D489/08
CPC分类号： A61K31/485 , A61K31/445 , A61K31/495 , A61K38/05 , A61K47/54 , A61K47/542 , C07D489/02 , C07D489/08
摘要： A method of providing a patient with controlled release of ketone-containing opioid using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing the ketone-containing opioid is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of the ketone-containing opioid from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.
摘要翻译： 公开了一种使用能够在酶活化和分子内环化释放含酮阿片样物质的前体药物给予含酮类阿片样物质的受控释放的患者的方法。 本公开还提供了这样的前药化合物和包含这些化合物的药物组合物。 这样的药物组合物可以任选地包括与酶相互作用的酶抑制剂，以介导来自前体药物的含酮阿片样物质的酶控释放，从而修饰前药的酶裂解。 还包括使用这些化合物和药物组合物的方法。
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6.发明授权公开(公告)号：US08802681B2
公开(公告)日：2014-08-12
申请号：US13121335
申请日：2009-10-16
IPC分类号： A61K31/497 , A61K31/4965 , A61K31/44 , A61K31/485 , A61K31/155
CPC分类号： C07K5/06121 , A61K31/135 , A61K31/155 , A61K31/195 , A61K31/439 , A61K31/445 , A61K31/451 , A61K31/485 , A61K31/495 , A61K31/55 , A61K38/05 , A61K47/50 , A61K47/54 , A61K47/543 , A61K47/56 , C07C215/64 , C07C257/18 , C07C279/18 , C07C2603/80 , C07D211/66 , C07D217/04 , C07D221/26 , C07D223/04 , C07D295/185 , C07D491/08
摘要： Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
摘要翻译： 提供了药物组合物及其使用方法，其中药物组合物包含提供酚类阿片样物质的酶控释放的酚类阿片样物质前药，以及与介导酶促控制释放的酶相互作用的酶抑制剂 来自前药的酚类阿片样物质，以减轻前药的酶裂解。
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公开(公告)号：US20130089504A1
公开(公告)日：2013-04-11
申请号：US13634528
申请日：2010-10-14
IPC分类号： A61K31/439 , A61K31/496 , C07D489/02
CPC分类号： A61K31/439 , A61K31/4748 , A61K31/496 , C07D489/02 , C07D491/08 , Y10T436/142222
摘要： The embodiments provide Compound PC-5, [2-((S)-2-malonylamino-6-amino-hexanoyl amino)-ethyl]-ethyl-carbamic acid hydromorphone ester, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a prodrug, Compound PC-5, that provides enzymatically-controlled release of hydromorphone, and, optionally, a trypsin inhibitor that interacts with the enzyme that mediates the enzymatically-controlled release of hydromorphone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
摘要翻译： 实施方案提供化合物PC-5，[2 - （（S）-2-丙酰基氨基-6-氨基 - 己酰基氨基） - 乙基] - 乙基 - 氨基甲酸氢吗啉酯，或其可接受的盐，溶剂合物和水合物。 本公开还提供药物组合物及其使用方法，其中药物组合物包含前药，化合物PC-5，其提供酶促控制释放的氢吗啡酮，以及任选地与与介导的酶相互作用的胰蛋白酶抑制剂 氢吗啡酮从前药的酶促控制释放，以减弱前药的酶裂解。
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8.发明申请Compositions Comprising Enzyme-Cleavable Phenol-Modified Opioid Prodrugs and Inhibitors Thereof 审中-公开包含酶 - 可裂解酚改性阿片类前体药物及其抑制剂的组合物公开(公告)号：US20110262360A1
公开(公告)日：2011-10-27
申请号：US12764883
申请日：2010-04-21
CPC分类号： C12Q1/37 , A61K31/485 , A61K47/556
摘要： Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenol-modified opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the phenol-modified opioid prodrug so as to modify enzymatic cleavage of the phenol-modified opioid prodrug.
摘要翻译： 提供了药物组合物及其使用方法，其中药物组合物包含提供酚类阿片样物质的酶控释放的酚修饰的阿片样物质前药，以及与介导酶控制的酶相互作用的酶抑制剂 从苯酚修饰的阿片样物质前药释放酚类阿片样物质，以改变苯酚修饰的阿片样物质前药的酶裂解。
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9.发明授权Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug 有权包含可酶切的苯酚修饰的他喷他多前药的组合物公开(公告)号：US09238020B2
公开(公告)日：2016-01-19
申请号：US13634530
申请日：2010-10-14
IPC分类号： A61K31/137 , A61K31/195 , A61K31/27 , C07C271/52 , C07C279/14
CPC分类号： A61K31/27 , A61K31/137 , A61K31/195 , C07C271/52 , C07C279/14 , A61K2300/00
摘要： A method of providing a patient with controlled release of tapentadol using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing tapentadol is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of tapentadol from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.
摘要翻译： 公开了一种使用能够在酶促活化和分子内环化作用释放他喷他多的前药的患者给予他喷他多的控制释放的方法。 本公开还提供了这样的前药化合物和包含这些化合物的药物组合物。 这样的药物组合物可以任选地包括与酶相互作用的酶抑制剂，以介导来自该前药的酶促释放的他喷他多，以便修饰前药的酶裂解。 还包括使用这些化合物和药物组合物的方法。
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10.发明申请COMPOSITIONS COMPRISING ENZYME-CLEAVABLE PRODRUGS OF ACTIVE AGENTS AND INHIBITORS THEREOF 审中-公开包含有效药剂及其抑制剂的酶可清除产物的组合物公开(公告)号：US20110262359A1
公开(公告)日：2011-10-27
申请号：US12764879
申请日：2010-04-21
IPC分类号： A61K49/00 , C07D489/08 , C07D489/02 , A61P43/00 , C07K5/083 , A61P19/00 , A61P25/00 , A61K38/05 , G01N33/53 , A61K38/06 , A61K31/485 , A61P29/00
CPC分类号： A61K9/0002 , A61K31/485 , A61K38/00 , A61K47/556 , C07D489/02 , C07D489/08 , C07K5/06078 , C07K5/06095 , C12Q1/37
摘要： The present disclosure provides pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a prodrug that provides enzymatically-controlled release of a drug and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the drug from the prodrug so as to attenuate enzymatic cleavage of the prodrug. The disclosure provides pharmaceutical compositions which comprise an enzyme inhibitor and a prodrug that contains an enzyme-cleavable moiety that, when cleaved, facilitates release of the drug.
摘要翻译： 本公开提供了药物组合物及其使用方法，其中药物组合物包含提供酶控制释放的药物的前体药物和与介导酶控释放的酶的酶抑制剂相互作用的酶抑制剂 来自前药的药物，以减轻前药的酶裂解。 本公开提供了药物组合物，其包含酶抑制剂和前体药物，其包含可切割的部分，其在被切割时促进药物的释放。
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