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公开(公告)号：US20100210676A1
公开(公告)日：2010-08-19
申请号：US12710167
申请日：2010-02-22
申请人： C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
发明人： C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
IPC分类号： A61K31/485 , A61P25/36
CPC分类号： A61K9/007 , A61K31/167 , A61K31/485 , A61K47/60 , C07C41/24
摘要： Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.
摘要翻译： 通过肺途径改变施用于受试者的药物的全身吸收速率的方法，所述方法包括将亲水性聚合物与药物共价共轭，其中所述药物具有从肺中消除的半衰期小于约180 分钟，以形成药物 - 聚合物缀合物，其中药物 - 聚合物缀合物具有净亲水特性和约50至约20,000道尔顿的重均分子量，并且其中从药物的肺中消除的半衰期 - 聚合物缀合物比从药物肺消除的半衰期大至少约1.5倍，其中通过支气管肺泡灌洗测量肺部消除的半衰期，然后测定残留的肺部材料。
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公开(公告)号：US20120088745A1
公开(公告)日：2012-04-12
申请号：US13271158
申请日：2011-10-11
申请人： C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
发明人： C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
IPC分类号： A61K31/16 , C07D489/08 , C07C43/13 , C07J5/00 , A61K31/573 , C07C233/21 , A61K31/485
CPC分类号： A61K9/007 , A61K31/167 , A61K31/485 , A61K47/60 , C07C41/24
摘要： Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.
摘要翻译： 通过肺途径改变施用于受试者的药物的全身吸收速率的方法，所述方法包括将亲水性聚合物与药物共价共轭，其中所述药物具有从肺中消除的半衰期小于约180 分钟，以形成药物 - 聚合物缀合物，其中药物 - 聚合物缀合物具有净亲水特性和约50至约20,000道尔顿的重均分子量，并且其中从药物的肺中消除的半衰期 - 聚合物缀合物比从药物肺消除的半衰期大至少约1.5倍，其中通过支气管肺泡灌洗测量肺部消除的半衰期，然后测定残留的肺部材料。
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公开(公告)号：US08067431B2
公开(公告)日：2011-11-29
申请号：US12710167
申请日：2010-02-22
申请人： C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
发明人： C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
IPC分类号： A61K31/485 , C07D489/08
CPC分类号： A61K9/007 , A61K31/167 , A61K31/485 , A61K47/60 , C07C41/24
摘要： Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.
摘要翻译： 通过肺途径改变施用于受试者的药物的全身吸收速率的方法，所述方法包括将亲水性聚合物与药物共价共轭，其中所述药物具有从肺中消除的半衰期小于约180 分钟，以形成药物 - 聚合物缀合物，其中药物 - 聚合物缀合物具有净亲水特性和约50至约20,000道尔顿的重均分子量，并且其中从药物的肺中消除的半衰期 - 聚合物缀合物比从药物肺消除的半衰期大至少约1.5倍，其中通过支气管肺泡灌洗测量肺部消除的半衰期，然后测定残留的肺部材料。
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公开(公告)号：US20060182692A1
公开(公告)日：2006-08-17
申请号：US11344404
申请日：2006-01-30
申请人： C. Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
发明人： C. Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
CPC分类号： A61K9/007 , A61K31/167 , A61K31/485 , A61K47/60 , C07C41/24
摘要： Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.
摘要翻译： 通过肺途径改变施用于受试者的药物的全身吸收速率的方法，所述方法包括将亲水性聚合物与药物共价共轭，其中所述药物具有从肺中消除的半衰期小于约180 分钟，以形成药物 - 聚合物缀合物，其中药物 - 聚合物缀合物具有净亲水特性和约50至约20,000道尔顿的重均分子量，并且其中从药物的肺中消除的半衰期 - 聚合物缀合物比从药物肺消除的半衰期大至少约1.5倍，其中通过支气管肺泡灌洗测量肺部消除的半衰期，然后测定残留的肺部材料。
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公开(公告)号：US20130317114A1
公开(公告)日：2013-11-28
申请号：US13992587
申请日：2011-12-09
IPC分类号： C07C217/52
CPC分类号： C07C217/52
摘要： The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water-soluble oligomer.
摘要翻译： 本发明提供通过共价连接水溶性低聚物进行化学修饰的小分子药物。 本发明化合物当通过多种施用途径中的任一种施用时，显示出与未附着于水溶性低聚物的小分子药物的特性不同的特征。
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公开(公告)号：US20110237614A1
公开(公告)日：2011-09-29
申请号：US13063919
申请日：2009-09-16
IPC分类号： A61K31/485 , A61P25/36 , A61P25/04 , C07D489/02
CPC分类号： A61K31/485 , A61K47/60
摘要： The invention provides opioid agonists covalently bound to a water-soluble oligomer having reduced potential for substance abuse and uses thereof. The compounds of the invention possess altered pharmacokinetic profiles relative to the opioid agonists alone, but are not subject to the risk of physical tampering that allows for the recovery and abuse of the opioid agonist associated with certain alternative delivery formulations.
摘要翻译： 本发明提供了与具有降低的药物滥用潜力的水溶性低聚物共价结合的阿片样物质激动剂及其应用。 本发明的化合物相对于单独的阿片样物质激动剂具有改变的药代动力学特征，但不具有物理篡改的风险，其允许与某些替代递送制剂相关的阿片样物质激动剂的恢复和滥用。
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公开(公告)号：US11033631B2
公开(公告)日：2021-06-15
申请号：US12993807
申请日：2009-06-09
IPC分类号： A61K31/155 , A61K31/145 , A61K8/43 , A61K47/60 , A61P9/12
摘要： The invention provides various methods comprising the administration of a CYP2D6 bioactive drug covalently bound to a water-soluble oligomer. Metabolism of CYP2D6 bioactive drug conjugates is diverted from CYP2D6 to alternative pathways, and the conjugates may therefore be utilized to alleviate the problems associated with interpopulation variation resulting from the genetic polymorphism in the CYP2D6 gene.
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公开(公告)号：US09090535B2
公开(公告)日：2015-07-28
申请号：US13992587
申请日：2011-12-09
IPC分类号： C07C217/52 , C07C217/54 , A61K31/137 , A61P25/08 , A61P25/24
CPC分类号： C07C217/52
摘要： The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water-soluble oligomer.
摘要翻译： 本发明提供通过共价连接水溶性低聚物进行化学修饰的小分子药物。 本发明化合物当通过多种施用途径中的任一种施用时，显示出与未附着于水溶性低聚物的小分子药物的特性不同的特征。
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9.发明申请公开(公告)号：US20130023553A1
公开(公告)日：2013-01-24
申请号：US13521556
申请日：2011-01-12
IPC分类号： C07D489/02 , A61P25/36 , A61P25/00 , A61K31/485
CPC分类号： A61K31/075 , A61K31/485
摘要： Provided are methods for reducing the addiction potential and/or reducing one or more CNS-side effects related to the administration of an opioid analgesic drug by administering the opioid analgesic drug in the form of an oligomeric polyethylene glycol conjugate compound. The compounds provided demonstrate notably reduced potential for substance abuse, and possess altered pharmacokinetic profiles relative to the opioid agonists alone, but are not subject to the risk of physical tampering that allows for the recovery and abuse of the opioid agonist associated with certain alternative delivery formulations.
摘要翻译： 提供了通过以寡聚聚乙二醇缀合化合物的形式施用阿片样物质止痛药，降低成瘾潜能和/或降低与阿片类止痛药的给药有关的一种或多种CNS副作用的方法。 所提供的化合物显示出显着降低药物滥用的潜力，并且相对于单独的阿片样物质激动剂具有改变的药代动力学特征，但不具有物理篡改的风险，其允许与某些替代递送制剂相关的阿片样物质激动剂的恢复和滥用 。
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公开(公告)号：US20110160186A1
公开(公告)日：2011-06-30
申请号：US12993807
申请日：2009-06-09
IPC分类号： A61K31/55 , A61K31/135 , A61K31/495 , C12Q1/26 , A61K31/472 , A61K31/138 , A61K31/5377 , C07D217/04 , C07C215/28 , C07D417/04 , C07D295/088 , C07D223/28 , A61P3/00
CPC分类号： A61K47/60
摘要： The invention provides various methods comprising the administration of a CYP2D6 bioactive drug covalently bound to a water-soluble oligomer. Metabolism of CYP2D6 bioactive drug conjugates is diverted from CYP2D6 to alternative pathways, and the conjugates may therefore be utilized to alleviate the problems associated with interpopulation variation resulting from the genetic polymorphism in the CYP2D6 gene.
摘要翻译： 本发明提供包括施用与水溶性低聚物共价结合的CYP2D6生物活性药物的各种方法。 CYP2D6生物活性药物偶联物的代谢从CYP2D6转向替代途径，因此可以利用缀合物来减轻CYP2D6基因遗传多态性引起的人口间变异相关的问题。
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