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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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5.发明申请Multifunctional Forms of Polyoxazoline Copolymers and Drug Compositions Comprising the Same 有权多官能团形式的聚恶唑啉共聚物和药物组合物组成公开(公告)号：US20120123055A1
公开(公告)日：2012-05-17
申请号：US13356552
申请日：2012-01-23
IPC分类号： C08G73/02
CPC分类号： A61K47/48207 , A61K38/09 , A61K47/59 , C08G73/0233
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
摘要翻译： 本公开提供了具有两个或三个也是化学正交的反应性官能团的2-取代-2-恶唑啉的共聚物。 所述共聚物可以是无规共聚物，嵌段共聚物或无规嵌段共聚物构型的混合物。 此外，本公开提供了用于合成上述聚合物并用于与靶标，诊断和治疗剂等分子缀合的新方法。
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6.发明授权公开(公告)号：US08101706B2
公开(公告)日：2012-01-24
申请号：US12787241
申请日：2010-05-25
CPC分类号： A61K47/48207 , A61K38/09 , A61K47/59 , C08G73/0233
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
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7.发明申请Multifunctional Forms of Polyoxazoline Copolymers and Drug Compositions Comprising the Same 有权多官能团形式的聚恶唑啉共聚物和药物组合物组成公开(公告)号：US20100330023A1
公开(公告)日：2010-12-30
申请号：US12787241
申请日：2010-05-25
IPC分类号： A61K31/785 , A61P35/00
CPC分类号： A61K47/48207 , A61K38/09 , A61K47/59 , C08G73/0233
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
摘要翻译： 本公开提供了具有两个或三个也是化学正交的反应性官能团的2-取代-2-恶唑啉的共聚物。 所述共聚物可以是无规共聚物，嵌段共聚物或无规嵌段共聚物构型的混合物。 此外，本公开提供了用于合成上述聚合物并用于与靶标，诊断和治疗剂等分子缀合的新方法。
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8.发明授权公开(公告)号：US08501899B2
公开(公告)日：2013-08-06
申请号：US13356552
申请日：2012-01-23
CPC分类号： A61K47/48207 , A61K38/09 , A61K47/59 , C08G73/0233
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
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公开(公告)号：US08383093B1
公开(公告)日：2013-02-26
申请号：US13524994
申请日：2012-06-15
申请人： Randall Moreadith , Michael David Bentley , Kunsang Yoon , Zhihao Fang , Rebecca Weimer , Bekir Dizman , Tacey Viegas
发明人： Randall Moreadith , Michael David Bentley , Kunsang Yoon , Zhihao Fang , Rebecca Weimer , Bekir Dizman , Tacey Viegas
IPC分类号： A61K31/00
CPC分类号： A61K47/48192 , A61K9/0019 , A61K31/381 , A61K31/4045 , A61K31/4462 , A61K31/4535 , A61K31/4745 , A61K31/7048 , A61K47/542 , A61K47/60 , A61K47/61
摘要： The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a hydrolyzable moiety.
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公开(公告)号：US20050136031A1
公开(公告)日：2005-06-23
申请号：US11015196
申请日：2004-12-16
申请人： Michael Bentley , Tacey Viegas , Richard Goodin , Lin Cheng , Xuan Zhao
发明人： Michael Bentley , Tacey Viegas , Richard Goodin , Lin Cheng , Xuan Zhao
IPC分类号： A61K31/765 , A61K31/785 , A61K47/48 , C08G65/08
CPC分类号： C08G65/337 , A61K47/60 , C08G65/332 , C08G65/33317 , C08G65/33396 , C08L2203/02
摘要： The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a monodisperse or bimodal water-soluble oligomer composition. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water-soluble oligomer.
摘要翻译： 本发明提供了通过共价连接由单分散或双峰水溶性低聚物组合物获得的水溶性低聚物进行化学修饰的小分子药物。 当与多种施用途径中的任何一种施用时，本发明的缀合物与未附着于水溶性低聚物的小分子药物的生物膜交联率相比，显示出降低的生物膜交叉率。
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