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公开(公告)号：US08394365B2
公开(公告)日：2013-03-12
申请号：US11948767
申请日：2007-11-30
申请人： Xuan Zhao , Michael David Bentley , Zhongxu Ren , Tacey X. Viegas
发明人： Xuan Zhao , Michael David Bentley , Zhongxu Ren , Tacey X. Viegas
IPC分类号： A61K31/74
CPC分类号： A61K47/64 , A61K31/4709 , A61K31/4745 , A61K47/48192 , A61K47/48207 , A61K47/48215 , A61K47/4823 , A61K47/59 , A61K47/595 , A61K47/60 , A61K47/61 , C08G65/3314 , C08G65/3324 , C08G65/33317 , C08G65/3348 , C08L2203/02
摘要： Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
摘要翻译： 本文提供的是水溶性前药，包含这些前药的组合物，以及制备和施用该前药的相关方法。 本发明的前药包含具有三个或更多个臂的水溶性聚合物，其中至少三个通常共价连接到活性剂例如小分子上。 本发明的共轭物提供聚合物尺寸和结构的最佳平衡以实现改善的药物负载，因为本发明的缀合物具有可释放地连接到多臂水溶性聚合物上的三种或更多种活性剂。 与未修饰的母体药物相比，本发明的前药在治疗上是有效的，并且在体内表现出改善的性质。
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公开(公告)号：US20090074704A1
公开(公告)日：2009-03-19
申请号：US11948767
申请日：2007-11-30
申请人： Xuan Zhao , Michael David Bentley , Zhongxu Ren , Tacey X. Viegas
发明人： Xuan Zhao , Michael David Bentley , Zhongxu Ren , Tacey X. Viegas
IPC分类号： A61K47/48 , C08G65/329 , A61P35/04 , C08G63/91
CPC分类号： A61K47/64 , A61K31/4709 , A61K31/4745 , A61K47/48192 , A61K47/48207 , A61K47/48215 , A61K47/4823 , A61K47/59 , A61K47/595 , A61K47/60 , A61K47/61 , C08G65/3314 , C08G65/3324 , C08G65/33317 , C08G65/3348 , C08L2203/02
摘要： Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
摘要翻译： 本文提供的是水溶性前药，包含这些前药的组合物，以及制备和施用该前药的相关方法。 本发明的前药包含具有三个或更多个臂的水溶性聚合物，其中至少三个通常共价连接到活性剂例如小分子上。 本发明的共轭物提供聚合物尺寸和结构的最佳平衡以实现改善的药物负载，因为本发明的缀合物具有三种或更多种可释放地连接至多臂水溶性聚合物的活性剂。 本发明的前药在治疗上是有效的，并且与未修饰的母体药物相比在体内表现出改善的性质。
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公开(公告)号：US20100152414A1
公开(公告)日：2010-06-17
申请号：US12709800
申请日：2010-02-22
申请人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
发明人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
IPC分类号： C08G73/10
摘要： Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
摘要翻译： 本文提供水溶性前药。 本发明的前药包含具有三个或更多个臂的水溶性聚合物，其中至少三个共价连接到活性剂例如小分子上。 由于本发明的共轭物具有三种或更多种可释放地连接到多臂水溶性聚合物上的活性剂，本发明的共轭物提供聚合物尺寸和结构的最佳平衡以实现改善的药物负载。 与未修饰的母体药物相比，本发明的前药在治疗上是有效的，并且在体内表现出改善的性质。
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公开(公告)号：US08263062B2
公开(公告)日：2012-09-11
申请号：US12709800
申请日：2010-02-22
申请人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
发明人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
摘要： Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
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公开(公告)号：US07744861B2
公开(公告)日：2010-06-29
申请号：US10943799
申请日：2004-09-17
申请人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
发明人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
摘要： Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
摘要翻译： 本文提供水溶性前药。 本发明的前药包含具有三个或更多个臂的水溶性聚合物，其中至少三个共价连接到活性剂例如小分子上。 由于本发明的共轭物具有三种或更多种可释放地连接到多臂水溶性聚合物上的活性剂，本发明的共轭物提供聚合物尺寸和结构的最佳平衡以实现改善的药物负载。 与未修饰的母体药物相比，本发明的前药在治疗上是有效的，并且在体内表现出改善的性质。
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公开(公告)号：US08318145B2
公开(公告)日：2012-11-27
申请号：US12728072
申请日：2010-03-19
申请人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
发明人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
IPC分类号： A61K31/74
摘要： Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
摘要翻译： 本文提供水溶性前药。 本发明的前药包含具有三个或更多个臂的水溶性聚合物，其中至少三个共价连接到活性剂例如小分子上。 由于本发明的共轭物具有三种或更多种可释放地连接到多臂水溶性聚合物上的活性剂，本发明的共轭物提供聚合物尺寸和结构的最佳平衡以实现改善的药物负载。 与未修饰的母体药物相比，本发明的前药在治疗上是有效的，并且在体内表现出改善的性质。
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公开(公告)号：US20100190933A1
公开(公告)日：2010-07-29
申请号：US12728072
申请日：2010-03-19
申请人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
发明人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
IPC分类号： C08G69/48
摘要： Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
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公开(公告)号：US20080194612A1
公开(公告)日：2008-08-14
申请号：US12069727
申请日：2008-02-11
申请人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
发明人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
IPC分类号： A61K47/48 , A61K31/436
摘要： Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
摘要翻译： 本文提供水溶性前药。 本发明的前药包含具有三个或更多个臂的水溶性聚合物，其中至少三个共价连接到活性剂例如小分子上。 由于本发明的共轭物具有三种或更多种可释放地连接到多臂水溶性聚合物上的活性剂，本发明的共轭物提供聚合物尺寸和结构的最佳平衡以实现改善的药物负载。 与未修饰的母体药物相比，本发明的前药在治疗上是有效的，并且在体内表现出改善的性质。
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公开(公告)号：US08034825B2
公开(公告)日：2011-10-11
申请号：US12822935
申请日：2010-06-24
申请人： Michael D. Bentley , Tacey X. Viegas , Richard R. Goodin , Lin Cheng , Xuan Zhao
发明人： Michael D. Bentley , Tacey X. Viegas , Richard R. Goodin , Lin Cheng , Xuan Zhao
IPC分类号： A61K31/485 , C07D489/08
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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公开(公告)号：US07786133B2
公开(公告)日：2010-08-31
申请号：US11015196
申请日：2004-12-16
申请人： Michael D. Bentley , Tacey X. Viegas , Richard R. Goodin , Lin Cheng , Xuan Zhao
发明人： Michael D. Bentley , Tacey X. Viegas , Richard R. Goodin , Lin Cheng , Xuan Zhao
IPC分类号： A61K31/485 , C07D489/08
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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