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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：US20100210505A1
公开(公告)日：2010-08-19
申请号：US12086687
申请日：2006-12-18
IPC分类号： A61K38/22 , C07K14/575 , A61K38/28 , A61P3/10
CPC分类号： C07K17/08 , A61K47/60 , C07K14/605
摘要： Conjugates of a GLP-I moiety may be covalently attached to one or more water-soluble polymers. For instance, a GLP-I polymer conjugate may include a GLP-I moiety releasably attached at its N-terminus to a water-soluble polymer. The GLP-I polymer conjugate may include a GLP-I moiety covalently attached to a water-soluble polymer, wherein the GLP-I moiety possesses an N-methyl substituent. The GLP-I polymer conjugate may include a GLP-I moiety covalently attached at a polymer attachment site to a water-soluble polymer, wherein the GLP-I moiety is glycosylated at a site separate from the polymer attachment site.
摘要翻译： GLP-1部分的缀合物可以共价连接到一种或多种水溶性聚合物上。 例如，GLP-1聚合物缀合物可以包括其N-末端可释放地连接到水溶性聚合物上的GLP-1部分。 GLP-1聚合物缀合物可以包括与水溶性聚合物共价连接的GLP-1部分，其中GLP-1部分具有N-甲基取代基。 GLP-1聚合物缀合物可以包括在聚合物附着位点共价连接到水溶性聚合物上的GLP-1部分，其中GLP-1部分在与聚合物附着部位分开的位置被糖基化。
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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：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：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：US5847023A
公开(公告)日：1998-12-08
申请号：US552973
申请日：1995-11-03
CPC分类号： A61K47/10 , A61K47/18 , A61K47/36 , A61K9/0048 , Y10S524/916 , Y10S525/937
摘要： Balanced pH, thermo-irreversible gels comprising a polyoxyalkylene compound and an ionic polysaccharide are ideal materials for the formation of a protective contact lens over the cornea of the eye of a mammal.
摘要翻译： 包含聚氧化烯化合物和离子多糖的平衡pH，热不可逆凝胶是在哺乳动物眼睛的角膜上形成保护性隐形眼镜的理想材料。
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公开(公告)号：US5587175A
公开(公告)日：1996-12-24
申请号：US174101
申请日：1993-12-28
IPC分类号： A61F9/008 , A61K9/00 , A61L15/22 , A61L15/44 , A61L24/00 , A61L24/04 , A61L27/26 , A61L27/52 , A61L27/54 , A61L31/04 , A61L31/16 , A61K31/77 , A61K31/725 , A61K31/73 , A61K2/14
CPC分类号： A61L31/16 , A61F9/00819 , A61K9/0048 , A61L15/225 , A61L15/44 , A61L24/0015 , A61L24/0031 , A61L24/043 , A61L27/26 , A61L27/52 , A61L27/54 , A61L31/041 , A61F2009/00872 , A61L2300/00 , A61L2430/16 , Y10S514/912 , Y10S514/913 , Y10S514/914 , Y10S514/944 , Y10S514/966 , Y10S514/967 , Y10S623/905
摘要： Balanced pH, hyperosmotic, hypoosmotic, or isoosmotic gels are ideal vehicles for drug delivery. They are especially suited for topical body cavity or injection application of drugs or diagnostic agents; for drug or diagnostic agent delivery to the eye of a mammal; as protective corneal shields; or as ablatable corneal masks useful in laser reprofiling of the cornea. The compositions without the addition of a drug or diagnostic agent are useful as medical devices, for instance, in separating surgically or otherwise injured tissue as a means of preventing adhesions.
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18.发明授权Body cavity drug delivery with thermo-irreversible polyoxyalkylene and ionic polysaccharide gels 失效体腔药物递送与热不可逆的聚氧化烯和离子多糖凝胶
公开(公告)号：US5346703A
公开(公告)日：1994-09-13
申请号：US939475
申请日：1992-08-31
CPC分类号： A61K9/0048 , A61K47/10 , A61K47/18 , A61K47/36 , A61K9/0014 , Y10S514/944 , Y10S514/966 , Y10S514/967
摘要： Balanced pH, thermo-irreversible gels are ideal vehicles for drug delivery to a body cavity of a mammal. The gels contain a mixture of a polyoxyalkylene block copolymer or polyether together with an ionic polysaccharide which is thermo-irreversibly gelled in the presence of a counter-ion.
摘要翻译： 平衡的pH，热不可逆凝胶是药物递送到哺乳动物体腔的理想载体。 凝胶含有聚氧化烯嵌段共聚物或聚醚与在抗衡离子存在下不可逆地凝胶化的离子多糖的混合物。
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19.发明授权Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide 失效具有聚氧亚氨基聚合物和离子多糖的热不可逆凝胶的眼药物递送
公开(公告)号：US5077033A
公开(公告)日：1991-12-31
申请号：US563638
申请日：1990-08-07
CPC分类号： A61K9/0048 , A61K47/10 , A61K47/18 , A61K47/36 , A61F9/00819 , Y10S514/912 , Y10S514/913 , Y10S514/914 , Y10S514/944 , Y10S525/916
摘要： Balanced pH, thermo-irreversible gels are ideal vehicles for drug delivery to the eye of a mammal.
摘要翻译： 平衡的pH，热不可逆凝胶是药物输送到哺乳动物眼睛的理想载体。
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公开(公告)号：US08598364B2
公开(公告)日：2013-12-03
申请号：US12530363
申请日：2008-03-12
申请人： Jennifer Riggs-Sauthier , Lin Cheng , Tacey X. Viegas , Xuyuan Gu , Franco J. Duarte , Wen Zhang
发明人： Jennifer Riggs-Sauthier , Lin Cheng , Tacey X. Viegas , Xuyuan Gu , Franco J. Duarte , Wen Zhang
IPC分类号： C07D239/02 , C07D401/00 , C07D217/00 , C07D405/00 , C07D213/00 , C07D277/30 , C07D493/00 , C07D307/02 , C07F9/28 , C07F9/06
CPC分类号： A61K47/48215 , A61K47/60
摘要： The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors 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蛋白酶抑制剂。 本发明的缀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蛋白酶抑制剂不同的特征。
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