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公开(公告)号：US20130053400A1
公开(公告)日：2013-02-28
申请号：US13568903
申请日：2012-09-07
IPC分类号： C07C217/44 , A61P37/00 , A61K31/495 , A61K31/135 , C07D295/088
CPC分类号： A61K31/137 , A61K31/495 , A61K47/60 , C07C217/48 , C07D295/088 , C07D295/15
摘要： The invention provides antihistamine drugs 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 characteristics of the antihistamine 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寡聚物进行化学修饰的抗组胺药物。 当通过多种施用途径中的任何一种施用时，本发明的缀合物显示出与未附着于水溶性低聚物的抗组胺药物的特征不同的特征。
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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：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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4.发明授权公开(公告)号：US06346272B1
公开(公告)日：2002-02-12
申请号：US08908747
申请日：1997-08-07
IPC分类号： A61K910
CPC分类号： A61K9/0048 , A61K9/0014 , A61K47/10 , A61K47/18 , A61K47/36 , 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.
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5.发明授权Ophthalmic drug delivery with thermoreversible polyoxyalkylene gels adjustable for pH 失效使用热可逆性聚氧化烯凝胶进行眼科药物输送可调节pH值
公开(公告)号：US5300295A
公开(公告)日：1994-04-05
申请号：US759234
申请日：1991-09-13
CPC分类号： A61K47/10 , A61K47/18 , A61K9/0048 , A61K9/06 , Y10S514/912 , Y10S514/944
摘要： Aqueous gel drug delivery compositions and medical devices, useful for treating an eye condition, having hyperosmotic, iso-osmotic or hypo-osmotic characteristics in the gel state, are obtained by calculating the osmolality required in the liquid state to reach a desired osmotic force in the gelled state by assuming that a polyoxyalkylene block copolymer does not contribute to the osmolality in the gel state.
摘要翻译： 通过计算在液体状态下达到期望的渗透压所需的重量摩尔渗透压浓度，可以获得在凝胶状态下具有高渗透性，渗透性或低渗透性的治疗眼睛状况的水凝胶药物递送组合物和医疗装置 通过假定聚氧化烯嵌段共聚物在凝胶状态下不影响重量摩尔渗透压浓度，则凝胶化状态。
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公开(公告)号：US20140371258A1
公开(公告)日：2014-12-18
申请号：US13995063
申请日：2011-12-16
IPC分类号： A61K47/48 , A61K31/4745
CPC分类号： A61K31/4745 , A61K47/60
摘要： Provided herein are water-soluble polymer conjugates of topotecan, along with compositions comprising the conjugates and related methods of making and using the same.
摘要翻译： 本文提供拓扑替康的水溶性聚合物共轭物，以及包含共轭物的组合物及其制备和使用它们的相关方法。
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公开(公告)号：US20110269677A1
公开(公告)日：2011-11-03
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： A61K38/05 , C07D213/56 , C07F9/655 , C07D401/06 , C07D239/10 , C07D401/12 , C07D217/26 , C07D417/12 , C07D405/12 , C07D493/04 , A61K31/635 , A61K31/4418 , A61K31/665 , A61K31/496 , A61K31/513 , A61K31/472 , A61K31/427 , A61K31/4433 , A61P31/18 , C07D307/20
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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公开(公告)号：US6136334A
公开(公告)日：2000-10-24
申请号：US330618
申请日：1999-06-11
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 , A61K31/74 , A61K9/50 , A61K31/765 , A61K31/785
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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公开(公告)号：US5376693A
公开(公告)日：1994-12-27
申请号：US604701
申请日：1990-10-26
IPC分类号： A61F9/008 , A61K9/00 , A61K47/10 , A61K47/18 , A61K47/36 , A61F2/14 , C08L5/04 , C08L71/02 , G02C7/04
CPC分类号： A61K9/0048 , A61K47/10 , A61K47/18 , A61K47/36 , A61F9/00819 , Y10S514/944 , 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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10.发明授权Topical drug delivery with polyoxyalkylene polymer thermoreversible gels adjustable for pH and osmolality 失效用聚氧亚烷基聚合物热可逆凝胶的局部药物递送可调节pH和重量摩尔渗透压浓度
公开(公告)号：US5298260A
公开(公告)日：1994-03-29
申请号：US895949
申请日：1992-06-09
CPC分类号： A61K9/0014 , A61K47/10 , A61K47/18 , Y10S514/944
摘要： Iso-osmotic, hyperosmotic, or hypo-osmotic, pH balanced, thermoreversible gels are ideal medical devices or vehicles for drug delivery to the skin of a mammal. The osmolality in the gel state can be calculated by assuming that a polyoxyalkylene block copolymer or polyether present in said gel does not contribute to the osmolality in the gel state, although it does contribute to the measured osmolality in the liquid state.
摘要翻译： 等渗，高渗或低渗，pH平衡的热可逆性凝胶是药物递送至哺乳动物皮肤的理想医疗装置或载体。 可以通过假定存在于所述凝胶中的聚氧化烯嵌段共聚物或聚醚对凝胶状态中的重量摩尔渗透压浓度没有贡献来计算凝胶状态下的重量摩尔渗透压浓度，尽管它确实有助于在液态中测量的重量摩尔渗透压浓度。
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