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31. 发明授权

US09199954B2 Non-ring hydroxy substituted taxanes and methods for synthesizing the same 有权
标题翻译：非环羟基取代的紫杉烷及其合成方法
公开(公告)号：US09199954B2
公开(公告)日：2015-12-01
申请号：US13995445
申请日：2011-12-22
申请人： Antoni Kozlowski , Samuel P. McManus
发明人： Antoni Kozlowski , Samuel P. McManus
IPC分类号： C07D305/00 , C07D305/14 , C07D305/06
CPC分类号： C07D305/14 , C07D305/06
摘要： The invention relates to (among other things) non-ring hydroxy substituted taxanes and methods for synthesizing the same. The invention further relates to conjugating the non-ring hydroxyl substituted taxanes to a water-soluble, non-peptidic polymer.
摘要翻译：本发明涉及（尤其是）非环羟基取代的紫杉烷类及其合成方法。本发明还涉及将非环羟基取代的紫杉烷与水溶性非肽聚合物缀合。

32. 发明授权

US09085659B2 Polymer derivatives comprising an imide branching point 有权
标题翻译：包含酰亚胺支化点的聚合物衍生物
公开(公告)号：US09085659B2
公开(公告)日：2015-07-21
申请号：US11579475
申请日：2005-05-03
申请人： Samuel P. McManus , Antoni Kozlowski
发明人： Samuel P. McManus , Antoni Kozlowski
IPC分类号： C08G65/08 , C08G69/08 , C07D207/46 , A61K47/48 , C08G65/333 , C08G73/08 , C08G73/10 , C08G73/12
CPC分类号： C08G65/33331 , A61K47/60 , A61K47/6903 , C08G73/08 , C08G73/1092 , C08G73/12
摘要： The invention provides a water-soluble polymer comprising (i) an imide group comprising a linking nitrogen atom, a first carbonyl group covalently attached to the linking nitrogen atom, and a second carbonyl group covalently attached to the linking nitrogen atom; (ii) a first water-soluble polymer segment covalently attached, either directly or through one or more atoms, to the first carbonyl group of the imide group and (iii) a second water-soluble polymer segment covalently attached, either directly or through one or more atoms, to the second carbonyl group of the imide group. The invention also provides, among other things, methods for preparing polymers, conjugates, pharmaceutical compositions and the like.
摘要翻译：本发明提供一种水溶性聚合物，其包含（i）包含连接氮原子的酰亚胺基团，共价连接到连接氮原子上的第一羰基和共价连接到连接氮原子上的第二羰基; （ii）直接或通过一个或多个原子共价连接到酰亚胺基团的第一个羰基的第一个水溶性聚合物链段和（iii）直接或通过一个共价连接的第二个水溶性聚合物链段以上的原子与酰亚胺基的第二个羰基反应。本发明还提供了制备聚合物，共轭物，药物组合物等的方法。

33. 发明授权

US08604159B2 Method for preparing functionalized polymers from polymer alcohols 有权
标题翻译：从聚合物醇制备官能化聚合物的方法
公开(公告)号：US08604159B2
公开(公告)日：2013-12-10
申请号：US10897386
申请日：2004-07-22
申请人： Samuel P. McManus , Antoni Kozlowski , J. Milton Harris
发明人： Samuel P. McManus , Antoni Kozlowski , J. Milton Harris
IPC分类号： C08G65/34 , A61K31/74 , A61K47/48 , C08G63/48 , C08G63/91 , C08L89/00
CPC分类号： C08G65/33337 , A61K47/60 , B01D15/361 , C08G65/00 , C08G65/30 , C08G65/322 , C08G65/323 , C08G65/329 , C08G65/3322 , C08G65/33306 , C08G65/33365 , C08G65/48 , C08G2650/38 , C08L2203/02
摘要： The present invention provides, among other things, methods for preparing functionalized and other polymers from polymer from polymer alcohols such as poly(ethylene glycol)s. In addition, polymer compositions, conjugates, polymeric reagents, are also provided.
摘要翻译：本发明尤其提供了从聚合物醇如聚（乙二醇）的聚合物制备官能化和其它聚合物的方法。此外，还提供了聚合物组合物，共轭物，聚合物试剂。

34. 发明授权

US08562965B2 Polymer derivatives comprising an acetal or ketal branching point 有权
标题翻译：包含缩醛或缩酮分支点的聚合物衍生物
公开(公告)号：US08562965B2
公开(公告)日：2013-10-22
申请号：US11579465
申请日：2005-05-03
申请人： Samuel P. McManus , Antoni Kozlowski
发明人： Samuel P. McManus , Antoni Kozlowski
IPC分类号： A61K47/48 , C08G65/02 , C08G73/06
CPC分类号： A61K47/48215 , A61K47/60 , C08G65/322 , C08G65/329 , C08G65/331 , C08G65/33306 , C08G65/33337 , C08G65/3348 , C08L2203/02
摘要： The invention provides a polymer comprising (i) a first water-soluble polymer segment that is covalently attached, either directly or through one or more atoms, to a first oxygen atom that is covalently attached to a linking carbon atom; (ii) a second water-soluble polymer segment is covalently attached, either directly or through one or more atoms, to a second oxygen atom that is covalently attached to the linking carbon atom; and (iii) a reactive group that is covalently attached, either directly or through one or more atoms, to the linking carbon atom. The invention also provides, among other things, methods for preparing polymers, conjugates, pharmaceutical compositions and the like.
摘要翻译：本发明提供一种聚合物，其包含（i）直接或通过一个或多个原子共价连接到共价连接到连接碳原子上的第一个氧原子的第一个水溶性聚合物链段; （ii）第二个水溶性聚合物链段直接或通过一个或多个原子共价连接到共价连接到连接碳原子上的第二个氧原子; 和（iii）直接或通过一个或多个原子共价连接到连接碳原子上的反应性基团。本发明还提供了制备聚合物，共轭物，药物组合物等的方法。

35. 发明授权

US08440787B2 Hydroxyapatite-targeting multiarm polymers and conjugates made therefrom 有权
标题翻译：羟基磷灰石靶向多聚体聚合物和由其制成的共轭物
公开(公告)号：US08440787B2
公开(公告)日：2013-05-14
申请号：US12738980
申请日：2008-10-23
申请人： Samuel P. McManus , Antoni Kozlowski
发明人： Samuel P. McManus , Antoni Kozlowski
IPC分类号： C08G79/00 , C08G65/327
CPC分类号： A61K47/48215 , A61K47/24 , A61K47/548 , A61K47/58 , A61K47/60 , A61K47/641
摘要： The present invention provides hydmoxyapatite-targeting, multiarm polymer reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains and a plurality of hydroxyapatile-targeting moieties located at the terminus of one or more of the polymer chains. The multiarm polymers are optionally divided or separated by one or more degradable linkages into polymer segments having a molecular weight suitable for renal clearance. The polymeric reagents of the invention can have a substantially linear structure, although branched or multiarm structures are contemplated as well. The invention is suited for applications in which use of a high molecular weight polymer is desired, such as a total polymer number average molecular weight of at least about 30,000 Da for linear polymers and 20,000 Da for multiarm polymers. Each structure includes one or more linkages capable of degradation in vivo. The use of multiple hydroxyapatite-targeting moieties on each polymer molecule enhances the ability of the polymer reagent to selectively target and bind to hydroxyapatite surfaces, which in turn, can increase the concentration of biologically active moiety delivered to the bone site.
摘要翻译：本发明提供了适于与生物活性剂反应以形成共轭物的羟基磷灰石靶向的多聚体聚合物试剂，所述聚合物试剂包含一个或多个聚合物链和位于聚合物中的一种或多种聚合物的末端的多个羟基磷酸酯靶向部分链条多聚物聚合物任选地被一个或多个可降解键分开或分离成具有适合于肾清除的分子量的聚合物链段。本发明的聚合物试剂可以具有基本上线性的结构，尽管也考虑了分支或多臂结构。本发明适用于需要使用高分子量聚合物的应用，例如线性聚合物的总聚合物数均分子量为至少约30,000Da，多聚聚合物为20,000Da。每个结构包括能够在体内降解的一种或多种键。在每个聚合物分子上使用多个羟基磷灰石靶向部分增强了聚合物试剂选择性地靶向和结合羟基磷灰石表面的能力，这进而可以增加递送至骨部位的生物活性部分的浓度。

36. 发明授权

US08304511B2 Maleamic acid polymer derivatives and their bioconjugates 有权
标题翻译：马来酰胺酸聚合物衍生物及其生物共轭物
公开(公告)号：US08304511B2
公开(公告)日：2012-11-06
申请号：US13172043
申请日：2011-06-29
申请人： Antoni Kozlowski , Remy F. Gross, III , Samuel P. McManus
发明人： Antoni Kozlowski , Remy F. Gross, III , Samuel P. McManus
IPC分类号： C08G73/10 , C08G73/00
CPC分类号： C08G65/33337 , A61K47/60 , C08G65/329 , C08L2203/02
摘要： The present invention is directed a method comprising administering a composition to an individual, wherein the composition comprises a plurality of conjugates, each conjugate in the plurality a protein derivatized with a water-soluble polymer, wherein the polymer is coupled to the protein via succinimide groups covalently attached to either cysteine sulfhydryl groups or lysine amino groups, and substantially all of the succinimide groups present in the composition are present in a ring-opened form.
摘要翻译：本发明涉及一种包括向个体施用组合物的方法，其中所述组合物包含多个缀合物，每个缀合物在多个中缀合有用水溶性聚合物衍生的蛋白质，其中所述聚合物通过琥珀酰亚胺基团与蛋白质偶联共价连接到半胱氨酸巯基或赖氨酸氨基上，并且存在于组合物中的基本上所有琥珀酰亚胺基团以开环形式存在。

37. 发明申请

US20120214952A1 Methods for Preparing Polymeric Reagents and Compositions of Polymeric Reagents 有权
标题翻译：制备聚合物试剂和聚合物试剂组合物的方法
公开(公告)号：US20120214952A1
公开(公告)日：2012-08-23
申请号：US13463686
申请日：2012-05-03
申请人： Antoni Kozlowski , Jon McKannan , Samuel P. McManus
发明人： Antoni Kozlowski , Jon McKannan , Samuel P. McManus
IPC分类号： C08L77/04
CPC分类号： C08G65/33396 , A61K47/60 , C07B47/00 , C08G65/329 , C08G65/332 , C08G65/48 , C08L71/02
摘要： Methods for preparing active carbonate esters of water-soluble polymers are provided. Also provided are other methods related to the active carbonate esters of water-soluble polymers, as well as corresponding compositions.
摘要翻译：提供了制备水溶性聚合物的活性碳酸酯的方法。还提供了与水溶性聚合物的活性碳酸酯相关的其它方法以及相应的组合物。

38. 发明申请

US20120123065A1 Hydrolytically Stable Maleimide-Terminated Polymers 有权
标题翻译：水解稳定的马来酰亚胺封端聚合物
公开(公告)号：US20120123065A1
公开(公告)日：2012-05-17
申请号：US13336886
申请日：2011-12-23
申请人： Antoni Kozlowski , Remy F. Gross, III , Samuel P. McManus
发明人： Antoni Kozlowski , Remy F. Gross, III , Samuel P. McManus
IPC分类号： C08G65/48
CPC分类号： C08G65/33396 , A61K47/48215 , A61K47/60 , C08G65/33337 , C08L63/10 , C08L2203/02
摘要： The present invention is directed to conjugates of hydrolytically stabilized maleimide-functionalized water soluble polymers and to methods for making and utilizing such polymers and their precursors.
摘要翻译：本发明涉及水解稳定的马来酰亚胺官能化水溶性聚合物的共轭物，以及制备和利用这些聚合物及其前体的方法。

39. 发明申请

US20120065429A1 WATER-SOLUBLE POLYMER ALKANALS 有权
标题翻译：水溶性聚合物碱
公开(公告)号：US20120065429A1
公开(公告)日：2012-03-15
申请号：US13301715
申请日：2011-11-21
申请人： Antoni Kozlowski
发明人： Antoni Kozlowski
IPC分类号： C07C45/42 , C07C231/14
CPC分类号： A61K47/48215 , A61K47/60 , C07C43/315 , C07C45/30 , C07C47/198 , C08G65/2603 , C08G65/329 , C08L2203/02 , C07C47/14
摘要： The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.
摘要翻译：本发明涉及水溶性聚合物如聚（乙二醇），它们相应的水合物和缩醛的链烷醛衍生物，以及制备和使用这种聚合物链烷醛的方法。本发明的聚合物链烷可以高纯度制备并显示储存稳定性。

40. 发明授权

US08076412B2 Water-soluble polymer alkanals 有权
标题翻译：水溶性聚合物链烷
公开(公告)号：US08076412B2
公开(公告)日：2011-12-13
申请号：US12908266
申请日：2010-10-20
申请人： Antoni Kozlowski
发明人： Antoni Kozlowski
IPC分类号： C08G63/48 , C08G63/91 , C08G10/00 , C08G12/00
CPC分类号： A61K47/48215 , A61K47/60 , C07C43/315 , C07C45/30 , C07C47/198 , C08G65/2603 , C08G65/329 , C08L2203/02 , C07C47/14
摘要： The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.
摘要翻译：本发明涉及水溶性聚合物如聚（乙二醇），它们相应的水合物和缩醛的链烷醛衍生物，以及制备和使用这种聚合物链烷醛的方法。本发明的聚合物链烷可以高纯度制备并显示储存稳定性。

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