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    Polymer derivatives comprising an imide branching point
    3.
    发明授权
    Polymer derivatives comprising an imide branching point 有权
    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

    Applicant: Samuel P. McManus ,  Antoni Kozlowski

    Inventor： Samuel P. McManus ,  Antoni Kozlowski

    IPC: C08G65/08 ,  C08G69/08 ,  C07D207/46 ,  A61K47/48 ,  C08G65/333 ,  C08G73/08 ,  C08G73/10 ,  C08G73/12

    CPC classification number: C08G65/33331 ,  A61K47/60 ,  A61K47/6903 ,  C08G73/08 ,  C08G73/1092 ,  C08G73/12

    Abstract: 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.

    Abstract translation: 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。

    Polymer derivatives comprising an acetal or ketal branching point
    5.
    发明授权
    Polymer derivatives comprising an acetal or ketal branching point 有权
    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

    Applicant: Samuel P. McManus ,  Antoni Kozlowski

    Inventor： Samuel P. McManus ,  Antoni Kozlowski

    IPC: A61K47/48 ,  C08G65/02 ,  C08G73/06

    CPC classification number: A61K47/48215 ,  A61K47/60 ,  C08G65/322 ,  C08G65/329 ,  C08G65/331 ,  C08G65/33306 ,  C08G65/33337 ,  C08G65/3348 ,  C08L2203/02

    Abstract: 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.

    Abstract translation: 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。

    Hydroxyapatite-targeting multiarm polymers and conjugates made therefrom
    6.
    发明授权
    Hydroxyapatite-targeting multiarm polymers and conjugates made therefrom 有权
    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

    Applicant: Samuel P. McManus ,  Antoni Kozlowski

    Inventor： Samuel P. McManus ,  Antoni Kozlowski

    IPC: C08G79/00 ,  C08G65/327

    CPC classification number: A61K47/48215 ,  A61K47/24 ,  A61K47/548 ,  A61K47/58 ,  A61K47/60 ,  A61K47/641

    Abstract: 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.

    Abstract translation: 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。

    Maleamic acid polymer derivatives and their bioconjugates
    7.
    发明授权
    Maleamic acid polymer derivatives and their bioconjugates 有权
    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

    Applicant: Antoni Kozlowski ,  Remy F. Gross, III ,  Samuel P. McManus

    Inventor： Antoni Kozlowski ,  Remy F. Gross, III ,  Samuel P. McManus

    IPC: C08G73/10 ,  C08G73/00

    CPC classification number: C08G65/33337 ,  A61K47/60 ,  C08G65/329 ,  C08L2203/02

    Abstract: 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.

    Abstract translation: 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。

    WATER-SOLUBLE POLYMER ALKANALS
    10.
    发明申请
    WATER-SOLUBLE POLYMER ALKANALS 有权
    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

    Applicant: Antoni Kozlowski

    Inventor： Antoni Kozlowski

    IPC: C07C45/42 ,  C07C231/14

    CPC classification number: A61K47/48215 ,  A61K47/60 ,  C07C43/315 ,  C07C45/30 ,  C07C47/198 ,  C08G65/2603 ,  C08G65/329 ,  C08L2203/02 ,  C07C47/14

    Abstract: 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.

    Abstract translation: 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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