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    Method Involving 1-Benzotriazolyl Carbonate Esters of Polymers
    14.
    发明申请
    Method Involving 1-Benzotriazolyl Carbonate Esters of Polymers 有权
    涉及聚合物的1-苯并三唑基碳酸酯酯的方法

    公开(公告)号：US20110237746A1

    公开(公告)日：2011-09-29

    申请号：US13154917

    申请日：2011-06-07

    Applicant: Antoni Kozlowski

    Inventor： Antoni Kozlowski

    IPC: C08G65/48

    CPC classification number: A61K47/58 ,  A61K31/7088 ,  A61K47/60 ,  A61K47/6901 ,  C08G63/91 ,  C08G65/48

    Abstract: The invention provides a method comprising the steps of (i) reacting a water-soluble and non-peptidic polymer having two or more terminal hydroxyl groups with di(1-benzotriazolyl)carbonate to form a water-soluble and non-peptidic polymer having two or more 1-benzotriazolylcarbonate ester groups; and (ii) reacting the water-soluble and non-peptidic polymer having two or more 1-benzotriazolylcarbonate ester groups with a water-soluble and non-peptidic polymer having three or more primary amino groups under conditions effective to form a cross-linked polymer composition.

    Abstract translation: 本发明提供了一种方法，其包括以下步骤：（i）使具有两个或多个末端羟基的水溶性和非肽类聚合物与二（1-苯并三唑基）碳酸酯反应，形成具有两个 或更多的1-苯并三唑基碳酸酯基团; 和（ii）在有效形成交联聚合物的条件下使具有两个或多个1-苯并三唑基碳酸酯基团的水溶性和非肽类聚合物与具有三个或更多个伯氨基的水溶性和非肽性聚合物反应 组成。

    Polymeric Alpha-Hydroxy Aldehyde and Ketone Reagents and Conjugation Method
    15.
    发明申请
    Polymeric Alpha-Hydroxy Aldehyde and Ketone Reagents and Conjugation Method 有权
    聚合α-羟基醛和酮试剂和共轭法

    公开(公告)号：US20110230618A1

    公开(公告)日：2011-09-22

    申请号：US13063720

    申请日：2009-09-11

    Applicant: Sean M. Culbertson ,  Xiaoming Shen ,  Antoni Kozlowski ,  Samuel P. McManus

    Inventor： Sean M. Culbertson ,  Xiaoming Shen ,  Antoni Kozlowski ,  Samuel P. McManus

    IPC: C08G65/48

    CPC classification number: C08G65/2606 ,  A61K38/00 ,  A61K47/60 ,  C07K1/003 ,  C07K17/08 ,  C08G65/26 ,  C08G65/2609 ,  C08G65/331 ,  C08G65/3315 ,  C08G65/3318 ,  C08G65/3326 ,  C08G65/33306 ,  C08G65/33313 ,  C08G65/33317 ,  C08G65/33327 ,  C08L71/02

    Abstract: Provided herein are polymeric α-hydroxy aldehyde or α-hydroxy ketone reagents which can be conjugated to amine-containing compounds to form stable conjugates in a single-step reaction. In selected embodiments, the polymeric reagent itself incorporates an internal proton-abstracting (basic) functional group, to promote more efficient reaction. The substituent is appropriately situated, via a linker if necessary, to position the group for proton abstraction, preferably providing a 4- or 5-bond spacing between the abstracting atom and the hydrogen atom on the α-carbon. Also provided are methods of using the reagents and stable, solubilized conjugates of the reagents with biologically active compounds. In preferred embodiments, the polymeric component of the reagent or conjugate is a polyethylene glycol.

    Abstract translation: 本文提供的是聚合α-羟基醛或α-羟基酮试剂，其可以与含胺化合物结合以在单步反应中形成稳定的共轭物。 在选择的实施方案中，聚合物试剂本身包含内部质子抽提（碱性）官能团，以促进更有效的反应。 如果需要，取代基通过接头适当地定位，以使基团定位以进行质子抽提，优选在提取的原子和α-碳上的氢原子之间提供4-或5-键的间隔。 还提供了使用试剂和试剂的稳定的，溶解的缀合物与生物活性化合物的方法。 在优选的实施方案中，试剂或缀合物的聚合物组分是聚乙二醇。

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