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163 条记录 (耗时 0.049 秒)

    Stabilized polymeric thiol reagents
    43.
    发明授权
    Stabilized polymeric thiol reagents 有权
    稳定的聚合硫醇试剂

    公开(公告)号：US08492488B2

    公开(公告)日：2013-07-23

    申请号：US13528103

    申请日：2012-06-20

    申请人： Antoni Kozlowski ,  Samuel P. McManus

    发明人： Antoni Kozlowski ,  Samuel P. McManus

    IPC分类号： C08G75/00 ,  C08F283/00 ,  C08L81/00 ,  A61K31/415

    CPC分类号： A61K47/48215 ,  A61K31/415 ,  A61K47/60 ,  C07C323/12 ,  C07D213/70 ,  C07D213/71

    摘要： Disclosed are water soluble polymeric conjugates comprising the structure POLY-[Y—S—S-A]x, where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 25, S—S is a disulfide group attached to an sp3 hybridized carbon of Y; and A is a covalently linked residue of a pharmacologically active molecule. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are polymeric reagents useful to prepare such conjugates, and methods of their formation and use.

    摘要翻译： 公开了包含结构POLY- [Y-S-S-A] x的水溶性聚合物共轭物，其中POLY是水溶性聚合物; Y为烃类间隔基，x为1〜25，S-S为连接于Y的sp3杂化碳的二硫基; 并且A是药理活性分子的共价连接的残基。 优选地，水溶性聚合物是PEG聚合物。 还公开了可用于制备这种缀合物的聚合物试剂，及其形成和用途的方法。

    Segmented degradable polymers and conjugates made therefrom
    44.
    发明授权
    Segmented degradable polymers and conjugates made therefrom 有权
    由其制成的分段可降解聚合物和共轭物

    公开(公告)号：US08309680B2

    公开(公告)日：2012-11-13

    申请号：US12224201

    申请日：2007-02-21

    申请人： Samuel P. McManus ,  Antoni Kozlowski

    发明人： Samuel P. McManus ,  Antoni Kozlowski

    IPC分类号： C08G65/00

    CPC分类号： A61K47/48215 ,  A61K47/60

    摘要： The present invention provides, among other things, segmented, degradable polymeric reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains divided or separated by one or more degradable linkages into polymer segments having a molecular weight suitable for renal clearance. The polymeric reagents can have a substantially linear structure, a branched structure, or a multiarm structure. Each structure includes one or more linkages capable of degradation in vivo.

    摘要翻译： 本发明尤其提供了适用于与生物活性剂反应以形成共轭物的分段的可降解聚合物试剂，所述聚合物试剂包含一个或多个由一个或多个可降解键分隔或分隔成聚合物链段的聚合物链，其具有分子量 适合肾清除。 聚合物试剂可以具有基本上线性的结构，分支结构或多臂结构。 每个结构包括能够在体内降解的一种或多种键。

    Method for preparing branched functionalized polymers using branched polyol cores
    50.
    发明授权
    Method for preparing branched functionalized polymers using branched polyol cores 有权
    使用支链多元醇芯制备支链官能化聚合物的方法

    公开(公告)号：US08568705B2

    公开(公告)日：2013-10-29

    申请号：US11458269

    申请日：2006-07-18

    申请人： Samuel P. McManus ,  Antoni Kozlowski

    发明人： Samuel P. McManus ,  Antoni Kozlowski

    IPC分类号： A61K31/74

    CPC分类号： A61K47/48061 ,  A61K31/74 ,  A61K31/765 ,  A61K47/60 ,  C07D405/14 ,  C08G65/329 ,  C08G65/34 ,  C08G65/48 ,  C08G71/04 ,  C08L2203/02 ,  Y02P20/582

    摘要： A method of preparing a multiarm polymer includes reacting a branched polyol with one or more functionalizing reagents to effect substitution of an ionizable functional group or a protected ionizable functional group, Y, to form a mixture comprising (i) unsubstituted branched polyol containing no Y groups; (ii) a monosubstituted polyol comprising one Y group, and (iii) a multisubstituted polyol (e.g., a disubstituted polyol comprising two Y groups); followed by purifying the mixture to separate the monosubstituted polyol from other species Thereafter, a water-soluble and non-peptidic polymer segment is attached to the monosubstituted branched polyol at the site of at least one of the hydroxyl groups. The invention also provides purified monosubstituted branched polyols and multiarm polymers prepared by the method and polyol precursors for use in the method.

    摘要翻译： 制备多聚合物聚合物的方法包括使支化多元醇与一种或多种官能化试剂反应以实现可离子化官能团或受保护的可离子化官能团Y的取代，以形成包含（i）不含Y基团的未取代的支链多元醇 ; （ii）包含一个Y基团的单取代多元醇，和（iii）多取代多元醇（例如，包含两个Y基团的二取代多元醇）; 然后纯化混合物以从其它物质分离单取代的多元醇然后，在至少一个羟基的位置处将水溶性和非肽聚合物链段连接到单取代的支化多元醇上。 本发明还提供了纯化的单取代的支化多元醇和通过该方法制备的多聚合物聚合物和用于该方法的多元醇前体。