Hydroxyapatite-targeting poly (ethylene glycol) and related polymers
    92.
    发明授权
    Hydroxyapatite-targeting poly (ethylene glycol) and related polymers 有权
    羟基磷灰石靶向聚(乙二醇)和相关聚合物

    公开(公告)号:US06436386B1

    公开(公告)日:2002-08-20

    申请号:US09712536

    申请日:2000-11-14

    CPC classification number: A61K47/60

    Abstract: Isolatable, hydroxyapatite-targeting polymeric structures, and biologically active conjugates thereof, are provided. The polymeric structure includes a linear or branched water-soluble and non-peptidic polymer backbone, such as a PEG backbone, having at least two termini, a first terminus being covalently bonded to a hydroxyapatite-targeting moiety, such as a bisphosphonate, and a second terminus covalently bonded to a chemically reactive group, wherein said chemically reactive group is protected or unprotected. Methods of preparing and using hydroxyapatite-targeting polymeric structures, and biologically active conjugates thereof, are also provided.

    Abstract translation: 提供可分离的羟基磷灰石靶向聚合物结构及其生物活性缀合物。 聚合物结构包括直链或支链的水溶性和非肽聚合物主链,例如具有至少两个末端的PEG主链,第一个末端与羟基磷灰石靶向部分如二膦酸共价键合,和 第二末端共价键合到化学反应基团,其中所述化学反应基团被保护或未被保护。 还提供了制备和使用羟基磷灰石靶向聚合物结构及其生物活性缀合物的方法。

    Method for preparing branched functionalized polymers using branched polyol cores
    98.
    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

    Abstract: 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.

    Abstract translation: 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。

    Method of Preparing Carboxylic Acid Functionalized Polymers
    99.
    发明申请
    Method of Preparing Carboxylic Acid Functionalized Polymers 有权
    羧酸官能化聚合物的制备方法

    公开(公告)号:US20130281634A1

    公开(公告)日:2013-10-24

    申请号:US13922020

    申请日:2013-06-19

    Abstract: Methods for preparing water soluble, non-peptidic polymers carrying carboxyl functional groups, particularly carboxylic acid functionalized poly(ethylene glycol) (PEG) polymers are disclosed, as are the products of these methods. In general, an ester reagent R(C═O)OR′, wherein R′ is a tertiary group and R comprises a functional group X, is reacted with a water soluble, non-peptidic polymer POLY-Y, where Y is a functional group which reacts with X to form a covalent bond, to form a tertiary ester of the polymer, which is then treated with a strong base in aqueous solution, to form a carboxylate salt of the polymer. Typically, this carboxylate salt is then treated with an inorganic acid in aqueous solution, to convert the carboxylate salt to a carboxylic acid, thereby forming a carboxylic acid functionalized polymer.

    Abstract translation: 公开了用于制备携带羧基官能团的水溶性非肽聚合物,特别是羧酸官能化聚(乙二醇)(PEG)聚合物的方法,以及这些方法的产物。 通常,其中R'是叔基,R包含官能团X的酯试剂R(C = O)OR'与水溶性非肽聚合物POLY-Y反应,其中Y是官能团 基团与X反应形成共价键,形成聚合物的叔酯,然后用强碱在水溶液中处理,形成聚合物的羧酸盐。 通常,该羧酸盐然后用水溶液中的无机酸处理,以将羧酸盐转化为羧酸,从而形成羧酸官能化聚合物。

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