Polymer Derivatives with Proximal Reactive Groups
    2.
    发明申请
    Polymer Derivatives with Proximal Reactive Groups 有权
    具有近端反应性基团的聚合物衍生物

    公开(公告)号:US20100184937A1

    公开(公告)日:2010-07-22

    申请号:US12749399

    申请日:2010-03-29

    IPC分类号: C08G73/06

    摘要: An activated, substantially water-soluble polyoxazoline is provided having a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups. The free reactive groups are capable of reacting with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated polyoxazoline and the biologically active agent.

    摘要翻译: 提供活化的基本上水溶性的聚恶唑啉,其具有直链或支链的聚(乙二醇)主链和至少一个通过水解稳定键连接至主链的末端,其中末端是支链的且具有近端反应性基团。 游离反应性基团能够与生物活性剂如蛋白质或肽中的活性部分反应,从而在活化的聚恶唑啉和生物活性剂之间形成共轭物。

    Poly(Ethylene Glycol) Derivatives with Proximal Reactive Groups
    3.
    发明申请
    Poly(Ethylene Glycol) Derivatives with Proximal Reactive Groups 有权
    具有近端反应性基团的聚(乙二醇)衍生物

    公开(公告)号:US20090186984A1

    公开(公告)日:2009-07-23

    申请号:US12410438

    申请日:2009-03-24

    IPC分类号: C08G65/333

    摘要: An activated, substantially water-soluble poly(ethylene glycol) is provided having of a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups. The free reactive groups are capable of reacting with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated (polyethylene glycol) and the biologically active agent.

    摘要翻译: 提供活化的,基本上水溶性的聚(乙二醇),其具有直链或支链的聚(乙二醇)主链和至少一个通过水解稳定键连接至主链的末端,其中末端是支链的并具有近端反应性 团体 游离反应性基团能够与生物活性剂如蛋白质或肽中的活性部分反应,从而在活化的(聚乙二醇)与生物活性剂之间形成共轭物。

    Poly (ethylene glycol) derivatives with proximal reactive groups
    4.
    发明授权
    Poly (ethylene glycol) derivatives with proximal reactive groups 有权
    具有近端反应性基团的聚(乙二醇)衍生物

    公开(公告)号:US07528202B2

    公开(公告)日:2009-05-05

    申请号:US11799259

    申请日:2007-04-30

    摘要: An activated, substantially water-soluble poly(ethylene glycol) is provided having of a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups. The free reactive groups are capable of reacting with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated (polyethylene glycol) and the biologically active agent.

    摘要翻译: 提供活化的,基本上水溶性的聚(乙二醇),其具有直链或支链的聚(乙二醇)主链和至少一个通过水解稳定键连接至主链的末端,其中末端是支链的并具有近端反应性 团体 游离反应性基团能够与生物活性剂如蛋白质或肽中的活性部分反应,从而在活化的(聚乙二醇)与生物活性剂之间形成共轭物。

    Polyethylene (glycol) derivatives with proximal reactive groups
    5.
    发明授权
    Polyethylene (glycol) derivatives with proximal reactive groups 有权
    具有近端反应性基团的聚乙烯(二醇)衍生物

    公开(公告)号:US07223803B2

    公开(公告)日:2007-05-29

    申请号:US11314912

    申请日:2005-12-21

    摘要: An activated, substantially water soluble poly(ethylene glycol) is provided having of a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups. The free reactive groups are capable of reacting with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated poly(ethylene glycol) and the biologically active agent.

    摘要翻译: 提供活化的基本上水溶性的聚(乙二醇),其具有直链或支链的聚(乙二醇)主链和至少一个通过水解稳定键连接至主链的末端,其中末端是支链的且具有近端反应性基团 。 自由活性基团能够与生物活性剂如蛋白质或肽中的活性部分反应,从而在活化的聚(乙二醇)与生物活性剂之间形成共轭物。

    Heterobifunctional poly(ethylene glycol) derivatives and methods for their preparation
    9.
    发明授权
    Heterobifunctional poly(ethylene glycol) derivatives and methods for their preparation 有权
    异双功能聚(乙二醇)衍生物及其制备方法

    公开(公告)号:US06448369B1

    公开(公告)日:2002-09-10

    申请号:US09186759

    申请日:1998-11-05

    IPC分类号: C08G6532

    CPC分类号: C08G65/329

    摘要: This invention provides a method for preparing, in high purity and high yield, heterobifunctional derivatives of poly(ethylene glycol) or related polymers. A chromatographic purification step is not necessary in the method. In accordance with the method of the invention, an intermediate polymer having a formula of W-Poly-OH is provided bearing a removable group W at one terminus. The intermediate polymer W-Poly-OH is first altered by modifying the OH group to a first functional group X, followed by the removal of W to generate a second hydroxyl group. The latter hydroxyl group may then be further converted to a second functional group Y, thus providing the desired heterobifunctional derivative.

    摘要翻译: 本发明提供一种以高纯度和高收率制备聚(乙二醇)或相关聚合物的异双功能衍生物的方法。 在该方法中不需要色谱纯化步骤。 根据本发明的方法,提供具有式W-聚-OH的中间体聚合物,其在一个末端具有可除去的基团W. 首先通过将OH基团改性为第一官能团X,然后除去W以产生第二羟基来改变中间体聚合物W-Poly-OH。 然后可以将后一羟基进一步转化为第二官能团Y,从而提供所需的异双功能衍生物。

    Method of preparing carboxylic acid functionalized polymers
    10.
    发明授权
    Method of preparing carboxylic acid functionalized polymers 有权
    制备羧酸官能化聚合物的方法

    公开(公告)号:US08067505B2

    公开(公告)日:2011-11-29

    申请号:US13023960

    申请日:2011-02-09

    IPC分类号: C08G65/332 C07C41/01

    摘要: 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═0)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.

    摘要翻译: 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'是叔基且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。