Endogenously-formed conjugate of albumin
    1.
    发明申请
    Endogenously-formed conjugate of albumin 审中-公开
    内源性白蛋白缀合物

    公开(公告)号:US20060058236A1

    公开(公告)日:2006-03-16

    申请号:US11217536

    申请日:2005-08-31

    IPC分类号: A61K38/38

    CPC分类号: A61K47/643 A61K47/60

    摘要: A conjugate formed in vivo and comprised of endogenous albumin and an amine-containing compound, such as a protein or a drug, is described. The conjugate is formed by in vivo cleavage of a polymer-dithiobenzyl-therapeutic agent conjugate to form an albumin-dithiobenzyl-therapeutic agent conjugate. The dithiol moiety of the albumin-therapeutic agent conjugate is cleaved in vivo to yield the free therapeutic agent in native form.

    摘要翻译: 描述了在体内形成的由内源白蛋白和含胺化合物如蛋白质或药物组成的缀合物。 通过体内裂解聚合物 - 二硫代苄基治疗剂缀合物形成白蛋白 - 二硫代苄基治疗剂缀合物来形成缀合物。 白蛋白治疗剂缀合物的二硫醇部分在体内裂解以产生天然形式的游离治疗剂。

    Releasable linkage and compositions containing same
    2.
    发明授权
    Releasable linkage and compositions containing same 有权
    可释放的连接物和含有它们的组合物

    公开(公告)号:US07592307B2

    公开(公告)日:2009-09-22

    申请号:US11810931

    申请日:2007-06-06

    摘要: A conjugate comprised of a hydrophilic polymer covalently yet reversibly linked to a amine-, hydroxy- or carboxyl-containing ligand is described. The resulting conjugate is capable of releasing the parent amine, hydroxy, or carboxyl-containing compound via thiol-mediated cleavage. The system allows for delivery of various amino-, hydroxy-, or carboxy-containing drugs in the form of their thiolytically cleavable macromolecular conjugates.

    摘要翻译: 描述了由共价但可逆地连接到含胺,羟基或羧基的配体的亲水性聚合物组成的缀合物。 所得的缀合物能够通过硫醇介导的切割释放母体胺,羟基或含羧基的化合物。 该系统允许以其可硫裂解的大分子缀合物的形式递送各种氨基,羟基或羧基的药物。

    Releasable linkage and compositions containing same
    3.
    发明申请
    Releasable linkage and compositions containing same 有权
    可释放的连接物和含有它们的组合物

    公开(公告)号:US20080279922A1

    公开(公告)日:2008-11-13

    申请号:US11810931

    申请日:2007-06-06

    IPC分类号: A61K9/127 C07K14/00 C07K14/52

    摘要: A conjugate comprised of a hydrophilic polymer covalently yet reversibly linked to a amine-, hydroxy- or carboxyl-containing ligand is described. The resulting conjugate is capable of releasing the parent amine, hydroxy, or carboxyl-containing compound via thiol-mediated cleavage. The system allows for delivery of various amino-, hydroxy-, or carboxy-containing drugs in the form of their thiolytically cleavable macromolecular conjugates.

    摘要翻译: 描述了由共价但可逆地连接到含胺,羟基或羧基的配体的亲水性聚合物组成的缀合物。 所得的缀合物能够通过硫醇介导的切割释放母体胺,羟基或含羧基的化合物。 该系统允许以其可硫裂解的大分子缀合物的形式递送各种氨基,羟基或羧基的药物。

    Releasable linkage and compositions containing same
    5.
    发明授权
    Releasable linkage and compositions containing same 有权
    可释放的连接物和含有它们的组合物

    公开(公告)号:US07238368B2

    公开(公告)日:2007-07-03

    申请号:US10723473

    申请日:2003-11-26

    摘要: A conjugate comprised of a hydrophilic polymer covalently yet reversibly linked to a amine-, hydroxy- or carboxyl-containing ligand is described. The resulting conjugate is capable of releasing the parent amine, hydroxy, or carboxyl-containing compound via thiol-mediated cleavage. The system allows for delivery of various amino-, hydroxy-, or carboxy-containing drugs in the form of their thiolytically cleavable macromolecular conjugates.

    摘要翻译: 描述了由共价但可逆地连接到含胺,羟基或羧基的配体的亲水性聚合物组成的缀合物。 所得的缀合物能够通过硫醇介导的切割释放母体胺,羟基或含羧基的化合物。 该系统允许以其可硫裂解的大分子缀合物的形式递送各种氨基,羟基或羧基的药物。

    Novel bioconjugation reactions for acylating polyethylene glycol reagents
    6.
    发明申请
    Novel bioconjugation reactions for acylating polyethylene glycol reagents 审中-公开
    用于酰化聚乙二醇试剂的新型生物缀合反应

    公开(公告)号:US20060286657A1

    公开(公告)日:2006-12-21

    申请号:US11445833

    申请日:2006-06-01

    CPC分类号: A61K47/60

    摘要: A method for conjugation of PEG to a protein in an aqueous solution at a pH less than or equal to about 7.0 or neutral pH comprising combining an activated PEG reagent and a protein in the presence of an activating agent at a pH of less than about 7.0 or neutral pH. In one embodiment, the method produces mixed populations of moderately PEGylated proteins, including 1:1, 2:1, and 3:1 PEGylated proteins.

    摘要翻译: 一种用于在pH小于或等于约7.0或中性pH的水溶液中将PEG与蛋白质缀合的方法,包括在活性剂存在下,在小于约7.0的pH下组合活化的PEG试剂和蛋白质 或中性pH。 在一个实施方案中,该方法产生中等聚乙二醇化蛋白质的混合群体,包括1:2,2:1和3:1聚乙二醇化蛋白质。

    Method for treating multi-drug resistant tumors
    7.
    发明授权
    Method for treating multi-drug resistant tumors 有权
    多药耐药肿瘤治疗方法

    公开(公告)号:US07303760B2

    公开(公告)日:2007-12-04

    申请号:US10714085

    申请日:2003-11-14

    摘要: Methods for administering mitomycin C to a multi-drug resistant cell and for reducing the toxicity of the compound are described. In the methods, mitoymic C is provided in the form of a prodrug conjugate, where the drug is linked to a hydrophobic moiety, such as a lipid, through a cleavable dithiobenzyl linkage. The dithiobenzyl linkage is susceptible to cleavage by mild thiolysis, resulting in release of mitomycin C in its original form. The linkage is stable under nonreducing conditions. The prodrug conjugate can be incorporated into liposomes for administration in vivo and release of mitomycin C in response to endogenous in vivo reducing conditions or in response to administration of an exogenous reducing agent.

    摘要翻译: 描述了向多药耐药细胞施用丝裂霉素C并降低化合物的毒性的方法。 在该方法中,丝裂蛋白C以前体药物缀合物的形式提供,其中药物通过可裂解的二硫代苄基键连接到疏水部分,例如脂质。 二硫代苄基键易受到轻度硫解的裂解,导致丝裂霉素C以其原始形式释放。 在非还原条件下,连接是稳定的。 可以将前体药物缀合物掺入用于体内施用的体内脂质体中,并响应内源性体内还原条件或响应外源性还原剂的施用而释放丝裂霉素C.