Cellular and serum protein anchors for modulating pharmacokinetics
    1.
    发明授权
    Cellular and serum protein anchors for modulating pharmacokinetics 失效
    用于调节药代动力学的细胞和血清蛋白锚点

    公开(公告)号:US5843440A

    公开(公告)日:1998-12-01

    申请号:US702127

    申请日:1996-08-14

    Abstract: Novel bifunctional reagents useful in reducing the biological effect of an undesirable blood-borne agent are provided. The reagents comprise conjugates of a first binding member specific for a blood-borne agent having a detrimental biological activity in a mammalina host, such as a growth factor, coagulation factor, enzyme, toxin, drug of abuse, microbe, autoreactive immune cell, infected or tumorous cell, joined to an second binding member specific for an anchor, where the anchor is a long-lived blood component, including cells, such as a erythrocyte, platelet or endothelial cell and serum proteins, such as albumin, ferritin, or steroid binding proteins. These conjugates find therapeutic use by coupling the agent and the blood component and thereby reducing the biological activity or effective concentration of free agent, modulating the volume of distribution of the agent, targeting the agent to sites of enhanced immune response, or facilitating agent clearance from the bloodstream.

    Abstract translation: 提供了可用于降低不期望的血液传染剂的生物学作用的新型双功能试剂。 试剂包括对哺乳动物宿主例如生长因子,凝血因子,酶,毒素,滥用药物,微生物,自身免疫细胞,感染的哺乳动物宿主中具有不利生物活性的血液传染剂特异性的第一结合成员的缀合物 或肿瘤细胞,其连接到针对锚的特异性的第二结合成员,其中锚是长寿命血液成分,包括细胞,例如红细胞,血小板或内皮细胞和血清蛋白,例如白蛋白,铁蛋白或类固醇 结合蛋白。 这些缀合物通过偶联药物和血液成分而发现治疗用途,从而降低游离剂的生物活性或有效浓度,调节药剂的分布体积,将药剂靶向增强的免疫应答的位点或促进药物清除 血流。

    Synthetic membrane vesicles containing functionally active fusion
peptides as drug delivery systems
    2.
    发明授权
    Synthetic membrane vesicles containing functionally active fusion peptides as drug delivery systems 失效
    含有功能活性融合肽作为药物递送系统的合成膜囊泡

    公开(公告)号:US6040167A

    公开(公告)日:2000-03-21

    申请号:US930593

    申请日:1992-11-02

    Abstract: The phospholipid bilayer contains at least one pharmaceutically active drug and comprises cell-specific markers on the membrane which have at least 90% biological activity when measured according to Luescher & Glueck, Antiviral Research 14, 39-50. In the membrane, the cholesterol content is preferably less than 2% by weight, the detergent content preferably less than 1 ppb. The vesicle diameter preferably is about 80 nm. the phospholipid in the membrane may comprise 70 to 95% by weight of phosphatidylcholine and preferably 10 to 20% by weight of phosphatidylethanolamine; preferably 6-8% by weight of a crosslinker, preferably of a sulfosuccinimidyl derivate, and at least one cell-specific fusion peptide are linked to the membrane. The vesicles are used for the preparation of pharmaceuticals against AIDS and carcinomas.

    Abstract translation: PCT No.PCT / EP92 / 00089 Sec。 371日期:1992年11月2日 102(e)日期1992年11月2日PCT提交1992年1月17日PCT公布。 出版物WO92 / 日期1992年8月20日当根据Luescher&Glueck,Antiviral Research 14,39-50测量时,磷脂双层含有至少一种药物活性药物,并且包括膜上的细胞特异性标记物,其具有至少90%的生物活性。 在膜中,胆固醇含量优选小于2重量%,洗涤剂含量优选小于1ppb。 泡囊直径优选为约80nm。 膜中的磷脂可以包含70至95重量%的磷脂酰胆碱,优选10至20重量%的磷脂酰乙醇胺; 优选6-8重量%的交联剂,优选磺基琥珀酰亚胺基衍生物,和至少一个细胞特异性融合肽连接到膜。 囊泡用于制备抗艾滋病和癌症的药物。

    Antiviral supramolecules containing target-binding molecules and
therapeutic molecules bound to spectrin
    4.
    发明授权
    Antiviral supramolecules containing target-binding molecules and therapeutic molecules bound to spectrin 失效
    含有靶结合分子和结合血影蛋白的治疗分子的抗病毒超分子

    公开(公告)号:US5997861A

    公开(公告)日:1999-12-07

    申请号:US627695

    申请日:1996-03-29

    Abstract: Complexes are prepared containing two or more different effector molecules joined to each other by a joining component. One effector molecule is a binding molecule such as an antibody or Fc receptor that binds to a molecular target such as a virus or antibody at a site of infection or tumor, and another effector molecule is a therapeutic molecule such as an enzyme or drug. The joining component may be a liposome, protein or an organic polymer (including a dendrimer type polymer), and may be of sufficient length and/or flexibility to permit the therapeutic molecule to physically interact with the target at the same time as the binding molecule. Supramolecules are formed containing at least two supramolecular component molecules that contain an effector molecule and a nucleic acid chain. A nucleic acid chain on a component molecule is complementary to a nucleic acid chain on another component molecule to enable binding of the component molecules of the supramolecule by the formation of double stranded nucleic acid chains between complementary chains. A targetable antiviral supramolecule is prepared containing spectrin as the joining component. The binding molecule can be an antibody specific for an antigen on a viral particle and the therapeutic molecule can be an enzyme capable of destroying infectivity of the virus by hydrolysis of viral coat protein or viral lipid.

    Abstract translation: 制备的复合物含有通过接合组分彼此连接的两个或更多个不同的效应分子。 一个效应分子是结合分子,例如抗体或Fc受体,其在感染或肿瘤部位与分子靶标如病毒或抗体结合,另一个效应分子是诸如酶或药物的治疗分子。 连接组分可以是脂质体,蛋白质或有机聚合物(包括树枝状聚合物类型的聚合物),并且可以具有足够的长度和/或柔性,以允许治疗性分子在与结合分子同时与物质相互作用 。 形成含有至少两个含有效应分子和核酸链的超分子组分分子的超分子。 组分分子上的核酸链与另一组分分子上的核酸链互补,以通过互补链之间的双链核酸链的形成来结合超分子的组分分子。 制备可靶向的抗病毒超分子,其包含作为连接组分的血影蛋白。 结合分子可以是对病毒颗粒上的抗原特异的抗体,并且治疗分子可以是能够通过病毒外壳蛋白或病毒脂质的水解来破坏病毒感染性的酶。

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