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    • 2. 发明申请
    • POLYMER-DRUG CONJUGATES
    • 聚合物 - 药物共轭物
    • WO2007047922A2
    • 2007-04-26
    • PCT/US2006041035
    • 2006-10-19
    • SMARTCELLS INCLANCASTER THOMAS AZION TODD CNELAWANSKI MATTHEW
    • LANCASTER THOMAS AZION TODD CNELAWANSKI MATTHEW
    • A61K38/28C07K14/605C07K14/61C07K14/62
    • C08B37/0084A61K38/25A61K38/26A61K38/28A61K47/60A61K47/61A61K47/6903C08B30/18C08B37/00C08B37/003C08B37/0069C08B37/0072Y10S436/827
    • A conjugate that includes a drag covalently linked to a polymer. Upon administration, the conjugate is digested by an enzyme that is present at the site of administration thereby releasing a therapeutic agent. The conjugate may demonstrate substantially the same pharmacokinetic and pharmacodynamic behavior as the drug itself. A material for controllably releasing a conjugate in response to the local concentration of a molecular indicator. The material includes a plurality of conjugates and a plurality of multivalent cross-linking agents. The polymers of the conjugates include an analog of the indicator within their covalent structure. The multivalent cross-linking agents include cross-link receptors that interact with the indicator analog and thereby cross-link the conjugates. These non-covalent interactions are competitively disrupted when an amount of the molecular indicator is present thereby causing the material to release the conjugate in a manner that is dependent on the local concentration of indicator.
    • 包含与聚合物共价连接的药物的偶联物。 施用后,缀合物被存在于施用部位的酶消化,由此释放治疗剂。 偶联物可以表现出与药物本身基本相同的药代动力学和药效学行为。 响应于分子指示剂的局部浓度而可控地释放缀合物的材料。 该材料包括多种缀合物和多种多价交联剂。 缀合物的聚合物包括其共价结构内的指示物的类似物。 多价交联剂包括与指示剂类似物相互作用从而交联缀合物的交联受体。 当存在一定量的分子指示剂时,这些非共价相互作用被竞争性地破坏,从而导致材料以取决于指示剂局部浓度的方式释放缀合物。