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    • 9. 发明申请
    • Glycopeptide compositions
    • 糖肽组合物
    • US20060198786A1
    • 2006-09-07
    • US11071975
    • 2005-03-04
    • I-Chien WeiDavid YangDong-Fang Yu
    • I-Chien WeiDavid YangDong-Fang Yu
    • A61K51/00C07K9/00
    • A61K31/505A61K31/66A61K51/025
    • The invention include glycopeptides having a glycoside and a peptide covalently bound through an amide bond. The glycopeptides may also include a diagnostic or therapeutic agent bound to the glycopeptide. A metal, such as a radionuclide, may also be chelated to the glycopeptide. Specific embodiments of the invention relate to glycopeptides made of chitosan covalently bound to a poly(amino acid) such as poly(glutamic acid) or poly(aspartic acid). Diagnostic agents conjugated to the glycopeptide may facilitate imaging. Specific therapeutic agents that may be conjugated to the glycopeptide include anticancer drugs, rheumatoid arthritis drugs, anticoagulants, anti-angiogenesis drugs, apoptosis drugs, osteoporosis drugs, steroids, and anti-inflammatory drugs. Some agents, such as radionuclides, may have both diagnostic and therapeutic effects. The glycopeptides may be made by combining a glycoside and a peptide in the presence of a carbodiimide and an acid group activator to form an amide bond between the glycoside and the peptide.
    • 本发明包括具有糖苷和通过酰胺键共价结合的肽的糖肽。 糖肽还可以包括与糖肽结合的诊断或治疗剂。 诸如放射性核素的金属也可以与糖肽螯合。 本发明的具体实施方案涉及由聚(氨基酸)如聚(谷氨酸)或聚(天冬氨酸)共价结合的壳聚糖制成的糖肽。 与糖肽缀合的诊断剂可以促进成像。 可以与糖肽结合的特异性治疗剂包括抗癌药物,类风湿关节炎药物,抗凝血剂,抗血管生成药物,凋亡药物,骨质疏松症药物,类固醇和抗炎药物。 一些药剂如放射性核素可能具有诊断和治疗作用。 糖肽可以通过在碳二亚胺和酸基活化剂的存在下组合糖苷和肽来在糖苷和肽之间形成酰胺键来制备。