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    • 3. 发明申请
    • HPMA-POLYAMINE CONJUGATES AND USES THEREFORE
    • HPMA-聚氨酯结合物及其用途
    • WO2003066068A1
    • 2003-08-14
    • PCT/US2003/002707
    • 2003-01-31
    • INTRADIGM CORPORATIONGHANDEHARI, HamidrezaWOODLE, Martin, C.SCARIA, Puthupparampil, V.NAN, Anjan
    • GHANDEHARI, HamidrezaWOODLE, Martin, C.SCARIA, Puthupparampil, V.NAN, Anjan
    • A61K31/74
    • C07K5/021A61K31/74A61K47/58C07K5/1008C07K5/1027C12N15/87C12N2810/405
    • The inventions provide compositions and methods for nucleic acid delivery comprising HPMA conjugated to a polyamine. These compositions have the benefit of the steric hindrance of HPMA and the nucleic acid binding capability of a polyamine. Useful polyamines for this purpose include spermine, spermidine and their analogues, and DFMO. These polyamines have the ability not only to bind nucleic acids, but also have anti-cancer effects themselves. The compounds provided can also include ligand binding domains, such as vascular endothelial growth factors, somatostatin and somatostatin analogs, transferring, melanotropin, ApoE and ApoE peptides, von Willebrand's factor and von Willebrand's factor peptides, adenoviral fiber protein and adenoviral fiber protein peptides, PD 1 and PD 1 peptides, EGF and EGF peptides, RGD peptides, CCK peptides, antibody and antibody fragments, folate, pyridoxyl and sialyl-LewisX and chemical analogs. Methods for using these compositions to achieve a therapeutic effect, including for vaccination, are also provided.
    • 本发明提供了包含与多胺缀合的HPMA的核酸递送的组合物和方法。 这些组合物具有HPMA的空间位阻和多胺的核酸结合能力的益处。 有用的多胺用于此目的包括精胺,亚精胺及其类似物,以及DFMO。 这些多胺不仅具有结合核酸的能力,而且还具有抗癌作用。 所提供的化合物还可以包括配体结合域,例如血管内皮生长因子,生长抑素和生长抑素类似物,转移,黑素素,ApoE和ApoE肽,血管性血友病因子和血管性血友病因子肽,腺病毒纤维蛋白和腺病毒纤维蛋白肽,PD 1和PD 1肽,EGF和EGF肽,RGD肽,CCK肽,抗体和抗体片段,叶酸,吡哆醛和唾液酸-LXXX和化学类似物。 还提供了使用这些组合物来实现治疗效果的方法,包括用于疫苗接种。