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    • 7. 发明申请
    • Long Acting Biologically Active Conjugates
    • 长效生物活性缀合物
    • US20070207952A1
    • 2007-09-06
    • US10550715
    • 2004-03-24
    • Abelardo SilvaJohn EricksonMichael EissenstatElena AfoninaSergei Gulnik
    • Abelardo SilvaJohn EricksonMichael EissenstatElena AfoninaSergei Gulnik
    • A61K38/16A61K38/10C07K14/47C07K7/08
    • C07K14/765A61K38/00A61K47/643
    • The invention provides biologically active compounds that may be reacted with macromolecules, such as albumin, to form covalent linked complexes wherein the resulting complexes exhibit a desired biological activity in vivo. More specifically, the complexes are isolated complexes comprising a biologically active moiety covalently bound to a linking group and a protein. The complexes are prepared by conjugating a biologically active moiety, for example, a renin inhibitor or a viral fusion inhibitor peptide, with purified and isolated protein. The complexes have extended lifetimes in the bloodstream as compared to the unconjugated molecule, and exhibit biological activity for extended periods of time as compared to the unconjugated molecule. The invention also provides anti-viral compounds that are inhibitors of viral infection and/or exhibit anti-fusiogenic properties. In particular, this invention provides compounds having inhibiting activity against viruses such as human immunodeficiency virus (HIV), respiratory syncytial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) and that have extended duration of action for the treatment of viral infections.
    • 本发明提供可与大分子如白蛋白反应的生物活性化合物以形成共价连接的络合物,其中所得的复合物在体内显示出所需的生物学活性。 更具体地,复合物是包含与连接基团和蛋白质共价结合的生物活性部分的分离的复合物。 通过将生物活性部分例如肾素抑制剂或病毒融合抑制剂肽与纯化和分离的蛋白质缀合来制备复合物。 与非共轭分子相比,复合物在血液中的寿命延长,与非共轭分子相比,延长的时间段具有生物活性。 本发明还提供了抗病毒化合物,其是病毒感染的抑制剂和/或表现出抗融合生物学特性。 特别地,本发明提供了对人体免疫缺陷病毒(HIV),呼吸道合胞病毒(RSV),人副流感病毒(HPV),麻疹病毒(MeV)和猿猴免疫缺陷病毒(SIV)等病毒具有抑制活性的化合物, 延长了治疗病毒感染的时间。