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Compstatin Analogs with Increased Solubility and Improved Pharmacokinetic Properties

机译:Compstatin类似物的溶解度增加和改善的药代动力学性质

摘要

Compounds comprising peptides capable of binding C3 protein and inhibiting complement activation are disclosed. The compounds comprise compstatin analogs in which the N-terminus and/or C-terminus contains an added component that improves (1) the peptide's solubility at physiological pH; (2) the peptide's plasma half-life; (3) the peptide's intraocular retention; and/or (4) the peptide's binding affinity to C3 or its fragments as compared to an unmodified compstatin peptide under equivalent conditions. Pharmaceutical compositions and methods of using the compounds are also disclosed.
机译:公开了包含能够结合C3蛋白和抑制补体激活的肽的化合物。 该化合物包含Compstatin类似物,其中N-末端和/或C-末端含有添加的组分,其改善(1)在生理pH下的肽的溶解度; (2)肽的血浆半衰期; (3)肽的眼内保留; 和/或(4)与未经修饰的Compstatin肽相比,肽对C3或其片段的结合亲和力与在等同条件下相比。 还公开了药物组合物和使用化合物的方法。

著录项

  • 公开/公告号US2021261617A1

    专利类型

  • 公开/公告日2021-08-26

    原文格式PDF

  • 申请/专利权人 THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA;

    申请/专利号US201917045018

  • 发明设计人 JOHN D. LAMBRIS;

    申请日2019-04-05

  • 分类号C07K7/08;A61K47/60;

  • 国家 US

  • 入库时间 2022-08-24 20:48:28

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