Modified Compstatin With Peptide Backbone And C-Terminal Modifications
    1.
    发明申请
    Modified Compstatin With Peptide Backbone And C-Terminal Modifications 有权
    改进的Compstatin与肽骨架和C端修饰

    公开(公告)号:US20120178694A1

    公开(公告)日:2012-07-12

    申请号:US13318272

    申请日:2010-05-03

    IPC分类号: A61K38/12 C07K7/64

    摘要: Compounds comprising peptides capable of binding C3 protein and inhibiting complement activation are disclosed. These compounds display greatly improved complement activation-inhibitory activity as compared with currently available compounds. The compounds comprise compstatin analogs having a constrained backbone at position 8 (glycine) and, optionally, specific substitutions for threonine at position 13.

    摘要翻译: 公开了包含能够结合C3蛋白并抑制补体活化的肽的化合物。 与目前可获得的化合物相比,这些化合物显示出显着改善的补体活化抑制活性。 该化合物包含在8位(甘氨酸)具有约束主链的化合物抑制物类似物,以及任选地,在13位的苏氨酸的特异性取代。

    Compstatin Analogs with Improved Pharmacokinetic Properties
    3.
    发明申请
    Compstatin Analogs with Improved Pharmacokinetic Properties 有权
    具有改善药代动力学性质的化合物类似物

    公开(公告)号:US20150158915A1

    公开(公告)日:2015-06-11

    申请号:US14343003

    申请日:2012-09-07

    IPC分类号: C07K7/64 A61K45/06 A61K38/12

    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 contains an added or substituted component that improves (1) the peptide's binding affinity to C3 or its fragments, (2) the peptide's solubility in aqueous liquids, (3) the peptide's plasma stability, (4) the peptide's in vivo retention and/or (5) the peptide's bioavailability, as compared with an unmodified compstatin peptide under equivalent conditions. Pharmaceutical compositions and methods of using the compounds are also disclosed.

    摘要翻译: 公开了包含能够结合C3蛋白并抑制补体活化的肽的化合物。 化合物包括其中N末端含有加成或取代的成分的化合物类似物,其改善(1)肽对C3或其片段的结合亲和力,(2)肽在水性液体中的溶解度,(3)肽的血浆稳定性, (4)与等效条件下未修饰的化合物肽相比,肽的体内保留和/或(5)肽的生物利用度。 还公开了使用该化合物的药物组合物和方法。

    Modified compstatin with peptide backbone and C-terminal modifications
    4.
    发明授权
    Modified compstatin with peptide backbone and C-terminal modifications 有权
    具有肽骨架和C末端修饰的修饰的compstatin

    公开(公告)号:US08946145B2

    公开(公告)日:2015-02-03

    申请号:US13318272

    申请日:2010-05-03

    摘要: Compounds comprising peptides capable of binding C3 protein and inhibiting complement activation are disclosed. These compounds display greatly improved complement activation-inhibitory activity as compared with currently available compounds. The compounds comprise compstatin analogs having a constrained backbone at position 8 (glycine) and, optionally, specific substitutions for threonine at position 13.

    摘要翻译: 公开了包含能够结合C3蛋白并抑制补体活化的肽的化合物。 与目前可获得的化合物相比,这些化合物显示出显着改善的补体活化抑制活性。 该化合物包含在8位(甘氨酸)具有约束主链的化合物抑制物类似物,以及任选地,在13位的苏氨酸的特异性取代。