Chemical peptide ligation with three or more components
    9.
    发明授权
    Chemical peptide ligation with three or more components 有权
    化学肽与三个或更多成分结合

    公开(公告)号:US07884182B2

    公开(公告)日:2011-02-08

    申请号:US10494928

    申请日:2002-11-14

    IPC分类号: A61K38/00

    摘要: The invention provides a method of assembling oligopeptide intermediates in a native chemical ligation reaction that eliminates self-ligation of bi-functional intermediates. An important aspect of the invention is a bi-functional intermediate with an N-terminal heterocyclic protecting group which effectively prevents self-ligation in the chemical assembly process. The present invention is useful in methods for convergent synthesis of polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where three or more peptide fragments are used to assemble a polypeptide or protein product.

    摘要翻译: 本发明提供了在天然化学连接反应中组装寡肽中间体的方法,其消除双功能中间体的自连接。 本发明的一个重要方面是具有N-末端杂环保护基的双功能中间体,其有效地防止化学组装过程中的自连接。 本发明可用于多肽和蛋白质的收敛合成的方法,并提高天然化学连接反应的效率,特别是在使用三个或更多个肽片段来组装多肽或蛋白质产物的情况下。

    AZIRIDINE ALDEHYDES, AZIRIDINE-CONJUGATED AMINO DERIVATIVES, AZIRIDINE-CONJUGATED BIOMOLECULES AND PROCESSES FOR THEIR PREPARATION
    10.
    发明申请
    AZIRIDINE ALDEHYDES, AZIRIDINE-CONJUGATED AMINO DERIVATIVES, AZIRIDINE-CONJUGATED BIOMOLECULES AND PROCESSES FOR THEIR PREPARATION 有权
    AZIRIDINE ALDEHYDES,AZIRIDINE-CONJUGATED AMINO DORIVATIVES,AZIRIDIN-CONJUGATED BIOMOLECULES AND PROCESSES FOR THE PRACARATION

    公开(公告)号:US20100317832A1

    公开(公告)日:2010-12-16

    申请号:US12446343

    申请日:2007-10-22

    摘要: The present invention applications for same. More particularly, the present invention relates to novel aziridine aldehydes and processes for preparing these novel compounds. The invention also relates to aziridine-conjugated amino derivatives, and processes for preparing the same. Pentacyclic compounds may be prepared using the aziridine aldehydes of the present invention, and the invention relates to these compounds and the processes by which they are made. The invention also relates to aziridine-conjugated bioactive molecules, such as amino acids and peptides, and processes for preparing such compounds.

    摘要翻译: 本发明同样适用。 更具体地说,本发明涉及新的氮杂环丁烷醛及其制备方法。 本发明还涉及氮丙啶缀合的氨基衍生物及其制备方法。 五环化合物可以使用本发明的氮丙啶醛制备,本发明涉及这些化合物及其制备方法。 本发明还涉及氮丙啶缀合的生物活性分子,例如氨基酸和肽,以及制备这些化合物的方法。