申请人:CELGENE CORPORATION
公开号:US10335495B2
公开(公告)日:2019-07-02
The present invention relates to biomolecule conjugates which comprise a biomolecule wherein at least one non-natural amino acid (NNAA) is integral to the structure of the biomolecule and wherein the NNAA is a point of attachment of a linker to which a payload, particularly a cytotoxic agent, is attached. More specifically, this invention relates to conjugates of cell-binding agents and active release products comprising cytotoxic agents wherein the conjugates are produced by means of a cycloaddition reaction. Methods of production, pharmaceutical compositions and methods of use are provided.
本发明涉及生物大分子共轭物,它包括生物大分子,其中至少有一个非天然氨基酸(NNAA)与生物大分子的结构不可分割,并且该非天然氨基酸是连接有效载荷(尤其是细胞毒剂)的连接点。更具体地说,本发明涉及细胞结合剂的共轭物和包含细胞毒剂的活性释放产物,其中共轭物是通过环化反应生产的。本发明还提供了生产方法、药物组合物和使用方法。