申请人:Liang Congxin
公开号:US08501763B2
公开(公告)日:2013-08-06
The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
本发明提供了针对聚焦粘附激酶(一种参与细胞细胞骨架与细胞外基质附着的酶)的抑制剂,该酶被认为参与了细胞迁移、细胞增殖和细胞存活等过程。这些抑制剂是5-取代-2,4-二氨基吡啶的衍生物,其中取代基如本文所定义。本发明还提供了一种使用这些抑制剂治疗癌症的方法,以及通过使用偶联反应制备这些抑制剂的方法。