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, proliferation, and survival. The inhibitors are derivatives of 2,4-diaminopyridine wherein the substituents are as defined. The invention also provides a method of using the inhibitors in treatment of cancer, and a method of preparation of the inhibitors by a palladium-catalyzed coupling reaction.本發明提供了黏著斑激酶抑制劑,該黏著斑激酶是一種參與細胞的細胞骨架與細胞外基質結合的酶,與諸如細胞遷移、增殖以及存活的過程有關。該抑制劑為2,4-二氨基吡啶的衍生物,其中的取代基如所定義的。本發明還提供了使用該抑制劑治療癌症的方法和藉由鈀催化的偶合反應製備該抑制劑的方法。