Src family of protein tyrosine kinases (SFKs) plays key roles in the regulation of signal transductions in cellular processes. However, hyper-activated SFKs lead to uncontrolled cell proliferation and cancers. Src-targeted compounds were developed to block the cell proliferation signal transductions for cancer therapy. Src kinase domain inhibitors were designed, synthesized and evaluated as anticancer agents, while the patents applied at the same time. Great progress has been made in the Src kinase inhibitor area. Herein, some predominant patents about Src kinase inhibitors of the recent years are reviewed.