Cancer is now recognized as a major threat to global health and a notable cause of human mortality. Rapid cell multiplication abilities and the unchecked cell expansion that develops from a single cell define it. The epidermal growth factor receptor is a member of the ERBB family of receptors (ERBB‐1/2/3/4), and cancer can occur due to EGFR mutations. A lot of research is now being done on 4‐aminoquinazolines to suppress EGFR. With FDA‐approved medications based on the 4‐aminoquinazoline core already in use, we think that this core holds a lot of promise for a novel type of cancer therapy with significant therapeutic benefits. In this patent review, we have surveyed a huge number of patents reported (2000‐present) involving 4‐aminoquinazoline core as an anticancer agent targeting EGFR. We attempt here, with a huge body of literature based on this core, to update researchers about the latest EGFR‐targeted developments utilizing 4‐aminoquinazolines, which will provide support for the development of novel kinase‐targeted cancer therapies.