Recent progress in small molecule TBK1 inhibitors: a patent review (2015-2020)

Introduction: TANK-binding kinase 1 (TBK1) is a key mediator of innate immunity processes and studies have reported on its role in inflammatory and autoimmune diseases. Moreover, several studies have also described the important role of TBK1 in cancer and metabolic disorders. Therefore, there is increasing interest in this noncanonical IKK serine/threonine kinase family member as a drug target in both the scientific community and the pharmaceutical industry as indicated by the growing number of patents reporting on these efforts. Areas covered: This review covers the patent literature from 2015 to 2020 issued by the World, US and European patent offices on novel TBK1 small molecule inhibitors as well as patents claiming new applications of TBK1 inhibitors. Expert opinion: The high complexity TBK1 biology greatly increases the challenge of pursuing it as a drug target. The recent discovery of several small molecule inhibitors, particularly those with high selectivity, will enable further exploration of TBK1s biological role and its validation as a drug target.

Automated summary

TBK1, a key mediator of innate immunity processes, plays important roles in inflammatory and autoimmune diseases, cancer, and metabolic disorders. The increasing interest in TBK1 as a drug target is evidenced by the growing number of patents reporting on novel TBK1 small molecule inhibitors and new applications of TBK1 inhibitors. The complexity of TBK1 biology presents challenges, but the discovery of selective small molecule inhibitors holds promise for further research on its biological role and validation as a drug target.