Synthesis and Pharmacological Properties of the Benzimidazole Scaffold: A Patent Review

Abstract

Benzimidazole derivatives were first discovered in the late 19th and early 20th centuries, marking a significant milestone in the field of chemistry. These compounds have since played a pivotal role in pharmacology, demonstrating a wide array of pharmacological properties that have had a profound impact on medicine and healthcare. The significance of benzimidazole derivatives in pharmacology is undeniable. These compounds have been extensively studied and developed for their diverse and valuable properties. They exhibit potent anticancer activity, with some derivatives displaying the ability to hinder the growth of cancer cells, offering hope in the fight against this disease. Furthermore, benzimidazole derivatives have been involved in the management of cardiovascular conditions as antihypertensive agents, aiding in the control of high blood pressure. Their potential as antidiabetic agents, by influencing glucose metabolism and insulin secretion, holds promise in diabetes treatment. The recent patent literature has focused on structural modifications to the benzimidazole core to expand the arsenal of effective drugs. This review takes a disease‐centric perspective on patented benzimidazoles from 2016 to 2023. The relevant granted patent applications were located using patent databases, USPTO, Google Patents, EPO, WIPO, Lens and Espacenet.