The transient receptor potential canonical (TRPC) channels have gained interest as potential therapeutic targets for respiratory diseases, neurological disorders, cardiovascular disorders, pain, cancer and several other pathological conditions. The TRPC receptor family consists of seven isoforms (C1-C7) and has been divided into three subfamilies based on structural and functional similarities. Several pharmaceutical companies and academic institutes are currently exploring the potential of these nonselective cation channels as therapeutic targets using small molecule inhibitors or modulators. This review covers patents on TRPC receptor modulators published from 2002 to 2014. The review mainly focuses on TRPC receptor target biology, small and large molecule modulators and their therapeutic potential.