title: P2X7 receptor antagonists: a patent review (2010-2015).
abstract: The P2X7 receptor (P2X7R) is a unique subtype among the family of seven purinergic P2X receptors, which are ATP-gated non-selective cation channels. P2X7R has been reported to have pathological roles in various diseases, including autoimmune diseases such as arthritis and inflammatory bowel disease, neurodegenerative diseases, chronic pain, mood disorders and cancers. Therefore, many pharmaceutical companies have endeavored to develop a clinical candidate targeting P2X7R. Areas covered: This review provides a summary of various patents on chemicals and biologics and their clinical use published between 2010 and 2015. The reader will gain information on structural claims, representative structures and biological activities of recently developed P2X7R antagonists. Expert opinion: P2X7R is a fascinating therapeutic target and potential biomarker for inflammation, pain disorders and cancers. Research on the development of P2X7R antagonists has continually increased despite the failure of AstraZeneca and Merck's compounds in phase II clinical trials. Various scaffolds have been disclosed by several pharmaceutical industries, and some compounds are currently under investigation in clinical trials.
authors.affiliation: a School of Life Sciences , Gwangju Institute of Science & Technology , Gwangju , Republic of Korea.|b New Drug Development Center (NDDC) , Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF) , Daegu , Republic of Korea.
authors.forename: Jin-Hee
authors.initials: JH
authors.lastname: Park
authors.affiliation: a School of Life Sciences , Gwangju Institute of Science & Technology , Gwangju , Republic of Korea.|c Department of Biomedical Science and Engineering , Gwangju Institute of Science & Technology , Gwangju , Republic of Korea.
authors.forename: Yong-Chul
authors.initials: YC
authors.lastname: Kim
mesh_terms: D000818:Animals; D015195:Drug Design; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000473:pathology; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D010146:Pain / Q000188:drug therapy / Q000473:pathology; D010330:Patents as Topic; D058920:Purinergic P2X Receptor Antagonists / Q000494:pharmacology*; D058486:Receptors, Purinergic P2X7 / Q000187:drug effects* / Q000378:metabolism
chemical_list: D058920:Purinergic P2X Receptor Antagonists; D058486:Receptors, Purinergic P2X7
keywords: IL-1β; P2X7 receptor; Purinergic receptor; ion channel