Transient receptor potential ankyrin 1 (TRPA1) antagonists: a patent review (2015-2019).

Expert Opinion on Therapeutic Patents
Huifen Chen, Jack A Terrett

Abstract

TRPA1 is a non-selective cation channel predominantly expressed in sensory neurons, and functions as an irritant sensor for a plethora of noxious external stimuli and endogenous ligands. Due to its involvement in pain, itch, and respiratory syndromes, TRPA1 has been pursued as a promising drug target. In this review, the small molecule patent literature of TRPA1 antagonists from 2015-2019 was surveyed. The patent applications are described with a focus on chemical structures, biochemical/pharmacological activities, and potential clinical applications. The development of TRPA1 antagonists in clinical trials has been highlighted. During 2015-2019, significant progress was made toward the discovery of new TRPA1 antagonists. A total of 14 organizations published 28 patent applications disclosing several distinct classes of chemical matter and potential uses. During this period, three new molecules entered the clinic (ODM-108, HX-100, and GDC-0334) bringing the total number of TRPA1 antagonists to reach clinical trials to five (including earlier molecules CB-625 and GRC 17536); however, to our knowledge, development of all five molecules have been discontinued. Further clinical trials of recent TRPA1 antagonists with good pharmacoki...Continue Reading

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Citations

Sep 7, 2020·Annals of the New York Academy of Sciences·Satyanarayana Achanta, Sven-Eric Jordt
Nov 17, 2020·Frontiers in Immunology·Harold A SilvermanEric H Chang
Apr 4, 2021·International Journal of Molecular Sciences·Roberto MaglieFrancesco De Logu
Mar 30, 2021·Frontiers in Pharmacology·Alessandro RimessiPaolo Pinton
Aug 10, 2021·International Journal of Pharmaceutics·Chun-Wan YenDennis H Leung
Sep 17, 2021·Nature Reviews. Drug Discovery·Ari-Pekka KoivistoArpad Szallasi

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