PMID- 35410559 OWN - NLM STAT- MEDLINE DCOM- 20220525 LR - 20220525 IS - 1744-7674 (Electronic) IS - 1354-3776 (Linking) VI - 32 IP - 6 DP - 2022 Jun TI - Soluble epoxide hydrolase inhibitors: an overview and patent review from the last decade. PG - 629-647 LID - 10.1080/13543776.2022.2054329 [doi] AB - INTRODUCTION: Biological effects mediated by the CYP450 arm of arachidonate cascade implicate the enzyme-soluble epoxide hydrolase (sEH) in hydrolyzing anti-inflammatory epoxy fatty acids to pro-inflammatory diols. Hence, inhibiting the sEH offers a therapeutic approach to treating inflammatory diseases. Over three decades of work has shown the role of sEH inhibitors (sEHis) in treating various disorders in rodents and larger veterinary subjects. Novel chemical strategies to enhance the efficacy of sEHi have now appeared. AREAS COVERED: A comprehensive review of patent literature related to soluble epoxide hydrolase inhibitors in the last decade (2010-2021) is provided. EXPERT OPINION: Soluble epoxide hydrolase (sEH) is an important enzyme that metabolizes the bioactive epoxy fatty acids (EFAs) in the arachidonic acid signaling pathway and converts them to vicinal diols, which appear to be pro-inflammatory. Inhibition of sEH hence offers a mechanism to increase in vivo epoxyeicosanoid levels and resolve pro-inflammatory pathways in disease states. Significant efforts in the field have led to potent single target as well as multi-target inhibitors with promising in vitro and widely encompassing in vivo activities. Successful clinical translation of compounds targeting sEH inhibition will further validate the promised therapeutic potential of this pathway in treating human diseases. FAU - Iyer, Malliga R AU - Iyer MR AUID- ORCID: 0000-0002-0116-4619 AD - Section on Medicinal Chemistry, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Rockville, Maryland, United States. FAU - Kundu, Biswajit AU - Kundu B AD - Section on Medicinal Chemistry, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Rockville, Maryland, United States. FAU - Wood, Casey M AU - Wood CM AD - Section on Medicinal Chemistry, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Rockville, Maryland, United States. LA - eng PT - Journal Article PT - Review DEP - 20220412 PL - England TA - Expert Opin Ther Pat JT - Expert opinion on therapeutic patents JID - 9516419 RN - 0 (Anti-Inflammatory Agents) RN - 0 (Enzyme Inhibitors) RN - 0 (Fatty Acids) RN - EC 3.3.2.- (Epoxide Hydrolases) SB - IM MH - Anti-Inflammatory Agents/pharmacology MH - Enzyme Inhibitors/pharmacology/therapeutic use MH - *Epoxide Hydrolases MH - Fatty Acids MH - Humans MH - *Patents as Topic OTO - NOTNLM OT - EETs OT - enzymatic activity OT - hypertension OT - inflammatory diseases OT - sEH inhibitor OT - sEH-P OT - soluble epoxide hydrolase EDAT- 2022/04/13 06:00 MHDA- 2022/05/26 06:00 CRDT- 2022/04/12 05:26 PHST- 2022/04/13 06:00 [pubmed] PHST- 2022/05/26 06:00 [medline] PHST- 2022/04/12 05:26 [entrez] AID - 10.1080/13543776.2022.2054329 [doi] PST - ppublish SO - Expert Opin Ther Pat. 2022 Jun;32(6):629-647. doi: 10.1080/13543776.2022.2054329. Epub 2022 Apr 12.