AMIDE DERIVATIVES OF LACTAM BASED N-ACYLETHANOLAMINE ACID AMIDASE (NAAA) INHIBITORS
申请人:The Regents of the University of California
公开号:US20160068483A1
公开(公告)日:2016-03-10
Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.
本文描述了一些化合物和制药组合物,它们能够抑制N-酰基乙醇胺酸酰化酶(NAAA)。本文还描述了一些合成上述化合物的方法,以及将这些化合物制成制药组合物的方法。此外,本文还描述了一些抑制NAAA的方法,以维持在NAE浓度降低的情况下,PEA和其他NAE的水平。此外,本文还描述了一些治疗和改善疼痛、炎症、炎症性疾病和其他疾病的方法,这些疾病中脂肪酸乙醇胺的调节在临床上或治疗上是相关的,或者NAE浓度降低与该疾病有关。