TABLE 3

Selected NRF2 inducers acting as NRF2–KEAP1 protein–protein interaction inhibitors

CompoundPatentTitleApplicant
GraphicWO2017060855Arylcyclohexyl pyrazoles as NRF2 regulatorsGlaxoSmithKline Astex Therapeutics
GraphicWO2016/202253NRF2 regulatorsGlaxoSmithKline Astex Therapeutics, GlaxoSmithKline (China), R&D
GraphicWO2014/197818Small-molecule activators of NRF2 pathwayGeneral Hospital, Regents of the University of California
GraphicWO2013/067036Direct inhibitors of KEAP1–NRF2 interaction as antioxidant inflammation modulatorsRutgers, The State University of New Jersey, Broad Institute
GraphicWO2011/156889Novel modulators of NRF2 and uses thereofTRT Pharma Gerald Batist, Jian Hui Wu
GraphicJP2011/0167537KEAP1 protein-binding compound, crystal of complex between the same and KEAP1 protein, and method for producing the sameToray Industries
GraphicWO20171248351-sulfonamido-4-aryloxy compound, and preparation method and medicinal application thereofChina Pharmaceutical University
GraphicWO2015/092713NRF2 regulatorsGlaxoSmithKline Astex Therapeutics Limited
GraphicWO2011156889A1Novel regulators of NRF2 and uses thereofTRT Pharma Gerald Batist, Jian Hui Wu
GraphicWO2016/202253NRF2 regulatorsGlaxoSmithKline Astex Therapeutics, GlaxoSmithKline (China), R&D CO., LTD