Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T88505 Target Info
Target Name Nuclear factor erythroid 2-related factor 2 (Nrf2)
Synonyms Nuclear factor, erythroid derived 2, like 2; NRF2; NFE2-related factor 2; NF-E2-related factor 2; HEBP1
Target Type Successful Target
Gene Name NFE2L2
Biochemical Class Basic leucine zipper bZIP
UniProt ID
NF2L2_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015092713
Title Nrf2 Regulators.
Abstract The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
Applicant(s) Glaxosmithkline Intellectual Property Development Limited
Representative Drug(s) D0Q8JZ Drug Info Kd = 1.3 nM Click to Show More [1]
2 D0MS7G Drug Info IC50 = 61 nM; Kd = 59000 nM [1]
3 D0O6LW Drug Info IC50 > 1000000 nM [1]
Patent ID WO2014197818
Title Small Molecule Activators of Nrf2 Pathway.
Abstract This disclosure relates to compounds that act as activators of the NRF2/KEAP1/ARE pathway. Specifically, the compounds provided herein can act as high affinity reversible bindings for the NRF2 inhibitor, KEAP1. In some cases, NRF2/KEAP1/ARE pathway activation compounds are capable of repressing expression of inflammatory markers and/or reducing levels of TNFa to provide neuroprotective anti-inflammatory effects in the CNS. Such compounds are useful in the treatment of a variety of diseases including Huntington's disease, Parkinson's disease, Alzheimer's disease, inflammation, and cancer.
Applicant(s) The General Hospital Corporation
Representative Drug(s) D0AR0L Drug Info Kd = 17000 nM Click to Show More [1]
2 D09MSN Drug Info Kd = 23000 nM [1]
3 D0I2DV Drug Info N.A. [1]
Patent ID WO2016065264
Title Diterpenoid Derivatives and Methods of Use Thereof.
Abstract Provided herein are compounds of formula (I) and compositions containing the compounds. The compounds and compositions are useful in the methods of treating, amelioration or prophylaxix of diseases associated with Nrf2/ NF-kappa pathways. The diseases associated include, but are not limited to a fibrotic disease such as lung fibrosis, liver fibrosis, kidney fibrosis, and scleroderma, or a neurodegenerative disease, such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, and Alzheimer's disease, and sickle cell disease.
Applicant(s) Biogen Ma Inc
Representative Drug(s) D09FZF Drug Info N.A. Click to Show More [1]
2 D0Q9QQ Drug Info N.A. [1]
Patent ID WO2016059269
Title Compounds Derived From 3-Alkylamino-1H-Indole Acrylate, and The Use Thereof In The Treatment of Neurodegenerative Diseases.
Abstract The invention relates to the methods for producing derivatives of 3-alkylamino-1H-indole acrylate (I) with transcription factor Nrf2-inducing activity, free radical scavenging activity and neuroprotective ability. The invention also relates to the use of the derivatives according to the invention for the treatment of diseases, the pathogenesis of which involves oxidative stress, or diseases involving the deregulation of the activity of phase II genes activated by the factor Nrf2, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, multiple sclerosis, ictus or amyotrophic lateral sclerosis.
Applicant(s) Fundacion Para La Investigacion Biomedica Del Hospital Universitario De La Princesa Universidad Autonoma De Madrid Dns Neuroscience
Representative Drug(s) D01PKZ Drug Info N.A. Click to Show More [1]
2 D0FH6P Drug Info N.A. [1]
3 D0FM3Q Drug Info N.A. [1]
4 D0L1JQ Drug Info N.A. [1]
5 D0MX0Q Drug Info N.A. [1]
6 D0SA1N Drug Info N.A. [1]
Patent ID WO2015187934
Title Functionalized Hetroaryl Enones Exhibiting Nrf2 Activation and Their Method of Use.
Abstract Pharmaceutical compositions are disclosed, which include functionalized hetroaryl enones and are useful for treating or preventing a disease, disorder or condition associated with an NRF2-regulated pathway and/or which involves oxidative stress.
Applicant(s) Cureveda, Llc
Representative Drug(s) D02SPI Drug Info N.A. Click to Show More [1]
2 D0EO3S Drug Info N.A. [1]
3 D0G1LS Drug Info N.A. [1]
Patent ID WO2015009881
Title Nrf2 Inhibitors and Compositions for Treating Mycobacterial Infections.
Abstract Provided herein are methods, compositions, and kits for Nr2 inhibitors and their use in treatment of mycobacterial infection and in combination therapy with known antitubercular drugs.
Applicant(s) The Hamner Institutes
Representative Drug(s) D04YKV Drug Info N.A. Click to Show More [1]
2 D05EMI Drug Info N.A. [1]
3 D0O5ZK Drug Info N.A. [1]
4 D0P9ZD Drug Info N.A. [1]
5 D0PF4H Drug Info N.A. [1]
6 D0RO7A Drug Info N.A. [1]
Patent ID WO2015009879
Title Compositions for Modulating Nrf2-Are Activity and Their Methods of Use.
Abstract The invention provides the identification of compounds having a novel activity of Nrf2 inhibition. Provided is use of the Nrf2 inhibitors in pharmaceutical compositions and in treatment modalities, and methods of use thereof, to treat cells having constitutive Nrf2 activation such as in solid nonlymphoid tumors and in viral infections.
Applicant(s) The Hamner Institutes
Representative Drug(s) D04YKV Drug Info N.A. Click to Show More [1]
2 D05EMI Drug Info N.A. [1]
3 D0O5ZK Drug Info N.A. [1]
4 D0P9ZD Drug Info N.A. [1]
5 D0PF4H Drug Info N.A. [1]
6 D0RO7A Drug Info N.A. [1]
Patent ID WO2014145642
Title Nrf2 Small Molecule Inhibitors for Cancer Therapy.
Abstract Small molecule inhibitors of Nrf2 and methods of their use are provided for treating or preventing a disease, disorder or condition associated with an Nrf2- regulated pathway. The compound can be administered as a single agent or can be administered to enhance the efficacy of a chemotherapeutic drug and/or radiation therapy.
Applicant(s) The Johns Hopkins University
Representative Drug(s) D00PGP Drug Info N.A. Click to Show More [1]
2 D0D8KO Drug Info N.A. [1]
3 D0DE0Y Drug Info N.A. [1]
4 D0T2LN Drug Info N.A. [1]
Patent ID WO2013163344
Title 2.2-Difluoropropionamide Derivatives of Bardoxolone Methyl, Polymorphic forms and Methods of Use Thereof.
Abstract The present invention relates generally to the compound: N-((4aS,6aR,6bS,8aR,12aS,14aR,14bS)-1 1-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b- octadecahydropicen-4a-yl)-2,2-difluoropropanamide, polymorphic forms thereof, methods for preparation and use thereof, pharmaceutical compositions thereof, and kits and articles of manufacture thereof.
Applicant(s) Reata Pharmaceuticals, Inc
Representative Drug(s) D0AX4Q Drug Info N.A. Click to Show More [1]
2 D0RM4V Drug Info N.A. [1]
Patent ID WO2013067036
Title Direct Inhibitors of Keap1-Nrf2 Interaction As Antioxidant Inflammation Modulators.
Abstract A method of identifying compounds as direct inhibitors of Keap1-Nrf2 interaction through high-throughput screening and lead development. The direct inhibitors of Keap1-Nrf2 interaction are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential drug candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, and Parkinson's. Novel compounds are identified and methods of preventing or treating diseases or conditions related to Keapl-Nrf2 interaction activity by use of the novel compounds identified or compositions containing such compounds are also disclosed.
Applicant(s) Rutgers, the State University of New Jersey the Broad Institute, Inc
Representative Drug(s) D02FWA Drug Info N.A. [1]
Patent ID WO2012125488
Title C4-Monomethyl Triterpenoid Derivatives and Methods of Use Thereof.
Abstract Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of the formula (I) wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.
Applicant(s) Reata Pharmaceuticals, Inc
Representative Drug(s) D01GTU Drug Info N.A. Click to Show More [1]
2 D0N9GH Drug Info N.A. [1]
Patent ID WO2016033132
Title Pyridyl Analogs of 1-(2-Cyano-3,12-Dioxooleana-1,9(11)Dien-28-Oyl) Imidazole.
Abstract Pyridyl analogs of 1-(2-cyano-3,12-dioxooleana- 1,9(11 ) -dien-28-oyl) imidazole and pharmaceutical compositions containing the same are provided. The present invention is a tnterpenoid compound of Formula I, or a hydrate, isomer, prodrug or pharmaceutically acceptabl salt thereof: wherein one or more of R, R or R is independently a substituted or unsubstituted aryl group, heteroaryl group, cycloalkyl group or heterocyclyl group, and the remaining R groups are hydrogen. The pyridyl analogs of CDDO-lm 1 have been developed, which are more stable in human plasma and achieve a higher concentration in target tissues such as liver, pancreas, kidney and lungs.
Applicant(s) Trusteses of Dartmouth College
Representative Drug(s) D0KX0J Drug Info N.A. [1]
Patent ID WO2014148455
Title Terpenoid Derivative.
Abstract Provided is a novel terpenoid derivative which exhibits anti-inflammatory action and cytoprotective action by activating Keap1/Nrf2/ARE signal transduction pathways. Terpenoid derivative A is represented by formula (1).
Applicant(s) Daiichi Sankyo Co., Ltd
Patent ID WO2014040073
Title C13-Hydroxy Derivatives of Oleanolic Acid and Methods of Use Thereof.
Abstract Disclosed herein are novel C13-hydroxy derivatives of oleanolic acid, including those of the formula (I): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.
Applicant(s) Reata Pharmaceuticals, Inc
Representative Drug(s) D0AJ2T Drug Info N.A. [1]
Patent ID WO2013165140
Title Benzyl Derivative Compound Containing Activated Vinyl Group Capable of Being Used for Preventing and Treating Neurological Disorders Through Nitric Oxide Generation Inhibition and Nrf2 Activation.
Abstract The present invention relates to: a benzyl derivative containing an activated vinyl group; a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing the compound as an ac.
Applicant(s) Korea Institute of Science and Technology
Representative Drug(s) D04ILM Drug Info N.A. [1]
Patent ID WO2012116362
Title Chalcone Derivatives As Nrf2 Activators.
Abstract Compounds and methods for treating or preventing a disease, disorder or condition associated with an Nrf2-regulated pathway, including those associated with an autoimmune disease, comorbidity associated with diabetes, such as retinopathy and nephropathy, bone marrow transplant for leukemia and related cancers, bone marrow deficiencies, inborn errors of metabolism, and other immune disorders, oxidative stress, respiratory infection, ischemia, neurodegenerative disorders, radiation injury, neutropenia caused by chemotherapy, autoimmunity, and congenital neutropenic disorders, and for restoring a corticosteroid responsiveness, in a subject are provided.
Applicant(s) The Johns Hopkins University
Patent ID WO2016092042
Title Pharmaceutical Combination Comprising A Selective S1P1 Receptor Agonist.
Abstract The present invention relates to a pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]- propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is selected from the group consisting of methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, and 2- (2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof.
Applicant(s) Actelion Pharmaceuticals Ltd
Patent ID WO2016090154
Title Multiple Sclerosis Treatment Regimen Using Dimethyl Fumarate.
Abstract Provided herein are methods of treating multiple sclerosis with dimethyl fumarate using an up-titration regimen. The methods provided herein are to reduce dimethyl fumarate-related gastro-intestinal adverse events in multiple sclerosis patients.
Applicant(s) Biogen Ma Inc
Patent ID WO2016089648
Title Bach 1 Inhibitors In Combination with Nrf2 Activators and Pharmaceutical Compositions Thereof.
Abstract The disclosure provides pharmaceutical compositions comprising Bach1 Inhibitors and Nrf2 Activators. The disclosure also provides methods of treating diseases such as psoriasis, multiple sclerosis, and COPD comprising administering a Bach1 Inhibitor and a Nrf2 Activator to a subject in need thereof.
Applicant(s) Vtv Therapeutics Llc
Patent ID WO2016081701
Title Cddo-Me As A Therapy for Lupus.
Abstract Triterpenoid drugs such as CDDO-Me can be used as to treat autoimmune diseases such as graft versus host disease, lupus, and lupus nephritis. Triterpenoid drugs can also be used to prevent the effects of an autoimmune disease.
Applicant(s) Chandra Mohan et al
Patent ID WO2015138917
Title Dimethyl Fumarate and Vaccination Regimens.
Abstract Provided herein is a method of treating or preventing a disease or disorder (e.g., MS) in a subject in need thereof, comprising (a) administering to the subject a first dose of a pharmaceutical composition comprising a fumarate agent (e.g., DMF) for a first dosing period; (b) administering a vaccine; and (c) administering to the subject a second dose of the pharmaceutical composition for a second dosing period.
Applicant(s) Biogen Ma Inc
Patent ID WO2015105757
Title Dimethyl Fumarate for Treating Multiple Sclerosis.
Abstract Provided is a method of treating or preventing a neurological disease or disorder (e.g., multiple sclerosis) in a subject in need thereof comprising orally administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of an active agent selected from the group consisting of monomethyl fumarate, a compound that can be metabolized into monomethyl fumarate in vivo, a pharmaceutically acceptable salt thereof, a deuterated analogue thereof, and combinations thereof, and a pharmaceutically acceptable excipient, wherein the subject is not fully responsive to a treatment of interferon beta.
Applicant(s) Biogen Ma Inc
Patent ID WO2015027206
Title Methods of Treating and Preventing Endothelial Dysfunction Using Bardoxolone Methyl or Analogs Thereof.
Abstract The present invention concerns methods for treating and preventing endothelial dysfunction and related disorders, including, for example, pulmonary arterial hypertension, using bardoxolone methyl or analogs thereof.
Applicant(s) Reata Pharmaceuticals, Inc
Patent ID WO2013092269
Title Pharmaceutical Compositions Comprising Glitazones and Nrf2 Activators.
Abstract The invention relates to pharmaceutical compositions comprising PPAR agonists and Nrf2 activators and methods of using combinations of PPAR agonists and Nrf2 activators for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis.
Applicant(s) Ares Trading Sa
Patent ID WO2012149478
Title Agents Useful for Treating Friedreich'S Ataxia and Other Neurodegenerative Diseases.
Abstract This invention provides methods of identifying agents useful to prevent, ameliorate or treat one or more symptoms of Friedreich's ataxia or other neurodegenerative disease, and methods of employing the identified agents to prevent, reduce, delay or inhibit one or more symptoms of Friedreich's ataxia or other neurodegenerative disease.
Applicant(s) Serket Pharma, Llc
United States Patent and Trademark Office (USPTO)
Patent ID US20150197498
Title Preparation of Benzo[D]Oxazole Derivatives Useful As Anticancer Supplement Agents.
Applicant(s) Korea Institute of Radiological & Medical Sciences
Representative Drug(s) D03RTM Drug Info N.A. Click to Show More [1]
2 D07TEZ Drug Info N.A. [1]
3 D0G8CF Drug Info N.A. [1]
4 D0M2ZX Drug Info N.A. [1]
Patent ID US20160067206
Title Dimethyl Fumarate for Preventing and Treating Renal Fibros.
Applicant(s) Kyungpook National University
Patent ID US2015119420
Title Treatment of Multiple Sclerosis with Combination of Laquinimod and Dimethyl Fumarate.
Applicant(s) Teva Pharmaceutical Industries Ltd
Patent ID US2014171504
Title Methods of Treating Sickle Cell Disease and Related Disorders Using Fumaric Acid Esters.
Applicant(s) Georgia Regents University
Patent ID US2012232142
Title Novel Use of Dimethyl Fumarate.
Applicant(s) Kyungpook National University
Patent ID US20120202298
Title High-Throughput Screening Fluorescence Polarization Assay for Inhibitors of Keap1-Nrf2 Interaction.
Applicant(s) The State University of New Jersey, Usa
European Patent Office (EPO)
Patent ID EP2992882
Title Use of Ergothioneine for Inducing Activity of Nuclear Factor Erythroid 2-Related Factor-2 (Nrf2) In Cell.
Applicant(s) China Medical University
Representative Drug(s) D0N1VC Drug Info N.A. [1]
Japan Patent Office (JPO)
Patent ID JP2012082173
Title Nrf2 Activators Containing 2-Hydroxybenzamide Derivative, Method for Activating Nrf2, and Pharmaceuticals Containing The Compound.
Applicant(s) Keio University
Representative Drug(s) D02YNU Drug Info N.A. [1]
Patent ID JP2013043851
Title Anti-Oxidative Stress Enzyme Expression Inducers and Promoters, Nrf2 Activators, and Nrf2 Nuclear Import Promoters.
Applicant(s) Kyorin Pharmaceutical Co., Ltd
Representative Drug(s) D0G4EK Drug Info N.A. [1]
China National Intellectual Property Administration (CNIPA)
Patent ID CN105566241
Title 1-Sulfonamido-4-Aryloxynaphthalene Compounds As Nrf2 Activators and Their Preparation, Pharmaceutical Compositions and Use In The Treatment of Diseases.
Applicant(s) China Pharmaceutical University
Representative Drug(s) D00TVL Drug Info IC50 = 81 nM Click to Show More [1]
2 D02JFV Drug Info IC50 = 84 nM [1]
3 D0O3KN Drug Info IC50 = 90 nM [1]
4 D0LL7V Drug Info IC50 = 140 nM [1]
Patent ID CN105566323
Title Pyridopyrazine Compounds As Nrf2 Activators and Their Preparation, Pharmaceutical Compositions and Use In The Treatment of Inflammation and Cancer.
Applicant(s) China Pharmaceutical University
Representative Drug(s) D01MZI Drug Info N.A. Click to Show More [1]
2 D06LEF Drug Info N.A. [1]
3 D0AZ8T Drug Info N.A. [1]
Patent ID CN105267225
Title Application of 15,16-Dihydrotanshinone I In Manufacture of Medicament for Protection of Vascular Endothelium.
Applicant(s) China Pharmaceutical University
Representative Drug(s) D0MQ3X Drug Info N.A. [1]
Patent ID CN104825443
Title Antioxidant Application of Artemisitene In Composition with Treatment or Health-Care Effect.
Applicant(s) Guangdong Hospital of Traditional Chinese Medicine
Representative Drug(s) D0C1PB Drug Info N.A. [1]
Patent ID CN104415026
Title Application of Deuterated Fumaric Acid Derivatives for Treating Multiple Sclerosis.
Applicant(s) Chengdu Sourcebio Limited Liability Company, Peop. Rep. China
Representative Drug(s) D0JH8Z Drug Info N.A. [1]
Patent ID CN103724198
Title Derivatives of Dimethyl Fumarate and Application In The Treatment of Multiple Sclerosis.
Applicant(s) Zhenjiang Shengan Pharmaceutical Co., Ltd., Peop. Rep. China
Representative Drug(s) D0JH8Z Drug Info N.A. [1]
Patent ID CN105622720
Title Sphyrna Flesh Antioxidant Peptide Capable of Activating Nrf2-Are Pathway.
Applicant(s) Zhejiang Ocean University
Patent ID CN103768045
Title Application of Dimethyl Fumarate In Preparation of Medicine for Treating Early Brain Damage After Subarachnoid Hemorrhage.
Applicant(s) The First Affiliated Hospital of Soochow University
Korean Intellectual Property Office (KIPO)
Patent ID KR2013079898
Title Nrf2 Inhibitors for Chemotherapy and Chemoradiotherapy.
Applicant(s) Korea Institute of Radiological & Medical Sciences
Representative Drug(s) D0R2AI Drug Info IC50 = 2900 nM Click to Show More [1]
2 D06KOH Drug Info N.A. [1]
3 D0ND6T Drug Info N.A. [1]
4 D0T7WW Drug Info N.A. [1]
Patent ID KR2012032372
Title Composition for Preventing or Treating Obesity Containing Dimethyl Fumarate or Its Salt As Active Ingredient.
Applicant(s) Korea Food Research Institute (Kfri)
References  Top
REF 1 Recent progress in the development of small molecule Nrf2 modulators: a patent review (2012-2016).Expert Opin Ther Pat. 2017 Jul;27(7):763-785.

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