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 T05387 Target Info
Target Name Tissue transglutaminase (TG2)
Synonyms Transglutaminase-2; Transglutaminase H; Transglutaminase C; Transglutaminase 2; Tranglutaminase 2; TTg; TGase-H; TGase-2; TGase H; TGase C; TGC; TG(C)Protein-glutamine gamma-glutamyltransferase; TG(C); Protein-glutamine gamma-glutamyltransferase 2
Target Type Clinical trial Target
Gene Name TGM2
Biochemical Class Acyltransferase
UniProt ID
TGM2_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014057266
Title Acylpiperazines As Inhibitors of Transglutaminase and Their Use In Medicine.
Abstract The present invention relates to novel compounds of Formula I capable of inhibiting tissue transglutaminase, and uses of the same in medicine. In particular, the invention provides compounds for use in the treatment of prevention of disease and conditions such as fibrosis (e.g. cystic fibrosis), scarring, neurodegenerative diseases (e.g. Alzheimer's disease, Huntington's disease and Parkinson's disease), autoimmune diseases (e.g. multiple sclerosis and coeliac disease), thrombosis, proliferative disorders (e.g. cancers), AIDS, psoriasis and inflammation (e.g. chronic inflammatory diseases).
Applicant(s) Aston University
Representative Drug(s) D06YBF Drug Info IC50 = 2.1 nM Click to Show More [1]
2 D01EKS Drug Info IC50 = 3.9 nM [1]
Patent ID WO2012078519
Title 3-Acylidene-2-Oxoindole Derivatives for Inhibition of Transglutaminase 2.
Abstract Provided herein are acylidene oxoindole derivatives, compositions including them, and methods of inhibiting transglutaminase 2 and treating diseases mediated by transglutaminase 2 by administering such derivatives and compositions.
Applicant(s) Numerate, Inc
Representative Drug(s) D0RX6D Drug Info IC50 = 570 nM Click to Show More [1]
2 D0L7MP Drug Info IC50 = 740 nM; Ki = 3300 nM [1]
Patent ID WO2007050795
Title Transglutaminase Inhibitors and Methods of Use Thereof.
Abstract Transglutaminases (TGases) are a class of enzymes that play multifunctional roles. Their protein-crosslinking activity has been linked to fibrosis and Huntingtons disease, their glutamine deamidation activity has been related to celiac disease and their GTP-binding activity has been implicated in cancer. All of these physiological disorders have prompted the development of inhibitors, which has accelerated dramatically over the past decade. This review presents an overview of TGase inhibitors published in the patent literature, from the first compounds developed in the late 1980s, to the current date. This article is focussed on the chemical structure of new inhibitors and their probable mechanism of action. Comparison of effective TGase inhibitors reveals common structural features that may guide future design. Many of these elements are embodied in the first TGase inhibitor to recently enter into clinical trials.
Applicant(s) Alvine Pharmaceuticals, Inc
Representative Drug(s) D06TXR Drug Info IC50 = 10000 nM Click to Show More [1]
2 D0G0EG Drug Info IC50 = 16000 nM [1]
Patent ID WO2012153125
Title Inhibitors of Tissue Transglutaminase In The Treatment and/or Prevention of Angiogenic Diseases of The Eye.
Applicant(s) Aston University
Representative Drug(s) D0Y6TX Drug Info IC50 = 5000 nM Click to Show More [1]
2 D0J4IP Drug Info IC50 = 10000 nM [1]
Patent ID WO2014047288
Title Transglutaminase Tg2 Inhibitors, Pharmaceutical Compositions, and Methods of Use Thereof.
Abstract Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
Applicant(s) Dominguez, et al
Representative Drug(s) D0UR1H Drug Info IC50 = 62 nM [1]
Patent ID WO2010074480
Title Novel Pyrazolodiazepine Compounds As A Transglutaminase Inhibitor, The Preparation Method Thereof and A Composition Containing The Same.
Abstract The present invention relates to the novel pyrazolodiazepine compounds which potently inhibit the activity of transglutaminase in a dose dependent manner. Accordingly, it has been confirmed that the inventive compounds show potent inhibiting effect on the hyper- activated transglutaminase when the transglutaminase is over-expressed. Therefore the compounds can be useful in treating or preventing the disease caused by increased activation of transglutaminase.
Applicant(s) National Cancer Center
Representative Drug(s) D0GR1X Drug Info IC50 = 8300 nM [1]
Patent ID WO2010062144
Title Ethacrynic Acid-Containing Composition and Method for Prevention and Treatment of Transglutaminase-Related Diseases.
Abstract The present invention relates to ethacrynic acid and a transglutaminase inhibitor comprising a pharmaceutically acceptable salt of ethacrynic acid; more particularly, to ethacrynic acid for inhibiting.
Applicant(s) National Cancer Center
Representative Drug(s) D0EZ6C Drug Info IC50 = 5000 nM [1]
Patent ID WO2010011117
Title Ndga-Containing Composition for The Suppression of Transglutaminase.
Abstract The present invention relates to a novel use of nordihydroguaiaretic acid (NDGA) for suppressing transglutaminase activity. More specifically, the present invention relates to a pharmaceutical composi.
Applicant(s) National Cancer Center
Representative Drug(s) D0DK4I Drug Info IC50 = 550 nM [1]
Patent ID WO2006060702
Title Substitued 3,4-Dihydrothieno [2,3-D] Pyrmidines As Tissue Transglutaminase Inhibitors.
Abstract The present invention provides novel compounds and methods useful for treating transglutaminase associated disorders such as celiac spru, Alzheimer's disease and Huntington's disease. Certain compounds of the invention are tissue transglutaminase inhibitors that comprise thiophene moieties. Methods of the invention include treatment of transglutaminase associated disorders with inhibitors of transglutaminase.
Applicant(s) The Brigham and Women'S Hospital, Inc
Representative Drug(s) D02LBZ Drug Info IC50 = 800 nM [1]
Patent ID WO2007026996
Title Glucosamine and Derivatives Thereof Useful As Tg Inhibitors.
Abstract Disclosed herein is a transglutaminase inhibitor comprising glucosamine or a derivative thereof. Exhibiting potent inhibitory activity against transglutaminase, the overexpression of which is responsible for the etiology of various diseases, glucosamine or derivatives thereof can be useful in the prevention and treatment of such diseases. Also, a pharmaceutical composition comprising glucosamine or a derivative thereof as an active ingredient and a method of inhibiting transglutaminase are disclosed. Featuring the use of the pharmaceutical composition, the method can be therapeutically safely and effectively- applied to patients afflicted with such diseases.
Applicant(s) National Cancer Center
Representative Drug(s) D0NX1O Drug Info N.A. [1]
Patent ID WO9213530
Title Transglutaminase Enzyme Inhibitors.
Applicant(s) Medicis Corp
Representative Drug(s) D0YP7A Drug Info N.A. [1]
Patent ID WO9108739
Title Growth Arrest of Proliferating Cells By Transglutaminase InhibiTors.
Applicant(s) University of Texas
Representative Drug(s) D0O6LL Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US8614233
Title Cinnamoyl Inhibitors of Transglutaminase.
Applicant(s) Universit De Montral
Representative Drug(s) D01CCT Drug Info IC50 = 2100 nM; Ki = 1000 nM Click to Show More [1]
2 D0QX6W Drug Info IC50 = 18000 nM [1]
3 D0W5ND Drug Info IC50 = 21000 nM [1]
Patent ID US8471063
Title Michael Systems As Transglutaminase Inhibitors.
Applicant(s) Zedira Gmbh
Representative Drug(s) D0Y7FK Drug Info IC50 = 20 nM Click to Show More [1]
2 D0S4YD Drug Info IC50 = 30 nM [1]
Patent ID US8871718
Title Transglutaminase Inhibitors and Methods of Use Thereof.
Applicant(s) Leland Stanford Junior University
Representative Drug(s) D0CL1D Drug Info N.A. Click to Show More [1]
2 D0PM3J Drug Info N.A. [1]
Patent ID US8765797
Title Tg2 Inhibitors and Uses Thereof.
Applicant(s) University of Texas
Representative Drug(s) D0H2DL Drug Info N.A. Click to Show More [1]
2 D0O9JZ Drug Info N.A. [1]
Patent ID US7723307
Title Amino Acid Derivatives and Pharmaceutical Uses Thereof.
Applicant(s) Aston University
Representative Drug(s) D05ZTV Drug Info N.A. Click to Show More [1]
2 D0H4PF Drug Info N.A. [1]
3 D0K6SZ Drug Info N.A. [1]
Patent ID US5098707
Title Imidazole Compounds and Their Use As Transglutaminase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D02XDG Drug Info N.A. Click to Show More [1]
2 D0A9OC Drug Info N.A. [1]
3 D0IE9E Drug Info N.A. [1]
4 D0Y3YK Drug Info N.A. [1]
Patent ID US5084444
Title Imidazole Compounds and Their Use As Transglutaminase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D02XDG Drug Info N.A. Click to Show More [1]
2 D0A9OC Drug Info N.A. [1]
3 D0IE9E Drug Info N.A. [1]
4 D0Y3YK Drug Info N.A. [1]
Patent ID US5030644
Title Imidazole Compounds and Their Use As Transglutaminase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D02XDG Drug Info N.A. Click to Show More [1]
2 D0A9OC Drug Info N.A. [1]
3 D0IE9E Drug Info N.A. [1]
4 D0Y3YK Drug Info N.A. [1]
Patent ID US5021440
Title Imidazole Compounds and Their Use As Transglutaminase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D02XDG Drug Info N.A. Click to Show More [1]
2 D0A9OC Drug Info N.A. [1]
3 D0IE9E Drug Info N.A. [1]
4 D0Y3YK Drug Info N.A. [1]
Patent ID US5019572
Title Imidazole Compounds and Their Use As Transglutaminase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D02XDG Drug Info N.A. Click to Show More [1]
2 D0A9OC Drug Info N.A. [1]
3 D0IE9E Drug Info N.A. [1]
4 D0Y3YK Drug Info N.A. [1]
Patent ID US4970297
Title Transglutaminase Inhibitors.
Applicant(s) Syntex, Inc
Representative Drug(s) D02OXG Drug Info N.A. Click to Show More [1]
2 D0MA2H Drug Info N.A. [1]
Patent ID US4968713
Title Certain Imidazole Compounds As Transglutaminase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D02XDG Drug Info N.A. Click to Show More [1]
2 D0A9OC Drug Info N.A. [1]
3 D0IE9E Drug Info N.A. [1]
4 D0Y3YK Drug Info N.A. [1]
Patent ID US4929630
Title Transglutaminase Inhibitors.
Applicant(s) Syntex, Inc
Representative Drug(s) D02OXG Drug Info N.A. Click to Show More [1]
2 D0MA2H Drug Info N.A. [1]
Patent ID US4912120
Title 3,5-Substituted 4,5-Dihydroisoxazoles As Transglutaminase Inhibitors.
Applicant(s) Syntex, Inc
Representative Drug(s) D02OXG Drug Info N.A. Click to Show More [1]
2 D0MA2H Drug Info N.A. [1]
Patent ID US20140322278
Title Modulation of Tissue Transglutaminase Activation In Disease.
Applicant(s) Leland Stanford Junior University
Representative Drug(s) D08UFW Drug Info N.A. Click to Show More [1]
2 D0KZ6T Drug Info N.A. [1]
3 D0Z1VM Drug Info N.A. [1]
Patent ID US8946197
Title Transglutaminse Tg2 Inhibitors, Pharmaceutical Compositions, and Methods of Use Thereof.
Applicant(s) Chdi Foundation, Inc
Representative Drug(s) D0U6CU Drug Info IC50 = 10 nM [1]
Patent ID US8937091
Title Inhibitor of Protein Crosslinking and Use of The Same.
Applicant(s) Japan Science and Technology Agency
Representative Drug(s) D00SAH Drug Info IC50 = 300 nM [1]
Patent ID US2013164813
Title Method for Inhibiting Transglutaminase 2 Activity Using 2-Alkyloxy-3-Phenylethynyl-4A,5- Dihydropyrido[2,3-B]Pyrazine Derivative.
Applicant(s) Dongguk University Industry-Academic Cooperation Foundation
Representative Drug(s) D0VC9V Drug Info IC50 = 33800 nM [1]
Patent ID US2010144860
Title Transglutaminase Inhibitor Comprising Egcg and A Method for Producing Thereof.
Applicant(s) National Cancer Center
Representative Drug(s) D0EA3E Drug Info IC50 = 520 nM [1]
Patent ID US8299040
Title Methods for Treating Cancer Targeting Transglutaminase.
Applicant(s) University of Texas
Representative Drug(s) D0QR0U Drug Info N.A. [1]
Patent ID US7265093
Title Drug Therapy for Celiac Sprue.
Applicant(s) Stanford University
Representative Drug(s) D0LO0I Drug Info N.A. [1]
Patent ID US5188830
Title Methods for Thrombolytic Therapy.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D04MQZ Drug Info N.A. [1]
Patent ID US2003225007
Title Sulfonamide Derivatives of 3-Substituted Imidazol[1,2-D]-1,2,4-Thiadiazoles and 3-Substituted-[1,2,4] Thiadiazolo [4,5-A] Benzimidazole As Inhibitors of Fibrin Cross-Linking and Transglutamin.
Applicant(s) Apotex Inc
Representative Drug(s) D0KK6L Drug Info N.A. [1]
Patent ID US2002132776
Title Inhibitors of Transglutaminase.
Applicant(s) N Zyme Biotech Gmbh
Representative Drug(s) D04LLK Drug Info N.A. [1]
Patent ID US8754033
Title Peptides for Inhibiting Transglutaminase.
Applicant(s) National Cancer Center
Patent ID US5047416
Title Triazole Compounds and Their Use As Transglutaminase Inhibitors.
Applicant(s) Merck & Co., Inc
Patent ID US5124358
Title Effect of Transglutaminase Inhibition On Microfilariae DevelOpment and Macrofilariae Viability.
European Patent Office (EPO)
Patent ID EP1648924
Title Transglutaminase Inhibitors and Methods of Using The Same.
Applicant(s) Aston University
Representative Drug(s) D05ZTV Drug Info N.A. Click to Show More [1]
2 D0H4PF Drug Info N.A. [1]
3 D0K6SZ Drug Info N.A. [1]
Patent ID EP1602719
Title Control of Transglutaminase Catalyzed Protein Modification By Selective Irreversible Transglutaminase Inhibitors.
Applicant(s) N Zyme Biotech Gmbh
Representative Drug(s) D03JCI Drug Info N.A. Click to Show More [1]
2 D0NB4O Drug Info N.A. [1]
Japan Patent Office (JPO)
Patent ID JP2013180955
Title Tissue TransglutamiNase Inhibitors Containing Chalcone Derivatives (1 Thienyl-3-Phenyl-2-Propen-1-Ones) and Anti-Alzheimer Agents Containing Them.
Applicant(s) Toray Industries, Inc
Representative Drug(s) D0G3QD Drug Info IC50 = 928 nM [1]
Italian Patent and Trademark Office (UIBM)
Patent ID IT1264084
Title Peptide Effective As Substrate and/or Inhibitor of The Transglutaminase Enzyme and Use Thereof for Diagnostics and Therapeutics.
Applicant(s) Raggio-Italgene Spa
Korean Intellectual Property Office (KIPO)
Patent ID KR20100056212
Title A Pharmaceutical Composition for Preventing or Treating Transglutaminase-Related Disease Comprising Sulfarlem, and A Method for Preventing or Treating Transglutaminase-Related Disease By Using Thereof.
Applicant(s) National Cancer Center
Representative Drug(s) D0C2QU Drug Info IC50 = 390 nM [1]
Patent ID KR20100011620
Title A Composition for Transglutaminase Inhibitor Comprising Curcumin.
Applicant(s) National Cancer Center
Representative Drug(s) D0IQ8I Drug Info IC50 = 7500 nM [1]
Patent ID KR1145930
Title Transglutaminase Inhibitor Containing Chlorogenic Acid and Its Preparation Method.
Applicant(s) National Cancer Center
Representative Drug(s) D0MF2V Drug Info IC50 = 1490 nM [1]
Patent ID KR101192699
Title A Pharmaceutical Composition for Preventing or Treating Transglutaminase-Related Disease Comprising Oltipraz, and A Method for Preventing or Treating Transglutaminase-Related Disease By Using Thereof.
Applicant(s) National Cancer Center
Representative Drug(s) D08QGR Drug Info IC50 = 2750 nM [1]
References  Top
REF 1 Transglutaminase inhibitors: a patent review.Expert Opin Ther Pat. 2016;26(1):49-63.

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