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 T40332 Target Info
Target Name Neutrophil elastase (NE)
Synonyms PMN elastase; Medullasin; Human leukocyte elastase; HLE; Elastase-2; ELA2; Bone marrow serine protease
Target Type Clinical trial Target
Gene Name ELANE
Biochemical Class Peptidase
UniProt ID
ELNE_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2013037809
Title Tetrahydrotriazolopyrimidine Derivatives As Human Neutrophil Elastase Inhibitors.
Abstract Compounds of formula (I) are inhibitors of human neutrophil elastase.
Applicant(s) Chiesi Farmaceutici Spa
Representative Drug(s) D07RRV Drug Info N.A. [1]
Patent ID WO2011110858
Title Pyrimidine Derivatives and Their Use In The Treatment of Respiratory Diseases Such As Copd.
Abstract Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C-R1 or N; -X1-X2- is CR15=N- or -NR19-CO-; and R1-R6, R15, R15 and R19 are as defined in the claims.
Applicant(s) Chiesi Farmaceutici Spa
Representative Drug(s) D02UCA Drug Info IC50 = 1 to 200 nM [1]
Patent ID WO2009130615
Title Use of Deuterium Oxide As An Elastase Inhibitor.
Abstract The invention relates to the use of deuterium oxide (D2O) as an elastase inhibitor and especially as an inhibitor of the human neutrophil elastase (HNE). The invention also relates to the use of deuterium oxide for the prophylaxis and/or treatment of HNE-related diseases.
Applicant(s) D2 Bioscience Group Ltd
Representative Drug(s) D02IXA Drug Info 40% inhibition = 100000 nM; IC50 = 3.5 to 350 nM [1]
Patent ID WO2017102674
Title Novel Tetrahydrotriazolopyrimidine Derivatives As Nhe Inhibitors.
Abstract This invention relates to triazolinone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.
Applicant(s) Chiesi Farmaceutici Spa
Patent ID WO2016050835
Title Selective Inhibitors of Neutrophil Elastase for Treating Neuropathic Pain and Chronic Pain States Harbouring A Neuropathic Component.
Abstract The present invention relates to selective inhibitors of neutrophil elastase, also called leukocyte elastase (LE) for use in the diagnosis, prognosis, prevention and/or treatment of neuropathic pain and chronic pain states harbouring a neuropathic component. The present invention further relates to pharmaceutical compositions and methods of diagnosing, prognosing, preventing and/or treating neuropathic pain and chronic pain states harbouring a neuropathic component.
Applicant(s) Ruprecht - Karls - Universit Heidelberg
Patent ID WO2015091281
Title Tetrahydrotriazolopyrimidine Derivatives As Human Neutrophil Elastase Inhibitors.
Abstract This invention relates to heterocyclic compounds, which are pyrimidinone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.
Applicant(s) Chiesi Farmaceutici Spa
United States Patent and Trademark Office (USPTO)
Patent ID US20148658604
Title Template-Fixed Beta-Hairpin Peptidomimetics with Protease Inhibitory Activity.
Representative Drug(s) D09ZUJ Drug Info IC50 = 6 nM Click to Show More [1]
2 D0M3NR Drug Info IC50 = 6 nM [1]
3 D0W3EJ Drug Info IC50 = 6 nM [1]
4 D00CDI Drug Info IC50 = 7 nM [1]
5 D0L9AS Drug Info IC50 = 7 nM [1]
6 D0K2RX Drug Info IC50 = 7.1 nM [1]
7 D00TCL Drug Info IC50 = 7.5 nM [1]
8 D0ZW9O Drug Info IC50 = 8 nM [1]
9 D0ZA3S Drug Info IC50 = 8.2 nM [1]
10 D0R7UI Drug Info IC50 = 8.3 nM [1]
11 D0O8MI Drug Info IC50 = 8.5 nM [1]
12 D0IL0Y Drug Info IC50 = 18 nM [1]
13 D0M6WD Drug Info IC50 = 28 nM [1]
Patent ID US20140057916
Title Substituted 4-Pyridones and Their Use As Inhibitors of Neutrophil Elastase Activity.
Representative Drug(s) D09EPZ Drug Info IC50 < 1 to 1900 nM Click to Show More [1]
2 D00WHH Drug Info IC50 = 3 to 98 nM [1]
Patent ID US20110003858
Title Multimeric Heterocyclic Compounds Useful As Neutrophil Elastase Inhibitors.
Representative Drug(s) D09VDQ Drug Info IC50 = 0.26 nM [1]
Patent ID US20100280048
Title Some 2-Pyrazinone Derivatives and Their Use As Inhibitors of Neutrophile Elastase.
Representative Drug(s) D0EE5S Drug Info IC50 = 1.4 nM Click to Show More [1]
2 D06TAS Drug Info IC50 = 2.2 nM [1]
3 D0S9NB Drug Info IC50 = 2.8 nM [1]
4 D0B5QU Drug Info IC50 = 3.5 nM [1]
5 D0M3EA Drug Info IC50 = 4.2 nM [1]
6 D0R2TH Drug Info IC50 = 11 nM [1]
Patent ID US20140249129
Title Substituted Bicyclic Dihydropyrimidinones and Their Use As Inhibitors of Neutrophil Elastase Activity.
Representative Drug(s) D0NS8V Drug Info IC50 < 1 to 7000 nM [1]
Patent ID US20140179670
Title Uracil Derivative and Use Thereof for Medical Purposes.
Representative Drug(s) D02IXA Drug Info 40% inhibition = 100000 nM; IC50 = 3.5 to 350 nM [1]
Patent ID US20128288402
Title 4-(4-Cyano-2-Thioaryl)Dihydropyrimidinones and Their Use.
Representative Drug(s) D0W6PE Drug Info IC50 < 0.3 to 10 nM [1]
Patent ID US20140221335
Title Substituted Bicyclic Dihydropyrimidinones and Their Use As Inhibitors of Neutrophil Elastase Activity.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D07RRV Drug Info N.A. [2]
Patent ID US20140045802
Title 4-(4-Cyano-2-Thioaryl)Dihydropyrimidinones and Their Use.
Applicant(s) Bayer Intellectual Property Gmbh
Representative Drug(s) D07RRV Drug Info N.A. [2]
Patent ID US9346794
Title Substituted 4-Pyridones and Their Use As Inhibitors of Neutrophil Elastase Activity.
Representative Drug(s) D07RRV Drug Info N.A. [2]
Patent ID US20170166574
Title Novel Compounds.
Applicant(s) Chiesi Farmaceutici Spa
Patent ID US20140287985
Title Novel Uses of Elafin.
Applicant(s) Proteo Biotech Ag
European Patent Office (EPO)
Patent ID EP20131663973
Title 2-Pyridone Derivatives As Neutrophil Elastase Inhibitors and Their Use.
Patent ID EP20122483244
Title 2-Pyridone Compounds Used As Inhibitors of Neutrophil Elastase.
Patent ID EP20122066662
Title Serine Hydrolase Inhibitors.
Patent ID EP20121723121
Title 1,4-Diaryl-Dihydropyrimidin-2-Ones and Their Use As Human Neutrophil Elastase Inhibitors.
Patent ID EP20102024367
Title Tetrahydropyrrolopyrimidinediones and Their Use As Human Neutrophil Elastase Inhibitors.
Representative Drug(s) D0HU0O Drug Info IC50 = 1 to 50 nM [1]
Patent ID EP20101856059
Title Multimers of Pyrimidinone Derivatives and Their Use As Human Neutrophil Elastase Inhibitors.
China National Intellectual Property Administration (CNIPA)
Patent ID CN103269585
Title Hypersulfated Disaccharides To Treat Elastase Related Disorders.
Representative Drug(s) D0VU3I Drug Info N.A. [1]
Canadian Intellectual Property Office (CIPO)
Patent ID CA2751436
Title Peptides Used In The Treatment and/or Care of The Skin, Mucous Membranes and/or Scalp and Their Use In Cosmetic or Pharmaceutical Compositions.
Representative Drug(s) D0TP0X Drug Info IC50 = 94000 nM Click to Show More [1]
2 D0A6AJ Drug Info IC50 = 103000 nM [1]
3 D08HBW Drug Info IC50 = 410000 nM [1]
Patent ID CA20142650553
Title 2-Pyrazinone Derivatives for The Treatment of Disease or Condition In Which Inhibition of Neutrophil Elastase Activity Is Beneficial.
Representative Drug(s) D00YXL Drug Info IC50 = 0.33 to 1 nM [1]
References  Top
REF 1 Neutrophil elastase inhibitors: a patent review and potential applications for inflammatory lung diseases (2010 - 2014).Expert Opin Ther Pat. 2015;25(10):1145-58.
REF 2 Serine protease inhibitors to treat inflammation: a patent review (2011-2016).Expert Opin Ther Pat. 2018 Feb;28(2):93-110.

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