Patent(s) and the Corresponding Patented Drug(s) |
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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 |
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[1] |
2
|
D0M3NR
|
Drug Info
|
IC50 = 6 nM
|
[1] |
3
|
D00CDI
|
Drug Info
|
IC50 = 7 nM
|
[1] |
4
|
D0L9AS
|
Drug Info
|
IC50 = 7 nM
|
[1] |
5
|
D0K2RX
|
Drug Info
|
IC50 = 7.1 nM
|
[1] |
6
|
D00TCL
|
Drug Info
|
IC50 = 7.5 nM
|
[1] |
7
|
D0R7UI
|
Drug Info
|
IC50 = 8.3 nM
|
[1] |
8
|
D0O8MI
|
Drug Info
|
IC50 = 8.5 nM
|
[1] |
9
|
D0IL0Y
|
Drug Info
|
IC50 = 18 nM
|
[1] |
10
|
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 |
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[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 |
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[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. |
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. |
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 |
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[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] |