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Approval Year

Substance Class
Concept
Record UNII
U9DE68P1CA
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BAY-85-8501
Code English
5-PYRIMIDINECARBONITRILE, 4-(4-CYANO-2-(METHYLSULFONYL)PHENYL)-1,2,3,4-TETRAHYDRO-3,6-DIMETHYL-2-OXO-1-(3-(TRIFLUOROMETHYL)PHENYL)-, (4S)-
Systematic Name English
(4S)-4-(4-CYANO-2-(METHYLSULFONYL)PHENYL)-1,2,3,4-TETRAHYDRO-3,6-DIMETHYL-2-OXO-1-(3-(TRIFLUOROMETHYL)PHENYL)-5-PYRIMIDINECARBONITRILE
Systematic Name English
BAY 85-8501
Code English
Code System Code Type Description
CLINICAL_TRIALS.GOV
BAY-85-8501
Created by admin on Fri Jun 25 23:44:37 UTC 2021 , Edited by admin on Fri Jun 25 23:44:37 UTC 2021
PRIMARY Official Title: A Phase IIa, Randomized, Double-blind, Placebo-controlled, Parallel Group Study to Assess the Safety and Efficacy of 28 Day Oral Administration of BAY85-8501 in Patients With Non-Cystic Fibrosis BronchiectasisPurpose: The primary objective of this study is to assess the safety and tolerability of 28 day oral administration of BAY85-8501 versus placebo in subjects with non-CF Bronchiectasis (BE).The secondary objectives are to examine the effect of BAY85-8501 on pulmonary function, biomarkers of inflammation and tissue damage, and the impact on overall health and perceived well-being and to evaluate the pharmacokinetics of BAY85-8501.
MANUFACTURER PRODUCT INFORMATION
BAY-85-8501
Created by admin on Fri Jun 25 23:44:37 UTC 2021 , Edited by admin on Fri Jun 25 23:44:37 UTC 2021
PRIMARY Human neutrophil elastase (HNE) is a key protease for matrix degradation. High HNE activity is observed in inflammatory diseases. Accordingly, HNE is a potential target for the treatment of pulmonary diseases such as chronic obstructive pulmonary disease (COPD), acute lung injury (ALI), acute respiratory distress syndrome (ARDS), bronchiectasis (BE), and pulmonary hypertension (PH).
PUBCHEM
66601502
Created by admin on Fri Jun 25 23:44:37 UTC 2021 , Edited by admin on Fri Jun 25 23:44:37 UTC 2021
PRIMARY
CAS
1161921-82-9
Created by admin on Fri Jun 25 23:44:37 UTC 2021 , Edited by admin on Fri Jun 25 23:44:37 UTC 2021
PRIMARY
FDA UNII
U9DE68P1CA
Created by admin on Fri Jun 25 23:44:37 UTC 2021 , Edited by admin on Fri Jun 25 23:44:37 UTC 2021
PRIMARY
This is a non-substance concept
Related Record Type Details
TARGET -> INHIBITOR
IC50
Related Record Type Details
ACTIVE MOIETY
Human neutrophil elastase (HNE) is a key protease for matrix degradation. High HNE activity is observed in inflammatory diseases. While maintaining outstanding target selectivity, picomolar potency was achieved by locking the bioactive conformation of these inhibitors with a strategically positioned methyl sulfone substituent. An induced-fit binding mode allowed tight interactions with the S2 and S1 pockets of HNE. BAY 85-8501 ((4S)-4-(4-cyano-2-(methylsulfonyl)phenyl)-3,6-dimethyl-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2,3,4-tetrahydropyrimidine-5-carbonitrile) was shown to be efficacious in a rodent animal model related to ALI. BAY 85-8501 is currently being tested in clinical studies for the treatment of pulmonary diseases.
This is a non-substance concept