1443211-72-0

Usage

Uses

Used in Pharmaceutical Industry:
Eleclazine is used as a therapeutic agent for the treatment of cardiovascular conditions, particularly those involving ischemia and arrhythmias. Its anti-ischemic and antiarrhythmic properties contribute to its potential effectiveness in managing and preventing complications related to these conditions.
Used in Clinical Research:
Eleclazine is used as a research compound in the development of new treatments for cardiovascular diseases. Its pre-clinical properties provide valuable insights into its potential applications and mechanisms of action, paving the way for further research and development in the field of cardiology.

Upstream product

• 4068-76-2 5-bromo-2-hydroxy-benzoic acid methyl ester 
• 936643-80-0 2-(chloromethyl)pyrimidine hydrogen chloride 
• 1430092-39-9 C₁₆H₁₂F₃NO₃ 
• 740842-72-2 7-bromo-2,3,4,5-tetrahydrobenzo[f ][1,4]oxazepine hydrochloride 
• 703-51-5 2,3-dihydro-1,4-benzoxazepin-5(4H)-one 
• 1641-00-5 (2-carbomethoxyphenoxy)acetonitrile 
• 58430-20-9 methyl 5-bromo-2-(cyanomethoxy)benzoate 
• 6329-74-4 5-bromo-2-hydroxybenzamide 
• 1167416-56-9 methyl 5-bromo-2-{[2-({[(1,1-dimethylethyl)oxy]carbonyl}amino)ethyl]oxy}benzoate 
• 5755-05-5 7-bromo-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one 
• 139301-27-2 4-trifluoromethoxyphenylboronic acid 
• 49660-57-3 6-bromochroman-4-one 

Downstream Products

• 1448754-43-5 4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one HCl salt 

Relevant academic research and scientific papers

Deuterium-Substituted Oxazepin Compounds

Described are deuterium-substituted oxazepin compounds of structural Formula I, which are inhibitors/blockers of the late sodium current. Also described are pharmaceutical compositions comprising the deuterium-substituted oxazepin compounds, and methods of use thereof.

Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Late sodium current (late INa) is enhanced during ischemia by reactive oxygen species (ROS) modifying the Nav 1.5 channel, resulting in incomplete inactivation. Compound 4 (GS-6615, eleclazine) a novel, potent, and selective inhibitor of late INa, is currently in clinical development for treatment of long QT-3 syndrome (LQT-3), hypertrophic cardiomyopathy (HCM), and ventricular tachycardia-ventricular fibrillation (VT-VF). We will describe structure-activity relationship (SAR) leading to the discovery of 4 that is vastly improved from the first generation late INa inhibitor 1 (ranolazine). Compound 4 was 42 times more potent than 1 in reducing ischemic burden in vivo (S-T segment elevation, 15 min left anteriorior descending, LAD, occlusion in rabbits) with EC50 values of 190 and 8000 nM, respectively. Compound 4 represents a new class of potent late INa inhibitors that will be useful in delineating the role of inhibitors of this current in the treatment of patients.

METHODS OF TREATING HYPERTROPHIC CARDIOMYOPATHY

The present disclosure relates to a compound of formula (I) or formula (II) or a pharmaceutically acceptable salt thereof, for use in the treatment of hypertrophic cardiomyopathy.

COMPOUND AND METHODS FOR TREATING LONG QT SYNDROME

Described herein is a method of treating long QT syndrome by administration of an effective amount of a potent and selective late sodium ion channel blocker

PROCESSES FOR PREPARING FUSED HETEROCYCLIC ION CHANNEL MODULATORS

The present disclosure provides processes for the preparation of a compound of formula: which is a selective late sodium current inhibitor. The disclosure also provides compounds that are synthetic intermediates.

COMBINATION THERAPIES USING LATE SODIUM ION CHANNEL BLOCKERS AND POTASSIUM ION CHANNEL BLOCKERS

Described herein is a method for the treatment or prevention of atrial fibrillation and/or atrial flutter comprising administration of an effective amount of one or more of a potassium channel blocker and an effective amount of one or more of a late sodium channel blocker. Also provided are methods for modulating ventricular and atrial rhythm and rate. Also provided are pharmaceutical formulations that are suitable for such combined administration.