4928-46-5

Usage

Classification

Class Ic antiarrhythmic agent

Uses

Treats various types of cardiac arrhythmias including atrial fibrillation, supraventricular tachycardia, and ventricular arrhythmias

Mechanism of action

Inhibits sodium channels in the heart, stabilizing the heart's electrical activity and preventing abnormal rhythms

Administration

Typically administered orally

Half-life

Relatively long, allowing for twice daily dosing in most patients

Contraindications

Should be used with caution in individuals with structural heart disease or a history of heart failure, as it can increase the risk of serious cardiac events

Side effects

Common side effects include dizziness, blurred vision, and nausea. Can also cause potentially life-threatening proarrhythmia in some patients.

Upstream product

• 5418-51-9 5-nitro-2-hydroxypyridine 
• 4548-45-2 2-chloro-5-nitropyridine 
• 25948-15-6 2-(methyl(5-nitropyridin-2-yl)amino)ethanol 

Downstream Products

• 1419603-59-0 phenyl 6-((2-hydroxyethyl)(methyl)amino)pyridin-3-ylcarbamate 
• 1435933-31-5 C₂₀H₂₇N₃O₃ 
• 1435933-34-8 C₂₀H₂₇N₃O₃ 
• 1435933-35-9 C₂₀H₂₇N₃O₃ 
• 1435933-36-0 C₁₆H₁₉N₃O₃ 
• 1435933-37-1 C₁₉H₂₅N₃O₃ 
• 1435933-38-2 C₁₇H₁₈F₃N₃O₃ 
• 1435933-39-3 C₂₆H₃₃N₃O₃ 
• 1435933-40-6 C₂₄H₃₅N₃O₃ 
• 1435933-41-7 C₂₀H₂₆BrN₃O₃ 
• 1419599-68-0 1-((1-(3-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl)methyl)-3-(6-((2-hydroxyethyl)(methyl)amino)pyridin-3-yl)urea 
• 1403246-79-6 5-[2-({6-[(2-hydroxyethyl)(methyl)amino]pyridin-3-yl}amino)pyrimidin-4-yl]-2-(tetrahydro-2H-pyran-4-yloxy)benzonitrile 

Relevant academic research and scientific papers

SUBSTITUTED HETEROAROMATIC PYRAZOLE-CONTAINING CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS

The invention relates to substituted heteroaromatic pyrazole-containing carboxamide and urea derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

Substituted Heteroaromatic Pyrazole-Containing Carboxamide and Urea Compounds as Vanilloid Receptor Ligands

Substituted heteroaromatic pyrazole-containing carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also to a method of using these compounds for treating and/or inhibiting pain and further diseases and/or disorders.

SUBSTITUTED HETEROCYCLIC AZA DERIVATIVES

The invention relates to heterocyclic aza derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

Substituted Heterocyclic Aza Compounds

Heterocyclic aza compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also methods of using these compounds for the treatment and/or inhibition of pain and further diseases and/or disorders.

Discovery of potent transient receptor potential vanilloid 1 antagonists: Design and synthesis of phenoxyacetamide derivatives

We aimed to discover a novel type of transient receptor potential vanilloid 1 (TRPV1) antagonist because such antagonists are possible drug candidates for treating various disorders. We modified the structure of hit compound 7 (human TRPV1 IC50 = 411 nM) and converted its pyrrolidino group to a (hydroxyethyl)methylamino group, which substantially improved inhibitory activity (15d; human TRPV1 IC50 = 33 nM). In addition, 15d ameliorated bladder overactivity in rats in vivo.

COMPOSITIONS AND THERAPEUTIC USES OF IKK-RELATED KINASE EPSILON AND TANKBINDING KINASE 1 INHIBITORS

The invention relates to compounds, pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders.

Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors

In a discovery effort to find safe and effective DGAT-1 inhibitors, we have identified 2-phenyloxazole 4-carboxamide 1 as a conformationally constrained analog of a hydrazide hit, which was previously identified from high-throughput screening. Further optimization of this series has led to chemically more stable 2-phenyloxazole-based DGAT-1 inhibitor 25 with improved solubility, cell-based activity, and pharmacokinetic properties. Compound 25 also demonstrated in vivo efficacy in a diet-induced obesity (DIO) rat model.

PYRIMIDINE DERIVATIVES CAPABLE OF INHIBITING ONE OR MORE KINASES

A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, formula (I): wherein: R1 is C3-8-cycloalkyl; X is O, NR7 or C3-6-heterocycloalkyl; R2 is aryl, heteroaryl, fused or unfused aryl-C3-6-heterocycloalkyl or fused or unfused heteroaryl-C3-6-heterocycIoalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C1-6-alkyl, C3-7-cycloalkyl and a group A, wherein said C1-6-alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R10 and a group A, said heteroaryl group is optionally substituted by one or more R10 groups; and wherein said C3-6-heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R3 is C1-6-alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, -NR4R5, -OR6, -NR7(CO)R6, -NR7(CO)NR4R5, -NR7SO2R6, -NR7COOR7, -CONR4R5, C3-6-heterocycloalkyl and formula (a, b, c): wherein R4-7 and A are as defined in the claims. Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases.

Diacylglycerol acyltransferase inhibitors

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.