1088991-73-4

Basic information

• Product Name: MK 6096
• Synonyms: Filorexant;MK 6096;MK6096;MK-6096;((2R,5R)-5-(((5-Fluoropyridin-2-yl)oxy)methyl)-2-methylpiperidin-1-yl)(5-methyl-2-(pyrimidin-2-yl)phenyl)methanone MK6096;[(2R,5R)-5-[[(5-Fluoro-2-pyridinyl)oxy]methyl]-2-methyl-1-piperidinyl][5-methyl-2-(2-pyrimidinyl)phenyl]methanone;Filorexant(MK-6096);filorexant / MK-6096, CID25128145
• CAS NO: 1088991-73-4
• Molecular Formula: C₂₄H₂₅FN₄O₂
• Molecular Weight: 420.4793032
• Mol File: 1088991-73-4.mol
• Article Data: 5

Chemical Properties

• Boiling Point: 540.2±50.0 °C(Predicted)
• Appearance: /
• Density: 1.203±0.06 g/cm3(Predicted)
• PKA: 1.54±0.22(Predicted)
• CAS DataBase Reference: MK 6096(CAS DataBase Reference)
• NIST Chemistry Reference: MK 6096(1088991-73-4)
• EPA Substance Registry System: MK 6096(1088991-73-4)

Safety Data

• Hazardous Substances Data: 1088991-73-4(Hazardous Substances Data)

Usage

Description

Filorexant is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 2.5 and 0.31 nM, respectively, for the recombinant human receptors). It selectively inhibits OX1R and OX2R over a panel of more than 170 receptors and enzymes. Filorexant inhibits orexin A-induced calcium mobilization in CHO cells expressing recombinant human OX1R or OX2R (Kb = 11 nM for both). It decreases locomotor activity in rats during the dark cycle when administered at a dose of 10 mg/kg. Filorexant (0.5 mg/kg) reduces the time spent awake and decreases the latency to slow-wave sleep stage 1 (SWS1) and SWS2, but not rapid eye movement (REM) sleep, in dogs. It increases the duration of SWS2, but not SWS1 or REM sleep, in the same model.

Uses

Filorexant is a selective dual orexin receptor antagonist with potent sleep-promoting properties. It has advanced into phase II clinical trials for the treatment of insomnia.

Upstream product

• 1088994-22-2 5-methyl-2-(pyrimidin-2-yl)benzoic acid 
• 21740-00-1 5-bromo-2-iodo-benzoic acid 
• 1088993-93-4 5-fluoro-2-((3R,6R)-6-methyl-piperidin-3-ylmethoxy)pyridine 
• 42872-83-3 2-bromo-5-methylbenzylnitrile 
• 1088994-07-3 ((3R)-6-methylpiperidin-3-yl)-methanol 
• 1088994-09-5 ((3R,6R)-6-methylpiperidin-3-yl)methanol (1S)-(+)-10-camphorsulfonic acid 
• 1088994-12-0 (2R,5R)-2-methyl-5-(toluene-4-sulfonyloxymethyl)piperidine-1-carboxylic cid tert-butyl ester 
• 1009376-93-5 (2R,5R)-tert-butyl 5-(hydroxymethyl)-2-methylpiperidine-1-carboxylate 
• 1088994-14-2 (2R,5R)-5-(5-fluoro-pyridin-2-yloxymethyl)-2-methylpiperidine-1-carboxylic acid tert-butyl ester 
• 1088994-18-6 5-methyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid methyl ester 
• 1088994-20-0 5-methyl-2-(pyrimidin-2-yl)benzoic acid methyl ester 
• 84476-99-3 2,5-difluoropyridine 
• 1373917-20-4 5-methyl-2-pyrimidin-2-ylbenzonitrile 
• 1088994-03-9 (6R)-methyl-6-methyl-2-oxopiperidine-3-carboxylate 

Relevant articles and documents

Unusual pyrimidine participation: Efficient stereoselective synthesis of potent dual orexin receptor antagonist MK-6096

An asymmetric synthesis of dual orexin receptor antagonist MK-6096 (1) is described. Key steps for the trans-2,5-disubstituted piperidinyl ether fragment include a biocatalytic transamination, a trans-selective Mukaiyama aldol, and a regioselective pyridy

PROCESS FOR THE PREPARATION OF AN OREXIN RECEPTOR ANTAGONIST

The present invention is directed to processes for preparing a pyridyl piperidine compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexi

PYRIDYL PIPERIDINE OREXIN RECEPTOR ANTAGONISTS

The present invention is. directed to pyridyl piperidine compounds of formula (I) which are antagonists of orexin receptors, and which are useful' in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.