676494-70-5

Upstream product

• 6271-78-9 6-chloro-3-pyridinecarboxamide 
• 123-08-0 4-hydroxy-benzaldehyde 
• 676501-68-1 6-(4-formylphenoxy)-3-pyridinecarbonitrile 
• 3939-12-6 6-fluoro-3-pyridinecarbonitrile 

Downstream Products

• 1000995-43-6 C₂₂H₂₁N₃O₂ 
• 1346133-15-0 6-[4-[ (3,3-dimethyl-2-phenyl-azetidin-1-yl)methyl]phenoxy]pyridine-3-carboxamide 
• 1346133-17-2 6-[4-[[(2S)-3,3-dimethyl-2-phenyl-azetidin-1-yl]methyl]phenoxy]pyridine-3-carboxamide 
• 1346133-16-1 6-[4-[[(2R)-3,3-dimethyl-2-phenyl-azetidin-1-yl]methyl]phenoxy]pyridine-3-carboxamide 
• 1346133-14-9 6-[4-[[ (3-hydroxy-2,2-dimethyl-1-phenyl-propyl)amino]methyl]phenoxy]pyridine-3-carboxamide 
• 1346133-06-9 6-[4-[ [2-(3-pyridyl)pyrrolidin-1-yl]methyl]phenoxy]pyridine-3-carboxamide 
• 1423875-10-8 C₃₃H₃₁N₃O₄S 
• 1423875-08-4 C₂₄H₂₅N₃O₃S 
• 1423875-07-3 C₂₄H₂₅N₃O₄ 
• 1423875-12-0 C₃₂H₂₈FN₃O₃S 
• 1423875-11-9 C₃₂H₂₈N₄O₅S 
• 676495-63-9 6-{4-[4-(4-fluoro-phenyl)-piperazin-1-ylmethyl]-phenoxy}-nicotinamide 

Relevant academic research and scientific papers

Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp

Compounds 8a-d have been designed as bioisosters of tariquidar for imaging P-gp expression and density by PET. The results displayed that compounds 8b and 8d could be considered potential P-gp/BCRP ligands suitable as 11C and 18F radiotracers, respectively.

Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: Application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer

Arylphenylpyrrolidinylmethylphenoxybenzamides were found to have high affinity and selectivity for κ opioid receptors. On the basis of receptor binding assays in Chinese hamster ovary (CHO) cells expressing cloned human opioid receptors, (S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl) phenoxy)benzamide (25) had a Ki = 0.565 nM for κ opioid receptor binding while having a Ki = 35.8 nM for μ opioid receptors and a Ki = 211 nM for δ opioid receptor binding. Compound 25 was also a potent antagonist of κ opioid receptors when tested in vitro using a [35S]-guanosine 5′O-[3-thiotriphosphate] ([35S]GTP-γ-S) functional assay in CHO cells expressing cloned human opioid receptors. Compounds were also evaluated for potential use as receptor occupancy tracers. Tracer evaluation was done in vivo, using liquid chromatography-tandem mass spectrometry (LC/MS/MS) methods, precluding the need for radiolabeling. (S)-3-Chloro-4-(4-((2-(pyridine-3-yl)pyrrolidin-1-yl)methyl) phenoxy)benzamide (18) was found to have favorable properties for a tracer for receptor occupancy, including good specific versus nonspecific binding and good brain uptake.

DIARYL ETHERS AS OPIOID RECEPTOR ANTAGONIST

A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3', E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.