676501-68-1

Upstream product

• 33252-28-7 6-chloronicotinonitrile 
• 123-08-0 4-hydroxy-benzaldehyde 
• 3939-12-6 6-fluoro-3-pyridinecarbonitrile 

Downstream Products

• 859505-26-3 6-{4-[(3-methyl-butylamino)-methyl]-phenoxy}-nicotino-nitrile 
• 676494-70-5 6-(4-formylphenoxy)pyridine-3-carboxamide 
• 1346133-06-9 6-[4-[ [2-(3-pyridyl)pyrrolidin-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 
• 1346133-15-0 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 
• 859505-32-1 6-{4-[(2-thiophen-2-yl-ethylamino)-methyl]-phenoxy}-nicotinonitrile 

Relevant academic research and scientific papers

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.

2,6-DISUBSTITUTED PYRIDINES AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS

Disclosed are compounds of formula (I) wherein R1 and R2 are independently selected from hydrogen, halo, CF3, C1-4alkyl and allyl; Y represents (II), (III), (IV) or (V) wherein R3 represents CF3 or C1-4alkyl; and R3a represents CF3 or C1-4alkyl.

OPIOID RECEPTOR ANTAGONISTS

A compound of the formula (I); wherein the variables X1 to X10, R1 to R7 including R3', E, W, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, d