676494-67-0

Upstream product

• 90178-71-5 4-(4-formylphenoxy)benzonitrile 
• 1194-02-1 4-fluorobenzonitrile 
• 123-08-0 4-hydroxy-benzaldehyde 
• 619-57-8 p-hydroxybenzamide 
• 459-57-4 4-fluorobenzaldehyde 

Downstream Products

• 1337568-20-3 4-[4-({4-[(5R)-3-cyclohexyl-2-oxo-5-phenylimidazolidin-1-yl]piperidin-1-yl}methyl)phenoxy]benzamide 
• 1394355-30-6 C₃₀H₃₁N₃O₄S₂ 
• 1394356-08-1 C₃₃H₃₆N₄O₄S₂ 
• 1394356-07-0 C₃₂H₃₄N₄O₄S₂ 
• 1394356-06-9 C₃₁H₃₂N₄O₄S₂ 
• 1394356-03-6 C₂₈H₂₇N₃O₅S₂ 
• 1394356-01-4 C₃₀H₂₉N₃O₅S₂ 
• 1394355-98-6 C₃₁H₃₁N₃O₄S₂ 
• 1394355-95-3 C₃₀H₂₉N₃O₄S₂ 
• 1394355-92-0 C₂₉H₂₉N₃O₄S₂ 

Relevant academic research and scientific papers

HETEROARYLPHENOXY BENZAMIDE KAPPA OPIOID LIGANDS

The present invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R9, X, m and n are as defined herein; processes for the prepa

4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10

Human Diphtheria toxin-like ADP-ribosyltranferases (ARTD) 10 is an enzyme carrying out mono-ADP-ribosylation of a range of cellular proteins and affecting their activities. It shuttles between cytoplasm and nucleus and influences signaling events in both compartments, such as nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) signaling and S phase DNA repair. Furthermore, overexpression of ARTD10 induces cell death. We recently reported on the discovery of a hit compound, OUL35 (compound 1), with 330 nM potency and remarkable selectivity towards ARTD10 over other enzymes in the human protein family. Here we aimed at establishing a structure-activity relationship of the OUL35 scaffold, by evaluating an array of 4-phenoxybenzamide derivatives. By exploring modifications on the linker between the aromatic rings, we identified also a 4-(benzyloxy)benzamide derivative, compound 32, which is potent (IC50 = 230 nM) and selective, and like OUL35 was able to rescue HeLa cells from ARTD10-induced cell death. Evaluation of an enlarged series of derivatives produced detailed knowledge on the structural requirements for ARTD10 inhibition and allowed the discovery of further tool compounds with submicromolar cellular potency that will help in understanding the roles of ARTD10 in biological systems.

NOVEL BRADYKININ B1-ANTAGONISTS

The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.

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.