72178-85-9

Upstream product

• 639517-92-3 3-(2-chlorophenoxy)benzonitrile 
• 95-57-8 2-monochlorophenol 
• 87199-16-4 3-Formylphenylboronic acid 
• 3132-99-8 m-bromobenzoic aldehyde 

Downstream Products

• 742054-39-3 2-(4-{1-[3-(2-chloro-phenoxy)-benzyl]-piperidin-4-ylcarbamoyl}-4-phenyl-piperidin-1-yl)-2-methyl-propionic acid ethyl ester 
• 521975-85-9 4-{1-[3-(2-chlorophenoxy)benzyl]piperidin-4-ylcarbamoyl}-4-phenylpiperidine-1-carboxylic acid tert-butyl ester 
• 889654-15-3 4-amino-1-[3-(2-chlorophenoxy)benzyl]piperidine-4-carboxylic acid methyl ester 

Relevant academic research and scientific papers

DUAL MAGL AND FAAH INHIBITORS

Provided herein are compounds and pharmaceutical compositions comprising said compounds useful as modulators of MAGL and/or FAAH. The subject compounds and compositions are useful for the treatment of pain and neurological disorders.

PYRAZOLE MAGL INHIBITORS

Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Probing the Hydrophobic Binding Pocket of G-Protein-Coupled Lysophosphatidylserine Receptor GPR34/LPS1 by Docking-Aided Structure-Activity Analysis

The ligands of certain G-protein-coupled receptors (GPCRs) have been identified as endogenous lipids, such as lysophosphatidylserine (LysoPS). Here, we analyzed the molecular basis of the structure-activity relationship of ligands of GPR34, one of the LysoPS receptor subtypes, focusing on recognition of the long-chain fatty acid moiety by the hydrophobic pocket. By introducing benzene ring(s) into the fatty acid moiety of 2-deoxy-LysoPS, we explored the binding site's preference for the hydrophobic shape. A tribenzene-containing fatty acid surrogate with modifications of the terminal aromatic moiety showed potent agonistic activity toward GPR34. Computational docking of these derivatives with a homology modeling/molecular dynamics-based virtual binding site of GPR34 indicated that a kink in the benzene-based lipid surrogates matches the L-shaped hydrophobic pocket of GPR34. A tetrabenzene-based lipid analogue bearing a bulky tert-butyl group at the 4-position of the terminal benzene ring exhibited potent GPR34 agonistic activity, validating the present hydrophobic binding pocket model.

Design, synthesis, and progress toward optimization of potent small molecule antagonists of CC chemokine receptor 8 (CCR8)

Activation of CCR8 by its ligand CCL1 may play an important role in diseases such as asthma, multiple sclerosis, and cancer. The study of small molecule CCR8 antagonists will help establish the validation of these hypotheses. We report the design, synthesis, and progress toward optimization of potent small molecule CCR8 antagonists identified from a high-throughput screen. These analogues exhibit good potency in binding and chemotaxis assays, show good selectivity versus the hERG channel, and have good eADME (early absorption, distribution, metabolism, and excretion) profiles.

INHIBITORS OF HCV NS5B POLYMERASE

The present invention porivdes compounds of Formula I, compositons and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases.