55114-90-4

Upstream product

• 67-56-1 methanol 
• 16807-37-7 5-methoxy-2-sulfanyl-benzoic acid 
• 2612-02-4 5-methoxysalicylic acid 
• 2905-82-0 methyl 5-methoxy-2-hydroxybenzoate 
• 104795-62-2 methyl-2-((N,N-dimethylcarbamoyl)thio)-5-methoxybenzoate 
• 345924-12-1 5-methoxy-2-trifluoromethanesulfonyloxy benzoic acid methyl ester 
• 104795-61-1 methyl 2-((dimethylcarbamothioyl)oxy)-5-methoxybenzoate 

Downstream Products

• 944061-01-2 methyl 2-[(cyanomethyl)thio]-5-methoxybenzoate 
• 944061-05-6 3-hydroxy-5-methoxy-1-benzothiophene-2-carbonitrile 
• 145903-32-8 7-methoxy-3,4-dihydrobenzo[f][1,4]thiazepin-5(2H)-one 
• 145903-31-7 7-methoxy-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine 

Relevant academic research and scientific papers

Discovery of Ziresovir as a Potent, Selective, and Orally Bioavailable Respiratory Syncytial Virus Fusion Protein Inhibitor

Ziresovir (RO-0529, AK0529) is reported here for the first time as a promising respiratory syncytial virus (RSV) fusion (F) protein inhibitor that currently is in phase 2 clinical trials. This article describes the process of RO-0529 as a potent, selective, and orally bioavailable RSV F protein inhibitor and highlights the in vitro and in vivo anti-RSV activities and pharmacokinetics in animal species. RO-0529 demonstrates single-digit nM EC50 potency against laboratory strains, as well as clinical isolates of RSV in cellular assays, and more than one log viral load reduction in BALB/c mouse model of RSV viral infection. RO-0529 was proven to be a specific RSV F protein inhibitor by identification of drug resistant mutations of D486N, D489V, and D489Y in RSV F protein and the inhibition of RSV F protein-induced cell-cell fusion in cellular assays.

HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS

ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.

Synthesis and structure activity relationship studies of benzothieno[3,2-b]furan derivatives as a novel class of IKKβ inhibitors

As a novel class of IKKβ inhibitors, a series of tricyclic furan derivatives was designed and synthesized based on the structure of known thiophene IKKβ inhibitors. Among the various fused furan derivatives synthesized, a benzothieno[3,2-b]furan derivative 13a displayed potent inhibitory activity towards IKKβ in enzymatic and cellular assays. The potent inhibitory activity originates from an intramolecular non-bonded S...O interaction which was confirmed by the X-ray structure of JNK3 with 16k. The introduction of further substituents on the core structure led to the discovery of the 6-alkoxy derivatives, which possessed a comparable IKKβ inhibitory activity to 13a and an improved metabolic stability. Among these, appropriately lipophilic compounds 16a, h, i, and 13g (logD>2) were found to possess good oral bioavailability.

1,4-benzothiazepine derivatives

An object of the invention is to provide compounds having a myocardial KD (Kinetic cell death)-inhibiting effect without being accompanied by a cardiodepressant effect. A 1,4-benzothiazepine derivative represented by the following Formula [I]: STR1 wherei