1616809-39-2

Upstream product

• 37098-75-2 2-fluoro-5-chlorosulfonylbenzoic acid 
• 3863-11-4 3,4-difluoroaniline 
• 445-29-4 o-fluoro-benzoic acid 
• 949485-81-8 5-(chlorosulfonyl)-2-fluorobenzoyl chloride 

Downstream Products

• 1616807-58-9 N-(3,4-difluorophenyl)-2-fluoro-5-(N-tert-pentylsulfamoyl)benzamide 
• 1616807-77-2 N-(3,4-difluorophenyl)-5-(N-(1-ethylcyclopropyl)sulfamoyl)-2-fluorobenzamide 
• 1616807-78-3 (R)-5-(N-(1-cyclopropylethyl)sulfamoyl)-N-(3,4-difluorophenyl)-2-fluorobenzamide 
• 1616807-98-7 N-(3,4-difluorophenyl)-2-fluoro-5-(N-(1-(pyrimidin-2-yl)ethyl)sulfamoyl)benzamide 
• 1616807-99-8 N-(3,4-difluorophenyl)-2-fluoro-5-(N-(1-(pyridin-2-yl)ethyl)sulfamoyl)benzamide 
• 1616808-07-1 (S)-5-(N-(1-cyclopropyl-2,2,2-trifluoroethyl)sulfamoyl)-N-(3,4-difluorophenyl)-2-fluorobenzamide 
• 1616809-05-2 (S)-2-(3-((3,4-difluorophenyl)carbamoyl)-4-fluorophenylsulfonamido)propanoic acid 
• 1616808-32-2 5-(N-cyclopropylsulfamoyl)-N-(3,4-difluorophenyl)-2-fluorobenzamide 

Relevant academic research and scientific papers

Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector

The synthesis of novel series of sulfamoylbenzamides as HBV capsid assembly effector is reported. The structure was divided into five parts which were independently modified as part of our lead optimization. All synthesized compounds were evaluated for their anti-HBV activity and toxicity in human hepatocytes, lymphocytes and other cells. Additionally, we assessed their effect on HBV cccDNA formation in an HBeAg reporter cell-based assay. Among the 27 compounds reported, several analogs exhibited submicromolar activities and significant reduction of HBeAg secretion. Selected compounds were studied under negative-stain electron microscopy for their ability to disrupt the HBV capsid formation. Structures were modeled into a binding site recently identified in the HBV capsid protein for similar molecules to rationalize the structure-activity relationships for this family of compounds.

ELIMINATION OF HEPATITIS B VIRUS WITH ANTIVIRAL AGENTS

The present invention is directed to compounds, compositions and methods for preventing, treating or curing Hepatitis B (HBV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment, prevention or eradication of HBV infection.

NOVEL ANTIVIRAL AGENTS AGAINST HBV INFECTION

The present invention is directed toward novel compounds and novel methods of use of said compounds of the formula (I), useful as nucleocapsid assembly inhibitors for the treatment of viruses, especially but not exclusively, including pregenomic RNA encapsidation inhibitors of HBV for the treatment of Hepatitis B virus (HBV) infection and related conditions. (Formula (I)) Including hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein A, R1, R2, R3, R4, R5, R6, R7, and R8 are defined herein.