716358-46-2

Upstream product

• 4025-64-3 3-Carboxybenzenesulfonyl chloride 
• 75-31-0 isopropylamine 

Downstream Products

• 1572510-78-1 C₁₇H₁₈F₂N₂O₃S 
• 1572510-72-5 C₁₇H₁₇F₃N₂O₃S 
• 1572515-81-1 N-(3-bromo-4,5-difluorophenyl)-3-(N-isopropylsulfamoyl)benzamide 
• 1572511-14-8 C₁₇H₁₉FN₂O₄S 
• 1572513-34-8 C₁₈H₂₁FN₂O₃S 
• 1572510-51-0 N-(4-fluoro-3-methylphenyl)-3-(isopropylsulfamoyl)benzamide 
• 1286906-97-5 N-(3,4-difluorophenyl)-3-(isopropylsulfamoyl)benzamide 
• 1328738-57-3 N-(4-fluorophenyl)-3-(isopropylsulfamoyl)benzamide 
• 1421506-62-8 (E)-3-(6-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-N-isopropyl-benzene-sulfonamide 
• 1421506-16-2 (E/Z)-3-(6-chloro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-N-isopropyl-benzenesulfonamide 
• 620600-39-7 3-(hydroxymethyl)-N-isopropylbenzenesulfonamide 

Relevant academic research and scientific papers

Synthesis and Evaluation of N-Phenyl-3-sulfamoyl-benzamide Derivatives as Capsid Assembly Modulators Inhibiting Hepatitis B Virus (HBV)

Small molecule induced hepatitis B virus (HBV) capsid assembly modulation is considered an attractive approach for new antiviral therapies against HBV. Here we describe efforts toward the discovery of a HBV capsid assembly modulator in a hit-to-lead optimization, resulting in JNJ-632, a tool compound used to further profile the mode of action. Administration of JNJ-632 (54) in HBV genotype D infected chimeric mice resulted in a 2.77 log reduction of the HBV DNA viral load.

COMPOUNDS, IN PARTICULAR FOR USE IN THE TREATMENT OF A DISEASE OR CONDITION FOR WHICH A BROMODOMAIN INHIBITOR IS INDICATED

The invention relates to a compound for use in the treatment of a disease or condition for which a bromodomain inhibitor is indicated characterized by a general formula (1) and a compound according to formula (3).

N'-Alkylaminosulfonyl Analogues of 6-Fluorobenzylideneindolinones with Desirable Physicochemical Profiles and Potent Growth Inhibitory Activities on Hepatocellular Carcinoma

The benzylideneindolinone 6-chloro-3-(3′-trifluoromethylbenzylidene)-1,3-dihydroindol-2-one (4) was reported to exhibit potent and selective growth inhibitory effects on hepatocellular carcinoma (HCC). Corroborative evidence supported multi-receptor tyrosine kinase (RTK) inhibition as a possible mode of action. However, the poor physicochemical properties of 4 limited its furtherance as a lead compound. In this study, the modification of 4 was investigated with the aim of improving its potency and physicochemical profile. The 6-fluorobenzylideneindolinone 3-12 bearing a 3′-N-propylaminosulfonyl substituent was found to be a promising substitute. Compound 3-12 [6-fluoro-3-(3′-N-propylaminosulfonylbenzylidene)-1,3-dihydroindol-2-one] was found to be tenfold more soluble than 4 and to have sub-micromolar growth inhibitory activities on HCC cells. It is apoptogenic and inhibits the phosphorylation of several RTKs in HuH7, of which the inhibition of FGFR4 and HER3 are prominent. Compound 3-12 decreased the tumor load in a physiologically relevant orthotopic HCC xenograft murine model. Structure-activity relationships support pivotal roles for the fluoro and N′-propylaminosulfonyl moieties in enhancing cell-based activity and moderating the physicochemical profile (solubility, permeability) of 3-12.

SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Inhibitors of HBV replication of Formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein B, R1, R2 and R4 have the meaning as defined herein. The present invention also relates to pharmaceutical compositions containing these inhibitors and to their use, alone or in combination with other HBV inhibitors, in HBV therapy.

SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Inhibitors of HBV replication of Formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein B, R1, R2 and R4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

BENZYLIDENE-INDOLINONE COMPOUNDS AND THEIR MEDICAL USE

Compounds of general formula I: wherein R1a, R1b, R2, R3a, R3b and X are as defined herein are tyrosine kinase inhibitors and are useful for the treatment of various diseases and conditions, for examp

CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS

The present invention relates to compounds of formula (I) or pharmaceutically acceptable derivatives thereof, useful in the treatment or prophylaxis of CCR5-related diseases and disorders, for example, in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).