349098-74-4

Upstream product

• 98-74-8 4-Nitrobenzenesulfonyl chloride 
• 88-17-5 2-(trifluoromethyl)benzenamine 

Downstream Products

• 1613304-91-8 4-amino-N-isobutyl-N-(2-trifluoromethylphenyl)benzenesulfonamide 
• 1613303-88-0 1-methanesulfonylpiperidine-4-carboxylic acid {4-[isobutyl-(2-trifluoromethylphenyl)sulfamoyl]phenyl}amide 
• 1613304-90-7 N-isobutyl-4-nitro-N-(2-trifluoromethylphenyl)benzenesulfonamide 

Relevant academic research and scientific papers

DDX3X Helicase Inhibitors as a New Strategy to Fight the West Nile Virus Infection

Increased frequency of arbovirus outbreaks in the last 10 years represents an important emergence for global health. Climate warming, extensive urbanization of tropical regions, and human migration flows facilitate the expansion of anthropophilic mosquitos and the emerging or re-emerging of new viral infections. Only recently the human adenosinetriphosphatase/RNA helicase X-linked DEAD-box polypeptide 3 (DDX3X) emerged as a novel therapeutic target in the fight against infectious diseases. Herein, starting from our previous studies, a new family of DDX3X inhibitors was designed, synthesized, validated on the target enzyme, and evaluated against the West Nile virus (WNV) infection. Time of addition experiments after virus infection indicated that the compounds exerted their antiviral activities after the entry process, likely at the protein translation step of WNV replication. Finally, the most interesting compounds were then analyzed for their in vitro pharmacokinetic parameters, revealing favorable absorption, distribution, metabolism, and excretion values. The good safety profile together with a good activity against WNV for which no treatments are currently available, make this new class of molecules a good starting point for further in vivo studies.

USE OF DDX3 INHIBITORS AS ANTIPROLIFERATIVE AGENTS

The present invention refers to compounds of formula I or II endowed with DDX3 inhibitory activity, relative pharmaceutical compositions and their use as antihyperproliferative agents. (I) or (II)

BENZENE SULFONAMIDE DERIVATIVES AND THEIR USE AS RORC MODULATORS

Compounds of the formula la or lb: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, D, E, G, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Palladium-catalyzed intramolecular oxidative coupling involving double C(sp2)-H bonds for the synthesis of annulated biaryl sultams

The palladium-catalyzed intramolecular oxidative coupling described herein involves a double C(sp2)-H bond functionalization in sulfonanilides, providing a workable access to biaryl sultams annulated into a six-membered ring that are otherwise difficult to obtain by literature methods. The other synthetic applications of this protocol including the synthesis of biaryl sultams containing a seven-membered ring and analogous sultones are also presented.

BENZYL SULFONAMIDE DERIVATIVES AS RORC MODULATORS

Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.