99856-72-1

Upstream product

• 69232-47-9 (4-(chlorosulfonyl)phenyl)methylene diacetate 
• 108-24-7 acetic anhydride 
• 70-55-3 toluene-4-sulfonamide 
• 64-19-7 acetic acid 
• 98-59-9 p-toluenesulfonyl chloride 

Downstream Products

• 1261153-02-9 (E)-5-nitro-3-[[4-(sulfamoyl)phenyl]methylene]indolin-2-one 
• 1261153-01-8 (E)-5-bromo-3-[[4-(sulfamoyl)phenyl]methylene]indolin-2-one 
• 1261153-00-7 (E)-6-chloro-3-[[4-(sulfamoyl)phenyl]methylene]indolin-2-one 
• 1261152-99-1 (E)-5-methyl-3-[[4-(sulfamoyl)phenyl]methylene]indolin-2-one 
• 1261152-98-0 (E)-5-chloro-3-[[4-(sulfamoyl)phenyl]methylene]indolin-2-one 
• 1261152-97-9 (E)-5-fluoro-3-[[4-(sulfamoyl)phenyl]methylene]indolin-2-one 
• 1261152-96-8 (E)-3-[[4-(sulfamoyl)phenyl]methylene]indolin-2-one 
• 3240-35-5 4-formyl-benzenesulfonamide 

Relevant academic research and scientific papers

Synthesis and biological evaluation of 3-[4-(amino/methylsulfonyl)phenyl] methylene-indolin-2-one derivatives as novel COX-1/2 and 5-LOX inhibitors

Fourteen new 3-[4-(amino/methylsulfonyl)phenyl]methylene-indolin-2-one derivatives were synthesized. Six compounds displayed potent inhibitory activities against COX-1/2 and 5-LOX with IC50 in the range of 0.10-9.87 μM. Particularly, 10f exhibited well balanced inhibitory action on these enzymes (IC50 = 0.10-0.56 μM). More importantly, 10f and several other compounds had comparable or stronger anti-inflammatory and analgesic activities, but better gastric tolerability in vivo, as compared with darbufelone mesilate and tenidap sodium. Therefore, our findings may aid in the design of new and safe anti-inflammatory reagents for the intervention of painful inflammatory diseases, such as rheumatoid arthritis at clinic.

CRYOPYRIN INHIBITORS FOR PREVENTING AND TREATING INFLAMMATION

Inhibitors that are anti-inflammatory agents are provided, as are methods of using the analogs to inhibit inflammation and prevent or treat diseases and conditions associated with inflammation, such as heart failure and autoimmune diseases.

DERIVATIVES OF PYRAZOLINE, PROCEDURE FOR OBTAINING THEM AND USE THEREOF AS THERAPEUTIC AGENTS

The invention relates to derivatives of general formula (I), and to their pharmaceutically acceptable salts, their stereoisomeric forms, preferably their pure enantiomeric or diastereomeric forms and their racemic forms, or a mixture thereof in any mixture ratio, and their N-oxides and the corresponding solvates or hydrates, to the processes for obtaining said derivatives and to the pharmaceutical compositions which contain them. Said derivatives are useful as anti-inflammatory and analgesic agents. In which R and R1 are different from each other and are selected from H and.