1256700-77-2

Upstream product

• 33252-63-0 5-(trifluoromethyl)-2(1H)-pyridone 
• 350-30-1 3-chloro-4-fluoronitrobenzene 
• 1365919-82-9 2-chloro-5-trifluoromethyl-pyridine 

Downstream Products

• 1256700-78-3 5-trifluoromenthyl-(1-(4-amino-2-chloro)phenyl)pyridine-2(1H)-one 
• 1256700-71-6 1-(2-chloro-4-((2-(2-hydroxyethoxy)ethyl)amino)-phenyl)-5-(trifluoromethyl) pyridin-2(1H)-one 
• 1256700-69-2 1-(4-(N,N-bis(2-hydroxyethyl)amino)-2-chlorophenyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1256700-68-1 5-trifluoromethyl-(1-(2-chloro-4-(2-hydroxylethyl)amino)phenyl)pyridine-2(1H)-one 
• 1256700-67-0 1-(4-((3-butoxypropyl) amino)-2-chlorophenyl)-5-(trifluoromethyl) pyridin-2(1H)-one 
• 1256700-74-9 1-(2-chloro-4-((2-morpholinoethyl)amino)phenyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1256700-65-8 1-(2-chloro-4-((3-morpholinopropyl)amino)phenyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1256700-73-8 1-(2-chloro-4-((2-(piperidin-1-yl)ethyl)amino)phenyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1256700-72-7 1-(2-chloro-4-((2-(piperazin-1-yl)ethyl)amino)phenyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1256700-70-5 1-(2-chloro-4-(((3-piperidin-1-yl)propyl)amino)phenyl)-5-(trifluoromethyl)pyridin-2(1H)-one hydrochloride 
• 1256700-66-9 1-(2-chloro-4-((3-(piperidin-1-yl)propyl)amino)phenyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1256700-79-4 1-(2-chloro-4-((2-chloroethyl)amino)-phenyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1256700-64-7 1-(2-chloro-4-((3-(4-methylpiperazin-1-yl)propyl)amino)phenyl)-5-(trifluoromethyl)pyridin-2(1H)-one 
• 1256700-76-1 1-(2-chloro-4-((2-(4-(2-hydroxyethyl)piperazin-1-yl)ethyl)amino)phenyl)-5-(trifluoromethyl)pyridin-2(1H)-one 

Relevant academic research and scientific papers

Discovery of 1-(4-((3-(4-methylpiperazin-1-yl)propyl)amino)benzyl)-5-(trifluoromethyl)pyridin-2(1H)-one, an orally active multi-target agent for the treatment of diabetic nephropathy

Oxidative stress, inflammation and fibrosis can cause irreversible damage on cell structure and function of kidney and are key pathological factors in Diabetic Nephropathy (DN). Therefore, multi-target agents are urgently need for the clinical treatment of DN. Using Pirfenidone as a lead compound and based on the previous research, two novel series (5-trifluoromethyl)-2(1H)-pyridone analogs were designed and synthesized. SAR of (5-trifluoromethyl)-2(1H)-pyridone derivatives containing nitrogen heterocyclic ring have been established for in vitro potency. In addition, compound 8, a novel agent that act on multiple targets of anti-DN with IC50 of 90 μM in NIH3T3 cell lines, t1/2 of 4.89 ± 1.33 h in male rats and LD50 > 2000 mg/kg in mice, has been advanced to preclinical studies as an oral treatment for DN.

ANTI-FIBROTIC PYRIDINONES

This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.

Synthesis and structure-activity relationship of 5-substituent-2(1H)- pyridone derivatives as anti-fibrosis agents

Pyridone compounds, such as pirfenidone (PFD) and fluorofenidone (AKF-PD), are multi-target anti-fibrotic agents. Using PFD and AKF-PD as the leading compounds, two series of novel (5-substituent)-2(1H)-pyridone compounds were synthesized with the purpose of maintaining multi-targeting property and overcoming the drawbacks of fast metabolism. These derivatives demonstrated good proliferation inhibiting activity against NIH3T3 cells by MTT assay with AKF-PD as the positive control. Compound 5b exhibited a high potent of anti-fibrosis with a IC50 of 0.08 mmol/L about 34 times of AKF-PD. The SAR of pyridone derivatives as anti-fibrosis agents was also discussed.

PREPARATION METHODS AND USES OF 1-(SUBSTITUTED ARYL)-5-TRIFLUOROMETHYL-2-(1H)-PYRIDONE COMPOUNDS AND THEIR SALTS

A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof.