120739-64-2

Upstream product

• 500-22-1 3-pyridinecarboxaldehyde 
• 75-04-7 ethylamine 
• 557-66-4 ethanamine hydrochloride 

Downstream Products

• 1321468-61-4 N-ethyl-N-(3-pyridylmethyl)-2-(8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide 
• 1321468-64-7 N-ethyl-N-(3-pyridylmethyl)-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide 
• 1321468-54-5 ethyl 4-(2-(N-ethyl,N-3-pyridylmethylamino)-2-oxoethylamino)2-phenylpyrimidine-5-carboxylate 
• 1321468-58-9 4-2-(N-ethyl,N-3-pyridylmethylamino)-2-oxoethylamino-2-phenylpyrimidine-5-carboxylic acid 

Relevant academic research and scientific papers

2-ARYL IMIDAZO[1,2-A]PYRIDINE-3-ACETAMIDE DERIVATIVES, PREPARATION METHODS AND USE THEREOF

Disclosed are 2-arylimidazo[1,2-a]pyridine-3-acetamide derivatives represented by formula I, their tautomer, racemate or optical isomer, their pharmaceutically acceptable salt, or their solvates, wherein R1, R2, R3 and R4 are defined as in the specification. Preparation methods of said compounds and use of said compounds in treating and/or preventing central nervous system disease associated with TSPO functional disorder

Synthesis and evaluation of novel carbon-11 labeled oxopurine analogues for positron emission tomography imaging of translocator protein (18 kDa) in peripheral organs

To develop a PET ligand for imaging TSPO in peripheral organs, we designed three novel oxopurine analogues [11C]3a-c (LogD: 1.81-2.17) by introducing a pyridine ring in place of a benzene ring in the lead compound [11C]2 (LogD: 3.48). The desmethyl precursors 10 for radiosynthesis were synthesized by reacting glycine 7 with picolylamines 4, followed by hydrolysis and by Curtius rearrangement with diphenylphosphoryl azide. Methylation of 10a-c with methyl iodide produced unlabeled compounds 3a-c. The radiosynthesis of [11C]3a-c was performed by reacting 10a-c with [11C]methyl iodide. Compounds 3a-c displayed high or moderate in vitro binding affinities (Ki: 5-40 nM) for TSPO. PET with [ 11C]3a-c in rats showed high uptake in the lung, heart, and kidney, which are organs with high TSPO expression. Metabolite analysis with [ 11C]3a showed that radioactivity in these organs mainly corresponded with unchanged [11C]3a. PET with [11C]3a using a rat model of lung inflammation showed a significant signal in the lipopolysaccharide- treated lung.

5-ALKYLOXY-INDOLIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPY

The present invention relates to derivatives of 5-alkyloxy-indolin-2-one, their method of production and their therapeutic applications. These novel derivatives have affinity and selectivity for the V2 receptors of vasopressin (“V2 receptors”) and can therefore constitute active principles of pharmaceutical compositions.