1586755-10-3

Basic information

• Product Name: 7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-4-((2-(trifluoromethoxy)-phenyl)amino)-1,5-naphthyridine-3-carboxylic acid
• CAS NO: 1586755-10-3
• Molecular Weight: 474.396
• Mol File: 1586755-10-3.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: 7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-4-((2-(trifluoromethoxy)-phenyl)amino)-1,5-naphthyridine-3-carboxylic acid(CAS DataBase Reference)
• NIST Chemistry Reference: 7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-4-((2-(trifluoromethoxy)-phenyl)amino)-1,5-naphthyridine-3-carboxylic acid(1586755-10-3)
• EPA Substance Registry System: 7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-4-((2-(trifluoromethoxy)-phenyl)amino)-1,5-naphthyridine-3-carboxylic acid(1586755-10-3)

Safety Data

• Hazardous Substances Data: 1586755-10-3(Hazardous Substances Data)

Upstream product

• 1586755-03-4 ethyl 7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-4-oxo-1,4-dihydro-1,5-naphthyridine-3-carboxylate 
• 1586755-05-6 ethyl 7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-4-((2-(trifluoromethoxy)phenyl)amino)-1,5-naphthyridine-3-carboxylate 
• 16114-47-9 3,5-dimethylisoxazole-4-boronic acid 
• 53242-18-5 5-bromo-6-methoxypyridin-3-amine 
• 1586755-24-9 diethyl 2-(((5-(3,5-dimethylisoxazol-4-yl)-6-methoxypyridin-3-yl)amino)methylene)malonate 
• 1586755-25-0 ethyl 4-chloro-7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-1,5-naphthyridine-3-carboxylate 
• 1586755-02-3 5-(3,5-dimethylisoxazol-4-yl)-6-methoxypyridin-3-amine 

Downstream Products

• 1586755-16-9 7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-4-((2-(trifluoromethoxy)-phenyl)amino)-1,5-naphthyridine-3-carboxamide 
• 1300736-27-9 7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-(2-(trifluoromethoxy)-phenyl)-1H-imidazo[4,5-c][1,5]naphthyridin-2(3H)-one 

Relevant articles and documents

Naphthyridines as novel bet family bromodomain inhibitors

Bromodomains (BRDs) are small protein domains found in a variety of proteins that recognize and bind to acetylated histone tails. This binding affects chromatin structure and facilitates the localisation of transcriptional complexes to specific genes, thereby regulating epigenetically controlled processes including gene transcription and mRNA elongation. Inhibitors of the bromodomain and extra-terminal (BET) proteins BRD2-4 and T, which prevent bromodomain binding to acetyl-modified histone tails, have shown therapeutic promise in several diseases. We report here the discovery of 1,5-naphthyridine derivatives as potent inhibitors of the BET bromodomain family with good cell activity and oral pharmacokinetic parameters. X-ray crystal structures of naphthyridine isomers have been solved and quantum mechanical calculations have been used to explain the higher affinity of the 1,5-isomer over the others. The best compounds were progressed in a mouse model of inflammation and exhibited dose-dependent anti-inflammatory pharmacology.