1283075-60-4

Upstream product

• 5049-61-6 2-Aminopyrazine 
• 1663-67-8 malonoyl dichloride 
• 131543-46-9 Glyoxal 
• 24484-99-9 4,6-dichloropyridine-2,3-diamine 

Downstream Products

• 1398057-29-8 8-chloro-6-(2-fluoro-phenyl)-pyrido[2,3-b]pyrazine 
• 1398056-96-6 [6-(2-fluoro-phenyl)-pyrido[2,3-b]pyrazin-8-yl]-pyridin-4-yl-amine 
• 1398057-31-2 [6-(2-fluorophenyl)pyrido[2,3-b]pyrazin-8-yl]-boronic acid 
• 1398057-34-5 6-(2-fluoro-phenyl)-8-(6-oxy-[2,6]naphthyridin-1-yl)-pyrido[2,3-b]pyrazine 
• 1398056-99-9 5-[6-(2-fluoro-phenyl)-pyrido[2,3-b]pyrazin-8-yl]-[2,6]naphthyridin-1-ylamine 
• 1398057-10-7 C₂₀H₁₂FN₅ 
• 1398057-18-5 6-(2-fluoro-phenyl)-8-[5-(1-methyl-1H-pyrazol-4-yl)-pyridin-3-yl]-pyrido[2,3-b]pyrazine 
• 1398057-36-7 4-(4-{5-[6-(2-fluoro-phenyl)-pyrido[2,3-b]pyrazin-8-yl]-pyridin-3-yl}-pyrazol-1-yl)-piperidine-1-carboxylic acid tert-butyl ester 
• 1398057-16-3 6-(2-fluoro-phenyl)-8-{5-[1-(1-methyl-piperidin-4-yl)-1H-pyrazol-4-yl]-pyridin-3-yl}-pyrido[2,3-b]pyrazine 
• 1613289-32-9 8-chloro-5-methylpyrido[2,3-b]pyrazin-6(5H)-one 

Relevant academic research and scientific papers

4-Aminoquinolone piperidine amides: Noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity

4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome sequencing of mutants raised against AQs, identified decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1) as the primary target responsible for the antitubercular activity. Mass spectrometry and enzyme kinetic studies indicated that AQs are noncovalent, reversible inhibitors of DprE1 with slow on rates and long residence times of ～100 min on the enzyme. In general, AQs have excellent leadlike properties and good in vitro secondary pharmacology profile. Although the scaffold started off as a single active compound with moderate potency from the whole cell screen, structure-activity relationship optimization of the scaffold led to compounds with potent DprE1 inhibition (IC50 10 nM) along with potent cellular activity (MIC = 60 nM) against Mtb.

PYRIDO [2, 3 - B] PYRAZINE DERIVATIVES AND THEIR THERAPEUTICAL USES

The present invention relates to novel pyrido[2,3-b]pyrazine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.