851883-01-7

Upstream product

• 613-92-3 N-hydroxybenzenecarboximidamide 
• 100-47-0 benzonitrile 

Downstream Products

• 1430424-13-7 C₂₁H₂₀ClN₃O₂ 
• 1430424-14-8 C₂₀H₁₉N₃O₂ 
• 1430424-15-9 C₂₁H₂₁N₃O₂ 
• 1430424-16-0 C₂₀H₁₈ClN₃O₂ 
• 1430424-17-1 C₂₀H₁₈ClN₃O₂ 
• 1430424-18-2 C₂₀H₁₈ClN₃O₂ 
• 1430424-19-3 C₂₁H₂₀ClN₃O₂ 
• 1430424-20-6 C₂₁H₂₀BrN₃O₂ 
• 1430424-21-7 C₂₁H₂₀IN₃O₂ 
• 1430424-22-8 C₁₉H₁₈N₄O₂ 
• 1430424-23-9 C₁₈H₁₇N₃O₃ 
• 1430424-24-0 C₁₉H₂₀N₄O₂ 
• 1430424-25-1 C₁₉H₁₈Br₂N₄O₂ 
• 1430424-26-2 C₂₃H₂₂N₄O₂ 

Relevant academic research and scientific papers

Design, synthesis and SAR of piperidyl-oxadiazoles as 11β- hydroxysteroid dehydrogenase 1 inhibitors

The potential roles of 11β-HSD1 inhibitors in metabolic syndrome, T2D and obesity were well established and currently several classes of 11β-HSD1 inhibitors have been developed as promising agents against metabolic diseases. To find potent compounds with good pharmacokinetics, we used the bioisosterism approach, and designed the compound 2 and 3 bearing an 1,2,4-oxadiazole ring to replace the amide group in compound 1. Guided by docking study, we then transformed compound 3 into a potent lead compound 4a by changing sulfonamide group to amide. To elaborate this series of piperidyl-oxadiazole derivatives as human 11β-HSD1 inhibitors, we explored the structure-activity relationship of several parts of the lead compound. Based on their potency toward human 11β-HSD1 two compounds 4h and 4q were advanced to pharmacokinetic study. It was found that 4h and 4q are potent and selective human 11β-HSD1 inhibitors with better pharmacokinetic properties than those of the original piperidine-3-carboxamide compound 1, and suitable for further in vivo preclinical study in primate model.

NOVEL OXADIAZOLE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS

The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q,W, R1 and R2 are defined in the description. Invention compounds are useful in the prevention or treatment of central or p

ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS

The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, Rl and R2 are defined in the description; invention compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.