1397683-45-2

Upstream product

• 1397683-93-0 C₁₄H₁₈N₂O₆S 
• 1270385-54-0 rac-2-amino-2-(3-nitro-phenyl)-propan-1-ol 
• 1397683-40-7 3-bromo-6-methyl-6-(3-nitrophenyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one 
• 1397683-47-4 ethyl 4-bromo-1-(2-((tert-butoxycarbonyl)amino)-2-(3-nitrophenyl)propyl)-1H-pyrazole-5-carboxylate 
• 1397683-35-0 t-butyl (1-(4-bromo-1H-pyrazol-1-yl)-2-(3-nitrophenyl)propan-2-yl)carbamate 
• 1397683-33-8 tert-butyl 4-methyl-4-(3-nitrophenyl)-1,2,3-oxathiazolidine-3-carboxylate-2,2-dioxide 
• 1397683-43-0 3-bromo-6-methyl-6-(3-nitrophenyl)-6,7-dihydropyrazolo[1,5-a]pyrazine-4(5H)-thione 

Downstream Products

• 1397683-46-3 rac-6-(3-amino-phenyl)-6-methyl-6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine 
• 1397683-44-1 6-(3-aminophenyl)-6-methyl-6,7-dihydropyrazolo[1,5-a]pyrazin-4-amine 
• 1397683-08-7 rac-5-cyano-pyridine-2-carboxylic acid[3-(4-amino-6-methyl-6,7-dihydro-pyrazolo[1,5-a]pyrazin-6-yl)-phenyl]-amide 

Relevant academic research and scientific papers

Evaluation of a Series of β-Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads

Despite several years of research, only a handful of β-secretase (BACE) 1 inhibitors have entered clinical trials as potential therapeutics against Alzheimer's disease. The intrinsic basic nature of low molecular weight, amidine-containing BACE 1 inhibitors makes them far from optimal as central nervous system drugs. Herein we present a set of novel heteroaryl-fused piperazine amidine inhibitors designed to lower the basicity of the key, enzyme binding, amidine functionality. This study resulted in the identification of highly potent (IC50 ≤ 10 nM), permeable lead compounds with a reduced propensity to suffer from P-glycoprotein-mediated efflux.

6,7-DIHYDRO-PYRAZOLO[1,5-A]PYRAZIN-4-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)

The present invention relates to novel 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-yl-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACEl, Asp2, or memapsin2. The invention is also directed to pharmaceu