1398112-69-0

Upstream product

• 1398113-03-5 (4R)-4-(5-bromo-2-fluorophenyl)-4-methyl-1,2,3-oxathiazolidine-3-carboxylic acid 2,2-dioxide 1,1-dimethylethyl ester 
• 1383742-04-8 tert-butyl N-[(1R)-1-(5-bromo-2-fluorophenyl)-2-hydroxy-1-methylethyl]carbamate 
• 1228571-14-9 (2R)-2-amino-2-(5-bromo-2-fluorophenyl)propan-1-ol 
• 1398113-22-8 C₁₄H₁₃BrFN₃ 
• 1398113-21-7 (R)-3-(5-bromo-2-fluorophenyl)-1-methoxy-3-methyl-3,4-dihydropyrrolo[1,2-a]pyrazine 
• 1398113-20-6 (R)-3-(5-bromo-2-fluorophenyl)-3-methyl-3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one 
• 1398113-19-3 C₁₆H₁₈BrFN₂O₂ 
• 2199-43-1 ethyl 1H-pyrrole-2-carboxylate 
• 1398113-23-9 (R)-3-(5-amino-2-fluorophenyl)-3-methyl-3,4-dihydropyrrolo[1,2-a]pyrazin-1-amine 
• 53234-55-2 5-cyano-pyridine-2-carboxylic acid 

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.

3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)

The present invention relates to novel 3,4-dihydro-pyrrolo[l,2-a]pyrazin-1-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.