1402413-06-2

Upstream product

• 1402412-91-2 (2S,3S)-ethyl 3-((R)-1,1-dimethylethylsulfinamido)-2,4-difluoro-3-(2-fluorophenyl)butanoate 
• 218771-68-7 1-(2-fluorophenyl)-2-hydroxyethan-1-one 
• 1402412-84-3 2-fluoro-1-(2-fluorophenyl)ethan-1-one 
• 1415914-97-4 (R)-2-methyl-propane-2-sulfinic acid [2-fluoro-1-(2-fluoro-phenyl)-eth-(E)-ylidene]-amide 

Downstream Products

• 1402413-24-4 (4R,5R)-5-fluoro-4-(2-fluoro-5-nitrophenyl)-4-(fluoromethyl)-5,6-dihydro-4H-1,3-oxazin-2-amine 
• 1402413-31-3 (4R,5S)-4-(5-amino-2-fluorophenyl)-5-fluoro-4-(fluoromethyl)-5,6-dihydro-4H-1,3-oxazin-2-amine 
• 1402413-14-2 (4R,5R)-5-fluoro-4-(fluoromethyl)-4-(2-fluorophenyl)-5,6-dihydro-4H-1,3-oxazin-2-amine 

Relevant academic research and scientific papers

β-secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease

An extensive fluorine scan of 1,3-oxazines revealed the power of fluorine(s) to lower the pKa and thereby dramatically change the pharmacological profile of this class of BACE1 inhibitors. The CF3 substituted oxazine 89, a potent and

1,3-OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS

The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

1,3 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS

The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.