1301740-77-1

Upstream product

• 506-68-3 bromocyane 
• 1075230-65-7 (S)-3-amino-3-(2-fluoro-5-nitrophenyl)butan-1-ol 
• 79110-05-7 1-(2-fluoro-5-nitrophenyl)ethanone 
• 1213413-42-3 (S)-3-amino-3-(2-fluoro-5-nitro-phenyl)-butyric acid methyl ester 
• 1075230-62-4 (R)-2-methylpropane-2-sulfinic acid [1-(2-fluoro-5-nitrophenyl)-(E)-ethylidene]amide 
• 1346145-61-6 (R)-2-methyl-propane-2-sulfinic acid [(S)-1-(2-fluoro-5-nitro-phenyl)-3-hydroxy-1-methyl-propyl]-amide 
• 1336669-71-6 (S)-3-amino-3-(2-fluoro-5-nitrophenyl)butan-1-ol 
• 1432511-52-8 (S)-ethyl 3-((R)-1,1-dimethylethylsulfinamido)-3-(2-fluoro-5-nitrophenyl)butanoate 
• 1301740-76-0 C₁₈H₁₆FN₃O₄ 
• 1301740-75-9 C₁₈H₁₈FN₃O₄S 
• 1301740-70-4 (S)-3-amino-3-(2-fluoro-5-nitrophenyl)butan-1-ol hydrochloride 

Downstream Products

• 1310374-16-3 [(S)-4-(2-fluoro-5-nitro-phenyl)-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-yl]-carbamic acid tert-butyl ester 
• 1310374-19-6 [(S)-4-(5-amino-2-fluoro-phenyl)-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-yl]-carbamic acid tert-butyl ester 
• 1310373-42-2 (S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-oxazin-4-yl)-4-fluorophenyl)-3,5-dichloropicolinamide 
• 1301740-78-2 (S)-4-(5-amino-2-fluorophenyl)-4-methyl-5,6-dihydro-4H-1,3-oxazin-2-amine 
• 1310373-43-3 (S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-oxazin-4-yl)-4-fluorophenyl)-5-chloropicolinamide 
• 1310373-67-1 5-cyano-pyridine-2-carboxylic acid [3-((S)-2-amino-4-methyl-5,6-dihydro-4H-[1,3]oxazin-4-yl)-4-fluoro-phenyl]-amide 

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

BACE1 inhibitors: A head group scan on a series of amides

A series of amides bearing a variety of amidine head groups was investigated as BACE1 inhibitors with respect to inhibitory activity in a BACE1 enzyme as well as a cell-based assay. Determination of their basicity as well as their properties as substrates

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

The present invention provides compounds 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 inv

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

The present invention provides compounds 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 inv

AMINOTHIAZINE OR AMINOOXAZINE DERIVATIVE HAVING AMINO LINKER

The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-2 proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3, R4, R5, X, L1, L2, A, ring B and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.

OXAZINE DERIVATIVES

The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-β proteins. A compound of the formula (I): wherein R1, Rs

AMINO OXAZINE DERIVATIVES

This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula wherein R1 to R5 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.

AMINO OXAZINE DERIVATIVES

This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula (I) wherein R1 to R5 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.