1313525-80-2

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 1600513-16-3 (R)-2-amino-2-(5-bromo-2-fluorophenyl)propan-1-ol HCl 
• 1266784-18-2 rac-2-amino-2-(5-bromo-2-fluoro-phenyl)-propionic acid methyl ester 
• 1374765-83-9 2-amino-2-(5-bromo-2-fluorophenyl)propanoic acid hydrochloride 
• 1350523-51-1 rac-2-amino-2-(5-bromo-2-fluoro-phenyl)-propionitrile 
• 1266784-23-9 (RS)-2-amino-2-(5-bromo-2-fluoro-phenyl)-propionic acid 
• 198477-89-3 1-(5-bromo-2-fluorophenyl)ethan-1-one 
• 1266784-24-0 (RS)-2-amino-2-(5-bromo-2-fluoro-phenyl)-propan-1-ol 

Downstream Products

• 1313525-81-3 (R)-tert-butyl 4-(5-bromo-2-fluorophenyl)-4-methyl-1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide 
• 1313525-82-4 rac-[1-(5-bromo-2-fluoro-phenyl)-1-methyl-2-methyl-amino-ethyl]-carbamic acid tert-butyl ester 
• 1313525-84-6 rac-5-(5-bromo-2-fluoro-phenyl)-1,5-dimethyl-piperazine-2,3-dione 
• 1313525-86-8 5-(5-bromo-2-fluorophenyl)-1,5-dimethyl-3-thioxopiperazin-2-one 
• 1313525-88-0 rac-3-amino-5-(5-bromo-2-fluoro-phenyl)-1,5-dimethyl-5,6-dihydro-1H-pyrazin-2-one 
• 1600510-87-9 (3R,6R)-5-amino-6-fluoro-3-(2-fluoro-5-((2-(trifluoromethyl)pyrido[3,4-b]pyrazin-5-yl)amino)phenyl)-3,6-dimethyl-3,6-dihydro-2H-1,4-thiazine 1,1-dioxide 
• 1600511-48-5 tert-butyl ((2R)-2-(5-bromo-2-fluorophenyl)-1-((1-cyanoethyl)sulfonyl)propan-2-yl)carbamate 
• 1600508-33-5 (3R,6R)-5-Amino-3-(5-((3-chloro-1,7-naphthyridin-8-yl)amino)-2-fluorophenyl)-6-fluoro-3,6-dimethyl-3,6-dihydro-2H-1,4-thiazine 1,1-dioxide 
• 1600508-34-6 (3R,6R)-5-Amino-3-((5-(7-chloropyrido[3,2-d]pyrimidin-4-yl)amino)-2-fluorophenyl)-6-fluoro-3,6-dimethyl-3,6-dihydro-2H-1,4-thiazine 1,1-dioxide 
• 1600508-36-8 N-(3-((3R,6R)-5-amino-6-fluoro-3,6-dimethyl-1,1-dioxido-3,6-dihydro-2H-1,4-thiazin-3-yl)-4-fluorophenyl)-7-methoxypyrido[3,2-d]pyrimidin-4-amine 
• 1600508-39-1 4-((3-((3R,6R)-5-Amino-6-fluoro-3,6-dimethyl-1,1-dioxido-3,6-dihydro-2H-1,4-thiazin-3-yl)-4-fluorophenyl)amino)pyrido[3,2-d]pyrimidine-7-carbonitrile 
• 1600511-49-6 tert-butyl ((2R,5R)-5-(5-amino-2-fluorophenyl)-2-fluoro-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2H-1,4-thiazin-3-yl)carbamate 
• 1600511-33-8 (R)-S-(2-(5-Bromo-2-fluorophenyl)-2-((tert-butoxy carbonyl)amino)propyl) ethanethioate 
• 1600507-35-4 N-(3-((3R)-5-amino-3,6-dimethyl-1,1-dioxido-3,6-dihydro-2H-1,4-thiazin-3-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide 

Relevant academic research and scientific papers

AMINO-DIHYDROTHIAZINE AND AMINO-DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE

The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.

3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND OTHER FORMS OF DEMENTIA

The present invention relates to novel 3-amino-5,6-dihydro-1H-pyrazin-2-one 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 com

3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATMENT OF ALZHEIMER?S DISEASE AND OTHER FORMS OF DEMENTIA

The present invention relates to novel 3-amino-5,6-dihydro-1H-pyrazin-2-one 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 com

PYRAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

The invention relates to novel heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.

Rational design and synthesis of aminopiperazinones as β-secretase (BACE) inhibitors

Aminopiperazinone inhibitors of BACE were identified by rational design. Structure based design guided idea prioritization and initial racemic hit 18a showed good activity. Modification in decoration and chiral separation resulted in the 40 nM inhibitor,