1600511-48-5

Upstream product

• 1313525-81-3 (R)-tert-butyl 4-(5-bromo-2-fluorophenyl)-4-methyl-1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide 
• 1600511-33-8 (R)-S-(2-(5-Bromo-2-fluorophenyl)-2-((tert-butoxy carbonyl)amino)propyl) ethanethioate 
• 19481-82-4 2-bromopropionitrile 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1313525-80-2 rac-[1-(5-bromo-2-fluoro-phenyl)-2-hydroxy-1-methyl-ethyl]-carbamic acid tert-butyl ester 
• 1600513-16-3 (R)-2-amino-2-(5-bromo-2-fluorophenyl)propan-1-ol HCl 
• 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 
• 1600511-35-0 tert-butyl ((2R)-2-(5-bromo-2-fluorophenyl)-1-((1-cyanoethyl)thio)propan-2-yl)carbamate 
• 1600511-39-4 R,S-5-Amino-3-(5-bromo-2-fluorophenyl)-3,6,6-trimethyl-3,6-dihydro-2H-1,4-thiazine 1,1-dioxide 

Downstream Products

• 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 
• 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 
• 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 
• 1600511-97-4 tert-butyl ((5R)-5-(5-amino-2-fluorophenyl)-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2H-1,4-thiazin-3-yl)carbamate 
• 1600507-55-8 (3R,6R)-5-Amino-3-(5-amino-2-fluorophenyl)-6-fluoro-3,6-dimethyl-3,6-dihydro-2H-1,4-thiazine 1,1-dioxide 
• 182181-19-7 6-chloroimidazo[1,2-a]pyridine-2-carboxylic acid 
• 1600506-36-2 (3R,6R)-5-Amino-3-(5-bromo-2-fluorophenyl)-6-fluoro-3,6-dimethyl-3,6-dihydro-2H-1,4-thiazine 1,1-dioxide 

Relevant academic research and scientific papers

BICYCLIC HETEROCYCLE DERIVATIVES HAVING SELECTIVE BACE1 INHIBITORY ACTIVITY

The present invention provides a compound which has an effect of inhibiting amyloid β production, especially an effect of inhibiting selective BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins. A compound of the formula (IA) or the like, wherein -A1- is alkylene optionally substituted with one or more halogen; R2 is substituted or unsubstituted alkyl or the like; R3 and R4 are each independently a hydrogen atom, halogen, alkyl or haloalkyl or the like; R5 is a hydrogen atom or halogen; A4 is N or CR6 wherein R6 is a hydrogen atom, halogen, or substituted or unsubstituted alkyl; A5 is NR7 or CR8R9; A6 is CR18 or N; R18 is a hydrogen atom; R7 is substituted or unsubstituted alkyl; R8 and R9 are each independently a hydrogen atom, halogen, alkyl or haloalkyl or the like; and Ring B is bicyclic ring; or a pharmaceutically acceptable salt thereof.

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.