1443259-41-3Relevant academic research and scientific papers
1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads
Rombouts, Frederik J. R.,Tresadern, Gary,Delgado, Oscar,Martínez-Lamenca, Carolina,Van Gool, Michiel,García-Molina, Aránzazu,Alonso De Diego, Sergio A.,Oehlrich, Daniel,Prokopcova, Hana,Alonso, José Manuel,Austin, Nigel,Borghys, Herman,Van Brandt, Sven,Surkyn, Michel,De Cleyn, Michel,Vos, Ann,Alexander, Richard,Macdonald, Gregor,Moechars, Dieder,Gijsen, Harrie,Trabanco, Andrés A.
, p. 8216 - 8235 (2015)
1,4-Oxazines are presented, which show good in vitro inhibition in enzymatic and cellular BACE1 assays. We describe lead optimization focused on reducing the amidine pKa while optimizing interactions in the BACE1 active site. Our strategy permi
5-(3-AMINOPHENYL)-5-ALKYL-5,6-DIHYDRO-2H-[1,4]OXAZIN-3-AMINE DERIVATIVES
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Paragraph 0109; 0110, (2015/01/06)
The present invention relates to novel 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also direct
5-(3-AMINOPHENYL)-5-ALKYL-5,6-DIHYDRO-2H-[1,4]OXAZIN-3-AMINE DERIVATIVES
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Page/Page column 27; 28, (2013/06/27)
The present invention relates to novel 5-(3-aminophenyl)-5-alkyl-5,6-dihydro- 2H-[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta- site amyloid cleaving enzyme, BACE, BACE 1, Asp2, or memapsin2. The invention is also dir
