1266784-24-0Relevant articles and documents
Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360
Rueeger, Heinrich,Lueoend, Rainer,Machauer, Rainer,Veenstra, Siem J.,Holzer, Philipp,Hurth, Konstanze,Voegtle, Markus,Frederiksen, Mathias,Rondeau, Jean-Michel,Tintelnot-Blomley, Marina,Jacobson, Laura H.,Staufenbiel, Matthias,Laue, Grit,Neumann, Ulf
supporting information, p. 4677 - 4696 (2021/05/06)
Starting from lead compound 4, the 1,4-oxazine headgroup was optimized to improve potency and brain penetration. Focusing at the 6-position of the 5-amino-1,4-oxazine, the insertion of a Me and a CF3 group delivered an excellent pharmacological profile wi
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 (2015/11/09)
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-AMINO[1,4]THIAZINES AS BACE 1 INHIBITORS
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, (2014/01/07)
The present invention provides a compound of formula I having BACE1 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.