1266784-18-2Relevant articles and documents
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.
3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND OTHER FORMS OF DEMENTIA
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Paragraph 0137; 0138, (2013/05/08)
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