1183013-69-5Relevant academic research and scientific papers
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
5-ARYL-1-IMINO-1-OXO-[1,2,4]THIADIAZINES
-
, (2015/07/07)
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
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
3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND OTHER FORMS OF DEMENTIA
-
Paragraph 0070; 0071, (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
4,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
-
Paragraph 0070; 0071, (2013/07/31)
The present invention relates to novel 4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-yl-amine 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 compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.
5-AMINO[1,4]THIAZINES AS BACE 1 INHIBITORS
-
Page/Page column 35; 36, (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.
NOVEL OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
-
Page/Page column 49-50, (2013/04/25)
The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
-
, (2012/08/07)
The present invention relates to 1,4 Oxazines of formula (I): having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the pre
3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATMENT OF ALZHEIMER?S DISEASE AND OTHER FORMS OF DEMENTIA
-
Page/Page column 19, (2012/01/14)
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
4,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
-
Page/Page column 25, (2012/04/10)
The present invention relates to novel 4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-yl- aminederivativesas inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretaseis involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associatedwith stroke, dementia associated with Parkinson's disease or dementia associated with beta- amyloid.
