- Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360
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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
- 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
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p. 4677 - 4696
(2021/05/06)
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- NOVEL OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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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.
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- 1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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The present invention provides 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 present
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Page/Page column 37; 38
(2012/08/08)
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- 1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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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
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Page/Page column 58-59
(2012/08/07)
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- 1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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The present invention relates to 1,4 Oxazines of formula I having BACE 1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the prese
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Page/Page column 32-33
(2012/07/28)
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- 3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINE DERIVATIVES
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The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[l,4]oxazine derivatives of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active
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Page/Page column 81
(2011/04/13)
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- 3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINES
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The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[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. T
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Page/Page column 36-37
(2011/04/14)
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