1415915-01-3Relevant academic research and scientific papers
HALOGEN-ALKYL-1,3 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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Page/Page column, (2014/04/03)
The present invention provides compounds 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 invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
β-secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease
Hilpert, Hans,Guba, Wolfgang,Woltering, Thomas J.,Wostl, Wolfgang,Pinard, Emmanuel,Mauser, Harald,Mayweg, Alexander V.,Rogers-Evans, Mark,Humm, Roland,Krummenacher, Daniela,Muser, Thorsten,Schnider, Christian,Jacobsen, Helmut,Ozmen, Laurence,Bergadano, Alessandra,Banner, David W.,Hochstrasser, Remo,Kuglstatter, Andreas,David-Pierson, Pascale,Fischer, Holger,Polara, Alessandra,Narquizian, Robert
, p. 3980 - 3995 (2013/06/27)
An extensive fluorine scan of 1,3-oxazines revealed the power of fluorine(s) to lower the pKa and thereby dramatically change the pharmacological profile of this class of BACE1 inhibitors. The CF3 substituted oxazine 89, a potent and
HALOGEN-ALKYL-1,3 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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Page/Page column 38, (2013/02/27)
The present invention provides compounds 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 i
