1301740-78-2Relevant academic research and scientific papers
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
BACE1 inhibitors: A head group scan on a series of amides
Woltering, Thomas J.,Wostl, Wolfgang,Hilpert, Hans,Rogers-Evans, Mark,Pinard, Emmanuel,Mayweg, Alexander,G?bel, Martin,Banner, David W.,Benz, J?rg,Travagli, Massimiliano,Pollastrini, Martina,Marconi, Guido,Gabellieri, Emanuele,Guba, Wolfgang,Mauser, Harald,Andreini, Matteo,Jacobsen, Helmut,Power, Eoin,Narquizian, Robert
, p. 4239 - 4243 (2013/07/26)
A series of amides bearing a variety of amidine head groups was investigated as BACE1 inhibitors with respect to inhibitory activity in a BACE1 enzyme as well as a cell-based assay. Determination of their basicity as well as their properties as substrates
1,3-OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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Page/Page column 96, (2012/12/13)
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 inv
1,3-OXAZINES AS BACE 1 AND/OR BACE2 INHIBITORS
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Page/Page column 52, (2012/12/13)
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 inv
AMINOTHIAZINE OR AMINOOXAZINE DERIVATIVE HAVING AMINO LINKER
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, (2012/09/25)
The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-2 proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3, R4, R5, X, L1, L2, A, ring B and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
OXAZINE DERIVATIVES
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, (2012/10/08)
The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-β proteins. A compound of the formula (I): wherein R1, Rs
