- 2-AMINO-6-METHYL-4,4a,5,6-TETRAHYDROPYRANO[3,4-d][1,3]THIAZIN-8a(8H)-YL-1,3-THIAZOL-4-YL AMIDES
-
The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula (I), and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
- -
-
Page/Page column 77; 81; 82
(2015/11/17)
-
- β-secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease
-
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
- 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)
-
- 1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
-
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
- -
-
-
- 1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS
-
This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/
- -
-
-
- 1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS
-
This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/
- -
-
-
- 1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
-
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
- -
-
-
- 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS
-
The present invention relates to 1,4-Oxazepines 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 pres
- -
-
-
- 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS
-
The present invention relates to 1,4-Oxazepines 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 pres
- -
-
-
- 1,3-OXAZINES AS BACE 1 AND/OR BACE2 INHIBITORS
-
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 BACE1 AND/OR BACE2 INHIBITORS
-
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 BACE1 AND/OR BACE2 INHIBITORS
-
The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines 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.
- -
-
-
- 1,3 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
-
The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines 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.
- -
-
-
- 2-AMINO-5,5-DIFLUORO-5,6-DIHYDRO-4H-[1,3]OXAZIN-4-YL)-PHENYL]-AMIDES
-
The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutical
- -
-
-
- 2-AMINO-5, 5-DIFLUORO-5, 6-DIHYDRO-4H-OXAZINES AS BACE 1 AND/OR BACE 2 INHIBITORS
-
The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)- phenyl]-amide derivatives of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as
- -
-
-
- 2,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS
-
This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments fo
- -
-
-
- 2,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS
-
This invention relates to compounds of the formula (I), wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as 5 medicam
- -
-
-