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US 2013/0172331 A1Published application
Novel oxazine derivatives and their use in the treatment of disease
AssigneeNovartis AG
InventorsRainer Martin LUEOEND, Rainer MACHAUER, Heinrich RUEEGER, Siem Jacob VEENSTRA
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Abstract
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.
Claims14
A compound of formula (I), or a pharmaceutically acceptable salt thereof,
- wherein
- R1 and R2 are independently hydrogen or halogen;
- R3 and R4 are independently hydrogen or C1-3alkyl;
- or R3 and R4 taken together are cyclopropyl;
- or R1 and R4 are hydrogen and R2 and R3 taken together are —CH2—O—CH2—;
- R5 is C1-3alkyl, halogen-C1-3alkyl or C1-3alkoxy-C1-3alkyl;
- and
- R6 is phenyl or a 5- or 6-membered monocyclic heteroaryl comprising 1, 2, 3 or 4 heteroatoms independently selected from N, O and S, and wherein said phenyl or heteroaryl is optionally substituted by 1, 2, 3 or 4 substituents independently selected from halogen, cyano, amino, hydroxy, C1-4alkyl, halogen-C1-4alkyl, halogen-C1-4alkylthio, halogen-C1-4alkoxy, C1-4alkoxy, C1-4alkoxy-C1-4alkyl, C1-4alkoxy-C1-4alkoxy, C1-4alkoxy-C1-4alkylthio, C1-4alkoxy-C2-4alkenyl, C1-4alkoxy-C2-4alkynyl, hydroxy-C1-4alkyl, hydroxy-C2-4alkenyl and hydroxy-C2-4alkynyl.
5 more elements
Dependencies are inferred from the claim text.