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US 11,633,403 B2Granted
6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes
AssigneeSprint Bioscience AB
InventorsJessica Martinsson, Martin Andersson, Johan Lindström, Rickard Forsblom, Fredrik Rahm, Tobias Ginman, Jenny Viklund
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Abstract
The invention provides novel 6-aryl or 6-heteroaryl 4-morpholin-4-yl-pyhdine-2-one compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, diabetes, inflammatory diseases, neurodegenerative disorders, cardiovascular disorders and viral infections; wherein R1, R2, R3 and R4 are as defined in the specification.
Claims20
A process for preparing a compound of formula (I)
- and pharmaceutically acceptable salts, tautomers, or stereoisomers thereof, wherein
- R1 is aryl or heteroaryl, said aryl and said heteroaryl being mono- or bicyclic and optionally substituted with one or more of R5, R6, R7, and R8;
- R2, R3, and R4 are independently selected from hydrogen, C1-C3haloalkyl, and C1-C3alkyl;
- R5, R6, R7, and R8 are independently selected from halogen, C1-C6alkyl, C1-C6alkoxy, C1-C6haloalkyl, amino, —NHSO2R9, hydroxy, phenyl, and a monocyclic heteroaryl;
- and
- R9 is C1-C6haloalkyl or C1-C3alkyl;
- the process comprising:
- reacting a compound of formula (III):
- with a deprotecting agent to produce the compound of formula (I),
- optionally in the presence of R2-I when R2 is C1-C3haloalkyl or C1-C3alkyl;
- wherein
- R10 is F, OCH3, OC(CH3)3, or OSiR′R″R′″ and R′, R″, and R′″ are independently aryl or alkyl;
- and
- R1, R3, and R4 are defined as above for the compound of formula (I).
11 more elements
Dependencies are inferred from the claim text.