Heteroaryl benzamide derivatives for use as glk activators in the treatment of diabetes
AssigneeAstraZeneca AB
InventorsDarren MCKERRECHER, Kurt Gordon Pike, Michael James Waring
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Abstract
Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
Claims10
1-16. (canceled)
The compound 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-2-hydroxy-1-methylethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide or a salt thereof.
A pharmaceutical composition comprising the compound 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-2-hydroxy-1-methylethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide or a pharmaceutically-acceptable salt thereof, together with a pharmaceutically acceptable diluent or carrier.
A method of treating GLK mediated diseases by administering an effective amount of the compound 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-2-hydroxy-1-methylethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide or a pharmaceutically-acceptable salt thereof, to a mammal in need of such treatment.
A method for the combined treatment of obesity and diabetes comprising administering an effective amount of the compound 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-2-hydroxy-1-methylethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide or a pharmaceutically-acceptable salt thereof, to a mammal in need of such treatment.
A process for the preparation of the compound 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-2-hydroxy-1-methylethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide or a salt thereof comprising reacting 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-[((1S)-2-{[(1,1-dimethylethyl)(dimethyl)silyl]oxy}-1-methylethyl)oxy]-N-(5-methylpyrazin-2-yl)benzamide with an acid to form 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-2-hydroxy-1-methylethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide and thereafter optionally forming a salt thereof.
A pharmaceutical composition comprising:
- the compound 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-2-hydroxy-1-methylethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide or a pharmaceutically-acceptable salt thereof;
- one or more substances for the treatment of diabetes and/or obesity;
- and
- a pharmaceutically acceptable diluent or carrier.
Dependencies are inferred from the claim text.