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US 7,396,834 B2Granted
4(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders
AssigneeAstraZeneca AB
InventorsWilliam Brown, Andrew Griffin, Niklas Plobeck, Christopher Walpole
Life of this patent
Estimating the term…
Abstract
Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
Claims9
A compound of formula I, pharmaceutically acceptable salts thereof, or mixtures thereof:
- wherein
- R1 is C6-C14 aryl, five-membered ring heteroaryl, six-membered ring heteroaryl, or N-oxido-pyridyl, wherein said C6-C14 aryl five-membered ring heteroaryl, and six-membered ring heteroaryl are each independently and optionally substituted with one or more groups selected from C1-6alkyl, halogenated C1-6alkyl, —NO2, —CF3, C1-6 alkoxy, chloro, fluoro, bromo, and iodo;
- and
- R2 is hydrogen or C1-12alkyl.
1 more element
A process for preparing a compound of formula II,
- comprising reacting a compound of formula III:
- with R1—CHO to form the compound of formula II
- wherein
- R1 is C6-C14 aryl, five-membered ring heteroaryl, six-membered ring heteroaryl, or N-oxido-pyridyl, wherein said C6-C14 aryl five-membered ring heteroaryl, and six-membered ring heteroaryl are each independently and optionally substituted with one or more groups selected from C1-6alkyl, halogenated C1-6alkyl, —NO2, CF3, C1-6 alkoxy, chloro, fluoro, bromo, and iodo.
1 more element
A process for preparing a compound of formula IV,
- comprising:
- reacting a compound of formula II,
- with an akali metal hydroxide in non-aqueous solvent to form the compound of formula IV:
- wherein
- R1 is C6-C14 aryl, five-membered ring heteroaryl, six-membered ring heteroaryl, or N-oxido-pyridyl, wherein said C6-C14 aryl five-membered ring heteroaryl, and six-membered ring heteroaryl are each independently and optionally substituted with one or more groups selected from C1-6alkyl, halogenated C1-6alkyl, —NO2, —CF3, C1-6 alkoxy, chloro, fluoro, bromo, and iodo.
2 more elements
Dependencies are inferred from the claim text.