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US 9,303,045 B2Granted
5-HT3 receptor antagonists
AssigneeTakeda Pharmaceutical Company Limited
InventorsStephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
Life of this patent
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Abstract
The present invention provides compounds of the formula: that are 5HT3 receptor antagonists and are therefore useful for the treatment of diseases treatable by inhibition of 5HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Claims11
A compound of Formula (I):
- wherein:
- Z is O or NRa;
- Ra is hydrogen or C1-6 alkyl;
- R1 is a ring of the formula (a), (d), (e), or (g) below:
- wherein:
- R2 is hydrogen, C1-6 alkyl, or C1-6 haloalkyl;
- each R3 is independently hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkoxy, or halo and can be present on any carbon atom in the rings;
- R4 is heteroaryl selected from the group consisting of furanyl, pyrrolyl, imidazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, isothiazolyl, thiadiazolyl, triazolyl, tetrazolyl, pyrazinyl, and pyridazinyl, each R4 heteroaryl is optionally substituted with one or two substituents independently selected from C1-6 alkyl, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 alkoxy, hydroxy, cyano, or halo;
- all of X1-X4 are CR5;
- each R5 is hydrogen;
- X5 is CR6 where R6 is hydrogen, C1-6 alkyl, or halo;
- or a pharmaceutically acceptable salt thereof or N-oxide thereof.
9 more elements
Dependencies are inferred from the claim text.