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 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 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.
Claims15
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof or N-oxide thereof, wherein:
- Z is O or NRa, wherein Ra is hydrogen or C1-6 alkyl;
- R1 is a ring of the formula (a)-(h) below:
- 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 pyridinyl or pyrazolyl, each optionally substituted with one or two substituents independently selected from C1-6 alkyl, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 alkoxy, cyano, and halo;
- all of X1, X2, X3, and X4 are CR5 or one of X1, X2, X3, and X4 is N and the others are CR5;
- each R5 is independently hydrogen, C1-6 alkyl, halo, hydroxy, or cyano, provided that at least one of R5 is hydrogen;
- and
- X5 is N or CR6, wherein R6 is hydrogen, C1-6 alkyl or halo.
The compound or pharmaceutically acceptable salt of claim wherein one of X1, X2, X3, and X4 is N and the others are CR5.
The compound or pharmaceutically acceptable salt of claim wherein X1 is N and X2, X3, and X4 are CR5.
Dependencies are inferred from the claim text.