2-OXAZOLAMINES AND THEIR USE AS 5-HT2B RECEPTOR ANTAGONISTS

摘要

The present invention relates to compounds of formula (I): wherein one of R1~and R4~ is selected from the group consisting of H, and optionally substituted C~1-6 alkyl, C~3-7 cycloalkyl, C~3-7 cycloalkyl-C~1-4 alkyl, and phenyl-C~1-4 alkyl; and the other of R1~ and R4~ is an optionally substitute d C~9-14 aryl group; R2~ and R3~ are either:(i) independently selected from H, R, R', SO~2R, C(=O)R, (CH~2)~nNR5~R6~, where n is from 1 to 4 and R5~ and R6 ~ are independently selected from H and R, where R is optionally substituted C ~1- 4 alkyl, and R' is optionally substituted phenyl-C~1-4 alkyl, or (ii) togeth er with the nitrogen atom to which they are attached, form an optionally substituted C~5-7 heterocyclic group; and their use as pharmaceuticals, in particular for treating conditions alleviated by the antagonism of a 5-HT~2B receptor.