5-HT2B RECEPTOR ANTAGONISTS

摘要

The present invention concerns compounds of formula (I): wherein R1~ 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;R2~ and R3~ are either: (i) independently selected from H, R, R', SO~2 R, 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 group, and R' is an optionally substituted phenyl- C ~1-4 alkyl group, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C ~5-7 heterocyclic group; R4~ is an optionally substituted C ~9-14 aryl group; their use as pharmaceuticals, in particular for treating conditions alleviated by antagonism of a 5-HT~2B receptor.