5-HT2B receptor antagonists

摘要

The present invention relates to compounds which include compounds of the formula I: or a pharmaceutically acceptable salt thereof, 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 substituted C_9-14 aryl group; R² and R³ are either: (i) independently selected from H, R, R', SO₂R, C(-O)R, (CH₂)_nNR⁵R⁶, 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) together with the nitrogen atom to which they are attached, form an optionally substituted C_5-7 heterocyclic group. The compounds are useful in the treatment of conditions including conditions which can be alleviated by antagonism of a 5-HT_2B receptor such as GI disorders and congestive heart failure.