5-Bicycloindoles as 5-HT_1D agonists

Abstract

In this patent, novel 3-(2-aminoethyl)-, 3-(piperidin-4-yl)- and (R)-3- (pyrrolidin-2-ylmethyl) 5-bicycloindole derivatives are claimed. They are claimed to be agonists at the 5-HT_1D receptors useful for the treatment of 5-HT_1D-mediated disorders such as migraine. The preparation of the compounds is illustrated by six schemes and exemplified by eight examples.The compounds were tested for their inhibition of [³H]-5-HT binding at 5-HT_1D and 5-HT_1B receptors. The compounds are stated to bind selectively to the 5-HT_1D receptor, relative particularly to the 5-HT_1B receptors.

• 5-bicycloindole
• antimigraine agent
• serotonin 5-HT1D receptor agonist