| 摘要 |
1,7-Annelated esters and amides of indolecarboxylic acids having formula 2, <IMAGE> (2) wherein R1 is halogen; n has a value of 0-2; Z together with the carbon atom, the nitrogen atom and the intermediate carbon atom, forms a heterocyclic group consisting of 6 ring atoms in which, besides the nitrogen atom already present, a second hetero atom of S is present, which ring may be annelated with a benzene ring; R3 is hydrogen, halogen, alkyl, alkoxy or alkylthio having 1-4 carbon atoms; and R2 is a group -CO-Y-R7 wherein Y is an oxygen atom, or a group -NR6, wherein R6 is hydrogen or alkyl having 1-3 C-atoms, and R7 represents a group of the formula <IMAGE> wherein p has the value 1 or 2, q has the value 2 or 3, R8 is hydrogen or alkyl or hydroxyalkyl having 1 or 2 C-atoms, r is 0 or 1, and R10 is absent. The compounds and their salts are very strong selective antagonists of neuronal 5-hydroxytryptamine (5-HT) receptors, and can be used for the treatment of symptoms which are caused by over-stimulation of those receptors.
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