INDOL-2-ONE DERIVATIVES DISUBSTITUTED IN THE 3-POSITION, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
The present invention relates to 3-disubstituted indol-2-one derivatives, to their preparation and to their therapeutic application.
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(2010/08/22)
Conformationally restricted thiazole derivatives as novel class of 5-HT3 receptor ligands
A new series of tricyclic derivatives of 2-methyl-naphtho[1,2-d] thiazole were synthesized in order to investigate the effects of the conformational restriction of bicyclic thiazole derivatives previously reported on the 5-HT3 receptor affinity. The basic moiety in these compounds is represented by the terminal nitrogen of N-methyl-piperazine or N-methyl-piperidine ring-linked at 2-methyl. All the tricyclic derivatives have a significant 5-HT3 receptor binding affinity and the terminal piperazine ring is more suitable than piperidine one.