6-METHOXY-1H-BENZOTRIAZOLE-5-CARBOXAMIDE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, AND MEDICINAL COMPOSITION CONTAINING THE SAME

摘要

6-Methoxy-1H-benzotriazole-5-carboxamide derivatives which are represented by the formula (I) below: Äin which R<1> stands for ethyl or cyclopropylmethyl group, R<2> stands for hydrogen atom, methyl or ethyl group, n is 1, 2 or 3, and the wavy line ( @ ) signifies that configuration of the substituents on the carbon atom bound to the N-atom in the amide moiety is racemic (RS) or optically active (R or S)Ü or their pharmaceutically acceptable acid addition salts; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or its pharmaceutically acceptable acid addition salt; and novel intermediates. The compounds of the present invention possess concurrently excellent antiemetic activity and gastrointestinal motility enhancing activity. They furthermore exhibit less central nervous system (CNS) depressant activity and, therefore, are used for treatments and prophylaxis of functional disorders of gastrointestinal tract associated with various diseases and therapeutical treatments, as gastrointestinal motility enhancing agent.