| 摘要 |
The present invention relates to new 1-hetero-arylazetidines and -pyrrolidines endowed with 5-HT3 agonist activity, of formula (I) <IMG> (I) in which A denotes a -CH=CH-, -CH=N- or -N=CH- group; R denotes a hydrogen atom, a halogen atom, a C1-C4 alkyl, C1-C4 alkoxy or C1-C4 alkylthio group, a cyano, carboxamido, trifluoromethyl, vinyl or formyl group, a carboxyl group in free, salt or esterified form, a hydroxyl, hydroxymethyl or mercapto group or an amino, mono- or di(C1-C4 alkyl)amino, aminomethyl, mono- or di(C1-C4 alkyl)aminomethyl, 1-piperidino, 1-pyrrolidino, 1-piperazino or 4-(C1-C4 alkyl)-1-piperazino group, it being possible for this group R to replace any one of the hydrogen atoms of the heteroaryl nucleus; R1 is a hydrogen atom or a methyl group: R2 and R3, which are identical or different, denote a hydrogen atom or a C1-C4 alkyl group; n is 1 or 2, m is 1 or O and m + n ? 2; and their addition salts with inorganic or organic acids. The invention also relates to the process for the preparation of said new compounds, the process intermediates and the use of the compounds (I) as drugs.
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