| 摘要 |
A class of phenylsulphonyl derivatives of the following formula (I) wherein Z represents halogen, cyano, nitro, trifluoromethyl, trifluoromethoxy, -R<a>, -OR<a>, -SR<a>, -SOR<a>, -SO2R<a>, -SO2NR<a>R<b>, -NR<a>R<b>, -NR<a>COR<b>, -NR<a>CO2R<b>; -COR<a>; -CO2R<a >or -CONR<a>R<b>; or Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or Z represents an optionally substituted six-membered heteroaromatic ring selected from pyridine, pyrazine, pyrimidine and pyridazine; R<a >and R<b >independently represent hydrogen of C1-6 alkyl, or R<a >and R<b>, when linked through a nitrogen atom, together represent the residue of an azetidine, pyrrolidine, piperidine or morpholine ring; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms, optionally incorporating an oxygen atom to form an ether linkage; R<1 >represents an optionally substituted aryl(C2-4)alkyl group; and R<2 >represents hydrogen or halogen, which are selective antagonists of the human 5-HT2A receptor an are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.
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