| 摘要 |
<p>3-Arylindole or 3-arylindazole derivatives having formula: <CHEM> wherein Ar is optionally substituted phenyl or a heteroaromatic group; R<1>-R<4> are independently selected from hydrogen, halogen, alkyl, alkoxy, hydroxy, nitro, alkylthio, alkylsulphonyl, alkyl- or dialkylamino, cyano, trifluoromethyl, or trifluoromethylthio; the dotted lines designate optional bonds; X is N or a group CR<6> wherein R<6> is hydrogen, halogen, trifluoromethyl or alkyl, or X is CH2; Y is N or CH, or Y is C ; R<5> is hydrogen, cycloalkyl, cycloalkylmethyl, alkyl or alkenyl, optionally substituted with one or two hydroxy groups, or R<5> is a group taken from structures 1a and 1b : <CHEM> wherein n is an integer from 2 - 6; W is O or S; U is N or CH ; Z is -(CH2)m-, m being 2 or 3, -CH=CH- , 1,2-phenylene or -COCH2- or -CSCH2-; V is O, S, CH2, or NR<7>; U<1> is O, S, CH2 or NR<8>; and V<1> is NR<9>R<1><0>, OR<1><1>, SR<1><2> or CR<1><3>R<1><4>R<1><5>, and R<7>-R<1><5> are independently hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkylalkyl ; may be prepared by methods known per se. The compounds are selective centrally acting 5-HT2-antagonists in the brain and are useful in treatment of anxiety, agression, depression, sleep disturbances, migraine, negative symptoms of schizophrenia, drug-induces Parkinsonism and Parkinson's disease.</p> |
