PHENOXYBENZYLAMINE DERIVATIVES AS SELECTIVE SEROTONIN RE-UPTAKE INHIBITORS

摘要

A compound of general formula (I) wherein R<1> and R<2> are H, C1-C6alkyl or (CH2)d(C3-C6cycloalkyl) wherein d = 0, 1, 2 or 3; or R<1> and R<2> together with the nitrogen to which they are attached from an azetidine ring; Z or Y is -SR<3> and the other Z or Y is halogen or -R<3>; wherein R<3> is C1-C4 alkyl optionally substituted with fluorine; except that R<3> is not CF3; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R<4> and R<5>, which may be the same or different, are: A-X, wherein A = -CH=CH- or -(CH2)p- where p is 0, 1 or 2; X is hydrogen, F, CI, Br, I, CONR<6>R<7>, SO2NR<6>R<7>, SO2NHC(=O)R<6>, OH, C1-4alkoxy, NR<8>SO2R<9>, NO2, NR<6>R<11>, CN, CO2R<10>, CHO, SR<10>, S(O)R<9> or SO2R<10>; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R<13>; wherein R<13> is hydroxy, C1-C4alkoxy, F, C1-C6alkyl, haloalkyl, haloalkoxy, -NH2, NH(C1-C6alkyl) or -N(C1-C6alkyl)2. The compounds of general formula (I) inhibit monoamine reuptake and in particular exhibit activity as selective serotonin reuptake inhibitors.