PHENOXYBENZYLAMINE DERIVATIVES AS SELECTIVE SEROTONIN RE-UPTAKE INHIBITORS

摘要

A compound of general formula (I) wherein R1 and R2 are H, C1-C6alkyl or (CH2)d(C3-C6cycloalkyl) wherein d = 0, 1, 2 or 3; or R1 and R2 together with the nitrogen to which they are attached from an azetidine ring; Z or Y is -S R3 and the other Z or Y is halogen or -R3; wherein R3 is C1-C4 alkyl optionally substituted with fluorine; except that R3 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; R4 and R5, 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, CONR6R7, SO2NR6R7 , SO2NHC(=O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently b y one or more R13; wherein R13 is hydroxy, C1-C4alkoxy, F, C1-C6alkyl, haloalkyl, haloalkoxy, -NH2, NH(C1-C6alkyl) or -N(C1-C6alkyl)2. The compound s of general formula (I) inhibit monoamine reuptake and in particular exhibit activity asselective serotonin reuptake inhibitors.