PURPOSE: Benzyl(idene)-lactam derivatives(formula 1) are useful as psychotherapeutic agents. CONSTITUTION: Formula (1) shows a compound wherein R¬1 is a five different formula; R¬2 is hydrogen, (C1-C4)alkyl, phenyl or naphthyl, wherein phenyl or naphthyl may optionally be substituted with one or more substituents; R¬3 is (CH2)mB, wherein m is zero, one, two or three and B is hydrogen, phenyl, naphthyl or a 5- or 6-membered heteroaryl group containing from one to four hetero atoms in the ring and wherein each of the foregoing aryl and hetero aryl groups may optionally be substituted with one or more substituents; Z is R¬4R¬5, wherein R¬4 and R¬5 are independently selected from hydrogen, (C1-C6)alkyl and trifluoromethyl; or Z maybe one of the aryl or heteroaryl groups; X is hydrogen, chloro, fluoro, bromo, iodo, cyano, (C1-C6)alkyl, hydroxy, trifluoromethyl, (C1-C6)alkoxy, -SOg(C1-C6)alkyl, wherein g is zero, one or two, CO2R¬6 or CONR¬7R¬8; each of R¬6, R¬8 is selected, independently, from the radicals set fourth in the definition of R¬2; or R¬7 and R¬8, together with the nitrogen to which they are attached, form a 5- to 7-membered ring; or a pharmaceutically acceptable salts thereof. These compounds are selective (ant)agonists of 5-HT1A(serotonin 1A) and/or 5-HTID(serotonin 1D) receptors.
- / - 1 / 1 / BENZYLIDENE-LACTAM DERIVATIVES THEIR PREPARATION AND THEIR USE AS SELECTIVE ANTAGONISTS OF 5-HT1A- AND/OR 5-HD1D RECEPTORS