New 3-piperidinyl -1,2-benz-isothiazole and -isoxazole derivs. - having antipsychotic and anti-serotonin activity

摘要

Piperidine derivs. of formula (I) and their pharmaceutically acceptable acid addn. salts are new. R = H or 1-6C alkyl; R1 and R2 = H, halo, OH, 1-6C alkoxy or 1-6C alkyl; X = O or S; Alk = 1-4C alkanediyl; Q = a gp. of formula (a) or (b); Y1 and Y2 = O or S; R3 = H, halo, 1-6C alkyl, 1-6C alkoxy, CF3, NO2, CN, OH, 2-11C alkenoyloxy, NH2, mono- or di(1-6C alkyl)amino, 2-11C alkanoylamino, benzyloxy or azido; R4 = H or halo, R5 = H or 1-6C alkyl; Z = S, CH2 or C(R6) = C(R7); R6 and R7 = H or 1-6C alkyl; A = CH2CH2, CH2CH2CH2 or C(R8)=C(R9); R8 and R9 = H, halo, NH2 or 1-6C alkyl. More specifically, R = H; R1 = H or halo; R2 = H, halo, OH or 1-6C alkoxy; R3 = H, halo or Me; Y1 = O; Z-A = SCH2CH2, S(CH2)3; S-CR8=CR9, CH=CH-CR8=CR9 or (CH2)4; R8 and R9 = H or Me. 2 Cpds. (I) including 3-(2-(4-(6-fluoro -1,2-benzioxazol-3-yl)-1 piperidinyl)ethyl)-6,7,8,9 -tetrahydro-2-methyl-4H -pyrido(1,2-a) pyrimidin-4-one (Ia) are specifically claimed.