EP0526434A1 — Benzimidazolone derivatives as 5-HT1A and 5-HT2 antagonists

USPTO Abstract

Pharmacologically active benzimidazolone derivatives as 5-HT 1A and 5-HT₂ receptors, useful in the treatment of CNS disorders of formula: wherein R₁ and R₂ may be at the same time or not a hydrogen atom, halogen, trifluoromethyl, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ alkylthio, C₁₋₆ acyl, carboxyl, C₁₋₆ alkoxy- carbonyl, hydroxy, nitro, amino optionally C₁₋₄ alkyl N-mono or di-substituted, C₁₋₆ acylamino, C₁₋₆ alkoxycarbonylamino, carbamoyl optionally C₁₋₄ alkyl N-mono or di-substituted, cyano, C₁₋₆ alkylsulphinyl, C₁₋₆ alkylsulphonyl, amino sulphonyl optionally C₁₋₄ alkyl N-mono or di-substituted, C₁₋₄ alkyl N-mono or di-substituted aminosulphonylamino, aminosulphonylamino;    R₃ is hydrogen, C₁₋₆ alkyl, C₂₋₆ alkenyl or C₂-C₆ alkynyl;    A is -CO- or -CONH- or it is absent;    B is a straight or branched, saturated or unsaturated C₂₋₆ alkyl;    m and n are both independently an integer from 1 to 3;    R₄ is an aryl, aralkyl, a heteroaryl or heteroaralkyl group, each group being optionally substituted by one or more substituents selected from halogen, trifluoromethyl, cyano, C₁₋₃ alkoxy, C₁₋₄ alkyland acid addition salts thereof.    The process for the preparation of the compounds of formula I as well as pharmaceutical compositions containing them are also described.