| abstract |
New pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid derivatives which are 5-HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents of the following formula:n wherein R represents a hydrogen atom, C₁₋₆ alkyl, C₁₋₆ alkenyl or C₁₋₆ alkynil; 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 alkoxycarbonyl, 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, C₁₋₆alkylsulphinyl, C₁₋₆ alkylsulphonyl, amino sulphonyl optionally C₁₋₄ alkyl N-mono or di-substituted, C₁₋₄ alkyl N-mono or di-substituted aminosulphonylamino, aminosulphonylamino; Y is oxygen or is N - R₃ in which R₃ is a hydrogen, a C₁₋₆ alkyl or optionally substituted by one or more C₁₋₆ alkoxy benzyl; A is a group selected from: n wherein p is 0, 1; r is 0, 1, 2, 3; R₄ is hydrogen atom or a C₁₋₄ alkyl; R₅ is a hydrogen atom, C₁₋₆ alkyl, C₃₋₈ cycloalkyl, C₃₋₈ cycloalkyl C₁₋₄ alkyl,substituted phenyl C₁₋₄ alkyl or R₅ is a group of formulan wherein R₆ is hydrogen atom, C₁₋₄ alkyl or an amino group and R₇ is hydrogen atom or C₁₋₆ alkyl, tautomers thereof and acid addition salts of the aforesaid compounds. n The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described. |