Benzofused-N-containing heterocycle derivatives

Abstract

Abstract Pharmacologically active benzofused-N-containing heterocycle derivatives are described as muscarinic receptor blocking agents useful for the treatment of gastrointestinal and respiratory tract disorders of the following formula: wherein R represents H or C₁₋₆ alkyl; R₁ and R₂ represent H, halogen, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ alkylthio, C₁₋₆ alkoxycarbonyl, carboxyl, hydroxy, nitro, cyano, optionally C₁₋₄ alkyl mono- or disubstituted carbamoyl, optionally C₁₋₄ alkyl mono- or disubstituted amino, C₁₋₆ acylamino, C₁₋₄ alkoxy carbonylamino, C₁₋₆ alkylsulphynyl, C₁₋₆ alkylsulphonyl, C₁₋₆ acyl; R₃ represents H, C₁₋₆ alkyl, aryl, aralkyl or it may be absent; A represents CO, C = S, S -> O or B represents nitrogen when R₃ is absent and the B-D bond is single, or it is carbon; D represents CO, CH₂-CH₂, when the B-D bond is single, or D is C-R when the D-B bond is double, in which R₄ represents H, C₁₋₆ alkyl, aryl, aralkyl, hydroxy, C₁₋₄ alkoxy and R₅ represents H; X represents oxygen, N-R or it is absent; Y represents a basic group selected from: in which n is 2 or 3; p is 0 or 1 at the same time or not; q is 0, 2 or 3; R₆ and R₇ may be at the same time or not H, C₁₋₄ alkyl, aralkyl or, when R₇ is H or C₁₋₄ alkyl, R₆ may be in which R₈ represents H, C₁₋₄ alkyl or amino. The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.

Inventors

• 👤 Rosamaria Micheletti
• 👤 Henri Nico Doods
• 👤 Marco Turconi
• 👤 Angelo Sagrada
• 👤 Arturo Donetti
• 👤 Battista Giovanni Schiavi

Bibliographic Details