Benzofused-N-containing heterocycle derivatives

• Main Authors: SCHIAVI, BATTISTA GIOVANNI, TURCONI, MARCO, SAGRADA, ANGELO, DONETTI, ARTURO, DOODS, HENRI NICO, MICHELETTI, ROSAMARIA
• Format: Patent
• Language: English; French; German
• Published: 27.12.1995
• Edition: 5
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

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.