Benzofused-n-containing heterocycle derivatives

Details Benzofused-n-containing heterocycle derivatives Benzofused-n-containing heterocycle derivatives

C - Chemistry, Metallurgy

07

D

167/208, 260/254

C07D 451/00 (2006.01) A61K 31/44 (2006.01) C07D 215/54 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 451/04 (2006.01) C07D 451/12 (2006.01) C07D 451/14 (2006.01) C07D 453/02 (2006.01) C07D 471/08 (2006.01) C07D 487/08 (2006.01)

Patent

CA 2009300

Abstract "Benzofused-N-containing Heterocycle Derivatives" 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: Image (I) wherein R represents a hydrogen atom or a Cl-6 alkyl group; R1 and R2, which may be the same or different, represent a hydrogen or halogen atom, or a 1-6 alkyl, C1-6 alkoxy, Cl-6 alkylthio, Cl-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 or C1-6 acyl group; R3 represents a hydrogen atom, or a C1-6 alkyl, aryl or aralkyl group, or it may be absent: A represents CO, C = S, S ? O or S°2; B represents a nitrogen atom when R3 is absent and the B-D bond is a single bond, or is a carbon atom; D represents a CO, -CH2-CH2 or C Image group when the B-D bond is a single bond, in which R4 represents a hydrogen atom, or a C1-6 alkyl, aryl, aralkyl, hydroxy or C1-4 alkoxy group and R5 represents a hydrogen atom, or D represents C-R when the D-B bond is a double bond, in which R is as defined above; X represents a oxygen atom, or a N-R group in which R is as defined above, or it is absent; Y represents a group selected from: Image a) Image b) Image c) in which n is 2 or 3; each p is 0 or 1, and is independent of the other value of p; q is 0, 2 or 3; R6 and R7, which may be the same or different, each represent a hydrogen atom, or a C1-4 alkyl or aralkyl group or, when R7 is a hydrogen atom or C1-4 alkyl group, R6 may additionally represent a Image = N - R group in which R8 represents a hydrogen atom, or a C1-4 alkyl or amino group, and R is as hereinbefore defined; and all optical isomers, tautomeric forms and mixtures thereof, and acid addition salts, internal salts or quaternary derivatives thereof. Processes for the preparation of the compounds of formula (I) and pharmaceutical compositions containing them are also described.

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