| 摘要 |
Compounds of formula (I) are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiritory tract diseases: wherein (i) R1 is C1-C6-alkyl or hydrogen; and R2 is hydrogen or a group-R7,-Z-Y-R7,-Z-NR9R10;-Z-CO-NR9 R10,-Z-NR9-[AE11]C(O)O-R7, or-Z-C(O)-R7; and R3 is a lone pair, or C 1C6-alkyl; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a lone pair or a group-R 7,-Z-Y-R7,-Z-NR9R10,-Z-CO-NR9R10,-Z-NR9-[AE12]C(O)O-R7; or;-Z-C(O)-R7; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group-Y-R 7,-Z-Y-R7,-Z-NR9R10;-Z-CO-NR9R10;-Z-NR9-[AE13]C(O)O-R7; or;-Z-C(O)-R7; and R3 is a lone pair, or C1-C6-aIkyl; R4 and R 5 are independently selected from the group consisting of aryl, arytfused-heterocycloalkyl, heteroaryl, C1-C6-alkyl, cycloalkyl; R6 is-OH, C1-C6-alkyl, C1-C6-alkoxy, hydroxy-C1-C6-alkyl, nitrile, a group CONR82 or a hydrogen atom; A is an oxygen or a sulfur atom; X is an alkylene, alkenylene or alkynylene group; R7 is an C1-C6-alkyl, aryl, aryl-fused-cycloalkyl, aryl-ffused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C 8-alkyl)-, cycloalkyl or heterocycloalkyl group; R8 is C1-C6-alkyl or a hydrogen atom; Z is a C1-C16-alkylene, C2-C16-alkenylene or C2-C16-alkynylene group; Y is a bond or oxygen atom; R9 and R10 are independently a hydrogen atom, C1-C6-alkyl, aryl, aryl-fused-heterocycloalkyl, aryl-fused-cycloalkyl, heteroaryl, aryl(C1-C6-alkyl)-, or heteroaryl(C1-C6-alkyl)-group; or R 9 and R10 together with the nitrogen atom to which they are attached form a heterocyclic ring of 48 atoms, optionally containing a further nitrogen or oxygen atom.
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