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    • 10. 发明公开
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    • 핀치,해리레이,니콜라스,찰스불,리차드,제임스반네일,모니크,보딜제닝스,앤드류,스티븐,로버트
    • C07C219/24C07C233/41C07C271/38
    • C07C271/38C07C219/24C07C235/36C07C2602/42C07D211/14C07D311/84C07D311/86C07D333/16C07D409/06C07D409/14
    • Compounds of formula (I) have muscarinic M3 receptor modulating activity; Formula(I) wherein A is an oxygen atom or group-N(R12)-;(i) R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group-R5,-Z-Y-R5-Z-NR9R10;-Z-CO-NR9R 10;-Z-NR9-CO-R5; or-Z-CO2H; and R3 is a lone pair,or C1-C6-aIkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R1 and R 3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a hydrogen atom; or a group-R5,-Z-Y-R5,-Z-NR9R10,-Z-CO-NR9R10,-Z-NR9-CO-R5, or-Z-CO2H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R 1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group-Y-R5,-Z-Y-R5,-Z-NR9R 10;-Z-CO-NR9R10;-Z-NR9-CO-R 5; or-Z-CO2H and R3 is a lone pair, or C 1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; R 4 is a group of formula (a), (b), (c) or (d); is an C1-C6-alkyl, aryl, aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group, and the remaining variables are as defined in the specification.
    • 式(I)化合物具有毒蕈碱M3受体调节活性; 式(I)其中A是氧原子或基团-N(R12) - ;(i)R1是C1-C6-烷基或氢原子; 并且R 2为氢原子或-R 5,-Z-Y-R 5 -Z-NR 9 R 10; -Z-CO-NR 9 R 10; -Z-NR 9 -CO-R 5; 或-Z-CO 2 H; 并且R 3是孤对的,或者C 1 -C 6烷基,在这种情况下,其所连接的氮原子是季氮并携带正电荷; 或(ii)R 1和R 3与它们所连接的氮一起形成杂环烷基环,并且R 2是氢原子; 或基团-R 5,-ZY-R 5,-Z-NR 9 R 10,-Z-CO-NR 9 R 10,-Z-NR 9 -CO-R 5或-Z-CO 2 H,其中附着的氮原子是 季氮并带正电荷; 或(iii)R 1和R 2与它们所连接的氮一起形成杂环烷基环,所述环被基团-Y-R 5,-ZY-R 5,-Z-NR 9 R 10,-Z-CO- NR9R10; -Z-NR9-CO-R5; 或-Z-CO 2 H,并且R 3是孤对或C 1 -C 6 - 烷基,在这种情况下,其所连接的氮原子是季氮并携带正电荷; R 4是式(a),(b),(c)或(d)的基团; 是C 1 -C 6烷基,芳基,芳基稠合环烷基,芳基 - 稠合 - 杂环烷基,杂芳基,芳基(C 1 -C 8 - 烷基) - ,杂芳基(C 1 -C 8 - 烷基) - ,环烷基或杂环烷基, 剩余的变量如规范中所定义。