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    • 2. 发明申请
    • BICYCLO[2.2.1]HEPT-7-YLAMINE DERIVATIVES AND THEIR USES
    • BICYCLO [2.2.1] HEPT-7-YLAMINE DERIVATIVES及其用途
    • US20110319446A1
    • 2011-12-29
    • US13164209
    • 2011-06-20
    • Harry FinchNicholas Charles RayRichard James BullMonique Bodil van NielAndrew Stephen Robert Jennings
    • Harry FinchNicholas Charles RayRichard James BullMonique Bodil van NielAndrew Stephen Robert Jennings
    • A61K31/136C07D409/06C07D215/227A61K31/381A61K31/4535A61K31/4709A61P11/00A61P1/00A61P9/00A61P11/08A61P11/06A61P37/08A61P1/06A61P1/04A61P13/02A61P13/06A61P13/10C07C211/53
    • C07C271/38C07C219/24C07C235/36C07C2602/42C07D211/14C07D311/84C07D311/86C07D333/16C07D409/06C07D409/14
    • Compounds of formula (I) have muscarinic M3 receptor modulating activity; 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—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H; and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R1 and R3 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) R1 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—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; R4 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; 其中A是氧原子或基团-N(R 12) - ; (ⅰ)R 1是C 1 -C 6 - 烷基或氢原子; R2为氢原子或基团-R5,-Z-Y-R5,-Z-NR9R10; -Z-CO-NR9R10; -Z-NR9-CO-R5; 或-Z-CO 2 H; 并且R 3是孤对的,或者是C 1 -C 6烷基,在这种情况下,与其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-R5,-Z-Y-R5,-Z-NR9R10,-Z-CO-NR9R10,-Z-NR9-CO-R5或-Z-CO2H,其中, 附着是季氮并带正电荷; 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,-Z-Y-R 5,-Z-NR 9 R 10取代; -Z-CO-NR9R10; -Z-NR9-CO-R5; 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,与其连接的氮原子是季氮并带正电荷; R4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。
    • 10. 发明申请
    • Bicyclo[2.2.1]hept-7-ylamine Derivatives and Their Uses
    • 双环[2.2.1]庚-7-基胺衍生物及其用途
    • US20100144852A1
    • 2010-06-10
    • US12063212
    • 2006-08-08
    • Harry FinchNicholas Charles RayRichard James BullMonique Bodil van NielAndrew Stephen Robert Jennings
    • Harry FinchNicholas Charles RayRichard James BullMonique Bodil van NielAndrew Stephen Robert Jennings
    • A61K31/381C07C269/00C07D409/06A61K31/24A61P11/06A61P1/00A61P9/10
    • 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—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H; and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R1 and R3 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) R1 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—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; R4 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)R 1是C 1 -C 6 - 烷基或氢原子; 并且R 2是氢原子或基团-R 5,-Z-Y-R 5 -Z-NR 9 R 10; -Z-CO-NR9R10; -Z-NR 9 -CO-R 5; 或-Z-CO 2 H; 并且R 3是孤对的,或者是C 1 -C 6烷基,在这种情况下,与其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-R5,-Z-Y-R5,-Z-NR9R10,-Z-CO-NR9R10,-Z-NR9-CO-R5或-Z-CO2H,其中, 附着是季氮并带正电荷; 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,-Z-Y-R 5,-Z-NR 9 R 10取代; -Z-CO-NR9R10; -Z-NR9-CO-R5; 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,与其连接的氮原子是季氮并带正电荷; R4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。