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    BICYCLO[2.2.1]HEPT-7-YLAMINE DERIVATIVES AND THEIR USES
    8.
    发明申请
    BICYCLO[2.2.1]HEPT-7-YLAMINE DERIVATIVES AND THEIR USES 审中-公开
    BICYCLO [2.2.1] HEPT-7-YLAMINE DERIVATIVES及其用途

    公开(公告)号：US20110319446A1

    公开(公告)日：2011-12-29

    申请号：US13164209

    申请日：2011-06-20

    申请人： Harry Finch ,  Nicholas Charles Ray ,  Richard James Bull ,  Monique Bodil van Niel ,  Andrew Stephen Robert Jennings

    发明人： Harry Finch ,  Nicholas Charles Ray ,  Richard James Bull ,  Monique Bodil van Niel ,  Andrew Stephen Robert Jennings

    IPC分类号： A61K31/136 ,  C07D409/06 ,  C07D215/227 ,  A61K31/381 ,  A61K31/4535 ,  A61K31/4709 ,  A61P11/00 ,  A61P1/00 ,  A61P9/00 ,  A61P11/08 ,  A61P11/06 ,  A61P37/08 ,  A61P1/06 ,  A61P1/04 ,  A61P13/02 ,  A61P13/06 ,  A61P13/10 ,  C07C211/53

    CPC分类号： C07C271/38 ,  C07C219/24 ,  C07C235/36 ,  C07C2602/42 ,  C07D211/14 ,  C07D311/84 ,  C07D311/86 ,  C07D333/16 ,  C07D409/06 ,  C07D409/14

    摘要： 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.

    摘要翻译： 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。

    ORALLY RAPIDLY DISINTEGRATING TABLET COMPRISING IMIDAFENACIN
    9.
    发明申请
    ORALLY RAPIDLY DISINTEGRATING TABLET COMPRISING IMIDAFENACIN 审中-公开
    ORATY快速消毒包含IMIDAFENACINCIN的片剂

    公开(公告)号：US20110002988A1

    公开(公告)日：2011-01-06

    申请号：US12865737

    申请日：2009-01-30

    申请人： Toshihiro Ishizaki ,  Yoshinobu Aoki

    发明人： Toshihiro Ishizaki ,  Yoshinobu Aoki

    IPC分类号： A61K9/20 ,  A61K31/4174 ,  A61P13/06

    CPC分类号： A61K9/1652 ,  A61K9/0056 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/5026 ,  A61K31/4164

    摘要： Provided herein is an imidafenacin-containing orally rapidly disintegrating tablet which is excellent in the photostability.The orally rapidly disintegrating tablets comprises (1) a granulated product containing imidafenacin or imidafenacin particles, which is or are coated with povidone or a gastric juice-soluble polymer; and (2) a composition containing an excipient and a disintegrating agent, wherein the resulting composition is subjected to compression molding.

    摘要翻译： 本发明提供了具有优异的光稳定性的含咪达那新的口服快速崩解片剂。 口服快速崩解片剂包括（1）含有咪达那新或亚胺多沙星颗粒的颗粒状产品，其是或被聚维酮或胃液可溶性聚合物包被; 和（2）含有赋形剂和崩解剂的组合物，其中所得组合物经受压塑。