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    OCTAHYDRO-PYRROLO[3,4-B]PYRROLE DERIVATIVES
    9.
    发明公开
    OCTAHYDRO-PYRROLO[3,4-B]PYRROLE DERIVATIVES 审中-公开
    十八烷基吡咯并[3,4-B]吡咯衍生物

    公开(公告)号：EP2001885A2

    公开(公告)日：2008-12-17

    申请号：EP07757130.5

    申请日：2007-02-16

    Applicant: ABBOTT LABORATORIES

    Inventor： COWART, Marlon, D. ,  ZHAO, Chen ,  SUN, Minghua ,  BLACK, Lawrence, A. ,  ZHENG, Guo Zhu ,  GREGG, Robert, J. ,  ZHANG, Geoff, G.Z. ,  SHEIKH, Ahmad, Y. ,  LOU, Xiaochun ,  HENRY, Rodger, F. ,  BARNES, David, M. ,  KOLACZKOWSKI, Lawrence ,  HAIGHT, Anthony, R. ,  CHANG, Sou-Jen ,  WITTENBERGER, Steven, J. ,  FICKES, Michael, G.

    IPC: C07D487/04 ,  A61K31/407

    CPC classification number: C07D487/04

    Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives or a pharmaceutically acceptable salt, ester, amide, prodrug, or radiolabeled form thereof, wherein R1 is alkyl, C3-C5 cycloalkyl. or (C3-C5 cycloalkyl)methyl; R2a, R2b, R2c, R2d, R2e, and R2f each are independently hydrogen, methyl, or fluoromethyl; R3a, R3b, R3c, and R3d each are independently hydrogen, alkyl, fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile, with the proviso that when one or more of R3a, R3b, R3c, and R3d are alkyl, then at least one of R3a, R3b, R3c, and R3d is fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile; L1 is a bond, oxygen, sulfur, carbonyl, alkylene,. alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR4, -C(=O) NR4-, or -NR4C(=O)-; R4 is hydrogen or alkyl; Cy1 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; Z is a substituent R6 or a group represented by -L3-Cy3; R6 is hydrogen, acyl, acyloxy, alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxyimino, alkoxysulfonyl, alkyl, alkylcarbonyl, alkylsulfonyl, alkynyl, amido, carboxy, cyano, cycloalkyl, fiuoroalkoxy, haloalkoxy, haloalkyl, halogen, hydroxy, hydroxyalkyl, mercapto, nitro, alkylthio, amino, NHR7, NR7R8, -N(R7)C(=O)R9, -C(=O)NR7R8, or N(R7)SO2(R10); L3 is a bond, oxygen, sulfur, carbonyl, alkylene, alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR11, -C(=O) NR11-, or -NR11C(=O)-;Cy3 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; R7, R8, R9, R10, and R11 at each occurrence are independently hydrogen,C1-4 alkyl, C3-C4 cycloalkyl, or a (C3-C4 cycloalkyl)amine; are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

    Abstract translation: 八氢 - 吡咯并[3,4-b]吡咯衍生物或其药学上可接受的盐，酯，酰胺，前药或放射性标记的形式，其中R 1为C 3 -C 5环烷基。 或（C 3 -C 5环烷基）甲基; R2a，R2b，R2c，R2d，R2e和R2f各自独立地为氢，甲基或氟甲基; R3a，R3b，R3c和R3d各自独立地为氢，烷基，氟代烷基，氟代烷氧基，烷氧基，硫代烷氧基，卤素或腈，条件是当R3a，R3b，R3c和R3d中的一个或多个为烷基时， R 3a，R 3b，R 3c和R 3d中的至少一个是氟烷基，氟烷氧基，烷氧基，硫代烷氧基，卤素或腈; L1是一个键，氧，硫，羰基，亚烷基。 （= N-O烷基） - ，NR 4，-C（= O）NR 4 - 或-NR 4 C（= O） - ; R4是氢或烷基; Cy1是芳基，环烷基，环烯基，杂芳基或杂环; Z是取代基R6或由-L3-Cy3表示的基团; 烷基羰基，烷基磺酰基，炔基，酰氨基，羧基，氰基，环烷基，氟代烷氧基，卤代烷氧基，卤代烷基，卤素，羟基，羟基烷基，烷基氨基， 巯基，硝基，烷硫基，氨基，NHR7，NR7R8，-N（R7）C（= O）R9，-C（= O）NR7R8或N（R7）SO2（R10）。 L3是键，氧，硫，羰基，亚烷基，烷基羰基，烷基氨基，-C（= N-O烷基） - ，NR 11，-C（= O）NR 11 - 或-NR 11 C（= O） - ; Cy 3是芳基 ，环烷基，环烯基，杂芳基或杂环; R7，R8，R9，R10和R11各自独立地为氢，C1-4烷基，C3-C4环烷基或（C3-C4环烷基）胺; 可用于治疗由组胺-3受体配体阻止或改善的病症或障碍。 本文公开了八氢 - 吡咯并[3,4-b]吡咯化合物，使用这些化合物的方法，制备它们的组合物以及制备这些化合物的方法。

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