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    2-AMINOPYRIDINE DERIVATIVES AS GLUCOKINASE ACTIVATORS
    8.
    发明申请
    2-AMINOPYRIDINE DERIVATIVES AS GLUCOKINASE ACTIVATORS 审中-公开
    2-氨基吡啶衍生物作为GLUCOKINASE激活剂

    公开(公告)号：WO2008091770A1

    公开(公告)日：2008-07-31

    申请号：PCT/US2008/051194

    申请日：2008-01-16

    Applicant: ARRAY BIOPHARMA INC. ,  AICHER, Thomas Daniel ,  BOYD, Steven Armen ,  CHICARELLI, Mark Joseph ,  CONDROSKI, Kevin Ronald ,  GARREY, Rustam Ferdinand ,  HINKLIN, Ronald Jay ,  SINGH, Ajay ,  TURNER, Timothy M.

    Inventor： AICHER, Thomas Daniel ,  BOYD, Steven Armen ,  CHICARELLI, Mark Joseph ,  CONDROSKI, Kevin Ronald ,  GARREY, Rustam Ferdinand ,  HINKLIN, Ronald Jay ,  SINGH, Ajay ,  TURNER, Timothy M.

    IPC: C07D417/14 ,  C07D495/04 ,  A61K31/4439

    CPC classification number: C07D495/04 ,  C07D417/14

    Abstract: Provided are compounds having the Formula (I) or salts thereof, wherein: L is O, S, SO, SO 2 , CHOH, C(O), or CH 2 ; D 2 is CR 12 or N; R 2 is aryl, heteroaryl, saturated or partially unsaturated cycloalkyl, or saturated or partially unsaturated heterocyclyl (optionally substituted with oxo), wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl are monocyclic or bicyclic and are further optionally substituted with one or more groups independently selected from C 1 -C 6 alkyl, F, Cl, Br, I, CF 3 , CN, OR 6 , C(=O)R 6 , C(=O)OR 6 , O(CH 2 ) n C(=O)OR 6 , C(=O)NR 6 R 7 , NO 2 and (1-6C alkyl)OR 6 ; R 3 is H, Br, OR 6 , SR 6 , C(O)OR 6 , C(O)NR 6 R 7 , C(O)R 6 , heteroaryl, or C 1 -C 6 alkyl substituted with one or more groups independently selected from V n -aryl, V n -OR 6 , V n - C(=O)OR 6 and V n -NR 6 R 7 ; R 11 is H or Cl; and R 13 is N-(1 -6C alkanoyl)piperidin-4-yl; that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

    Abstract translation: 提供具有式（I）或其盐的化合物，其中：L是O，S，SO，SO 2，CHOH，C（O）或CH 2 ; D 是CR 12或N; R 2是芳基，杂芳基，饱和或部分不饱和的环烷基或饱和或部分不饱和的杂环基（任选被氧代取代），其中所述芳基，杂芳基，环烷基和杂环基是单环或双环的， 被一个或多个独立地选自C 1 -C 6烷基，F，Cl，Br，I，CF 3 N，CN， C（= O）R 6，C（= O）OR 6，O（CH 2）2， C（= O）OR 6，C（= O）NR 6 R 7，NO 2和（1-6C烷基）OR 6; R 3是H，Br，OR 6，SR 6，C（O）OR 6，C（O） O）NR 6 R 7，C（O）R 6，杂芳基或C 1 -C 6烷基， 被一个或多个独立地选自以下的基团取代的亚烷基烷基：V n - 芳基，V n -OR 6，V C（= O）OR 6和V 6和-NR 6 R 7， SUP>; R 11是H或Cl; 和R 13是N-（1-6C烷酰基）哌啶-4-基; 其可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病。 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

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