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    INDOLE AND AZAINDOLE DERIVATIVE HAVING AMPK-ACTIVATING ACTIVITY
    5.
    发明申请
    INDOLE AND AZAINDOLE DERIVATIVE HAVING AMPK-ACTIVATING ACTIVITY 有权
    具有AMPK活化活性的吲哚和吖啶衍生物

    公开(公告)号：US20150203450A1

    公开(公告)日：2015-07-23

    申请号：US14413337

    申请日：2014-02-26

    申请人： SHIONOGI & CO., LTD

    发明人： Yuusuke Tamura ,  Eiichi Kojima ,  Hidaka Ikemoto ,  Yu Hinata

    IPC分类号： C07D209/34 ,  C07D471/04 ,  C07D405/12 ,  C07D493/04 ,  C07D519/00

    CPC分类号： C07D209/34 ,  A61K31/4045 ,  A61K31/5377 ,  C07D209/42 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04 ,  C07D493/04 ,  C07D519/00 ,  C07H17/02

    摘要： Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or its pharmaceutically acceptable salt, wherein Y is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, or substituted or unsubstituted heterocyclyl; T is —CR7═ or —N═; U is —CR8═ or —N═; R2 is hydrogen, halogen, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted acyl, substituted or unsubstituted carbamoyl, substituted or unsubstituted alkylthio, substituted or unsubstituted alkylsulfinyl, substituted or unsubstituted alkylsulfonyl, or substituted or unsubstituted alkyloxycarbonyl; R3 is halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl, or the like; and R4, R7 and R8 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl, or the like.

    摘要翻译： 公开了可用作AMPK活化剂的化合物。 取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基，取代或未取代的杂芳基，取代或未取代的环烷基，取代或未取代的环烯基， 或取代或未取代的杂环基; T为-CR7 =或-N =; U为-CR8 =或-N =; 取代或未取代的酰基，取代或未取代的氨基甲酰基，取代或未取代的烷硫基，取代或未取代的烷基亚磺酰基，取代或未取代的烷基磺酰基，或取代或未取代的烷基磺酰基， 未取代的烷氧基羰基; 取代或未取代的芳基，取代或未取代的杂芳基，取代或未取代的环烷基，取代或未取代的环烯基，取代或未取代的杂环基等; 取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基，取代或未取代的杂芳基，取代或未取代的环烷基 取代或未取代的环烯基，取代或未取代的杂环基等。

    Heterocyclic derivative having AMPK-activating activity
    6.
    发明授权
    Heterocyclic derivative having AMPK-activating activity 有权

    公开(公告)号：US10123994B2

    公开(公告)日：2018-11-13

    申请号：US15522504

    申请日：2015-10-27

    申请人： SHIONOGI & CO., LTD.

    发明人： Eiichi Kojima ,  Yu Hinata ,  Toshihiro Wada

    IPC分类号： A61K31/4188 ,  C07D419/14 ,  A61K31/382 ,  A61K31/34 ,  A61K31/5375 ,  A61K31/415

    摘要： A compound of formula: or its pharmaceutically acceptable salt. L is NR2R3, SR7, SO2R8, alkyl, or alkenyl; R2 is hydrogen, alkyl, alkenyl, or alkynyl; R3 is hydrogen, alkyl, alkenyl, alkynyl; R7 is hydrogen, alkyl, alkenyl, or alkynyl; R8 is hydrogen, alkyl, alkenyl, or alkynyl, provided that R8 is not unsubstituted methyl or trifluoromethyl; Y is alkyl, alkenyl, alkynyl, aryl, provided that Y is not unsubstituted methyl or unsubstituted ethyl; Z is —CR6═, or —N═; R1 is hydrogen, or alkyl; R4, R5 and R6 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, alkyl, alkenyl, or alkynyl.

    Azaindole derivative having AMPK-activating activity
    7.
    发明授权
    Azaindole derivative having AMPK-activating activity 有权

    公开(公告)号：US09980948B2

    公开(公告)日：2018-05-29

    申请号：US15505772

    申请日：2015-08-26

    申请人： Shionogi & Co., Ltd.

    发明人： Yuusuke Tamura ,  Yu Hinata ,  Eiichi Kojima ,  Hiroki Ozasa

    IPC分类号： C07D401/02 ,  C07D401/10 ,  C07D401/14 ,  A61K31/437 ,  A61K31/4353 ,  A61K31/444 ,  A61K31/5377 ,  C07D471/04 ,  C07D519/00 ,  A61K31/03 ,  A61K31/10 ,  A61K31/343

    CPC分类号： A61K31/437 ,  A61K31/03 ,  A61K31/10 ,  A61K31/343 ,  A61K31/444 ,  A61K31/5377 ,  C07D471/04 ,  C07D519/00

    摘要： Disclosed is a compound which is useful as an AMPK activator.A compound represented by formula: or its pharmaceutically acceptable salt, wherein X is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, or substituted or unsubstituted heterocyclyl; R1 is hydrogen, halogen, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted acyl, substituted or unsubstituted carbamoyl, substituted or unsubstituted alkylthio, substituted or unsubstituted alkylsulfinyl, substituted or unsubstituted alkylsulfonyl, or substituted or unsubstituted alkyloxycarbonyl; R2 is halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl, or the like; R3 is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl, or the like; and R4 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like.