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    6-AZAINDOLE COMPOUND
    1.
    发明申请
    6-AZAINDOLE COMPOUND 审中-公开
    6-AZAINDOLE化合物

    公开(公告)号：WO2005097129A2

    公开(公告)日：2005-10-20

    申请号：PCT/US2005/011531

    申请日：2005-04-04

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  HORIGUCHI, Yoshiaki ,  IMOTO, Hiroshi ,  WOLF, Mark, A.

    Inventor： HORIGUCHI, Yoshiaki ,  IMOTO, Hiroshi ,  WOLF, Mark, A.

    IPC: A61K31/4745

    CPC classification number: C07D471/04

    Abstract: A compound represented by the formula (I) wherein R 1 , R 2 , R 3 and R 6 are the same or different and each is a hydrogen atom or a substituent; one of R 4 and R 5 is a hydrogen atom and the other is a group represented by the formula: -C(=X)-R 7 wherein X is N-O-R 8 or N-NH-R 9 wherein R 8 and R 9 are the same or different and each is a hydrogen atom or a group bonded via a carbon atom; and R 7 is a hydrogen atom or a substituent, and the like and a salt thereof have a superior IκB kinase inhibitory activity, and useful as pharmaceutical agents such as agents for preventing or treating diabetes and the like.

    Abstract translation: 由式（I）表示的化合物，其中R 1，R 2，R 3和R 6相同或不同，各自为氢原子或取代基; R 4和R 5之一是氢原子，另一个是由下式表示的基团-C（= X）-R 7其中X是NOR 8或N-NH-R 其中R 8和R 9相同或不同，各自为氢原子或通过碳原子键合的基团; R 7为氢原子或取代基等，并且其盐具有优异的IkappaB激酶抑制活性，可用作药物，例如糖尿病的预防或治疗剂等。

    GIP RECEPTOR AGONIST PEPTIDE COMPOUNDS AND USES THEREOF
    2.
    发明申请
    GIP RECEPTOR AGONIST PEPTIDE COMPOUNDS AND USES THEREOF 审中-公开

    公开(公告)号：WO2020067557A2

    公开(公告)日：2020-04-02

    申请号：PCT/JP2019/038441

    申请日：2019-09-24

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

    Inventor： IMOTO, Hiroshi ,  ADACHI, Mari ,  KANEMATSU, Yoko ,  ASAMI, Taiji ,  NIIDA, Ayumu ,  NISHIZAWA, Naoki ,  COLE, Derek, Cecil ,  FLINSPACH, Mack ,  SCORAH, Nick ,  BHAT, Abhijit, Suresh

    Abstract: The present disclosure provides GIP receptor agonist peptide compounds having an activating action on GIP receptors and use of the GIP receptor agonist peptide as a medicament for the treatment and/or prevention of diabetes, obesity, emesis, or a symptom or condition associated with diabetes, obesity, or emesis. Specifically, a GIP receptor agonist peptide containing a sequence represented by the formula (I) or a salt thereof, and a medicament comprising the same are provided. Formula I: P 1 - A 1 - A2- A3 - A4- A5 - A6- A7 - A8-A9-A 10- A 11 - A 12- A 13- A 14- A 15-A 16-A 17-A18-A19-A20-A21 -A22-A23-A24-A25- A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-A37-A38-A39-A40-A41-P2 (SEQ ID NO: 4), or a salt thereof, wherein each symbol is as defined herein, with the proviso that the GIP receptor agonist peptide does not have an amino acid sequence as provided in SEQ ID NOs: 4-569 disclosed in PCT/JP2018/013540.

    FUSED HETEROCYCLIC RING COMPOUND
    8.
    发明公开
    FUSED HETEROCYCLIC RING COMPOUND 审中-公开
    FUSIONIERTE HETEROZYKLISCHE RINGVERBINDUNG

    公开(公告)号：EP2399914A1

    公开(公告)日：2011-12-28

    申请号：EP10743789.9

    申请日：2010-02-17

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： RIKIMARU, Kentaro ,  IMOTO, Hiroshi ,  KAMAURA, Masahiro

    IPC: C07D401/14 ,  A61K31/454 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61P1/00 ,  A61P1/02 ,  A61P1/04 ,  A61P1/08 ,  A61P1/12 ,  A61P1/16 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P7/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12

    CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04

    Abstract: A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy:

    wherein
    P: substituted 6-membered aromatic ring,
    Q: (substituted) 6-membered aromatic ring,
    A 1 : CR 4a R 4b , NR 4c , O, S, SO or SO 2 {R 4a-4c : H etc.},
    L 1 : (substituted) C 1-5 alkylene,
    L 2 : a bond or (substituted) C 1-3 alkylene,
    L 3-4 : (substituted) C 1-3 alkylene,
    R 1 : H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A 1 ,
    R 2 : H, CN, (substituted) hydrocarbon, and
    R 3a : -COSR A1 , (substituted) 5- or 6-membered aromatic ring {R A1 : (substituted) hydrocarbon or (substituted) heterocycle}.

    Abstract translation: 具有GPR119激动剂作用的由下式表示的化合物或其盐可用于预防或治疗糖尿病，肥胖症等，并且显示出优异的疗效：其中P：取代的6元芳环Q ：（取代的）6元芳环，A 1：CR 4a R 4b，NR 4c，O，S，SO或SO 2 {R 4a-4c：H等}，L 1：（取代的）C 1-5 亚烷基，L 2：键或（取代的）C 1-3亚烷基，L 3-4：（取代的）C 1-3亚烷基，R 1：H，X，CN，（取代的）烃，（取代的）杂环或 （取代的）OH，或（取代的）4至8元（杂环）环与A 1，R 2：H，CN，（取代的）烃和R 3a：-COSR A1，（取代的） 6元芳环{R A1：（取代的）烃或（取代的）杂环}。

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