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    METHOD FOR STEREOSELECTIVELY PRODUCING SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVE
    2.
    发明公开
    METHOD FOR STEREOSELECTIVELY PRODUCING SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVE 审中-公开

    公开(公告)号：EP3693373A1

    公开(公告)日：2020-08-12

    申请号：EP18865221.8

    申请日：2018-10-05

    申请人： Shionogi & Co., Ltd.

    发明人： OKAMOTO, Kazuya ,  UENO, Tatsuhiko ,  HATO, Yoshio ,  HAKOGI, Toshikazu ,  MAJIMA, Shohei

    IPC分类号： C07D498/14 ,  C07D213/89 ,  C07D401/12

    摘要： The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity.
    In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof.

    AROMATIC HETEROCYCLIC FIVE-MEMBERED RING DERIVATIVE HAVING TRPV4 INHIBITORY ACTIVITY
    3.
    发明公开
    AROMATIC HETEROCYCLIC FIVE-MEMBERED RING DERIVATIVE HAVING TRPV4 INHIBITORY ACTIVITY 审中-公开
    具有TRPV4抑制活性的芳香族杂环五员环衍生物

    公开(公告)号：EP2832731A1

    公开(公告)日：2015-02-04

    申请号：EP13769523.5

    申请日：2013-03-26

    申请人： Shionogi & Co., Ltd.

    发明人： YUKIMASA, Akira ,  KOBAYASHI, Naotake ,  TAKAYA, Kenji ,  HATO, Yoshio

    IPC分类号： C07D277/24 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61P1/04 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P11/06 ,  A61P13/02 ,  A61P13/10 ,  A61P17/00 ,  A61P19/08 ,  A61P19/10 ,  A61P25/04

    CPC分类号： C07D417/14 ,  C07D277/44 ,  C07D277/46 ,  C07D277/48 ,  C07D277/56 ,  C07D401/04 ,  C07D401/14 ,  C07D417/04 ,  C07D417/12

    摘要： The present invention is related to a compound represented by formula (I)

    wherein R 1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is -N(R 3 )-, -O-, or -S-; Y is =C(R 4 )-, or =N-; Z is -N(R 7 )-, -O-, or -S-;
    R 2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: -(CR 2a R 2b ) n -R 2c , wherein R 2a is each independently a hydrogen atom, halogen, or the like; R 2b is each independently a hydrogen atom, halogen, or the like; R 2a and R 2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R 2a which are attached to the adjacent carbon atoms and/or two of R 2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R 2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3;
    R 3 and R 7 are each independently a hydrogen atom, substituted or unsubstituted alkyl, or the like;
    R 4 and R 5 are each independently a hydrogen atom, halogen, substituted or unsubstituted alkyl, or the like;
    R 6 is a hydrogen atom, halogen, substituted or unsubstituted alkyl, or the like,
    or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.

    摘要翻译： 本发明涉及由式（I）表示的化合物，其中R 1为氢原子，取代或未取代的烷基，取代或未取代的芳族碳环基等; X是-N（R3） - ， - O-或-S-; Y是= C（R4） - ，或= N-; Z是-N（R 7） - ， - O-或-S-; R2为取代或未取代的烷氧基等，或由下式表示的基团： - （CR2aR2b）n-R2c，其中R2a各自独立地为氢原子，卤素等; R 2b各自独立地为氢原子，卤素等; 连接到相同碳原子上的R2a和R2b可以一起形成氧代，取代或未取代的非芳族碳环等; 与相邻碳原子连接的R2a中的两个和/或与相邻碳原子连接的R2b中的两个可结合在一起形成键; R2c是取代或未取代的芳族碳环基等; n是1至3的整数; R3和R7各自独立地为氢原子，取代或未取代的烷基等; R4和R5各自独立地为氢原子，卤素，取代或未取代的烷基等; R6是氢原子，卤素，取代或未取代的烷基等，或其药学上可接受的盐或包含其的药物组合物。