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    METHOD FOR PRODUCING CYCLOHEXANE DERIVATIVE
    5.
    发明公开
    METHOD FOR PRODUCING CYCLOHEXANE DERIVATIVE 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINES CYCLOHEXANDERIVATS

    公开(公告)号：EP2505584A1

    公开(公告)日：2012-10-03

    申请号：EP10833197.6

    申请日：2010-11-24

    申请人： Shionogi & Co., Ltd.

    发明人： KUNITANI, Ryosuke ,  TAKAYA, Kenji ,  IMAMURA, Yoshiaki ,  HASEGAWA, Aiko

    IPC分类号： C07D263/58 ,  C07D277/82

    CPC分类号： C07D263/58 ,  C07D277/82

    摘要： A process for the preparation of a compound of formula (I):

    wherein R 1 is each independently halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy or C1-C6 alkylcarbonyl,
    R 3 is C1-C6 alkyl; C3-C8 cycloalkyl; or phenyl optionally substituted with one or more substituents selected from the group consisting of halogen, C1-C6 alkyl; C1-C6 alkoxy, C1-C6 haloalkyl and C1-C6 haloalkoxy,
    n is an integer of 0 to 2,
    X is S atom or O atom,

    its salt or solvate thereof characterized by reacting a compound of formula (IV):

    wherein R 1 , n and X have the same meaning as defined above, and
    R 2 is C1-C6 alkyl; C1-C6 haloalkyl; or phenyl optionally substituted with one or more substituents selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy and nitro,

    with a compound of formula (V):

    wherein R 3 has the same meaning as defined above.

    摘要翻译： 一种制备式（I）化合物的方法：其中R 1各自独立地为卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷基，C 1 -C 6卤代烷氧基或C 1 -C 6烷基羰基，R 3为 C1-C6烷基; C3-C8环烷基; 或任选被一个或多个选自以下的取代基取代的苯基：卤素，C 1 -C 6烷基; C1-C6烷氧基，C1-C6卤代烷基和C1-C6卤代烷氧基，n是0-2的整数，X是S原子或O原子，其盐或溶剂合物的特征在于使式（Ⅳ）化合物：其中R 1，n和X具有与上述相同的含义，R 2是C 1 -C 6烷基; C1-C6卤代烷基; 或任选被一个或多个选自卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷基，C 1 -C 6卤代烷氧基和硝基的取代基取代的苯基与式（Ⅴ）化合物反应：其中R 3具有与上述相同的含义。

    AROMATIC HETEROCYCLIC FIVE-MEMBERED RING DERIVATIVE HAVING TRPV4 INHIBITORY ACTIVITY
    6.
    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。