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    METHOD FOR PRODUCING PYRAZOLECARBOXYLIC ACID DERIVATIVE
    1.
    发明公开
    METHOD FOR PRODUCING PYRAZOLECARBOXYLIC ACID DERIVATIVE 审中-公开
    生产吡唑羧酸衍生物的方法

    公开(公告)号：EP2687515A1

    公开(公告)日：2014-01-22

    申请号：EP12758005.8

    申请日：2012-03-15

    申请人： Shionogi & Co., Ltd.

    发明人： UENAKA, Masaaki ,  YONEZAWA, Shuji ,  IIDA, Akira ,  TAKAKI, Mutsumi ,  OGAWA, Tomoyuki ,  GODA, Satoshi ,  HIROSE, Yoshikatsu ,  FUKUDA, Tomohiro

    IPC分类号： C07D231/20 ,  C07C241/02 ,  C07C243/16

    CPC分类号： C07D231/20 ,  C07C243/16 ,  C07D413/06 ,  C07C241/02

    摘要： Disclosed is a process for producing a pyrazole carboxylic acid derivative which is useful as a significant intermediate of an 11βHSD-1 inhibitor.
    A compound represented by the Formula (XI):

    is useful as a significant intermediate of an 11βHSD-1 inhibitor,
    wherein R 1 and R 2 are each independently hydrogen or substituted or unsubstituted alkyl, R 3 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocyclyl and R 4 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocyclyl.

    摘要翻译： 本发明公开了一种制备可用作11βHSD-1抑制剂的重要中间体的吡唑羧酸衍生物的方法。 由式（XI）表示的化合物可用作11βHSD-1抑制剂的重要中间体，其中R 1和R 2各自独立地为氢或取代或未取代的烷基，R 3为取代或未取代的烷基，取代或未取代的链烯基，取代 取代或未取代的环烷基，取代或未取代的环烯基，取代或未取代的芳基，取代或未取代的杂芳基或取代或未取代的杂环基，并且R4为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， 取代或未取代的环烯基，取代或未取代的芳基，取代或未取代的杂芳基或取代或未取代的杂环基。

    ISOXAZOLE DERIVATIVE AND ISOTHIAZOLE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11 BETA -HYDROXYSTEROID DEHYDROGENASE TYPE I
    2.
    发明公开
    ISOXAZOLE DERIVATIVE AND ISOTHIAZOLE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11 BETA -HYDROXYSTEROID DEHYDROGENASE TYPE I 审中-公开
    ISOXAZOLDERIVAT UND ISOTHIAZOLDERIVAT MIT HEMMENDER WIRKUNG AUF DIE 11 BETA-HYDROXYSTEROIDDEHYDROGENASE VOM TYP I

    公开(公告)号：EP2006286A2

    公开(公告)日：2008-12-24

    申请号：EP07739976.4

    申请日：2007-03-28

    申请人： Shionogi Co., Ltd.

    发明人： OGAWA, Tomoyuki ,  CHOMEI, Nobuo ,  MASUDA, Koji ,  TANAKA, Satoru

    IPC分类号： C07D261/18 ,  A61K31/42 ,  A61K31/425 ,  A61K31/454 ,  A61P3/10 ,  A61P43/00 ,  C07D275/02 ,  C07D413/12

    CPC分类号： C07D261/18 ,  C07D275/02 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10

    摘要： Disclosed is a compound useful as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1.
    A compound represented by the formula:

    a pharmaceutically acceptable salt or solvate thereof,
    wherein
    R 1 is a group of the formula: -C(=O)NR 4 R 5 ,
    (wherein R 4 and R 5 are each independently, hydrogen, optionally substituted alkyl or the like) or
    a group of the formula: -NR 6 C(=O)R 7 ,
    (wherein R 6 and R 7 are each independently, hydrogen, optionally substituted alkyl or the like),
    X and Y are each independently -0- or the like,
    Z is a bond or the like,
    R 2 is optionally substituted alkyl, optionally substituted alkenyl or the like,
    R 3 is optionally substituted alkyl, optionally substituted alkenyl or the like.

    摘要翻译： 公开了用作11β-羟基类固醇脱氢酶1型抑制剂的化合物。下式表示的化合物：其药学上可接受的盐或溶剂化物，其中R 1是下式的基团-C（= O）NR 4 R 5，（其中R 4和R 5各自独立地为氢，任选取代的烷基等）或下式-NR 6 C（= O）R 7基团（其中R 6和R 7各自独立地为 ，氢，任选取代的烷基等），X和Y各自独立地为-O-等，Z为键或类似物，R 2为任选取代的烷基，任选取代的烯基等，R 3为任选取代的 取代的烷基，任选取代的烯基等。

    NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVE HAVING 11 BETA-HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORY ACTIVITY
    8.
    发明公开
    NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVE HAVING 11 BETA-HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORY ACTIVITY 有权
    蛋白酶抑制剂杂交细胞衍生物麻醉剂11BETA-羟肟酸脱氢酶TYP-1-HEMMUNGSAKTIVITÄT

    公开(公告)号：EP2163543A1

    公开(公告)日：2010-03-17

    申请号：EP08764258.3

    申请日：2008-05-07

    申请人： Shionogi&Co., Ltd.

    发明人： MASUDA, Koji ,  OGAWA, Tomoyuki ,  NAKATANI, Takuji

    IPC分类号： C07D231/14 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/5377 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P43/00 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D405/12

    CPC分类号： C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/20 ,  C07D231/38 ,  C07D405/12 ,  C07D413/06

    摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.
    A compound represented by the formula:

    , its pharmaceutically acceptable salt, or a solvate thereof,
    wherein Ring A is a group represented by the formula:

    Ring B is optionally substituted heteroaryl, provided that optionally substituted isoxazole is excluded, or optionally substituted heterocycle,
    R 1 is hydrogen or optionally substituted alkyl,
    R 2 is -OR 5 , -SR 5 , halogen, halogenated alkyl or the like,
    R 3 is optionally substituted alkyl or the like,
    R 4 is optionally substituted alkyl or the like,
    R 5 is optionally substituted alkyl or the like,
    R 6 is hydrogen or the like,
    R 7 and R 8 are each independently hydrogen or the like,
    R 10 and R 11 are each independently hydrogen or the like,
    R 12 is optionally substituted alkyl or the like,
    m and p are each independently integer of 1 to 3.

    摘要翻译： 公开了可用作11β-羟基类固醇脱氢酶1型抑制剂的化合物。 由下式表示的化合物，其药学上可接受的盐或其溶剂化物，其中环A是由下式表示的基团：环B是任选取代的杂芳基，条件是排除任选取代的异唑或任选取代的杂环，R 1是氢或任选取代的烷基，R 2是-OR 5，-SR 5，卤素，卤代烷基等，R 3是任选取代的烷基等，R 4是任选取代的烷基等，R 5是 任选取代的烷基等，R 6为氢等，R 7和R 8各自独立地为氢等，R 10和R 11各自独立地为氢等，R 12为任选取代的烷基等 ，m和p各自独立地为1〜3的整数。

    BICYCLIC NITROGENATED HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
    9.
    发明公开
    BICYCLIC NITROGENATED HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME 审中-公开

    公开(公告)号：EP3527568A1

    公开(公告)日：2019-08-21

    申请号：EP17863024.0

    申请日：2017-10-16

    申请人： Shionogi & Co., Ltd

    发明人： MASUDA, Koji ,  SUGIYAMA, Shuichi ,  YAMADA, Toru ,  KOJIMA, Eiichi ,  OGAWA, Tomoyuki ,  KOBAYASHI, Naotake ,  KAI, Hiroyuki

    IPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/5383 ,  A61P43/00 ,  C07D487/04 ,  C07D498/04

    摘要： Provided are a novel compound having an antagonistic activity for the P2X 7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X 7 receptor. A compound represented by Formula (I):

    wherein Z 1 is C(R 4 ) or the like; R 4 is a hydrogen atom or the like; Z 2 is C(R 5a )(R 5a' ) or the like; the dashed line represents the presence or absence of a bond; when the dashed line represents the presence of a bond, then R 5a' is absent; R 5a and R 5a' are each independently a hydrogen atom or the like; Ring Q is a substituted or unsubstituted 5-membered non-aromatic heterocycle or the like; Y 1 is O or the like; R 2a is a group represented by the formula: -(C(R 2a' )(R 2b' )) n -R 1 ; R 2b is a hydrogen atom or the like; R 2a' and R 2b' is each independently a hydrogen atom or the like; R 1 is substituted or unsubstituted aromatic carbocyclyl or the like; X is N(R 7a ) or the like; R 7a is a hydrogen atom or the like; R 3 is substituted or unsubstituted aromatic carbocyclyl or the like; n is an integer from 0 to 4; and m is an integer from 0 to 4, or a pharmaceutically acceptable salt thereof.