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。

公开(公告)号：EP2832729A1

公开(公告)日：2015-02-04

申请号：EP13769121.8

申请日：2013-03-29

申请人： Shionogi & Co., Ltd.

发明人： KITAMURA, Hideyuki ,  GODA, Satoshi ,  YAMAMOTO, Mitsuru

IPC分类号： C07D263/32 ,  C07B61/00

CPC分类号： C07D263/32

摘要： The present invention provides the salt and the crystal thereof of 2-(oxazole-2-yl)phenol derivative which are the intermediate in the process of producing N-phenyl-N'-phenylsulfonyl piperazine derivative, and the process of producing the salt as well as the process of producing N-phenyl-N'-phenylsulfonyl piperazine derivative through the salt.
A method of producing the salt and the crystal thereof of the compound represented by Formula(I):

wherein X is halogen;
and the process of producing the salt as well as the process of producing N-phenyl-N'-phenylsulfonyl piperazine derivative through the salt.

摘要翻译： 本发明提供作为制备N-苯基-N'-苯磺酰基哌嗪衍生物的方法中的中间体2-（恶唑-2-基）苯酚衍生物的盐及其晶体，以及将该盐制备为 以及通过盐制备N-苯基-N'-苯磺酰基哌嗪衍生物的方法。 由式（I）表示的化合物的盐及其晶体的制备方法：其中X是卤素; 以及生产盐的方法以及通过盐生产N-苯基-N'-苯磺酰基哌嗪衍生物的方法。