公开(公告)号：EP2940013B1

公开(公告)日：2018-02-21

申请号：EP13868493.1

申请日：2013-12-27

申请人： UBE INDUSTRIES, LTD.

发明人： IWASE, Noriaki ,  NISHIDA, Hiroshi ,  OKUDO, Makoto ,  ITO, Masaaki ,  KONO, Shigeyuki ,  MATOYAMA, Masaaki ,  USHIYAMA, Shigeru ,  OKANARI, Eiji ,  MATSUNAGA, Hirofumi ,  NISHIKAWA, Kenji ,  KIMURA, Tomio

IPC分类号： C07D333/36 ,  A61K31/381 ,  A61K31/427 ,  A61K31/443 ,  A61P13/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D409/04 ,  C07D409/14 ,  C07D417/12

CPC分类号： C07D333/36 ,  A61K31/381 ,  A61K31/427 ,  A61K31/443 ,  A61P13/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

摘要： A novel ±-halogen-substituted thiophene compound or a pharmacologically acceptable salt thereof, which has a potent LPA receptor-antagonist activity and is useful as a medicament is provided. A compound represented by the general formula (I) wherein A represents, a phenyl ring, a thiophene ring, or an isothiazole ring; R 1 is the same or different, and represents a halogen atom, or a C 1 -C 3 alkyl group; R 2 represents a hydrogen atom, or a C 1 -C 6 alkyl group; p represents an integer of 0 to 5; V represents CR 3 wherein R 3 represents a hydrogen atom, an amino group, a nitro group, or a C 1 -C 3 alkoxy group, or V represents a nitrogen atom; and X represents a halogen atom, or a salt thereof.

公开(公告)号：EP2940013A1

公开(公告)日：2015-11-04

申请号：EP13868493.1

申请日：2013-12-27

申请人： UBE Industries, Ltd.

发明人： IWASE, Noriaki ,  NISHIDA, Hiroshi ,  OKUDO, Makoto ,  ITO, Masaaki ,  KONO, Shigeyuki ,  MATOYAMA, Masaaki ,  USHIYAMA, Shigeru ,  OKANARI, Eiji ,  MATSUNAGA, Hirofumi ,  NISHIKAWA, Kenji ,  KIMURA, Tomio

IPC分类号： C07D333/36 ,  A61K31/381 ,  A61K31/427 ,  A61K31/443 ,  A61P13/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D409/04 ,  C07D409/14 ,  C07D417/12

CPC分类号： C07D333/36 ,  A61K31/381 ,  A61K31/427 ,  A61K31/443 ,  A61P13/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

摘要： A novel α-halogen-substituted thiophene compound or a pharmacologically acceptable salt thereof, which has a potent LPA receptor-antagonist activity and is useful as a medicament is provided.
A compound represented by the general formula (I) wherein A represents, a phenyl ring, a thiophene ring, or an isothiazole ring; R 1 is the same or different, and represents a halogen atom, or a C 1 -C 3 alkyl group; R 2 represents a hydrogen atom, or a C 1 -C 6 alkyl group; p represents an integer of 0 to 5; V represents CR 3 wherein R 3 represents a hydrogen atom, an amino group, a nitro group, or a C 1 -C 3 alkoxy group, or V represents a nitrogen atom; and X represents a halogen atom, or a salt thereof.

摘要翻译： 提供了一种具有有效的LPA受体 - 拮抗剂活性并可用作药物的新型的 - - 卤素取代的噻吩化合物或其药学上可接受的盐。 由通式（I）表示的化合物，其中A表示苯基环，噻吩环或异噻唑环; R 1相同或不同，表示卤素原子或C 1〜C 3烷基; R 2表示氢原子或C 1 -C 6烷基; p表示0〜5的整数， V表示CR 3，其中R 3表示氢原子，氨基，硝基或C 1 -C 3烷氧基，或V表示氮原子; X表示卤素原子或其盐。

公开(公告)号：EP3162801B1

公开(公告)日：2020-07-22

申请号：EP15812460.2

申请日：2015-06-26

申请人： UBE Industries, Ltd.

发明人： IWASE, Noriaki ,  NISHIDA, Hiroshi ,  OKUDO, Makoto ,  ITO, Masaaki ,  KONO, Shigeyuki ,  MATOYAMA, Masaaki ,  USHIYAMA, Shigeru ,  OKANARI, Eiji ,  MATSUNAGA, Hirofumi ,  NISHIKAWA, Kenji ,  KIMURA, Tomio

IPC分类号： C07D333/36 ,  A61K31/381 ,  A61P13/00 ,  A61P19/04 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00

公开(公告)号：EP3378491A1

公开(公告)日：2018-09-26

申请号：EP16866430.8

申请日：2016-11-18

申请人： UBE Industries, Ltd.

发明人： NISHIKAWA, Kenji ,  MATSUNAGA, Hirofumi ,  SHINOHARA, Yuuko ,  OKANARI, Eiji ,  USHIYAMA, Shigeru ,  NONOUCHI, Shinpei

IPC分类号： A61K45/00 ,  A61K31/381 ,  A61P1/16 ,  A61P43/00 ,  C07D333/36

CPC分类号： A61K31/381 ,  A61K45/00 ,  C07D333/36

摘要： The present invention provides the pharmaceutical use of LPA1 antagonists, for example, α-halogenated thiophene compounds having a specific structure or pharmacologically acceptable salts thereof, as drugs for the treatment and/or prevention of NASH.
A pharmaceutical composition for the treatment and/or prevention of NASH includes, as an active ingredient, an LPA1 antagonist, for example, a compound represented by the general formula (I):

wherein R 1 is a hydrogen atom or a methoxy group, R 2 is a hydrogen atom or a C 1 -C 6 alkyl group, X is a halogen atom, and A is a group selected from the group consisting of groups:

, or a pharmacologically acceptable salt thereof.