公开(公告)号：EP3026054B1

公开(公告)日：2019-03-06

申请号：EP14829168.5

申请日：2014-07-18

申请人： Eisai R&D Management Co., Ltd.

发明人： TANAKA, Keigo ,  FUKUYAMA, Takashi ,  MURAI, Norio ,  ITANO, Wataru ,  HIROTA, Shinsuke ,  IIDA, Daisuke ,  AZUMA, Hiroshi

IPC分类号： C07D491/048 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F7/22 ,  A61K31/34 ,  A61K31/381 ,  A61K31/407 ,  A61K31/429 ,  A61K31/4355 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519 ,  A61P1/04 ,  A61P9/10 ,  A61P31/10 ,  C07B61/00

公开(公告)号：EP2065379A1

公开(公告)日：2009-06-03

申请号：EP07829601.9

申请日：2007-10-11

申请人： Eisai R&D Management Co., Ltd.

发明人： UEDA, Masato ,  IIDA, Daisuke ,  KIKUCHI, Sachiko ,  GOTODA, Masaharu

IPC分类号： C07D401/12 ,  A61K31/4439 ,  A61K31/549 ,  A61P1/04 ,  A61P31/04 ,  A61P43/00 ,  C07D405/14 ,  C07D493/10 ,  C07D513/14 ,  C07D519/00

CPC分类号： C07D401/12 ,  C07D405/14 ,  C07D493/10 ,  C07D513/14 ,  C07D519/00

摘要： The present invention provides a compound that has superior gastric acid secretion inhibitory action, ample long-lasting gastric acid secretion inhibitory action, and is able to maintain intragastric pH at a high level for an extended period of time, making it useful as a therapeutic or prophylactic agent for diseases or symptoms caused by gastric acid, as well as an active form of this compound (form to which the compound is converted in the body following administration thereof) in the form of a compound represented by general formula (1 a) (wherein R2 represents a group represented by formula (I) or the like, and R1, R3, W1 and X - are as defined in the description).

摘要翻译： 本发明提供了具有优良的胃酸分泌抑制作用，充足的持久胃酸分泌抑制作用的化合物，能够将胃内pH保持在高水平长时间，使其成为治疗性或 由胃酸引起的疾病或症状的预防剂以及该化合物的活性形式（化合物在给药后在体内转化的形式）以通式（1a）表示的化合物的形式（ 其中R 2表示由式（I）等表示的基团，R 1，R 3，W 1和X - 如说明书中所定义）。

公开(公告)号：EP3026054A1

公开(公告)日：2016-06-01

申请号：EP14829168.5

申请日：2014-07-18

申请人： Eisai R&D Management Co., Ltd.

发明人： TANAKA, Keigo ,  FUKUYAMA, Takashi ,  MURAI, Norio ,  ITANO, Wataru ,  HIROTA, Shinsuke ,  IIDA, Daisuke ,  AZUMA, Hiroshi

IPC分类号： C07D491/048 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F7/22 ,  A61K31/34 ,  A61K31/381 ,  A61K31/407 ,  A61K31/429 ,  A61K31/4355 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519 ,  A61P1/04 ,  A61P9/10 ,  A61P31/10 ,  C07B61/00

CPC分类号： C07F7/2208 ,  C07D491/048 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F5/025 ,  C07F5/027

摘要： A compound represented by the formula (I) or a salt thereof:

wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; X 1 is a hydrogen atom, a hydroxy group, a hydroxy C 1-6 alkyl group, -B(OH) 2 , a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, -BF 3 M n1 , -Sn(R 12 )(R 13 )(R 14 ), a leaving group, a carboxy group, a formyl group, or -NR 16 R 17 ; and X 2 is a hydrogen atom or -CO 2 R 18 .

摘要翻译： 由式（I）表示的化合物或其盐：其中环Z是环中具有一个或两个杂原子的5至6元杂芳环; X 1为氢原子，羟基，羟基C 1-6烷基，-B（OH）2，硼酸酯基，环状硼酸酯基，硼烷基，环状硼烷基，-BF 3 M n1，-Sn（R 12）（R 13）（R 14），离去基团，羧基，甲酰基或-NR 16 R 17; X 2为氢原子或-CO 2 R 18。

公开(公告)号：EP1439175B1

公开(公告)日：2011-04-27

申请号：EP02802050.1

申请日：2002-10-22

申请人： Eisai R&D Management Co., Ltd.

发明人： HARADA, Hitoshi ,  ASANO, Osamu ,  UEDA, Masato ,  MIYAZAWA, Shuhei ,  KOTAKE, Yoshihiko ,  KABASAWA, Yasuhiro ,  YASUDA, Masahiro ,  YASUDA, Nobuyuki ,  IIDA, Daisuke ,  NAGAKAWA, Junichi ,  HIROTA, Kazuo ,  NAKAGAWA, Makoto

IPC分类号： C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  A61K31/506 ,  A61P1/00 ,  A61P1/10 ,  A61P3/04 ,  A61P3/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/02 ,  A61P19/10 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00

CPC分类号： C07D405/14 ,  A61K31/506 ,  C07D401/04 ,  C07D409/14

摘要： A novel pyrimidine compound having an excellent antagonistic activity against adenosine receptors (A1, A2A, and A2B receptors). Specifically, it is a compound represented by the following formula, a salt of the compound, or a solvate of either. (I) In the formula, R1 and R2 are the same or different and each represents hydrogen, optionally substituted C1-6 alkyl, etc.; R3 represents hydrogen, halogeno, etc.; R4 represents an optionally substituted C6-14 aromatic hydrocarbon ring group, optionally substituted 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond, etc.; and R5 represents an optionally substituted C6-14 aromatic hydrocarbon ring group or optionally substituted 5- to 14-membered aromatic heterocyclic group.