公开(公告)号：EP0580378B1

公开(公告)日：1996-06-26

申请号：EP93305630.1

申请日：1993-07-19

申请人： SHIONOGI & CO., LTD.

发明人： Matsutani, Shigeru ,  Yoshida, Tadashi ,  Sakazaki, Ryuji ,  Fujii, Yasuhiko ,  Tanaka, Kazushige

IPC分类号： C07C69/92 ,  C07C229/38 ,  C07C271/20 ,  A61K31/235

CPC分类号： C07C271/22 ,  C07C69/92 ,  C07C229/38

公开(公告)号：EP3957627A1

公开(公告)日：2022-02-23

申请号：EP21196697.3

申请日：2016-04-22

申请人： Shionogi & Co., Ltd

发明人： Tanaka, Satoru ,  Ogawa, Tomoyuki ,  Kai, Hiroyuki ,  Ogata, Yuki ,  Hirai, Keiichiro ,  Kurose, Noriyuki ,  Fujii, Yasuhiko

IPC分类号： C07D213/69 ,  A61K31/4412 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61P1/02 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P13/00 ,  A61P13/08 ,  A61P13/10 ,  A61P13/12 ,  A61P17/02

摘要： A compound for use as P2X7 antagonist represented by Formula (I):

wherein

or the like
Y 1 is O or the like; Z 1 is C(R 4 ) or N; Z 2a is C(R 5a ) or the like; Z 3a is C(R 6 ) or the like;
R 4 , R 5a and R 6 are each independently a hydrogen atom or the like; R 1 is substituted or unsubstituted aromatic carbocyclyl or the like; R 2a , R 2b , R 2c and R 2d are each independently a hydrogen atom or the like; X is N(R 7a ) or the like; R 7a is a hydrogen atom or the like; R 3 is

or the like
Ring B is a 6-membered aromatic carbocycle or the like; R 9a and R 10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p1 is an integer from 0 to 3,
or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP0580378A1

公开(公告)日：1994-01-26

申请号：EP93305630.1

申请日：1993-07-19

申请人： SHIONOGI & CO., LTD.

发明人： Matsutani, Shigeru ,  Yoshida, Tadashi ,  Sakazaki, Ryuji ,  Fujii, Yasuhiko ,  Tanaka, Kazushige

IPC分类号： C07C69/92 ,  C07C229/38 ,  C07C271/20 ,  A61K31/235

CPC分类号： C07C271/22 ,  C07C69/92 ,  C07C229/38

摘要： The present invention relates to the compounds of the formula:

in which R¹, R², R³, R⁴, R⁵, R⁶, R⁷, and R⁸ are independently hydrogen, lower alkyl which is optionally substituted, lower alkoxy which is optionally substituted, hydroxy, acyloxy, or halogen; R⁹ is hydrogen, hydroxy, acyloxy, lower alkyl which is optionally substituted, lower alkoxy which is optionally substituted, or lower alkylamino which is optionally substituted; E¹ is hydrogen, or an ester residue; m is an integer of from 1 to 4;
or a pharmaceutically acceptable salt thereof. The compounds of the present invention exhibit phospholipase A₂ inhibitory activity, and can be used in treating inflammatory conditions.

摘要翻译： 本发明涉及下式的化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7， R 8独立地为氢，任选取代的低级烷基，任选取代的低级烷氧基，羟基，酰氧基或卤素; R 9是氢，羟基，酰氧基，任选被取代的低级烷基，任选被取代的低级烷氧基或任选取代的低级烷基氨基; E 1是氢或酯残基; m为1〜4的整数， 或其药学上可接受的盐。 本发明化合物表现出磷脂酶A2抑制活性，可用于治疗炎性病症。