公开(公告)号：EP2128134A1

公开(公告)日：2009-12-02

申请号：EP07830926.7

申请日：2007-10-31

申请人： Shionogi&Co., Ltd.

发明人： ENDOH, Takeshi ,  FUJII, Yasuhiko ,  KOJIMA, Eiichi ,  TADANO, Genta ,  YAMAGUCHI, Naoko ,  ADACHI, Yo ,  TAGASHIRA, Sachie ,  TACHIBANA, Yuki ,  ONODERA, Naohiro

IPC分类号： C07D209/08 ,  A61K31/4418 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/02 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D209/86 ,  C07D211/96 ,  C07D213/81 ,  C07D215/20

CPC分类号： C07D209/86 ,  C07D211/96 ,  C07D213/81 ,  C07D215/20 ,  C07D241/04 ,  C07D243/08 ,  C07D263/32 ,  C07D277/28 ,  C07D295/22 ,  C07D295/26 ,  C07D307/81 ,  C07D307/91

摘要： A compound represented by the general formula (I):

wherein R 1 is

wherein R 26 and R 28 are each independently lower alkyloxy and the like; n 1 is an integer of 0 to 3; Z is a optionally substituted C1-C5 alkynylene which may be interrupted with a substituent selected from Substituent group a and the like; A is a group represented by the formula:

wherein R 6 and R 7 are each independently lower alkyl and the like; m and n are each independently 0, 1, or 2; R 2 is a hydrogen atom and the like; R 3 is optionally substituted lower alkyl and the like; R 4 is a hydrogen atom; or R 3 and R 4 may be taken together with an adjacent carbon atom to from a ring; R 5 is hydroxyl and the like, or an optically active isomer, a pharmaceutically acceptable salt or a solvate thereof.

摘要翻译： 由通式（I）表示的化合物：其中R 1是其中R 26和R 28各自独立地为低级烷氧基等; n 1为0〜3的整数， Z是可以被选自取代基组a等的取代基中断的任选取代的C 1 -C 5亚炔基; A是由下式表示的基团：其中R 6和R 7各自独立地为低级烷基等; m和n各自独立地为0,1或2; R 2是氢原子等; R 3是任选取代的低级烷基等; R 4是氢原子; 或R 3和R 4可以与相邻的碳原子一起与环一起取代; R 5是羟基等，或光学活性异构体，其药学上可接受的盐或溶剂化物。

公开(公告)号：EP1939175A1

公开(公告)日：2008-07-02

申请号：EP06810485.0

申请日：2006-09-25

申请人： Shionogi&Co., Ltd.

发明人： KUGIMIYA, Akira ,  FUJIOKA, Masahiko ,  TACHIBANA, Yuki ,  MURASHI, Takami ,  ONODERA, Naohiro

IPC分类号： C07D207/48 ,  A61K31/40 ,  A61K31/445 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61P11/06 ,  A61P37/08 ,  A61P43/00 ,  C07D207/14 ,  C07D211/58 ,  C07D211/70 ,  C07D211/96 ,  C07D213/38 ,  C07D213/71 ,  C07D213/74 ,  C07D231/12 ,  C07D235/08 ,  C07D235/32

CPC分类号： C07D295/26 ,  C07D207/14 ,  C07D207/48 ,  C07D211/58 ,  C07D211/70 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/64 ,  C07D213/71 ,  C07D213/74 ,  C07D231/12 ,  C07D231/40 ,  C07D235/08 ,  C07D235/30 ,  C07D235/32 ,  C07D243/08 ,  C07D261/08 ,  C07D261/18 ,  C07D263/32 ,  C07D263/58 ,  C07D265/36 ,  C07D271/10 ,  C07D277/24 ,  C07D277/28 ,  C07D285/12 ,  C07D285/135 ,  C07D295/096 ,  C07D295/155 ,  C07D307/42 ,  C07D307/52 ,  C07D307/56 ,  C07D307/68 ,  C07D333/36 ,  C07D401/12 ,  C07D413/12

摘要： The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.
A compound of the general formula (II):

wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.;
a pharmaceutically acceptable salt or a hydrate thereof.

公开(公告)号：EP3394042A1

公开(公告)日：2018-10-31

申请号：EP16826192.3

申请日：2016-12-22

申请人： Shionogi & Co., Ltd

发明人： ONODERA, Naohiro ,  NOGUCHI, Kouichi ,  ANDO, Shigeru ,  NAGAMATSU, Daiki ,  ISHIBASHI, Kenichi ,  OCHI, Shunsuke ,  HASEGAWA, Aiko ,  ODA, Katsuo

IPC分类号： C07D279/06 ,  C07D417/12

CPC分类号： C07D279/06 ,  C07D417/12

摘要： The present invention provides a process for preparation of the compound of formula (VI), wherein each symbol is as defined in the specification, without using any intermediate compound showing mutagenicity. The process comprises salt formation of the intermediate compound of formula (I) with acid to enable optical resolution to isolate the intermediate compound of formula (II) in a stereo-selective manner.

公开(公告)号：EP1939175B1

公开(公告)日：2017-03-01

申请号：EP06810485.0

申请日：2006-09-25

申请人： Shionogi & Co., Ltd.

发明人： KUGIMIYA, Akira ,  FUJIOKA, Masahiko ,  TACHIBANA, Yuki ,  MURASHI, Takami ,  ONODERA, Naohiro

IPC分类号： C07D207/48 ,  C07D207/14 ,  A61K31/40 ,  A61K31/445 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61P11/06 ,  A61P37/08 ,  A61P43/00

CPC分类号： C07D295/26 ,  C07D207/14 ,  C07D207/48 ,  C07D211/58 ,  C07D211/70 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/64 ,  C07D213/71 ,  C07D213/74 ,  C07D231/12 ,  C07D231/40 ,  C07D235/08 ,  C07D235/30 ,  C07D235/32 ,  C07D243/08 ,  C07D261/08 ,  C07D261/18 ,  C07D263/32 ,  C07D263/58 ,  C07D265/36 ,  C07D271/10 ,  C07D277/24 ,  C07D277/28 ,  C07D285/12 ,  C07D285/135 ,  C07D295/096 ,  C07D295/155 ,  C07D307/42 ,  C07D307/52 ,  C07D307/56 ,  C07D307/68 ,  C07D333/36 ,  C07D401/12 ,  C07D413/12

公开(公告)号：EP2703399A1

公开(公告)日：2014-03-05

申请号：EP12777494.1

申请日：2012-04-25

申请人： Shionogi & Co., Ltd.

发明人： MASUI, Moriyasu ,  MITSUOKA, Yasunori ,  YOSHIDA, Syuhei ,  KUSAKABE, Ken-ichi ,  ONODERA, Naohiro ,  KUROSE, Noriyuki

IPC分类号： C07D413/12 ,  A61K31/5355 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00

CPC分类号： C07D413/14 ,  C07D413/12

摘要： The present invention provides a compound of formula (I):

wherein
-X= is -CR 7 = or -N=,
ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle,
R 1 is substituted or unsubstituted alkyl or the like,
R 2a and R 2b are each independently hydrogen, substituted or unsubstituted alkyl or the like,
R 3 and R 4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like,
R 5 is hydrogen, substituted or unsubstituted alkyl or the like,
each R 6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R 7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like,
p is an integer of 0 to 3,
or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins.

摘要翻译： 本发明提供式（I）化合物：其中-X =为-CR 7 =或-N =，环B为取代或未取代的碳环或取代或未取代的杂环，R 1为取代或未取代的烷基或 R 2a和R 2b各自独立地为氢，取代或未取代的烷基等，R 3和R 4各自独立地为氢，卤素，取代或未取代的烷基等，R 5为氢，取代或未取代的烷基或 每个R 6独立地为卤素，羟基，取代或未取代的烷基等，R 7为氢，卤素，羟基，取代或未取代的烷基等，p为0〜3的整数，或药学上可接受的 其具有抑制淀粉样蛋白²产生的作用，特别是抑制BACE1的作用，并且其可用作由淀粉样蛋白²蛋白质的产生，分泌和/或沉积诱导的疾病的治疗或预防剂。