公开(公告)号：EP0924207A4

公开(公告)日：2001-06-13

申请号：EP97935855

申请日：1997-08-22

申请人： SHIONOGI & CO

发明人： ISHIZUKA NATSUKI ,  MATSUMURA KEN-ICHI ,  SAKAI KATSUNORI ,  KONOIKE TOSHIRO ,  YORIFUJI TADAHIKO ,  HARA SEIJIRO ,  MATSUO YOSHIYUKI

IPC分类号： C07D311/22 ,  C07D311/60 ,  C07D407/04 ,  C07D407/14 ,  C07D409/04 ,  C07D409/14 ,  C07D311/58 ,  C07D311/64 ,  C07D311/68 ,  C07D335/06 ,  C07D407/12 ,  A61K31/352

CPC分类号： C07D407/04 ,  C07D311/60 ,  C07D407/14 ,  C07D409/04 ,  C07D409/14

摘要： Compounds represented by general formula (I), pharmaceutically acceptable salts thereof, and hydrates of the same; and medicinal compositions such as endothelin receptor antagonists, remedies for peripheral circulatory insufficiency or macrophage foaming inhibitors containing these compounds. In said formula (I), R?1, R2, R3 and R4¿ independently represent each hydrogen, optionally substituted alkyl, hydroxy, optionally substituted alkoxy, etc.; R5 represents optionally substituted alkyl, optionally substituted aryl, optionally substituted heterocycle, etc.; R6 represents hydrogen, optionally substituted alkyl, etc.; R7 represents hydrogen, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heterocycle, etc.; A represents S or O; and the broken line means the presence or absence of a bond.

公开(公告)号：EP1057824A4

公开(公告)日：2002-01-09

申请号：EP99902911

申请日：1999-02-16

申请人： SHIONOGI & CO

发明人： KONOIKE TOSHIRO ,  YORIFUJI TADAHIKO ,  SHINOMOTO SHOJI ,  IDE YUTAKA ,  OHYA TAKASHI ,  MATSUMURA KEN-ICHI

IPC分类号： C07D311/30 ,  C07D407/04 ,  A61K31/35 ,  A61K31/36 ,  A61K31/38 ,  C07B57/00 ,  C07D335/06 ,  C07D409/04

CPC分类号： C07D407/04 ,  C07D311/30 ,  Y02P20/582

摘要： A process for producing a compound represented by formula (II) (wherein R?1, R2, R3, and R4¿ each independently represents hydrogen, alkyl, alkoxy, etc.; R5 represents alkyl or alkoxyalkyl; A represents O or S; Ar represents aryl, etc.; * indicates the position of an asymmetric carbon atom and that the compound is the (R) or (S) isomer; and Q represents an optically active reagent), characterized by isolating the target compound as crystals from a solution or suspension containing a compound represented by formula (II) (wherein * indicates the position of an asymmetric carbon atom and that the compound is the (R) or (S) isomer or is a mixture of both, and the other symbols have the same meanings as the above).

公开(公告)号：EP1283210A4

公开(公告)日：2003-08-06

申请号：EP01921842

申请日：2001-04-16

申请人： SHIONOGI & CO

发明人： KONOIKE TOSHIRO ,  OKUYAMA AKIRA ,  MASUI YOSHIYUKI ,  SAKATA TERUO

IPC分类号： A61K31/405 ,  A61P29/00 ,  A61P43/00 ,  C07D409/12

CPC分类号： C07D409/12 ,  A61K31/405

摘要： A process for the preparation of compound (I'): which is characterized by reacting in a solvent a compound of the general formula (III): (wherein X is halogeno) with p-tolylacetylene, a cuprous salt, a catalyst, and a base, and then treating the resulting reaction mixture with an acid.

摘要翻译： 一种制备化合物（1'）的方法：其特征在于在溶剂中使通式（III）的化合物：其中X为卤素的化合物与对甲苯基乙炔，亚铜盐，催化剂和 碱，然后用酸处理得到的反应混合物。

公开(公告)号：EP1072588A4

公开(公告)日：2001-07-18

申请号：EP99913673

申请日：1999-04-15

申请人： SHIONOGI & CO

发明人： AOKI TSUTOMU ,  KONOIKE TOSHIRO

IPC分类号： C07C313/08 ,  C07C319/14 ,  C07C323/09 ,  C07D233/84 ,  C07D401/06 ,  B01J31/02 ,  C07C321/28 ,  C07C323/62

CPC分类号： C07D401/06 ,  C07C313/08 ,  C07C319/14 ,  C07C323/09 ,  C07D233/84

摘要： A process for producing a compound represented by formula (I) which comprises reacting a compound represented by formula (V) with a compound represented by formula (VI) in the presence of a base; a process for producing a compound represented by formula (II) which comprises causing a halogenating agent to act on the compound represented by formula (I); a process for producing a compound represented by formula (IV) which comprises reacting the compound represented by formula (II) with a compound represented by formula (III); and the compound represented by formula (I), wherein Alk represents branched alkyl; Hal1 and Hal2 each represents halogeno; R?1 and R2¿ each independently represents halogeno, alkyl, alkoxy, nitro, and cyano; R?3 and R5¿ each represents hydrogen or an organic residue; and R4 represents an organic residue.

摘要翻译： （I）表示的化合物的制备方法，其包括在碱的存在下使式（V）所示的化合物与式（VI）所示的化合物反应; （II）表示的化合物的制备方法，其包括使卤化剂作用于式（I）表示的化合物; （IV）所示化合物的制备方法，其包括使式（II）所示化合物与式（III）所示化合物反应; 和由式（I）表示的化合物，其中Alk表示支链烷基; Hal1和Hal2各自代表卤代; R 1和R 2各自独立地表示卤代，烷基，烷氧基，硝基和氰基; R 3和R 5各自代表氢或有机残基; 和R4代表有机残基。

公开(公告)号：EP1767538A4

公开(公告)日：2010-04-28

申请号：EP05734618

申请日：2005-04-20

申请人： SHIONOGI & CO

发明人： KONOIKE TOSHIRO

IPC分类号： C07D498/04 ,  C07D505/06 ,  C07D505/00 ,  C07D505/18

CPC分类号： C07D505/00 ,  Y02P20/55

公开(公告)号：EP0739903A4

公开(公告)日：1998-07-08

申请号：EP95907849

申请日：1995-02-07

申请人： SHIONOGI & CO

发明人： HAGISHITA SANJI ,  KAMATA SUSUMU ,  MURAKAMI YASUSHI ,  HAGA NOBUHIRO ,  ISHIHARA YASUNOBU ,  KONOIKE TOSHIRO

IPC分类号： A61K31/17 ,  A61K38/00 ,  A61K38/05 ,  A61P1/04 ,  C07C275/28 ,  C07K5/06 ,  C07K5/062

CPC分类号： C07K5/0606 ,  A61K38/00 ,  C07C275/28 ,  C07K5/06026 ,  C07K5/06139

摘要： A compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, having a strong affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors and hence being useful for curing diseases related to gastrin receptors and/or CCK-B receptors without inducing side effect related to CCK-A receptors, wherein R1 represents hydrogen or lower alkyl; R2 represents lower alkoxy, lower alkylamino, lower cycloalkyl, optionally substituted phenyl or optionally substituted heterocycle; R3 represents optionally substituted phenyl; and R4 represents optionally substituted phenyl, optionally substituted cycloalkyl, optionally substituted alkyl or optionally substituted heterocycle.

摘要翻译： 由通式（I）表示的化合物或其药学上可接受的盐对胃泌素受体和/或CCK-B受体具有强亲和力，但对CCK-A受体不具有强亲和力，因此可用于治疗与胃泌素受体和/ 或CCK-B受体而不诱导与CCK-A受体有关的副作用，其中R1代表氢或低级烷基; R2代表低级烷氧基，低级烷基氨基，低级环烷基，任选取代的苯基或任选取代的杂环; R3代表任选取代的苯基; 并且R4代表任选取代的苯基，任选取代的环烷基，任选取代的烷基或任选取代的杂环。