公开(公告)号：EP0883622A1

公开(公告)日：1998-12-16

申请号：EP97903172.0

申请日：1997-02-26

申请人： APOTEX INC.

发明人： KARIMIAN, Khashayar ,  TAM, Tim, F. ,  DESILETS, Denis ,  LEE, Sue ,  CAPPELLETTO, Tullio ,  LI, Wanren

IPC分类号： A61K31 ,  A61P1 ,  A61P43 ,  C07D513

CPC分类号： C07D513/04

摘要： Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating peptic ulcers by inhibition of the proton pump enzyme H+/K+-ATPase. The compounds are 3-substituted 1,2,4-thiadiazole [4,5-a]benzimidazole and 3-substituted imidazo[1,2-d]-1,2,4-thiadiazoles corresponding to general formula (I) where X and Z either represented an optionally substituted benzene ring fused to the diazole nucleus, or represent a variety of independent chemical groupings (hydrogen, lower alkyl, halo, etc.) and Y is selected from a wide range, e.g. heterocyclics and carbonyl groups.

公开(公告)号：EP0883622B1

公开(公告)日：2002-05-15

申请号：EP97903172.1

申请日：1997-02-26

申请人： APOTEX INC.

发明人： KARIMIAN, Khashayar ,  TAM, Tim, F. ,  DESILETS, Denis ,  LEE, Sue ,  CAPPELLETTO, Tullio ,  LI, Wanren

IPC分类号： C07D513/04 ,  A61K31/415

CPC分类号： C07D513/04

摘要： Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating peptic ulcers by inhibition of the proton pump enzyme H+/K+-ATPase. The compounds are 3-substituted 1,2,4-thiadiazole [4,5-a]benzimidazole and 3-substituted imidazo[1,2-d]-1,2,4-thiadiazoles corresponding to general formula (I) where X and Z either represented an optionally substituted benzene ring fused to the diazole nucleus, or represent a variety of independent chemical groupings (hydrogen, lower alkyl, halo, etc.) and Y is selected from a wide range, e.g. heterocyclics and carbonyl groups.

公开(公告)号：EP0883606A1

公开(公告)日：1998-12-16

申请号：EP97903184.0

申请日：1997-02-26

申请人： APOTEX INC.

发明人： KARIMIAN, Khashayar ,  TAM, Tim, F. ,  DESILETS, Denis ,  LEE, Sue ,  CAPPELLETTO, Tullio ,  LI, Wanren

IPC分类号： A61K31 ,  A61P1 ,  A61P43 ,  C07C319 ,  C07C321 ,  C07D285 ,  C07D513

CPC分类号： C07D285/08 ,  C07C319/24 ,  C07C321/20 ,  C07C321/22

摘要： Thiols are trapped, and converted to disulfide compounds, by a process of reacting them with compounds containing a 1,2,4-thiadiazole ring structure carrying a substituent at position 3 of the thiadiazole ring, and being unsubstituted at position N-2. The process is useful pharmacologically, in inhibiting certain thiol-containing enzymes such as H+/K+-ATPase (the proton pump), and industrially, in selective removal of thiol compounds from gas or liquid mixtures.