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公开(公告)号：EP2057139B1
公开(公告)日：2013-09-04
申请号：EP07763931.8
申请日：2007-07-18
IPC分类号： C07C219/14 , C07C327/48 , C07D209/18 , C07D209/32 , C07D309/30 , C07D339/04 , C07D409/12 , A61K31/385 , A61P29/00
CPC分类号： C07C327/48 , C07C219/14 , C07D209/18 , C07D209/32 , C07D309/30 , C07D339/04 , C07D409/12
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公开(公告)号：EP2057139A1
公开(公告)日：2009-05-13
申请号：EP07763931.8
申请日：2007-07-18
IPC分类号： C07D339/04 , A61K31/385 , A61P29/00 , C07C327/48 , C07C331/28 , C07D209/28
CPC分类号： C07C327/48 , C07C219/14 , C07D209/18 , C07D209/32 , C07D309/30 , C07D339/04 , C07D409/12
摘要： The present invention relates to derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) having improved anti-inflammatory properties useful in the treatment of inflammation, pain and fever. More particularly, NSAIDs are derivatized with a hydrogen sulfide (H2S) releasing moiety to produce novel anti-inflammatory compounds having reduced side effects.
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公开(公告)号：EP1883645B1
公开(公告)日：2011-06-29
申请号：EP06721742.2
申请日：2006-03-31
发明人： WALLACE, John L. , SPARATORE, Anna , CIRINO, Giuseppe , CALIENDO, Giuseppe , SANTAGADA, Vincenzo , FIORUCCI, Stefano
IPC分类号： C07F9/6578 , C07D339/04 , A61K31/16 , A61K31/27 , A61K31/255 , C07C333/02 , C07C327/40 , C07C321/14 , A61K31/325 , A61P1/00
CPC分类号： C07C327/42 , C07C323/12 , C07C323/59 , C07C323/60 , C07C327/48 , C07D339/04 , C07F9/6578 , C07F9/6587
摘要： The present invention provides new derivatives of 4-or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4-or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4-or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.
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公开(公告)号：EP2041108A1
公开(公告)日：2009-04-01
申请号：EP07763921.9
申请日：2007-07-18
IPC分类号： C07D309/30 , C07C327/48
CPC分类号： C07C327/48 , C07C219/14 , C07D209/18 , C07D209/32 , C07D309/30 , C07D339/04 , C07D409/12
摘要： Derivatives of drugs are provided, said derivatives comprising the H2S-releasing moiety 4-hydroxythiobenzamide that is either covalently linked to the drug or forms a salt with the drug. The compounds of the present invention exhibit enhanced activity or reduced side effects or both.
摘要翻译： 提供了药物衍生物，所述衍生物包含H2S释放部分4-羟基硫代苯甲酰胺，其与药物共价连接或与药物形成盐。 本发明的化合物表现出增强的活性或降低的副作用或两者。
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公开(公告)号：EP2024323A1
公开(公告)日：2009-02-18
申请号：EP07719924.8
申请日：2007-06-06
IPC分类号： C07C219/14 , A61K31/24 , A61P29/00 , C07C213/08 , C07C327/48 , C07D339/04
CPC分类号： C07C279/32 , C07C219/22 , C07C323/60 , C07C327/48 , C07D339/04
摘要： Unique salts of trimebutine and N-monodesmethyl trimebutine, and their corresponding stereoisomers, having improved analgesic properties useful in the treatment of visceral pain are provided. The salts of the present invention are particularly useful in the treatment of conditions characterized by abdominal pain, such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS), diabetic gastroparesis, and dyspepsia.
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公开(公告)号：EP1883645A1
公开(公告)日：2008-02-06
申请号：EP06721742.2
申请日：2006-03-31
发明人： WALLACE, John L. , SPARATORE, Anna , CIRINO, Giuseppe , CALIENDO, Giuseppe , SANTAGADA, Vincenzo , FIORUCCI, Stefano
IPC分类号： C07F9/6578 , C07D339/04 , A61K31/16 , A61K31/27 , A61K31/255 , C07C333/02 , C07C327/40 , C07C321/14 , A61K31/325
CPC分类号： C07C327/42 , C07C323/12 , C07C323/59 , C07C323/60 , C07C327/48 , C07D339/04 , C07F9/6578 , C07F9/6587
摘要： The present invention provides new derivatives of 4-or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4-or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4-or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.
摘要翻译： 本发明提供4-或5-氨基水杨酸的新衍生物和含有这些4-或5-氨基水杨酸衍生物作为活性成分的药物组合物，其可用于治疗肠道疾病如炎症性肠病（IBD）和 肠易激综合征（IBS）和结肠癌的预防/治疗。 更特别地，这些衍生物包含通过偶氮，酯，酸酐，硫酯或酰胺键与4-或5-氨基水杨酸分子连接的硫化氢释放部分。 此外，本发明提供了制备这些化合物的方法及其用于治疗IBD和IBS以及预防/治疗结肠癌的用途。
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公开(公告)号：EP1751096A2
公开(公告)日：2007-02-14
申请号：EP05748584.9
申请日：2005-05-27
IPC分类号： C07C279/00
CPC分类号： C07C279/14 , C07C229/64
摘要： The present invention provides L-arginine salts of 4-ammosalicylic acid and 5-ammosalicylic acid (mesalamine) Pharmaceutical compositions containing these L-argmme salts are useful for the treatment of inflammatory conditions of the gastrointestinal (GI) tract such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) The compositions may be used to treat Crohn's disease, gastritis, celiac disease, peptic ulcer disease, inflammatory conditions of the mouth and esophagus, pre-cancerous lesions of the stomach, non-ulcer dyspepsia, bacterial overgrowth, peptic ulcer disease, fissures of the intestine, ulcerative colitis, infectious colitis, precancerous conditions of the colon, proctitis, inflammation associated with hemorrhoids, protalgia fugax, rectal fissures, and liver gallbladder and/or bilary tract conditions.
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