公开(公告)号：US20110130368A1

公开(公告)日：2011-06-02

申请号：US12980985

申请日：2010-12-29

申请人： JOHN L. WALLACE ,  VINCENZO SANTAGADA ,  STEFANO FIORUCCI ,  GIUSEPPE CIRINO ,  GIUSEPPE CALIENDO ,  ANNA SPARATORE

发明人： JOHN L. WALLACE ,  VINCENZO SANTAGADA ,  STEFANO FIORUCCI ,  GIUSEPPE CIRINO ,  GIUSEPPE CALIENDO ,  ANNA SPARATORE

IPC分类号： A61K31/625 ,  A61P1/00 ,  A61P1/04 ,  A61P35/00 ,  A61K31/655

CPC分类号： C07C323/59 ,  C07C323/60 ,  C07C327/42 ,  C07C327/48 ,  C07D339/04 ,  C07F9/3895 ,  C07F9/65785

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.

公开(公告)号：US20110098257A1

公开(公告)日：2011-04-28

申请号：US12981008

申请日：2010-12-29

申请人： JOHN L. WALLACE ,  GIUSEPPE CIRINO ,  GIUSEPPE CALIENDO ,  ANNA SPARATORE ,  VINCENZO SANTAGADA ,  STEFANO FIORUCCI

发明人： JOHN L. WALLACE ,  GIUSEPPE CIRINO ,  GIUSEPPE CALIENDO ,  ANNA SPARATORE ,  VINCENZO SANTAGADA ,  STEFANO FIORUCCI

IPC分类号： A61K31/625 ,  A61P35/00 ,  A61P29/00 ,  A61P1/04

CPC分类号： C07C323/59 ,  C07C323/60 ,  C07C327/42 ,  C07C327/48 ,  C07D339/04 ,  C07F9/3895 ,  C07F9/65785

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，其可用于治疗肠疾病如炎性肠病（IBD）和 肠易激综合征（IBS）和预防/治疗结肠癌。 更具体地说，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。

公开(公告)号：US20080004245A1

公开(公告)日：2008-01-03

申请号：US11779849

申请日：2007-07-18

申请人： JOHN WALLACE ,  GIUSEPPE CIRINO ,  VINCENZO SANTAGADA ,  GIUSEPPE CALIENDO

发明人： JOHN WALLACE ,  GIUSEPPE CIRINO ,  VINCENZO SANTAGADA ,  GIUSEPPE CALIENDO

IPC分类号： A61K31/385 ,  C07D409/02 ,  A61K31/405 ,  A61K31/60

CPC分类号： C07C219/14 ,  C07C327/48 ,  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.

摘要翻译： 本发明涉及具有改善抗炎性质的非甾体抗炎药（NSAID）的衍生物，其可用于治疗炎症，疼痛和发烧。 更具体地，NSAID用硫化氢（H 2 S 2 S）释放部分衍生化，以产生具有降低的副作用的新型抗炎化合物。

公开(公告)号：US20100210607A1

公开(公告)日：2010-08-19

申请号：US12704412

申请日：2010-02-11

申请人： JOHN WALLACE ,  GIUSEPPE CIRINO ,  VINCENZO SANTAGADA ,  GIUSEPPE CALIENDO

发明人： JOHN WALLACE ,  GIUSEPPE CIRINO ,  VINCENZO SANTAGADA ,  GIUSEPPE CALIENDO

IPC分类号： A61K47/48 ,  C07D339/04 ,  C07C327/48 ,  C07D409/12 ,  C07D209/18 ,  A61K31/385 ,  A61K31/24 ,  A61K31/235 ,  A61K31/404 ,  A61K31/60

CPC分类号： C07C219/14 ,  C07C327/48 ,  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.

摘要翻译： 本发明涉及具有改善抗炎性质的非甾体抗炎药（NSAID）的衍生物，其可用于治疗炎症，疼痛和发烧。 更具体地，NSAID用硫化氢（H 2 S）释放部分衍生化，以产生具有降低的副作用的新型抗炎化合物。

公开(公告)号：US20070275905A1

公开(公告)日：2007-11-29

申请号：US11759154

申请日：2007-06-06

申请人： JOHN WALLACE ,  GIUSEPPE CIRINO ,  VINCENZO SANTAGADA ,  GIUSEPPE CALIENDO

发明人： JOHN WALLACE ,  GIUSEPPE CIRINO ,  VINCENZO SANTAGADA ,  GIUSEPPE CALIENDO

IPC分类号： A61K38/04 ,  A61K31/24 ,  C07C279/32

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.

摘要翻译： 提供了三甲双胍和N-单甲基甲基三苯妥丁的独特盐及其相应的立体异构体，具有改善的镇痛作用，可用于治疗内脏痛。 本发明的盐特别可用于治疗特征为腹痛（诸如炎性肠病（IBD）和肠易激综合征（IBS），糖尿病性胃轻瘫和消化不良的病症。