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公开(公告)号：US10258633B2
公开(公告)日：2019-04-16
申请号：US15299559
申请日：2016-10-21
IPC分类号： A61K31/56 , A61K31/575
摘要： The present invention relates to a method for inhibiting fibrosis that occurs in an organ where the farnesoid X receptor (FXR) is expressed. This method involves the step of administering a high potency, activating ligand of FXR in an effective amount to a patient who is not suffering from a cholestatic condition. The invention also provides pharmaceutical compositions containing an effective amount of an FXR ligand and kits for dispensing the pharmaceutical compositions.
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公开(公告)号：US08114858B2
公开(公告)日：2012-02-14
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： A61K31/60 , C07D339/04
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.
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公开(公告)号：US20060270635A1
公开(公告)日：2006-11-30
申请号：US11139871
申请日：2005-05-27
申请人： John Wallace , Giuseppe Cirino , Giuseppe Caliendo , Anna Sparatore , Vincenzo Santagada , Stefano Fiorucci
发明人： John Wallace , Giuseppe Cirino , Giuseppe Caliendo , Anna Sparatore , Vincenzo Santagada , Stefano Fiorucci
IPC分类号： C07F9/02 , A61K31/385
CPC分类号： C07D339/04 , C07C323/59 , C07C323/60 , C07C327/42 , C07C327/48 , C07F9/3895
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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4.发明申请Bile Acid Derivatives As FXR Ligands For The Prevention Or Treatment Of FXR-Mediated Diseases Or Conditions 有权胆酸衍生物作为FXR配体用于预防或治疗FXR介导的疾病或病症公开(公告)号：US20120283234A1
公开(公告)日：2012-11-08
申请号：US13082261
申请日：2011-04-07
IPC分类号： A61K31/575 , A61P1/16 , A61P1/00 , A61P13/12 , A61P3/04 , A61P3/00 , A61P1/04 , A61P9/10 , A61P3/10 , C07J9/00 , A61P9/00
CPC分类号： A61K31/575 , C07J9/00 , C07J31/006
摘要： The present invention relates to compounds of formula (I): wherein R is hydrogen or alpha-hydroxy, the hydroxyl group in position 7 is in the alpha or beta position; and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.
摘要翻译： 本发明涉及式（I）的化合物：其中R是氢或α-羟基，位置7的羟基位于α或β位; 及其药学上可接受的盐，溶剂合物或氨基酸缀合物。
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5.发明授权Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions 有权胆酸衍生物作为FXR配体，用于预防或治疗FXR介导的疾病或病症公开(公告)号：US07858608B2
公开(公告)日：2010-12-28
申请号：US12435063
申请日：2009-05-04
IPC分类号： A61K31/575 , C07J41/00
摘要： The present invention relates to compounds of formula (I) wherein: R1 is hydrogen or an alkyl group; R2 is hydrogen or a halogen, nitro, alkyloxy, amino or carboxy group; Y is CH2, oxygen or sulfur; n is an integer from 1 to 4, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof for the treatment of FXR-mediated diseases or conditions.
摘要翻译： 本发明涉及式（I）化合物，其中：R1是氢或烷基; R2是氢或卤素，硝基，烷氧基，氨基或羧基; Y是CH 2，氧或硫; n是1至4的整数，以及其药学上可接受的盐，溶剂合物或氨基酸缀合物，用于治疗FXR介导的疾病或病症。
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公开(公告)号：US20060069070A1
公开(公告)日：2006-03-30
申请号：US11081002
申请日：2005-03-14
IPC分类号： A61K31/56
CPC分类号： A61K31/575 , A61K31/56
摘要： The present invention relates to a method for inhibiting fibrosis that occurs in an organ where the farnesoid X receptor (FXR) is expressed. This method involves the step of administering a high potency, activating ligand of FXR in an effective amount to a patient who is not suffering from a cholestatic condition. The invention also provides pharmaceutical compositions containing an effective amount of an FXR ligand and kits for dispensing the pharmaceutical compositions.
摘要翻译： 本发明涉及在法尼酯X受体（FXR）表达的器官中发生的抑制纤维化的方法。 该方法包括向没有患胆汁淤滞状况的患者施用有效量的高效力FXR激活配体的步骤。 本发明还提供含有有效量的FXR配体的药物组合物和用于分配药物组合物的试剂盒。
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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.
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8.发明授权Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions 有权胆酸衍生物作为FXR配体，用于预防或治疗FXR介导的疾病或病症公开(公告)号：US07932244B2
公开(公告)日：2011-04-26
申请号：US11819517
申请日：2007-06-27
IPC分类号： A61K31/575 , C07C9/00
CPC分类号： A61K31/575 , C07J9/00 , C07J31/006
摘要： The present invention relates to compounds of formula (I): wherein R is hydrogen or alpha-hydroxy, the hydroxyl group in position 7 is in the alpha or beta position; and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.
摘要翻译： 本发明涉及式（I）的化合物：其中R是氢或α-羟基，位置7的羟基位于α或β位; 及其药学上可接受的盐，溶剂合物或氨基酸缀合物。
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公开(公告)号：US20070197479A1
公开(公告)日：2007-08-23
申请号：US11278395
申请日：2006-03-31
申请人： John Wallace , Giuseppe Cirino , Giuseppe Caliendo , Anna Sparatore , Vincenzo Santagada , Stefano Fiorucci
发明人： John Wallace , Giuseppe Cirino , Giuseppe Caliendo , Anna Sparatore , Vincenzo Santagada , Stefano Fiorucci
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。
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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。
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