公开(公告)号：US08541398B2

公开(公告)日：2013-09-24

申请号：US12704412

申请日：2010-02-11

Applicant: John L. Wallace ,  Giuseppe Cirino ,  Vincenzo Santagada ,  Giuseppe Caliendo

Inventor： John L. Wallace ,  Giuseppe Cirino ,  Vincenzo Santagada ,  Giuseppe Caliendo

IPC: A61K31/603 ,  A61K31/606 ,  C07D209/04 ,  C07C69/76

CPC classification number: C07C219/14 ,  C07C327/48 ,  C07D209/18 ,  C07D209/32 ,  C07D309/30 ,  C07D339/04 ,  C07D409/12

Abstract: 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.

Abstract translation: 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：US08314140B2

公开(公告)日：2012-11-20

申请号：US12374273

申请日：2007-07-18

Applicant: John Wallace ,  Giuseppe Cirino ,  Vincenzo Santagada ,  Giuseppe Caliendo

Inventor： John Wallace ,  Giuseppe Cirino ,  Vincenzo Santagada ,  Giuseppe Caliendo

IPC: A61K31/405 ,  A61K31/40 ,  A61K31/35 ,  C07D207/00 ,  C07D209/00 ,  C07D309/30 ,  C07D313/04 ,  C07C61/04 ,  C07C321/00

CPC classification number: C07C327/48 ,  C07C219/14 ,  C07D209/18 ,  C07D209/32 ,  C07D309/30 ,  C07D339/04 ,  C07D409/12

Abstract: 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.

Abstract translation: 提供药物的衍生物，所述衍生物包含与药物共价连接或与药物形成盐的H 2 S-释放部分4-羟基硫代苯甲酰胺。 本发明的化合物表现出增强的活性或减少的副作用或两者。

公开(公告)号：US08114857B2

公开(公告)日：2012-02-14

申请号：US12980985

申请日：2010-12-29

Applicant: John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vicenzo Santagada ,  Stefano Fiorucci

Inventor： John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vicenzo Santagada ,  Stefano Fiorucci

IPC: A61K31/655 ,  A61K31/60 ,  C07C241/00 ,  C07C229/00

CPC classification number: C07C323/59 ,  C07C323/60 ,  C07C327/42 ,  C07C327/48 ,  C07D339/04 ,  C07F9/3895 ,  C07F9/65785

Abstract: 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.

Abstract translation: 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：US20110144188A1

公开(公告)日：2011-06-16

申请号：US12303082

申请日：2007-06-06

Applicant: John L. Wallace ,  Giuseppe Cirino ,  Vincenzo Santagada ,  Giuseppe Caliendo

Inventor： John L. Wallace ,  Giuseppe Cirino ,  Vincenzo Santagada ,  Giuseppe Caliendo

IPC: A61K31/385 ,  C07C69/732 ,  C07D339/04 ,  A61K31/24 ,  C07C211/22 ,  C07C211/26 ,  A61P25/00

CPC classification number: C07C279/32 ,  C07C219/22 ,  C07C323/60 ,  C07C327/48 ,  C07D339/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07910568B2

公开(公告)日：2011-03-22

申请号：US11915305

申请日：2006-03-31

Applicant: John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vincenzo Santagada ,  Stefano Fiorucci

Inventor： John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vincenzo Santagada ,  Stefano Fiorucci

IPC: A61K31/67 ,  C07D339/02

CPC classification number: C07C327/42 ,  C07C323/12 ,  C07C323/59 ,  C07C323/60 ,  C07C327/48 ,  C07D339/04 ,  C07F9/6578 ,  C07F9/6587

Abstract: 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.

Abstract translation: 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：US07879827B2

公开(公告)日：2011-02-01

申请号：US12368846

申请日：2009-02-10

Applicant: John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vincenzo Santagada ,  Stefano Fiorucci

Inventor： John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vincenzo Santagada ,  Stefano Fiorucci

IPC: A61K31/655 ,  A61K31/603 ,  A61K31/606 ,  C07C243/10 ,  C07C229/48

CPC classification number: C07C323/59 ,  C07C323/60 ,  C07C327/42 ,  C07C327/48 ,  C07D339/04 ,  C07F9/3895 ,  C07F9/65785

Abstract: 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：US20090233886A1

公开(公告)日：2009-09-17

申请号：US12368846

申请日：2009-02-10

Applicant: John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vincenzo Santagada ,  Stefano Fiorucci

Inventor： John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vincenzo Santagada ,  Stefano Fiorucci

IPC: A61K31/655 ,  A61K31/198

CPC classification number: C07C323/59 ,  C07C323/60 ,  C07C327/42 ,  C07C327/48 ,  C07D339/04 ,  C07F9/3895 ,  C07F9/65785

Abstract: 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.

Abstract translation: 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：US07498355B2

公开(公告)日：2009-03-03

申请号：US11278395

申请日：2006-03-31

Applicant: John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vincenzo Santagada ,  Stefano Fiorucci

Inventor： John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vincenzo Santagada ,  Stefano Fiorucci

IPC: A61K31/381 ,  C07D339/04

CPC classification number: C07C323/59 ,  C07C323/60 ,  C07C327/42 ,  C07C327/48 ,  C07D339/04 ,  C07F9/3895 ,  C07F9/65785

Abstract: 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.

Abstract translation: 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：US08114858B2

公开(公告)日：2012-02-14

申请号：US12981008

申请日：2010-12-29

Applicant: John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vincenzo Santagada ,  Stefano Fiorucci

Inventor： John L. Wallace ,  Giuseppe Cirino ,  Giuseppe Caliendo ,  Anna Sparatore ,  Vincenzo Santagada ,  Stefano Fiorucci

IPC: A61K31/60 ,  C07D339/04

CPC classification number: C07C323/59 ,  C07C323/60 ,  C07C327/42 ,  C07C327/48 ,  C07D339/04 ,  C07F9/3895 ,  C07F9/65785

Abstract: 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：US20100210607A1

公开(公告)日：2010-08-19

申请号：US12704412

申请日：2010-02-11

Applicant: JOHN WALLACE ,  GIUSEPPE CIRINO ,  VINCENZO SANTAGADA ,  GIUSEPPE CALIENDO

Inventor： JOHN WALLACE ,  GIUSEPPE CIRINO ,  VINCENZO SANTAGADA ,  GIUSEPPE CALIENDO

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

CPC classification number: C07C219/14 ,  C07C327/48 ,  C07D209/18 ,  C07D209/32 ,  C07D309/30 ,  C07D339/04 ,  C07D409/12

Abstract: 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.

Abstract translation: 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。