公开(公告)号：WO2006017124A3

公开(公告)日：2009-04-09

申请号：PCT/US2005024130

申请日：2005-07-08

Applicant: CENGENT THERAPEUTICS INC ,  CHERUVALLATH ZACCHARIA S ,  SEMPLE JOSEPH E ,  WANG JING ,  NUTT RUTH F ,  MYLVAGANAM SHANKARI

Inventor： CHERUVALLATH ZACCHARIA S ,  SEMPLE JOSEPH E ,  WANG JING ,  NUTT RUTH F ,  MYLVAGANAM SHANKARI

IPC: A61K31/42

CPC classification number: A61K31/4245 ,  C07D263/48 ,  C07D271/07 ,  C07D413/10 ,  C07F9/653 ,  C07F9/65312 ,  C07F9/65583

Abstract: Compounds, pharmaceutical compositions, and methods for treating, preventing, or ameliorating symptoms associated with diseases such as diabetes, cancer, neurodegenerative diseases, and obesity are provided. The compounds and compositions inhibit protein tyrosine phosphatase enzymes, e.g., PTP-1B.

Abstract translation: 提供了用于治疗，预防或改善与诸如糖尿病，癌症，神经变性疾病和肥胖症等疾病相关的症状的化合物，药物组合物和方法。 化合物和组合物抑制蛋白酪氨酸磷酸酶，例如PTP-1B。

公开(公告)号：WO2006078698A1

公开(公告)日：2006-07-27

申请号：PCT/US2006/001708

申请日：2006-01-17

Applicant: CENGENT THERAPEUTICS, INC. ,  CHERUVALLATH, Zacharia ,  SEMPLE, Joseph ,  RAJAPPAN, Vasanthakumar ,  RIDEOUT, Darryl ,  YALAMOORI, Venkatachalapathi ,  TSAI, Chung ,  WU, Feiyu ,  THORESEN, Lars ,  SHENDEROVICH, Mark

Inventor： CHERUVALLATH, Zacharia ,  SEMPLE, Joseph ,  RAJAPPAN, Vasanthakumar ,  RIDEOUT, Darryl ,  YALAMOORI, Venkatachalapathi ,  TSAI, Chung ,  WU, Feiyu ,  THORESEN, Lars ,  SHENDEROVICH, Mark

IPC: C07F9/6506 ,  A61K31/675 ,  A61P3/10

CPC classification number: C07F9/65583 ,  C07F9/65061 ,  C07F9/65068 ,  C07F9/65586

Abstract: Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. The compounds for use in the compositions and methods provided herein have formulae (I) Protein tyrosine hosaphatase, including PTB-1B, mediated diseases and disorders include diabetes including Type 1 and Type 2 diabetes (and associated complications such as hypertension, ischemic diseases of the large and small blood vessels, blindness, circulatory problems, kidney failure and atherosclerosis), syndrome X, methabolic syndrome, glucose intolerance, insulin resistance, obesity, cancer, neurodegenerative diseases.

Abstract translation: 提供化合物和组合物用于调节蛋白酪氨酸磷酸酶的活性。 用于本文提供的组合物和方法的化合物具有式（I）蛋白酪氨酸霍沙帕酶，包括PTB-1B，介导的疾病和病症包括糖尿病，包括1型和2型糖尿病（以及相关并发症，例如高血压，缺血性疾病 综合征X，代谢综合征，葡萄糖不耐受，胰岛素抵抗，肥胖，癌症，神经退行性疾病等。

公开(公告)号：WO2006009876A3

公开(公告)日：2006-03-30

申请号：PCT/US2005021540

申请日：2005-06-17

Applicant: CENGENT THERAPEUTICS INC ,  SEMPLE JOSEPH E ,  RIDEOUT DARRYL ,  NUTT RUTH F ,  SHERNDEROVICH MARK ,  WANG JING ,  MYLVAGANAM SHANKARI ,  WU FEIYUE ,  TSAI CHUNG-YING ,  YALAMOORI VENKATACHALAPATHI ,  LOWETH COLIN J

Inventor： SEMPLE JOSEPH E ,  RIDEOUT DARRYL ,  NUTT RUTH F ,  SHERNDEROVICH MARK ,  WANG JING ,  MYLVAGANAM SHANKARI ,  WU FEIYUE ,  TSAI CHUNG-YING ,  YALAMOORI VENKATACHALAPATHI ,  LOWETH COLIN J

IPC: A61K31/41 ,  A61K31/18 ,  C07C303/00 ,  C07D257/04

CPC classification number: A61K31/66 ,  C07C311/16 ,  C07C311/18 ,  C07C311/19 ,  C07C311/29 ,  C07C311/51 ,  C07C317/32 ,  C07C2601/04 ,  C07D207/337 ,  C07D257/04 ,  C07D295/26 ,  C07D333/34 ,  C07F9/3882 ,  C07F9/4056 ,  C07F9/4075 ,  C07F9/4426 ,  C07F9/4465 ,  C07F9/591 ,  C07F9/598 ,  C07F9/6524 ,  C07F9/65517

Abstract: Compounds, compositions and methods are provided for modulating the activity of protein tyrosine phosphatases, including PTP-1B. In one embodiment, the compounds are N,N-dibenzylarylsulfonamides.

Abstract translation: 提供了用于调节蛋白酪氨酸磷酸酶（包括PTP-1B）活性的化合物，组合物和方法。 在一个实施方案中，所述化合物是N，N-二苄基芳基磺酰胺。

公开(公告)号：WO2006028970A1

公开(公告)日：2006-03-16

申请号：PCT/US2005/031332

申请日：2005-09-01

Applicant: CENGENT THERAPEUTICS, INC. ,  CHERUVALLATH, Zacharia, S. ,  LOWETH, Colin, J. ,  NUTT, Ruth, F. ,  RIDEOUT, Darryl ,  SEMPLE, J., Edward ,  WANG, Jing ,  WU, Feiyue ,  MYLVAGANAM, Shankari ,  ZHU, Hengyi ,  SUN, Jianzhong

Inventor： CHERUVALLATH, Zacharia, S. ,  LOWETH, Colin, J. ,  NUTT, Ruth, F. ,  RIDEOUT, Darryl ,  SEMPLE, J., Edward ,  WANG, Jing ,  WU, Feiyue ,  MYLVAGANAM, Shankari ,  ZHU, Hengyi ,  SUN, Jianzhong

IPC: C07D277/42 ,  C07F9/6539 ,  C07D285/12 ,  C07D417/12 ,  C07D417/14 ,  C07D277/40 ,  C07F9/6558 ,  A61K31/675 ,  A61K31/426 ,  A61K31/433 ,  A61P3/10 ,  A61P3/04

CPC classification number: C07D277/38 ,  C07D277/42 ,  C07D285/135 ,  C07D417/12 ,  C07D417/14 ,  C07F9/6539 ,  C07F9/65395

Abstract: Provided herein are compounds and compositions for modulation of tyrosine phosphatase activity. In one embodiment, compounds and compositions for inhibiting protein tyrosine phosphatase activity are provided. In another embodiment, provided herein are compounds and compositions that are useful in the treatment, prevention, or amelioration of one or more symptoms of diseases caused by dysfunctional signal transduction, or in which dysfunctional signal transduction is implicated. In another embodiment, provided herein are compounds and compositions for treatment, prevention, or amelioration of one or more symptoms of diabetes. The compounds have following formulas: (II), (I), (III), and (IV).

Abstract translation: 本文提供了用于调节酪氨酸磷酸酶活性的化合物和组合物。 在一个实施方案中，提供了用于抑制蛋白酪氨酸磷酸酶活性的化合物和组合物。 在另一个实施方案中，本文提供了可用于治疗，预防或改善由功能障碍性信号转导引起的疾病或涉及功能障碍信号转导的一种或多种疾病症状的化合物和组合物。 在另一个实施方案中，本文提供了用于治疗，预防或改善一种或多种糖尿病症状的化合物和组合物。 所述化合物具有下式：（II），（I），（III）和（IV）。

公开(公告)号：WO2006017124A2

公开(公告)日：2006-02-16

申请号：PCT/US2005/024130

申请日：2005-07-08

Applicant: CENGENT THERAPEUTICS, INC. ,  CHERUVALLATH, Zaccharia, S. ,  SEMPLE, Joseph, E. ,  WANG, Jing ,  NUTT, Ruth, F. ,  MYLVAGANAM, Shankari

Inventor： CHERUVALLATH, Zaccharia, S. ,  SEMPLE, Joseph, E. ,  WANG, Jing ,  NUTT, Ruth, F. ,  MYLVAGANAM, Shankari

IPC: A61K31/4245

CPC classification number: A61K31/4245 ,  C07D263/48 ,  C07D271/07 ,  C07D413/10 ,  C07F9/653 ,  C07F9/65312 ,  C07F9/65583

Abstract: Compounds, pharmaceutical compositions, and methods for treating, preventing, or ameliorating symptoms associated with diseases such as diabetes, cancer, neurodegenerative diseases, and obesity are provided. The compounds and compositions inhibit protein tyrosine phosphatase enzymes, e.g., PTP-1B.

Abstract translation: 提供了用于治疗，预防或改善与诸如糖尿病，癌症，神经变性疾病和肥胖症等疾病相关的症状的化合物，药物组合物和方法。 化合物和组合物抑制蛋白酪氨酸磷酸酶，例如PTP-1B。

公开(公告)号：WO2006009876A2

公开(公告)日：2006-01-26

申请号：PCT/US2005/021540

申请日：2005-06-17

Applicant: CENGENT THERAPEUTICS, INC. ,  SEMPLE, Joseph, E. ,  RIDEOUT, Darryl ,  NUTT, Ruth, F. ,  SHERNDEROVICH, Mark ,  WANG, Jing ,  MYLVAGANAM, Shankari ,  WU, Feiyue ,  TSAI, Chung-Ying ,  YALAMOORI, Venkatachalapathi ,  LOWETH, Colin, J.

Inventor： SEMPLE, Joseph, E. ,  RIDEOUT, Darryl ,  NUTT, Ruth, F. ,  SHERNDEROVICH, Mark ,  WANG, Jing ,  MYLVAGANAM, Shankari ,  WU, Feiyue ,  TSAI, Chung-Ying ,  YALAMOORI, Venkatachalapathi ,  LOWETH, Colin, J.

IPC: A61K31/66

CPC classification number: A61K31/66 ,  C07C311/16 ,  C07C311/18 ,  C07C311/19 ,  C07C311/29 ,  C07C311/51 ,  C07C317/32 ,  C07C2601/04 ,  C07D207/337 ,  C07D257/04 ,  C07D295/26 ,  C07D333/34 ,  C07F9/3882 ,  C07F9/4056 ,  C07F9/4075 ,  C07F9/4426 ,  C07F9/4465 ,  C07F9/591 ,  C07F9/598 ,  C07F9/6524 ,  C07F9/65517

Abstract: Compounds, compositions and methods are provided for modulating the activity of protein tyrosine phosphatases, including PTP-1B. In one embodiment, the compounds are N,N-dibenzylarylsulfonamides.

Abstract translation: 提供化合物，组合物和方法用于调节蛋白酪氨酸磷酸酶（包括PTP-1B）的活性。 在一个实施方案中，化合物是N，N-二苄基芳基磺酰胺。