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公开(公告)号：EP1301516B1
公开(公告)日：2006-03-22
申请号：EP01949271.9
申请日：2001-06-28
发明人： ANDERSEN, Henrik, Sune , HANSEN, Thomas, Kruse , LAU, Jesper , MOLLER, Niels Peter, Hundahl , OLSEN, Ole, Hvilsted , AXE, Frank, Urban , BAKIR, Farid , GE, Yu , HOLSWORTH, Daniel, Dale , JUDGE, Luke, Milburn , NEWMAN, Michael, James , UYEDA, Roy, Teruyuki , SHAPIRA, Barry, Zvi
IPC分类号： C07D495/04 , A61K31/4365 , A61P3/00 , A61P5/48 , A61P37/00 , A61P35/00 , A61P43/00
CPC分类号： C07D495/04 , A61K31/4365
摘要： The present invention provides novel thienopyridines, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP; wherein X, R1, R2, R3 and R4 are defined more fully in the description. The compounds are useful in the treatment of type diabetes, type 2 diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
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公开(公告)号：EP1214324A1
公开(公告)日：2002-06-19
申请号：EP00958276.8
申请日：2000-09-11
发明人： ANDERSEN, Henrik, Sune , HANSEN, Thomas, Kruse , LAU, Jesper , M LLER, Niels, Peter, Hundahl , OLSEN, Ole, Hvilsted , AXE, Frank, Urban , GE, Yu , HOLSWORTH, Daniel, Dale , JONES, Todd, Kevin , JUDGE, Luke, Milburn , RIPKA, Wiliam, Charles , SHAPIRA, Barry, Zvi , UYEDA, Roy, Teruyuki
IPC分类号： C07D495/04 , C07D491/04 , A61K31/4365 , A61K31/4355 , A61P3/00 , A61P5/00 , A61P7/00 , A61P17/00 , A61P19/00 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00
CPC分类号： C07D495/04 , A61K31/4365 , A61K45/06 , A61K2300/00
摘要： The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula (1) are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP, wherein n, m, X, R1, R2, R3, R4, R5, R6, and R7 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
摘要翻译： 本发明提供了新的化合物，新组合物，它们的使用方法和它们的制造方法，其中这些式（1）化合物是蛋白质酪氨酸磷酸酶（PTPase's）的药理学上有用的抑制剂，包括PTP1B，T细胞PTP， 在说明书中更全面地定义了m，X，R1，R2，R3，R4，R5，R6和R7。 这些化合物可用于治疗I型糖尿病，II型糖尿病，葡萄糖耐量降低，胰岛素抵抗，肥胖和其他疾病。
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公开(公告)号：EP1301516A1
公开(公告)日：2003-04-16
申请号：EP01949271.9
申请日：2001-06-28
发明人： ANDERSEN, Henrik, Sune , HANSEN, Thomas, Kruse , LAU, Jesper , MOLLER, Niels Peter, Hundahl , OLSEN, Ole, Hvilsted , AXE, Frank, Urban , BAKIR, Farid , GE, Yu , HOLSWORTH, Daniel, Dale , JUDGE, Luke, Milburn , NEWMAN, Michael, James , UYEDA, Roy, Teruyuki , SHAPIRA, Barry, Zvi
IPC分类号： C07D495/04 , A61K31/4365 , A61P3/00 , A61P5/48 , A61P37/00 , A61P35/00 , A61P43/00
CPC分类号： C07D495/04 , A61K31/4365
摘要： The present invention provides novel thienopyridines, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP; wherein X, R1, R2, R3 and R4 are defined more fully in the description. The compounds are useful in the treatment of type diabetes, type 2 diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
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公开(公告)号：EP1214325A1
公开(公告)日：2002-06-19
申请号：EP00958277.6
申请日：2000-09-11
发明人： ANDERSEN, Henrik, Sune , HANSEN, Thomas, Kruse , LAU, Jesper , M LLER, Niels, Peter, Hundahl , OLSEN, Ole, Hvilsted , AXE, Frank, Urban , GE, Yu , HOLSWORTH, Daniel, Dale , JONES, Todd, Kevin , JUDGE, Luke, Milburn , RIPKA, Wiliam, Charles , SHAPIRA, Barry, Zvi , UYEDA, Roy, Teruyuki
IPC分类号： C07D495/04 , C07D513/04 , C07D493/04 , A61K31/381 , A61K31/395 , A61P3/00 , A61P5/00 , A61P7/00 , A61P17/00 , A61P19/00 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00
CPC分类号： C07D495/04
摘要： The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula (1) are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like, wherein n, m, X, Y, R1, R2, R3, R4, R5 and R6 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
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公开(公告)号：EP1214324B1
公开(公告)日：2006-06-14
申请号：EP00958276.8
申请日：2000-09-11
发明人： ANDERSEN, Henrik, Sune , HANSEN, Thomas, Kruse , LAU, Jesper , MOLLER, Niels, Peter, Hundahl , OLSEN, Ole, Hvilsted , AXE, Frank, Urban , GE, Yu , HOLSWORTH, Daniel, Dale , JONES, Todd, Kevin , JUDGE, Luke, Milburn , RIPKA, Wiliam, Charles , SHAPIRA, Barry, Zvi , UYEDA, Roy, Teruyuki
IPC分类号： C07D495/04 , C07D491/04 , A61K31/4365 , A61K31/4355 , A61P3/00 , A61P5/00 , A61P7/00 , A61P17/00 , A61P19/00 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00
CPC分类号： C07D495/04 , A61K31/4365 , A61K45/06 , A61K2300/00
摘要： The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula (1) are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP, wherein n, m, X, R1, R2, R3, R4, R5, R6, and R7 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
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公开(公告)号：EP1080095B1
公开(公告)日：2005-11-02
申请号：EP99907332.3
申请日：1999-03-11
发明人： MOLLER, Niels, Peter, Hundahl , ANDERSEN, Henrik, Sune , IVERSEN, Lars, Fogh , OLSEN, Ole, Hvilsted , BRANNER, Sven , HOLSWORTH, Daniel, Dale , BAKIR, Farid , JUDGE, Luke, Milburn , AXE, Frank, Urban , JONES, Todd, Kevin , RIPKA, Wiliam, Charles , GE, Yu , UYEDA, Roy, Teruyuki
IPC分类号： C07D513/04 , C07D333/62 , C07D497/04 , C07D209/18 , A61K31/38 , A61K31/395
摘要： The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTP alpha , LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
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公开(公告)号：EP1214325B1
公开(公告)日：2005-11-09
申请号：EP00958277.6
申请日：2000-09-11
发明人： ANDERSEN, Henrik, Sune , HANSEN, Thomas, Kruse , LAU, Jesper , M LLER, Niels, Peter, Hundahl , OLSEN, Ole, Hvilsted , AXE, Frank, Urban , GE, Yu , HOLSWORTH, Daniel, Dale , JONES, Todd, Kevin , JUDGE, Luke, Milburn , RIPKA, Wiliam, Charles , SHAPIRA, Barry, Zvi , UYEDA, Roy, Teruyuki
IPC分类号： C07D495/04 , C07D513/04 , C07D493/04 , A61K31/381 , A61K31/395 , A61P3/00 , A61P5/00 , A61P7/00 , A61P17/00 , A61P19/00 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00
CPC分类号： C07D495/04
摘要： The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula (1) are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like, wherein n, m, X, Y, R1, R2, R3, R4, R5 and R6 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
摘要翻译： 本发明提供了新的化合物，新组合物，它们的使用方法和它们的制造方法，其中这些式（1）化合物是蛋白质酪氨酸磷酸酶（PTPases）的药理学上有用的抑制剂，例如PTP1B，CD45，SHP-1， SHP-2，PTPα，LAR和HePTP等，其中n，m，X，Y，R 1，R 2，R 3，R 4，R 5和R 6在说明书中更全面地定义。 这些化合物可用于治疗I型糖尿病，II型糖尿病，葡萄糖耐量降低，胰岛素抵抗，肥胖和其他疾病。
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公开(公告)号：EP1080095A1
公开(公告)日：2001-03-07
申请号：EP99907332.3
申请日：1999-03-11
发明人： MOLLER, Niels, Peter, Hundahl , ANDERSEN, Henrik, Sune , IVERSEN, Lars, Fogh , OLSEN, Ole, Hvilsted , BRANNER, Sven , HOLSWORTH, Daniel, Dale , BAKIR, Farid , JUDGE, Luke, Milburn , AXE, Frank, Urban , JONES, Todd, Kevin , RIPKA, Wiliam, Charles , GE, Yu , UYEDA, Roy, Teruyuki
IPC分类号： C07D513/04 , C07D333/62 , C07D497/04 , C07D209/18 , A61K31/38 , A61K31/395
摘要： The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
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公开(公告)号：EP1062204A1
公开(公告)日：2000-12-27
申请号：EP99907334.9
申请日：1999-03-11
发明人： JEPPESEN, Lone , ANDERSEN, Henrik, Sune , OLSEN, Ole, Hvilsted , JUDGE, Luke, Milburn , HOLSWORTH, Daniel, Dale , BAKIR, Farid , AXE, Frank, Urban , GE, Yu
IPC分类号： C07D207/34 , C07D231/14 , C07D333/26 , A61K31/40 , A61K31/41 , A61K31/38
摘要： The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
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10.发明公开METHOD OF INHIBITING PROTEIN TYROSINE PHOSPHATASE 1B AND/OR T-CELL PROTEIN TYROSINE PHOSPHATASE AND/OR OTHER PTPASES WITH AN ASP RESIDUE AT POSITION 48 审中-公开用于抑制TYROSINPHOPHATASE 1B和/或T细胞蛋白TYRONSINPHOSPHATASE WITH A ASP REST在4位和/或其他的PTPases
公开(公告)号：EP1214060A2
公开(公告)日：2002-06-19
申请号：EP00963340.5
申请日：2000-09-11
发明人： ANDERSEN, Henrik, Sune , HANSEN, Thomas, Kruse , Iverson, Lars Fogh , LAU, Jesper , M LLER, Niels, Peter, Hundahl , OLSEN, Ole, Hvilsted , AXE, Frank, Urban , GE, Yu , HOLSWORTH, Daniel, Dale , JONES, Todd, Kevin , JUDGE, Luke, Milburn , RIPKA, William, Charles , SHAPIRA, Barry, Zvi , UYEDA, Roy Teruyuki
IPC分类号： A61K31/00 , A61K31/435 , A61K31/381 , A61K31/38
CPC分类号： C07D495/04 , A61K31/00 , A61K31/38 , A61K31/381 , A61K31/435 , A61K45/06
摘要： The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTPα, PTPε, PTPν, PTPδ, PTPσ, PTPz, PTPβ, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.
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