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公开(公告)号：EP1017697A1
公开(公告)日：2000-07-12
申请号：EP98945078.8
申请日：1998-09-21
发明人： ANDERSEN, Henrik, Sune , BRANNER, Sven , JEPPESEN, Claus, Bekker , MOLLER, Niels, Peter, Hundahl , SARSHAR, Sepehr , MJALLI, Adnan
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention provides novel compounds of Formula (1) or Formula (2) and compositions thereof, methods of their use, and methods of their manufacture, wherein X, Y, Z, W, R1, R2 and R3 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 a number of 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：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：EP1062199A1
公开(公告)日：2000-12-27
申请号：EP99907333.1
申请日：1999-03-11
发明人： RICHTER, Lutz Stefan , ANDERSEN, Henrik, Sune , VAGNER, Josef , JEPPESEN, Claus, Bekker , MOLLER, Niels, Peter, Hundahl , BRANNER, Sven , SU, Jing , BAKIR, Farid , JUDGE, Luke, Milburn
IPC分类号： C07C235/84 , C07D213/55 , C07D239/28 , C07D241/24 , A61K31/17 , A61K31/44 , A61K31/50 , A61K31/505
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：EP0529010B1
公开(公告)日：1995-09-06
申请号：EP91920970.0
申请日：1991-04-30
申请人： NOVO NORDISK A/S
发明人： WIBERG, Finn, Christoph , OLSEN, Frank , BOEL, Esper , KJELDSEN, Thomas, Borglum , MOLLER, Niels, Peter, Hundahl
CPC分类号： C07K14/71 , C07K14/705 , C07K14/72 , C07K2319/00 , C07K2319/32
摘要： Mammalian cells containing a hybrid DNA insert which comprises a first DNA sequence encoding part of the extracellular domain of a first cellular receptor and a second DNA sequence encoding part of the extracellular domain of second cellular receptor which is specific for a different ligand than the first cellular receptor have favourable growth properties in serum-containing as well as serum-free media.
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7.发明授权
公开(公告)号：EP0558529B1
公开(公告)日：1996-01-10
申请号：EP91919614.7
申请日：1991-10-18
申请人： NOVO NORDISK A/S
IPC分类号： A61K39/395
摘要： A pharmaceutical preparation which, as an active component contains an agent that will block EPI activity (EPI inhibitor), is useful in the treatment of patients with prolonged coagulation time.
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公开(公告)号：EP0529010A1
公开(公告)日：1993-03-03
申请号：EP91920970.0
申请日：1991-04-30
申请人： NOVO NORDISK A/S
发明人： WIBERG, Finn, Christoph , OLSEN, Frank , BOEL, Esper , KJELDSEN, Thomas, Borglum , MOLLER, Niels, Peter, Hundahl
CPC分类号： C07K14/71 , C07K14/705 , C07K14/72 , C07K2319/00 , C07K2319/32
摘要： Cellules de mammifères contenant un insert d'ADN hydride qui comprend une première séquence d'ADN codant une partie du domaine extracellulaire d'un premier récepteur cellulaire et une deuxième séquence d'ADN codant une partie du domaine extracellulaire d'un deuxième récepteur cellulaire spécifique à un liant différent du premier récepteur cellulaire. ces cellules possèdent des propriétés de croissance efficaces dans des milieux contenant ou non du sérum.
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9.发明授权METHOD OF INHIBITING PTP 1B AND/OR T-CELL PTP AND/OR OTHER PTPASES WITH AN ASP RESIDUE AT POSITION 48 有权用于抑制酪氨酸磷酸酶1B和/或T细胞中的蛋白质酪氨酸磷酸酶WITH A ASP REST和/或其他的PTPases IN POSITION 48
公开(公告)号：EP1404682B1
公开(公告)日：2005-09-14
申请号：EP02740410.2
申请日：2002-06-25
申请人： NOVO NORDISK A/S
发明人： HANSEN, Thomas, Kruse , OLSEN, Ole, Hvilsted , PETERSEN, Anders, Klarskov , LAU, Jesper , ANDERSEN, Henrik, Sune , MOLLER, Niels, Peter, Hundahl
IPC分类号： C07D495/08 , C07D495/18 , C07D498/08 , A61K31/4365 , A61K31/4375 , A61K31/5365
CPC分类号： C07D495/18 , C07D498/18
摘要： This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al., Proc. Natl. Acad. Sci. USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1. This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.
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10.发明公开METHOD OF INHIBITING PTP 1B AND/OR T-CELL PTP AND/OR OTHER PTPASES WITH AN ASP RESIDUE AT POSITION 48 有权用于抑制酪氨酸磷酸酶1B和/或T细胞中的蛋白质酪氨酸磷酸酶WITH A ASP REST和/或其他的PTPases IN POSITION 48
公开(公告)号：EP1404682A1
公开(公告)日：2004-04-07
申请号：EP02740410.2
申请日：2002-06-25
申请人： Novo Nordisk A/S
发明人： HANSEN, Thomas, Kruse , OLSEN, Ole, Hvilsted , PETERSEN, Anders, Klarskov , LAU, Jesper , ANDERSEN, Henrik, Sune , MOLLER, Niels, Peter, Hundahl
IPC分类号： C07D495/08 , C07D495/18 , C07D498/08 , A61K31/4365 , A61K31/4375 , A61K31/5365
CPC分类号： C07D495/18 , C07D498/18
摘要： This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al., Proc. Natl. Acad. Sci. USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1. This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.
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