专利号:WO-0119801-A1 优先权日:1999-09-16 标题 :Bioactive substance containing derivatives of 2-amino-6-aryloxypyrimidines and intermediary products of synthesis thereof 发明人:ASHKINAZI RIMMA ILIINICHNA; GANINA MARIYA BORISOVNA; STUDENTSOV EVGENY PAVLOVICH 权利人:ASHKINAZI RIMMA ILIINICHNA; GANINA MARIYA BORISOVNA; STUDENTSOV EVGENY PAVLOVICH 摘要:The invention relates to novel bioactive compounds of the family of pyrimidines and to intermediary products, of the synthesis of such compounds. The novel compounds have a strong antimicrobial activity (especially in respect to a strain of mycobacterium resisting to the existing drugs) and a strong antiviral activity in addition to a strong immunostimulating (interferonogenic) activity while at the same time having a low toxicity level. The derivatives of 2-amino-6-aryloxypyrimidines and intermediary products of the synthesis of such compounds correspond to the following general formula: (formula I) where R1 is preferably selected from a group containing amino, C1-C4 monoalkylamino, dialkylamino, carboxyalkylamino, arylamino, heterylamino groups; R2 represents halogen atoms or an alkyl, hydroxyl, amino or alkoxy group; R3 represents hydrogen or halogen atoms; R4 represents halogen atoms, aryloxy groups with functional X substituents in ortho-, meta- and para positions of the aryl fragment, whereby X substituents are halogen atoms, alkyls C1-C4, cycloalkyl, alkenyl, alkoxy and nitro groups. The invention also relates to the pharmaceutically acceptable salts thereof.
专利号:US-6225329-B1 优先权日:1998-03-12 标 题 :Modulators of protein tyrosine phosphatases (PTPases) 发明人:RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOELLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN 权利人:NOVO NORDISK AS 摘要:The present invention provides novel compounds of Formula 1, compositions containing these compounds, 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, n wherein A, R 1 , R 2 , R 3 , R 4 , R 16 and R 17 are as defined in the specification. 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.
专利号:US-2005119332-A1 优先权日:1998-03-12 标 题 :Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases) 发明人:JEPPESEN LONE; ANDERSEN HENRIK S; OLSEN OLE H; JUDGE LUKE M; HOLSWORTH DANIEL D; BAKIR FARID; AXE FRANK U; GE YU 摘要:The present invention provides novel compounds of formula 1a, n nnovel 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.
专利号:WO-9946244-A1 优先权日:1998-03-12 标题 :Modulators of protein tyrosine phosphatases (ptpases) 发明人:JEPPESEN LONE; ANDERSEN HENRIK SUNE; OLSEN OLE HVILSTED; JUDGE LUKE MILBURN; HOLSWORTH DANIEL DALE; BAKIR FARID; AXE FRANK URBAN; GE YU 权利人:NOVO NORDISK AS; ONTOGEN CORP 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.
专利号:WO-9946267-A1 优先权日:1998-03-12 标题 :Modulators of protein tyrosine phosphatases (ptpases) 发明人:MOELLER 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 权利人:NOVO NORDISK AS; ONTOGEN CORP 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.
专利号:US-6951878-B2 优先权日:1998-03-12 标 题:Benzo[b]thiophenyl or tetrahydro-benzo[b]thiophenyl modulators of protein tyrosine phosphatases (PTPases) 发明人:MOELLER 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 WILLIAM CHARLES; GE YU; UYEDA ROY TERUYUKI 权利人:NOVO NORDISK AS 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. n 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.