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公开(公告)号：US06410556B1
公开(公告)日：2002-06-25
申请号：US09659547
申请日：2000-09-11
申请人： Henrik Sune Andersen , Thomas Kruse Hansen , Jesper Lau , Niels Peter Hundahl Møller , Ole Hvilsted Olsen , Frank Urban Axe , Yu Ge , Daniel Dale Holsworth , Todd Kevin Jones , Luke Milburn Judge , Wiliam Charles Ripka , Barry Zvi Shapira , Roy Teruyuki Uyeda
发明人： Henrik Sune Andersen , Thomas Kruse Hansen , Jesper Lau , Niels Peter Hundahl Møller , Ole Hvilsted Olsen , Frank Urban Axe , Yu Ge , Daniel Dale Holsworth , Todd Kevin Jones , Luke Milburn Judge , Wiliam Charles Ripka , Barry Zvi Shapira , Roy Teruyuki Uyeda
IPC分类号： A61K31435
CPC分类号： C07D495/04 , A61K31/4365 , A61K45/06 , A61K2300/00
摘要： Disclosed are 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： 公开了新型化合物，新组合物，其使用方法及其制备方法，其中式1的这种化合物是包括PTP1B，T细胞PTP的蛋白质酪氨酸磷酸酶（PTPase）的药理学上有用的抑制剂，其中n，m，X， R1，R2，R3，R4，R5，R6和R7在说明书中更充分地定义。 该化合物可用于治疗I型糖尿病，II型糖尿病，葡萄糖耐量降低，胰岛素抵抗，肥胖症等疾病。
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公开(公告)号：US06262044B1
公开(公告)日：2001-07-17
申请号：US09268490
申请日：1999-03-11
申请人： Niels Peter Hundahl Møller , Henrik Sune Andersen , Lars Fogh Iversen , Ole Hvilsted Olsen , Sven Branner , Daniel Dale Holsworth , Farid Bakir , Luke Milburn Judge , Frank Urban Axe , Todd Kevin Jones , William Charles Ripka , Yu Ge , Roy Teruyuki Uyeda
发明人： Niels Peter Hundahl Møller , Henrik Sune Andersen , Lars Fogh Iversen , Ole Hvilsted Olsen , Sven Branner , Daniel Dale Holsworth , Farid Bakir , Luke Milburn Judge , Frank Urban Axe , Todd Kevin Jones , William Charles Ripka , Yu Ge , Roy Teruyuki Uyeda
IPC分类号： A61K31546
CPC分类号： C07D213/79 , C07C233/56 , C07C237/22 , C07D207/34 , C07D209/08 , C07D209/14 , C07D213/80 , C07D231/40 , C07D239/42 , C07D239/557 , C07D261/08 , C07D271/10 , C07D333/38 , C07D333/66 , C07D333/68 , C07D409/04 , C07D409/06 , C07D413/04 , C07D495/04 , C07D495/10 , C07D495/14
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, PTP&agr;, 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.
摘要翻译： 本发明提供新型化合物，新型组合物，其使用方法及其制备方法，其中这些化合物是蛋白酪氨酸磷酸酶（PTPase）如PTP1B，CD45，SHP-1，SHP-2，PTPα的药理学有用的抑制剂 ，LAR和HePTP等。 该化合物可用于治疗I型糖尿病，II型糖尿病，葡萄糖耐量降低，胰岛素抵抗，肥胖症，免疫功能障碍，包括凝血系统功能障碍的自身免疫性疾病，包括哮喘，过度性疾病，骨质疏松症，包括癌症和牛皮癣在内的增殖性疾病 ，具有减少或增加的生长激素合成或作用的疾病，调节生长激素释放/或对生长激素的反应，包括阿尔茨海默氏病和精神分裂症的疾病以及传染病的激素或细胞因子合成减少或增加的疾病。
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公开(公告)号：US06169087A
公开(公告)日：2001-01-02
申请号：US09157792
申请日：1998-09-21
申请人： Henrik Sune Andersen , Sven Branner , Claus Bekker Jeppesen , Niels Peter Hundahl Moeller , Adnan M. M. Mjalli , Sepehr Sarshar
发明人： Henrik Sune Andersen , Sven Branner , Claus Bekker Jeppesen , Niels Peter Hundahl Moeller , Adnan M. M. Mjalli , Sepehr Sarshar
IPC分类号： A61K314985
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. These 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.
摘要翻译： 本发明提供式1或式2的新化合物及其组合物，其用途及其制备方法，其中X，Y，Z，W，R 1，R 2和R 3在本说明书中更充分地定义。 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，肥胖症和许多其他疾病。
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公开(公告)号：US6063800A
公开(公告)日：2000-05-16
申请号：US253443
申请日：1999-02-19
IPC分类号： C07D231/20 , C07D249/14 , C07D257/04 , C07D271/10 , C07D271/113 , C07D277/34 , C07D285/08 , C07D285/12 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/38 , A61K31/425 , C07D209/82 , C07D277/04
CPC分类号： C07D271/113 , C07D231/20 , C07D249/14 , C07D257/04 , C07D277/34 , C07D285/08 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/3834 , C07F9/3882
摘要： The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.
摘要翻译： 本发明涉及新型有机化合物，其制备方法，含有它们的组合物，其用于治疗人和动物疾病的用途，其用于蛋白质或糖蛋白的纯化及其在诊断中的用途。 本发明涉及在体外系统，微生物，真核细胞，整个动物和人类中调节具有磷酸 - 酪氨酸识别单元的分子的活性，包括蛋白酪氨酸磷酸酶（PTPases）和具有Src-同源性-2结构域的蛋白质。 新型有机化合物是式（I）（L）n-Ar1-R1-A（I）的化合物，其中（L）n，n，Ar1，R1和A如申请中所定义。
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公开(公告)号：US09737612B2
公开(公告)日：2017-08-22
申请号：US13982617
申请日：2012-03-01
申请人： Mette Dahl Andersen , Peder Lisby Noerby , Kristian Kjaergaard , Albrecht Gruhler , Susanne Nedergaard Grell , Jens Buchardt , Henrik Sune Andersen , Soeren Padkjaer , Jesper Kastrup , Katarina Haakansson , Lars Hornum , Birgitte Friedrichsen , Dorrit Baunsgaard
发明人： Mette Dahl Andersen , Peder Lisby Noerby , Kristian Kjaergaard , Albrecht Gruhler , Susanne Nedergaard Grell , Jens Buchardt , Henrik Sune Andersen , Soeren Padkjaer , Jesper Kastrup , Katarina Haakansson , Lars Hornum , Birgitte Friedrichsen , Dorrit Baunsgaard
CPC分类号： A61K47/6803 , A61K47/545 , A61K2039/505 , C07K14/70578 , C07K16/2863 , C07K16/2878 , C07K2317/24 , C07K2317/30 , C07K2317/34 , C07K2317/55 , C07K2317/73 , C07K2317/75 , C07K2317/76 , C07K2317/92 , C07K2317/94 , C07K2319/30
摘要： The present disclosure relates to treatment of inflammatory diseases. In particular, the present disclosure relates to antagonistic DR3 ligands useful for treating inflammatory diseases.
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公开(公告)号：US20130330360A1
公开(公告)日：2013-12-12
申请号：US13982617
申请日：2012-03-01
申请人： Mette Dahl Andersen , Peder Lisby Noerby , Kristian Kjaergaard , Albrecht Gruhler , Susanne Nedergaard Grell , Jens Buchardt , Henrik Sune Andersen , Soeren Padkjaer , Jesper Kastrup , Katarina Haakansson , Lars Hornum , Birgitte Friedrichsen , Dorrit Baunsgaard
发明人： Mette Dahl Andersen , Peder Lisby Noerby , Kristian Kjaergaard , Albrecht Gruhler , Susanne Nedergaard Grell , Jens Buchardt , Henrik Sune Andersen , Soeren Padkjaer , Jesper Kastrup , Katarina Haakansson , Lars Hornum , Birgitte Friedrichsen , Dorrit Baunsgaard
IPC分类号： C07K16/28
CPC分类号： A61K47/6803 , A61K47/545 , A61K2039/505 , C07K14/70578 , C07K16/2863 , C07K16/2878 , C07K2317/24 , C07K2317/30 , C07K2317/34 , C07K2317/55 , C07K2317/73 , C07K2317/75 , C07K2317/76 , C07K2317/92 , C07K2317/94 , C07K2319/30
摘要： The present disclosure relates to treatment of inflammatory diseases. In particular, the present disclosure relates to antagonistic DR3 ligands useful for treating inflammatory diseases.
摘要翻译： 本公开涉及炎性疾病的治疗。 特别地，本公开涉及用于治疗炎性疾病的拮抗性DR3配体。
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公开(公告)号：US08383668B2
公开(公告)日：2013-02-26
申请号：US13235200
申请日：2011-09-16
申请人： Soren Ebdrup , Henrik Sune Andersen
发明人： Soren Ebdrup , Henrik Sune Andersen
IPC分类号： A61K31/402 , C07D207/08 , C07D207/12 , C07D207/14
CPC分类号： C07D487/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D471/08 , C07D491/08
摘要： The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
摘要翻译： 描述了使用取代的酰胺调节11＆bgr-羟基类固醇脱氢酶1型（11＆amp; HSD1）的活性以及这些化合物作为药物组合物的用途。 还有一类新颖的通式I的取代酰胺。它们在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途被描述。 本发明化合物是调节剂，更具体地是11和BDI HSDI的活性抑制剂，并且可用于治疗一系列需要活性糖皮质激素的细胞内浓度降低的医学疾病。
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公开(公告)号：US08138342B2
公开(公告)日：2012-03-20
申请号：US11665103
申请日：2005-10-12
IPC分类号： C07D401/04 , A61K31/438
CPC分类号： C07D221/20 , C07D401/06 , C07D401/10 , C07D471/10
摘要： A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11 β-hydroxy-Steroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
摘要翻译： 描述了一类新颖的通式（I）化合物，其在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途。 本发明化合物调节11β-羟基类固醇脱氢酶1（11＆amp; HSD1）的活性，因此可用于治疗这种调节有益的疾病，例如， 代谢综合征。
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公开(公告)号：US20110312949A1
公开(公告)日：2011-12-22
申请号：US13220843
申请日：2011-08-30
IPC分类号： A61K31/4184 , C07D401/14 , C07D403/10 , C07D413/14 , C07D401/10 , A61P3/00 , A61K31/454 , A61K31/5377 , A61K31/4709 , A61K31/541 , C07D403/14 , C07D405/14 , C07D417/14
CPC分类号： C07D405/14 , A61K31/404 , A61K31/4184 , C07D209/08 , C07D235/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D413/14 , C07D451/06
摘要： The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
摘要翻译： 描述了使用取代的酰胺调节11＆bgr-羟基类固醇脱氢酶1型（11＆amp; HSD1）的活性以及这些化合物作为药物组合物的用途。 还描述了一类新颖的取代的酰胺，它们在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途。 本发明化合物是调节剂，更具体地说是11β和HSD1活性的抑制剂，并且可用于治疗，预防和/或预防一系列医学病症，其中期望活性糖皮质激素的细胞内浓度降低。
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公开(公告)号：US20110223151A1
公开(公告)日：2011-09-15
申请号：US13055871
申请日：2009-08-06
申请人： Carsten Behrens , Patrick William Garibay , Soren Østergaard , Henrik Sune Andersen , Johansen Nils Langeland , Peschke Bernd , Bak Sonja
发明人： Carsten Behrens , Patrick William Garibay , Soren Østergaard , Henrik Sune Andersen , Johansen Nils Langeland , Peschke Bernd , Bak Sonja
CPC分类号： A61K47/48023 , A61K47/54 , A61K47/64
摘要： The invention relates to conjugated proteins, in particular but not exclusively, blood coagulation factors, to processes for preparing said conjugates, to pharmaceutical compositions comprising said conjugates and to the use of the conjugates in therapy, in particular but not exclusively, for the treatment of diseases alleviated by blood coagulation factors such as the prophylactic treatment of hemophilia.
摘要翻译： 本发明涉及缀合蛋白，特别是但不仅限于，凝血因子，制备所述缀合物的方法，包含所述缀合物的药物组合物以及所述缀合物在治疗中的用途，特别是但不排他地用于治疗 通过凝血因子如血友病的预防性治疗减轻疾病。
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