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公开(公告)号：US20140073563A1
公开(公告)日：2014-03-13
申请号：US14019735
申请日：2013-09-06
申请人： Oliver BOSCHEINEN , Matthias DREYER , Paul HABERMANN , Hans-Ludwig SCHAEFER , Mark SOMMERFELD , Thomas LANGER
发明人： Oliver BOSCHEINEN , Matthias DREYER , Paul HABERMANN , Hans-Ludwig SCHAEFER , Mark SOMMERFELD , Thomas LANGER
IPC分类号： C07K14/50 , C07K14/605
CPC分类号： C07K14/605 , A61K38/1825 , A61K38/26 , A61K47/60 , A61K2300/00 , C07K14/50 , C07K14/575 , C07K14/57563 , C07K2319/00 , C07K2319/21 , C07K2319/30 , C07K2319/31 , C07K2319/50 , C07K2319/90
摘要： The invention is directed to a fusion protein comprising at least one FGF-21 (fibroblast growth factor-21) compound and at least one GLP-1R (glucagon-like peptide-1 receptor) agonist as well as to pharmaceutical compositions, medical uses and methods of treatment involving the fusion protein, particularly in the field of diabetes, dyslipidemia, obesity and/or adipositas.
摘要翻译： 本发明涉及包含至少一种FGF-21（成纤维细胞生长因子-21）化合物和至少一种GLP-1R（胰高血糖素样肽-1受体）激动剂以及药物组合物，医学用途和 涉及融合蛋白的治疗方法，特别是在糖尿病，血脂异常，肥胖和/或脂肪酸领域。
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2.发明授权1,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof 有权被苄基取代的1,4-苯并噻吩1,1-二氧化物衍生物，其制备方法，包含这些化合物的药物及其用途公开(公告)号：US07956085B2
公开(公告)日：2011-06-07
申请号：US12465911
申请日：2009-05-14
申请人： Wendelin Frick , Heiner Glombik , Stefan Theis , Hubert Heuer , Hans-Ludwig Schaefer , Werner Kramer
发明人： Wendelin Frick , Heiner Glombik , Stefan Theis , Hubert Heuer , Hans-Ludwig Schaefer , Werner Kramer
IPC分类号： A61K31/38 , C07D409/08
CPC分类号： C07H5/06 , A61K31/38 , A61K31/7028 , A61K45/06 , C07D409/12 , C07H5/04 , C07H7/02 , C07H7/027 , C07H13/12 , C07H15/26 , A61K2300/00
摘要： This invention relates to Novel 1,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof.
摘要翻译： 本发明涉及由苄基取代的新型1,4-苯并噻吩1,1-二氧化物衍生物，其制备方法，包含这些化合物的药物及其用途。
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![N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, pharmaceutical compositions thereof and methods for their therapeutic use](/abs-image/US/2010/12/28/US07858647B2/abs.jpg.150x150.jpg)
3.发明授权N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, pharmaceutical compositions thereof and methods for their therapeutic use 有权N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺，其药物组合物及其治疗用途的方法公开(公告)号：US07858647B2
公开(公告)日：2010-12-28
申请号：US12062764
申请日：2008-04-04
申请人： Stefanie Keil , Hans Matter , Karl Schoenafinger , Matthias Urmann , Maike Glien , Wolfgang Wendler , Hans-Ludwig Schaefer , Eugen Falk
发明人： Stefanie Keil , Hans Matter , Karl Schoenafinger , Matthias Urmann , Maike Glien , Wolfgang Wendler , Hans-Ludwig Schaefer , Eugen Falk
IPC分类号： A61K31/4436 , A61K31/433 , C07D417/12 , C07D285/135
CPC分类号： C07D417/12 , C07D285/135
摘要： The present invention comprises N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their physiologically acceptable salts and functional derivatives that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, And the isomers thereof wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
摘要翻译： 本发明包括显示过氧化物酶体增殖物激活受体（PPAR）PPARδ和PPARγ激动剂活性的N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺，其生理上可接受的盐和功能性衍生物。 本发明化合物的结构由下式I定义，其各种取代基在本文中定义的异构体，包括其生理上可接受的盐。 还公开了化合物制备的方法。 该化合物适用于治疗脂肪酸代谢和葡萄糖利用障碍，涉及胰岛素抵抗的疾病以及中枢和周围神经系统的脱髓鞘和其他神经变性疾病。
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![N-[1,3,4]-THIADIAZOL-2-YL-BENZENE SULFONAMIDES, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHODS FOR THEIR THERAPEUTIC USE](/abs-image/US/2009/02/26/US20090054494A1/abs.jpg.150x150.jpg)
4.发明申请N-[1,3,4]-THIADIAZOL-2-YL-BENZENE SULFONAMIDES, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHODS FOR THEIR THERAPEUTIC USE 有权N- [1,3,4] - 十二烷基-2-Y-BENZENE SULFONAMIDES，其药物组合物及其治疗用途的方法公开(公告)号：US20090054494A1
公开(公告)日：2009-02-26
申请号：US12062764
申请日：2008-04-04
申请人： Stefanie KEIL , Hans MATTER , Karl SCHOENAFINGER , Mathias URMANN , Maike GLIEN , Wolfgang WENDLER , Hans-Ludwig SCHAEFER , Eugen FALK
发明人： Stefanie KEIL , Hans MATTER , Karl SCHOENAFINGER , Mathias URMANN , Maike GLIEN , Wolfgang WENDLER , Hans-Ludwig SCHAEFER , Eugen FALK
IPC分类号： A61K31/433 , C07D285/135 , A61K31/4439 , A61P3/00 , C07D417/12
CPC分类号： C07D417/12 , C07D285/135
摘要： The present invention comprises N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their physiologically acceptable salts and functional derivatives that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, And the isomers thereof wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
摘要翻译： 本发明包括显示过氧化物酶体增殖物激活受体（PPAR）PPARδ和PPARγ激动剂活性的N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺，其生理上可接受的盐和功能性衍生物。 本发明化合物的结构由下式I定义，其各种取代基在本文中定义的异构体，包括其生理上可接受的盐。 还公开了化合物制备的方法。 该化合物适用于治疗脂肪酸代谢和葡萄糖利用障碍，涉及胰岛素抵抗的疾病以及中枢和周围神经系统的脱髓鞘和其他神经变性疾病。
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5.发明申请Hydroxy-Substituted Diphenylazetidinones for the Treatment of Hyperlipidemia 审中-公开羟基取代的二苯基氮杂环丁酮用于治疗高脂血症公开(公告)号：US20080274947A1
公开(公告)日：2008-11-06
申请号：US12122991
申请日：2008-05-19
申请人： Gerhard JAEHNE , Wendelin FRICK , Andreas LINDENSCHMIDT , Hubert HEUER , Hans-Ludwig SCHAEFER , Werner KRAMER , Wolfgang SCHMIDER
发明人： Gerhard JAEHNE , Wendelin FRICK , Andreas LINDENSCHMIDT , Hubert HEUER , Hans-Ludwig SCHAEFER , Werner KRAMER , Wolfgang SCHMIDER
IPC分类号： A61K38/28 , C07D403/12 , A61P3/10 , A61P9/10 , A61K31/496
CPC分类号： C07D205/08 , C07D401/12 , C07D403/12 , C07D487/08
摘要： The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistance and the like comprising diphenylazetidinones compounds which have an additional hydroxy function in the 2″ position and their salts. The invention therefore relates to compounds of formula I: in which the meanings R1, R2, R3, R4, R5, R6 are defined herein.
摘要翻译： 本发明包括用于治疗代谢性疾病的化合物和组合物，更具体地，涉及血液中的这些胰岛素相关代谢紊乱，例如高脂血症，糖尿病，胰岛素抵抗等，其包含在2位中具有额外羟基功能的二苯基氮杂环丁酮化合物 的位置和盐。 因此，本发明涉及式I化合物：其中R 1，R 2，R 3，R 4，R 5，R 6的定义在本文中。
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6.发明申请1,4-BENZOTHIAZEPINE 1,1-DIOXIDE DERIVATIVE, PROCESS FOR ITS PREPARATION, MEDICAMENTS COMPRISING THIS COMPOUND, AND USE THEREOF AS A HYPOLIPIDAEMIC 失效1,4-BENZOTHIAZEPINE 1,1-二氧化物衍生物，其制备方法，包含该化合物的药物及其作为高血压药物的用途公开(公告)号：US20080207534A1
公开(公告)日：2008-08-28
申请号：US11970281
申请日：2008-01-07
IPC分类号： A61K31/7052 , C07H17/00 , A61P3/00
CPC分类号： C07H13/12
摘要： The invention relates to the compound of the formula (A) and also to its physiologically acceptable salts. The compound is suitable as, for example, a hypolipidemic.
摘要翻译： 本发明涉及式（A）的化合物以及其生理上可接受的盐。 该化合物适合作为例如降血脂药。
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7.发明申请6-OXAZOL-4-YLMETHOLMETHOXY-ALKO-ALKOXYMETHYL SUBSTITUTED BENZOIC ACID DERIVATIVES FORMING PEROXISOME PROLIFERATOR - ACTIVATED RECEPTOR (PPAR) LIGANDS, PROCESS FOR THEIR PREPARATION AND METHODS OF USE THEREOF 有权形成过氧化物增效剂 - 活化受体（PPAR）配体的6-氧杂-4-甲基-4-羟基乙氧基-α-烷氧基甲基取代的苯甲酸衍生物，其制备方法及其使用方法公开(公告)号：US20080171776A1
公开(公告)日：2008-07-17
申请号：US11949833
申请日：2007-12-04
申请人： Christian STAPPER , Heiner GLOMBIK , Eugen FALK , Stefanie KEIL , Hans-Ludwig SCHAEFER , Wolfgang WENDLER , Stephanie HACHTEL
发明人： Christian STAPPER , Heiner GLOMBIK , Eugen FALK , Stefanie KEIL , Hans-Ludwig SCHAEFER , Wolfgang WENDLER , Stephanie HACHTEL
IPC分类号： A61K31/421 , C07D263/32 , A61P3/00 , A61P3/10 , A61P3/08
CPC分类号： C07D263/32 , C07D413/04
摘要： The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistance and the like comprising acetic acid derivatives with cyclohexylmethoxy substituents and their salts. Known as peroxisome proliferator-activated receptor (PPAR) agonists/antagonists, the invention relates to compounds of formula I wherein R1-R6 are further defined herein.
摘要翻译： 本发明包括用于治疗代谢紊乱的化合物和组合物，更具体地，涉及含有环己基甲氧基取代基的乙酸衍生物及其盐的血液中的这些与胰岛素有关的代谢性疾病如高脂血症，糖尿病，胰岛素抵抗等。 被称为过氧化物酶体增殖物激活受体（PPAR）激动剂/拮抗剂的本发明涉及式I化合物，其中R 1 -R 6在本文中进一步定义。
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8.发明申请NOVEL DIPHENYLAZETIDINONE WITH IMPROVED PHYSIOLOGICAL PROPERTIES, PROCESS FOR ITS PREPARATION, MEDICAMENTS COMPRISING THIS COMPOUND, AND ITS USE 失效具有改善的生理特性的新型二氢噻吩酮，其制备方法，包含该化合物的药物及其用途公开(公告)号：US20070197498A1
公开(公告)日：2007-08-23
申请号：US11690993
申请日：2007-03-26
申请人： Gerhard JAEHNE , Wendelin Frick , Andreas Lindenschmidt , Stefanie Flohr , Hubert Heuer , Hans-Ludwig Schaefer , Werner Kramer , Eric Galia , Heiner Glombik
发明人： Gerhard JAEHNE , Wendelin Frick , Andreas Lindenschmidt , Stefanie Flohr , Hubert Heuer , Hans-Ludwig Schaefer , Werner Kramer , Eric Galia , Heiner Glombik
IPC分类号： A61K31/397 , C07D205/02
CPC分类号： C07C233/18 , C07D205/08
摘要： Novel diphenylazetidinone, process for its preparation, medicaments comprising this compound and their use The invention relates to the compound of the formula 1 and to its physiologically acceptable salts. The compound is suitable, for example, as a hypolipidemic.
摘要翻译： 新型二苯基氮杂环丁酮，其制备方法，包含该化合物的药物及其用途本发明涉及式1的化合物及其生理上可接受的盐。 该化合物例如可用作降血脂药物。
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公开(公告)号：US20070043017A1
公开(公告)日：2007-02-22
申请号：US11544718
申请日：2006-10-10
申请人： Gerhard Jaehne , Wendelin Frick , Stefanie Flohr , Andreas Lindenschmidt , Heiner Glombik , Werner Kramer , Hubert Heuer , Hans-Ludwig Schaefer
发明人： Gerhard Jaehne , Wendelin Frick , Stefanie Flohr , Andreas Lindenschmidt , Heiner Glombik , Werner Kramer , Hubert Heuer , Hans-Ludwig Schaefer
IPC分类号： A61K31/397 , C07D205/02 , C07D403/02
CPC分类号： C07D403/12 , C07D205/08 , C07D453/02 , C07D487/08 , Y10S930/28
摘要： One embodiment of the invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification. Other embodiments of the invention relate to physiologically acceptable salts of compounds of formula I, to processes for their preparation and to medicaments comprising these compounds. The compounds of the invention are suitable for use, for example, as hypolipidemics.
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10.发明授权Combination product of a 1,4-benzothiepine 1,1-dioxide compound with at least one other active ingredient and the use of the product 有权1,4-苯并噻吩1,1-二氧化物化合物与至少一种其它活性成分的组合产物和产物的用途公开(公告)号：US07179792B2
公开(公告)日：2007-02-20
申请号：US10699967
申请日：2003-11-03
CPC分类号： A61K45/06 , A61K31/395 , A61K31/55 , A61K2300/00
摘要： The present invention is directed to a 1,4-benzothiepine 1,1-dioxide compound of formula I in which the radicals have the meanings defined herein, or a pharmaceutically acceptable salt or physiologically functional derivative thereof, with at least one other active ingredient, or a pharmaceutically acceptable salt or physiologically functional derivative thereof. The invention is also directed to the use of the combination product, pharmaceutical composition comprising the combination product and method for preparing the pharmaceutical composition.
摘要翻译： 本发明涉及其中基团具有本文定义的含义，或其药学上可接受的盐或生理功能衍生物的式I的1,4-苯并硫代1,1-二氧化物化合物与至少一种其它活性成分， 或其药学上可接受的盐或生理功能衍生物。 本发明还涉及组合产品，包含组合产品和方法的药物组合物用于制备药物组合物的用途。
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