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公开(公告)号：US20100303728A1
公开(公告)日：2010-12-02
申请号：US12695604
申请日：2010-01-28
IPC分类号： A61K49/00 , C07K7/06 , C07D487/04 , C08G69/48
CPC分类号： C12Q1/37 , G01N33/542 , G01N2333/96466
摘要： The present invention relates to molecular probes of formula (I) {L1-R1-L}n-A-CO—NH—R2-L2 (I) as defined herein that allow for the observation of the catalytic activity of a selected caspase in in vitro assays, in cells or in multicellular organisms, a method for their preparation and the use thereof.
摘要翻译： 本发明涉及如本文所定义的式（I）{L1-R1-L} nA-CO-NH-R2-L2（I）的分子探针，其允许在体外观察所选半胱天冬酶的催化活性 测定，在细胞或多细胞生物体中，其制备方法及其用途。
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2.发明授权Acyl-4-carboxyphenylurea derivatives, processes for preparing them and their use 有权酰基-4-羧基苯基脲衍生物，其制备方法及其用途公开(公告)号：US07223796B2
公开(公告)日：2007-05-29
申请号：US10410601
申请日：2003-04-10
申请人： Elisabeth Defossa , Dieter Kadereit , Karl Schoenafinger , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt , Erich Von Roedern , Alfons Enhsen , Joerg Rieke-Zapp
发明人： Elisabeth Defossa , Dieter Kadereit , Karl Schoenafinger , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt , Erich Von Roedern , Alfons Enhsen , Joerg Rieke-Zapp
IPC分类号： A61K31/24 , C07C265/30 , C07C275/06 , C07D207/04 , C07D263/34
CPC分类号： C07D295/155 , C07C275/54
摘要： The invention relates to acyl-4-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives.The invention particularly relates to compounds of formula I, in which the radicals have the given meanings described herein, and to their physiologically tolerated salts and processes for preparing them. The compounds are, for example, suitable for use as antidiabetics.
摘要翻译： 本发明涉及酰基-4-羧基苯基脲衍生物及其生理上耐受的盐和生理功能衍生物。 本发明特别涉及式I化合物，其中基团具有本文所述的给定含义，以及其生理学上耐受的盐及其制备方法。 化合物例如适合用作抗糖尿病药。
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公开(公告)号：US20110059018A1
公开(公告)日：2011-03-10
申请号：US12860544
申请日：2010-08-20
IPC分类号： A61K49/00 , C07D295/215 , C07D295/155 , C07D487/04 , C07D413/12 , C07D495/04 , C07D311/82 , C07D403/06 , C12Q1/02 , G01N21/00
CPC分类号： C07D295/215 , C07D209/14 , C07D311/82 , C07D487/04 , C07D495/04
摘要： The present invention relates to molecular probes of the formula (I) L1-R1-L-A-X (I) as defined herein that allow for the observation of the catalytic activity of a selected caspase, cathepsin, MMP and carboxypeptidase in in vitro assays, in cells or in multicellular organisms, a method for their preparation and the use thereof.
摘要翻译： 本发明涉及如本文所定义的式（I）L1-R1-LAX（I）的分子探针，其允许在体外测定中观察细胞中所选择的胱天蛋白酶，组织蛋白酶，MMP和羧肽酶的催化活性 或多细胞生物体，其制备方法及其用途。
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4.发明授权Heterocyclically substituted 7-amino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments 有权杂环取代的7-氨基-4-喹诺酮-3-羧酸衍生物，其制备方法及其作为药物的用途公开(公告)号：US07498341B2
公开(公告)日：2009-03-03
申请号：US11042589
申请日：2005-01-25
申请人： Elisabeth Defossa , Dieter Kadereit , Sven Ruf , Thomas Klabunde , Dieter Schmoll , Andreas Herling , Karl-Ulrich Wendt
发明人： Elisabeth Defossa , Dieter Kadereit , Sven Ruf , Thomas Klabunde , Dieter Schmoll , Andreas Herling , Karl-Ulrich Wendt
IPC分类号： A61K31/4375
CPC分类号： C07D215/56 , C07D401/12 , C07D417/12 , C07D471/04
摘要： The invention relates to heterocyclically substituted 7-amino-4-quinolone-3-carboxylic acid derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof.The invention relates to compounds of the formula I in which the radicals have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example as medicaments for the prevention and treatment of type 2 diabetes.
摘要翻译： 本发明涉及杂环取代的7-氨基-4-喹诺酮-3-羧酸衍生物及其生理上耐受的盐和生理功能衍生物。 本发明涉及其中基团具有所述含义的式I化合物及其生理上耐受的盐。 该化合物适用于例如用于预防和治疗2型糖尿病的药物。
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5.发明申请7-phenylamino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments 有权7-苯基氨基-4-喹诺酮-3-羧酸衍生物，其制备方法及其作为药物的用途公开(公告)号：US20050182085A1
公开(公告)日：2005-08-18
申请号：US11042023
申请日：2005-01-25
申请人： Elisabeth Defossa , Dieter Kadereit , Sven Ruf , Thomas Klabunde , Dieter Schmoll , Andreas Herling , Karl-Ulrich Wendt
发明人： Elisabeth Defossa , Dieter Kadereit , Sven Ruf , Thomas Klabunde , Dieter Schmoll , Andreas Herling , Karl-Ulrich Wendt
IPC分类号： A61K31/4709 , A61K31/4745 , C07D215/36 , C07D471/02
CPC分类号： C07D215/56 , C07D401/06 , C07D471/04
摘要： 7-Phenylamino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments The invention relates to 7-phenylamino-4-quinolone-3-carboxylic acid derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. The invention relates to compounds of the formula I in which the radicals have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example as medicaments for the prevention and treatment of type 2 diabetes.
摘要翻译： 7-苯基氨基-4-喹诺酮-3-羧酸衍生物，其制备方法及其作为药物的用途本发明涉及7-苯基氨基-4-喹诺酮-3-羧酸衍生物以及生理上耐受的盐和生理功能衍生物 其中。 本发明涉及其中基团具有所述含义的式I化合物及其生理上耐受的盐。 该化合物适用于例如用于预防和治疗2型糖尿病的药物。
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6.发明授权Cycloalkyl-substituted 7-amino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments 有权环烷基取代的7-氨基-4-喹诺酮-3-羧酸衍生物，其制备方法及其作为药物的用途公开(公告)号：US07470706B2
公开(公告)日：2008-12-30
申请号：US11042770
申请日：2005-01-25
申请人： Elisabeth Defossa , Dieter Kadereit , Thomas Klabunde , Dieter Schmoll , Andreas Herling , Karl-Ulrich Wendt , Sven Ruf
发明人： Elisabeth Defossa , Dieter Kadereit , Thomas Klabunde , Dieter Schmoll , Andreas Herling , Karl-Ulrich Wendt , Sven Ruf
IPC分类号： A61K31/4375
CPC分类号： C07D471/04 , C07D215/36
摘要： The invention relates to cycloalkyl-substituted 7-amino-4-quinolone-3-carboxylic acid derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof.The invention relates to compounds of the formula I in which the radicals have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example as medicaments for the prevention and treatment of type 2 diabetes.
摘要翻译： 本发明涉及环烷基取代的7-氨基-4-喹诺酮-3-羧酸衍生物及其生理上耐受的盐和生理功能衍生物。 本发明涉及其中基团具有所述含义的式I化合物及其生理上可耐受的盐。 该化合物适用于例如用于预防和治疗2型糖尿病的药物。
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7.发明授权7-Phenylamino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments 有权7-苯基氨基-4-喹诺酮-3-羧酸衍生物，其制备方法及其作为药物的用途公开(公告)号：US07402674B2
公开(公告)日：2008-07-22
申请号：US11042023
申请日：2005-01-25
申请人： Elisabeth Defossa , Dieter Kadereit , Sven Ruf , Thomas Klabunde , Dieter Schmoll , Andreas Herling , Karl-Ulrich Wendt
发明人： Elisabeth Defossa , Dieter Kadereit , Sven Ruf , Thomas Klabunde , Dieter Schmoll , Andreas Herling , Karl-Ulrich Wendt
IPC分类号： C07D471/02 , C07D215/38 , A61K31/44 , A61K31/47
CPC分类号： C07D215/56 , C07D401/06 , C07D471/04
摘要： 7-Phenylamino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicamentsThe invention relates to 7-phenylamino-4-quinolone-3-carboxylic acid derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof.The invention relates to compounds of the formula I in which the radicals have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example as medicaments for the prevention and treatment of type 2 diabetes.
摘要翻译： 7-苯基氨基-4-喹诺酮-3-羧酸衍生物，其制备方法及其作为药物的用途本发明涉及7-苯基氨基-4-喹诺酮-3-羧酸衍生物以及生理上耐受的盐和生理功能衍生物 其中。 本发明涉及其中基团具有所述含义的式I化合物及其生理上耐受的盐。 该化合物适用于例如用于预防和治疗2型糖尿病的药物。
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8.发明授权Heterocyclically substituted benzoylureas, process for their preparation and their use as pharmaceuticals 有权杂环取代的苯甲酰脲，其制备方法及其作为药物的用途公开(公告)号：US07138414B2
公开(公告)日：2006-11-21
申请号：US10617498
申请日：2003-07-11
申请人： Karl Schoenafinger , Elisabeth Defossa , Dieter Kadereit , Erich Von Roedern , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt
发明人： Karl Schoenafinger , Elisabeth Defossa , Dieter Kadereit , Erich Von Roedern , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt
IPC分类号： C07D235/02 , C07D251/00 , A61K31/395 , A61K31/445
CPC分类号： C07D211/60 , C07D211/62 , C07D231/12 , C07D231/26 , C07D233/56 , C07D235/18 , C07D249/08 , C07D249/12 , C07D253/07 , C07D257/04 , C07D271/10 , C07D271/113 , C07D307/68
摘要： The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives.Compounds are described of the formula I where the radicals are defined as specified, and also their pharmaceutically acceptable salts and processes for their preparation. The compounds are suitable, for example, for treating type 2 diabetes.
摘要翻译： 本发明涉及杂环取代的苯甲酰脲，也涉及其生理上耐受的盐和生理功能衍生物。 化合物描述为其中基团被定义为特定的式I，以及它们的药学上可接受的盐及其制备方法。 该化合物适用于例如治疗2型糖尿病。
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公开(公告)号：US07078404B2
公开(公告)日：2006-07-18
申请号：US10410892
申请日：2003-04-10
申请人： Elisabeth Defossa , Dieter Kadereit , Karl Schoenafinger , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt , Erich Von Roedern , Alfons Enhsen
发明人： Elisabeth Defossa , Dieter Kadereit , Karl Schoenafinger , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt , Erich Von Roedern , Alfons Enhsen
IPC分类号： A61K31/50 , C07D241/04 , C07D263/32 , C07D307/06 , C07C243/09
CPC分类号： C07C275/54
摘要： The invention relates to acyl-3-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives.The invention relates to compounds of formula I, in which the radicals have the given meanings, and to their physiologically tolerated salts and processes for preparing them. The compounds are, for example, suitable for use as antidiabetics.
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10.发明授权Urea- and urethane-substituted acylureas, process for their preparation and their use 有权尿素和氨基甲酸酯取代的酰基脲，其制备方法及其用途公开(公告)号：US08247452B2
公开(公告)日：2012-08-21
申请号：US11845242
申请日：2007-08-27
申请人： Elisabeth DeFossa , Dieter Kadereit , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt , Erich Von Roedern , Karl Schoenafinger
发明人： Elisabeth DeFossa , Dieter Kadereit , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt , Erich Von Roedern , Karl Schoenafinger
IPC分类号： C07C275/24 , A61K31/277
CPC分类号： C07C275/54 , C07D213/75 , C07D239/96 , C07D295/135
摘要： The invention relates to urea- and urethane-substituted acylureas and to their physiologically tolerated salts and physiologically functional derivatives. In particular, the invention relates to the compounds of the formula I wherein the radicals have meanings described herein, and to their physiologically tolerated salts and to processes for their preparation. The compounds are suitable for example as antidiabetics.
摘要翻译： 本发明涉及脲和氨基甲酸酯取代的酰基脲及其生理上耐受的盐和生理功能衍生物。 特别地，本发明涉及式I化合物，其中基团具有本文所述的含义及其生理学耐受的盐及其制备方法。 该化合物例如适用于抗糖尿病药。
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