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公开(公告)号：US09492436B2
公开(公告)日：2016-11-15
申请号：US14331359
申请日：2014-07-15
IPC分类号： C07D471/02 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/541 , A61K45/06 , C07D493/04 , C07D519/00
CPC分类号： A61K31/437 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/541 , A61K45/06 , C07D493/04 , C07D519/00
摘要： The present invention relates to compounds of general formula I, wherein the group R1, R2, X and Y are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
摘要翻译： 本发明涉及通式I的化合物，其中R1，R2，X和Y基团如权利要求1中所定义，其具有有价值的药理学性质，特别是结合AMP活化蛋白激酶（AMPK）并调节其 活动。 该化合物适用于治疗和预防可受该受体影响的疾病，如代谢疾病，特别是2型糖尿病。
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![Furo[3,4-c]quinoline derivatives, medicaments containing such compounds, their use and process for their preparation](/abs-image/US/2015/10/06/US09150583B2/abs.jpg.150x150.jpg)
2.发明授权Furo[3,4-c]quinoline derivatives, medicaments containing such compounds, their use and process for their preparation 有权呋喃并[3,4-c]喹啉衍生物，含有这些化合物的药物，其用途和制备方法公开(公告)号：US09150583B2
公开(公告)日：2015-10-06
申请号：US13586977
申请日：2012-08-16
IPC分类号： C07D491/20 , A61K31/4747 , A61K45/06
CPC分类号： C07D491/20 , A61K31/4747 , A61K45/06
摘要： The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this protein.
摘要翻译： 本发明涉及由式I定义的化合物，其中变量R1-R8如描述中所定义，具有有价值的药理学活性。 特别地，化合物是胆固醇酯转移蛋白（CETP）的抑制剂，因此适用于治疗和预防可受该蛋白质抑制影响的疾病。
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公开(公告)号：US20130252937A1
公开(公告)日：2013-09-26
申请号：US13803237
申请日：2013-03-14
申请人： Matthias ECKHARDT , Sara FRATTINI , Dieter HAMPRECHT , Frank HIMMELSBACH , Elke LANGKOPF , Iain LINGARD , Stefan PETERS , Holger WAGNER
发明人： Matthias ECKHARDT , Sara FRATTINI , Dieter HAMPRECHT , Frank HIMMELSBACH , Elke LANGKOPF , Iain LINGARD , Stefan PETERS , Holger WAGNER
IPC分类号： C07D405/12 , A61K31/343 , C07D307/80 , A61K31/351 , A61K31/506 , C07D413/12 , A61K31/422 , A61K31/4155 , A61K31/443 , A61K31/397 , C07D409/12 , A61K31/382 , C07D417/12 , A61K31/427 , A61K31/541 , A61K31/4025 , A61K31/4196 , A61K31/513 , A61K31/501 , A61K31/41 , C07D405/14 , A61K31/497 , C07D413/14 , A61K31/553 , A61K31/5377 , A61K31/4178 , A61K31/4245 , A61K45/06 , C07D407/12
CPC分类号： C07D405/12 , A61K31/343 , A61K31/351 , A61K31/382 , A61K31/397 , A61K31/4025 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/443 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/553 , A61K45/06 , C07D307/80 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
摘要翻译： 本发明涉及通式I的化合物，其中R1，R2和m基团如权利要求1中所定义，其具有有价值的药理学性质，特别是与GPR40受体结合并调节其活性。 该化合物适用于治疗和预防可受该受体影响的疾病，如代谢疾病，特别是2型糖尿病。
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公开(公告)号：US08531751B2
公开(公告)日：2013-09-10
申请号：US13213360
申请日：2011-08-19
IPC分类号： G02B26/08
CPC分类号： G02F1/11 , G02B26/124 , G02B27/0955 , G02B27/30 , H04N1/04 , H04N1/0408 , H04N1/0443
摘要： A direct imaging system comprises an illumination unit comprising a plurality of light sources, the plurality of light sources configured to emit a plurality of beams, an optical system for forming the plurality of beams to be aligned in position or angle, an acoustic optical modulator positioned to receive the plurality of beams aligned in one of position or angle and to consecutively diffract different portions of the plurality of beams as an acoustic wave propagates in an acoustic direction, and a scanning element adapted to scan an exposure plane with the plurality of beams modulated by the acoustic optical modulator at a scanning velocity, wherein the scanning velocity is selected to incoherently unite the different portions of the plurality of beams into a single exposure spot.
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5.发明申请公开(公告)号：US20130053404A1
公开(公告)日：2013-02-28
申请号：US13397855
申请日：2012-02-16
申请人： Holger Wagner , Daniela Berta , Klaus Fuchs , Riccardo Giovannini , Dieter Wolfgang Hamprecht , Ingo Konetzki , Ruediger Streicher , Thomas Trieselmann
发明人： Holger Wagner , Daniela Berta , Klaus Fuchs , Riccardo Giovannini , Dieter Wolfgang Hamprecht , Ingo Konetzki , Ruediger Streicher , Thomas Trieselmann
IPC分类号： C07D491/048 , A61K31/4747 , A61K31/506 , C07D491/20 , A61P9/10 , C07D221/20 , A61P9/00 , A61P3/00 , A61P3/06 , A61K31/4741 , C07D215/56
CPC分类号： C07D491/048 , C07D491/107 , C07D491/18
摘要： The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
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6.发明授权Substituted arylsulphonylglycines, the preparation thereof and the use thereof as pharmaceutical compositions 有权取代的芳基磺酰基甘氨酸，其制备方法及其作为药物组合物的用途公开(公告)号：US08232312B2
公开(公告)日：2012-07-31
申请号：US12530507
申请日：2008-03-14
申请人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
发明人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/428 , A61K31/4184 , A61K31/416 , A61K31/404 , C07D413/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D277/64 , C07D333/60 , C07D235/26 , C07D235/08 , C07D231/56 , C07D209/42 , C07D209/08 , C07D209/88
CPC分类号： C07D209/08 , C07D209/18 , C07D209/42 , C07D209/88 , C07D231/56 , C07D235/06 , C07D235/26 , C07D277/64 , C07D333/68 , C07D333/70 , C07D401/12 , C07D403/06 , C07D403/12 , C07F7/0812
摘要： The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及通式（I）的取代芳基磺酰基甘氨酸，其中R，X，Y和Z如权利要求1所定义，其互变异构体，对映异构体，非对映体，其混合物及其盐具有有价值的药理学性质，特别是抑制 的糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，以及它们作为药物组合物的用途。
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7.发明申请公开(公告)号：US20120053197A1
公开(公告)日：2012-03-01
申请号：US13029690
申请日：2011-02-17
申请人： Holger WAGNER , Daniela BERTA , Klaus FUCHS , Riccardo GIOVANNINI , Dieter Wolfgang HAMPRECHT , Ingo KONETZKI , Ruediger STREICHER , Thomas TRIESELMANN
发明人： Holger WAGNER , Daniela BERTA , Klaus FUCHS , Riccardo GIOVANNINI , Dieter Wolfgang HAMPRECHT , Ingo KONETZKI , Ruediger STREICHER , Thomas TRIESELMANN
IPC分类号： A61K31/4355 , C07D491/20 , A61P3/00 , C07D215/56 , A61P9/00 , C07D491/107
CPC分类号： C07D491/04 , A61K31/506 , C07D215/56 , C07D491/20
摘要： The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
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8.发明申请TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION 有权三环吡啶衍生物，含有这些化合物的药物，其使用及其制备方法公开(公告)号：US20120046304A1
公开(公告)日：2012-02-23
申请号：US13029697
申请日：2011-02-17
申请人： Holger WAGNER , Daniela BERTA , Klaus FUCHS , Riccardo GIOVANNINI , Dieter Wolfgang HAMPRECHT , Ingo KONETZKI , Ruediger STREICHER , Thomas TRIESELMANN
发明人： Holger WAGNER , Daniela BERTA , Klaus FUCHS , Riccardo GIOVANNINI , Dieter Wolfgang HAMPRECHT , Ingo KONETZKI , Ruediger STREICHER , Thomas TRIESELMANN
IPC分类号： A61K31/506 , A61K31/4355 , C07D491/20 , C07D215/56 , A61P3/00 , A61P9/10 , A61P3/06 , C07D491/048 , A61P9/00
CPC分类号： C07D491/04 , A61K31/506 , C07D215/56 , C07D491/20
摘要： The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
摘要翻译： 本发明涉及由式I定义的化合物，其中变量R1-R8如描述中所定义，具有有价值的药理学活性。 特别地，化合物是胆固醇酯转移蛋白（CETP）的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病。
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9.发明授权Substituted, bicyclic 8-pyrrolidinoxanthines, and methods for their use as inhibitors of dipeptidyl peptidase 有权取代的双环8-吡咯烷基亚基黄嘌呤及其作为二肽基肽酶抑制剂的方法公开(公告)号：US07888343B2
公开(公告)日：2011-02-15
申请号：US11624511
申请日：2007-01-18
申请人： Karl Schoenafinger , Gerhard Jaehne , Elisabeth Defossa , Lothar Schwink , Holger Wagner , Christian Buning , Georg Tschank , Ulrich Werner
发明人： Karl Schoenafinger , Gerhard Jaehne , Elisabeth Defossa , Lothar Schwink , Holger Wagner , Christian Buning , Georg Tschank , Ulrich Werner
IPC分类号： C07D519/00 , A61K31/522 , A61P3/06 , A61P3/10 , C07D471/04 , C07D487/04
CPC分类号： C07D519/00
摘要： The present invention involves substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are defined herein. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds and methods for the treatment of metabolic disorders such as type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerosis diseases and the like through the administration of said compositions.
摘要翻译： 本发明涉及取代的双环8-吡咯烷基亚基黄嘌呤及其式I的衍生物：其中各种R基团在本文中定义。 本发明还包括包含它们的药物组合物以及这些化合物的制备方法和通过施用所述组合物治疗代谢紊乱如2型糖尿病，胰岛素抵抗，高血糖症，动脉硬化疾病等的方法 。
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10.发明授权Cyanopyrrolidides, process for their preparation and their use as medicaments 有权氰基吡咯烷酮，其制备过程及其作为药物的用途公开(公告)号：US07094800B2
公开(公告)日：2006-08-22
申请号：US10898752
申请日：2004-07-26
申请人： Karl Schoenafinger , Holger Wagner , Gerhard Jaehne , Holger Gaul , Christian Buning , Georg Tschank , Ulrich Werner
发明人： Karl Schoenafinger , Holger Wagner , Gerhard Jaehne , Holger Gaul , Christian Buning , Georg Tschank , Ulrich Werner
IPC分类号： A61K31/40 , A61K31/4439 , C07D209/02 , C07D401/02
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the formula I in which the radicals have the meanings stated in the text, their stereoisomeric forms, and their physiologically tolerated salts, physiologically functional derivatives and process for their preparation. The compounds are suitable for the treatment of disorders of metabolism, such as type 2 diabetes.
摘要翻译： 本发明涉及式I化合物，其中基团具有文中所述的含义，它们的立体异构形式及其生理学上可耐受的盐，生理功能衍生物及其制备方法。 该化合物适用于治疗代谢紊乱，如2型糖尿病。
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