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1.发明授权Crystalline complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(ss-d-glucopyranos-1-yl)-benzene, methods for its preparation and the use thereof for preparing medicaments 有权1-氰基-2-（4-环丙基 - 苄基）-4-（β-D-吡喃葡萄糖-1-基） - 苯的结晶配合物，其制备方法及其制备药物的用途公开(公告)号：US09145434B2
公开(公告)日：2015-09-29
申请号：US13948751
申请日：2013-07-23
Applicant: Matthias Eckhardt , Tanja Butz , Frank Himmelsbach , Hans-Juergen Martin
Inventor： Matthias Eckhardt , Tanja Butz , Frank Himmelsbach , Hans-Juergen Martin
IPC: C07H7/04 , A61K31/70 , C07H15/26 , C07D309/10
CPC classification number: C07H15/26 , C07D309/10 , C07H7/04
Abstract: The invention relates to a crystalline complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(β-D-glucopyranos-1-yl)-benzene and a natural amino acid, to methods for the preparation thereof, as well as to uses thereof for preparing medicaments.
Abstract translation: 本发明涉及1-氰基-2-（4-环丙基 - 苄基）-4-（＆bgr-D-吡喃葡萄糖-1-基） - 苯和天然氨基酸的结晶配合物，其制备方法 ，以及其用于制备药物的用途。
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2.发明申请ARYL-AND HETEROARYLCARBONYL DERIVATIVES OF HEXAHYDROINDENOPYRIDINE AND OCTAHYDROBENZOQUINOLINE 有权四氢呋喃并吡咯啉的亚芳基和异丁烯基衍生物公开(公告)号：US20140249174A1
公开(公告)日：2014-09-04
申请号：US14190899
申请日：2014-02-26
Applicant: Matthias Eckhardt , Hans-Juergen Martin , Martin Schuehle , Sandra Sick , Bing Shiou Yang
Inventor： Matthias Eckhardt , Hans-Juergen Martin , Martin Schuehle , Sandra Sick , Bing Shiou Yang
IPC: C07D401/06
CPC classification number: C07D401/06
Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
Abstract translation: 本发明涉及由式I定义的化合物，其中变量R1，R2，R3，R4和m如权利要求1所定义，具有有价值的药理学活性。 特别地，化合物是11β-羟基类固醇脱氢酶（HSD）1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，例如代谢疾病，特别是2型糖尿病，肥胖症和 血脂异常
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![2,3-dihydrofuro[2,3-c]pyridines, their use as modulators of the G-protein-coupled receptor GPR119 and pharmaceutical compositions thereof](/abs-image/US/2014/08/19/US08809361B2/abs.jpg.150x150.jpg)
3.发明授权2,3-dihydrofuro[2,3-c]pyridines, their use as modulators of the G-protein-coupled receptor GPR119 and pharmaceutical compositions thereof 有权2,3-二氢呋喃并[2,3-c]吡啶，它们用作G蛋白偶联受体GPR119的调节剂及其药物组合物公开(公告)号：US08809361B2
公开(公告)日：2014-08-19
申请号：US13887887
申请日：2013-05-06
Applicant: Matthias Eckhardt
Inventor： Matthias Eckhardt
IPC: C07D491/20 , A61K31/438
CPC classification number: C07D491/20 , A61K31/438
Abstract: The present invention relates to compounds of general formula I, wherein the groups R1 and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
Abstract translation: 本发明涉及通式I的化合物，其中基团R1和A如本申请中所定义，其具有有价值的药理学性质，特别是与GPR119受体结合并调节其活性。
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4.发明申请CRYSTALLINE COMPLEX OF 1-CYANO-2-(4-CYCLOPROPYL-BENZYL)-4-(SS- D-GLUCOPYRANOS-1-YL)-BENZENE, METHODS FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS 有权1-氰基-2-（4-环丙基苯基）-4-（SS-D-吡喃葡萄糖-1-基）苯基的晶体复合物，其制备方法及其制备用途的用途公开(公告)号：US20140031540A1
公开(公告)日：2014-01-30
申请号：US13948751
申请日：2013-07-23
Applicant: Matthias ECKHARDT , Tanja BUTZ , Frank HIMMELSBACH , Hans-Juergen MARTIN
Inventor： Matthias ECKHARDT , Tanja BUTZ , Frank HIMMELSBACH , Hans-Juergen MARTIN
IPC: C07H15/26
CPC classification number: C07H15/26 , C07D309/10 , C07H7/04
Abstract: The invention relates to a crystalline complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(β-D-glucopyranos-1-yl)-benzene and a natural amino acid, to methods for the preparation thereof, as well as to uses thereof for preparing medicaments.
Abstract translation: 本发明涉及1-氰基-2-（4-环丙基 - 苄基）-4-（β-D-吡喃葡萄糖-1-基） - 苯和天然氨基酸的结晶配合物，其制备方法， 以及其用于制备药物的用途。
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公开(公告)号：US08569292B2
公开(公告)日：2013-10-29
申请号：US12990306
申请日：2009-04-30
Applicant: David A. Claremon , Linghang Zhuang , Katerina Leftheris , Colin M. Tice , Zhenrong Xu , Yuanjie Ye , Suresh B. Singh , Salvacion Cacatian , Frank Himmelsbach , Matthias Eckhardt , Wei Zhao
Inventor： David A. Claremon , Linghang Zhuang , Katerina Leftheris , Colin M. Tice , Zhenrong Xu , Yuanjie Ye , Suresh B. Singh , Salvacion Cacatian , Frank Himmelsbach , Matthias Eckhardt , Wei Zhao
IPC: C07D413/10 , C07D413/14 , A61K31/5355
CPC classification number: C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
Abstract: This invention relates to novel compounds of the Formula I, Ik, Iq1-21, Ir1-21, Is1-21, It1-7, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
Abstract translation: 本发明涉及式I，Ik，Iq1-21，Ir1-21，Is1-21，It1-7，其药学上可接受的盐及其药物组合物的新型化合物，其可用于治疗与 哺乳动物中11β-HSD1的调节或抑制。 本发明进一步涉及新化合物的药物组合物及其用于减少或控制细胞中皮质醇产生或抑制细胞中可的松转化为皮质醇的方法。
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Patent Agency Ranking
公开(公告)号：US20130252937A1
公开(公告)日：2013-09-26
申请号：US13803237
申请日：2013-03-14
Applicant: Matthias ECKHARDT , Sara FRATTINI , Dieter HAMPRECHT , Frank HIMMELSBACH , Elke LANGKOPF , Iain LINGARD , Stefan PETERS , Holger WAGNER
Inventor： Matthias ECKHARDT , Sara FRATTINI , Dieter HAMPRECHT , Frank HIMMELSBACH , Elke LANGKOPF , Iain LINGARD , Stefan PETERS , Holger WAGNER
IPC: 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 classification number: 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
Abstract: 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.
Abstract translation: 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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7.发明申请Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions 审中-公开黄嘌呤衍生物，其制备及其作为药物组合物的用途公开(公告)号：US20120252783A1
公开(公告)日：2012-10-04
申请号：US13523939
申请日：2012-06-15
Applicant: Frank HIMMELSBACH , Michael MARK , Matthias ECKHARDT , Elke LANGKOPF , Roland MAIER , Ralf LOTZ
Inventor： Frank HIMMELSBACH , Michael MARK , Matthias ECKHARDT , Elke LANGKOPF , Roland MAIER , Ralf LOTZ
IPC: A61K31/522 , A61K31/55 , A61P3/10 , A61K31/5377 , A61P3/04 , C07D473/08 , C07D473/06
CPC classification number: C07D473/08 , C07D473/04 , C07D473/06 , C07D473/10 , C07D473/12
Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
Abstract translation: 本发明涉及通式为其中R1至R4如本文所定义的取代黄嘌呤，其互变异构体及其立体异构体，其混合物，其前体药物及其盐具有有价值的药理学性质，特别是对 酶二肽肽酶-IV（DPP-IV）。
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![8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2012/08/16/US20120208831A1/abs.jpg.150x150.jpg)
公开(公告)号：US20120208831A1
公开(公告)日：2012-08-16
申请号：US13448495
申请日：2012-04-17
Applicant: Frank HIMMELSBACH , Elke LANGKOPF , Matthias ECKHARDT , Michael MARK , Roland MAIER , Ralf R. H. LOTZ , Mohammad TADAYYON
Inventor： Frank HIMMELSBACH , Elke LANGKOPF , Matthias ECKHARDT , Michael MARK , Roland MAIER , Ralf R. H. LOTZ , Mohammad TADAYYON
CPC classification number: C07D473/04 , C07D473/06 , C07D473/08 , C07D519/00
Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
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9.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
Applicant: Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
Inventor： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
IPC: 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 classification number: 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
Abstract: 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.
Abstract translation: 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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![8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2012/02/21/US08119648B2/abs.jpg.150x150.jpg)
10.发明授权公开(公告)号：US08119648B2
公开(公告)日：2012-02-21
申请号：US12143219
申请日：2008-06-20
Applicant: Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf Lotz
Inventor： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf Lotz
IPC: A61P3/10 , A61P3/04 , A61P19/02 , C07D473/06 , C07D519/00 , A61K31/53
CPC classification number: C07D473/04 , C07D473/06 , C07D473/08 , C07D519/00
Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
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