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公开(公告)号：US08946438B2
公开(公告)日：2015-02-03
申请号：US14196436
申请日：2014-03-04
申请人： Holger Wagner , Elke Langkopf , Frank Himmelsbach , Rolf Goeggel , Birgit Jung
发明人： Holger Wagner , Elke Langkopf , Frank Himmelsbach , Rolf Goeggel , Birgit Jung
IPC分类号： C07D213/30 , C07D401/06 , C07D413/06 , A61K31/44 , A61K31/4427 , A61P11/00 , A61P11/06 , C07D403/04 , C07D213/68 , C07D213/74 , C07D213/89 , C07D239/42 , C07D401/04 , C07D401/12 , C07D239/24 , C07D239/34 , C07D239/46 , C07D239/47 , A61K31/505 , A61K31/506
CPC分类号： C07D403/04 , C07D213/68 , C07D213/74 , C07D213/89 , C07D239/34 , C07D239/42 , C07D239/46 , C07D401/04 , C07D401/06 , C07D401/12
摘要： Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
摘要翻译： 通式I的杂芳氧基取代的苯甲酸酰胺，其中基团R 1至R 7以及X和Y如权利要求1所定义，包括互变异构体，立体异构体，其混合物和盐。 根据本发明的化合物适合于治疗呼吸道疾病，特别是COPD和哮喘。
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公开(公告)号：US08809376B2
公开(公告)日：2014-08-19
申请号：US13869144
申请日：2013-04-24
IPC分类号： A61K31/44 , C07D307/87
CPC分类号： C07D307/80 , A61K31/343 , A61K31/443 , A61K45/06 , C07D405/12 , A61K2300/00
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.
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公开(公告)号：US08778926B2
公开(公告)日：2014-07-15
申请号：US13354356
申请日：2012-01-20
申请人： Frank Himmelsbach , Elke Langkopf , Bernd Nosse
发明人： Frank Himmelsbach , Elke Langkopf , Bernd Nosse
IPC分类号： A61K31/506 , C07D491/048 , C07D413/14 , C07D407/14
CPC分类号： C07D407/14 , C07D413/14 , C07D491/048
摘要： The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
摘要翻译： 本发明涉及通式I的化合物，其中基团R1，LP，LQ，X1，X2，X3，A，n和m如申请中所定义。 式I化合物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.发明授权Substituted arylsulfonylaminomethylphosphonic acid derivatives, their preparation and their use in the treatment of type I and II diabetes mellitus 有权取代的芳基磺酰氨基甲基膦酸衍生物，其制备及其在治疗I型和II型糖尿病中的应用公开(公告)号：US08357689B2
公开(公告)日：2013-01-22
申请号：US12669978
申请日：2008-07-25
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： A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , C07D237/04 , C07D403/04
CPC分类号： C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65324 , C07F9/6541 , C07F9/655354 , C07F9/65583 , C07F9/65586
摘要： The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula 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： 本发明涉及以下通式的取代芳基磺酰氨基甲基膦酸衍生物其中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， 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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5.发明申请BICYCLIC HETEROCYCLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESSES FOR PREPARING THEM 有权双相异构体，含有这些化合物的药物组合物，其制备方法及其制备方法公开(公告)号：US20120329778A1
公开(公告)日：2012-12-27
申请号：US13603476
申请日：2012-09-05
申请人： Frank HIMMELSBACH , Elke LANGKOPF , Thomas METZ , Flavio SOLCA , Birgit JUNG , Anke BAUM
发明人： Frank HIMMELSBACH , Elke LANGKOPF , Thomas METZ , Flavio SOLCA , Birgit JUNG , Anke BAUM
IPC分类号： A61K31/517 , C07D403/12 , C07D413/12 , C07D417/12 , C07D239/94 , C07D405/12 , C07D405/14 , A61K31/551 , A61K31/5377 , A61K31/541 , A61P35/00 , A61P11/00 , A61P1/00 , A61P1/16 , C07D401/12
CPC分类号： C07D405/12 , C07D215/42 , C07D215/54 , C07D239/94 , C07D401/12
摘要： The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
摘要翻译： 本发明涉及通式的双环杂环，其中R a至R c，A至E和X如权利要求1中所定义，互变异构体，立体异构体和盐，特别是其与无机或有机酸或碱的生理上可接受的盐，其具有 特别是对由酪氨酸激酶介导的信号转导的抑制作用，它们在治疗疾病尤其是肿瘤疾病和肺和气道疾病中的应用及其制备。
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6.发明申请ARYLSULPHONYLGLYCINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS MEDICAMENTS 审中-公开芳基磺酰胺衍生物，其制备方法及其作为药物使用公开(公告)号：US20110269761A1
公开(公告)日：2011-11-03
申请号：US12988452
申请日：2009-04-17
申请人： Elke Langkopf , Frank Himmelsbach , Juergen Mack , Alexander Pautsch , Corinna Schoelch , Annette Schuler-Metz , Ruediger Streicher , Holger Wagner
发明人： Elke Langkopf , Frank Himmelsbach , Juergen Mack , Alexander Pautsch , Corinna Schoelch , Annette Schuler-Metz , Ruediger Streicher , Holger Wagner
IPC分类号： A61K31/5377 , A61K31/277 , C07C271/12 , A61K31/27 , C07C309/65 , C07D271/06 , A61K31/4245 , C07D271/10 , C07D239/02 , A61K31/505 , C07D213/55 , A61K31/44 , C07D295/00 , A61K31/5375 , C07D241/04 , A61K31/495 , C07D215/38 , A61K31/47 , C07D403/04 , A61K31/506 , C07D413/04 , A61P3/10 , C07C255/57
CPC分类号： C07D271/06 , C07C311/21 , C07D213/40 , C07D213/74 , C07D215/40 , C07D239/26 , C07D271/10 , C07D295/108 , C07D295/15 , C07D307/52
摘要： The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
摘要翻译： 本发明涉及通式（I）的取代的芳基 - 磺酰基甘氨酸衍生物，其中基团Ra至Rf，A和Z如说明书和权利要求中所定义，其适于制备用于治疗代谢紊乱的药物组合物，特别是 1型或2型糖尿病。
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公开(公告)号：US20100210594A1
公开(公告)日：2010-08-19
申请号：US12669978
申请日：2008-07-25
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： A61K31/675 , C07F9/6512 , C07F9/572 , C07F9/6509 , C07F9/645 , C07F9/6533 , C07F9/6521 , C07F9/6544 , C07F9/6503 , A61P3/10
CPC分类号： C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65324 , C07F9/6541 , C07F9/655354 , C07F9/65583 , C07F9/65586
摘要： The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula 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.
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8.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：US20100204250A1
公开(公告)日：2010-08-12
申请号：US12767855
申请日：2010-04-27
申请人： Frank HIMMELSBACH , Michael MARK , Matthias ECKHARDT , Elke LANGKOPF , Roland MAIER , Ralf LOTZ
发明人： Frank HIMMELSBACH , Michael MARK , Matthias ECKHARDT , Elke LANGKOPF , Roland MAIER , Ralf LOTZ
IPC分类号： A61K31/522 , C07D473/28 , A61P3/04 , A61P3/08
CPC分类号： C07D473/08 , C07D473/04 , C07D473/06 , C07D473/10 , C07D473/12
摘要： 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).
摘要翻译： 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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9.发明申请IMIDAZOLES AND TRIAZOLES, THEIR PREPARATION, AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS 有权咪唑和三唑，其制备及其作为药物组合物的用途公开(公告)号：US20080312243A1
公开(公告)日：2008-12-18
申请号：US12192589
申请日：2008-08-15
IPC分类号： A61K31/4439 , A61K31/498 , A61P3/10
CPC分类号： C07D471/04 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14
摘要： The present invention relates to imidazoles and triazoles of general formula wherein R1 to R4 and X are defined as in claims 1 to 8, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的咪唑和三唑，其中R 1至R 4和X如权利要求1至8中所定义，互变异构体，对映异构体，非对映异构体，其混合物及其盐具有有价值的药理学性质，特别是 对二肽基肽酶-IV（DPP-IV）的活性具有抑制作用。
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10.发明申请Bicyclic Heterocycles, Pharmaceutical Compositions Containing These Compounds, Their Use and Processes for Preparing Them 审中-公开双环杂环，包含这些化合物的药物组合物，它们的用途和制备方法公开(公告)号：US20070185091A1
公开(公告)日：2007-08-09
申请号：US11734350
申请日：2007-04-12
申请人： Frank Himmelsbach , Elke Langkopf , Thomas Metz , Flavio Solca , Birgit Jung , Anke Baum
发明人： Frank Himmelsbach , Elke Langkopf , Thomas Metz , Flavio Solca , Birgit Jung , Anke Baum
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/4709 , C07D413/02 , C07D403/02
CPC分类号： C07D405/12 , C07D215/42 , C07D215/54 , C07D239/94 , C07D401/12
摘要： The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
摘要翻译： 本发明涉及通式的双环杂环，其中R a至R c，A至E和X如权利要求1所定义，互变异构体，立体异构体及其盐 特别是其具有有价值的药理学特性的无机或有机酸或碱的生理上可接受的盐，特别是对由酪氨酸激酶介导的信号转导的抑制作用，它们在治疗疾病尤其是肿瘤疾病和肺疾病中的用途以及 气道及其制备。
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