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1.发明授权Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation 有权三环吡啶衍生物，含有此类化合物的药物，其用途及其制备方法公开(公告)号：US08703793B2
公开(公告)日：2014-04-22
申请号：US12920722
申请日：2009-03-02
申请人： Holger Wagner , Daniela Berta , Riccardo Giovannini , Alessandro Mazzacani , Ruediger Streicher , Klaus Fuchs
发明人： Holger Wagner , Daniela Berta , Riccardo Giovannini , Alessandro Mazzacani , Ruediger Streicher , Klaus Fuchs
IPC分类号： A61K31/4355 , C07D491/048
CPC分类号： C07D493/04 , C07D493/10
摘要： Compounds of formula (I) wherein the groups R1 to R8 have the meanings indicated in the description, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof have valuable pharmacological properties, which make them useful for the treatment of cardiovascular and related disorders.
摘要翻译： 式（I）的化合物，其中基团R 1至R 8具有说明书中所述的含义，互变异构体，立体异构体，其混合物及其盐具有有价值的药理学性质，使其可用于治疗心血管和相关疾病 。
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2.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，含有此类化合物的药物，其用途及其制备方法公开(公告)号：US20110021550A1
公开(公告)日：2011-01-27
申请号：US12920722
申请日：2009-03-02
申请人： Holger Wagner , Daniela Berta , Riccardo Giovannini , Alessandro Mazzacani , Ruediger Streicher , Klaus Fuchs
发明人： Holger Wagner , Daniela Berta , Riccardo Giovannini , Alessandro Mazzacani , Ruediger Streicher , Klaus Fuchs
IPC分类号： A61K31/438 , C07D491/04 , C07D491/10 , A61K31/4355 , A61P9/10
CPC分类号： C07D493/04 , C07D493/10
摘要： Compounds of formula (I) wherein the groups R1 to R8 have the meanings indicated in the description, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof have valuable pharmacological properties, which make them useful for the treatment of cardiovascular and related disorders.
摘要翻译： 式（I）化合物，其中基团R 1至R 8具有说明书中所述的含义，互变异构体，立体异构体，其混合物及其盐具有有价值的药理学性质，使其可用于治疗心血管和相关疾病 。
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3.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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4.发明授权Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation 有权三环吡啶衍生物，含有此类化合物的药物，其用途及其制备方法公开(公告)号：US09029544B2
公开(公告)日：2015-05-12
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： C07D491/20 , A61K31/506 , C07D491/048 , C07D491/04 , C07D215/56
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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5.发明申请ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS 有权芳基磺酰氨基乙基磷酸衍生物，其制备方法及其作为药物组合物的用途公开(公告)号：US20100261677A1
公开(公告)日：2010-10-14
申请号：US12676319
申请日：2008-09-04
申请人： Elke Langkopf , Alexander Pautsch , Corinna Schoelch , Annette Schuler-Metz , Ruediger Streicher , Holger Wagner
发明人： Elke Langkopf , Alexander Pautsch , Corinna Schoelch , Annette Schuler-Metz , Ruediger Streicher , Holger Wagner
IPC分类号： A61K31/675 , C07F9/28 , A61K31/662 , A61P3/10
CPC分类号： C07D215/38 , C07D217/22 , C07D219/08 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/72 , C07D239/74 , C07D241/42 , C07D263/56 , C07D277/66 , C07D471/04
摘要： The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament 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）的取代芳基磺酰基氨基甲基膦酸衍生物，其中基团Ra至Rf，A和Z定义如说明书和权利要求中所述，其适用于制备用于治疗代谢紊乱的药物，特别是类型 1或2型糖尿病。
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6.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：US08211923B2
公开(公告)日：2012-07-03
申请号：US12669979
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 , C07D277/62 , C07D263/54 , C07D235/04 , C07D231/56 , C07D209/04
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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7.发明申请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乙基磷酸衍生物，其制备及其在治疗I型和II型糖尿病的用途公开(公告)号：US20100210595A1
公开(公告)日：2010-08-19
申请号：US12669979
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 , C07F9/572 , C07F9/6541 , C07F9/653 , C07F9/6533 , C07F9/6558 , A61K31/683 , C07F9/59 , C07F9/6509 , 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.
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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8.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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9.发明授权Arylsulfonylaminomethylphosphonic acid derivatives, the preparation thereof and the use thereof as pharmaceutical compositions 有权芳基磺酰氨基甲基膦酸衍生物，其制备方法及其作为药物组合物的用途公开(公告)号：US08163911B2
公开(公告)日：2012-04-24
申请号：US12676319
申请日：2008-09-04
申请人： Elke Langkopf , Alexander Pautsch , Corinna Schoelch , Annette Schuler-Metz , Ruediger Streicher , Holger Wagner
发明人： Elke Langkopf , Alexander Pautsch , Corinna Schoelch , Annette Schuler-Metz , Ruediger Streicher , Holger Wagner
IPC分类号： C07F9/28
CPC分类号： C07D215/38 , C07D217/22 , C07D219/08 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/72 , C07D239/74 , C07D241/42 , C07D263/56 , C07D277/66 , C07D471/04
摘要： The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament 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）的取代芳基磺酰基氨基甲基膦酸衍生物，其中基团Ra至Rf，A和Z定义如说明书和权利要求中所述，其适用于制备用于治疗代谢紊乱的药物，特别是类型 1或2型糖尿病。
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10.发明申请SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS 有权取代的氨基磺酰胺，其制备方法及其作为药物组合物的用途公开(公告)号：US20100130557A1
公开(公告)日：2010-05-27
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： A61K31/404 , A61K31/4439 , A61K31/403 , C07D401/12 , C07D209/82 , C07D209/04 , A61P3/10
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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