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![SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C](/abs-image/US/2014/09/18/US20140275025A1/abs.jpg.150x150.jpg)
11.发明申请SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C 有权取代的2-AZA-BICYCLO [2.2.1]乙酰-3-羧酸（苄基 - 氰基 - 甲基） - CATHEPSIN C的胺抑制剂公开(公告)号：US20140275025A1
公开(公告)日：2014-09-18
申请号：US14205861
申请日：2014-03-12
Applicant: Ralf ANDERSKEWITZ , Florian BINDER , Matthias GRAUERT , Marc GRUNDL , Peter Wilhelm HAEBEL , Thorsten OOST , Alexander PAUTSCH , Stefan PETERS , Viktor VINTONYAK
Inventor： Ralf ANDERSKEWITZ , Florian BINDER , Matthias GRAUERT , Marc GRUNDL , Peter Wilhelm HAEBEL , Thorsten OOST , Alexander PAUTSCH , Stefan PETERS , Viktor VINTONYAK
IPC: C07D209/52 , A61K31/4035 , A61K45/06 , C07D405/12 , A61K31/403 , C07D401/12 , A61K31/438 , A61K31/496 , A61K31/4045 , C07D403/14 , A61K31/4192 , A61K31/4155 , C07D498/04 , A61K31/5383 , A61K31/551 , C07D487/10 , C07D403/12
CPC classification number: A61K31/403 , A61K31/397 , A61K31/4035 , A61K31/404 , A61K31/4045 , A61K31/4155 , A61K31/416 , A61K31/4192 , A61K31/423 , A61K31/438 , A61K31/473 , A61K31/496 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D209/52 , C07D401/10 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D413/14 , C07D417/12 , C07D471/08 , C07D487/10 , C07D498/04 , Y02A50/409
Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
Abstract translation: 本发明涉及式1的2-氮杂 - 双环[2.2.1]庚烷-3-羧酸（苄基 - 氰基 - 甲基） - 酰胺及其作为组织蛋白酶C抑制剂的用途，含有该组合物的药物组合物和方法 使用与用于治疗和/或预防与二肽基肽酶I活性相关的疾病的药剂，例如， 呼吸疾病。
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公开(公告)号：US08232286B2
公开(公告)日：2012-07-31
申请号：US12366248
申请日：2009-02-05
Applicant: Steffen Breitfelder , Udo Maier , Trixi Brandl , Christoph Hoenke , Matthias Grauert , Alexander Pautsch , Matthias Hoffmann , Frank Kalkbrenner , Anne T. Joergensen , Gerhard Schaenze , Stefan Peters , Frank Buettner , Eckhart Bauer
Inventor： Steffen Breitfelder , Udo Maier , Trixi Brandl , Christoph Hoenke , Matthias Grauert , Alexander Pautsch , Matthias Hoffmann , Frank Kalkbrenner , Anne T. Joergensen , Gerhard Schaenze , Stefan Peters , Frank Buettner , Eckhart Bauer
IPC: C07D487/04 , A61K31/519 , A61P11/06 , A61P19/02 , A61P17/06
CPC classification number: C07D513/04 , C07D277/84
Abstract: New compounds of formula 1 are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.
Abstract translation: 提供新的式1化合物，其由于其药物活性，因为PI3-激酶调节剂可用于治疗炎症或过敏性疾病的治疗领域。 这些实例包括炎性和过敏性呼吸道疾病，胃肠道炎症性疾病和运动器官，炎性和过敏性皮肤疾病，炎症性眼病，鼻粘膜疾病，涉及自身免疫反应或炎症的炎性或过敏性疾病 。
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13.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
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: A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , C07D277/62 , C07D263/54 , C07D235/04 , C07D231/56 , C07D209/04
CPC classification number: C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65324 , C07F9/6541 , C07F9/655354 , C07F9/65583 , C07F9/65586
Abstract: 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.
Abstract translation: 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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14.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
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: A61K31/675 , C07F9/572 , C07F9/6541 , C07F9/653 , C07F9/6533 , C07F9/6558 , A61K31/683 , C07F9/59 , C07F9/6509 , A61P3/10
CPC classification number: C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65324 , C07F9/6541 , C07F9/655354 , C07F9/65583 , C07F9/65586
Abstract: 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.
Abstract translation: 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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15.发明申请公开(公告)号：US20100145041A1
公开(公告)日：2010-06-10
申请号：US12706936
申请日：2010-02-17
Applicant: Trixi BRANDL , Udo MAIER , Matthias HOFFMANN , Stefan SCHEUERER , Anne T. JOERGENSEN , Alexander PAUTSCH , Steffen BREITFELDER , Matthias GRAUERT , Christoph HOENKE , Klaus ERB , Michael PIEPER , Ingo PRAGST
Inventor： Trixi BRANDL , Udo MAIER , Matthias HOFFMANN , Stefan SCHEUERER , Anne T. JOERGENSEN , Alexander PAUTSCH , Steffen BREITFELDER , Matthias GRAUERT , Christoph HOENKE , Klaus ERB , Michael PIEPER , Ingo PRAGST
IPC: C07D417/14 , C07D413/14 , C07D513/04 , C07D277/82
CPC classification number: C07D513/04
Abstract: Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing these compounds and their use as pharmaceutical compositions.
Abstract translation: 公开了通式（I）的噻唑基 - 二氢 - 喹唑啉，其中基团R 1至R 4具有权利要求书和说明书中给出的含义，其异构体，以及这些化合物的制备方法及其作为药物组合物的用途。
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Patent Agency Ranking
![Method of using substituted 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C](/abs-image/US/2015/07/07/US09073869B2/abs.jpg.150x150.jpg)
16.发明授权Method of using substituted 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C 有权使用取代的2-氮杂 - 双环[2.2.2]辛烷-3-羧酸（苄基 - 氰基 - 甲基） - 酰胺组织蛋白酶C抑制剂的方法公开(公告)号：US09073869B2
公开(公告)日：2015-07-07
申请号：US14483217
申请日：2014-09-11
Applicant: Ralf Anderskewitz , Matthias Grauert , Marc Grundl , Thorsten Oost , Alexander Pautsch , Stefan Peters
Inventor： Ralf Anderskewitz , Matthias Grauert , Marc Grundl , Thorsten Oost , Alexander Pautsch , Stefan Peters
IPC: A61K31/439 , A61K31/4725 , A61K45/06 , C07D221/22 , C07D401/12 , C07D417/12 , C07D453/06
CPC classification number: C07D221/22 , A61K31/439 , A61K31/4725 , A61K45/06 , C07D401/12 , C07D417/12 , C07D453/06
Abstract: This invention relates to 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
Abstract translation: 本发明涉及式1的2-氮杂 - 双环[2.2.2]辛烷-3-羧酸（苄基 - 氰基 - 甲基） - 酰胺及其作为组织蛋白酶C抑制剂的用途，含有它们的药物组合物和方法 使用与用于治疗和/或预防与二肽基肽酶I活性相关的疾病的药剂，例如， 呼吸疾病。
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![METHOD OF USING SUBSTITUTED 2-AZA-BICYCLO[2.2.2]OCTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C](/abs-image/US/2014/12/25/US20140378504A1/abs.jpg.150x150.jpg)
17.发明申请METHOD OF USING SUBSTITUTED 2-AZA-BICYCLO[2.2.2]OCTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C 审中-公开使用取代的2-AZA-BICYCLO的方法[2.2.2] 3-羟基-3-羧酸（苄基 - 氰基 - 甲基） - 胺类C的抑制剂公开(公告)号：US20140378504A1
公开(公告)日：2014-12-25
申请号：US14483217
申请日：2014-09-11
Applicant: Ralf ANDERSKEWITZ , Matthias GRAUERT , Marc GRUNDL , Thorsten OOST , Alexander PAUTSCH , Stefan PETERS
Inventor： Ralf ANDERSKEWITZ , Matthias GRAUERT , Marc GRUNDL , Thorsten OOST , Alexander PAUTSCH , Stefan PETERS
IPC: C07D221/22
CPC classification number: C07D221/22 , A61K31/439 , A61K31/4725 , A61K45/06 , C07D401/12 , C07D417/12 , C07D453/06
Abstract: This invention relates to 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
Abstract translation: 本发明涉及式1的2-氮杂 - 双环[2.2.2]辛烷-3-羧酸（苄基 - 氰基 - 甲基） - 酰胺及其作为组织蛋白酶C抑制剂的用途，含有它们的药物组合物和方法 使用与用于治疗和/或预防与二肽基肽酶I活性相关的疾病的药剂，例如， 呼吸疾病。
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![Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides inhibitors of cathepsin C](/abs-image/US/2014/10/28/US08871783B2/abs.jpg.150x150.jpg)
18.发明授权Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides inhibitors of cathepsin C 有权取代的2-氮杂 - 双环[2.2.1]庚烷-3-羧酸（氰基 - 甲基）酰胺组织蛋白酶C的抑制剂公开(公告)号：US08871783B2
公开(公告)日：2014-10-28
申请号：US14205881
申请日：2014-03-12
Applicant: Ralf Anderskewitz , Marc Grundl , Gerd Morschhaeuser , Thorsten Oost , Alexander Pautsch
Inventor： Ralf Anderskewitz , Marc Grundl , Gerd Morschhaeuser , Thorsten Oost , Alexander Pautsch
IPC: A61K31/44 , C07D221/02
CPC classification number: C07D409/12 , A61K45/06 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14
Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
Abstract translation: 本发明涉及式1的2-氮杂 - 双环[2.2.1]庚烷-3-甲酸（氰基 - 甲基） - 酰胺及其作为组织蛋白酶C抑制剂的用途，含有该组合物的药物组合物和使用 与用于治疗和/或预防与二肽基肽酶I活性相关的疾病的药剂相同，例如 呼吸疾病。
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公开(公告)号：US08420630B2
公开(公告)日：2013-04-16
申请号：US12711364
申请日：2010-02-24
Applicant: Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schnapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
Inventor： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schnapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
IPC: C07D239/48 , C07D403/12 , C07D401/12 , A61K31/506
CPC classification number: C07D239/48 , C07D231/12 , C07D233/56 , C07D239/50 , C07D239/80 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D451/04 , C07D451/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterized by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
Abstract translation: 本发明涉及式（I）的三取代嘧啶，其中0Ra至Re如权利要求1所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，其用于制备具有上述药物组合物的用途 性质及其制备方法。
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20.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
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: A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , C07D237/04 , C07D403/04
CPC classification number: C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65324 , C07F9/6541 , C07F9/655354 , C07F9/65583 , C07F9/65586
Abstract: 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.
Abstract translation: 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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