公开(公告)号：US08354418B2

公开(公告)日：2013-01-15

申请号：US12351017

申请日：2009-01-09

Applicant: Trixi Brandl ,  Udo Maier ,  Christoph Hoenke ,  Anne T. Joergensen ,  Alexander Pautsch ,  Steffen Breitfelder ,  Matthias Grauert ,  Matthias Hoffmann ,  Stefan Scheuerer ,  Klaus Erb ,  Michael Pieper ,  Ingo Pragst

Inventor： Trixi Brandl ,  Udo Maier ,  Christoph Hoenke ,  Anne T. Joergensen ,  Alexander Pautsch ,  Steffen Breitfelder ,  Matthias Grauert ,  Matthias Hoffmann ,  Stefan Scheuerer ,  Klaus Erb ,  Michael Pieper ,  Ingo Pragst

IPC: C07D239/00 ,  A01N43/54 ,  A61K31/505

CPC classification number: C07D513/04

Abstract: The present invention relates to compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.

Abstract translation: 本发明涉及通式（I）的化合物，其中基团A，R 1，R 2，R a和R b具有权利要求书和说明书中给出的含义，互变异构体，外消旋体，对映体，非对映异构体及其混合物， 其药理学上可接受的酸加成盐，溶剂合物和水合物，以及制备这些噻唑基 - 二氢 - 喹唑啉的方法及其作为药物组合物的用途。

公开(公告)号：US20110269761A1

公开(公告)日：2011-11-03

申请号：US12988452

申请日：2009-04-17

Applicant: Elke Langkopf ,  Frank Himmelsbach ,  Juergen Mack ,  Alexander Pautsch ,  Corinna Schoelch ,  Annette Schuler-Metz ,  Ruediger Streicher ,  Holger Wagner

Inventor： Elke Langkopf ,  Frank Himmelsbach ,  Juergen Mack ,  Alexander Pautsch ,  Corinna Schoelch ,  Annette Schuler-Metz ,  Ruediger Streicher ,  Holger Wagner

IPC: 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 classification number: C07D271/06 ,  C07C311/21 ,  C07D213/40 ,  C07D213/74 ,  C07D215/40 ,  C07D239/26 ,  C07D271/10 ,  C07D295/108 ,  C07D295/15 ,  C07D307/52

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100210594A1

公开(公告)日：2010-08-19

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: A61K31/675 ,  C07F9/6512 ,  C07F9/572 ,  C07F9/6509 ,  C07F9/645 ,  C07F9/6533 ,  C07F9/6521 ,  C07F9/6544 ,  C07F9/6503 ,  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.

公开(公告)号：US20070244104A1

公开(公告)日：2007-10-18

申请号：US11690362

申请日：2007-03-23

Applicant: Trixi Brandl ,  Udo Maier ,  Matthias Hoffmann ,  Stefan Scheuerer ,  Anne 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 Joergensen ,  Alexander Pautsch ,  Steffen Breitfelder ,  Matthias Grauert ,  Christoph Hoenke ,  Klaus Erb ,  Michael Pieper ,  Ingo Pragst

IPC: A61K31/541 ,  A61K31/5377 ,  A61K31/519 ,  A61K31/496 ,  A61K31/4745 ,  C07D498/02

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，其异构体和 制备这些化合物的方法及其作为药物组合物的用途。

公开(公告)号：US20070238746A1

公开(公告)日：2007-10-11

申请号：US11690355

申请日：2007-03-23

Applicant: Trixi Brandl ,  Udo Maier ,  Christoph Hoenke ,  Anne Joergensen ,  Alexander Pautsch ,  Steffen Breitfelder ,  Matthias Grauert ,  Matthias Hoffmann ,  Stefan Scheuerer ,  Klaus Erb ,  Michael Pieper ,  Ingo Pragst

Inventor： Trixi Brandl ,  Udo Maier ,  Christoph Hoenke ,  Anne Joergensen ,  Alexander Pautsch ,  Steffen Breitfelder ,  Matthias Grauert ,  Matthias Hoffmann ,  Stefan Scheuerer ,  Klaus Erb ,  Michael Pieper ,  Ingo Pragst

IPC: A61K31/519 ,  A61K31/4745 ,  C07D498/02

CPC classification number: C07D513/04

Abstract: Disclosed are compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.

Abstract translation: 公开了通式（I）的化合物，其中基团A，R 1，R 2，R a和R b 具有权利要求和说明书中给出的含义，互变异构体，外消旋体，对映异构体，非对映异构体及其混合物，以及任选的药理学上可接受的酸加成盐，溶剂合物和水合物，以及制备这些噻唑基 - 喹唑啉及其作为药物组合物的用途。

公开(公告)号：US20070238718A1

公开(公告)日：2007-10-11

申请号：US11690351

申请日：2007-03-23

Applicant: Matthias GRAUERT ,  Udo Maier ,  Matthias Hoffmann ,  Stefan Scheuerer ,  Anne Joergensen ,  Alexander Pautsch ,  Trixi Brandl ,  Christoph Hoenke ,  Steffen Breitfelder ,  Klaus Erb ,  Michael Pieper ,  Ingo Pragst

Inventor： Matthias GRAUERT ,  Udo Maier ,  Matthias Hoffmann ,  Stefan Scheuerer ,  Anne Joergensen ,  Alexander Pautsch ,  Trixi Brandl ,  Christoph Hoenke ,  Steffen Breitfelder ,  Klaus Erb ,  Michael Pieper ,  Ingo Pragst

IPC: A61K31/55 ,  A61K31/4747 ,  A61K31/43 ,  C07D498/02

CPC classification number: C07D513/04

Abstract: The present invention relates to new thiazolyl-dihydro-indazoles of general formula (I) wherein the groups R1, R2 and R3 have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-indazoles and the use thereof as pharmaceutical compositions.

Abstract translation: 本发明涉及通式（I）的新的噻唑基 - 二氢 - 吲唑，其中R 1，R 2和R 3基团具有 权利要求和说明书中给出的含义，互变异构体，外消旋物，对映异构体，非对映异构体及其混合物，以及任选的药理学上可接受的酸加成盐，溶剂合物和水合物，以及制备这些噻唑基 - 二氢 - 吲唑的方法及其用途 作为药物组合物。

公开(公告)号：US08334378B2

公开(公告)日：2012-12-18

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

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。

公开(公告)号：US08163911B2

公开(公告)日：2012-04-24

申请号：US12676319

申请日：2008-09-04

Applicant: Elke Langkopf ,  Alexander Pautsch ,  Corinna Schoelch ,  Annette Schuler-Metz ,  Ruediger Streicher ,  Holger Wagner

Inventor： Elke Langkopf ,  Alexander Pautsch ,  Corinna Schoelch ,  Annette Schuler-Metz ,  Ruediger Streicher ,  Holger Wagner

IPC: C07F9/28

CPC classification number: C07D215/38 ,  C07D217/22 ,  C07D219/08 ,  C07D231/56 ,  C07D237/28 ,  C07D239/42 ,  C07D239/72 ,  C07D239/74 ,  C07D241/42 ,  C07D263/56 ,  C07D277/66 ,  C07D471/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100152167A1

公开(公告)日：2010-06-17

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: A61K31/505 ,  C07D239/50 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/506 ,  C07D403/04 ,  A61K31/55 ,  C07D403/12 ,  A61K31/551 ,  A61P31/00 ,  A61P35/00 ,  A61P9/00 ,  A61P19/08

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) wherein0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterised 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。

公开(公告)号：US20100130557A1

公开(公告)日：2010-05-27

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: A61K31/404 ,  A61K31/4439 ,  A61K31/403 ,  C07D401/12 ,  C07D209/82 ,  C07D209/04 ,  A61P3/10

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。