公开(公告)号：US08772323B2

公开(公告)日：2014-07-08

申请号：US13696094

申请日：2011-05-06

Applicant: Matthias Grauert ,  Remko Bakker ,  Steffen Breitfelder ,  Frank Buettner ,  Peter Eickelmann ,  Thomas Fox ,  Marc Grundl ,  Thorsten Lehmann-Lintz ,  Wolfgang Rist

Inventor： Matthias Grauert ,  Remko Bakker ,  Steffen Breitfelder ,  Frank Buettner ,  Peter Eickelmann ,  Thomas Fox ,  Marc Grundl ,  Thorsten Lehmann-Lintz ,  Wolfgang Rist

IPC: A61K31/423 ,  C07D263/54

CPC classification number: C07D413/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D453/02 ,  C07D498/04

Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, 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的哒嗪酮衍生物，其中基团A，G和R 1如本申请中所定义，其互变异构体，其立体异构体，其混合物及其盐具有有价值的药理学性质， 特异性结合GPR119受体并调节其活性。

公开(公告)号：US20100099680A1

公开(公告)日：2010-04-22

申请号：US12524791

申请日：2008-01-28

Applicant: Riccardo Giovannini ,  Sara Frattini ,  Trixi Brandl ,  Steffen Breitfelder ,  Enzo Cereda ,  Matthias Grauert ,  Matthias Hoffmann ,  Anne T. Joergensen ,  Udo Maier ,  Alexander Pautsch ,  Monica Quai ,  Stefan Scheuerer

Inventor： Riccardo Giovannini ,  Sara Frattini ,  Trixi Brandl ,  Steffen Breitfelder ,  Enzo Cereda ,  Matthias Grauert ,  Matthias Hoffmann ,  Anne T. Joergensen ,  Udo Maier ,  Alexander Pautsch ,  Monica Quai ,  Stefan Scheuerer

IPC: A61K31/519 ,  C07D475/00 ,  A61P29/00 ,  A61P37/08 ,  A61P11/00

CPC classification number: C07D487/04

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: 提供式（1）的新化合物，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 。

公开(公告)号：US20090156554A1

公开(公告)日：2009-06-18

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 SCHAENZLE ,  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 SCHAENZLE ,  Stefan PETERS ,  Frank BUETTNER ,  Eckhart BAUER

IPC: A61K31/695 ,  C07D513/04 ,  A61K31/429 ,  C07F7/10 ,  A61K31/519 ,  C07D277/46 ,  A61K31/426 ,  A61P37/08 ,  A61K31/5377 ,  A61K31/454

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 。

公开(公告)号：US07517995B2

公开(公告)日：2009-04-14

申请号：US11690356

申请日：2007-03-23

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

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

IPC: A61K31/429 ,  C07D513/04

CPC classification number: C07D513/04

Abstract: Disclosed are compounds of general formula (I), wherein the groups 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-cyclopentapyrazoles and the use thereof as pharmaceutical compositions.

Abstract translation: 公开了通式（I）的化合物，其中基团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，对映异构体，非对映异构体及其混合物，以及任选的药理学可接受的酸加成 盐，溶剂合物和水合物，以及制备这些噻唑基 - 二氢环戊吡唑的方法及其作为药物组合物的用途。

公开(公告)号：US07041674B2

公开(公告)日：2006-05-09

申请号：US10718403

申请日：2003-11-20

Applicant: Steffen Breitfelder ,  Matthias Hoffmann ,  Matthias Grauert ,  Michael P. Pieper ,  Georg Speck

Inventor： Steffen Breitfelder ,  Matthias Hoffmann ,  Matthias Grauert ,  Michael P. Pieper ,  Georg Speck

IPC: A61K31/46 ,  C07D491/08

CPC classification number: C07D451/06

Abstract: A compound of formula 1 wherein X−, A, R1, R2, R3, and R4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in pharmaceutical compositions, and methods of treating patients using them.

Abstract translation: 式1的化合物，其中X，O，A，R 1，R 2，R 3和R 3， 可以具有权利要求书和说明书中给出的含义，其制备方法，它们在药物组合物中的用途，以及使用它们治疗患者的方法。

公开(公告)号：US06861422B2

公开(公告)日：2005-03-01

申请号：US10374876

申请日：2003-02-26

Applicant: Matthias Hoffmann ,  Matthias Grauert ,  Trixi Brandl ,  Steffen Breitfelder ,  Christian Eickmeier ,  Martin Steegmaier ,  Gisela Schnapp ,  Anke Baum ,  Jens Juergen Quant ,  Flavio Solca ,  Florian Colbatzky

Inventor： Matthias Hoffmann ,  Matthias Grauert ,  Trixi Brandl ,  Steffen Breitfelder ,  Christian Eickmeier ,  Martin Steegmaier ,  Gisela Schnapp ,  Anke Baum ,  Jens Juergen Quant ,  Flavio Solca ,  Florian Colbatzky

IPC: A61P35/00 ,  C07D475/00 ,  C07D519/00 ,  C07D487/04 ,  A61K31/4985

CPC classification number: C07D295/073 ,  C07D475/00

Abstract: The present invention relates to new dihydropteridinones of general formula (I): wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.

Abstract translation: 本发明涉及通式（I）的新的二氢蝶啶酮：其中基团L和R 1 -R 5具有权利要求书和说明书中给出的含义，其异构体，制备这些二氢蝶啶的方法和用途 作为药物组合物。

公开(公告)号：US20050014760A1

公开(公告)日：2005-01-20

申请号：US10903807

申请日：2004-07-30

Applicant: Matthias Hoffmann ,  Matthias Grauert ,  Trixi Brandl ,  Steffen Breitfelder ,  Christian Eickmeier ,  Martin Steegmaier ,  Gisela Schnapp ,  Anke Baum ,  Jens Quant ,  Flavio Solca ,  Florian Colbatzky

Inventor： Matthias Hoffmann ,  Matthias Grauert ,  Trixi Brandl ,  Steffen Breitfelder ,  Christian Eickmeier ,  Martin Steegmaier ,  Gisela Schnapp ,  Anke Baum ,  Jens Quant ,  Flavio Solca ,  Florian Colbatzky

IPC: A61P35/00 ,  C07D475/00 ,  C07D519/00 ,  A61K31/525

CPC classification number: C07D295/073 ,  C07D475/00

Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.

Abstract translation: 公开了通式（I）的新的二氢蝶啶酮，其中基团L和R 1 -R 5具有权利要求书和说明书中给出的含义，其异构体，制备这些二氢蝶呤的中间体和方法及其用途 药物组合物。

公开(公告)号：US20130065906A1

公开(公告)日：2013-03-14

申请号：US13418376

申请日：2012-03-13

Applicant: Bernd NOSSE ,  Andreas BLUM ,  Steffen BREITFELDER ,  Armin HECKEL ,  Frank HIMMELSBACH ,  Elke LANGKOPF ,  Bernd WELLENZOHN ,  Neil J. ASHWEEK ,  Nicole HARRIOTT

Inventor： Bernd NOSSE ,  Andreas BLUM ,  Steffen BREITFELDER ,  Armin HECKEL ,  Frank HIMMELSBACH ,  Elke LANGKOPF ,  Bernd WELLENZOHN ,  Neil J. ASHWEEK ,  Nicole HARRIOTT

IPC: C07D413/14 ,  A61K31/4545 ,  C07D417/14 ,  A61K31/506 ,  A61P3/06 ,  A61K31/497 ,  A61K31/501 ,  C07D401/14 ,  A61P3/10 ,  A61P3/04 ,  A61K31/454 ,  C07D413/04

CPC classification number: C07D413/14 ,  C07D413/04 ,  C07D417/14

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, Ar, m and n 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R1，LP，LQ，Ar，m和n基团如本申请中所定义，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 。

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 。

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。