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公开(公告)号:US08354418B2
公开(公告)日:2013-01-15
申请号:US12351017
申请日:2009-01-09
申请人: 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
发明人: 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分类号: C07D239/00 , A01N43/54 , A61K31/505
CPC分类号: C07D513/04
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US07691888B2
公开(公告)日:2010-04-06
申请号:US11243796
申请日:2005-10-05
申请人: Bodo Betzemeier , Trixi Brandl , Steffen Breitfelder , Ralph Brueckner , Thomas Gerstberger , Michael Gmachl , Matthias Grauert , Frank Hilberg , Christoph Hoenke , Matthias Hoffmann , Maria Impagnatiello , Dirk Kessler , Christian Klein , Bernd Krist , Udo Maier , Darryl McConnell , Charlotte Reither , Stefan Scheuerer , Andreas Schoop , Norbert Schweifer , Oliver Simon , Martin Steegmaier , Steffen Steurer , Irene Waizenegger , Ulrike Weyer-Czernilofsky , Andreas Zoephel
发明人: Bodo Betzemeier , Trixi Brandl , Steffen Breitfelder , Ralph Brueckner , Thomas Gerstberger , Michael Gmachl , Matthias Grauert , Frank Hilberg , Christoph Hoenke , Matthias Hoffmann , Maria Impagnatiello , Dirk Kessler , Christian Klein , Bernd Krist , Udo Maier , Darryl McConnell , Charlotte Reither , Stefan Scheuerer , Andreas Schoop , Norbert Schweifer , Oliver Simon , Martin Steegmaier , Steffen Steurer , Irene Waizenegger , Ulrike Weyer-Czernilofsky , Andreas Zoephel
IPC分类号: A61K31/429 , A61K31/4162 , C07D513/02 , C07D417/14
CPC分类号: C07D513/04 , C07D277/84
摘要: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.
摘要翻译: 本发明包括通式(1)的化合物,其中R 1至R 3如权利要求1中所定义,其适用于治疗特征为过度或异常细胞增殖的疾病,以及其用于制备具有上述 属性。
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公开(公告)号:US20070244104A1
公开(公告)日:2007-10-18
申请号:US11690362
申请日:2007-03-23
申请人: Trixi Brandl , Udo Maier , Matthias Hoffmann , Stefan Scheuerer , Anne Joergensen , Alexander Pautsch , Steffen Breitfelder , Matthias Grauert , Christoph Hoenke , Klaus Erb , Michael Pieper , Ingo Pragst
发明人: 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分类号: A61K31/541 , A61K31/5377 , A61K31/519 , A61K31/496 , A61K31/4745 , C07D498/02
CPC分类号: C07D513/04
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US20070238746A1
公开(公告)日:2007-10-11
申请号:US11690355
申请日:2007-03-23
申请人: Trixi Brandl , Udo Maier , Christoph Hoenke , Anne Joergensen , Alexander Pautsch , Steffen Breitfelder , Matthias Grauert , Matthias Hoffmann , Stefan Scheuerer , Klaus Erb , Michael Pieper , Ingo Pragst
发明人: 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分类号: A61K31/519 , A61K31/4745 , C07D498/02
CPC分类号: C07D513/04
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US08410100B2
公开(公告)日:2013-04-02
申请号:US12524791
申请日:2008-01-28
申请人: Riccardo Giovannini , Sara Frattini , Trixi Brandl , Steffen Breitfelder , Enzo Cereda , Matthias Grauert , Matthias Hoffman , Anne T. Joergensen , Udo Maier , Alexander Pautsch , Monica Quai , Stefan Scheuerer
发明人: Riccardo Giovannini , Sara Frattini , Trixi Brandl , Steffen Breitfelder , Enzo Cereda , Matthias Grauert , Matthias Hoffman , Anne T. Joergensen , Udo Maier , Alexander Pautsch , Monica Quai , Stefan Scheuerer
IPC分类号: A61K31/50 , A61K31/525
CPC分类号: C07D487/04
摘要: 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.
摘要翻译: 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 。
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公开(公告)号:US08207349B2
公开(公告)日:2012-06-26
申请号:US12685213
申请日:2010-01-11
申请人: Bodo Betzemeier , Trixi Brandl , Steffen Breitfelder , Ralph Brueckner , Thomas Gerstberger , Michael Gmachl , Matthias Grauert , Frank Hilberg , Christoph Hoenke , Matthias Hoffmann , Maria Impagnatiello , Dirk Kessler , Christian Klein , Bernd Krist , Udo Maier , Darryl McConnell , Charlotte Reither , Stefan Scheuerer , Andreas Schoop , Norbert Schweifer , Oliver Simon , Martin Steegmaier , Steffen Steurer , Irene Waizenegger , Ulrike Weyer-Czernilofsky , Andreas Zoephel
发明人: Bodo Betzemeier , Trixi Brandl , Steffen Breitfelder , Ralph Brueckner , Thomas Gerstberger , Michael Gmachl , Matthias Grauert , Frank Hilberg , Christoph Hoenke , Matthias Hoffmann , Maria Impagnatiello , Dirk Kessler , Christian Klein , Bernd Krist , Udo Maier , Darryl McConnell , Charlotte Reither , Stefan Scheuerer , Andreas Schoop , Norbert Schweifer , Oliver Simon , Martin Steegmaier , Steffen Steurer , Irene Waizenegger , Ulrike Weyer-Czernilofsky , Andreas Zoephel
IPC分类号: C07D277/60
CPC分类号: C07D513/04 , C07D277/84
摘要: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.
摘要翻译: 本发明包括通式(1)的化合物,其中R 1至R 3如权利要求1中所定义,其适用于治疗特征为过度或异常细胞增殖的疾病,以及其用于制备具有上述 属性。
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公开(公告)号:US20070259855A1
公开(公告)日:2007-11-08
申请号:US11690360
申请日:2007-03-23
申请人: Udo Maier , Matthias Grauert , Matthias Hoffmann , Christoph Hoenke , Anne Joergensen , Alexander Pautsch , Trixi Brandl , Steffen Breitfelder , Stefan Scheuerer , Klaus Erb , Michael Pieper , Ingo Pragst
发明人: Udo Maier , Matthias Grauert , Matthias Hoffmann , Christoph Hoenke , Anne Joergensen , Alexander Pautsch , Trixi Brandl , Steffen Breitfelder , Stefan Scheuerer , Klaus Erb , Michael Pieper , Ingo Pragst
IPC分类号: A61K31/429 , A61K31/428 , A61K31/44 , A61K31/517 , A61K31/549 , A61K31/55 , A61K31/551 , A61P11/00 , A61P17/00 , A61P19/00 , A61P29/00 , A61P31/00 , A61P37/00 , C07D417/06 , C07D513/04
CPC分类号: C07D513/04
摘要: 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-indazoles and the use thereof as pharmaceutical compositions.
摘要翻译: 公开了通式(I)的化合物,其中基团R 1,R 2,R a和R b, SUP>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 - 吲唑的方法和 其作为药物组合物的用途。
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公开(公告)号:US20060106013A1
公开(公告)日:2006-05-18
申请号:US11244299
申请日:2005-10-05
申请人: Steffen Breitfelder , Udo Maier , Trixi Brandl , Christoph Hoenke , Matthias Grauert , Alexander Pautsch , Matthias Hoffmann , Frank Kalkbrenner , Anne Joergensen , Gerhard Schaenzle , Stefan Peters , Frank Buettner , Eckhart Bauer
发明人: Steffen Breitfelder , Udo Maier , Trixi Brandl , Christoph Hoenke , Matthias Grauert , Alexander Pautsch , Matthias Hoffmann , Frank Kalkbrenner , Anne Joergensen , Gerhard Schaenzle , Stefan Peters , Frank Buettner , Eckhart Bauer
IPC分类号: A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/43 , C07D498/02
CPC分类号: C07D513/04 , C07D277/84
摘要: 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 gastrointestinal 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.
摘要翻译: 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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公开(公告)号:US20060100254A1
公开(公告)日:2006-05-11
申请号:US11243796
申请日:2005-10-05
申请人: Bodo Betzemeier , Trixi Brandl , Steffen Breitfelder , Ralph Brueckner , Thomas Gerstberger , Michael Gmachl , Matthias Grauert , Frank Hilberg , Christoph Hoenke , Matthias Hoffmann , Maria Impagnatiello , Dirk Kessler , Christian Klein , Bernd Krist , Udo Maier , Darryl McConnell , Charlotte Reither , Stefan Scheuerer , Andreas Schoop , Norbert Schweifer , Oliver Simon , Martin Steegmaier , Steffen Steurer , Irene Waizenegger , Ulrike Weyer-Czernilofsky , Andreas Zoephel
发明人: Bodo Betzemeier , Trixi Brandl , Steffen Breitfelder , Ralph Brueckner , Thomas Gerstberger , Michael Gmachl , Matthias Grauert , Frank Hilberg , Christoph Hoenke , Matthias Hoffmann , Maria Impagnatiello , Dirk Kessler , Christian Klein , Bernd Krist , Udo Maier , Darryl McConnell , Charlotte Reither , Stefan Scheuerer , Andreas Schoop , Norbert Schweifer , Oliver Simon , Martin Steegmaier , Steffen Steurer , Irene Waizenegger , Ulrike Weyer-Czernilofsky , Andreas Zoephel
IPC分类号: A61K31/429 , C07D513/02
CPC分类号: C07D513/04 , C07D277/84
摘要: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in Claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.
摘要翻译: 本发明包括通式(1)的化合物,其中R 1至R 3定义如权利要求1,其适用于治疗以下特征的疾病: 过度或异常细胞增殖,以及它们用于制备具有上述性质的药物。
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公开(公告)号:US20130172323A1
公开(公告)日:2013-07-04
申请号:US13696094
申请日:2011-05-06
申请人: Matthias Grauert , Remko Bakker , Steffen Breitfelder , Frank Buettner , Peter Eickelmann , Thomas Fox , Marc Grundl , Thorsten Lehmann-Lintz , Wolfgang Rist
发明人: Matthias Grauert , Remko Bakker , Steffen Breitfelder , Frank Buettner , Peter Eickelmann , Thomas Fox , Marc Grundl , Thorsten Lehmann-Lintz , Wolfgang Rist
IPC分类号: C07D413/10 , C07D498/04 , C07D417/14 , C07D413/14 , C07D453/02
CPC分类号: C07D413/10 , C07D413/04 , C07D413/14 , C07D417/14 , C07D453/02 , C07D498/04
摘要: 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.
摘要翻译: 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。
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