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公开(公告)号:US20130065876A1
公开(公告)日:2013-03-14
申请号:US13609429
申请日:2012-09-11
申请人: Uwe Grether , Paul Hebeisen , Peter Mohr , Fabienne Ricklin , Stephan Roever
发明人: Uwe Grether , Paul Hebeisen , Peter Mohr , Fabienne Ricklin , Stephan Roever
IPC分类号: A61K31/4545 , A61K31/4439 , A61K31/5377 , A61K31/496 , C07D405/04 , A61K31/501 , C07D405/14 , C07D401/06 , A61K31/44 , C07D417/12 , C07D413/12 , A61K31/4433 , C07D401/12 , C07D213/78 , C07D401/14
CPC分类号: C07D213/87 , C07D401/06 , C07D405/04 , C07D413/12 , C07D413/14 , C07D417/12
摘要: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.
摘要翻译: 本发明涉及式I化合物,其中R 1至R 5在说明书和权利要求书中定义,以及其药学上可接受的盐。 本发明还涉及所述化合物的制造,含有它们的药物组合物以及用于治疗和/或预防可用HDL-胆固醇升高剂如血脂异常,动脉粥样硬化和心血管疾病治疗的疾病的方法。
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公开(公告)号:US08648099B2
公开(公告)日:2014-02-11
申请号:US13609429
申请日:2012-09-11
申请人: Uwe Grether , Paul Hebeisen , Peter Mohr , Fabienne Ricklin , Stephan Roever
发明人: Uwe Grether , Paul Hebeisen , Peter Mohr , Fabienne Ricklin , Stephan Roever
IPC分类号: A61K31/44 , A01N43/40 , C07D213/62 , C07D213/78 , C07D211/72 , C07D211/84
CPC分类号: C07D213/87 , C07D401/06 , C07D405/04 , C07D413/12 , C07D413/14 , C07D417/12
摘要: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.
摘要翻译: 本发明涉及式I化合物,其中R 1至R 5在说明书和权利要求书中定义,以及其药学上可接受的盐。 本发明还涉及所述化合物的制造,含有它们的药物组合物以及用于治疗和/或预防可用HDL-胆固醇升高剂如血脂异常,动脉粥样硬化和心血管疾病治疗的疾病的方法。
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公开(公告)号:US07572801B2
公开(公告)日:2009-08-11
申请号:US11801863
申请日:2007-05-11
申请人: Aurelia Conte , Henrietta Dehmlow , Uwe Grether , Nicole A. Kratochwil , Holger Kuehne , Robert Narquizian , Constantinos Panousis , Jens-Uwe Peters , Fabienne Ricklin , Stephan Roever
发明人: Aurelia Conte , Henrietta Dehmlow , Uwe Grether , Nicole A. Kratochwil , Holger Kuehne , Robert Narquizian , Constantinos Panousis , Jens-Uwe Peters , Fabienne Ricklin , Stephan Roever
IPC分类号: A61K31/519 , C07D471/04 , A61P9/10 , A61P3/00 , A61P3/10
CPC分类号: C07D471/04
摘要: The invention is concerned with novel pyridopyrimidinone derivatives of formula (I): wherein R1 to R8, X, Y, m and n are as defined in the description and in the claims. The compounds of the present invention are HM74A agonists with improved properties compared to niacin and can be used for the treatment and/or prevention of diseases such as dyslipidemia, atherosclerosis, diabetes, metabolic syndrome, and other related diseases associated with HM74A.
摘要翻译: 本发明涉及式(I)的新颖的吡啶并嘧啶酮衍生物:其中R1至R8,X,Y,m和n如说明书和权利要求中所定义。 本发明的化合物是与烟酸相比具有改进性质的HM74A激动剂,可用于治疗和/或预防诸如血脂异常,动脉粥样硬化,糖尿病,代谢综合征和与HM74A相关的其它相关疾病的疾病。
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公开(公告)号:US20070275987A1
公开(公告)日:2007-11-29
申请号:US11801863
申请日:2007-05-11
申请人: Aurelia Conte , Henrietta Dehmlow , Uwe Grether , Nicole A. Kratochwil , Holger Kuehne , Robert Narquizian , Constantinos Panousis , Jens-Uwe Peters , Fabienne Ricklin , Stephan Roever
发明人: Aurelia Conte , Henrietta Dehmlow , Uwe Grether , Nicole A. Kratochwil , Holger Kuehne , Robert Narquizian , Constantinos Panousis , Jens-Uwe Peters , Fabienne Ricklin , Stephan Roever
IPC分类号: A61K31/519 , C07D487/02
CPC分类号: C07D471/04
摘要: The invention is concerned with novel pyridopyrimidinone derivatives of formula (I): wherein R1 to R8, X, Y, m and n are as defined in the description and in the claims. The compounds of the present invention are HM74A agonists with improved properties compared to niacin and can be used for the treatment and/or prevention of diseases such as dyslipidemia, atherosclerosis, diabetes, metabolic syndrome, and other related diseases associated with HM74A.
摘要翻译: 本发明涉及式(I)的新型吡啶并嘧啶酮衍生物:其中R 1至R 8,X,Y,m和n如说明书和 索赔。 本发明的化合物是与烟酸相比具有改进性质的HM74A激动剂,可用于治疗和/或预防诸如血脂异常,动脉粥样硬化,糖尿病,代谢综合征和与HM74A相关的其它相关疾病的疾病。
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公开(公告)号:US06969725B2
公开(公告)日:2005-11-29
申请号:US10679604
申请日:2003-10-06
申请人: Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
发明人: Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
IPC分类号: A61K31/421 , A61P3/10 , C07D263/32 , C07D263/30
CPC分类号: C07D263/32
摘要: The present invention relates to compounds of formula (I) wherein wherein R1, R2, R3, R4, R5, R6 and n are as described herein. The compounds of the present invention can be used as medicaments for the treatment and/or prevention of diseases which are modulated by PPARα and/or PPARγ agonists. Examples of such diseases are diabetes, particularly non-insulin dependent diabetes mellitus, elevated blood pressure, increased lipid and cholesterol levels, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, polycystic ovary syndrome, inflammatory diseases (such as e.g. crown disease, inflammatory bowel disease, collitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as e.g. Alzheimer's disease or impaired/improvable cognitive function) and proliferative diseases.
摘要翻译: 本发明涉及式(I)化合物,其中R 1,R 2,R 3,R 4, R 5,R 5,R 6和n如本文所述。 本发明的化合物可用作治疗和/或预防由PPARα和/或PPARγ激动剂调节的疾病的药物。 这些疾病的例子包括糖尿病,特别是非胰岛素依赖性糖尿病,升高的血压,升高的脂质和胆固醇水平,动脉粥样硬化疾病,代谢综合征,内皮功能障碍,促凝血状态,血脂异常,多囊卵巢综合征,炎性疾病(例如冠 疾病,炎性肠病,结肠炎,胰腺炎,胆汁郁积/肝脏纤维化,以及具有诸如阿尔茨海默病和受损/可改善的认知功能等炎症成分的疾病)和增殖性疾病。
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公开(公告)号:US06642389B2
公开(公告)日:2003-11-04
申请号:US10142567
申请日:2002-05-09
申请人: Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
发明人: Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
IPC分类号: C07D26332
CPC分类号: C07D413/12 , C07D263/32 , C07D413/14
摘要: The present invention relates to novel oxazole compounds which act as PPAR&agr; and PPAR&ggr; agonists and are accordingly useful for the treatment of diseases modulated by PPAR&agr; and PPAR&ggr; such as diabetes.
摘要翻译: 本发明涉及作为PPARα和PPARγ激动剂的新型恶唑化合物,因此可用于治疗由PPARα和PPARγ等调节的疾病如糖尿病。
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公开(公告)号:US07348349B2
公开(公告)日:2008-03-25
申请号:US11183360
申请日:2005-07-18
申请人: Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
发明人: Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
IPC分类号: A61K31/421 , C07D263/30
CPC分类号: C07D263/32
摘要: The present invention relates to compounds of formula (I) wherein wherein R1, R2, R3, R4, R5, R6 and n are as described herein. The compounds of the present invention can be used as medicaments for the treatment and/or prevention of diseases which are modulated by PPARα and/or PPARγ agonists. Examples of such diseases are diabetes, particularly non-insulin dependent diabetes mellitus, elevated blood pressure, increased lipid and cholesterol levels, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, polycystic ovary syndrome, inflammatory diseases (such as e.g. crown disease, inflammatory bowel disease, collitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as e.g. Alzheimer's disease or impaired/improvable cognitive function) and proliferative diseases.
摘要翻译: 本发明涉及式(I)化合物,其中R 1,R 2,R 3,R 4, R 5,R 5,R 6和n如本文所述。 本发明的化合物可用作治疗和/或预防由PPARα和/或PPARγ激动剂调节的疾病的药物。 这些疾病的例子包括糖尿病,特别是非胰岛素依赖性糖尿病,升高的血压,升高的脂质和胆固醇水平,动脉粥样硬化疾病,代谢综合征,内皮功能障碍,促凝血状态,血脂异常,多囊卵巢综合征,炎性疾病(例如冠 疾病,炎性肠病,结肠炎,胰腺炎,胆汁郁积/肝脏纤维化,以及具有诸如阿尔茨海默病和受损/可改善的认知功能等炎症成分的疾病)和增殖性疾病。
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公开(公告)号:US20050267180A1
公开(公告)日:2005-12-01
申请号:US11183360
申请日:2005-07-18
申请人: Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
发明人: Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
IPC分类号: A61K31/421 , A61P3/10 , C07D263/32
CPC分类号: C07D263/32
摘要: The present invention relates to compounds of formula (I) wherein wherein R1, R2, R3, R4, R5, R6 and n are as described herein. The compounds of the present invention can be used as medicaments for the treatment and/or prevention of diseases which are modulated by PPARα and/or PPARγ agonists. Examples of such diseases are diabetes, particularly non-insulin dependent diabetes mellitus, elevated blood pressure, increased lipid and cholesterol levels, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, polycystic ovary syndrome, inflammatory diseases (such as e.g. crown disease, inflammatory bowel disease, collitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as e.g. Alzheimer's disease or impaired/improvable cognitive function) and proliferative diseases.
摘要翻译: 本发明涉及式(I)化合物,其中R 1,R 2,R 3,R 4, R 5,R 5,R 6和n如本文所述。 本发明的化合物可用作治疗和/或预防由PPARα和/或PPARγ激动剂调节的疾病的药物。 这些疾病的例子包括糖尿病,特别是非胰岛素依赖性糖尿病,升高的血压,升高的脂质和胆固醇水平,动脉粥样硬化疾病,代谢综合征,内皮功能障碍,促凝血状态,血脂异常,多囊卵巢综合征,炎性疾病(例如冠 疾病,炎性肠病,结肠炎,胰腺炎,胆汁郁积/肝脏纤维化,以及具有诸如阿尔茨海默病和受损/可改善的认知功能等炎症成分的疾病)和增殖性疾病。
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公开(公告)号:US20080234277A1
公开(公告)日:2008-09-25
申请号:US12049460
申请日:2008-03-17
申请人: Aurelia Conte , Henrietta Dehmlow , Uwe Grether , Nicole A. Kratochwil , Holger Kuehne , Robert Narquizian , Constantinos G. Panousis , Jens-Uwe Peters , Fabienne Ricklin
发明人: Aurelia Conte , Henrietta Dehmlow , Uwe Grether , Nicole A. Kratochwil , Holger Kuehne , Robert Narquizian , Constantinos G. Panousis , Jens-Uwe Peters , Fabienne Ricklin
IPC分类号: A61K31/53 , C07D471/04 , C07D475/00 , A61K31/5025 , A61K31/519 , A61P9/10
CPC分类号: C07D487/04 , C07D475/02
摘要: The invention is concerned with novel aza-pyridopyrimidinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, X1, X2, X3, Y, Z, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used in treating or preventing diseases which are modulated by HM74A agonists.
摘要翻译: 本发明涉及式(I)的新型氮杂 - 吡啶并嘧啶酮衍生物:其中R 1,R 2,R 3,R SUP R 4,R 5,X 1,X 2,X 3,Y,Z ,m和n如在说明书和权利要求书中所定义,以及其生理上可接受的盐和酯。 这些化合物是HM74A激动剂,可用于治疗或预防由HM74A激动剂调节的疾病。
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公开(公告)号:US07928106B2
公开(公告)日:2011-04-19
申请号:US12049460
申请日:2008-03-17
申请人: Aurelia Conte , Henrietta Dehmlow , Uwe Grether , Nicole A. Kratochwil , Holger Kuehne , Robert Narquizian , Constantinos G. Panousis , Jens-Uwe Peters , Fabienne Ricklin
发明人: Aurelia Conte , Henrietta Dehmlow , Uwe Grether , Nicole A. Kratochwil , Holger Kuehne , Robert Narquizian , Constantinos G. Panousis , Jens-Uwe Peters , Fabienne Ricklin
IPC分类号: A61K31/50 , A61K31/501 , C07D487/00
CPC分类号: C07D487/04 , C07D475/02
摘要: The invention is concerned with novel aza-pyridopyrimidinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, X1, X2, X3, Y, Z, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used in treating or preventing diseases which are modulated by HM74A agonists.
摘要翻译: 本发明涉及式(I)的新的氮杂 - 吡啶并嘧啶酮衍生物:其中R1,R2,R3,R4,R5,X1,X2,X3,Y,Z,m和n如说明书和权利要求书中所定义 ,以及其生理上可接受的盐和酯。 这些化合物是HM74A激动剂,可用于治疗或预防由HM74A激动剂调节的疾病。
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