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公开(公告)号:US08883786B2
公开(公告)日:2014-11-11
申请号:US13371834
申请日:2012-02-13
申请人: Jacques Bailly , Cornelia Hertel , Daniel Hunziker , Christian Lerner , Ulrike Obst Sander , Jens-Uwe Peters , Philippe Pflieger , Tanja Schulz-Gasch
发明人: Jacques Bailly , Cornelia Hertel , Daniel Hunziker , Christian Lerner , Ulrike Obst Sander , Jens-Uwe Peters , Philippe Pflieger , Tanja Schulz-Gasch
IPC分类号: A61K31/498 , A61K31/502 , A61K31/4965 , C07D277/24 , C07D277/62 , C07D498/04 , C07D231/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D401/04 , C07D215/14 , C07D471/04 , C07D213/64 , C07D213/61 , C07D217/16 , C07D401/06 , C07D249/18 , C07D213/30 , C07D237/08
CPC分类号: C07D241/12 , C07D213/30 , C07D213/61 , C07D213/64 , C07D215/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D237/08 , C07D239/26 , C07D249/18 , C07D277/24 , C07D277/62 , C07D401/04 , C07D401/06 , C07D471/04 , C07D498/04
摘要: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
摘要翻译: 本发明涉及式I化合物,其中A,n,R 1a至R 1d和R 2至R 5如在说明书和权利要求书中所定义,及其药学上可接受的盐。 该化合物是可用于治疗和/或预防糖尿病,血脂异常,肥胖,高血压,心血管疾病,肾上腺不平衡或抑郁症等疾病的糖皮质激素受体拮抗剂。
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公开(公告)号:US07186798B2
公开(公告)日:2007-03-06
申请号:US11299533
申请日:2005-12-12
IPC分类号: A61K38/00
摘要: The present invention relates to a fluorescently labeled growth hormone secretagogue which can be used for the identification of compounds capable of binding to growth hormone secretagogue receptors, in particular by high throughput screening.
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公开(公告)号:US20060073522A1
公开(公告)日:2006-04-06
申请号:US11299533
申请日:2005-12-12
申请人: Thilo Enderle , Martin Graf , Cornelia Hertel , Sannah Zoffmann , Eric Kitas
发明人: Thilo Enderle , Martin Graf , Cornelia Hertel , Sannah Zoffmann , Eric Kitas
摘要: The present invention relates to a fluorescently labeled growth hormone secretagogue which can be used for the identification of compounds capable of binding to growth hormone secretagogue receptors, in particular by high throughput screening.
摘要翻译: 本发明涉及荧光标记的生长激素促分泌素,其可用于鉴定能够结合生长激素促分泌素受体的化合物,特别是通过高通量筛选。
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公开(公告)号:US20050282864A1
公开(公告)日:2005-12-22
申请号:US11157093
申请日:2005-06-20
申请人: Silvia McArthur , Cornelia Hertel , Matthias Nettekoven , Susanne Raab , Olivier Roche , Rosa Rodriguez-Sarmiento , Franz Schuler , Jean Marc Plancher
发明人: Silvia McArthur , Cornelia Hertel , Matthias Nettekoven , Susanne Raab , Olivier Roche , Rosa Rodriguez-Sarmiento , Franz Schuler , Jean Marc Plancher
IPC分类号: C07D209/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , A61K31/454 , C07D43/02
CPC分类号: C07D405/14 , C07D209/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
摘要: The present invention relates to compounds of formula I: wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译: 本发明涉及式I化合物:其中X,R 1,R 2,R 3,R 4, SUP和R 5如在说明书和权利要求书及其药学上可接受的盐中所定义,用于制备这些化合物和含有它们的药物组合物。 该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。
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公开(公告)号:US20050085421A1
公开(公告)日:2005-04-21
申请号:US10964878
申请日:2004-10-14
申请人: Thilo Enderle , Martin Graf , Cornelia Hertel , Sannah Zoffmann , Eric Kitas
发明人: Thilo Enderle , Martin Graf , Cornelia Hertel , Sannah Zoffmann , Eric Kitas
IPC分类号: G01N33/53 , A61K45/00 , A61P5/06 , A61P43/00 , C07K7/08 , C07K14/60 , G01N31/22 , G01N33/566 , G01N33/58 , A61K38/22 , C07K14/575
摘要: The present invention relates to a fluorescently labeled growth hormone secretagogue which can be used for the identification of compounds capable of binding to growth hormone secretagogue receptors, in particular by high throughput screening.
摘要翻译: 本发明涉及荧光标记的生长激素促分泌素,其可用于鉴定能够结合生长激素促分泌素受体的化合物,特别是通过高通量筛选。
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公开(公告)号:US06512001B1
公开(公告)日:2003-01-28
申请号:US09636076
申请日:2000-08-10
IPC分类号: A61K314025
CPC分类号: C07D231/12 , C07D207/16 , C07D207/22 , C07D233/56 , C07D249/08 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D419/14
摘要: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.
摘要翻译: 新化合物具有下式:其中R,R 1,X和Y具有本文所述的含义。 阐述了合成这些化合物和使用这些化合物治疗与淀粉样变性相关疾病如阿尔茨海默病,成熟发病的糖尿病,家族性淀粉样多发性神经病,瘙痒病和克雷伊兹费尔德 - 雅各布病的方法。
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公开(公告)号:US08592426B2
公开(公告)日:2013-11-26
申请号:US13351253
申请日:2012-01-17
申请人: Johannes Aebi , Alfred Binggeli , Cornelia Hertel , Anish Ashok Konkar , Holger Kuehne , Bernd Kuhn , Hans P. Maerki , Haiyan Wang
发明人: Johannes Aebi , Alfred Binggeli , Cornelia Hertel , Anish Ashok Konkar , Holger Kuehne , Bernd Kuhn , Hans P. Maerki , Haiyan Wang
IPC分类号: A61K31/24 , A61K31/42 , C07D271/06
CPC分类号: C07C237/24 , C07C2602/02 , C07C2602/08 , C07C2602/10 , C07D257/04 , C07D271/06 , C07D271/10 , C07D305/08 , C07D401/10 , C07D401/14 , C07D405/10 , C07D405/12 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14
摘要: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 and n are as described herein, compositions including the compounds and methods of using the compounds.
摘要翻译: 本发明提供具有通式(I)的新化合物,其中R1,R2,R3,R4,R5,R6,R7,R8,R9,R10,R11,R12,A1,A2和n如本文所述, 化合物和使用该化合物的方法。
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公开(公告)号:US20090088425A1
公开(公告)日:2009-04-02
申请号:US12210247
申请日:2008-09-15
申请人: Jacques Bailly , Cornelia Hertel , Daniel Hunziker , Christian Lerner , Ulrike Obst Sander , Jens-Uwe Peters , Philippe Pflieger , Tanja Schulz-Gasch
发明人: Jacques Bailly , Cornelia Hertel , Daniel Hunziker , Christian Lerner , Ulrike Obst Sander , Jens-Uwe Peters , Philippe Pflieger , Tanja Schulz-Gasch
IPC分类号: A61K31/4965 , C07D241/10 , C07D241/40 , A61K31/5383 , A61P3/10 , A61K31/498 , C07D498/04
CPC分类号: C07D241/12 , C07D213/30 , C07D213/61 , C07D213/64 , C07D215/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D237/08 , C07D239/26 , C07D249/18 , C07D277/24 , C07D277/62 , C07D401/04 , C07D401/06 , C07D471/04 , C07D498/04
摘要: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
摘要翻译: 本发明涉及式I化合物,其中A,n,R 1a至R 1d和R 2至R 5如在说明书和权利要求书中所定义,及其药学上可接受的盐。 该化合物是可用于治疗和/或预防糖尿病,血脂异常,肥胖,高血压,心血管疾病,肾上腺不平衡或抑郁症等疾病的糖皮质激素受体拮抗剂。
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公开(公告)号:US20060204436A1
公开(公告)日:2006-09-14
申请号:US10561654
申请日:2004-06-18
IPC分类号: A61K51/00 , C07D487/10
CPC分类号: A61K51/0455
摘要: The present invention relates to a tritiated growth hormone secretagogue which can be used for the identification of compounds capable of binding to growth hormone secretagogue receptors, or of compounds having activity as growth hormone secretagogues.
摘要翻译: 本发明涉及可用于鉴定能够结合生长激素促分泌素受体的化合物或具有活性作为生长激素促分泌素的化合物的氚生长激素促分泌素。
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公开(公告)号:US20130045972A1
公开(公告)日:2013-02-21
申请号:US13371834
申请日:2012-02-13
申请人: Jacques Bailly , Cornelia Hertel , Daniel Hunziker , Christian Lerner , Ulrike Obst Sander , Jens-Uwe Peters , Philippe Pflieger , Tanja Schulz-Gasch
发明人: Jacques Bailly , Cornelia Hertel , Daniel Hunziker , Christian Lerner , Ulrike Obst Sander , Jens-Uwe Peters , Philippe Pflieger , Tanja Schulz-Gasch
IPC分类号: A61K31/44 , C07D241/12 , C07D213/30 , A61K31/505 , A61P43/00 , A61K31/498 , C07D241/42 , A61K31/5365 , C07D498/04 , C07D401/12 , A61K31/4965 , C07D239/26
CPC分类号: C07D241/12 , C07D213/30 , C07D213/61 , C07D213/64 , C07D215/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D237/08 , C07D239/26 , C07D249/18 , C07D277/24 , C07D277/62 , C07D401/04 , C07D401/06 , C07D471/04 , C07D498/04
摘要: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
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