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公开(公告)号：US08097634B2
公开(公告)日：2012-01-17
申请号：US13082433
申请日：2011-04-08
申请人： Jean Ackermann , Aurelia Conte , Daniel Hunziker , Werner Neidhart , Matthias Nettekoven , Tanja Schulz-Gasch , Stanley Wertheimer
发明人： Jean Ackermann , Aurelia Conte , Daniel Hunziker , Werner Neidhart , Matthias Nettekoven , Tanja Schulz-Gasch , Stanley Wertheimer
IPC分类号： A61K31/438 , C07D471/10
CPC分类号： C07D471/10
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2 and A are as described herein, compositions including the compounds and methods of using the compounds. The compounds inhibit hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, and obesity.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R 1，R 2和A如本文所述，包括该化合物的组合物和使用该化合物的方法。 该化合物抑制激素敏感性脂肪酶（HSL），可用于治疗糖尿病，代谢综合征和肥胖症。
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12.发明申请New Hexahydrocyclopentapyrrolone, Hexahydropyrrolopyrrolone, Octahydropyrrolopyridinone and Octahydropyridinone Compounds 有权新六氢环戊吡咯酮，六氢吡咯并吡咯酮，八氢吡咯并吡喃酮和八氢吡啶酮化合物公开(公告)号：US20120295934A1
公开(公告)日：2012-11-22
申请号：US13463863
申请日：2012-05-04
IPC分类号： A61K31/437 , C07D209/52 , A61K31/403 , C07D487/04 , A61K31/407 , A61P1/16 , A61P3/00 , A61P3/06 , A61P9/10 , A61P3/04 , A61P9/00 , A61P29/00 , C07D471/04 , A61P3/10
CPC分类号： C07D471/04 , C07D209/52 , C07D487/04
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, A, E, G and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used for the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R1，R2，A，E，G和n如本文所述，包括该化合物的组合物和使用该化合物的方法。 该化合物可用作激素敏感性脂肪酶（HSL）的抑制剂，可用于治疗糖尿病，代谢综合征，血脂异常，动脉粥样硬化，肥胖，心血管疾病，心肌功能障碍，炎症，非酒精性脂肪性肝病或非酒精性脂肪肝 脂肪性肝炎
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13.发明授权Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds 有权六氢环戊吡咯啉酮，六氢吡咯并吡咯啉酮，八氢吡咯并吡喃酮和八氢吡啶酮化合物公开(公告)号：US08501768B2
公开(公告)日：2013-08-06
申请号：US13463863
申请日：2012-05-04
IPC分类号： C07D209/52
CPC分类号： C07D471/04 , C07D209/52 , C07D487/04
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, A, E, G and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used for the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R1，R2，A，E，G和n如本文所述，包括该化合物的组合物和使用该化合物的方法。 该化合物可用作激素敏感性脂肪酶（HSL）的抑制剂，可用于治疗糖尿病，代谢综合征，血脂异常，动脉粥样硬化，肥胖，心血管疾病，心肌功能障碍，炎症，非酒精性脂肪性肝病或非酒精性脂肪肝 脂肪性肝炎
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公开(公告)号：US08497288B2
公开(公告)日：2013-07-30
申请号：US13461835
申请日：2012-05-02
IPC分类号： A61K31/4188 , A61K31/4439 , C07D401/02
CPC分类号： C07D487/04
摘要： The invention provides novel compounds having the general formula (I), wherein R1, R2, R3 and A are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease and non-alcoholic steatohepatitis.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 3和A如本文所述，包括该化合物的组合物和使用该化合物的方法。 这些化合物可用作激素敏感性脂肪酶（HSL）的抑制剂，可用于治疗糖尿病，代谢综合征，血脂异常，动脉粥样硬化，肥胖症，心血管疾病，心肌功能障碍，炎症，非酒精性脂肪性肝病和非酒精性脂肪肝 脂肪性肝炎
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公开(公告)号：US20120289549A1
公开(公告)日：2012-11-15
申请号：US13461835
申请日：2012-05-02
IPC分类号： A61K31/4188 , C07D487/04 , A61P3/10 , A61P3/00 , A61P1/16 , A61P9/10 , A61P3/04 , A61P9/00 , A61P29/00 , A61K31/4439 , A61P3/06
CPC分类号： C07D487/04
摘要： The invention provides novel compounds having the general formula (I), wherein R1, R2, R3 and A are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease and non-alcoholic steatohepatitis.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 3和A如本文所述，包括该化合物的组合物和使用该化合物的方法。 这些化合物可用作激素敏感性脂肪酶（HSL）的抑制剂，可用于治疗糖尿病，代谢综合征，血脂异常，动脉粥样硬化，肥胖症，心血管疾病，心肌功能障碍，炎症，非酒精性脂肪性肝病和非酒精性脂肪肝 脂肪性肝炎
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公开(公告)号：US09290451B2
公开(公告)日：2016-03-22
申请号：US13486057
申请日：2012-06-01
申请人： Caterina Bissantz , Uwe Grether , Paul Hebeisen , Atsushi Kimbara , Qingping Liu , Matthias Nettekoven , Marco Prunotto , Stephan Roever , Mark Rogers-Evans , Tanja Schulz-Gasch , Christoph Ullmer , Zhiwei Wang , Wulun Yang
发明人： Caterina Bissantz , Uwe Grether , Paul Hebeisen , Atsushi Kimbara , Qingping Liu , Matthias Nettekoven , Marco Prunotto , Stephan Roever , Mark Rogers-Evans , Tanja Schulz-Gasch , Christoph Ullmer , Zhiwei Wang , Wulun Yang
IPC分类号： C07D211/68 , C07D211/80 , C07D213/02 , C07D401/00 , C07D419/00 , C07D417/00 , C07D405/00 , C07D213/62 , C07D213/78 , C07D211/78 , C07D211/90 , C07D213/81 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D491/107
摘要： The invention relates to a compound of formula (I) Wherein R1, R2, R3 and R4 are defined as in the description and in the claims. The said compounds of the invention are preferential agoniste of the Carsonabinocid Receptor 2 and thus useful as medicaments and may be used in treatment of chronic pain, atherosclerosis, ischemic/reperfusion injury and other related diseases.A representative compound of this invention is 6-cyclopropylmethoxy-5-(tetrahydro-pyradine-2-carboxglic acid [1-methyl-1-(5-methyl-(1,2,4]oxadiazol-3-yl)-ethyl)-amide.
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公开(公告)号：US09321727B2
公开(公告)日：2016-04-26
申请号：US13486057
申请日：2012-06-01
申请人： Caterina Bissantz , Uwe Grether , Paul Hebeisen , Atsushi Kimbara , Qingping Liu , Matthias Nettekoven , Marco Prunotto , Stephan Roever , Mark Rogers-Evans , Tanja Schulz-Gasch , Christoph Ullmer , Zhiwei Wang , Wulun Yang
发明人： Caterina Bissantz , Uwe Grether , Paul Hebeisen , Atsushi Kimbara , Qingping Liu , Matthias Nettekoven , Marco Prunotto , Stephan Roever , Mark Rogers-Evans , Tanja Schulz-Gasch , Christoph Ullmer , Zhiwei Wang , Wulun Yang
IPC分类号： C07D211/68 , C07D211/80 , C07D213/02 , C07D401/00 , C07D419/00 , C07D417/00 , C07D405/00 , C07D213/62 , C07D213/78 , C07D211/78 , C07D211/90 , C07D213/81 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D491/107
CPC分类号： C07D213/81 , C07D213/79 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D491/107
摘要： The invention relates to a compound of formula (I) Wherein R1, R2, R3 and R4 are defined as in the description and in the claims. The said compounds of the invention are preferential agoniste of the Carsonabinocid Receptor 2 and thus useful as medicaments and may be used in treatment of chronic pain, atherosclerosis, ischemic/reperfusion injury and other related diseases.A representative compound of this invention is 6-cyclopropylmethoxy-5-(tetrahydro-pyradine-2-carboxglic acid [1-methyl-1-(5-methyl-(1,2,4]oxadiazol-3-yl)-ethyl)-amide.
摘要翻译： 本发明涉及式（I）化合物，其中R1，R2，R3和R4如说明书和权利要求中所定义。 所述本发明的化合物是卡桑那啶类受体2的优选激动剂，因此可用作药物，并且可用于治疗慢性疼痛，动脉粥样硬化，缺血/再灌注损伤和其它相关疾病。 本发明的代表性化合物是6-环丙基甲氧基-5-（四氢 - 吡啶-2-羧酸[1-甲基-1-（5-甲基 - （1,2,4]恶二唑-3-基） - 乙基） 酰胺。
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公开(公告)号：US20120316147A1
公开(公告)日：2012-12-13
申请号：US13486057
申请日：2012-06-01
申请人： Caterina Bissantz , Uwe Grether , Paul Hebeisen , Atsushi Kimbara , Qingping Liu , Matthias Nettekoven , Marco Prunotto , Stephan Roever , Mark Rogers-Evans , Tanja Schulz-Gasch , Christoph Ullmer , Zhiwei Wang , Wulun Yang
发明人： Caterina Bissantz , Uwe Grether , Paul Hebeisen , Atsushi Kimbara , Qingping Liu , Matthias Nettekoven , Marco Prunotto , Stephan Roever , Mark Rogers-Evans , Tanja Schulz-Gasch , Christoph Ullmer , Zhiwei Wang , Wulun Yang
IPC分类号： A61K31/4439 , C07D213/81 , A61K31/4418 , C07D413/12 , A61K31/44 , C07D405/04 , A61K31/4433 , C07D413/14 , C07D401/12 , A61K31/4545 , C07D417/12 , C07D401/04 , C07D417/14 , A61K31/541 , C07D401/14 , C07D491/107 , A61K31/5377 , C07D405/14 , A61K31/4709 , A61K31/501 , C07D405/12 , A61K31/506 , A61K31/5355 , A61P29/00 , A61P9/10 , A61P19/08 , A61P1/16 , A61P13/12 , A61P9/04 , A61P17/02 , A61P35/00 , A61K31/4427
CPC分类号： C07D213/81 , C07D213/79 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D491/107
摘要： The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
摘要翻译： 本发明涉及式（I）化合物，其中R 1至R 4如说明书和权利要求中所定义。 式（I）化合物可以用作药物。
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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：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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