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公开(公告)号：US06350760B1
公开(公告)日：2002-02-26
申请号：US09585111
申请日：2000-06-01
申请人： Raman K. Bakshi , Khaled J. Barakat , Ravi P. Nargund , Brenda L. Palucki , Arthur A. Patchett , Iyassu Sebhat , Zhixiong Ye , Leonardus H. T. Van Der Ploeg
发明人： Raman K. Bakshi , Khaled J. Barakat , Ravi P. Nargund , Brenda L. Palucki , Arthur A. Patchett , Iyassu Sebhat , Zhixiong Ye , Leonardus H. T. Van Der Ploeg
IPC分类号： A61K3144
CPC分类号： C07D231/12 , A61K31/4725 , A61K31/4985 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction. Also provided are methods of treating sexual dysfunction with a compound that is a selective agonist of MC-4R over any other human melanocortin receptor.
摘要翻译： 某些新的取代的哌啶化合物是人类黑皮质素受体的激动剂，特别是人黑素皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。 还提供了使用作为MC-4R的选择性激动剂的化合物超过任何其它人类黑皮质素受体来治疗性功能障碍的方法。
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公开(公告)号：US20060035935A1
公开(公告)日：2006-02-16
申请号：US11239721
申请日：2005-09-30
申请人： Mark Goulet , Ravi Nargund , Iyassu Sebhat , Feroze Ujjainwalla , Thomas Walsh , Daniel Warner , Zhixiong Ye , Jonathan Young , Raman Bakshi
发明人： Mark Goulet , Ravi Nargund , Iyassu Sebhat , Feroze Ujjainwalla , Thomas Walsh , Daniel Warner , Zhixiong Ye , Jonathan Young , Raman Bakshi
IPC分类号： A61K31/454 , C07D417/02 , C07D413/02 , C07D403/02 , C07D401/02
CPC分类号： C07D491/08 , A61K31/445 , C07D211/62 , C07D211/64 , C07D401/06 , C07D401/14 , C07D413/06 , C07D413/14
摘要： Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
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3.发明申请公开(公告)号：US20080051430A1
公开(公告)日：2008-02-28
申请号：US11632001
申请日：2005-07-13
申请人： Khaled Barakat , Liangqin Guo , Jian Liu , Ravi Nargund , Iyassu Sebhat , Zhixiong Ye
发明人： Khaled Barakat , Liangqin Guo , Jian Liu , Ravi Nargund , Iyassu Sebhat , Zhixiong Ye
IPC分类号： A61K31/451 , A61P15/00 , A61P15/10 , A61P3/04 , C07D401/06 , C07D411/14
CPC分类号： C07D211/62 , C07D401/06 , C07D401/14
摘要： Certain novel N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
摘要翻译： 某些新的N-酰化哌啶衍生物是人类黑皮质素受体的激动剂，特别是人黑皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。
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4.发明申请公开(公告)号：US20060183904A1
公开(公告)日：2006-08-17
申请号：US10548350
申请日：2004-03-31
申请人： Liangqin Guo , Shuwen He , Tianying Jian , Jian Liu , Yingjie Lai , Ravi Nargund , Iyassu Sebhat , Feroze Ujjainwalla , Zhixiong Ye , Jonathan Young
发明人： Liangqin Guo , Shuwen He , Tianying Jian , Jian Liu , Yingjie Lai , Ravi Nargund , Iyassu Sebhat , Feroze Ujjainwalla , Zhixiong Ye , Jonathan Young
IPC分类号： C07D401/00 , C07D453/00
CPC分类号： A61K31/445 , C07D401/06 , C07D401/14 , C07D471/10 , C07D491/10
摘要： Certain novel N-acylated spiropiperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
摘要翻译： 某些新的N-酰化螺哌啶衍生物是人类黑皮质素受体的激动剂，特别是人黑素皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。
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公开(公告)号：US08394969B2
公开(公告)日：2013-03-12
申请号：US12563782
申请日：2009-09-21
申请人： Brett C. Bookser , Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka
发明人： Brett C. Bookser , Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka
IPC分类号： A61K31/4184 , C07D235/26 , C07D235/28 , C07D235/30
CPC分类号： C07D235/26 , C07D235/28 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
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公开(公告)号：US20110218174A1
公开(公告)日：2011-09-08
申请号：US13125345
申请日：2009-10-22
申请人： Jianming Bao , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , Dariusz Wodka , Qun Dang , De Michael Chung , Tony S. Gibson , Hongjian Jiang , Daniel K. Cashion
发明人： Jianming Bao , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , Dariusz Wodka , Qun Dang , De Michael Chung , Tony S. Gibson , Hongjian Jiang , Daniel K. Cashion
IPC分类号： A61K31/675 , C07F9/6506 , C07F9/6533 , C07F9/6574 , A61P35/00 , A61P3/10 , A61P3/00 , A61P3/04 , A61P9/12 , A61P3/06
CPC分类号： C07F9/65068 , A61K31/366 , A61K31/397 , A61K31/4184 , A61K31/4412 , A61K45/06 , C07F9/65583 , C07F9/65742 , A61K2300/00
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
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公开(公告)号：US20160002224A1
公开(公告)日：2016-01-07
申请号：US14769159
申请日：2014-03-10
申请人： John J. ACTON, III , Rajan ANAND , Ashok ARASAPPAN , Qun DANG , Iyassu SEBHAT , Zhifa PU , Takao SUZUKI , MERCK SHARP & DOHME CORP.
发明人： John J. Acton, III , Rajan Anand , Ashok Arasappan , Qun Dang , Iyassu Sebhat , Zhifa Pu , Takao Suzuki
IPC分类号： C07D471/04 , A61K31/404 , A61K31/437 , A61K31/4985 , A61K31/4439 , A61K31/366 , A61K31/397 , C07D209/08 , C07D401/10
CPC分类号： C07D471/04 , A61K31/366 , A61K31/397 , A61K31/404 , A61K31/437 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/541 , C07D209/08 , C07D209/12 , C07D209/18 , C07D209/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/10 , C07D413/04 , C07D413/10 , C07D493/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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![NOVEL AZABENZIMIDAZOLE HEXAHYDROFURO[E,2-B]FURAN DERIVATIVES](/abs-image/US/2015/10/08/US20150284411A1/abs.jpg.150x150.jpg)
公开(公告)号：US20150284411A1
公开(公告)日：2015-10-08
申请号：US14419774
申请日：2013-08-19
申请人： James M. APGAR , Ashok ARASAPPAN , Tesfaye BIFTU , Ping CHEN , Danqing FENG , Erin GUIDRY , Jacqueline HICKS , Ahmet KEKEC , Kenneth LEAVITT , Bing LI , Troy MCCRACKEN , Iyassu SEBHAT , Xiaoxia QIAN , Lan WEI , Robert WILKENING , Zhicai WU , Merck Sharp & Dohme Corp.
发明人： James M. Apgar , Ashok Arasappan , Tesfaye Biftu , Ping Chen , Danqing Feng , Erin Guidry , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Troy McCracken , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： C07D519/00 , A61K31/438 , A61K45/06 , A61K31/501 , A61K31/5377 , A61K31/541 , A61K31/437 , A61K31/506
CPC分类号： C07D519/00 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/438 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K2300/00
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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9.发明申请公开(公告)号：US20110195964A1
公开(公告)日：2011-08-11
申请号：US13125329
申请日：2009-10-19
申请人： Qun Dang , De Michael Chung , Tony S. Gibson , Daniel K. Cashion , HongJian Jiang , Jianming Bao , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , Dariusz Wodka
发明人： Qun Dang , De Michael Chung , Tony S. Gibson , Daniel K. Cashion , HongJian Jiang , Jianming Bao , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , Dariusz Wodka
IPC分类号： A61K31/5377 , C07D235/28 , A61K31/4184 , A61P3/10 , A61P3/04 , A61P3/06 , A61P35/00 , A61P9/12 , C07D405/10 , C07D401/10 , A61K31/4439 , A61K31/454 , C07D413/10 , C07D403/10 , A61K31/497
CPC分类号： C07D235/28 , C07D235/26 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/10 , C07D405/04 , C07D409/04 , C07D409/06 , C07D417/04
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖，高胆固醇血症和高血压。
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10.发明申请公开(公告)号：US20100081643A1
公开(公告)日：2010-04-01
申请号：US12563782
申请日：2009-09-21
申请人： BRETT C. BOOKSER , Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka
发明人： BRETT C. BOOKSER , Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka
IPC分类号： A61K31/4184 , C07D235/26 , C07D403/12 , C07D401/12 , C07D413/10 , A61K31/397 , A61K31/44 , A61K31/5025 , A61K31/4439 , A61P3/00 , A61P9/00
CPC分类号： C07D235/26 , C07D235/28 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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