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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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2.发明申请NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS 有权用作抗糖尿病药物的新型CYABAZABENZIMIDAZOLE衍生物公开(公告)号：US20130123237A1
公开(公告)日：2013-05-16
申请号：US13812536
申请日：2012-02-23
申请人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
发明人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： A61K31/5377 , A61K31/437 , A61K31/4985 , A61K31/351 , A61K31/397 , A61K31/4412 , C07D471/04 , A61K31/496
CPC分类号： A61K31/5377 , A61K31/351 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/4412 , A61K31/496 , A61K31/4985 , A61K31/519 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of 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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公开(公告)号：US08796258B2
公开(公告)日：2014-08-05
申请号：US13812536
申请日：2012-02-23
申请人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
发明人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： A61K31/00 , C07D513/02
CPC分类号： A61K31/5377 , A61K31/351 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/4412 , A61K31/496 , A61K31/4985 , A61K31/519 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of 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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4.发明申请SUBSTITUTED SEVEN-MEMBERED HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES 有权作为用于治疗糖尿病的DIPEPTIDYDEPDDIV-IV抑制剂的取代的七分子杂环化合物公开(公告)号：US20130203786A1
公开(公告)日：2013-08-08
申请号：US13643121
申请日：2011-05-16
IPC分类号： C07D487/04 , A61K31/506 , A61K45/06 , A61K31/519 , A61K31/437 , A61K31/4162 , A61K31/4439
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K45/06 , C07D471/04
摘要： The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及结构式（I）的新型氨基取代的七元杂环化合物，其为二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防其中二肽基肽酶-IV酶 涉及糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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5.发明授权Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes 有权取代的七元杂环化合物作为二肽基肽酶-IV抑制剂用于治疗糖尿病公开(公告)号：US08980929B2
公开(公告)日：2015-03-17
申请号：US13643121
申请日：2011-05-16
IPC分类号： A01N43/78 , A61K31/425 , C07D413/00 , C07D498/00 , C07D417/00 , C07D513/00 , C07D271/12 , C07D285/14 , C07D487/04 , C07D471/04 , A61K31/4162 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K45/06
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K45/06 , C07D471/04
摘要： The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及结构式（I）的新型氨基取代的七元杂环化合物，其为二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防其中二肽基肽酶-IV酶 涉及糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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公开(公告)号：US20190352294A1
公开(公告)日：2019-11-21
申请号：US16461849
申请日：2017-11-13
申请人： Ashwin RAO , Brian Alexander MCKITTRICK , Matthew LOMBARDO , Jacqueline D. HICKS , Amy Bittner MCCRACKEN , Hong Dong CHU , Sung-Sau SO , Peter ORTH , Zhicai WU , Ping LAN , John S. DEBENHAM , Brent R. WHITEHEAD , Jerry A. TAYLOR , Zhongxiang SUN , Revathi Reddy KATIPALLY , Jonathan E. GABLE , Markus K. DAHLGREN , Sathesh P. BHAT , Merck Sharp & Dohme Corp.
发明人： Ashwin U. Rao , Brian Alexander McKittrick , Matthew Lombardo , Jacqueline D. Hicks , Amy Bittner McCracken , Hong Dong Chu , Sung-Sau So , Peter Orth , Zhicai Wu , Ping Lan , John S. Debenham , Brent R. Whitehead , Jerry A. Taylor , Zhongxiang Sun , Revathi Reddy Katipally , Jonathan E. Gable , Markus K. Dahlgren , Sathesh P. Bhat
IPC分类号： C07D413/14 , C07D495/04 , A61P7/02
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIIa inhibitors.
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公开(公告)号：US09868733B2
公开(公告)日：2018-01-16
申请号：US14419825
申请日：2013-08-19
发明人： James M. Apgar , Tesfaye Biftu , Ping Chen , Danqing Feng , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu , Ashok Arasappan
IPC分类号： C07D471/04 , C07D519/00 , A61K31/366 , A61K31/397 , A61K31/4985 , A61K31/19 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/5377 , C07C53/18
CPC分类号： C07D471/04 , A61K31/19 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/4985 , A61K31/5377 , C07C53/18 , 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.
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公开(公告)号：US09527839B2
公开(公告)日：2016-12-27
申请号：US14420090
申请日：2013-08-15
发明人： James M. Apgar , Tesfaye Biftu , Ping Chen , Danqing Feng , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , A61K31/4184 , A61K31/4196 , A61K31/427 , A61K31/506 , A61K31/5377 , A61K45/06
CPC分类号： C07D417/14 , A61K31/4184 , A61K31/4196 , A61K31/427 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D405/12 , C07D405/14 , C07D413/14
摘要： Novel compounds described herein are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPKactivated 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： 本文所述的新型化合物是AMP-蛋白激酶的活化剂，并且可用于治疗，预防和抑制由AMPK活化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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公开(公告)号：US09540364B2
公开(公告)日：2017-01-10
申请号：US14420024
申请日：2013-08-15
发明人： James M. Apgar , Tesfaye Biftu , Ping Chen , Danqing Feng , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , A61K31/366 , A61K31/397 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/427 , A61K31/4985 , A61K31/506 , A61K31/5377
CPC分类号： C07D417/14 , A61K31/366 , A61K31/397 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/427 , A61K31/4985 , A61K31/506 , A61K31/5377 , C07D405/12 , C07D405/14 , C07D413/14
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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![Azabenzimidazole hexahydrofuro[3,2-b]furan derivatives](/abs-image/US/2016/03/22/US09290517B2/abs.jpg.150x150.jpg)
公开(公告)号：US09290517B2
公开(公告)日：2016-03-22
申请号：US14419774
申请日：2013-08-19
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： C07D401/14 , A61K31/437 , C07D519/00 , A61K31/438 , A61K31/506 , A61K31/501 , A61K31/5377 , A61K31/541 , A61K45/06
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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