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公开(公告)号：US20210115044A1
公开(公告)日：2021-04-22
申请号：US17048811
申请日：2019-04-22
发明人： Tao Yu , James M. Apgar , Alan Whitehead , Yonglian Zhang , Zhiyong Hu , Valerie W. Shurtleff , John A. McCauley , Izzat T. Raheem
IPC分类号： C07D471/16 , A61K31/4985 , A61P31/18 , A61K31/52 , A61K31/435 , A61K31/5383 , A61K31/506 , A61K31/513 , A61K31/685 , A61K31/427
摘要： The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
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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：US10786488B2
公开(公告)日：2020-09-29
申请号：US16479997
申请日：2018-01-23
发明人： Tao Yu , John A. McCauley , Alan Whitehead , James M. Apgar , Izzat T. Raheem , Guizhen Dong , Sherman T. Waddell , Hong Li
IPC分类号： A61K31/4375 , A61K31/427 , A61K31/4402 , A61K31/47 , A61K31/506 , A61K31/5365 , A61K31/675 , A61K31/7068 , A61K31/7076 , C07D491/147
摘要： The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
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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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公开(公告)号：US10144741B2
公开(公告)日：2018-12-04
申请号：US15910571
申请日：2018-03-02
发明人： Katherine Young , David B. Olsen , Sheo B. Singh , Jing Su , Robert R. Wilkening , James M. Apgar , Dongfang Meng , Dann Parker , Mihir Mandal , Lihu Yang , Ronald E. Painter , Qun Dang , Takao Suzuki
IPC分类号： C07D493/08 , C07F7/18 , C07D493/18 , C07C309/06 , C07C53/18
摘要： The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.
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公开(公告)号：US09944654B2
公开(公告)日：2018-04-17
申请号：US15517570
申请日：2015-10-21
发明人： Katherine Young , David B. Olsen , Sheo B. Singh , Jing Su , Robert R. Wilkening , James M. Apgar , Dongfang Meng , Dann Parker , Mihir Mandal , Lihu Yang , Ronald E. Painter , Qun Dang , Takao Suzuki
IPC分类号： C07D493/08 , C07C53/18 , C07C309/06 , C07D493/18 , C07F7/18
CPC分类号： C07D493/08 , C07C53/18 , C07C309/06 , C07D493/18 , C07D519/00 , C07F7/1804
摘要： The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.
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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：US20180186808A1
公开(公告)日：2018-07-05
申请号：US15910571
申请日：2018-03-02
发明人： Katherine Young , David B. Olsen , Sheo B. Singh , Jing Su , Robert R. Wilkening , James M. Apgar , Dongfang Meng , Dann Parker , Mihir Mandal , Lihu Yang , Ronald E. Painter , Qun Dang , Takao Suzuki
IPC分类号： C07D493/08 , C07F7/18 , C07C53/18 , C07C309/06 , C07D493/18
CPC分类号： C07D493/08 , C07C53/18 , C07C309/06 , C07D493/18 , C07D519/00 , C07F7/1804
摘要： The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.
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公开(公告)号：US09382243B2
公开(公告)日：2016-07-05
申请号：US14419842
申请日：2013-08-16
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： C07D471/02 , A61K31/00 , C07D471/04 , A61K31/366 , A61K31/397 , A61K31/4985 , A61K31/437 , A61K31/444 , A61K45/06
CPC分类号： C07D471/04 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/444 , A61K31/4985 , 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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公开(公告)号：US20150218149A1
公开(公告)日：2015-08-06
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： C07D417/14 , A61K31/4184 , C07D405/14 , A61K31/4192 , C07D413/14 , A61K31/4985 , A61K31/4196 , A61K31/427 , A61K31/506 , A61K31/366 , A61K31/397 , C07D405/12 , 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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