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。

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。

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.

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。

公开(公告)号：US08410284B2

公开(公告)日：2013-04-02

申请号：US13124898

申请日：2009-10-12

申请人： 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 ,  Brett C. Bookser

发明人： 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 ,  Brett C. Bookser

IPC分类号： A61K31/675 ,  C07F9/00 ,  C07F9/6506

CPC分类号： C07F9/65068 ,  C07F9/65583 ,  C07F9/657181

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。

公开(公告)号：US20110263533A1

公开(公告)日：2011-10-27

申请号：US13124898

申请日：2009-10-12

申请人： 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 ,  Brett C. Bookser

发明人： 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 ,  Brett C. Bookser

IPC分类号： A61K31/675 ,  C07F9/40 ,  C07F9/6574 ,  A61P35/00 ,  A61P3/04 ,  A61P3/06 ,  A61P9/12 ,  C07F9/6506 ,  A61P3/10

CPC分类号： C07F9/65068 ,  C07F9/65583 ,  C07F9/657181

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。

公开(公告)号：US20130040929A1

公开(公告)日：2013-02-14

申请号：US13642646

申请日：2011-05-06

申请人： Jeffrey J. Hale ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Zhicai Wu ,  Cangming Yang

发明人： Jeffrey J. Hale ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Zhicai Wu ,  Cangming Yang

IPC分类号： A61K31/506 ,  C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61P3/00 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/4985 ,  A61P3/04 ,  A61P3/10 ,  C07D401/14 ,  A61K31/497

CPC分类号： C07D401/04 ,  C07D401/14

摘要： Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.

公开(公告)号：US09365539B2

公开(公告)日：2016-06-14

申请号：US13642646

申请日：2011-05-06

申请人： Jeffrey J. Hale ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Zhicai Wu ,  Cangming Yang

发明人： Jeffrey J. Hale ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Zhicai Wu ,  Cangming Yang

IPC分类号： A61K31/397 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D401/04 ,  C07D401/14

摘要： Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.

公开(公告)号：US10208064B2

公开(公告)日：2019-02-19

申请号：US15323989

申请日：2015-07-09

申请人： MERCK SHARP & DOHME CORP. ,  Alexander Pasternak ,  Ian Davies ,  Fa-Xiang Ding ,  Jinlong Jiang ,  Shuzhi Dong ,  Xin Gu ,  Takao Suzuki ,  Joseph P. Vacca ,  Zhifa Pu ,  Shouning Xu

发明人： Alexander Pasternak ,  Ian Davies ,  Fa-Xiang Ding ,  Jinlong Jiang ,  Shuzhi Dong ,  Xin Gu ,  Takao Suzuki ,  Joseph P. Vacca ,  Zhifa Pu ,  Shouning Xu

IPC分类号： C07D513/10 ,  C07D519/00 ,  A61K45/06 ,  A61K31/435 ,  A61K31/4745 ,  A61K31/4375

摘要： The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

公开(公告)号：US20170197989A1

公开(公告)日：2017-07-13

申请号：US15323989

申请日：2015-07-09

申请人： Alexander PASTERNAK ,  Ian DAVIES ,  Fa-Xiang DING ,  Jinlong JIANG ,  Shuzhi DONG ,  Xin GU ,  Takao SUZUKI ,  Joseph P. VACCA ,  Zhifa PU ,  Shouning XU ,  Merck Sharp & Dohme Corp.

发明人： Alexander Pasternak ,  Ian Davies ,  Fa-Xiang Ding ,  Jinlong Jiang ,  Shuzhi Dong ,  Xin Gu ,  Takao Suzuki ,  Joseph P. Vacca ,  Zhifa Pu ,  Shouning Xu

IPC分类号： C07D519/00 ,  A61K31/4745 ,  A61K31/4375 ,  A61K31/435

CPC分类号： C07D519/00 ,  A61K31/435 ,  A61K31/4375 ,  A61K31/4745 ,  A61K45/06

摘要： The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.