公开(公告)号：US20130059830A1

公开(公告)日：2013-03-07

申请号：US13696831

申请日：2011-05-16

申请人： Fa-Xiang Ding ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Cangming Yang

发明人： Fa-Xiang Ding ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Cangming Yang

IPC分类号： A61K31/506 ,  C07D413/14 ,  A61P3/00 ,  A61K31/55 ,  A61P3/04 ,  A61P3/10 ,  C07D401/14 ,  A61K31/5377

CPC分类号： C07D401/14 ,  C07D413/14

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：US08785634B2

公开(公告)日：2014-07-22

申请号：US13638976

申请日：2011-04-21

申请人： Fa-Xiang Ding ,  JinLong Jiang ,  Dong-Ming Shen ,  Hong Shen ,  Zhi-Cai Shi

发明人： Fa-Xiang Ding ,  JinLong Jiang ,  Dong-Ming Shen ,  Hong Shen ,  Zhi-Cai Shi

IPC分类号： C07D401/00

CPC分类号： C07D491/20 ,  C07D491/10

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 enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.

摘要翻译： 结构式（I）的化合物是脯氨酰羧肽酶（PrCP）的抑制剂。 本发明的化合物可用于预防和治疗与PrCP的酶活性相关的病症，例如异常代谢，包括肥胖症; 糖尿病; 代谢综合征; 肥胖相关疾病; 和糖尿病相关疾病。

公开(公告)号：US20130023515A1

公开(公告)日：2013-01-24

申请号：US13638976

申请日：2011-04-21

申请人： Fa-Xiang Ding ,  Jinlong Jiang ,  Dong-Ming Shen ,  Hong Shen ,  Zhi-Cai Shi

发明人： Fa-Xiang Ding ,  Jinlong Jiang ,  Dong-Ming Shen ,  Hong Shen ,  Zhi-Cai Shi

IPC分类号： C07D491/107 ,  C07D491/20 ,  A61K31/438 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/497 ,  A61K31/501 ,  A61K31/519 ,  A61K31/4985 ,  A61K31/44 ,  A61P3/04 ,  A61P3/10 ,  A61P3/00 ,  A61K31/444

CPC分类号： C07D491/20 ,  C07D491/10

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 enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.

摘要翻译： 结构式（I）的化合物是脯氨酰羧肽酶（PrCP）的抑制剂。 本发明的化合物可用于预防和治疗与PrCP的酶活性相关的病症，例如异常代谢，包括肥胖症; 糖尿病; 代谢综合征; 肥胖相关障碍; 和糖尿病相关疾病。

公开(公告)号：US20160024091A1

公开(公告)日：2016-01-28

申请号：US14774390

申请日：2014-03-10

申请人： Alexander PASTERNAK ,  Fa-Xiang DING ,  Shuzhi DONG ,  Haifeng TANG ,  Jinlong JIANG ,  Cangming YANG ,  Dipshikha BISWAS ,  MERCK SHARP & DOHME CORP.

发明人： Alexander Pasternak ,  Fa-Xiang Ding ,  Shuzhi Dong ,  Dipshikha Biswas ,  Haifeng Tang ,  Jinlong Jiang ,  Cangming Yang ,  Xin Gu

IPC分类号： C07D471/10 ,  A61K31/444 ,  A61K31/506 ,  A61K31/435 ,  A61K31/5386 ,  A61K31/501 ,  C07D471/20 ,  A61K31/4995 ,  C07D498/20 ,  A61K45/06 ,  A61K31/497

CPC分类号： C07D471/10 ,  A61K31/24 ,  A61K31/401 ,  A61K31/403 ,  A61K31/405 ,  A61K31/407 ,  A61K31/41 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/4422 ,  A61K31/444 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/551 ,  A61K31/554 ,  A61K31/585 ,  A61K31/675 ,  A61K45/06 ,  C07D471/20 ,  C07D498/20 ,  A61K2300/00

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.

摘要翻译： 本发明提供式I化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。 这些化合物可以用作利尿剂和/或利尿钠剂，并且用于治疗和预防包括心血管疾病如高血压，心力衰竭和慢性肾脏疾病以及与过量的盐和水保留有关的病症的医学病症。

公开(公告)号：US10947222B2

公开(公告)日：2021-03-16

申请号：US16461880

申请日：2017-11-13

申请人： Merck Sharp & Dohme Corp. ,  Dong-Ming Shen ,  Thomas H. Graham ,  Jinlong Jiang ,  Fa-Xiang Ding ,  Clare Tudge

发明人： Dong-Ming Shen ,  Thomas H. Graham ,  Jinlong Jiang ,  Fa-Xiang Ding ,  Clare Tudge

IPC分类号： C07D401/12 ,  C07D409/12 ,  A61P1/16 ,  C07D209/08 ,  C07D409/14 ,  C07D413/12 ,  A61K31/506 ,  A61K45/06 ,  C07D413/14 ,  A61K31/404 ,  A61K31/4439 ,  C07D209/10

摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

公开(公告)号：US20190276443A1

公开(公告)日：2019-09-12

申请号：US16461880

申请日：2017-11-13

申请人： Dong-Ming SHEN ,  Thomas H. GRAHAM ,  Jinlong JIANG ,  Fa-Xiang DING ,  Clare TUDGE ,  Merck Sharp & Dohme Corp.

发明人： Dong-Ming Shen ,  Thomas H. Graham ,  Jinlong Jiang ,  Fa-Xiang Ding ,  Clare Tudge

IPC分类号： C07D409/12 ,  A61P1/16 ,  C07D209/08 ,  C07D401/12 ,  C07D413/12 ,  C07D409/14

摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

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.

公开(公告)号：US20160324833A1

公开(公告)日：2016-11-10

申请号：US15101481

申请日：2014-12-19

申请人： Shuzhi DONG ,  Alexander PASTERNAK ,  Xin GU ,  Qinghong FU ,  Jinlong JIANG ,  Fa-Xiang DING ,  Haifeng TANG ,  Reynalda K. DEJESUS ,  Takao SUZUKI ,  MERCK SHARP & DOHME CORP.

发明人： Shuzhi Dong ,  Alexander Pasternak ,  Xin Gu ,  Qinghong Fu ,  Jinlong Jiang ,  Fa-Xiang Ding ,  Haifeng Tang ,  Reynalda K. DeJesus ,  Takao Suzuki

IPC分类号： A61K31/435 ,  C07D471/10 ,  A61K31/444 ,  A61K31/506 ,  A61K31/438 ,  C07D498/10 ,  A61K31/537 ,  A61K31/497 ,  C07D519/00 ,  A61K31/437 ,  A61K45/06 ,  A61K31/501

CPC分类号： A61K31/435 ,  A61K31/437 ,  A61K31/438 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/537 ,  A61K45/06 ,  C07D471/10 ,  C07D498/10 ,  C07D519/00 ,  A61K2300/00

摘要： Novel spirocyclic compounds of formula I: and pharmaceutically acceptable salts thereof are disclosed as 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. Pharmaceutical compositions and methods of treatment are also included.

公开(公告)号：US20160002259A1

公开(公告)日：2016-01-07

申请号：US14768245

申请日：2014-02-12

申请人： Alexander PASTERNAK ,  Reynalda Keh DE JESUS ,  Fa-xiang DING ,  Shuzhi DONG ,  Jessica FRIE ,  Xin GU ,  Jinlong JIANG ,  Aurash SHAHRIPOUR ,  Barbara PIO ,  Haifeng TANG ,  Shawn WALSH ,  MERCK SHARP & DOHME CORP.

发明人： Alexander Pasternak ,  Reynalda Keh DeJesus ,  Fa-Xiang Ding ,  Shuzhi Dong ,  Jessica L. Frie ,  Xin Gu ,  Jinlong Jiang ,  Aurash Shahripour ,  Barbara Pio ,  Haifeng Tang ,  Shawn Walsh

IPC分类号： C07D498/04 ,  A61K45/06 ,  A61K31/4985 ,  A61K31/5383 ,  C07D487/04

CPC分类号： C07D498/04 ,  A61K31/401 ,  A61K31/403 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4422 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/55 ,  A61K31/675 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00 ,  A61K2300/00

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, kidney disease, edema, and conditions associated with excessive salt and water retention.

摘要翻译： 本发明提供式I化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。 该化合物可以用作利尿剂和/或利尿钠剂，并用于治疗和预防包括心血管疾病如高血压，心力衰竭，肾脏疾病，水肿以及与过量的盐和水保留有关的病症的医学病症。