公开(公告)号：US20140206618A1

公开(公告)日：2014-07-24

申请号：US14239649

申请日：2012-08-16

申请人： Alexander Pasternak ,  Timothy Blizzard ,  Harry Chobanian ,  Reynalda de Jesus ,  Fa-Xiang Ding ,  Shuzhi Dong ,  Candido Gude ,  Dooseop Kim ,  Haifeng Tang ,  Shawn Walsh ,  Barbara Pio ,  Jinlong Jiang

发明人： Alexander Pasternak ,  Timothy Blizzard ,  Harry Chobanian ,  Reynalda de Jesus ,  Fa-Xiang Ding ,  Shuzhi Dong ,  Candido Gude ,  Dooseop Kim ,  Haifeng Tang ,  Shawn Walsh ,  Barbara Pio ,  Jinlong Jiang

IPC分类号： C07D498/04 ,  A61K45/06 ,  A61K31/4985 ,  C07D513/04 ,  A61K31/542 ,  C07D487/04 ,  A61K31/5383 ,  A61K31/553

CPC分类号： C07D498/04 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/553 ,  A61K45/06 ,  C07D487/04 ,  C07D513/04

摘要： The present invention provides compounds of Formula Ia 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 conditions associated with excessive salt and water retention.

摘要翻译： 本发明提供式Ia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，心力衰竭以及与过量盐和保水有关的病症的医学病症。

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。