公开(公告)号：US20170275283A1

公开(公告)日：2017-09-28

申请号：US15505277

申请日：2015-10-26

Applicant: Alexander PASTERNAK ,  Fa-Xiang DING ,  Shuzhi DONG ,  Jinlong JIANG ,  Haifeng TANG ,  Xin GU ,  Reynalda K. DEJESUS ,  Jessica FRIE ,  Qinghong FU ,  Takao SUZUKI ,  Zhifa PU ,  Merck Sharp & Dohme Corp.

Inventor： Alexander Pasternak ,  Fa-Xiang Ding ,  Shuzhi Dong ,  Jinlong Jiang ,  Haifeng Tang ,  Xin Gu ,  Reynalda K. DeJesus ,  Jessica Frie ,  Qinghong Fu ,  Takao Suzuki ,  Zhifa Pu

IPC: C07D471/10 ,  C07D498/10 ,  A61K31/5386 ,  A61K45/06 ,  A61K31/435 ,  A61K31/537 ,  C07D498/20 ,  A61K31/553 ,  A61K31/499 ,  A61K31/55

CPC classification number: C07D471/10 ,  A61K31/401 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/4422 ,  A61K31/499 ,  A61K31/537 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D487/10 ,  C07D498/10 ,  C07D498/20 ,  A61K2300/00

Abstract: 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：US09527830B2

公开(公告)日：2016-12-27

申请号：US14344681

申请日：2012-09-10

Applicant: Shawn Walsh ,  Alexander Pasternak ,  Brian Cato ,  Paul E. Finke ,  Jessica Frie ,  Qinghong Fu ,  Dooseop Kim ,  Barbara Pio ,  Aurash Shahripour ,  Zhi-Cai Shi ,  Haifeng Tang

Inventor： Shawn Walsh ,  Alexander Pasternak ,  Brian Cato ,  Paul E. Finke ,  Jessica Frie ,  Qinghong Fu ,  Dooseop Kim ,  Barbara Pio ,  Aurash Shahripour ,  Zhi-Cai Shi ,  Haifeng Tang

IPC: C07D403/14 ,  C07D401/10 ,  C07D405/14 ,  C07D413/14 ,  C07D403/10 ,  C07D405/06 ,  C07D405/12 ,  C07D487/04 ,  C07D211/28 ,  C07D211/62 ,  C07D211/48 ,  C07D471/08

CPC classification number: C07D401/10 ,  C07D211/28 ,  C07D211/48 ,  C07D211/62 ,  C07D403/10 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D471/08 ,  C07D487/04

Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.

公开(公告)号：US20070281969A1

公开(公告)日：2007-12-06

申请号：US11791183

申请日：2005-11-18

Applicant: Steven Colletti ,  James Tata ,  Hong Shen ,  Fa-Xiang Ding ,  Jessica Frie ,  Jason Imbriglio ,  Weichun Chen

Inventor： Steven Colletti ,  James Tata ,  Hong Shen ,  Fa-Xiang Ding ,  Jessica Frie ,  Jason Imbriglio ,  Weichun Chen

IPC: A61K31/192 ,  A61K31/47 ,  A61P3/00 ,  A61P9/10 ,  C07C229/40 ,  C07D215/12

CPC classification number: C07D217/02 ,  C07C233/55 ,  C07C235/38 ,  C07C317/44 ,  C07D209/08 ,  C07D209/88 ,  C07D209/94 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/80 ,  C07D215/12 ,  C07D231/12 ,  C07D231/56 ,  C07D239/26 ,  C07D261/08 ,  C07D271/113 ,  C07D277/30 ,  C07D307/54 ,  C07D307/79 ,  C07D317/60 ,  C07D333/24 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/14

Abstract: The present invention encompasses compounds of Formula (I); as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.

Abstract translation: 本发明包括式（I）的化合物; 以及其药学上可接受的盐和水合物，其可用于治疗血脂异常。 还包括药物组合物和使用方法。

公开(公告)号：US20160002259A1

公开(公告)日：2016-01-07

申请号：US14768245

申请日：2014-02-12

Applicant: 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.

Inventor： 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: C07D498/04 ,  A61K45/06 ,  A61K31/4985 ,  A61K31/5383 ,  C07D487/04

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20070299101A1

公开(公告)日：2007-12-27

申请号：US11666966

申请日：2005-10-31

Applicant: Steven Colletti ,  Richard Beresis ,  Weichun Chen ,  James Tata ,  Hong Shen ,  Daria Marley ,  Qiaolin Deng ,  Jessica Frie ,  Fa-Xiang Ding

Inventor： Steven Colletti ,  Richard Beresis ,  Weichun Chen ,  James Tata ,  Hong Shen ,  Daria Marley ,  Qiaolin Deng ,  Jessica Frie ,  Fa-Xiang Ding

IPC: A61K31/47 ,  A61K31/195 ,  A61K31/403 ,  A61K31/41 ,  A61P3/10 ,  C07C233/64 ,  C07D215/02 ,  C07D257/04 ,  C07D487/00 ,  C07D513/00 ,  C07D471/02 ,  C07D217/00 ,  C07D209/56 ,  A61P9/00 ,  A61K31/425 ,  A61K31/428 ,  A61K31/437

CPC classification number: C07C233/55 ,  C07C235/38 ,  C07C237/20 ,  C07C237/22 ,  C07C255/57 ,  C07C259/10 ,  C07C271/30 ,  C07C271/58 ,  C07C275/42 ,  C07C311/08 ,  C07C311/13 ,  C07D213/80 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/227 ,  C07D215/38 ,  C07D217/02 ,  C07D217/24 ,  C07D231/54 ,  C07D231/56 ,  C07D235/30 ,  C07D257/04 ,  C07D261/20 ,  C07D277/82 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention relates to niacin receptor agonists of formula: (I); as well as pharmaceutically acceptable salts and solvates. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels. Pharmaceutical compositions and methods of treatment are also included.

Abstract translation: 本发明涉及式（I）的烟酸受体激动剂： 以及药学上可接受的盐和溶剂合物。 该化合物可用于治疗血脂异常，特别是降低血清LDL，VLDL和甘油三酸酯，并提高HDL水平。 还包括药物组合物和治疗方法。

公开(公告)号：US20180016263A1

公开(公告)日：2018-01-18

申请号：US15545891

申请日：2016-02-08

Applicant: Alexander PASTERNAK ,  Jessica FRIE ,  Shuzhi DONG ,  Takao SUZUKI ,  Shouning XU ,  Merck Sharp & Dohme Corp.

Inventor： Alexander Pasternak ,  Jessica Frie ,  Shuzhi Dong ,  Takao Suzuki ,  Shouning Xu

IPC: C07D405/14 ,  A61K31/496 ,  C07D413/14

CPC classification number: C07D405/14 ,  A61K31/496 ,  A61K2300/00 ,  A61P9/00 ,  C07D413/14

Abstract: 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：US09850245B2

公开(公告)日：2017-12-26

申请号：US15505277

申请日：2015-10-26

Applicant: Merck Sharp & Dohme Corp. ,  Alexander Pasternak ,  Fa-Xiang Ding ,  Shuzhi Dong ,  Jinlong Jiang ,  Haifeng Tang ,  Xin Gu ,  Reynalda K. DeJesus ,  Jessica Frie ,  Qinghong Fu ,  Takao Suzuki ,  Zhifa Pu

Inventor： Alexander Pasternak ,  Fa-Xiang Ding ,  Shuzhi Dong ,  Jinlong Jiang ,  Haifeng Tang ,  Xin Gu ,  Reynalda K. DeJesus ,  Jessica Frie ,  Qinghong Fu ,  Takao Suzuki ,  Zhifa Pu

IPC: C07D471/10 ,  A61K31/499 ,  C07D498/10 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/435 ,  A61K31/537 ,  C07D498/20 ,  A61K31/553 ,  A61K45/06

CPC classification number: C07D471/10 ,  A61K31/401 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/4422 ,  A61K31/499 ,  A61K31/537 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D487/10 ,  C07D498/10 ,  C07D498/20 ,  A61K2300/00

Abstract: 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.