公开(公告)号：US20080039494A1

公开(公告)日：2008-02-14

申请号：US11667908

申请日：2005-11-29

申请人： Jianming Bao ,  Robert DeVita ,  Jinlong Jiang ,  Sander Mills

发明人： Jianming Bao ,  Robert DeVita ,  Jinlong Jiang ,  Sander Mills

IPC分类号： A61K31/47 ,  A61P29/00 ,  C07D217/22

CPC分类号： C07D215/20 ,  C07D215/22 ,  C07D215/60

摘要： The present invention is directed to certain 8-phenyl-5,6,7,8-hydroquinolinecompounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

摘要翻译： 本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂的某些8-苯基-5,6,7,8-氢喹啉化合物，以及速激肽抑制剂，特别是物质P。本发明还涉及 其中包含这些化合物作为活性成分的药物制剂以及化合物及其制剂在治疗某些疾病（包括呕吐，尿失禁，抑郁和焦虑）中的用途。

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。

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：US07345083B2

公开(公告)日：2008-03-18

申请号：US11714352

申请日：2007-03-06

申请人： Jaime Lynn Bunda ,  Robert J. DeVita ,  Jinlong Jiang ,  Sander G. Mills

发明人： Jaime Lynn Bunda ,  Robert J. DeVita ,  Jinlong Jiang ,  Sander G. Mills

IPC分类号： A61K31/4035 ,  C07D209/44

CPC分类号： C07D209/44

摘要： The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

摘要翻译： 本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些加氢异吲哚啉化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和 使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。

公开(公告)号：US20050165083A1

公开(公告)日：2005-07-28

申请号：US11043213

申请日：2005-01-26

申请人： Jaime Bunda ,  Robert DeVita ,  Jinlong Jiang ,  Sander Mills

发明人： Jaime Bunda ,  Robert DeVita ,  Jinlong Jiang ,  Sander Mills

IPC分类号： C07D209/44 ,  A61K31/4035

CPC分类号： C07D209/44

摘要： The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

摘要翻译： 本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些加氢异吲哚啉化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和 使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。

公开(公告)号：US6150352A

公开(公告)日：2000-11-21

申请号：US180662

申请日：1998-11-12

申请人： Mark Goulet ,  Eric E Allen ,  Matthew J. Wyvratt, Jr. ,  Jinlong Jiang ,  Richard B. Toupence ,  Thomas F Walsh ,  Feroze Ujjainwalla ,  Jonathan R Young ,  Robert J. Devita

发明人： Mark Goulet ,  Eric E Allen ,  Matthew J. Wyvratt, Jr. ,  Jinlong Jiang ,  Richard B. Toupence ,  Thomas F Walsh ,  Feroze Ujjainwalla ,  Jonathan R Young ,  Robert J. Devita

IPC分类号： C07D473/00 ,  A61K31/00 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/529 ,  A61P5/00 ,  A61P5/06 ,  A61P5/24 ,  A61P15/00 ,  A61P25/20 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/02 ,  C07D453/02 ,  C07D473/32 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04 ,  C07D31/47

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/02 ,  C07D473/32 ,  C07D487/04 ,  C07D495/04

摘要： There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions in both men and women.

摘要翻译： PCT No.PCT / US97 / 08432 Sec。 371日期：1998年11月12日 102（e）1998年11月12日日期PCT提交1997年5月16日PCT公布。 公开号WO97 / 44339 日期1997年11月27日公开了可用作GnRH拮抗剂的式（I）化合物及其药学上可接受的盐，因此可用于治疗男性和女性中各种性激素相关病症。

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.