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：US08138219B2

公开(公告)日：2012-03-20

申请号：US12739984

申请日：2008-11-25

申请人： Alexander Pasternak ,  Michael J. Szymonifka

发明人： Alexander Pasternak ,  Michael J. Szymonifka

IPC分类号： A61K31/404 ,  C07D209/14

CPC分类号： C07D209/16

摘要： Novel compounds of the structural formula (I) are antagonists of the 5-HT6 receptor and are useful in the treatment, prevention and suppression of diseases mediated by the 5-HT6 receptor. The compounds of the present invention are useful in the treatment of obesity, diabetes, metabolic disorder, cognitive disorders, age related cognitive disorder, depression, mania, bipolar disorders, schizophrenia, anxiety, generalized anxiety disorder, panic disorder, and obsessive compulsive disorder, epilepsy, convulsions, migraine, substance withdrawal from substances including but not limited to opiates, nicotine, tobacco products, alcohol, benzodiazepines, sedatives, and the like, sleep disorders, attention deficit/hyperactivity disorder, and Alzheimer's disease.

摘要翻译： 结构式（I）的新型化合物是5-HT 6受体的拮抗剂，可用于治疗，预防和抑制由5-HT 6受体介导的疾病。 本发明的化合物可用于治疗肥胖，糖尿病，代谢紊乱，认知障碍，与年龄相关的认知障碍，抑郁症，躁狂症，双相情感障碍，精神分裂症，焦虑症，广泛性焦虑症，恐慌症和强迫症， 癫痫症，惊厥，偏头痛，物质从物质包括但不限于阿片剂，尼古丁，烟草产品，酒精，苯二氮卓类，镇静剂等，物质戒断，睡眠障碍，注意力缺陷/多动症和阿尔茨海默病。

公开(公告)号：US20100184758A1

公开(公告)日：2010-07-22

申请号：US12668822

申请日：2008-07-15

申请人： Peter H. Dobbelaar ,  Wu Du ,  Liangqin Guo ,  William K. Hagmann ,  Shuwen He ,  Tianying Jian ,  Jian Liu ,  Ravi P. Nargund ,  Alexander Pasternak ,  Shrenik K. Shah ,  Quang T. Truong ,  Zhixiong Ye ,  James Deliureficio ,  Raman Bakshi

发明人： Peter H. Dobbelaar ,  Wu Du ,  Liangqin Guo ,  William K. Hagmann ,  Shuwen He ,  Tianying Jian ,  Jian Liu ,  Ravi P. Nargund ,  Alexander Pasternak ,  Shrenik K. Shah ,  Quang T. Truong ,  Zhixiong Ye ,  James Deliureficio ,  Raman Bakshi

IPC分类号： A61K31/5377 ,  C07D471/14 ,  A61K31/437 ,  C07D413/14 ,  C07D403/14 ,  A61K31/501 ,  A61K31/4995 ,  A61K31/506 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00 ,  A61P3/06 ,  A61P9/12

CPC分类号： C07D471/04

摘要： Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.

摘要翻译： 结构式I的β-咔啉衍生物是生长抑素亚型受体3（SSTR3）的选择性拮抗剂，可用于治疗2型糖尿病和通常与该疾病相关的病症，包括高血糖症，胰岛素抵抗，肥胖症， 脂质障碍和高血压。 这些化合物也可用于治疗抑郁症和焦虑症。

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。

公开(公告)号：US08999990B2

公开(公告)日：2015-04-07

申请号：US14353410

申请日：2012-10-22

申请人： Haifeng Tang ,  Barbara Pio ,  Nardos Teumelsan ,  Alexander Pasternak ,  Reynalda DeJesus

发明人： Haifeng Tang ,  Barbara Pio ,  Nardos Teumelsan ,  Alexander Pasternak ,  Reynalda DeJesus

IPC分类号： A61K31/495 ,  A61K31/496 ,  C07D295/22 ,  C07D401/06 ,  C07D403/10 ,  C07D407/10 ,  C07D413/10 ,  C07D405/14 ,  C07D413/14 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06 ,  C07D241/08 ,  A61K45/06 ,  C07D241/04

CPC分类号： C07D413/10 ,  A61K31/495 ,  A61K31/496 ,  A61K45/06 ,  C07D241/04 ,  C07D241/08 ,  C07D401/06 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D405/14 ,  C07D407/10 ,  C07D413/06 ,  C07D413/14

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 act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from 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。 该化合物作为利尿剂和利尿钠，并且是用于治疗和预防包括心血管疾病如高血压在内的医学病症和由于过量的盐和水保留引起的病症的有价值的药物活性化合物。

公开(公告)号：US11267786B2

公开(公告)日：2022-03-08

申请号：US17057959

申请日：2019-05-28

申请人： Merck Sharp & Dohme Corp. ,  Shuwen He ,  Yongxin Han ,  Alexander Pasternak

发明人： Shuwen He ,  Yongxin Han ,  Alexander Pasternak

IPC分类号： C07D215/14 ,  A61K45/06

摘要： Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US09206199B2

公开(公告)日：2015-12-08

申请号：US14364908

申请日：2012-12-11

申请人： Barbara Pio ,  Alexander Pasternak ,  Aurash Shahripour ,  Haifeng Tang ,  Shawn Walsh

发明人： Barbara Pio ,  Alexander Pasternak ,  Aurash Shahripour ,  Haifeng Tang ,  Shawn Walsh

IPC分类号： C07D498/04 ,  A61K31/5383 ,  A61P7/12 ,  A61P9/02 ,  A61P9/04 ,  C07D513/04 ,  A61K31/4985 ,  A61K45/06 ,  A61K31/401 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4422 ,  A61K31/585 ,  A61K31/675 ,  A61K31/542 ,  A61K31/553 ,  C07D487/04

CPC分类号： C07D513/04 ,  A61K31/401 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4422 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/553 ,  A61K31/585 ,  A61K31/675 ,  A61K45/06 ,  C07D487/04 ,  C07D498/04 ,  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 act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.