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.

公开(公告)号：US08785634B2

公开(公告)日：2014-07-22

申请号：US13638976

申请日：2011-04-21

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

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

IPC: C07D401/00

CPC classification number: C07D491/20 ,  C07D491/10

Abstract: 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.

Abstract translation: 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

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

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

IPC: 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 classification number: C07D491/20 ,  C07D491/10

Abstract: 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.

Abstract translation: 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：US07629376B2

公开(公告)日：2009-12-08

申请号：US11674385

申请日：2007-02-13

Applicant: William Arthur Metz, Jr. ,  Fa-Xiang Ding

Inventor： William Arthur Metz, Jr. ,  Fa-Xiang Ding

IPC: A61K31/404 ,  A61K31/4045 ,  C07D209/34

CPC classification number: C07D491/10 ,  C07D209/42 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

Abstract: The present invention discloses and claims compounds of formula (I) and formula (II) as inhibitors of human casein kinase Iε, and methods of using the compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) are also disclosed and claimed.

Abstract translation: 本发明公开并要求作为人酪蛋白激酶Iepsilon抑制剂的式（I）和式（II）的化合物，以及使用式（I）和式（II）化合物治疗中枢神经系统疾病和病症的方法，包括 情绪障碍和睡眠障碍。 R基取代基在本文中定义，并且还公开并要求保护包含式（I）或式（II）化合物的药物组合物。

公开(公告)号：US20060293364A1

公开(公告)日：2006-12-28

申请号：US11474646

申请日：2006-06-26

Applicant: Subharekha Raghavan ,  Steven Colletti ,  Fa-Xiang Ding ,  Hong Shen ,  James Tata ,  Ashley Lins ,  Abigail Smenton ,  Weichun Chen ,  Darby Schmidt ,  George Tria

Inventor： Subharekha Raghavan ,  Steven Colletti ,  Fa-Xiang Ding ,  Hong Shen ,  James Tata ,  Ashley Lins ,  Abigail Smenton ,  Weichun Chen ,  Darby Schmidt ,  George Tria

IPC: A61K31/4439 ,  A61K31/43 ,  A61K31/427 ,  A61K31/4245 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/35 ,  A61K31/195

CPC classification number: C07D261/20 ,  C07C233/52 ,  C07C233/55 ,  C07C235/36 ,  C07C237/20 ,  C07C2601/10 ,  C07C2601/16 ,  C07D231/12 ,  C07D249/06 ,  C07D249/08 ,  C07D257/04 ,  C07D271/06 ,  C07D277/30 ,  C07D307/79 ,  C07D309/14 ,  C07D309/28 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D513/04

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

Abstract translation: 本发明包括可用于治疗动脉粥样硬化，血脂异常等的式I化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。

公开(公告)号：US09062070B2

公开(公告)日：2015-06-23

申请号：US14239649

申请日：2012-08-16

Applicant: 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

Inventor： 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: C07D498/04 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/553 ,  A61K45/06 ,  C07D487/04 ,  C07D513/04

CPC classification number: C07D498/04 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/553 ,  A61K45/06 ,  C07D487/04 ,  C07D513/04

Abstract: 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.

Abstract translation: 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。 该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水滞留有关的病症的医学病症。

公开(公告)号：US20140206618A1

公开(公告)日：2014-07-24

申请号：US14239649

申请日：2012-08-16

Applicant: 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

Inventor： 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: C07D498/04 ,  A61K45/06 ,  A61K31/4985 ,  C07D513/04 ,  A61K31/542 ,  C07D487/04 ,  A61K31/5383 ,  A61K31/553

CPC classification number: C07D498/04 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/553 ,  A61K45/06 ,  C07D487/04 ,  C07D513/04

Abstract: 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.

Abstract translation: 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：US08455520B2

公开(公告)日：2013-06-04

申请号：US12668494

申请日：2008-07-11

Applicant: Steven L. Colletti ,  Hong Shen ,  Fa-Xiang Ding

Inventor： Steven L. Colletti ,  Hong Shen ,  Fa-Xiang Ding

IPC: A61K31/4985 ,  A61K31/4725 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/451 ,  A61K31/445 ,  C07D417/12 ,  C07D413/12 ,  C07D413/04 ,  C07D401/12 ,  C07D401/06 ,  C07D401/04 ,  C07D211/60 ,  C07D211/56 ,  C07D211/62 ,  C07D211/34 ,  C07D211/22 ,  C07D211/16

CPC classification number: C07D211/22 ,  C07D211/16 ,  C07D211/34 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.

Abstract translation: 公开了可用于治疗高血压，糖尿病，炎症，动脉粥样硬化，疼痛等的式（I）化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。

公开(公告)号：US08168649B2

公开(公告)日：2012-05-01

申请号：US11922629

申请日：2006-06-26

Applicant: Subharekha Raghavan ,  Steven L. Colletti ,  Fa-Xiang Ding ,  Hong Shen ,  James R. Tata ,  Ashley Rouse Lins ,  Abigail Lee Smenton ,  Weichun Chen ,  Darby Rye Schmidt ,  George Scott Tria

Inventor： Subharekha Raghavan ,  Steven L. Colletti ,  Fa-Xiang Ding ,  Hong Shen ,  James R. Tata ,  Ashley Rouse Lins ,  Abigail Lee Smenton ,  Weichun Chen ,  Darby Rye Schmidt ,  George Scott Tria

IPC: A61K31/44 ,  A01N43/40 ,  A61K31/19 ,  A61K31/165

CPC classification number: C07D261/20 ,  C07C233/52 ,  C07C233/55 ,  C07C235/36 ,  C07C237/20 ,  C07C2601/10 ,  C07C2601/16 ,  C07D231/12 ,  C07D249/06 ,  C07D249/08 ,  C07D257/04 ,  C07D271/06 ,  C07D277/30 ,  C07D307/79 ,  C07D309/14 ,  C07D309/28 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D513/04

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

Abstract translation: 本发明包括可用于治疗动脉粥样硬化，血脂异常等的式（I）化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。

公开(公告)号：US20110003849A1

公开(公告)日：2011-01-06

申请号：US12919323

申请日：2009-02-24

Applicant: Hong Shen ,  Fa-Xiang Ding ,  Steven L. Colletti

Inventor： Hong Shen ,  Fa-Xiang Ding ,  Steven L. Colletti

IPC: A61K31/439 ,  C07D451/02 ,  C07D453/02 ,  C07D487/08 ,  A61K31/4439 ,  A61P3/10

CPC classification number: C07D413/04 ,  C07D209/52 ,  C07D453/06 ,  C07D471/08 ,  C07D487/08

Abstract: Compounds of the formula: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating diabetes, inflammation, atherosclerosis, hypertension, pain and the like are disclosed. Pharmaceutical compositions and methods of use are also included.

Abstract translation: 公开了可用于治疗糖尿病，炎症，动脉粥样硬化，高血压，疼痛等的下式的化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。