公开(公告)号：US20220363707A1

公开(公告)日：2022-11-17

申请号：US17266521

申请日：2019-08-05

Applicant: Merck Sharp & Dohme Corp. ,  MSD International GmbH

Inventor： Michelle Machacek ,  David Witter ,  Craig Gibeau ,  Chunhui Huang ,  Shuhei Kawamura ,  David L. Sloman ,  Phieng Siliphaivanh ,  Ryan Quiroz ,  Murray Wan ,  Sebastian Schneider ,  Charles S. Yeung ,  Michael H. Reutershan ,  Timothy J. Henderson ,  Jean-Laurent Paparin ,  Houcine Rahali ,  Jonathan M. E. Hughes ,  Sulagna Sanyal ,  Yingchun Ye ,  David A. Candito ,  Patrick S. Fier ,  Steven M. Silverman

IPC: C07H19/14 ,  C07D487/04 ,  A61P35/00

Abstract: The present invention provides a compound of Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.

公开(公告)号：US20180312499A1

公开(公告)日：2018-11-01

申请号：US15769079

申请日：2016-11-28

Applicant: Merck Sharp & Dohme Corp.

Inventor： Yongxin Han ,  Satyanarayana Tummanapalli ,  Phieng Siliphaivanh ,  Kerrie Spencer

IPC: C07D417/14 ,  C07D405/14 ,  A61P3/10

CPC classification number: C07D417/14 ,  A61K31/35 ,  A61P3/10 ,  C07D311/22 ,  C07D311/58 ,  C07D405/14

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.

公开(公告)号：US20180305342A1

公开(公告)日：2018-10-25

申请号：US15767371

申请日：2016-11-28

Applicant: Yongxin HAN ,  Jongwon LIM ,  Phieng SILIPHAIVANH ,  Kerrie SPENCER ,  Satyanarayana TUMMANAPALLI ,  Merck Sharp & Dohme Corp.

Inventor： Yongxin Han ,  Jongwon Lim ,  Satyanarayana Tummanapalli ,  Phieng Siliphaivanh ,  Kerrie Spencer

IPC: C07D405/06 ,  C07D311/22 ,  C07D417/06 ,  C07D413/06

CPC classification number: C07D405/06 ,  A61K9/2054 ,  A61K31/353 ,  C07D311/22 ,  C07D413/06 ,  C07D417/06

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension. Non-alcoholic fatty liver disease/nonalcoholic steatoepatitis metabolic syndrome, atherosclerosis, and cancer.

公开(公告)号：US10065967B2

公开(公告)日：2018-09-04

申请号：US15656176

申请日：2017-07-21

Applicant: Merck Sharp & Dohme Corp.

Inventor： Jongwon Lim ,  Xianhai Huang ,  Ronald D. Ferguson ,  Wei Zhou ,  Christopher W. Boyce ,  Phieng Siliphaivanh ,  David J. Witter ,  Milana M. Maletic ,  Joseph A. Kozlowski ,  Kevin J. Wilson

IPC: C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  C07D471/14

Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I).

公开(公告)号：US20170266167A1

公开(公告)日：2017-09-21

申请号：US15531759

申请日：2015-12-10

Applicant: Merck Sharp & Dohme Corp.

Inventor： Phieng Siliphaivanh ,  Joey Methot ,  Kathryn Ann Lipford ,  Danielle Molinari ,  David L. Sloman ,  David Witter ,  Hua Zhou ,  Christopher Boyce ,  Xianhai Huang ,  Jongwon Lim ,  David Guerin ,  Ganesh Babu Karunakaran ,  Raman Kumar Bakshi ,  Ziping Liu ,  Jianmin Fu ,  Zhilong Wan ,  Wei Liu

IPC: A61K31/437 ,  C07D519/00 ,  C07D471/04 ,  A61K31/4545 ,  A61K31/444

CPC classification number: A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.

公开(公告)号：US20160068532A1

公开(公告)日：2016-03-10

申请号：US14787280

申请日：2014-04-25

Applicant: Jongwon LIM ,  Xianhai HUANG ,  Ronald D. FERGUSON ,  Wei ZHOU ,  Christopher W. BOYCE ,  Phieng SILIPHAIVANH ,  David J. WITTER ,  Milana M. MALETIC ,  Joseph A. KOZLOWSKI ,  Kevin J. WILSON ,  MERCK SHARP & DOHME CORP.

Inventor： Jongwon Lim ,  Xianhai Huang ,  Ronald D. Ferguson ,  Wei Zhou ,  Christopher W. Boyce ,  Phieng Siliphaivanh ,  David J. Witter ,  Milana M. Maletic ,  Joseph A. Kozlowski ,  Kevin J. Wilson

IPC: C07D487/04 ,  C07D471/14 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00

Abstract: Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I).

Abstract translation: 公开了式（I）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（I）化合物治疗癌症的方法。 本发明还提供了包含有效量的至少一种式（I）化合物和药学上可接受的载体的药物组合物。 本发明还提供一种药物组合物，其包含有效量的至少一种式（I）化合物和有效量的至少一种其它药学活性成分（例如化学治疗剂）和药学上可接受的载体 。 本发明还提供了在需要这种治疗的患者中抑制ERK（即，抑制ERK2的活性）的方法，包括向所述患者施用有效量的至少一种式（I）化合物。

公开(公告)号：US09226922B2

公开(公告)日：2016-01-05

申请号：US14431485

申请日：2013-09-26

Applicant: Merck Sharp & Dohme Corp.

Inventor： Kevin J. Wilson ,  David J. Witter ,  Matthew H. Daniels ,  Angie R. Angeles ,  Phieng Siliphaivanh ,  David Sloman ,  Brendan O'Boyle ,  Danielle Falcone ,  Catherine White ,  Ron Ferguson ,  Wei Zhou ,  Kathryn Lipford ,  Umar Faruk Mansoor ,  Salem Fevrier ,  Xianhai Huang ,  Ravi Kurukulasuriya ,  Judson E. Richard ,  Shuyi Tang ,  Christopher Boyce ,  Joseph Kozlowski ,  Raman Kumar Bakshi ,  Ganesh Babu Karunakaran

IPC: C07D401/14 ,  A61K31/437 ,  C07D471/04 ,  A61K45/06 ,  A61K31/4545

CPC classification number: A61K31/437 ,  A61K31/4545 ,  A61K45/06 ,  C07D471/04

Abstract: Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).

Abstract translation: 公开了具有吡唑并吡啶基结构的式（1.0）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1.0）化合物治疗癌症的方法。

公开(公告)号：US20140296203A1

公开(公告)日：2014-10-02

申请号：US14353381

申请日：2012-10-25

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Jongwon Lim ,  Elizabeth Helen Kelley ,  Joey L. Methot ,  Hua Zhou ,  Alessia Petrocchi ,  Faruk Mansoor ,  Christian Fischer ,  Brendan O'Boyle ,  David Joseph Guerin ,  Corey E. Bienstock ,  Christopher W. Boyce ,  Matthew H. Daniels ,  Danielle Falcone ,  Ronald D. Ferguson ,  Salem Fevrier ,  Xianhai Huang ,  Kathryn Ann Lipford ,  David L. Sloman ,  Kevin Wilson ,  Wei Zhou ,  David Witter ,  Milana M. Maletic ,  Phieng Siliphaivanh

IPC: C07D471/04 ,  A61K31/444 ,  A61K31/437 ,  A61K45/06 ,  A61K31/501 ,  A61K31/4709 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/506

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D519/00

Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).

Abstract translation: 公开了式（1）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1）的化合物治疗癌症的方法。