公开(公告)号：US20200048258A1

公开(公告)日：2020-02-13

申请号：US16341313

申请日：2017-10-06

Applicant: UMAR Faruk MANSOOR ,  Christian Fischer ,  Phieng Siliphaivanh ,  Luis Torres ,  Hakan Gunaydin ,  David Sloman ,  Merck Sharp & Dohme Corp.

Inventor： UMAR FARUK MANSOOR ,  Christian Fischer ,  Phieng Siliphaivanh ,  Luis Torres ,  Hakan Gunaydin ,  David L. Sloman

IPC: C07D487/04

Abstract: The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.

公开(公告)号：US09884048B2

公开(公告)日：2018-02-06

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 ,  A61K31/4545 ,  A61K31/444 ,  C07D471/04 ,  C07D519/00

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：US20170320882A1

公开(公告)日：2017-11-09

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

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D471/14 ,  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 (I).

公开(公告)号：US20150266895A1

公开(公告)日：2015-09-24

申请号：US14431462

申请日：2013-09-26

Applicant: Kevin J. WILSON ,  David J. WITTER ,  Phieng SILIPHAIVANH ,  Kathryn KIPFORD ,  David SLOMAN ,  Danielle FALCONE ,  Brendan O'BOYLE ,  Umar Faruk MANSOOR ,  Jongwon LIM ,  Joey L. METHOT ,  Christopher BOYCE ,  Lei CHEN ,  Matthew H. DANIELS ,  Salem FEVRIER ,  Xianhai HUANG ,  Ravi KURUKULASURIYA ,  Ling TONG ,  Wei ZHOU ,  Joseph KOZLOWSKI ,  Milana M. MALETIC ,  Bidhan A. SHINKRE ,  Jayanth Thiruvellore THATAI ,  Raman Kumar BAKSHI ,  Ganesh Babu KARUNAKARAN ,  MERCK SHARP & DOHME CORP.

Inventor： Kevin J. Wilson ,  David J. Witter ,  Phieng Siliphaivanh ,  Kathryn Lipford ,  David Sloman ,  Danielle Falcone ,  Brendan O'Boyle ,  Umar Faruk Mansoor ,  Jongwon Lim ,  Joey L. Methot ,  Christopher Boyce ,  Lei Chen ,  Matthew H. Daniels ,  Salem Fevrier ,  Xianhai Huang ,  Ravi Kurukulasuriya ,  Ling Tong ,  Wei Zhou ,  Joseph Kozlowski ,  Milana M. Maletic ,  Bidhan A. Shinkre ,  Jayanth Thiruvellore Thatai ,  Raman Kumar Bakshi ,  Ganesh Babu Karunakaran

IPC: C07D498/18 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/496 ,  A61K45/06 ,  A61K31/4375 ,  C07D498/14 ,  A61K31/553 ,  C07D519/00 ,  C07D471/04 ,  C07D471/14

CPC classification number: C07D498/18 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/553 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/16 ,  C07D498/14 ,  C07D498/16 ,  C07D519/00 ,  A61K2300/00

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。

公开(公告)号：US20140228348A1

公开(公告)日：2014-08-14

申请号：US14345978

申请日：2012-09-21

Applicant: MERCK SHARP& DOHME CORP.

Inventor： Jason Brubaker ,  Matthew Lloyd Childers ,  Matthew Christopher ,  Joshua T. Close ,  Jason David Katz ,  Joon Jung ,  Scott Peterson ,  Phieng Siliphaivanh ,  Tony Siu ,  Graham Frank Smith ,  Luis E. Torres ,  Hyun Chong Woo ,  Jonathan R. Young ,  Hongjun Zhang

IPC: C07D231/38 ,  C07D405/04 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04

CPC classification number: C07D405/08 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

Abstract translation: 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。

公开(公告)号：US20210277009A1

公开(公告)日：2021-09-09

申请号：US17266474

申请日：2019-08-05

Applicant: David WITTER ,  Shuhei KAWAMURA ,  Michelle MACHACEK ,  Ryan QUIROZ ,  Michael H. REUTERSHAN ,  Sebastian SCHNEIDER ,  Phieng SILIPHAIVANH ,  Yingchun YE ,  Charles S. YEUNG ,  Merck Sharp & Dohme Corp.

Inventor： David Witter ,  Shuhei Kawamura ,  Michelle Machacek ,  Ryan Quiroz ,  Michael H. Reutershan ,  Sebastian Schneider ,  Phieng Siliphaivanh ,  Yingchun Ye ,  Charles S. Yeung

IPC: C07D487/04 ,  C07D519/00

Abstract: The present invention provides a compound of Formula (I) Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.

公开(公告)号：US10759805B2

公开(公告)日：2020-09-01

申请号：US16032715

申请日：2018-07-11

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

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：US10336733B2

公开(公告)日：2019-07-02

申请号：US15767371

申请日：2016-11-28

Applicant: Merck Sharp & Dohme Corp. ,  Yongxin Han ,  Jongwon Lim ,  Satyanarayana Tummanapalli ,  Phieng Siliphaivanh ,  Kerrie Spencer

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

IPC: C07D417/06 ,  C07D413/06 ,  C07D311/22 ,  C07D405/06 ,  A61K31/353 ,  A61K9/20

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：US09988397B2

公开(公告)日：2018-06-05

申请号：US15531771

申请日：2015-12-10

Applicant: Merck Sharp & Dohme Corp. ,  MSD R&D (China) Co., Ltd.

Inventor： Phieng Siliphaivanh ,  David L. Sloman ,  David Witter ,  Umar Faruk Mansoor ,  Joseph Kozlowski ,  Ziping Liu ,  Jianmin Fu ,  Zhilong Wan ,  Wei Liu ,  Yimin Qian ,  Xianhai Huang

IPC: C07D498/18 ,  C07D471/18 ,  C07D471/22

CPC classification number: C07D498/18 ,  A61K31/437 ,  A61K31/444 ,  C07D471/18 ,  C07D471/22

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 method of inhibiting 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). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).

公开(公告)号：US09745307B2

公开(公告)日：2017-08-29

申请号：US14787280

申请日：2014-04-25

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: C07D243/00 ,  C07D513/00 ,  C07D491/00 ,  C07D239/02 ,  C07D487/04 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00

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).