公开(公告)号：US10975084B2

公开(公告)日：2021-04-13

申请号：US16341313

申请日：2017-10-06

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

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：US20190382363A1

公开(公告)日：2019-12-19

申请号：US15768880

申请日：2016-11-28

Applicant: Merck Sharp & Dohme Corp.

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

IPC: C07D311/22 ,  C07D409/06 ,  C07D405/06 ,  C07D417/06 ,  C07D413/06 ,  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：US10450309B2

公开(公告)日：2019-10-22

申请号：US15769079

申请日：2016-11-28

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

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

IPC: A61K31/35 ,  A61P3/10 ,  C07D311/22 ,  C07D311/58 ,  C07D405/14 ,  C07D417/14

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：US20180291017A1

公开(公告)日：2018-10-11

申请号：US15768097

申请日：2016-11-28

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

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

IPC: C07D417/14 ,  A61P3/10

CPC classification number: C07D417/14 ,  A61K9/2054 ,  A61P3/10

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：US20200048259A1

公开(公告)日：2020-02-13

申请号：US16341323

申请日：2017-10-06

Applicant: Umar Faruk MANSOOR ,  Christian FISCHER ,  Phieng SILIPHAIVANH ,  Hakan GUNAYDIN ,  Merck Sharp & Dohme Corp.

Inventor： UMAR FARUK MANSOOR ,  Christian Fischer ,  Phieng Siliphaivanh ,  Hakan Gunaydin

IPC: C07D487/04

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

公开(公告)号：US10370368B2

公开(公告)日：2019-08-06

申请号：US15768097

申请日：2016-11-28

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

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

IPC: A61K9/20 ,  A61P3/10 ,  C07D417/14

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：US20180319804A1

公开(公告)日：2018-11-08

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

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：US09233979B2

公开(公告)日：2016-01-12

申请号：US14431462

申请日：2013-09-26

Applicant: 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: C07D401/14 ,  A61K31/437 ,  C07D498/18 ,  C07D471/04 ,  A61K31/5377 ,  A61K31/496 ,  C07D471/14 ,  A61K31/4375 ,  C07D498/14 ,  A61K31/553 ,  C07D519/00 ,  A61K45/06

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).

公开(公告)号：US20150258074A1

公开(公告)日：2015-09-17

申请号：US14431485

申请日：2013-09-26

Applicant: Kevin J. WILSON ,  David J. WITTER ,  Matthew H. DANIELS ,  Angie R. ANGELES ,  Phieng SILIPHAIVANH ,  David L. SLOMAN ,  Brendan O'BOYLE ,  Danielle FALCONE ,  Catherine WHITE ,  Ron FERGUSON ,  Wei ZHOU ,  Kathryn LIPFORD ,  Umar Faruk MANSOOR ,  Salem FEVRIRE ,  Xianhai HUANG ,  Ravi KURUKULASURIYA ,  Judson E. RICHARD ,  Shuyi TANG ,  Christopher BOYCE ,  Joseph KOZLOWSKI ,  Raman Kumar BAKSHI ,  Ganesh Babu UNAKARAN ,  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: A61K31/437 ,  A61K45/06 ,  A61K31/4545 ,  C07D471/04

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：US20220363656A1

公开(公告)日：2022-11-17

申请号：US17343994

申请日：2021-06-10

Applicant: Merck Sharp & Dohme Corp.

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

IPC: C07D311/22 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  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, Nonalcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.