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：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：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：US09546168B2

公开(公告)日：2017-01-17

申请号：US15103893

申请日：2014-12-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： Kathryn Lipford ,  Danielle Falcone ,  David L. Sloman ,  David J. Witter

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K45/06

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K45/06 ,  A61K2300/00

Abstract: Disclosed are the ERK inhibitors of formula (1.0) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). This invention provides compounds that are ERK inhibitors (i.e., ERK2 inhibitors). This invention also provides a pharmaceutical composition comprising an effective amount of at least one (e.g., 1) compound of formula (1.0) and a pharmaceutically acceptable carrier.

Abstract translation: 公开了式（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。 本发明提供了作为ERK抑制剂（即ERK2抑制剂）的化合物。 本发明还提供了包含有效量的至少一种（例如1）式（1.0）化合物和药学上可接受的载体的药物组合物。

公开(公告)号：US20160311819A1

公开(公告)日：2016-10-27

申请号：US15103893

申请日：2014-12-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： Kathryn Lipford ,  Danielle Falcone ,  David L. Sloman ,  David J. Witter

IPC: C07D471/04 ,  A61K31/444 ,  A61K45/06 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K45/06 ,  A61K2300/00

Abstract: Disclosed are the ERK inhibitors of formula (1.0) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). This invention provides compounds that are ERK inhibitors (i.e., ERK2 inhibitors). This invention also provides a pharmaceutical composition comprising an effective amount of at least one (e.g., 1) compound of formula (1.0) and a pharmaceutically acceptable carrier.