公开(公告)号：US11208407B2

公开(公告)日：2021-12-28

申请号：US16631191

申请日：2018-07-30

Applicant: Merck Sharp & Dohme Corp.

Inventor： Hua Zhou ,  Abdelghani Achab ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Meredeth A. McGowan ,  Nunzio Sciammetta ,  David L. Sloman ,  Wensheng Yu

IPC: C07D471/04 ,  C07D235/14

Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I) Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20210122764A1

公开(公告)日：2021-04-29

申请号：US17081477

申请日：2020-10-27

Applicant: Merck Sharp & Dohme Corp.

Inventor： Indu Bharathan ,  Symon Gathiaka ,  Yongxin Han ,  Xiaoshen Ma ,  Ryan D. Otte ,  David L. Sloman ,  Thomas H. Graham ,  Timothy Henderson ,  Elizabeth Hennessy ,  Anandan Palani

IPC: C07D498/22 ,  A61P35/00 ,  A61K31/519 ,  C07D471/22 ,  C07D519/00

Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

公开(公告)号：US10086000B2

公开(公告)日：2018-10-02

申请号：US15532548

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Dann L. Parker, Jr. ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Wanying Sun ,  Feroze Ujjainwalla ,  Chunhui Huang

IPC: C07D471/04 ,  A61K31/5513 ,  A61K45/06 ,  C07D471/14 ,  A01N43/00 ,  C07D519/00

Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N═; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

公开(公告)号：US20210403469A1

公开(公告)日：2021-12-30

申请号：US17289062

申请日：2019-11-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Yongxin Han ,  David Jonathan Bennett ,  Indu Bharathan ,  Liangqin Guo ,  Brett A. Hopkins ,  Xianhai Huang ,  Derun Li ,  Min Lu ,  Alexander Pasternak ,  David L. Sloman ,  Hongjun Zhang ,  Hua Zhou

IPC: C07D471/04 ,  C07D401/04 ,  C07D215/14 ,  C07D209/94 ,  C07D403/04

Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Formula (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20200216443A1

公开(公告)日：2020-07-09

申请号：US16631191

申请日：2018-07-30

Applicant: Merck Sharp & Dohme Corp.

Inventor： Hua Zhou ,  Abdelghani Achab ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Meredeth A. McGowan ,  Nunzio Sciammetta ,  David L. Sloman ,  Wensheng Yu

IPC: C07D471/04 ,  C07D235/14

Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I) Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

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：US10508108B2

公开(公告)日：2019-12-17

申请号：US15532552

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Dawn M. Hoffman ,  Chunhui Huang ,  Solomon D. Kattar ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Dann L. Parker, Jr. ,  Michael H. Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Wanying Sun ,  Feroze Ujjainwalla ,  Zhicai Wu ,  Yang Yu ,  Craig R. Gibeau

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

Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is —C(R1)═ or —N═; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

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：US20170369507A1

公开(公告)日：2017-12-28

申请号：US15532549

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Fischer Christian ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  Michael J. Ellis ,  Sara Esposite ,  Qingmei Hong ,  Chunhui Huang ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Ryan D. Otte ,  Dann L. Parker, Jr. ,  Michael H. Reutershan ,  Nunzio Sciammetta ,  Patrick Pengcheng Shao ,  David L. Sloman ,  Feroze Ujjainwalla ,  Catherine White ,  Zhicai Wu ,  Yang Yu ,  Kake Zhao ,  Craig R. Gibeau

IPC: C07D498/08 ,  C07D471/04 ,  C07D498/10 ,  C07D471/08 ,  A01N43/00

CPC classification number: C07D498/08 ,  A01N43/00 ,  A61K31/551 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D498/04 ,  C07D498/10

Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

公开(公告)号：US20170362220A1

公开(公告)日：2017-12-21

申请号：US15532552

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  Michael J. Ellis ,  Sara Esposite ,  Dawn M. Hoffman ,  Chunhui Huang ,  Solomon D. Kattar ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Dann L. Parker, Jr. ,  Michael H. Reutershan ,  Nunzio Sciammetta ,  Patrick Pengcheng Shao ,  David L. Sloman ,  Wanying Sun ,  Feroze Ujjainwalla ,  Zhicai Wu ,  Yang Yu ,  Craig R. Gibeau

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

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

Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is —C(R1)═ or —N═; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.