公开(公告)号：US11208407B2

公开(公告)日：2021-12-28

申请号：US16631191

申请日：2018-07-30

申请人： Merck Sharp & Dohme Corp.

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

IPC分类号： C07D471/04 ,  C07D235/14

摘要： 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

申请人： Merck Sharp & Dohme Corp.

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

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

摘要： 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

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： C07D471/04 ,  A61K31/5513 ,  A61K45/06 ,  C07D471/14 ,  A01N43/00 ,  C07D519/00

摘要： 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：US20220402916A1

公开(公告)日：2022-12-22

申请号：US17761433

申请日：2020-09-18

申请人： Merck Sharp & Dohme Corp.

发明人： Andrew J. Hoover ,  Thomas H. Graham ,  Xiaoshen Ma ,  Zahid Hussain ,  Mihir Mandal ,  Symon Gathiaka ,  Yongxin Han ,  David L. Sloman

IPC分类号： C07D471/04 ,  A61P35/00

摘要： Provided are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein Y, CY, R1, R3, R4, R5, R6, R2a, R2b, RMa, RMb, and the subscripts m, n, and q 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 treatment of cancer. Also provided are pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. Also provided are 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：US20220363707A1

公开(公告)日：2022-11-17

申请号：US17266521

申请日：2019-08-05

申请人： Merck Sharp & Dohme Corp. ,  MSD International GmbH

发明人： 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分类号： C07H19/14 ,  C07D487/04 ,  A61P35/00

摘要： 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：US20170266167A1

公开(公告)日：2017-09-21

申请号：US15531759

申请日：2015-12-10

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： A61K31/437 ,  C07D519/00 ,  C07D471/04 ,  A61K31/4545 ,  A61K31/444

CPC分类号： A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  C07D471/04 ,  C07D519/00

摘要： 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：US20140296203A1

公开(公告)日：2014-10-02

申请号：US14353381

申请日：2012-10-25

申请人： MERCK SHARP & DOHME CORP.

发明人： 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分类号： C07D471/04 ,  A61K31/444 ,  A61K31/437 ,  A61K45/06 ,  A61K31/501 ,  A61K31/4709 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/506

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

摘要： 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).

摘要翻译： 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：US20210403469A1

公开(公告)日：2021-12-30

申请号：US17289062

申请日：2019-11-01

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： C07D471/04 ,  C07D401/04 ,  C07D215/14 ,  C07D209/94 ,  C07D403/04

摘要： 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

申请人： Merck Sharp & Dohme Corp.

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

IPC分类号： C07D471/04 ,  C07D235/14

摘要： 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

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

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

IPC分类号： C07D487/04

摘要： 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.