公开(公告)号：US20230322785A1

公开(公告)日：2023-10-12

申请号：US18015387

申请日：2022-07-21

申请人： Christopher W. BOYCE ,  Thomas H. GRAHAM ,  Andrew J. HOOVER ,  Xianhai HUANG ,  Rognze KUANG ,  Jae-Hun KIM ,  Joseph M. KELLY ,  Michael Man-Chu LO ,  Jing SU ,  Dong XIAO ,  Xiaohong ZHU ,  Merck Sharp & Dohme LLC

发明人： Amjad Ali ,  Christopher W. Boyce ,  Jared N. Cumming ,  Duane DeMong ,  Thomas H. Graham ,  Subrahmanyam Gudipati ,  Andrew J. Hoover ,  Xianhai Huang ,  Rongze Kuang ,  Jae-Hun Kim ,  Joseph M. Kelly ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Jesus Moreno ,  Jing Su ,  Heping Wu ,  Dong Xiao ,  Younong Yu ,  Xiaohong Zhu

IPC分类号： C07D487/04 ,  C07K16/28 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61P35/00 ,  C07K16/2896

摘要： The present invention provides compounds of the structural Formula (I) and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US20240076297A1

公开(公告)日：2024-03-07

申请号：US18015364

申请日：2021-07-22

申请人： Merck Sharp & Dohme LLC

发明人： Amjad Ali ,  Jared N. Cumming ,  Manuel De Lera Ruiz ,  Duane DeMong ,  Thomas H. Graham ,  Elisabeth T. Hennessy ,  Joseph M. Kelly ,  Rongze Kuang ,  Michael Man-Chu Lo ,  Umar Faruk Mansoor ,  Jesus Moreno ,  Uma Swaminathan ,  Heping Wu ,  Yingchun Ye ,  Younong Yu

IPC分类号： C07D487/04 ,  A61K45/06 ,  C07D519/00 ,  C07K16/28

CPC分类号： C07D487/04 ,  A61K45/06 ,  C07D519/00 ,  C07K16/2818

摘要： The present invention provides compounds of the structural Formula (I), and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US11766435B2

公开(公告)日：2023-09-26

申请号：US16076400

申请日：2017-02-13

申请人： Merck Sharp & Dohme LLC ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Tanweer A. Khan ,  Jared N. Cumming ,  David B. Olsen ,  Justin A. Boddey ,  Alan F. Cowman ,  Brad E. Sleebs

IPC分类号： A61K31/4709 ,  A61K9/06 ,  A61K47/10 ,  A61K47/12 ,  A61P17/10 ,  A61P17/00 ,  A61P17/04 ,  A61P31/04 ,  A61K31/513 ,  A61P33/06 ,  A61K31/527 ,  A61K9/00 ,  A61K45/06

CPC分类号： A61K31/513 ,  A61K31/527 ,  A61P33/06 ,  A61K9/0019 ,  A61K9/0053 ,  A61K45/06

摘要： The present invention provides methods of treating malaria comprising administration of an N3-substituted iminopyrimidinone of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables R1, R2, R3, R4, R5, A, B, L, m, and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

公开(公告)号：US11702430B2

公开(公告)日：2023-07-18

申请号：US17040192

申请日：2019-03-28

申请人： Merck Sharp & Dohme LLC ,  Michael D. Altman ,  Brandon D. Cash ,  Jared N. Cumming ,  Duane E. DeMong ,  Andrew M. Haidle ,  James P. Jewell ,  Matthew A. Larsen ,  Min Lu ,  Ryan D. Otte ,  Brandon M. Taoka ,  Benjamin Wesley Trotter ,  Quang T. Truong

发明人： Michael D. Altman ,  Brandon D. Cash ,  Jared N. Cumming ,  Duane E. DeMong ,  Andrew M. Haidle ,  James P. Jewell ,  Matthew A. Larsen ,  Min Lu ,  Ryan D. Otte ,  Brandon M. Taoka ,  Benjamin Wesley Trotter ,  Quang T. Truong

IPC分类号： C07D513/04 ,  C07D495/04 ,  C07D277/64 ,  A61P37/04 ,  A61P35/00

CPC分类号： C07D513/04 ,  A61P37/04 ,  C07D495/04

摘要： Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R5, R6, R8, R9, A, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.