Patents Assigned to Merck, Sharp & Dohms, Corp.
  • Publication number: 20200392468
    Abstract: The present invention provides an efficient process for culturing viruses in the presence of an endonuclease and for producing vaccines, typically from live attenuated viruses, under conditions to reduce the presence of host cell DNA and eliminate the need for a post-harvest DNA digestion step.
    Type: Application
    Filed: March 28, 2018
    Publication date: December 17, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Yi Li, Matthew Woodling, Adam Kristopeit
  • Publication number: 20200390760
    Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Application
    Filed: December 12, 2018
    Publication date: December 17, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Meredeth A. McGowan, Jason D. Katz, Hua Zhou, David James Witter, Chaomin Li, Kathryn A. Lipford, Joey L. Methot, Abdelghani A. Achab, Xavier Fradera, Shimin Xu, Jianmin Fu
  • Patent number: 10864211
    Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: December 11, 2017
    Date of Patent: December 15, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John S. Debenham, Jason M. Cox, Ping Lan, Zhongxiang Sun, Zhe Feng, Chunrui Sun, W. Michael Seganish, Zhong Lai, Cheng Zhu, Thomas Bara, Murali Rajagopalan, Qun Dang, Hyunjin M. Kim, Bin Hu, Jinglai Hao
  • Publication number: 20200385404
    Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
    Type: Application
    Filed: May 21, 2020
    Publication date: December 10, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: David Waller, Gregory Gazda, Zachary Minden, Lisa Barton, Clifton Leigh
  • Patent number: 10858686
    Abstract: The present invention is directed to methods and compositions for the production of Fc-containing polypeptides having improved properties and comprising mutations at positions 243 and 264 of the Fc region.
    Type: Grant
    Filed: June 13, 2018
    Date of Patent: December 8, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Terrance A. Stadheim, Dongxing Zha
  • Publication number: 20200375987
    Abstract: The present invention relates to metallo-?-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein RA, R1, and Z are as defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
    Type: Application
    Filed: December 20, 2018
    Publication date: December 3, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Shuzhi Dong, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Dexi Yang, Li Xiao, Xin Gu, Jinlong Jiang
  • Publication number: 20200369657
    Abstract: The present invention relates to PCSK9 allosteric binding compounds of Formula I: (Formula (I)) and pharmaceutically acceptable salts thereof wherein X1, X2, Y, R1, R2, RA, RB and n are as defined herein. The present invention also relates to compositions which comprise an allosteric binding compound of the invention or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The invention further relates, inter alia, to methods for inducing PCSK9 protein degradation in a subject, and methods for treating atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions, comprising administering to a subject an effective amount of a compound or a pharmaceutically acceptable salt of the invention. The invention also provides a means for the in vitro labeling, detection and/or quantification of PCSK9 in biological samples.
    Type: Application
    Filed: September 15, 2017
    Publication date: November 26, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jason Eugene Imbriglio, Whitney Lane Petrilli, Yusheng Xiong, Zhe Feng, Hyewon Youm, Wonsuk Chang, Rui Liang, Zhijian Lu, Jerry Andrew Taylor, Scott B. Hoyt
  • Publication number: 20200361931
    Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
    Type: Application
    Filed: November 5, 2018
    Publication date: November 19, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michelle R. Machacek, David J. Witter, Michael Hale Reutershan, Michael D. Altman, Paul Anthony Stupple
  • Publication number: 20200360500
    Abstract: The present invention provides polysaccharide-protein conjugate vaccine formulations comprising a buffer, surfactant, sugar, alkali or alkaline salt, aluminum adjuvant, optionally a bulking agent, and optionally a polymer.
    Type: Application
    Filed: August 13, 2018
    Publication date: November 19, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ramesh V. Chintala, Akhilesh Bhambhani, Christopher David Mensch, Denise K. Nawrocki, Jeffrey Thomas Blue
  • Publication number: 20200360360
    Abstract: Disclosed are pharmaceutical compositions comprising tedizolid phosphate, methods of preparing such pharmaceutical compositions, and methods of treating bacterial infections with such pharmaceutical compositions. Specifically, a pharmaceutical composition comprising tedizolid phosphate, an acid; and a suspending agent; and wherein the pH of the composition upon constitution with water is between about pH 2-4.5, is provided, wherein the acid is not citric acid or malic acid.
    Type: Application
    Filed: December 10, 2018
    Publication date: November 19, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Lixia Cai, David Dubost, David Harris, Yongjun Li, Majid Mahjour, Dan Zhang
  • Publication number: 20200361928
    Abstract: The present invention relates to biaryl monobactam compounds of Formula I and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A1, Q, A2, M, W, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.
    Type: Application
    Filed: June 25, 2020
    Publication date: November 19, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Weiguo Liu, Fa-Xiang Ding, Wanying Sun, Yi Zang, Weidong Pan, Anthony Ogawa, Linda Brockunier, Xianhai Huang, Hongwu Wang, Rudrajit Mal, Tesfaye Biftu, Min Park, Yan Guo, Jinlong Jiang, Helen Y. Chen, Christopher W. Plummer
  • Patent number: 10839571
    Abstract: Large data sets (e.g., with millions of records) are represented by a heat map within a user interface (UI). Each record in the data set includes a label. The labels of the records are assigned to leaf nodes of a data structure. The leaf nodes are mapped to a grid of cells according to a layout method. Furthermore, values are determined for the cells based on data records having the labels mapped to the cells. A visual property is selected for each cell based on the corresponding value. Since the data labels are stored in leaf nodes that are connected to internal nodes, if a zoom state of the heat map results in a display of a number of data labels that exceeds the number of cells in the grid, values of the cells can be updated according to values determined from the internal nodes without losing the connections between the cells and the underlying leaf nodes.
    Type: Grant
    Filed: November 9, 2018
    Date of Patent: November 17, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Stephen C. North, David J. Tabacco, David B. Hurry
  • Patent number: 10836775
    Abstract: The present invention is directed to 6,6-fused heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors 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 diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Grant
    Filed: December 18, 2017
    Date of Patent: November 17, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xiaolei Gao, Sandra L. Knowles, Chunsing Li, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Ling Tong
  • Publication number: 20200354453
    Abstract: The present invention relates to stable formulations of antibodies against T cell immunoreceptor with Ig and ITIM domains (TIGIT), optionally further containing an anti-human programmed death receptor 1 (PD-1) antibody or antigen binding fragment thereof. Also provided are methods of treating various cancers and chronic infections with the formulations of the invention.
    Type: Application
    Filed: May 1, 2018
    Publication date: November 12, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Arnab De, Chakravarthy Nachu Narasimhan
  • Publication number: 20200354377
    Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
    Type: Application
    Filed: November 5, 2018
    Publication date: November 12, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michelle R. Machacek, David J. Witter, Michael Hale Reutershan, David L. Sloman, Michael D. Altman
  • Publication number: 20200347020
    Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: July 22, 2020
    Publication date: November 5, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Gregory L. Adams, Jason M. Cox, John S. Debenham, Scott Edmondson, Eric J. Gilbert, Yan Guo, Yu Jiang, Hubert Josien, Hyunjin M. Kim, Ping Lan, Shouwu Miao, Christopher W. Plummer, Murali Rajagopalan, Unmesh Shah, Zhongxiang Sun, Quang T. Truong, Feroze Ujjainwalla, Francisco Velazquez, Srikanth Venkatraman, Takao Suzuki, Nengxue Wang
  • Patent number: 10822338
    Abstract: The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
    Type: Grant
    Filed: July 5, 2016
    Date of Patent: November 3, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Xianhai Huang, Yeon-Hee Lim, Rongze Kuang, Heping Wu, Rajan Anand, Younong Yu, Edward Metzger, Michael Man-Chu Lo, Pauline C. Ting, Andrew W. Stamford, Paul Tempest
  • Patent number: 10821175
    Abstract: The instant invention provides for novel lipid nanoparticle (LNP) formulations, containing cationic lipids, for use as vaccine adjuvants and/or as antigen delivery systems. It is an object of the instant invention to provide LNP formulations that demonstrate enhancements in humoral and cellular immunogenicity of vaccine antigens, particularly subunit vaccine antigens, when utilized alone or in combination with immunostimulatory agents (e.g. small molecule or oligonucleotide TLR agonists). The instant invention further identifies physical and chemical properties of the LNP formulations that can be manipulated to enhance antigen efficiency and adjuvant tolerability in vivo.
    Type: Grant
    Filed: February 23, 2015
    Date of Patent: November 3, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Marian Gindy, Danilo R. Casimiro, Andrew Bett, Jan H. Ter Meulen
  • Patent number: 10815214
    Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
    Type: Grant
    Filed: September 19, 2019
    Date of Patent: October 27, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Cheol K. Chung, Mark E. Scott, Paul G. Bulger, Kevin M. Belyk, John Limanto, Guy R. Humphrey
  • Publication number: 20200330427
    Abstract: Therapies comprising administering at least one benzo[b]thiophene compound that activates the Stimulator of Interferon Genes (STING) pathway, and the use of such therapies in the treatment of cell-proliferation disorders such as cancer, are disclosed herein.
    Type: Application
    Filed: July 30, 2018
    Publication date: October 22, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Saso CEMERSKI, Jared N. CUMMING, Johnny E. KOPINJA, Samanthi A. PERERA, Benjamin Wesley TROTTER, Archie Ngai-Chiu TSE