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
Abstract: Described are antibody peptide conjugates (APCs) comprising an antibody conjugated to a peptide analog of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have agonist activity at the glucagon (GCG) receptor and the glucagon-like peptide 1 (GLP-1) receptor and the use of such APCs for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.
Type:
Application
Filed:
August 27, 2020
Publication date:
December 17, 2020
Applicants:
Merck Sharp & Dohme Corp., Ambrx, Inc.
Inventors:
Paul E. Carrington, Grigori Ermakov, Robert M. Garbaccio, Wolfgang Seghezzi, Elisabetta Bianchi, Federica Orvieto, Dennis Gately, Nick Knudsen, Anthony Manibusan
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
Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
Type:
Grant
Filed:
September 11, 2013
Date of Patent:
December 15, 2020
Assignees:
MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
Inventors:
Daniel Bensen, Allen Borchardt, Zhiyong Chen, John M. Finn, Thanh To Lam, Suk Joong Lee, Xiaoming Li, Leslie William Tari, Min Teng, Michael Trzoss, Junhu Zhang, Michael E. Jung, Felice C. Lightstone, Sergio E. Wong, Toan B. Nguyen
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
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.
Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
Type:
Grant
Filed:
July 7, 2017
Date of Patent:
December 8, 2020
Assignees:
MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
Inventors:
Daniel Bensen, Zhiyong Chen, John Finn, Thanh T. Lam, Suk J. Lee, Xiaoming Li, Douglas W. Phillipson, Leslie W. Tari, Michael Trzoss, Junhu Zhang, Felice C. Lightstone, Toan B. Nguyen, Sergio E. Wong, Paul Aristoff, Michael Jung
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
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
Abstract: The instant invention relates to pharmaceutical compositions comprising doravirine, tenofovir disoproxil fumarate and lamivudine. These compositions are useful for the treatment of HIV infection. Also disclosed are processes for making said pharmaceutical compositions.
Type:
Grant
Filed:
February 14, 2020
Date of Patent:
November 24, 2020
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Santipharp Panmai, Aditya Tatavarti, Andrew M. Farrington, Varsha Biyyala, Leonardo R. Allain, Marcela Nefliu, Gerard R. Klinzing, Jie Ren, Matthew Lamm
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
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
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
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
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
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
Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
Type:
Grant
Filed:
June 20, 2019
Date of Patent:
November 10, 2020
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Thomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley