Patents Assigned to Merck Sharp & Dohme LLC
  • CORONAVIRUS REPLICONS FOR ANTIVIRAL SCREENING AND TESTING
    Publication number: 20230357870
    Abstract: This application provides materials and methods related to replication competent, noninfectious coronavirus reporter replicons, such as for SARS-CoV-2, MERS, or SARS-CoV-1 comprising at least one coronavirus gene and at least one reporter gene. The application also provides methods for assaying candidate agents for inhibition of coronavirus viral replication.
    Type: Application
    Filed: September 23, 2021
    Publication date: November 9, 2023
    Applicant: MERCK SHARP & DOHME LLC
    Inventors: Xi HE, Shuo QUAN, Dai WANG, Min XU
  • PLASMA KALLIKREIN INHIBITORS
    Publication number: 20230348428
    Abstract: The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.
    Type: Application
    Filed: July 6, 2021
    Publication date: November 2, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Jacqueline D. HICKS, Rongze Kuang, Christopher J. Sinz, Matthew J. Lombardo, Jovan Alexander Lopez, Rohan Rajiv Merchant, Phillip Patrick Sharp, Zhicai Wu, Zhiqiang Zhao, Alan C. Cheng, Song Yang, Jianming Bao, Maoqun Tian, Galen Paul Shearn-Nance
  • 2-oxoimidazolidine-4-carboxamides as NA1.8 inhibitors
    Patent number: 11802122
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
    Type: Grant
    Filed: June 15, 2021
    Date of Patent: October 31, 2023
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Ashok Arasappan, Ian M. Bell, Christopher James Bungard, Christopher S. Burgey, Jason M. Cox, Michael J. Kelly, III, Mark E. Layton, Hong Liu, Jian Liu, James J. Perkins, Akshay A. Shah, Michael David VanHeyst, Zhe Wu
  • COMPOSITIONS COMPRISING STREPTOCOCCUS PNEUMONIAE POLYSACCHARIDE-PROTEIN CONJUGATES AND METHODS OF USE THEREOF
    Publication number: 20230338498
    Abstract: The invention is related to multivalent immunogenic compositions comprising more than one S. pneumoniae polysaccharide protein conjugates, wherein each of the conjugates comprises a polysaccharide from an S. pneumoniae serotype conjugated to a carrier protein, wherein the serotypes of S. pneumoniae are as defined herein. Also provided are methods for inducing a protective immune response in a human patient comprising administering the multivalent immunogenic compositions of the invention to the patient. The multivalent immunogenic compositions are useful for providing protection against S. pneumoniae infection and/or pneumococcal diseases caused by S. pneumoniae.
    Type: Application
    Filed: March 23, 2023
    Publication date: October 26, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Chitrananda Abeygunawardana, Yadong Adam Cui, Romulo Ferrero, Jian He, Luwy Musey, Tanaz Petigara, Julie M. Skinner
  • METHODS OF TREATING CANCER USING A COMBINATION OF A PD-1 ANTAGONIST, A CHEMORADIATION THERAPY AND A PARP INHIBITOR
    Publication number: 20230338521
    Abstract: Provided herein are methods of treating cancer using a combination of (a) one or more programmed death 1 protein (PD-1) antagonists, (b) a radiotherapy, (c) one or more poly (ADP-ribose) polymerase (PARP) inhibitor, and optionally, (d) one or more chemotherapies. Also provided herein is a kit for pharmaceutical administration comprising: (a) a PD-1 antagonist; (b) a radiotherapy; (c) a PARP inhibitor; and (d) optionally, a chemotherapy. Further provided herein are uses of a combination for treating cancer in a human patient, wherein the combination comprises: (a) an effective amount of one or more PD-1 antagonists, (b) an effective amount of a radiotherapy, (c) an effective amount of a PARP inhibitor, and (d) optionally, one or more chemotherapies.
    Type: Application
    Filed: April 29, 2021
    Publication date: October 26, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Roger M. Perlmutter, Maria Catherine Pietanza
  • Substituted 6-membered aryl or heteroaryl allosteric modulators of nicotinic acetylcholine receptors
    Patent number: 11793821
    Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation
    Type: Grant
    Filed: March 5, 2021
    Date of Patent: October 24, 2023
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Brendan M. Crowley, Ian M. Bell, Andrew John Harvey
  • LAG3 ANTAGONIST CELL BASED POTENCY ASSAY
    Publication number: 20230333090
    Abstract: The present disclosure describes a murine T cell 3A9 comprising a polynucleotide sequence encoding human LAG3, and a murine IL-2 promotor operably associated with a reporter gene. The disclosure also describes a cell-based potency assay for measuring LAG3 antagonist activity using a co-cultured system with the murine T cells and LK35.2 murine B cells, and hen egg lysozyme peptide.
    Type: Application
    Filed: December 16, 2020
    Publication date: October 19, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Kevin B. Gurney, Yue Zhang, Linda Liang, Cuiwei Ai
  • Diacylglyceride O-acyltransferase 2 inhibitors
    Patent number: 11787810
    Abstract: Invented are compounds of formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 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 hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.
    Type: Grant
    Filed: May 13, 2021
    Date of Patent: October 17, 2023
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Yeon-Hee Lim, Cedric Lorenz Hugelshofer, Victor W. Mak, James Patrick Roane, Jillian R. Sanzone, Samantha E. Shockley, Rose Yen
  • STABLE FORMULATIONS OF PROGRAMMED DEATH RECEPTOR 1 (PD-1) ANTIBODIES AND METHODS OF USE THEREOF
    Publication number: 20230321234
    Abstract: The invention relates to stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof. In some embodiments the formulations of the invention comprise between 5-200 mg/mL anti- PD-1 antibody, or antigen binding fragment thereof. The invention further provides methods for treating various cancers with stable formulations of the invention. In some embodiments of the methods of the invention, the formulations are administered to a subject by intravenous or subcutaneous administration.
    Type: Application
    Filed: March 10, 2023
    Publication date: October 12, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Manoj K. Sharma, Wendy Benjamin, Sarita Mittal, Ashwin Basarkar, Chakravarthy Nachu Narasimhan, Ramesh S. Kashi, Mohammed Shameem, Soumendu Bhattacharya, William P. Forrest, Jr., Yogita Krishnamachari
  • ADENOSINE A2A AND A2B RECEPTOR DUAL ANTAGONISTS FOR IMMUNO-ONCOLOGY
    Publication number: 20230322785
    Abstract: 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.
    Type: Application
    Filed: July 21, 2022
    Publication date: October 12, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: 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
  • PROCESS FOR PREPARING SUGAMMADEX
    Publication number: 20230312887
    Abstract: The present invention relates to a process for drying crystalline sugammadex to meet solvent specifications that is independent of API crystallinity or crystalline form generated. It further relates to use of sugammadex in the reversal of neuromuscular blockade induced by recuronium bromide or by vecuronium bromide in adults undergoing surgery.
    Type: Application
    Filed: September 8, 2021
    Publication date: October 5, 2023
    Applicants: Merck Sharp & Dohme LLC, Werthenstein BioPharma GMBH
    Inventors: David J. Lamberto, Paolo Avalle, Lorenzo Codan, Patrick Larpent, Jochen Schoell, Jeffrey S. Neuhaus
  • INJECTABLE DEPOT COMPOSITIONS FOR THE DELIVERY OF ANTIVIRAL AGENTS
    Publication number: 20230310309
    Abstract: This invention relates to novel injectable depot compositions for long-acting delivery of antiviral drugs. These compositions are useful for the treatment or prevention of human immunodeficiency virus (HIV) infection.
    Type: Application
    Filed: August 23, 2021
    Publication date: October 5, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Stephanie Elizabeth Barrett, Seth P. Forster, Marian E. Gindy
  • INSULIN RECEPTOR PARTIAL AGONISTS
    Publication number: 20230310551
    Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
    Type: Application
    Filed: August 24, 2021
    Publication date: October 5, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Christina B. Madsen-Duggan, Danqing Feng, Pei Huo, Ahmet Kekec, Songnian Lin, Ravi Nargund, Christopher R. Moyes, Dmitri A. Pissarnitski, Zhicai Shi, Zhicai Wu, Lin Yan, Yuping Zhu
  • 2-OXO-IMIDAZOLIDINE-4-CARBOXAMIDES AS NAV1.8 INHIBITORS
    Publication number: 20230312528
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
    Type: Application
    Filed: June 5, 2023
    Publication date: October 5, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Ashok Arasappan, Ian M. Bell, Christopher James Bungard, Christopher S. Burgey, Jason M. Cox, Michael J. Kelly, III, Mark E. Layton, Hong Liu, Jian Liu, James J. Perkins, Akshay A. Shah, Michael David VanHeyst, Zhe Wu
  • Progressively-trained scale-invariant and boundary-aware deep neural network for the automatic 3D segmentation of lung lesions
    Patent number: 11776130
    Abstract: A system and method are disclosed for segmenting a set of two-dimensional CT slices corresponding to a lesion. In an embodiment, for each of at least a subset of the set of CT slices, the system inputs the CT slice into a plurality of branches of a trained segmentation block. Each branch of the segmentation block includes a convolutional neural network (CNN) with filters at a different scale, and produces a plurality of levels of output. The system generates, for each CT slice in the subset, feature maps for each level of output. The system generates a segmentation of each CT slice in the subset based on the feature maps of each level of output. The system aggregates the segmentations of each slice in the subset to generate a three-dimensional segmentation of the lesion. The system provides data representing the three-dimensional segmentation for display.
    Type: Grant
    Filed: January 18, 2022
    Date of Patent: October 3, 2023
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Antong Chen, Gregory Goldmacher, Bo Zhou
  • Antibody peptide conjugates that have agonist activity at both the glucagon and glucagon-like peptide 1 receptors
    Patent number: 11773150
    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: Grant
    Filed: August 27, 2020
    Date of Patent: October 3, 2023
    Assignees: Merck Sharp & Dohme LLC, Ambrx, Inc.
    Inventors: Paul E. Carrington, Grigori Ermakov, Robert M. Garbaccio, Wolfgang Seghezzi, Elisabetta Bianchi, Federica Orvieto, Dennis Gately, Nick Knudsen, Anthony Manibusan
  • 2-AMINOQUINAZOLINES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
    Publication number: 20230303540
    Abstract: The present invention is directed to certain 2-aminoquinzaoline derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R3, R4, X1, and X2 are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
    Type: Application
    Filed: September 1, 2021
    Publication date: September 28, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: John J. Acton, III, Ryan Chau, Peter H. Fuller, Anmol Gulati, Rebecca Elizabeth Johnson, Solomon Kattar, Mitchell H. Keylor, Derun Li, Kaila A. Margrey, Gregori J. Morriello, Xin Yan
  • N3-substituted iminopyrimidinones as antimalarial agents
    Patent number: 11766435
    Abstract: 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.
    Type: Grant
    Filed: February 13, 2017
    Date of Patent: September 26, 2023
    Assignees: Merck Sharp & Dohme LLC, The Walter and Eliza Hall Institute of Medical Research
    Inventors: Tanweer A. Khan, Jared N. Cumming, David B. Olsen, Justin A. Boddey, Alan F. Cowman, Brad E. Sleebs
  • Pneumococcal polysaccharides and their use in immunogenic polysaccharide-carrier protein conjugates
    Patent number: 11759510
    Abstract: The present invention provides capsular polysaccharides from Streptococcus pneumoniae serotypes identified using NMR. The present invention further provides polysaccharide-protein conjugates in which capsular polysaccharides from one or more of these serotypes are conjugated to a carrier protein such as CRM197. Polysaccharide-protein conjugates from one or more of these serotypes may be included in multivalent pneumococcal conjugate vaccines having polysaccharides from multiple additional Streptococcus pneumoniae serotypes.
    Type: Grant
    Filed: June 24, 2022
    Date of Patent: September 19, 2023
    Assignee: Merck, Sharp & Dohme LLC
    Inventors: Richard J. Porambo, Chitrananda Abeygunawardana, Luwy Kavuka Musey, Michael J. Kosinski, Yadong Adam Cui
  • Pneumococcal polysaccharides and their use in immunogenic polysaccharide-carrier protein conjugates
    Patent number: 11759523
    Abstract: The present invention provides capsular polysaccharides from Streptococcus pneumoniae serotypes identified using NMR. The present invention further provides polysaccharide-protein conjugates in which capsular polysaccharides from one or more of these serotypes are conjugated to a carrier protein such as CRM197. Polysaccharide-protein conjugates from one or more of these serotypes may be included in multivalent pneumococcal conjugate vaccines having polysaccharides from multiple additional Streptococcus pneumoniae serotypes.
    Type: Grant
    Filed: June 24, 2022
    Date of Patent: September 19, 2023
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Richard J. Porambo, Chitrananda Abeygunawardana, Luwy Kavuka Musey, Michael J. Kosinski, Yadong Adam Cui