Patents Assigned to Merck Sharp & Dohme
  • AZIDE INSULIN ANALOGUES
    Publication number: 20230365646
    Abstract: The present invention relates to insulin analogues and processes of making such insulin analogues by direct conversion of a free amine to an azide via diazo-transfer with an azotransfer agent.
    Type: Application
    Filed: July 31, 2023
    Publication date: November 16, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Sobhana Babu Boga, Ahmet Kekec, Songnian Lin, Craig A. Parish, Weijuan Tang, Lin Yan
  • BICYCLOHEPTANE PYRROLIDINE OREXIN RECEPTOR AGONISTS
    Publication number: 20230365533
    Abstract: The present invention is directed to bicyclo[4.1 0]heptane pyrrolidine compounds of formula (I) which are agonists of orexin receptors. 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 orexin 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 orexin receptors are involved.
    Type: Application
    Filed: August 16, 2021
    Publication date: November 16, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Stephane L. Bogen, Dane James Clausen, Deodial Guy Guiadeen, Jinsong Hao, Shishi Lin, Michael T. Rudd, Lan Wei, Li Xiao, Dexi Yang
  • INHIBITORS OF HUMAN RESPIRATORY SYNCYTIAL VIRUS AND METAPNEUMOVIRUS
    Publication number: 20230365551
    Abstract: The present disclosure is directed to compounds of Formula I or a pharmaceutically acceptable salt thereof, and their use for the treatment of hRSV and hMPV.
    Type: Application
    Filed: May 11, 2023
    Publication date: November 16, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Douglas C. Beshore, Brett R. Ambler, Kira A. Armacost, Christopher James Bungard, Danielle M. Hurzy, Peter J. Manley, Kelly-Ann S. Schlegel, Linda M. Suen-Lai, Mahdieh Yazdani
  • BINDING PROTEINS AND ANTIGEN BINDING FRAGMENTS THEREOF THAT BIND ABETA
    Publication number: 20230365667
    Abstract: Binding proteins that bind amyloid beta (Abeta) are described, including heavy chain antibody variable domain (VHH) constructs comprising human-like VHH comprising three synthetically generated complementarity determining region (CDR) areas. Human-like VHHs identified using these libraries may be useful for the manufacture of therapeutics for treating diseases and disorders.
    Type: Application
    Filed: September 27, 2021
    Publication date: November 16, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Alexander Mario Sevy, Ming-Tang Chen
  • STABLE FORMULATIONS OF PROGRAMMED DEATH RECEPTOR 1 (PD-1) ANTIBODIES AND HYALURONIDASE VARIANTS AND FRAGMENTS THEREOF AND METHODS OF USE THEREOF
    Publication number: 20230365692
    Abstract: The invention relates to stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof and a PH20 variant or fragment thereof. The invention further provides methods for treating various cancers with formulations of the invention. In some embodiments of the methods of the invention, the formulations are administered to a subject by subcutaneous administration.
    Type: Application
    Filed: September 23, 2021
    Publication date: November 16, 2023
    Applicant: MERCK SHARP & DOHME LLC
    Inventors: Yogita KRISHNAMACHARI, Sachin MITTAL, Sahil S. SANGANI, William P. FORREST, Jr., Yongchao SU, Xi ZHAO, Katelyn Jean SMITH
  • DOSING REGIMENS OF ANTI-ILT4 ANTIBODY OR ITS COMBINATION WITH ANTI-PD-1 ANTIBODY FOR TREATING CANCER
    Publication number: 20230365678
    Abstract: Provided herein are dosing regimens of an anti-immunoglobulin-like transcript 4 (anti-ILT4) antibody for treating cancer. Further provided are dosing regimens for treating cancer using a combination of an anti-ILT4 antibody and another agent (e.g., a PD-1 antagonist, such as an anti-PD-1 antibody or an anti-PD-L 1 antibody).
    Type: Application
    Filed: September 15, 2021
    Publication date: November 16, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Anson K. Abraham, Rachel A. Altura, Douglas C. Wilson
  • 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
  • TETRAHYDROQUINAZOLINE DERIVATIVES AS SELECTIVE CYTOTOXIC AGENTS
    Publication number: 20230357204
    Abstract: The present disclosure is directed to tetrahydroquinazoline derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naïve cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
    Type: Application
    Filed: August 25, 2021
    Publication date: November 9, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Antonella Converso, Abdellatif El Marrouni, Anthony W. Shaw, David N. Hunter, Ashley Forster, Cheng Wang, Yunlong Zhang
  • METHODS OF CHEMOVACCINATION AGAINST PLASMODIUM INFECTIONS
    Publication number: 20230355622
    Abstract: A method of chemovaccination against Plasmodium infections comprising administering to a patient, an effective amount of a dual inhibitor of plasmepsin IX and X, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 20, 2021
    Publication date: November 9, 2023
    Applicants: Merck Sharp & Dohme LLC, The Walter and Eliza Hall Institute of Medical Research
    Inventors: Justin A. Boddey, David B. Olsen, Ryan Steel
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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