Patents Assigned to Merck Sharp
  • Methods of treating or reducing the risk of cardiovascular events and related diseases using SGLT-2 inhibitors
    Patent number: 12036203
    Abstract: The present invention relates to the use of certain SGLT-2 inhibitors, such as ertugliflozin or a pharmaceutically acceptable salt or a co-crystal thereof, for treating, reducing the risk of and/or preventing heart failure, myocardial infarction, cardiovascular disease or cardiovascular death in animals without type 2 or type 1 diabetes mellitus, or in animals with pre-diabetes, or in animals with type 2 or type 1 diabetes mellitus or pre-diabetes.
    Type: Grant
    Filed: October 10, 2019
    Date of Patent: July 16, 2024
    Assignees: Merck Sharp & Dohme LLC, Pfizer Inc.
    Inventors: Brett Lauring, Samuel S. Engel, Steven G. Terra, James M. Rusnak
  • Pyridopyrazine and pyridotriazine inhibitors of influenza virus replication
    Patent number: 12037333
    Abstract: Provided herein are compounds that can inhibit the replication of influenza viruses, reduce the amount of influenza viruses, and/or treat influenza.
    Type: Grant
    Filed: September 10, 2019
    Date of Patent: July 16, 2024
    Assignees: COCRYSTAL PHARMA, INC., MERCK SHARP & DOHME LLC
    Inventors: Irina C. Jacobson, Biing Yuan Lin, Emiliano J. Sanchez, Sam S K Lee, Hong Xiao
  • Enzymatic synthesis of 4?-ethynyl nucleoside analogs
    Patent number: 12037623
    Abstract: The present invention relates to an enzymatic synthesis of 4?-ethynyl-2?-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.
    Type: Grant
    Filed: July 2, 2019
    Date of Patent: July 16, 2024
    Assignee: Merck, Sharp & Dohme LLC
    Inventors: Mark A. Huffman, Anna Fryszkowska, Joshua N. Kolev, Paul N. Devine, Kevin R. Campos, Matthew Truppo, Christopher C. Nawrat
  • BLOW-FILL SEALING METHOD FOR FILLING AND PACKAGING
    Publication number: 20240226439
    Abstract: A method of controlling a temperature of a biopharmaceutical product during blow-fill sealing, includes developing a model based on heat transfer mechanisms that incorporates the effects of the blow-fill sealing on the biopharmaceutical product, providing a parison to a blow-fill sealing machine for accepting the biopharmaceutical product during the blow-fill sealing, predicting a temperature of at least one the biopharmaceutical product, the parison, and a component of the blow-fill sealing machine at a stage in the blow-fill sealing, and adjusting a parameter of the blow-fill sealing machine to reduce damage to the biopharmaceutical product.
    Type: Application
    Filed: October 11, 2023
    Publication date: July 11, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Carl Chew, Matthew H. Flamm, Jeremy A. Haddock, Rikhabh Jain, Atul Karande, Brit L. Rudeen
  • ANTI-ILT4 ANTIBODIES AND ANTIGEN-BINDING FRAGMENTS
    Publication number: 20240228614
    Abstract: The present invention provides antibodies and antigen-binding fragments thereof that bind to ILT4 (immunoglobulin-like transcript 4) and combinations thereof, e.g., with an anti-PD1 antibody. Also provided are methods of use thereof, for example, for treating or preventing cancer in a subject; and methods of making such antibodies and fragments.
    Type: Application
    Filed: December 20, 2023
    Publication date: July 11, 2024
    Applicants: Merck Sharp & Dohme LLC, Agenus Inc.
    Inventors: Milan Blanusa, Barbara Joyce-Shaikh, Andrea Claudia Schuster, Kornelia Schultze, Luis A. Zuniga
  • RIPK1 INHIBITORS AND METHODS OF USE
    Publication number: 20240228506
    Abstract: Described herein are compounds of Formula II, or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.
    Type: Application
    Filed: April 21, 2022
    Publication date: July 11, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Erin F. DiMauro, Xavier Fradera, Peter H. Fuller, Min Lu, Joey L. Methot, Matthew J. Mitcheltree, Andrew J. Musacchio, Phieng Siliphaivanh, Jing Su
  • COMBINATION THERAPIES FOR TREATING CANCER
    Publication number: 20240226082
    Abstract: The present invention provides methods of treatment for recurrent cancer(s) through combination therapy with an agent that inhibits programmed death-1 protein (PD-1) signaling and an agent that inhibits poly [ADP-ribose] polymerase (PARP) signaling.
    Type: Application
    Filed: December 15, 2023
    Publication date: July 11, 2024
    Applicants: TESARO, Inc., MERCK SHARP & DOHME B.V.
    Inventors: Dmitri Bobilev, Bruce Dezube, Peng Sun, Andrew R. Ferguson
  • PROTEASE INHIBITORS FOR TREATING OR PREVENTING CORONAVIRUS INFECTION
    Publication number: 20240228535
    Abstract: The present invention provides a compound of Formula I wherein R1, R2, R3, R4, R5, R6, R7, and subscripts x and n are as described herein and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for the treatment, inhibition, or amelioration of one or more disease states that could benefit from inhibition of a coronavirus, including SARS-CoV, MERS-CoV and SARS-CoV-2. The compounds of this invention could further be used in combination with other therapeutically effective agents, including but not limited to, other drugs useful for the treatment of coronavirus infection. The invention furthermore relates to processes for preparing compounds of Formula I, and pharmaceutical compositions which comprise compounds of Formula I and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: November 20, 2023
    Publication date: July 11, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: John J. Acton, III, Mayuri Gupta, Michael J. Kelly, III, Franca-Maria Klingler, Mark Eric Layton, John A. McCauley, Gregori J. Morriello, Christopher Charles Nawrat, Craig A. Parish, Anthony J. Roecker, Manuel de Lera Ruiz, Jing Su, Valerie W. Shurtleff, Quang T. Truong
  • N-heteroaryl indazole derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof
    Patent number: 12030872
    Abstract: The present invention is directed to substituted certain N-heteroaryl indazole derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z 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 diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.
    Type: Grant
    Filed: October 25, 2019
    Date of Patent: July 9, 2024
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Vladimir Simov, William P. Kaplan, John J. Acton, III, Michael J. Ardolino, Joanna L Chen, Peter H. Fuller, Hakan Gunaydin, Derun Li, Ping Liu, Kaitlyn Marie Logan, Joey Methot, Gregori J. Morriello, Santhosh F. Neelamkavil, Luis Torres, Xin Yan, Hua Zhou
  • NOVEL FORMS OF CYCLIC DINUCLEOTIDE COMPOUNDS
    Publication number: 20240218009
    Abstract: Novel forms of 2-amino-9-[(2R,5R,7R,8S,10R,12aR, 14R,15S,15aR,16R)-14-(6-amino-9H-purin-9-yl)-15,16-difluoro-2,10-dihydroxy-2,10-disulfidooctahydro-12H-5,8-methanofuro[3,2-1][1,3,6,9,11,2,10]pentaoxadiphospha-cyclotetradecin-7-yl]-1,9-dihydro-6H-purin-6-one, which include adducts of 2-amino-9-[(2R,5R,7R,8S,10R,12aR, 14R,15S,15aR,16R)-14-(6-amino-9H-purin-9-yl)-15,16-difluoro-2,10-dihydroxy-2,10-disulfidooctahydro-12H-5,8-methanofuro[3,2-1][1,3,6,9,11,2,10]pentaoxadiphospha-cyclotetradecin-7-yl]-1,9-dihydro-6H-purin-6-one and L-histidine, may be useful as inductors of type I interferon production, specifically as STING active agents.
    Type: Application
    Filed: April 18, 2022
    Publication date: July 4, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Stephanus Axnanda, Andrew Patrick Jude Brunskill, Erin N. Guidry, Eric A. Kemp, Courtney K. Maguire, Mikhail Reibarkh, Matthew S. Winston
  • OXAZOLIDINONE COMPOUND AND METHODS OF USE THEREOF AS AN ANTIBACTERIAL AGENT
    Publication number: 20240208958
    Abstract: The present invention relates to the oxazolidinone compound of Formula (I): and pharmaceutically acceptable salts thereof. The present invention also relates to compositions containing the compound of Formula (I). The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering a therapeutically effective amount of Formula (I) and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
    Type: Application
    Filed: March 20, 2021
    Publication date: June 27, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Brendan M. CROWLEY, Philippe NANTERMET, David B. OLSEN, Takao SUZUKI, Lihu YANG, Lanying YOU
  • AURISTATIN LINKER-PAYLOADS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
    Publication number: 20240207425
    Abstract: The present disclosure is directed to linker-payloads, and pharmaceutically acceptable salts, solvates, or stereoisomer thereof, comprising a structure of formula I: The disclosure is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds, intermediates thereof, and compositions in the prevention or treatment of cancers and/or tumors.
    Type: Application
    Filed: December 12, 2023
    Publication date: June 27, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Manoj B. Charati, John A. Flygare, Rebecca Elizabeth Johnson, Simon B. Lang, W. Michael Seganish
  • PLASMA KALLIKREIN INHIBITORS
    Publication number: 20240208994
    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 degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.
    Type: Application
    Filed: April 18, 2022
    Publication date: June 27, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Alan C. Cheng, Ying-Duo Gao, Song Yang, Mihir Mandal, Jiafang He, Jovan Alexander Lopez, Maoqun Tian
  • EXATECAN-DERIVED ADC LINKER-PAYLOADS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
    Publication number: 20240208987
    Abstract: The present disclosure is directed to linker-payloads, and salts (including pharmaceutically acceptable salts), solvates, or stereoisomers thereof, comprising a structure of formula I: The disclosure is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds, intermediates thereof, and compositions in the prevention or treatment of cancers and/or tumors.
    Type: Application
    Filed: October 23, 2023
    Publication date: June 27, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Vlad Bacauanu, Manoj B. Charati, Sijie Chen, Rebecca Elizabeth Johnson, Simon B. Lang, Christian L. Morales, Ryan Quiroz, W. Michael Seganish, Nancy Zepeda
  • PHENYL AZEPINES AS RIPK1 INHIBITORS AND METHODS OF USE THEREOF
    Publication number: 20240208986
    Abstract: Described herein are compounds of Formula I: (I), or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.
    Type: Application
    Filed: April 21, 2022
    Publication date: June 27, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Joanna L. Chen, Erin F. DiMauro, Kevin D. Dykstra, Xavier Fradera, Peter H. Fuller, Charles A. Lesburg, Min Lu, Joey L. Methot, Matthew J. Mitcheltree, Jing Su
  • Container system and method for freezing and thawing a liquid product
    Patent number: 12016330
    Abstract: Container system and method for freezing (and subsequently thawing) a liquid such as a drug substance, such that all containers in a set have a uniform width, hence uniform freeze-path length, in the widthwise direction and perpendicular to major walls of the containers, irrespective of the particular length, height, and volumetric capacity of the various containers in the set. This leads to uniform freezing performance and thereby reduces cryoconcentration. The system also eliminates or reduces ice-bridging, and the potential for containers rupturing during freezing and thawing operations.
    Type: Grant
    Filed: December 8, 2021
    Date of Patent: June 25, 2024
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Jeffrey Charles Johnson, Anthony Flammino, Mark Anton Petrich, Scott McFeaters, John H. Roosa, Jr., Robert Ian Alpern, Joseph W. Locurcio, Matthew H. Flamm
  • Compositions comprising polysaccharide-protein conjugates and methods of use thereof
    Patent number: 12016914
    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: Grant
    Filed: March 23, 2023
    Date of Patent: June 25, 2024
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Chitrananda Abeygunawardana, Yadong Adam Cui, Romulo Ferrero, Jian He, Luwy Musey, Tanaz Petigara, Julie M. Skinner
  • ROTAVIRUS VECTORS FOR HETEROLOGOUS GENE DELIVERY
    Publication number: 20240200099
    Abstract: Rotavirus vectors encoding in their genome a heterologous gene, and nucleic acid constructs encoding such rotavirus vectors. The rotavirus vector genome may include a rotavirus non-structural protein, a 2A peptide downstream of the rotavirus non-structural protein, and a heterologous protein downstream of the 2A peptide. The heterologous gene may be, for example, a SARS-CoV-2 spike protein or a fragment thereof, or an RSV F protein or a fragment thereof.
    Type: Application
    Filed: April 11, 2022
    Publication date: June 20, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Dai Wang, Jiajie Wei
  • SYNTHESIS OF FLUORINATED CYCLIC DINUCLEOTIDES
    Publication number: 20240199680
    Abstract: The present invention relates to efficient processes useful in the preparation of fluorinated cyclic dinucleosides, such as [P(R)]-2?-deoxy-2?-fluoro-5?-O—[(R)-hydroxymercaptophosphinyl]-P-thio-?-D-arabino-adenylyl-(3??5?)-3?-deoxy-3?-fluoroguanosine cyclic nucleotide, which is also known as (2R,5R,7R,8S,10R,12aR,14R,15S,15aR,16R)-7-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-14-(6-amino-9H-purin-9-yl)-15,16-difluoro-2, 10-bis(sulfanyl)octahydro-2H,10H, 12H-2?5,10?5-5,8-methanofuro[3,2-1][1, 3,6,9,11,2,10]pentaoxadiphosphacyclotetradecine-2,10-dione. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
    Type: Application
    Filed: March 28, 2022
    Publication date: June 20, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Chihui An, Patrick S. Fier, Kaori Hiraga, Zhijian Liu, Nicholas M. Marshall, John McIntosh, Steven P. Miller, Jeffrey C. Moore, Grant S. Murphy, Jennifer V. Obligacion, Weilan Pan, Feng Peng, Nastaran Salehi Marzijarani, Matthew S. Winston
  • Cyclic polypeptides for PCSK9 inhibition
    Patent number: 12012468
    Abstract: Provided herein are cyclic polypeptide compounds that can, e.g., bind specifically to human proprotein convertase subtilisin/kexin type 9 (PCSK9) and optionally also inhibit interaction between human PCSK9 and human low density lipoprotein receptor (LDLR), and pharmaceutical compositions comprising one or more of these compounds. Also provided are methods of reducing LDL cholesterol level in a subject in need thereof that include administering to the subject one or more of the cyclic polypeptide compounds or a pharmaceutical composition provided herein.
    Type: Grant
    Filed: September 27, 2022
    Date of Patent: June 18, 2024
    Assignees: MERCK SHARP & DOHME LLC, RA PHARMACEUTICALS, INC.
    Inventors: Alonso Ricardo, Thomas Joseph Tucker, Nicolas Cedric Boyer, Joseph R. Stringer, Derek M. LaPlaca, Angela Dawn Kerekes, Chengwei Wu, Sookhee Nicole Ha, Hyewon Youm, Mark W. Embrey, Elisabetta Bianchi, Danila Branca, Raffaele Ingenito, Willy Costantini, Alessia Santoprete, Roberto Costante, Immacolata Conte, Stefania Colarusso, Eric J. Gilbert, Aurash Shahripour, Yusheng Xiong