Patents Assigned to Merck Sharp & Dohme
  • FUNCTIONAL CELL-BASED POTENCY ASSAY FOR MEASURING BIOLOGICAL ACTIVITY OF INTERLEUKIN 2 (IL-2) ANALOGS
    Publication number: 20240255492
    Abstract: A functional cell-based potency assay for measuring the biological activity of IL-2 mutants with biased activity for the IL-2 receptor beta-gamma complex is described. In particular, the present invention relates to a Kit225 cell line that lacks expression of the IL-2 receptor alpha and its use in said functional cell-based potency assay.
    Type: Application
    Filed: June 2, 2022
    Publication date: August 1, 2024
    Applicant: MERCK SHARP & DOHME LLC
    Inventors: DANILA G. GIACONE, DAVID P. SANDEN, AARRON WILLINGHAM, JUNMING YIE
  • TRANSAMINASE ENZYMES FOR THE TRANSAMINATION OF (1S,5R)-6,8-DIOXABICYCLO[3.2.1]OCTAN-4-ONE
    Publication number: 20240247240
    Abstract: The present disclosure provides transaminase enzymes having improved properties and are capable of reducing (1S,5R)-6,8-dioxabicyclo[3.2.1]octan-4-one with high selectivity. Also provided are polynucleotides encoding the transaminase enzymes, host cells capable of expressing the transaminase enzymes, and methods of using the transaminase enzymes to synthesize (1S,4R,5R)-6,8-dioxabicyclo[3.2.1]octan-4-amine.
    Type: Application
    Filed: May 26, 2022
    Publication date: July 25, 2024
    Applicant: MERCK SHARP & DOHME LLC
    Inventors: Karla M. Camacho Soto, Wai Ling Cheung-Lee, Hsing-I Ho, John McIntosh, Grant S. Murphy, Weilan Pan, Christopher K. Prier, Deeptak Verma
  • ARYL 3-OXOPIPERAZINE CARBOXAMIDES AND HETEROARYL 3-OXOPIPERAZINE CARBOXAMIDES AS NAV1.8 INHIBITORS
    Publication number: 20240246932
    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: May 2, 2022
    Publication date: July 25, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Ashok Arasappan, Ian M. Bell, Jason M. Cox, Michael J. Kelly, III, Mark Eric Layton, Hong Liu, Jian Liu, Akshay A. Shah, Michael D. VanHeyst
  • ANTIBODY NEUTRALIZING HUMAN RESPIRATORY SYNCYTIAL VIRUS
    Publication number: 20240247052
    Abstract: The present invention relates to monoclonal antibodies which have high anti-RSV neutralizing titers. The invention further provides for isolated nucleic acids encoding the antibodies of the invention and host cells transformed therewith. The invention yet further provides for diagnostic, prophylactic and therapeutic methods employing the antibodies and nucleic acids of the invention, particularly as a passive immunotherapy agent in infants and the elderly.
    Type: Application
    Filed: April 9, 2024
    Publication date: July 25, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Kalpit A. Vora, Kara S. Cox, Aimin Tang, Zhifeng Chen, Daniel DiStefano, Lan Zhang, Hua-Poo Su
  • METHODS OF TREATMENT OF CANCER PATIENTS HAVING ALTERED SETD2 BIOMARKER WITH A PD-1 ANTAGONIST
    Publication number: 20240247065
    Abstract: The present disclosure describes methods of treatment of cancer in patients with altered activity or amount of a SETD2 biomarker with a treatment regimen comprising an antagonist of Programmed Death 1 receptor (PD-1).
    Type: Application
    Filed: May 16, 2022
    Publication date: July 25, 2024
    Applicant: MERCK SHARP & DOHME LLC
    Inventors: Razvan CRISTESCU, Elisha DETTMAN, Yongjin LI, Karla Gabriela RODRIGUEZ-LOPEZ, Michael NEBOZHYN, Rodolfo Fleury PERINI, Raluca Andreia PREDOIU, Yiwei ZHANG
  • IL4I1 INHIBITORS AND METHODS OF USE
    Publication number: 20240246937
    Abstract: The invention discloses a synthesizing method of benzimidazole derivant and intermediate, which is characterized by the following: proceeding arylation among aryl halide and primary amine; adopting L-pro as additive, cuprous iodide as catalyst; proceeding molecular arylation coupling reaction for aryl iodide or aryl bromide and primary amine; adopting iodo phenylamine compound and bromophenylamine compound as starting material; synthesizing the material through several-step transformation.
    Type: Application
    Filed: April 28, 2022
    Publication date: July 25, 2024
    Applicants: MERCK SHARP & DOHME LLC, MSD R&D (CHINA) CO., LTD.
    Inventors: George Madalin GIAMBASU, Andrew M. HAIDLE, Brett A. HOPKINS, James P. JEWELL, Matthew A. LARSEN, Charles A. LESBURG, Ping LIU, Qinglin PU, Sulagna SANYAL, Phieng SILIPHAIVANH, Matthew TUDOR, Catherine M. WHITE, Xin YAN, Lianyun ZHAO, Xiao Mei ZHENG, William P. KAPLAN, Michaelyn Claire LUX, Derun LI, Rebecca JOHNSON
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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