Patents Assigned to Merck Sharp & Dohme LLC
  • FACTOR XIA INHIBITORS
    Publication number: 20240101567
    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 thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Application
    Filed: January 24, 2022
    Publication date: March 28, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: John S. Debenham, Cheng Zhu, Amjad Ali, Sung-Sau So, Ying-Duo Gao
  • UREA OREXIN RECEPTOR AGONISTS
    Publication number: 20240101555
    Abstract: The present invention is directed to urea compounds 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: December 14, 2021
    Publication date: March 28, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Kira A. Armacost, Maria Irina Chiriac, Danielle M. Hurzy, Jeffrey C. Kern, Jian Liu, Peter J. Manley, Philippe Nantermet, Vanessa L. Rada, Michael T. Rudd, Craig A. Stump
  • HUMAN INTERLEUKIN-2 CONJUGATES BIASED FOR THE INTERLEUKIN-2 RECEPTOR BETA-GAMMAC DIMER AND CONJUGATED TO A NONPEPTIDIC, WATER-SOLUBLE POLYMER
    Publication number: 20240101631
    Abstract: Interleukin-2 (IL-2) conjugates comprising at least one or more amino acid substitutions that bias binding to the IL-2 receptor ??c dimer over binding the IL-2 receptor ???c trimer and a non-natural amino acid at or near the N-terminus conjugated to a water-soluble polymer are described. The IL-2 conjugates are useful for treatment and prevention of cell proliferation and cancer in a patient.
    Type: Application
    Filed: October 11, 2023
    Publication date: March 28, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Cristina Abrahams, Edward Bowman, Xiaofan Li, Songnian Lin, Willy Solis, Ryan Stafford, Aarron Willingham, Alice Yam, Junhao Yang, Gang Yin
  • METHODS FOR TREATING CANCER OR INFECTION USING A COMBINATION OF AN ANTI-PD-1 ANTIBODY, AN ANTI-LAG3 ANTIBODY, AND AN ANTI-TIGIT ANTIBODY
    Publication number: 20240092902
    Abstract: Provided herein are methods of treating cancer or infection, which comprise administering to a human patient in need thereof: (a) an anti-human PD-1 monoclonal antibody or antigen binding fragment thereof; (b) an anti-human LAG3 monoclonal antibody or antigen binding fragment thereof; and (c) an anti-human TIGIT monoclonal antibody or antigen binding fragment thereof. Also provided are pharmaceutical compositions and kits containing such agents for the treatment of cancer or infection.
    Type: Application
    Filed: September 6, 2023
    Publication date: March 21, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Mingmei Cai, Rene de Waal Malefyt, Laurence Fayadat-Dilman, Ying Li, Ruban Mangadu, Uyen Phan
  • SYNTHESIS OF ANTIVIRAL NUCLEOSIDES
    Publication number: 20240092818
    Abstract: The present invention relates to efficient synthetic processes useful in the preparation of antiviral nucleosides, particularly uridine 4-oxime 5?-(2-methylpropanoate) {(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(hydroxyimino)-2-oxo-3,4-dihydropyrimidin-1(2H)-yl]oxolan-2-yl}methyl 2-methylpropanoate and pharmaceutically acceptable salts, derivatives, tautomers, isomers, and prodrugs of, which may be active as antiviral agents, as well as compositions and methods thereof. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
    Type: Application
    Filed: December 17, 2021
    Publication date: March 21, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Tamas Benkovics, Patrick S. Fier, Anna Fryszkowska, Mark A. Huffman, Tetsuji Itoh, Jongrock Kong, Peter E. Maligres, Kevin M. Maloney, John McIntosh, Grant S. Murphy, Steven M. Silverman, Hao Yang
  • Chromane amidine monobactam compounds for the treatment of bacterial infections
    Patent number: 11932637
    Abstract: The present invention relates to monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof. The present invention also relates to compositions which comprise a monobactam compound of structural formula I 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 structural formula I, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.
    Type: Grant
    Filed: November 16, 2022
    Date of Patent: March 19, 2024
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Helen Y. Chen, Shuzhi Dong, Zhiyong Hu, Jing Su, Tao Yu, Yong Zhang
  • Cyclic polypeptides for PCSK9 inhibition
    Patent number: 11932705
    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: August 29, 2022
    Date of Patent: March 19, 2024
    Assignees: MERCK SHARP & DOHME LLC, RA PHARMACEUTICALS, INC.
    Inventors: Alonso Ricardo, Thomas Joseph Tucker, Nicolas Cedric Boyer, Ketki Ashok Dhamnaskar, Zhong Ma, Angela Dawn Kerekes, Chengwei Wu, Sookhee Nicole Ha, Hyewon Youm, Elisabetta Bianchi, Danila Branca, Raffaele Ingenito, Willy Costantini, Aurash Shahripour, Yusheng Xiong
  • AMIDO-SUBSTITUTED PYRIDYL COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HERPESVIRUSES
    Publication number: 20240083910
    Abstract: The present invention relates to novel Amido-Substituted Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Heterocycle Compounds for treating or preventing a herpesvirus infection in a patient.
    Type: Application
    Filed: December 14, 2021
    Publication date: March 14, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Richard Thaddeus Berger, JR., Christopher Douglas Cox, Brendan M. Crowley, Marc Labroli, Michael Aaron Plotkin, Izzat Tiedje Raheem, Deyou Sha, Anthony W. Shaw, Jason W. Skudlarek, Ling Tong
  • ARYL ETHER COMPOUNDS AS TEAD MODULATORS
    Publication number: 20240083903
    Abstract: The present invention is directed to a compound of Formula I: or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising them and methods of using such compounds or pharmaceutical salts thereof.
    Type: Application
    Filed: February 15, 2022
    Publication date: March 14, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Jongwon Lim, Vladimir Simov, Brandon A. Vara, Charles S. Yeung, Sebastian E. Schneider, Erin F. DiMauro
  • MODIFIED ISOINDOLINONES AS GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
    Publication number: 20240076291
    Abstract: The present invention relates to compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula (I), and methods of using the compounds of Formula (I) for treatment or prophylaxis of lysosomal storage diseases, neurodegenerative disease, cystic disease, cancer, or a diseases or disorders associated with elevated levels of glucosylceramide (GlcCer), glucosylsphingosine (GlcSph) and/or other glucosylceramide-based glycosphingolipids (GSLs).
    Type: Application
    Filed: November 18, 2021
    Publication date: March 7, 2024
    Applicant: MERCK SHARP & DOHME LLC
    Inventors: Michael J. Breslin, Mark E. Fraley, H. Marie Loughran, James J. Mulhearn, Anthony J. Roecker, Kathy M. Schirripa, Shawn J. Stachel
  • ADENOSINE A2A AND A2B RECEPTOR DUAL ANTAGONISTS FOR IMMUNO-ONCOLOGY
    Publication number: 20240076297
    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 22, 2021
    Publication date: March 7, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Amjad Ali, Jared N. Cumming, Manuel De Lera Ruiz, Duane DeMong, Thomas H. Graham, Elisabeth T. Hennessy, Joseph M. Kelly, Rongze Kuang, Michael Man-Chu Lo, Umar Faruk Mansoor, Jesus Moreno, Uma Swaminathan, Heping Wu, Yingchun Ye, Younong Yu
  • S-METHYLTHIORIBOSE KINASE POLYPEPTIDES AND PROCESSES FOR MAKING AND USING S-METHYLTHIORIBOSE KINASE POLYPEPTIDES
    Publication number: 20240076703
    Abstract: The present disclosure provides MTR kinase polypeptides having improved properties as compared to a naturally occurring wild-type MTR kinase polypeptide including the capability of phosphorylating D-ribose and 5?-D-isobutyrylribose to give alpha-D-ribose-1-phosphate and alpha 5?-D-isobutyrylribose-1-phosphate. Also provided are polynucleotides encoding the MTR kinase polypeptides, host cells capable of expressing the MTR kinase polypeptides, and methods of using the MTR kinase polypeptides to synthesize alpha-D-ribose-1-phosphate and alpha 5?-D-isobutyrylribose-1-phosphate.
    Type: Application
    Filed: December 9, 2021
    Publication date: March 7, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Tamas Benkovics, Hsing-I Ho, John McIntosh, Grant S. Murphy, Weilan Pan, Deeptak Verma, Hao Yang
  • Combination of a PD-1 antagonist and CpG-C type oligonucleotide for treating cancer
    Patent number: 11918648
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a Toll-like receptor 9 (TLR9) agonist that is a CpG-C type oligonucleotide, and the use of the combination therapies for the treatment of cancer.
    Type: Grant
    Filed: August 21, 2020
    Date of Patent: March 5, 2024
    Assignees: MERCK SHARP & DOHME LLC, TRISALUS LIFE SCIENCES, INC.
    Inventors: Ying Yu, Andrew Evan Denker, Svetlana Sadekova, Uyen Truong Phan, Robert A. Kastelein, David Ross Kaufman, Robert L. Coffman, Cristiana Guiducci, Robert S. Janssen
  • Pro drugs of PDE10 compounds
    Patent number: 11919894
    Abstract: The present invention is directed to pro drugs of 2-methyl-N-((5-methyl-1,3,4-thiadiazol-2-yl)methyl)-6-(((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methoxy)pyrimidin-4-amine which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: March 15, 2022
    Date of Patent: March 5, 2024
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Sachin Mittal, Jason W. Skudlarek, Izzat T. Raheem
  • AMIDO-SUBSTITUTED PYRIDYL COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HERPESVIRUSES
    Publication number: 20240067657
    Abstract: The present invention relates to novel Amido-Substituted Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R7, and R8 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Heterocycle Compound, and methods of using the Amido-Substituted Heterocycle Compounds for treating or preventing a herpesvirus infection in a patient.
    Type: Application
    Filed: December 21, 2021
    Publication date: February 29, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Kira A. Armacost, Richard Thaddeus Berger, Jr., Andrew J. Cooke, Christopher Douglas Cox, Brendan M. Crowley, Marc Labroli, Michael Aaron Plotkin, Izzat Tiedje Raheem, Anthony W. Shaw, Kelly-Ann S. Schlegel, Jason W. Skudlarek, Ling Tong
  • FUSED BICYCLIC PYRAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF HERPESVIRUSES
    Publication number: 20240059693
    Abstract: The present invention relates to novel Fused Bicyclic Pyrazole Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. The present invention also relates to compositions comprising at least one Fused Bicyclic Pyrazole Derivative, and methods of using the Fused Bicyclic Pyrazole Derivatives for treating or preventing a herpesvirus infection in a patient.
    Type: Application
    Filed: December 14, 2021
    Publication date: February 22, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Ronald K. Chang, Andrew J. Cooke, JR., Christopher Douglas Cox, Marc Labroli, Izzat Tiedje Raheem, Jack D. Scott, Jeffrey W. Schubert, Jason W. Skudlarek, Zheng Tan, Ling Tong
  • NOVEL DIACYLGLYCERIDE O-ACYLTRANSFERASE 2 INHIBITORS
    Publication number: 20240059700
    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: Application
    Filed: September 12, 2023
    Publication date: February 22, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Yeon-Hee Lim, Jianming Bao, Faben A. Cruz, Fa-Xiang Ding, Cedric Lorenz Hugelshofer, Victor W. Mak, James Patrick Roane, Jillian R. Sanzone, Samantha E. Shockley, Rose Yen
  • FUSED [7,5] BICYCLIC PYRAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF HERPESVIRUSES
    Publication number: 20240051963
    Abstract: The present invention relates to novel Fused [7,5] Bicyclic Pyrazole Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, and R4 are as defined herein. The present invention also relates to compositions comprising at least one Fused [7,5] Bicyclic Pyrazole Derivative, and methods of using the Fused [7,5] Bicyclic Pyrazole Derivatives for treating or preventing a herpesvirus infection in a patient.
    Type: Application
    Filed: December 9, 2021
    Publication date: February 15, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Andrew J. Cooke, JR., Jeffrey W. Schubert, Jason W. Skudlarek
  • LIPID NANOPARTICLE COMPOSITIONS CONTAINING MONOESTER CATIONIC LIPIDS
    Publication number: 20240050378
    Abstract: The present disclosure provides, among other things, lipid nanoparticle formulations that include monoester cationic lipids. The present invention also provides compositions that include monoester cationic lipid nanoparticles and nucleic acids. The present disclosure also provides lipid nanoparticles encapsulating agents. The present disclosure further provides methods of producing lipid nanoparticles with encapsulated nucleic acids.
    Type: Application
    Filed: December 1, 2021
    Publication date: February 15, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Marian E. Gindy, Andrew Bett, Izzat Tiedje Raheem, Ronald M. Kim
  • FORMULATIONS OF ANTI-LAG3 ANTIBODIES AND CO-FORMULATIONS OF ANTI-LAG3 ANTIBODIES AND ANTI-PD-1 ANTIBODIES
    Publication number: 20240052036
    Abstract: The present invention provides formulations of anti-LAG3 antibodies, and co-formulations of anti-PD-1 antibodies and anti-LAG3 antibodies, and their use in treating various disorders.
    Type: Application
    Filed: October 12, 2023
    Publication date: February 15, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Preeti G. Desai, Shuai Shi, Valentyn Antochshuk, Rubi Burlage, Smita Raghava