Patents Assigned to Merck Sharp & Dohme LLC
  • Arginase inhibitors and methods of use
    Patent number: 12215116
    Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
    Type: Grant
    Filed: March 8, 2019
    Date of Patent: February 4, 2025
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Abdelghani Abe Achab, Matthew L. Childers, Jared N. Cumming, Christian Fischer, Symon Gathiaka, Hakan Gunaydin, Charles A. Lesburg, Derun Li, Min Lu, Anandan Palani, Rachel L. Palte, Qinglin Pu, David L. Sloman, Sung-Sau So, Chunrui Sun, Hongjun Zhang
  • C-TERMINAL EXTENDED P53 ACTIVATOR CROSSLINKED PEPTIDOMIMETIC MACROCYCLES AGAINST MDM2/MDMX
    Publication number: 20250034211
    Abstract: The crosslinked peptidomimetic macrocycles disclosed herein comprise an alkene or alkyne staple and a poly-amino acid C-terminal tail. These crosslinked peptidomimetic macrocycles have improved binding to MDM2 and MDMX (aka MDM4), are protease resistant, cell permeable without inducing membrane disruption, and intracellularly activate p53 by binding MDM2 and MDMX thereby antagonizing MDM2 and MDMX binding to p53. These peptidomimetic macrocycles may be useful in anticancer therapies, particularly in combination with chemotherapy or radiation therapy.
    Type: Application
    Filed: November 23, 2022
    Publication date: January 30, 2025
    Applicants: Merck Sharp & Dohme LLC, MSD International GmbH, Agency for Science, Technology and Research
    Inventors: Hubert Josien, Arun Chandramohan, Charles William Johannes, Christopher J. Brown, Srinivasaraghavan Kannan, Anthony William Partridge, Chandra Shekhar Verma, Lin Yan, Tsz Ying Yuen
  • BLOCKING AND NON-BLOCKING SINGLE DOMAIN ANTIBODIES AND USES THEREOF
    Publication number: 20250034258
    Abstract: The invention relates, in part, to single domain antibody constructs. In particular, the invention relates, in part, to single domain antibody constructs that include a non-blocking ?-PDL1 VHH that would provide minimal disruption of the PD-1/?PD-L1 binding interaction. The invention further relates to a method for detecting cell-cell interactions using the VHH sequences provided herein.
    Type: Application
    Filed: December 1, 2022
    Publication date: January 30, 2025
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Edward P. Bowman, Olugbeminiyi O. Fadeyi, Rob C. Oslund
  • Formulations of dengue virus vaccine compositions
    Patent number: 12208135
    Abstract: The present invention relates to formulations of dengue virus vaccine comprising at least one live, attenuated dengue virus or live, attenuated chimeric flavivirus, a buffer, a sugar, a cellulose derivative, a glycol or sugar alcohol, optionally an alkali or alkaline salt and an amino acid; and formulations of dengue virus vaccine comprising at least one live, attenuated dengue virus or live, attenuated chimeric flavivirus, a buffer, a sugar of at least 150 mg/ml, a carrier, and optionally an alkali or alkaline salt and an amino acid.
    Type: Grant
    Filed: December 6, 2023
    Date of Patent: January 28, 2025
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Michael S. Ryan, Sherrie-Ann P. Martin, Morrisa Jones, Justin Stanbro, Akhilesh Bhambhani, Jeffrey Thomas Blue, Heidi Joanne Pixley, Erin J. Green-Trexler, Lynne Ann Isopi
  • FUSED PYRAZOLE UREA ANALOGS AS GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
    Publication number: 20250026762
    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 28, 2022
    Publication date: January 23, 2025
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Mark E. Fraley, Tao Liang, H. Marie Loughran, Anthony J. Roecker, Kathy M. Schirripa, Ling Tong, Ashwin U. Rao
  • TETRAHYDROQUINAZOLINE DERIVATIVES AS SELECTIVE CYTOTOXIC AGENTS
    Publication number: 20250026759
    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: July 5, 2024
    Publication date: January 23, 2025
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Michael J. Breslin, Antonella Converso, Abdellatif El Marrouni, Ashley Forster, David N. Hunter, Anthony W. Shaw, William D. Shipe, Yunlong Zhang
  • CHROMANE AMIDINE MONOBACTAM ANTIBIOTICS
    Publication number: 20250019376
    Abstract: The present invention relates to monobactam compounds of Formula I: The present invention also relates to pharmaceutical compositions comprising a monobactam compound of structural formula I or a pharmaceutically acceptable salt thereof. The invention further relates to the compounds of formula (I) for use in methods for treating a bacterial infection, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic. The present invention discloses the synthesis and characterisation of exemplary compounds as well as biological assays thereof. An exemplary compound is e.g.
    Type: Application
    Filed: November 16, 2022
    Publication date: January 16, 2025
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Helen Y. Chen, Shuzhi Dong, Zhiyong Hu, Jing Su, Tao Yu, Yong Zhang
  • 2-amino-N-heteroaryl-nicotinamides as Na1.8 inhibitors
    Patent number: 12195445
    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: May 24, 2022
    Date of Patent: January 14, 2025
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Ashok Arasappan, Ian M. Bell, Michael J. Breslin, Christopher James Bungard, Christopher S. Burgey, Harry R. Chobanian, Jason M. Cox, Anthony T. Ginnetti, Deodial Guy Guiadeen, Kristen L. G. Jones, Mark E. Layton, Hong Liu, Jian Liu, James J. Perkins, Shawn J. Stachel, Linda M. Suen-Lai, Zhe Wu
  • SCALABLE CHROMATOGRAPHY PROCESS FOR PURIFICATION OF HUMAN CYTOMEGALOVIRUS
    Publication number: 20250011732
    Abstract: The present invention relates to a scalable process for the purification of human cytomegalovirus particles from cell culture medium. In particular, the process involves a two step chromatography process starting with an anion exchange chromatography step followed by a polishing chromatography step selected from mixed mode chromatography or cation exchange chromatography.
    Type: Application
    Filed: July 11, 2024
    Publication date: January 9, 2025
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Adam Kristopeit, Janelle Konietzko, Wanli MA, Katherine Phillips, Andrew Swartz, Sheng-Ching Wang, Marc D. Wenger, Matthew Woodling, Tiago Matos
  • METHODS FOR TREATING CANCER USING A COMBINATION OF A PD-1 ANTAGONIST, AN ILT4 ANTAGONIST, AND CHEMOTHERAPEUTIC AGENTS
    Publication number: 20250011453
    Abstract: Provided herein are methods of treating cancer (e.g., ovarian, mesothelioma, triple-negative breast cancer), which comprise administering to a human patient in need thereof: (a) a PD-1 antagonist; (b) an ILT4 antagonist; and (c) one or more chemotherapeutic agents. Also provided are pharmaceutical compositions and kits containing such agents for the treatment of cancer.
    Type: Application
    Filed: July 18, 2022
    Publication date: January 9, 2025
    Applicant: Merck Sharp & Dohme LLC
    Inventor: Rachel A. Altura
  • FORMULATIONS OF ANTIVIRAL COMPOUNDS
    Publication number: 20250009751
    Abstract: The present disclosure is directed to pharmaceutical formulations comprising an amorphous inhibitor of hepatitis C virus NS5A. These pharmaceutical formulations may be prepared by roller-compaction or wet-granulation methods. The present disclosure is also directed to oral dosage forms, such as tablets, comprising such pharmaceutical formulations.
    Type: Application
    Filed: September 23, 2024
    Publication date: January 9, 2025
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Sutthilug Sotthivirat, Joyce Stellabott, Walter R. Wasylaschuk
  • COMBINATION THERAPIES FOR THE TREATMENT OF NON-SMALL CELL LUNG CANCER
    Publication number: 20250000994
    Abstract: The present disclosure relates to methods of treating a cellular proliferative disorder (e.g., cancer) comprising administering: (a) an anti-human PD-1 antibody or antigen binding fragment thereof; and (b) an Immunoconjugate of Formula (I): wherein: Ab is an antibody that binds to Trop-2; and n is an integer from 1 to 10. Also disclosed are therapeutic combinations and kits containing such agents for the treatment of cancers.
    Type: Application
    Filed: December 7, 2023
    Publication date: January 2, 2025
    Applicants: Merck Sharp & Dohme LLC, Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.
    Inventors: Junyou Ge, Xiaoping Jin, Yina Diao, Yalan Yang, Yujie Fu, Dian Jing, Hongbo Zhong, Omobolaji Akala, Elliot Keith Chartash, Maria Catherine Pietanza, Bin Zhao
  • COMBINATION THERAPIES FOR THE TREATMENT OF CANCER
    Publication number: 20250000990
    Abstract: The present disclosure relates to methods of treating a cellular proliferative disorder (e.g., cancer) comprising administering: (a) an anti-human PD-1 antibody or antigen binding fragment thereof; and (b) an Immunoconjugate of Formula (I): wherein: Ab is an antibody that binds to Trop-2; and n is an integer from 1 to 10. Also disclosed are therapeutic combinations and kits containing such agents for the treatment of cancers.
    Type: Application
    Filed: December 7, 2023
    Publication date: January 2, 2025
    Applicants: Merck Sharp & Dohme LLC, Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.
    Inventors: Junyou Ge, Xiaoping Jin, Yina Diao, Jiacheng Yang, Yujie Fu, Zhijiao Qiao, Lihua Chen, Omobolaji Akala, Elliot Keith Chartash, Sarper Toker, Christian H. Poehlein, Blanca Homet Moreno
  • AMPOULE FOR ORAL VACCINE ADMINISTRATION AND METHODS OF USE
    Publication number: 20250000744
    Abstract: An ampoule includes a body having a cavity for storing a medicament, a neck coupled to the body and defining a nozzle in communication with the cavity of the body, a removable cap coupled to the nozzle, and an anti-choking miter coupled to the removable cap, the anti-chocking miter being wider than the removable cap.
    Type: Application
    Filed: November 11, 2022
    Publication date: January 2, 2025
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Ramprasad B. Halthore, Atul Karande, Derrick M. Smith
  • Spirotricycle RIPK1 inhibitors and methods of uses thereof
    Patent number: 12180226
    Abstract: Described herein are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein A, R1, R2, R3, W, X, Y, Z, m, n and p are as defined herein. 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: Grant
    Filed: October 25, 2022
    Date of Patent: December 31, 2024
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Abdelghani Abe Achab, Zachary G. Brill, Jenny Lorena Rico Duque, Xavier Fradera, Joey L. Methot, Phieng Siliphaivanh, Jing Su, Brandon A. Vara, Erin F. DiMauro
  • GLUCOSE-RESPONSIVE INSULIN CONJUGATES COMPRISING A TETRA-VALENT SUGAR CLUSTER FOR TREATMENT OF DIABETES
    Publication number: 20240424109
    Abstract: An insulin conjugate comprising or consisting of a tetra-valent sugar cluster is described. The tetra-valent sugar cluster is provided by tetra-dentate linker having four arms, wherein each arm of the tetra-dentate linker is independently covalently linked to a ligand comprising or consisting of a saccharide, such as a monosaccharide, disaccharide, trisaccharide, tetrasaccharide, or branched trisaccharide. In particular aspects, the insulin conjugate displays a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose.
    Type: Application
    Filed: November 16, 2022
    Publication date: December 26, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Pei Huo, Songnian Lin, Christopher R. Moyes, Dmitri A. Pissarnitski, Zhiqiang Zhao, David N. Hunter, Yuping Zhu
  • COMPOSITIONS OF PROGRAMMED DEATH RECEPTOR 1 (PD-1) ANTIBODIES AND METHODS OF OBTAINING THE COMPOSITIONS THEREOF
    Publication number: 20240425596
    Abstract: The invention provides compositions of anti-PD-1 antibodies or antigen-binding fragments thereof with less than or equal to about 3.0% oxidation of Met105 in the CDRH3 heavy chain region, and methods of obtaining the purified compositions. The invention also provides compositions comprising anti-PD-1 antibody main species and acidic species thereof, wherein the amount of acidic species is about 1.0-12.0%.
    Type: Application
    Filed: September 6, 2024
    Publication date: December 26, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Mark A. Brower, Chung-Jr Huang, Brian Wai Kwan, William Nicholas Napoli, Bhumit A. Patel, Nuno J. Dos Santos Pinto, Douglas Dennis Richardson, II, Sen Xu
  • VIAL-TO-SYRINGE CONVERTER AND METHODS OF MAKING AND USING SAME
    Publication number: 20240424218
    Abstract: In some examples, a vial-to-syringe converter includes a plunger rod, an adapter including a body having a piercing spike, a receiver and a lumen extending between the spike and the receiver, the body further including at least one laterally-extending flange, and a needle in communication with the receiver and configured to deliver a medicament to a patient's body.
    Type: Application
    Filed: November 1, 2022
    Publication date: December 26, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Daniel A. Bonanno, Eduardo Cristofolli, Cassie Megna, Wail A. Rasheed, Ophelia L. Wells
  • SPIROTRICYCLE RIPK1 INHIBITORS AND METHODS OF USES THEREOF
    Publication number: 20240425524
    Abstract: Described herein are compounds of Formula I; and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, m, n, and p are as defined herein. The compounds of Formula I, and pharmaceutically acceptable salts thereof, act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.
    Type: Application
    Filed: October 24, 2022
    Publication date: December 26, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Abdelghani Abe Achab, Jenny Lorena Rico Duque, Xavier Fradera, Joey L. Methot, Phieng Siliphaivanh, Brandon A. Vara, Hongjun Zhang
  • PRMT5 inhibitors
    Patent number: 12173026
    Abstract: The present invention provides a compound of Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 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 cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
    Type: Grant
    Filed: August 5, 2019
    Date of Patent: December 24, 2024
    Assignees: Merck Sharp & Dohme LLC, MSD International GmbH
    Inventors: Michelle Machacek, David Witter, Craig Gibeau, Chunhui Huang, Shuhei Kawamura, David L. Sloman, Phieng Siliphaivanh, Ryan Quiroz, Murray Wan, Sebastian Schneider, Charles S. Yeung, Michael H. Reutershan, Timothy J. Henderson, Jean-Laurent Paparin, Houcine Rahali, Jonathan M. E. Hughes, Sulagna Sanyal, Yingchun Ye, David A. Candito, Patrick S. Fier, Steven M. Silverman