Patents Assigned to Merck Sharp & Dohme LLC
  • 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
  • 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
  • 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
  • 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
  • ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20250002448
    Abstract: The present disclosure relates to compounds of formula (I) that are useful as modulators of a7 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: Application
    Filed: September 19, 2022
    Publication date: January 2, 2025
    Applicant: MERCK SHARP & DOHME LLC
    Inventors: Ian M. Bell, Brendan M. Crowley, James Fells, Patrick Bazzini, Jean-Marie Contreras, Fabrice Garrido, Belinda C. Huff, Christophe Joseph, Christophe Morice, Dharam Paul, Aurelie Witzel
  • 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
  • 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
  • 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
  • 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
  • PCSK9 antagonist compounds
    Patent number: 12178842
    Abstract: Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof: where A, X, R1, and R2 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
    Type: Grant
    Filed: October 31, 2022
    Date of Patent: December 31, 2024
    Assignee: MERCK SHARP & DOHME LLC
    Inventors: Hubert Josien, Abbas Walji, Harold B. Wood, Fa-Xiang Ding, Jian Liu, Thomas Joseph Tucker, Michael Man-Chu Lo, Liangqin Guo
  • Process for preparing beta 3 agonists and intermediates
    Patent number: 12180219
    Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.
    Type: Grant
    Filed: April 29, 2024
    Date of Patent: December 31, 2024
    Assignee: MERCK SHARP & DOHME LLC
    Inventors: Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
  • 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
  • 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
  • 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
  • 3D segmentation of lesions in CT images using self-supervised pretraining with augmentation
    Patent number: 12175679
    Abstract: A method or system for training a convolutional neural network (CNN) for medical imaging analysis. The system pre-trains the CNN's encoder using a dataset of unlabeled 3D medical images. Each 3D image includes an annotated slice delineating a boundary of a lesion and multiple non-annotated 2D slices above and below the annotated slice. The system then fine-tunes the pre-trained encoder using an annotated 2D image dataset. The annotated 2D image dataset includes multiple 2D slices of lesions, each including an annotation that delineates a boundary of a corresponding lesion.
    Type: Grant
    Filed: November 28, 2023
    Date of Patent: December 24, 2024
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Yiqiao Liu, Antong Chen, Gregory Goldmacher