Patents Assigned to Merck Sharp & Dohme
  • PYRAZOLO[4,3-d]PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF CELLULAR PROLIFERATIVE DISORDERS
    Publication number: 20230219962
    Abstract: The present invention relates to novel Pyrazolo[4,3 -d]Pyrimidine Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Pyrazolo[4,3-d]Pyrimidine Derivative, and methods of using the Pyrazolo[4,3-d]Pyrimidine Derivatives for treating or preventing a cellular proliferative disorder in a patient.
    Type: Application
    Filed: June 3, 2021
    Publication date: July 13, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Jianming Bao, Natalija Cernaka, Scott A. Hollingsworth, Madeleine Eileen Kieffer, Simon B. Lang, Akash M. Patel, W. Michael Seganish
  • Small molecule inhibitors of KRAS G12C mutant
    Patent number: 11697657
    Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
    Type: Grant
    Filed: October 27, 2020
    Date of Patent: July 11, 2023
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Indu Bharathan, Symon Gathiaka, Yongxin Han, Xiaoshen Ma, Ryan D. Otte, David L. Sloman, Thomas H. Graham, Timothy Henderson, Elisabeth Hennessy, Anandan Palani
  • ANTIBODY NEUTRALIZING HUMAN RESPIRATORY SYNCYTIAL VIRUS
    Publication number: 20230212269
    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: December 13, 2022
    Publication date: July 6, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Kalpit A. Vora, Kara S. Cox, Aimin Tang, Zhifeng Chen, Daniel DiStefano, Lan Zhang, Hua-Poo Su
  • METHODS FOR TREATING CANCER OR VON-HIPPEL LINDAU DISEASE USING A COMBINATION OF A HIF-2 ALPHA INHIBITOR AND LENVATINIB
    Publication number: 20230210838
    Abstract: Provided herein are methods of treating cancer (e.g., RCC) or von-Hippel Lindau disease, which comprise administering to a human patient in need thereof: (a) a HIF-2? inhibitor; and (b) lenvatinib, or a pharmaceutically acceptable salt thereof. Also provided are kits containing such agents and uses of therapeutic combinations of such agents for the treatment of cancer or von-Hippel Lindau disease.
    Type: Application
    Filed: June 21, 2021
    Publication date: July 6, 2023
    Applicants: Merck Sharp & Dohme LLC, Eisai R&D Management Co., Ltd.
    Inventors: Rodolfo Fleury Perini, Elaine M. Pinheiro, Jacqueline Willemann-Rogerio
  • PNEUMOCOCCAL CONJUGATE VACCINE FORMULATIONS
    Publication number: 20230201338
    Abstract: The present invention provides pneumococcal conjugate vaccine formulations comprising surfactant systems incorporating polysorbate 20 or a combination of a poloxamer and a polyol.
    Type: Application
    Filed: February 15, 2023
    Publication date: June 29, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: William J. Smith, Cecilia Giovarelli, Denise K. Nawrocki
  • Cyclic di-nucleotide compounds as sting agonists
    Patent number: 11685761
    Abstract: A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a, and R9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.
    Type: Grant
    Filed: December 17, 2018
    Date of Patent: June 27, 2023
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Brian M. Andresen, Frank Bennett, Wonsuk Chang, Matthew Lloyd Childers, Jared N. Cumming, Jongwon Lim, Min Lu, Benjamin Wesley Trotter, Wen-Lian Wu
  • ADJUVANTED VACCINES
    Publication number: 20230192489
    Abstract: Vaccine formulations are described comprising physically separated, lyophilized antigens and adjuvant components, which may be in lyoparticle form, as well as methods of using and making such formulations. Reconstituted formulations are also described.
    Type: Application
    Filed: February 22, 2023
    Publication date: June 22, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Akhilesh Bhambhani, Muneeswara Babu Medi, Maya Salnikova, William James Smith, David S. Thiriot
  • DOSING REGIMEN OF ANTI-CD27 ANTIBODIES FOR TREATMENT OF CANCER
    Publication number: 20230192876
    Abstract: The present invention relates to methods of treating cancer by administering an anti-CD27 antibody as a monotherapy or as a part of a combination thereof.
    Type: Application
    Filed: October 29, 2020
    Publication date: June 22, 2023
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Elliot K. Chartash, Amy M. Beebe, Jason K. Cheung, Konstantin Dobrenkov, Claire H. Li, Richard Wnek
  • Bicycloheptane pyrrolidine orexin receptor agonists
    Patent number: 11680060
    Abstract: The present invention is directed to bicyclo[4.1.0]heptane pyrrolidine 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: Grant
    Filed: August 16, 2021
    Date of Patent: June 20, 2023
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Stephane L. Bogen, Dane James Clausen, Deodial Guy Guiadeen, Jinsong Hao, Shishi Lin, Michael T. Rudd, Lan Wei, Li Xiao, Dexi Yang
  • IL4I1 INHIBITORS AND METHODS OF USE
    Publication number: 20230183214
    Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as IL4I1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for IL4I1-related diseases.
    Type: Application
    Filed: May 4, 2021
    Publication date: June 15, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Brandon D. CASH, Wenlang FU, George Madalin GIAMBASU, Andrew M. HAIDLE, Brett A. HOPKINS, Matthew A. LARSEN, Charles A. LESBURG, Ping LIU, Meredeth A. MCGOWAN, Qinglin PU, Sulagna SANYAL, Phieng SILIPHAIVANH, Catherine M. WHITE, Xin YAN
  • Niraparib compositions
    Patent number: 11673877
    Abstract: The present invention relates to compositions comprising the compound niraparib, in particular certain solid forms of niraparib.
    Type: Grant
    Filed: June 4, 2021
    Date of Patent: June 13, 2023
    Assignees: Tesaro, Inc., Merck Sharp & Dohme Corp.
    Inventors: George Wu, John Chaber, Arlene E. McKeown, Jennifer R. Foley
  • MOISTURE PROTECTION FEATURES FOR A BOTTLE FOR STORING SOLID PHARMACEUTICAL PRODUCTS AND METHODS OF MAKING SAME
    Publication number: 20230172805
    Abstract: A bottle for storing solid pharmaceutical products includes a substantially cylindrical body having a sidewall, a top and a base defining an interior chamber, a first opening disposed on the top of the body, the first opening providing communication to the interior chamber and being eccentric with respect to the central longitudinal axis of the body, and a second opening disposed adjacent the first opening, the second opening being smaller than the first opening.
    Type: Application
    Filed: March 25, 2021
    Publication date: June 8, 2023
    Applicant: MERCK SHARP & DOHME LLC
    Inventors: Wail A. RASHEED, Cassie R. MEGNA, Ophelia L. WELLS, John B. CLINE
  • NOVEL DIACYLGLYCERIDE O-ACYLTRANSFERASE 2 INHIBITORS
    Publication number: 20230174521
    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: May 13, 2021
    Publication date: June 8, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Yeon-Hee Lim, Jianming Bao, James Patrick Roane
  • REDUCTASE ENZYMES AND PROCESSES FOR MAKING AND USING REDUCTASE ENZYMES
    Publication number: 20230174992
    Abstract: The present disclosure provides ketoreductase enzymes having improved properties as compared to a naturally occurring wild-type ketoreductase enzyme including the capability of reducing N-(7-((2S,4R,5R)-4-fluoro-3,3-dihydroxy-5-(hydroxymethyl) tetrahydrofuran-2-yl)-4-oxo-4,7-dihydro-3H-pyrrolo[3,2-d]pyrimidin-2-yl)isobutyramide. Also provided are polynucleotides encoding the ketoreductase enzymes, host cells capable of expressing the ketoreductase enzymes, and methods of using the ketoreductase enzymes to synthesize N-(9-((2R,3S,4S,5R)-4-fluoro-3-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-6-oxo-6,9-dihydro-1H-purin-2-yl)isobutyramide.
    Type: Application
    Filed: May 20, 2021
    Publication date: June 8, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Tamas Benkovics, Karla M. Camacho Soto, John McIntosh, Jeffrey C. Moore, Weilan Pan, Deeptak Verma, Li Xiao
  • SYNTHESIS OF FLUORINATED NUCLEOTIDES
    Publication number: 20230174567
    Abstract: The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3?-fluoro-thio-guanosine monophosphate or 3?-F-thio-GMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
    Type: Application
    Filed: May 20, 2021
    Publication date: June 8, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Travis Armiger, Kevin M. Belyk, Tamas Benkovics, Cheol K. Chung, Yining Ji Chen, Heather Claire Johnson, Artis Klapars, Zhijian Liu, Zhuqing Liu, Jeffrey C. Moore, Andrew J. Neel, Feng Peng, Stephan M. Rummelt, Nastaran Salehi Marzuarani, Benjamin D. Sherry, Zhiguo Jake Song, Ben William Hulme Turnbull, Lu Wang, Feng Xu
  • FACTOR XI ACTIVATION INHIBITORS
    Publication number: 20230167085
    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 XI activation inhibitors.
    Type: Application
    Filed: May 7, 2021
    Publication date: June 1, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Jacqueline D. HICKS, John S. Debenham, Amjad Ali, Ying-Duo Gao, Lan Wei, Dexi Yang, Rongze Kuang, Alan Hruza, Peter Nizner, Daniel A. Tatosian
  • HIGH AFFINITY ANTIBODIES TARGETING TAU PHOSPHORYLATED AT SERINE 413
    Publication number: 20230167168
    Abstract: Provided herein are high affinity antibodies or antigen binding fragments thereof that specifically bind to human tau-pS413. Also provided are compositions, kits, methods, and uses involving such antibodies or antigen binding fragments thereof.
    Type: Application
    Filed: June 23, 2021
    Publication date: June 1, 2023
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jeanne E. Baker, Sophie Parmentier Batteur, Ming-Tang Chen, Alan C. Cheng, Chung-Ming Hsieh, Carl Mieczkowski, Sokreine Suon
  • Anti-coagulation factor XI antibodies
    Patent number: 11661460
    Abstract: Antibodies that bind the apple 3 domain of human coagulation Factor XI and inhibit activation of FXI by coagulation factor XIIa as well as activation of FIX by FXIa are described.
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: May 30, 2023
    Assignees: Merck Sharp & Dohme LLC, Adimab, LLC
    Inventors: Zhu Chen, Kenneth Ellsworth, James Milligan, Elizabeth Oldham, Dietmar Seiffert, Vaishnavi Ganti, Mohammad Tabrizifard, Bianka Prinz
  • SPIROTRICYCLE RIPK1 INHIBITORS AND METHODS OF USES THEREOF
    Publication number: 20230159558
    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: Application
    Filed: October 25, 2022
    Publication date: May 25, 2023
    Applicant: 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
  • CHROMANE AMIDINE MONOBACTAM COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
    Publication number: 20230159517
    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 therof, 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: Application
    Filed: November 16, 2022
    Publication date: May 25, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Helen Y. Chen, Shuzhi Dong, Zhiyong Hu, Jing Su, Tao Yu, Yong Zhang