Patents Assigned to Merck Sharp & Dohme LLC
  • CYCLOPENTAPYRROLE OREXIN RECEPTOR AGONISTS
    Publication number: 20230257348
    Abstract: The present invention is directed to cyclopentapyrrole, furopyrrole and azabicycloheptane 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: August 16, 2021
    Publication date: August 17, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Stephane L. Bogen, Dane James Clausen, Michael T. Rudd, Dong Xiao, Dexi Yang
  • METHODS FOR TREATING CANCER OR VON-HIPPEL LINDAU DISEASE USING A COMBINATION OF A PD-1 ANTAGONIST, A HIF-2 ALPHA INHIBITOR, AND LENVATINIB OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
    Publication number: 20230250182
    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 PD-1 antagonist; (b) a HIF-2? inhibitor; and (c) 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.
    Type: Application
    Filed: June 21, 2021
    Publication date: August 10, 2023
    Applicants: Merck Sharp & Dohme LLC, Eisai R&D Management Co., Ltd.
    Inventors: Rodolfo Fleury Perini, Elaine M. Pinheiro, Jacqueline Willemann-Rogerio
  • ADJUVANTED VACCINES
    Publication number: 20230234850
    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: July 27, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Akhilesh Bhambhani, Muneeswara Babu Medi, Maya Salnikova, William James Smith, David S. Thiriot
  • 5-OXOPYRROLIDINE-3-CARBOXAMIDES AS NAV1.8 INHIBITORS
    Publication number: 20230227405
    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: June 14, 2021
    Publication date: July 20, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Ashok Arasappan, Ian M. Bell, Jason Michael Cox, Michael J. Kelly, III, Mark E. Layton, Hong Liu, Jian Liu, Akshay A. Shah, Michael David VanHeyst
  • 2-OXO-OXAZOLIDINE-5-CARBOXAMIDES AS NAV1.8 INHIBITORS
    Publication number: 20230227441
    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: June 14, 2021
    Publication date: July 20, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Ashok Arasappan, Ian M. Bell, Christopher James Bungard, Christopher S. Burgey, Jason Michael Cox, Deodial Guy Guiadeen, III, Michael J. Kelly, III, Mark E. Layton, Hong Liu, Jian Liu, James T. Olsen, James J. Perkins, Jeffrey W. Schubert, Akshay A. Shah, Shawn J. Stachel, Michael David VanHeyst, Zhe Wu
  • High affinity antibodies targeting tau phosphorylated at serine 413
    Patent number: 11702467
    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: Grant
    Filed: June 23, 2021
    Date of Patent: July 18, 2023
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Jeanne E. Baker, Sophie Parmentier Batteur, Ming-Tang Chen, Alan C. Cheng, Chung-Ming Hsieh, Carl Mieczkowski, Sokreine Suon
  • Aza-benzothiophene compounds as STING agonists
    Patent number: 11702430
    Abstract: Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R5, R6, R8, R9, A, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.
    Type: Grant
    Filed: March 28, 2019
    Date of Patent: July 18, 2023
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Michael D. Altman, Brandon D. Cash, Jared N. Cumming, Duane E. DeMong, Andrew M. Haidle, James P. Jewell, Matthew A. Larsen, Min Lu, Ryan D. Otte, Brandon M. Taoka, Benjamin Wesley Trotter, Quang T. Truong
  • 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
  • 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
  • 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
  • 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
  • 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