Patents Assigned to Merck Sharp and Dohme Corp.
  • BICYCLOHEPTANE PYRROLIDINE OREXIN RECEPTOR AGONISTS
    Publication number: 20220056017
    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: Application
    Filed: August 16, 2021
    Publication date: February 24, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Stephane L. BOGEN, Dane James CLAUSEN, Deodial Guy GUIADEEN, Jinsong HAO, Shishi LIN, Michael T. RUDD, Lan WEI, Li XIAO, Dexi YANG
  • ARGINASE INHIBITORS AND METHODS OF USE
    Publication number: 20220056051
    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: Application
    Filed: December 13, 2019
    Publication date: February 24, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Abdelghani Abe Achab, Matthew L. Childers, Jared N. Cumming, Symon Gathiaka, Charles A. Lesburg, Derun Li, Min Lu, Matthew J. Mitcheltree, Anandan Palani, Rachel L. Palte, Hongjun Zhang
  • SUBSTITUTED AMINO TRIAZOLOPYRIMIDINE AND AMINO TRIAZOLOPYRAZINE ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE
    Publication number: 20220040184
    Abstract: In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): and, and pharmaceutically acceptable salts thereof, wherein, R1, n, R2, and R3 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 their use 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: November 15, 2019
    Publication date: February 10, 2022
    Applicant: Merck Sharp Dohme Corp.
    Inventors: Zachary G. Brill, Amjad Ali, Jared Cumming, Duane DeMong, Qiaolin Deng, Gioconda V. Gallo-Etienne, Thomas H. Graham, Rongze Kuang, Matthew A. Larsen, Yeon-Hee Lim, Kun Liu, Umar Faruk Mansoor, Jesus Moreno, Brandon A. Vara, Huijun Wang, Yonglian Zhang
  • PD1 AND/OR LAG3 BINDERS
    Publication number: 20220041727
    Abstract: The present invention provides molecules, such as ISVDs and Nanobodies, that bind to PD1 and LAG3 and, optionally to human serum albumin. These molecules have been engineered so as to reduce the incidence of binding by pre-existing antibodies in the bodies of a subject administered such a molecule. Methods for increasing immune response, treating cancer and/or treating an infectious disease with such molecules are provided.
    Type: Application
    Filed: October 8, 2021
    Publication date: February 10, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Edward Bowman, Maribel Beaumont, Marie-Ange Buyse, Carlo Boutton, Bruno Dombrecht, Robert A. Kastelein, David Vlerick
  • ANTIBODIES SPECIFIC FOR IMMUNOGLOBULIN-LIKE TRANSCRIPT 3 (ILT3) AND USES THEREOF
    Publication number: 20220033497
    Abstract: Humanized, non-promiscuous monoclonal antibodies specific for immunoglobulin-like transcript 3 (ILT3), also known as Leukocyte immunoglobulin-like receptor subfamily B member 4 (LILRB4), are described.
    Type: Application
    Filed: July 16, 2021
    Publication date: February 3, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael A. Meehl, Philip E. Brandish, Laurence Fayadat-Dilman, Veronica Juan, Carl Mieczkowski, Latika Singh
  • Cyclic Di-Nucleotide Compounds as STING Agonists
    Publication number: 20220033431
    Abstract: A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2a, R3, R3a, 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: Application
    Filed: December 2, 2019
    Publication date: February 3, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Wonsuk Chang, Jared N. Cumming, Hong Liu, Benjamin Wesley Trotter
  • Cyclic Di-Nucleotide Compounds as STING Agonists
    Publication number: 20220033435
    Abstract: A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, R4, R5, R5a, 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 (I).
    Type: Application
    Filed: December 2, 2019
    Publication date: February 3, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Wonsuk Chang, Jared N. Cumming, Hong Liu, Benjamin Wesley Trotter
  • ANTI-ILT4 ANTIBODIES AND ANTIGEN-BINDING FRAGMENTS
    Publication number: 20220033496
    Abstract: The present invention provides antibodies and antigen-binding fragments thereof that bind to ILT4 (immunoglobulin-like transcript 4) and combinations thereof, e.g., with an anti-PD1 antibody. Also provided are methods of use thereof, for example, for treating or preventing cancer in a subject; and methods of making such antibodies and fragments.
    Type: Application
    Filed: June 3, 2021
    Publication date: February 3, 2022
    Applicants: Merck Sharp & Dohme Corp., Agenus Inc.
    Inventors: Milan BLANUSA, Barbara JOYCE-SHAIKH, Andrea Claudia SCHUSTER, Kornelia SCHULTZE, Luis A. ZUNIGA
  • EXPRESSION VECTORS FOR EUKARYOTIC EXPRESSION SYSTEMS
    Publication number: 20220033845
    Abstract: The invention provides expression vectors for expressing recombinant proteins (e.g., biologics) in mammalian cells. Also provided are host cells comprising the expression vectors, methods of producing the recombinant proteins, and methods of propagating the expression vectors.
    Type: Application
    Filed: September 23, 2019
    Publication date: February 3, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Zhimei Du, Bo Jiang, Xiaoyan Tang
  • METHOD FOR IDENTIFYING HIGH AFFINITY MONOCLONAL ANTIBODY HEAVY AND LIGHT CHAIN PAIRS FROM HIGH THROUGHPUT SCREENS OF B-CELL AND HYBRIDOMA LIBRARIES
    Publication number: 20220034902
    Abstract: A method is described for identifying high affinity monoclonal antibody heavy and light chain pairs from high throughput screens of antibody producing cell libraries such as B-cell and hybridoma libraries. Specifically, the method relates to application of reversed immunocapture and high resolution tandem mass spectrometry for the identification of heavy and light chain pairs of binding antibodies obtained from high throughput screens of antibody producing cell libraries.
    Type: Application
    Filed: December 6, 2019
    Publication date: February 3, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Eberhard Durr, Yaping Liu, Zhifeng Chen, Arthur Fridman
  • PNEUMOCOCCAL CONJUGATE VACCINE FORMULATIONS
    Publication number: 20220031837
    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: August 26, 2021
    Publication date: February 3, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: William J. Smith, Cecilia Giovarelli, Denise K. Nawrocki
  • COMBINATION OF A PD-1 ANTAGONIST AND A VEGFR/FGFR/RET TYROSINE KINASE INHIBITOR FOR TREATING CANCER
    Publication number: 20220023285
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a multi-RTK inhibitor, and the use of the combination therapies for the treatment of cancer. The multi-RTK inhibitor may be represented by Formula (I): wherein R1 is C1-6 alkyl or C3-8 cycloalkyl, R2 is a hydrogen atom or C1-6 alkoxy, and R3 is a hydrogen atom or a halogen atom. A tumor therapeutic agent is disclosed that combines a compound or pharmaceutically acceptable salt thereof represented by Formula I and an anti-PD-1 antibody.
    Type: Application
    Filed: October 15, 2021
    Publication date: January 27, 2022
    Applicants: MERCK SHARP & DOHME CORP., EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Andrew Evan DENKER, Yu KATO, Kimiyo TABATA, Yusaku HORI
  • ANTIBODIES SPECIFIC FOR IMMUNOGLOBULIN-LIKE TRANSCRIPT 3 (ILT3) AND USES THEREOF
    Publication number: 20220025043
    Abstract: Humanized, non-promiscuous monoclonal antibodies specific for immunoglobulin-like transcript 3 (ILT3), also known as Leukocyte immunoglobulin-like receptor subfamily B member 4 (LILRB4), are described.
    Type: Application
    Filed: July 16, 2021
    Publication date: January 27, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael A. Meehl, Philip E. Brandish, Laurence Fayadat-Dilman, Veronica Juan, Carl Mieczkowski, Latika Singh
  • Cyclic Di-Nucleotide Compounds as STING Agonists
    Publication number: 20220024964
    Abstract: A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2a, R3, R3a, R4, R5, R5a, 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 (I).
    Type: Application
    Filed: December 2, 2019
    Publication date: January 27, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Wonsuk Chang, Jared N. Cumming, Hong Liu, Benjamin Wesley Trotter
  • ANTIBODIES SPECIFIC FOR IMMUNOGLOBULIN-LIKE TRANSCRIPT 3 (ILT3) AND USES THEREOF
    Publication number: 20220025042
    Abstract: Humanized, non-promiscuous monoclonal antibodies specific for immunoglobulin-like transcript 3 (ILT3), also known as Leukocyte immunoglobulin-like receptor subfamily B member 4 (LILRB4), are described.
    Type: Application
    Filed: July 16, 2021
    Publication date: January 27, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael A. Meehl, Philip E. Brandish, Laurence Fayadat-Dilman, Veronica Juan, Carl Mieczkowski, Latika Singh
  • CELL-BASED BIOIDENTITY TEST FOR INSULIN
    Publication number: 20220026414
    Abstract: A functional cell-based assay for use as a bioidentity assay for insulin or insulin analogs is described. The assay may be used as a replacement of the rabbit blood sugar method disclosed in USP<121> Insulin Assays.
    Type: Application
    Filed: December 6, 2019
    Publication date: January 27, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Junming Yie
  • 6,5-fused heteroaryl piperidine ether allosteric modulators of the M4 muscarinic acetylcholine receptor
    Patent number: 11230556
    Abstract: The present invention is directed to 6,5-fused heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. 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 M4 muscarinic acetylcholine 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 M4 muscarinic acetylcholine receptors are involved.
    Type: Grant
    Filed: December 18, 2017
    Date of Patent: January 25, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xiaolei Gao, Sandra L. Knowles, Chunsing Li, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Debra L. Ondeyka
  • Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections
    Patent number: 11230543
    Abstract: The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A1, Q, A2, M, W, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention 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 the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.
    Type: Grant
    Filed: June 25, 2020
    Date of Patent: January 25, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Weiguo Liu, Fa-Xiang Ding, Wanying Sun, Yi Zang, Weidong Pan, Anthony Ogawa, Linda Brockunier, Xianhai Huang, Hongwu Wang, Rudrajit Mal, Tesfaye Biftu, Min Park, Yan Guo, Jinlong Jiang, Helen Y. Chen, Christopher W. Plummer
  • Progressively-trained scale-invariant and boundary-aware deep neural network for the automatic 3D segmentation of lung lesions
    Patent number: 11232572
    Abstract: A system and method are disclosed for segmenting a set of two-dimensional CT slices corresponding to a lesion. In an embodiment, for each of at least a subset of the set of CT slices, the system inputs the CT slice into a plurality of branches of a trained segmentation block. Each branch of the segmentation block includes a convolutional neural network (CNN) with filters at a different scale, and produces one or more levels of output. The system generates, for each CT slice in the subset, feature maps for each level of output. The system generates a segmentation of each CT slice in the subset based on the feature maps of each level of output. The system aggregates the segmentations of each slice in the subset to generate a three-dimensional segmentation of the lesion. The system transmits data representing the three-dimensional segmentation to a user interface for display.
    Type: Grant
    Filed: April 14, 2020
    Date of Patent: January 25, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Antong Chen, Gregory Goldmacher, Bo Zhou
  • Purine inhibitors of human phosphatidylinositol 3-kinase delta
    Patent number: 11230547
    Abstract: The instant invention provides compounds of formulas Ia and Ib which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Grant
    Filed: December 12, 2018
    Date of Patent: January 25, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Meredeth A. McGowan, Jason D. Katz, Matthew Christopher, Hua Zhou, David James Witter, Chaomin Li, John Lampe, Joey L. Methot, Abdelghani A. Achab, Xavier Fradera, Shimin Xu