Patents Assigned to Merck Sharp and Dohme Corp.
  • Publication number: 20210221815
    Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
    Type: Application
    Filed: January 22, 2021
    Publication date: July 22, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John Y.L. CHUNG, Kevin CAMPOS, Edward CLEATOR, Robert F. DUNN, Andrew GIBSON, R. Scott HOERRNER, Stephen KEEN, Dave LIEBERMAN, Zhuqing LIU, Joseph LYNCH, Kevin M. MALONEY, Feng XU, Nobuyoshi YASUDA, Naoki YOSHIKAWA, Yong-Li ZHONG
  • Publication number: 20210223262
    Abstract: The present invention provides lyophilized pellets of low concentrations of antibodies in the form of lyospheres. These lyospheres provide pre-measured antibody concentrations suitable for diagnostic and quality control assays.
    Type: Application
    Filed: June 3, 2019
    Publication date: July 22, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Akhilesh Bhambhani, Thorsten Verch, Morrisa C. Jones, Mary Retzlaff, Jessica R. Sinacola, Silikhone L. Bouaraphan
  • Patent number: 11066396
    Abstract: The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: July 20, 2021
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Abbas Walji, Richard Berger, Craig A. Stump, Kelly-Ann S. Schlegel, James J. Mulhearn, Thomas J. Greshock, Deping Wang, Mark E. Fraley, Kristen G. Jones
  • Publication number: 20210214308
    Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an DO-associated disease or disorder.
    Type: Application
    Filed: May 28, 2019
    Publication date: July 15, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shuwen He, Yongxin Han, Alexander Pasternak
  • Patent number: 11058775
    Abstract: Insulin dimers conjugated to peptides having at least one incretin activity are disclosed.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: July 13, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anandan Palani, Zhiqiang Yang, Lin Yan, Songnian Lin, Pei Huo, Ravi Nargund
  • Patent number: 11059835
    Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
    Type: Grant
    Filed: May 21, 2020
    Date of Patent: July 13, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David Waller, Gregory Gazda, Zachary Minden, Lisa Barton, Clifton Leigh
  • Publication number: 20210206796
    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: Application
    Filed: December 17, 2018
    Publication date: July 8, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Brian M. Andresen, Frank Bennett, Wonsuk Chang, Matthew Lloyd Childers, Jared N. Cumming, Jongwon Lim, Min Lu, Benjamin Wesley Trotter, Wen-Lian Wu
  • Publication number: 20210206884
    Abstract: The present invention provides processes for the preparation of sugammadex: (I) In one aspect, there is provided a process for the preparation of sugammadex from 8-per-deoxy-8-bromo-?-cyclodextrin and 3-mercaptopropionic acid. In another aspect, there is provided an alternative process for the preparation of sugammadex from 8-per-deoxy-8-bromo-?-cyclodextrin and disodium 3-mercaptopropionate. In another aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-?-cyclodextrin, which may be used in the production of sugammadex. In one such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-?-cyclodextrin from ?-cyclodextrin and a brominating agent. In another such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-?-cyclodextrin comprising, inter alia, reacting ?-cyclodextrin with an electrophilic brominating agent, a deoxygenating agent, and an acid in the presence of an organic solvent.
    Type: Application
    Filed: June 3, 2019
    Publication date: July 8, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jamie M. McCabe Dunn, Nadine Kuhl, Wenyong Chen, Yang Cao, Donald R. Gauthier, Jr., Alan Michael Hyde, Susan L. Zultanski
  • Patent number: 11053243
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: March 25, 2020
    Date of Patent: July 6, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Steven W. Ludmerer, Kun Liu, Hao Wu, Richard Soil, Bin Zhong, Jian Zhu
  • Patent number: 11053315
    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: Grant
    Filed: April 5, 2018
    Date of Patent: July 6, 2021
    Assignees: Merck Sharp & Dohme Corp., Agenus Inc.
    Inventors: Barbara Joyce-Shaikh, Luis A. Zuniga, Milan Blanusa, Andrea Claudia Schuster, Kornelia Schultze
  • Patent number: 11052065
    Abstract: The present invention relates to methods of treating a cell proliferation disorder (e.g., cancer) comprising administering: (a) a compound having the Formula (I), wherein R1 or R2 are as herein defined, or a pharmaceutically acceptable salt thereof; and (b) an anti-human PD-1 antibody or antigen binding fragment thereof to a human patient in need thereof. Also disclosed are therapeutic combinations and kits containing such agents for the treatment of cancers.
    Type: Grant
    Filed: September 24, 2018
    Date of Patent: July 6, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Elaine M Pinheiro, Michael Rosenzweig, Robert A. Kastelein, David R. Kaufman, Deborah A. Law
  • Publication number: 20210198339
    Abstract: The present disclosure provides conjugates that comprise an insulin molecule conjugated via a conjugate framework to two or more separate ligands that each include a saccharide, wherein the framework, ligand, saccharide and insulin molecule optionally comprise a fatty chain (e.g., a C8-30 fatty chain), wherein when said insulin molecule is conjugated both to a C8-30 fatty chain and one or more separate ligands that each include a saccharide, said C8-30 fatty chain is linked to insulin molecule only, and wherein when the framework or ligand comprises a fatty chain the insulin molecule is conjugated to two or more separate ligands. In certain embodiments, a conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic (PK) and/or pharmacodynamic (PD) property of the conjugate is sensitive to serum concentration of a second saccharide. In certain embodiments, a conjugate is also characterized by having a protracted PK profile.
    Type: Application
    Filed: December 13, 2018
    Publication date: July 1, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Lin Yan, Pei Huo, Ahmet Kekec, Danqing D. Feng, Yuping Zhu, Dmitri Pissarnitski, Chris Moyes, Songnian Lin
  • Publication number: 20210196734
    Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of ?7 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: March 5, 2021
    Publication date: July 1, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Brendan M. Crowley, Ian M. Bell, Andrew John Harvey, Brian T. Campbell, Thomas J. Greshock, Vanessa L. Rada
  • Publication number: 20210198190
    Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Application
    Filed: May 28, 2019
    Publication date: July 1, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shuwen He, Dane Clausen, Liangqin Guo, Yongxin Han, Xianhai Huang, Alexander Pasternak, Qinglin Pu, Dong Xiao, Li Xiao, Feng Ye, Hongjun Zhang
  • Patent number: 11046714
    Abstract: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.
    Type: Grant
    Filed: August 25, 2014
    Date of Patent: June 29, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ali Amjad, Gioconda V. Gallo, Timothy J. Henderson, Rongze Kuang, Yeon-Hee Lim, Michael Man-Chu Lo, Edward Metzger, Manuel de Lera Ruiz, Andrew Stamford, Paul Tempest, Brent Whitehead, Heping Wu
  • Patent number: 11045547
    Abstract: The present invention includes antibodies and antigen-binding fragments thereof that specifically bind to human or cynomolgous monkey LAG3 as well as immunoglobulin chains thereof and polynucleotides encoding the same along with injection devices comprising such antibodies or fragments. Vaccines including such antibodies and fragments as well as compositions comprising the antibodies and fragments (e.g., including anti-PD1 antibodies) are included in the invention. Methods for treating or preventing cancer or infection using such compositions are also provided. In addition, methods for recombinant expression of the antibodies and fragments are part of the present invention.
    Type: Grant
    Filed: December 13, 2016
    Date of Patent: June 29, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rene De Waal Malefyt, Laurence Fayadat-Dilman, Linda Liang
  • Patent number: 11046951
    Abstract: Methods for display of recombinant whole immunoglobulins or immunoglobulin libraries on the surface of eukaryote host cells, including yeast and filamentous fungi, are described. The methods are useful for screening libraries of recombinant immunoglobulins in eukaryote host cells to identify immunoglobulins that are specific for an antigen of interest.
    Type: Grant
    Filed: October 3, 2018
    Date of Patent: June 29, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bianka Prinz, Natarajan Sethuraman, Dongxing Zha, Stefan Wildt, Piotr Bobrowicz
  • Publication number: 20210188951
    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 8, 2020
    Publication date: June 24, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kalpit A. Vora, Kara S. Cox, Aimin Tang, Zhifeng Chen, Daniel DiStefano, Lan Zhang, Hua-Poo Su
  • Publication number: 20210188818
    Abstract: The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1A, R1B, X, Y, RZ and R2 are as defined herein, which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
    Type: Application
    Filed: October 8, 2018
    Publication date: June 24, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John Acton, David Annunziato Candito, J. Michael Ellis, Peter H. Fuller, Hakan Gunaydin, Blair T. Lapointe, Weiguo Liu, Joey L. Methot, Santhosh F. Neelamkavil, Barbara Pio, Vladimir Simov, Harold B. Wood
  • Publication number: 20210187049
    Abstract: The present invention relates to purified compositions of enteroviruses, pharmaceutical compositions thereof and a glutathione affinity chromatography process for the purification of enteroviruses.
    Type: Application
    Filed: December 17, 2020
    Publication date: June 24, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Erik M. Curtis, Spyridon Konstantinidis, Murphy Poplyk, Andrew Ryan Swartz, Marc D. Wenger