Patents Assigned to Merck Sharp
  • COMPOSITIONS AND METHODS FOR TREATING CANCER WITH A COMBINATION OF PROGRAMMED DEATH RECEPTOR (PD-1) ANTIBODIES AND A CXCR2 ANTAGONIST
    Publication number: 20200276153
    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: Application
    Filed: September 24, 2018
    Publication date: September 3, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Elaine M Pinheiro, Michael Rosenzweig, Robert A. Kastelein, David R. Kaufman, Deborah A. Law
  • Compounds that are ERK inhibitors
    Patent number: 10759805
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I).
    Type: Grant
    Filed: July 11, 2018
    Date of Patent: September 1, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Xianhai Huang, Ronald D. Ferguson, Wei Zhou, Christopher W. Boyce, Phieng Siliphaivanh, David J. Witter, Milana M. Maletic, Joseph A. Kozlowski, Kevin J. Wilson
  • Cyclic di-nucleotide compounds as STING agonists
    Patent number: 10759825
    Abstract: A class of polycyclic compounds of general formula (I), of general formula (I?), or of general formula (I?), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a 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: February 1, 2018
    Date of Patent: September 1, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brian Andresen, Wonsuk Chang, Matthew Lloyd Childers, Jared N. Cumming, James P. Jewell, Jongwon Lim, Alan B. Northrup, Ryan D. Otte, Benjamin Wesley Trotter, Quang T. Truong, Shawn P. Walsh, Kake Zhao
  • ANTI-TIGIT ANTIBODIES
    Publication number: 20200270346
    Abstract: The present invention relates to anti-TIGIT antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.
    Type: Application
    Filed: May 15, 2020
    Publication date: August 27, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sybil M. G. Williams, Drake LaFace, Laurence Fayadat-Dilman, Gopalan Raghunathan, Linda Liang, Wolfgang Seghezzi
  • VARIABLE, MULTI-DOSE MICROTABLET DISPENSER
    Publication number: 20200268612
    Abstract: A microtablet dispenser is provided herein including: a microtablet reservoir disc including a plurality of wells each formed to accommodate at least one microtablet, the wells being arranged in at least one array; a screen plate having at least one opening shaped to expose all of the wells of one of the arrays when aligned therewith; and, a dose selector plate including a plurality of dosing apertures arranged in a plurality of dosing arrays of different patterns. With one of the arrays being aligned with the at least one opening of the screen plate and with a selected dosing array, the microtablets accommodated in the wells aligned with dosing apertures are free to pass through the corresponding dosing apertures so as to be dispensed therefrom, while the wells of the array not aligned with dosing apertures are obstructed by solid portions of the dose selector plate.
    Type: Application
    Filed: February 5, 2020
    Publication date: August 27, 2020
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Annaniy Berenshteyn, Mikhail Gotliboym, Christopher Granelli
  • ANTI-COAGULATION FACTOR XI ANTIBODIES
    Publication number: 20200270364
    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: Application
    Filed: May 1, 2020
    Publication date: August 27, 2020
    Applicants: Merck Sharp & Dohme Corp., Adimab, LLC
    Inventors: Zhu Chen, Kenneth Ellsworth, James Milligan, Elizabeth Oldham, Dietmar Seiffert, Vaishnavi Ganti, Mohammad Tabrizifard, Bianka Prinz
  • LONG-ACTING CO-AGONISTS OF THE GLUCAGON AND GLP-1 RECEPTORS
    Publication number: 20200270325
    Abstract: Long-acting co-agonists of the glucagon and GLP-1 receptors are described.
    Type: Application
    Filed: September 21, 2018
    Publication date: August 27, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Anandan Palani, Qiaolin Deng, Chunhui Huang, Yuping Zhu, Elisabetta Bianchi, Federica Orvieto
  • Oxazolidinone compounds and methods of use thereof as antibacterial agents
    Patent number: 10752621
    Abstract: The present invention relates to oxazolidinone Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
    Type: Grant
    Filed: March 15, 2018
    Date of Patent: August 25, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jing Su, Lihu Yang, Takao Suzuki
  • Homobispiperidinyl derivatives as liver X receptor beta agonists, compositions and their use
    Patent number: 10752587
    Abstract: In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-? receptor (LXR?) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: August 25, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael T. Rudd, David Jonathan Bennett, Jenny Wai, Zhaoyang Meng
  • Combination of a PD-1 antagonist and CPG-C type oligonucleotide for treating cancer
    Patent number: 10751412
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a Toll-like receptor 9 (TLR9) agonist that is a CpG-C type oligonucleotide, and the use of the combination therapies for the treatment of cancer.
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: August 25, 2020
    Assignees: MERCK SHARP & DOHME CORP., DYNAVAX TECHNOLOGIES CORPORATION
    Inventors: Ying Yu, Andrew Evan Denker, Svetlana Sadekova, Uyen Truong Phan, Robert A. Kastelein, David Ross Kaufman, Robert L. Coffman, Cristiana Guiducci, Robert S. Janssen
  • HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20200262826
    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 (I).
    Type: Application
    Filed: September 14, 2018
    Publication date: August 20, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Brendan M. Crowley, Peter J. Manley, William D. Shipe
  • Factor XIIa Inhibitors
    Publication number: 20200262831
    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 XIIa inhibitors.
    Type: Application
    Filed: November 13, 2017
    Publication date: August 20, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jacqueline D. Hicks, Brian Alexander McKittrick, Brent R. Whitehead, Matthew Lombardo, Xiaoqing Han, Jerry A. Taylor, Hong Dong Chu, Sung-Sau So, Peter Orth, Zhicai Wu
  • OXAZOLIDINONES AS TARO INHIBITORS
    Publication number: 20200261436
    Abstract: Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a ?-lactam antibiotic.
    Type: Application
    Filed: December 13, 2016
    Publication date: August 20, 2020
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: John P. CALDWELL, Reynalda DE JESUS, Fa-Xiang DING, Charles J. GIll, Ginny Dai HO, Sookhee N. HA, Sandra J. KOSEOGLU, Marc A. LABROLI, Sang Ho LEE, Christina MADSEN-DUGGAN, Mihir MANDAL, Terry ROEMER, Jing SU, Christopher Michael TAN, Zheng TAN, Haifeng TANG, Hao WANG, Christine YANG, Shu-Wei YANG
  • INHIBITORS OF HEPATITIS C VIRUS REPLICATION
    Publication number: 20200262836
    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: Application
    Filed: March 25, 2020
    Publication date: August 20, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: CRAIG A. COBURN, STEVEN W. LUDMERER, KUN LIU, Hao Wu, Richard Soll, Bin Zhong, Jian Zhu
  • STABLE FORMULATIONS OF ANTI-CTLA4 ANTIBODIES ALONE AND IN COMBINATION WITH PROGRAMMED DEATH RECEPTOR 1 (PD-1) ANTIBODIES AND METHODS OF USE THEREOF
    Publication number: 20200262922
    Abstract: The invention relates to stable formulations comprising antibodies or antigen binding fragments thereof that bind to cytotoxic T lymphocyte associated antigen 4 (CTLA4), optionally further containing an anti-human programmed death receptor 1 (PD-1) antibody or antigen binding fragment thereof. Also provided are methods of treating various cancers and chronic infections with the formulations of the invention.
    Type: Application
    Filed: May 1, 2018
    Publication date: August 20, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Soumendu Bhattacharya, Chakravarthy Nachu Narasimhan, Manoj K. Sharma, Xiaoyu Yang, Arnab De, Rubi Burlage, Jason K. Cheung
  • BENZIMIDAZOLES AND INDOLES AS TARO INHIBITORS
    Publication number: 20200261410
    Abstract: Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a ?-lactam antibiotic.
    Type: Application
    Filed: December 13, 2016
    Publication date: August 20, 2020
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: John P. CALDWELL, Ginny Dai HO, Sookhee N. HA, Sandra J. KOSEOGLU, Marc A. LABROLI, Sang Ho LEE, Christina MADSEN-DUGGAN, Mihir MANDAL, Jianping PAN, Weidong PAN, Terry ROEMER, Jin SU, Christopher Michael TAN, Zheng TAN, Hao WANG, Christine YANG, Shu-Wei YANG
  • PROCESS FOR PREPARING PHARMACEUTICAL COMPOSITIONS
    Publication number: 20200261365
    Abstract: A process for preparing and isolating pharmaceutical active ingredient particles having a particle size of between about 0.1 and 30 microns, wherein a slurry comprising the active ingredient and one or more pharmaceutically acceptable excipients is fed into a thin film evaporator under suitable conditions for less than 10 minutes sufficient to generate solid matrix particles comprising active ingredient and one or more excipients, wherein the particles have less than 5% residual solvent.
    Type: Application
    Filed: December 13, 2016
    Publication date: August 20, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Luke R. Schenck, David J. Lamberto, Joseph L. Kukura, II, Francisco J. Guzman, Aaron Cote, Athanas Koynov
  • HETEROCYCLIC COMPOUNDS AS HIV PROTEASE INHIBITORS
    Publication number: 20200261421
    Abstract: The present invention is directed to compounds of Formula I, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
    Type: Application
    Filed: December 19, 2017
    Publication date: August 20, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Brian McKittrick, John P. Caldwell, John A. McCauley, Henry Vaccaro, Tin-Yau Chan, Hyunjin Kim, Elizabeth Smith, Liwu Hong, Tanweer Khan, Shihong Ying, Hongwu Wang
  • Piperidine or piperazine linked imidazole and triazole derivatives and methods of use
    Patent number: 10745377
    Abstract: The present invention relates to piperidine or piperazine linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: August 18, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Milana M. Maletic, Yunfu Luo, Zhiqi Qi, Tingting Yu, Richard Soll
  • Antiviral phosphodiamide prodrugs of tenofovir
    Patent number: 10745428
    Abstract: Compounds of Formula I and pharmaceutically acceptable salts and co-crystals thereof are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: December 5, 2016
    Date of Patent: August 18, 2020
    Assignees: IDENIX PHARMACEUTICALS LLC, MERCK SHARP & DOHME CORP.
    Inventors: Izzat Tiedje Raheem, Timothy J. Hartingh, John Schreier, Jean-Laurent Paparin