Abstract: Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.
Type:
Application
Filed:
November 13, 2017
Publication date:
April 30, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Thomas J. Greshock, James Mulhearn, Anthony J. Roecker, Tianying Jian, Gang Zhou, Liangqin Guo, Walter Won, Ting Zhang, Rajan Anand, John E. Stelmach, Deping Wang, Ronald M. Kim, Mark E. Layton, Christopher S. Burgey, Philippe G. Nantermet
Abstract: The present invention relates to anti-CD27 antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.
Inventors:
Amy M. Beebe, Jason Ka Jen Cheung, Veronica Juan, Laurence Fayadat-Dilman, Svetlana Sadekova, Jerelyn Wong, Hans van Eenennaam, Andrea van Elsas, Lars Guelen, Thierry Olivier Fischmann, Winifred W. Prosise
Abstract: The present invention relates to purified antibody and antigen-binding fragment compositions that lack sulfated tyrosine on one or more tyrosine residues in the immunoglobulin chains. Purification methods for removing sulfated tyrosine variants from antibody and antigen-binding fragment compositions are also provided.
Abstract: The present invention relates to Spirocyclic Pyridotriazine Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Pyridotriazine Derivative, and methods of using the Spirocyclic Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
Type:
Grant
Filed:
November 11, 2016
Date of Patent:
April 21, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Thomas H. Graham, Tao Yu, Sherman T. Waddell, John A. McCauley, Andrew Stamford, Wengsheng Liu, Jay A. Grobler, Libo Xu
Abstract: A proof of provenance system receives database logs from an existing system that does not natively provide data provenance verification. The system produces a local representation of the database (or a portion thereof). The system periodically or in response to another triggering event flattens the local representation of the database to generate an aggregated slice, which is stored in an aggregated slice store. A reduced representation of the aggregated slice (e.g., a hash or checksum) is determined and appended to a distributed ledger, such as a blockchain. The provenance of data from the existing system can then be verified by redetermining the reduced representation and comparing it to the version appended to the distributed ledger.
Abstract: Therapies comprising administering at least one cyclic dinucleotide compound that activates the Stimulator of Interferon Genes (STING) pathway, and the use of such therapies in the treatment of cell-proliferation disorders such as cancer, are disclosed herein.
Type:
Application
Filed:
December 15, 2017
Publication date:
April 16, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Saso Cemerski, Jared N. Cumming, Lauren M. Flateland, Johnny E. Kopinja, Yanhong Ma, Samanthi A. Perera, Benjamin Wesley Trotter, Archie Ngai-Chiu Tse
Abstract: The present invention relates to method for treating cancer comprising administering an antagonist of PD-1, e.g., anti-PD-1 antibody or antigen binding fragment thereof, and an anti-CTLA4 antibody or antigen binding fragment thereof, wherein the CTLA4 antibody or antigen binding fragment thereof is given at a fixed dose. Also provided are compositions and kits comprising a dosage of an anti-PD-1 antibody and a dosage of an anti-CTLA4 antibody, and uses thereof.
Type:
Application
Filed:
March 28, 2018
Publication date:
April 16, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Blanca Homet Moreno, Nageatte Ibrahim, Scot W. Ebbinghaus, Lokesh Jain, Scott Diede
Abstract: The present invention is directed to process for making Compounds of Formula (II): (II), and salts thereof, wherein B, X, R2, R3, R4 R7, R8 and R9 are defined herein.
Type:
Grant
Filed:
March 28, 2016
Date of Patent:
April 14, 2020
Assignee:
Merck Sharp & Dohme
Inventors:
Steven M. Silverman, Bryon Ladd Simmons, Zhuqing Liu, Jing Liao, Artis Klapars, Kevin R. Campos, Ana Inés Bellomo Peraza
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:
Grant
Filed:
November 20, 2017
Date of Patent:
April 14, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Sybil M. G. Williams, Drake LaFace, Laurence Fayadat-Dilman, Gopalan Raghunathan, Linda Liang, Wolfgang Seghezzi
Abstract: The present invention provides a process for preparing enterically-coated lyospheres comprising a therapeutic agent comprising: a.) providing lyospheres comprising the therapeutic agent; b.) coating said lyospheres with an enteric polymer coating composition; and c.) isolating said enterically-coated lyospheres. In other embodiments, the invention provides dosage forms comprising a lyosphere comprising an effective amount of a therapeutic agent and an enteric polymer coating. In some embodiments, the therapeutic agent in the process or dosage form is a polypeptide, a protein, a peptide, a lipopeptide, a glycoprotein, a fusion protein, a protein conjugate, a cytokine, an enzyme, an antibody, an oligonucleotide, a vaccine vector, small molecule, a live virus, an inactivated virus, a virus-like particle, a viral protein subunit, an adjuvant, microbiome, a prebiotic, a probiotic, or an ectobiotic.
Type:
Grant
Filed:
October 11, 2016
Date of Patent:
April 14, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Akhilesh Bhambhani, Robert K. Evans, Pranav Gupta, Ronald L. Smith, Donna M. Williams
Abstract: This invention provides an improved processes for the preparation of verubecestat (Compound of Formula (I)), a potent inhibitor of BACE-1 and BACE-2.
Type:
Grant
Filed:
February 10, 2017
Date of Patent:
April 14, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
William J. Morris, David Thaisrivongs, Thomas W. Lyons
Abstract: The present invention is directed to 5-(pyridine-3-yl)oxaxole 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:
Application
Filed:
June 22, 2018
Publication date:
April 9, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Jianming BAO, Timothy J. HENDERSON, Chunsing LI, Michael Man-Chu LO, Robert D. Mazzola, Jr., Meng NA, Michael T. RUDD, David M. TELLERS, Ling TONG
Abstract: Aspects of the present disclosure provide methods for determining the eligibility of a subject having a malignancy for treatment with an anti-PD therapeutic agent based on a Combined Positive Score (CPS) for a tumor tissue sample from the subject. Compositions and kits or performing the disclosed methods are also provided.
Abstract: The present invention is directed to methods for inhibition of HIV reverse transcriptase, treatment of infection by HIV, prophylaxis of infection by HIV, and the treatment, prophylaxis and/or delay in the onset or progression of AIDS or ARC by administering a compound of structural Formula I or a pharmaceutically acceptable salt or co-crystal thereof, wherein X is —F or —Cl, less frequently than once daily.
Type:
Application
Filed:
December 11, 2019
Publication date:
April 2, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof. Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Type:
Application
Filed:
March 23, 2018
Publication date:
April 2, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Liangqin Guo, Yongxin Han, Kun Liu, Shuwen He, Joseph Kozlowski, Ravi Nargund, Wensheng Yu, Hongjun Zhang, Qinglin Pu, Derun Li, Abdelghani Achab, Guoqing Li
Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiadiazine dioxide compounds bearing an ether linker, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, R2, RA, ring A, ring C, and m are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
Type:
Grant
Filed:
February 6, 2017
Date of Patent:
March 31, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Shawn P. Walsh, Jared N. Cumming, Xing Dai
Abstract: The instant invention relates to pharmaceutical compositions comprising doravirine, tenofovir disoproxil fumarate and lamivudine. These compositions are useful for the treatment of HIV infection. Also disclosed are processes for making said pharmaceutical compositions.
Type:
Grant
Filed:
November 29, 2016
Date of Patent:
March 31, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Santipharp Panmai, Aditya Tatavarti, Andrew M. Farrington, Varsha Biyyala, Leonardo R. Allain, Marcela Nefliu, Gerard R. Klinzing, Jie Ren, Matthew Lamm
Abstract: Disclosed are methods of administering cephalosporin/tazobactam to human patients with end stage renal disease undergoing hemodialysis and suffering from a complicated intra-abdominal infection or a complicated urinary tract infection.
Type:
Application
Filed:
July 29, 2019
Publication date:
March 26, 2020
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
Gopal KRISHNA, Gurudatt CHANDORKAR, Elham HERSHBERGER, Benjamin MILLER, Alan XIAO
Abstract: Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Type:
Application
Filed:
February 19, 2018
Publication date:
March 26, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Kun Liu, Dane Clausen, Liangqin Guo, Yongxin Han, Shuwen He, Joseph Kozlowski, Derun Li, Qinglin Pu, Wensheng Yu, Hongjun Zhang
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:
Application
Filed:
December 18, 2017
Publication date:
March 26, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Xiaolei GAO, Sandra L. KNOWLES, Chunsing LI, Michael Man-Chu LO, Robert D. MAZZOLA, JR., Debra L. ONDEYKA