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:
Grant
Filed:
December 13, 2016
Date of Patent:
October 12, 2021
Assignee:
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, Jing Su, Christopher Michael Tan, Zheng Tan, Hao Wang, Christine Yang, Shu-Wei Yang
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:
Grant
Filed:
December 13, 2016
Date of Patent:
October 12, 2021
Assignee:
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
Abstract: The present invention provides a compound of formula (I) Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, are PRMT5 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 cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
Type:
Application
Filed:
August 5, 2019
Publication date:
October 7, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Michelle Machacek, David Witter, Chunhui Huang, Shuhei Kawamura, Sebastian Schneider, Murray Wan
Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, where-in R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
Type:
Application
Filed:
May 31, 2019
Publication date:
October 7, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Tao YU, Alan WHITEHEAD, Yili CHEN, Chunrui SUN, Zhiyong HU, Kake ZHAO, Ronald M. KIM, John A. McCAULEY
Abstract: The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.
Abstract: The present invention relates to stable formulations of a cytomegalovirus (CMV) comprising for example, a genetically modified CMV that is conditionally replication defective, a buffer, alkali or alkaline salt, a sugar, a cellulose derivative and optionally a polyol.
Type:
Application
Filed:
October 29, 2018
Publication date:
September 30, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Muneeswara Babu Medi, Harrison Bradford Davis, Lorenzo H. Chen, Lynne Ann Isopi, Jeffrey Thomas Blue, Heidi Joanne Pixley, Erin J. Green-Trexler
Abstract: Provided herein are anti-LAP antibodies (e.g., recombinant humanized, chimeric, and human anti-LAP antibodies) or antigen binding fragments thereof which have therapeutically beneficial properties, such as binding specifically to LAP-TGF?1 on cells but not to LAP-TGF?1 in extracellular matrix, as well as compositions including the same. Also provided are uses of these antibodies or antigen binding fragments in therapeutic applications, such as in the treatment of cancer, and diagnostic applications.
Abstract: The instant invention describes a virus reduction neutralization test (VRNT) which is a rapid, high throughput alternative to current standard low throughput and laborious neutralization assays. The VRNT utilizes imaging cytometry to count virus-infected cells at about one day post-infection (thus eliminating the wait time other assays employ allowing for viral infection cell to cell), reducing overall assay time and increasing throughput at least 15-fold.
Type:
Application
Filed:
August 9, 2019
Publication date:
September 23, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Melissa C. Whiteman, Joseph M. Antonello, Leah A. Bogardus, Danila G. Giacone, Dengyun Sun, Amy H.M. Tou, Kevin B. Gurney, Leonard J. Rubinstein
Abstract: The present invention is directed to compressed tablets for oral administration, which comprise an intragranular component comprising the potassium salt of raltegravir, an inert superdisintegrant, and a binder; and an extragranular component comprising a superdisintegrant and a lubricant.
Abstract: Compounds of Formula I: and their pharmaceutically acceptable salts 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.
Abstract: The present invention is directed to a process for preparing a compound of formula I-11 through multiple-step reactions:
Type:
Grant
Filed:
February 20, 2020
Date of Patent:
September 21, 2021
Assignee:
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
Abstract: The present invention relates to drug delivery systems that cannot be reloaded or reused and further include a passive safety shield system. The drug delivery devices described herein include a drug container comprising at least one bellow, a needle, wherein the needle is in liquid communication with the drug container; a plunger extending between a proximal end and a distal end, wherein the plunger is in communication with the drug container and where upon axial movement of the plunger, the drug container is compressed.
Type:
Grant
Filed:
January 13, 2017
Date of Patent:
September 21, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Peter A. Basile, Steven Carl Persak, Mikhail Gotliboym, Brad Britland, Stephen G. Miggels, Henry J. Mack, Jr., Oliver J. Sha
Abstract: The instant invention relates to a method for reducing the risk for development of anti-viral treatment resistance due to an HIV mutation in a human subject infected with HIV, comprising administering EFdA in combination with one or more anti-viral agents.
Abstract: The invention is related to multivalent immunogenic compositions comprising more than one S. pneumoniae polysaccharide protein conjugates, wherein each of the conjugates comprises a polysaccharide from an S. pneumoniae serotype conjugated to a carrier protein, wherein the serotypes of S. pneumoniae are as defined herein. In some embodiments, at least one of the polysaccharide protein conjugates is formed by a conjugation reaction comprising an aprotic solvent. In further embodiments, each of the polysaccharide protein conjugates is formed by a conjugation reaction comprising an aprotic solvent. Also provided are methods for inducing a protective immune response in a human patient comprising administering the multivalent immunogenic compositions of the invention to the patient. The multivalent immunogenic compositions are useful for providing protection against S. pneumoniae infection and diseases caused by S. pneumoniae.
Type:
Grant
Filed:
December 4, 2018
Date of Patent:
September 14, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
William J. Smith, Patrick McHugh, Michael Albert Winters, Julie M. Skinner, Jian He, Luwy Musey, Chitrananda Abeygunawardana, Yadong Adam Cui, Michael J. Kosinski
Abstract: The present invention relates to Compounds of Formula (I): Formula (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, Ra, Rb, A and B are as defined herein. The present invention also relates to compositions comprising at least one compound of Formula (I), and methods of using the compounds of Formula (I) for treating or preventing HIV infection in a subject.
Type:
Application
Filed:
July 26, 2019
Publication date:
September 9, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Jian Liu, Dane James Clausen, Wensheng Yu, Joseph M. Kelly, Hyunjin M. Kim, Joseph A. Kozlowski
Abstract: The present invention provides a compound of Formula (I) Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
Type:
Application
Filed:
August 5, 2019
Publication date:
September 9, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
David Witter, Shuhei Kawamura, Michelle Machacek, Ryan Quiroz, Michael H. Reutershan, Sebastian Schneider, Phieng Siliphaivanh, Yingchun Ye, Charles S. Yeung
Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound 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 a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
Type:
Grant
Filed:
October 4, 2018
Date of Patent:
September 7, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Catherine M. White, Abdelghani Achab, Indu T. Bharathan, Xavier Fradera, Yongxin Han, Derun Li, Jongwon Lim, Kun Liu, Meredeth Ann McGowan, Nunzio Sciammetta, Wensheng Yu, Hongjun Zhang, Hua Zhou
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:
Grant
Filed:
November 15, 2018
Date of Patent:
September 7, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael A. Meehl, Philip E. Brandish, Laurence Fayadat-Dilman, Veronica Juan, Carl Mieczkowski, Latika Singh
Abstract: The present invention relates to a compound represented by formula I?: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
Type:
Grant
Filed:
November 13, 2017
Date of Patent:
August 31, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Dong-Ming Shen, Thomas H. Graham, Wensheng Liu, Clare Tudge, Andreas Verras, Jinlong Jiang