Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: 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:
October 11, 2019
Publication date:
December 9, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Dane Clausen, Ping Chen, Xavier Fradera, Liangqin Guo, Yongxin Han, Shuwen He, Jongwon Lim, Theodore A. Martinot, Alexander Pasternak, Li Xiao, Wensheng Yu
Abstract: The invention relates to stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof. In some embodiments the formulations of the invention comprise between 5-250 mg/mL anti-PD-1 antibody, or antigen binding fragment thereof, a buffer, a stabilizer, a surfactant, and an antioxidant in the amounts specified herein. In particular embodiments, the anti-PD-1 antibody is pembrolizumab. The invention further provides methods for treating various cancers with stable formulations of the invention. In some embodiments of the methods of the invention, the formulations are administered to a subject by intravenous or subcutaneous administration.
Type:
Application
Filed:
November 6, 2019
Publication date:
December 9, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
William P. Forrest, Jr., Chakravarthy Nachu Narasimhan, Yogita Krishnamachari
Abstract: The present invention is directed to pyrazol-4-yl-pyridine 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.
Inventors:
John J. ACTON, III, Jianming BAO, Qiaolin DENG, Melissa EGBERTSON, Ronald FERGUSON, II, Xiaolei GAO, Scott Timothy HARRISON, Timothy J. HENDERSON, Sandra L. KNOWLES, Chunsing LI, Michael Man-Chu LO, Robert D. MAZZOLA, Jr., Meng NA, Michael T. RUDD, Oleg B. Selyutin, David M. TELLERS, Ling TONG, Fengqi ZHANG, Takao SUZUKI
Abstract: A syringe holder for holding and stabilizing syringes, the syringe holder comprising a base, and both a vertical mount and a horizontal mount extending from one side of the base. The vertical mount comprises a cylindrical cavity configured to receive and rotatably attach the syringe to the base such that the syringe is held to the base in a generally vertical orientation, while the horizontal mount comprises a lower barrel support and an upper barrel support configured to receive and rotatably attach the bottom end of the barrel and the top end of the barrel of the syringe to the base such that the syringe is held to the base in a generally horizontal orientation. In both orientations, the syringe holder of the present invention provides easy access to most of the exterior surfaces of the syringes and reduces safety hazards associated with creating sample defects on syringes for purposes of qualification testing for syringe inspectors.
Abstract: A vial holder for holding and stabilizing vials, the vial holder comprising a base, and both a vertical mount and a horizontal mount extending from one side of the base. The vertical mount comprises a cylindrical cavity configured to receive and rotatably attach the vial to the base such that the vial is held to the base in a generally vertical orientation, while the horizontal mount comprises a body support and a neck support configured to receive and rotatably attach the body and the neck of the vial to the base such that the vial is held to the base in a generally horizontal orientation. In both orientations, the vial holder of the present invention provides easy access to most of the exterior surfaces of the vials and reduces safety hazards associated with creating sample defects on vials for purposes of qualification testing for vial inspectors.
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:
Application
Filed:
July 13, 2021
Publication date:
December 9, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
William J. Smith, Patrick McHugh, Michael A. Winters, Julie M. Skinner, Jian He, Luwy Musey, Chitrananda Abeygunawardana, Yadong Adam Cui, Michael J. Kosinski
Abstract: The invention provides methods for using and compositions of humanized antibodies that bind tau protein that is phosphorylated at the serine at position 413.
Inventors:
Hiroshi Eguchi, Takashi Murakami, Naoko Namiki, Akira Tanokura, Jeanne E. Baker, Sophie Parmentier Batteur, Angela Marie Jablonski, Daniel Stephen Malashock, Carl Mieczkowski, Gopalan (Raghu) Raghunathan
Abstract: The present disclosure provides processes for describing and quantifying the expression of human programmed death ligand-1 (PD-L1) in tumor tissue sections as detected by immunohistochemical assay using an antibody that specifically binds to PD-L1. The results generated using these processes have a variety of experimental, diagnostic and prognostic applications.
Type:
Grant
Filed:
September 22, 2017
Date of Patent:
December 7, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Marisa Dolled-Filhart, Kenneth Emancipator, Frank Lynch, Robert H. Pierce, Dianna Wu
Abstract: Invented are compounds of formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 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 hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.
Type:
Application
Filed:
May 13, 2021
Publication date:
November 25, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Yeon-Hee Lim, Jianming Bao, Faben A. Cruz, Fa-Xiang Ding, Cedric Lorenz Hugelshofer, Victor W. Mak, James Patrick Roane, Jillian R. Sanzone, Samantha E. Shockley, Rose Yen
Abstract: Provided herein are methods of treating cancer or infection, which comprise administering to a human patient in need thereof: (a) an anti-human PD-1 monoclonal antibody or antigen binding fragment thereof; (b) an anti-human LAG3 monoclonal antibody or antigen binding fragment thereof; and (c) an anti-human TIGIT monoclonal antibody or antigen binding fragment thereof. Also provided are pharmaceutical compositions and kits containing such agents for the treatment of cancer or infection.
Abstract: The present disclosure is directed to pharmaceutical formulations comprising an amorphous inhibitor of hepatitis C vims NS5A. These pharmaceutical formulations may be prepared by roller-compaction or wet-granulation methods. The present disclosure is also directed to oral dosage forms, such as tablets, comprising such pharmaceutical formulations.
Type:
Application
Filed:
October 21, 2019
Publication date:
November 25, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Sutthilug Sotthivirat, Joyce Stellabott, Walter R. Wasylaschuk
Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, Z, R1 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:
February 11, 2019
Publication date:
November 25, 2021
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Mark W. Embrey, Timothy John Hartingh, Marc Labroli, Izzat T. Raheem
Abstract: This invention relates to carbapenem compounds of the following formula: wherein A, Z, X, R1, and R4 are as described herein, as well as stereoisomers, pharmaceutically acceptable salts or N-oxides thereof, which may be useful for the treatment of bacterial infections, particularly drug-resistant bacterial infections, as well as the processes for the preparation of compounds, the pharmaceutical compositions of these compounds and their use in the treatment of bacterial infection.
Abstract: The instant invention provides compounds of formula I 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:
November 23, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Meredeth A. McGowan, Jason D. Katz, Hua Zhou, David James Witter, Chaomin Li, Kathryn A. Lipford, Joey L. Methot, Abdelghani A. Achab, Xavier Fradera, Shimin Xu, Jianmin Fu
Abstract: As a part of routine maintenance and testing, one must ensure that eye wash stations have access to clean water that flows appropriately and at the proper water pressure. Testing appropriate water flow and water pressure is messy. The inspection splash guards of the instant invention minimize water from splashing outside a wash basin area and are transparent to ensure proper visualization during eye wash station maintenance and testing.
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 XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Abstract: A manually actuated drug-injecting device is configured such that the grip strength of the entire hand (i.e., majority of fingers closing toward the palm or heel of the hand) is employed to discharge medication through a hypodermic needle and into a patient's body. The device is well suited for delivering medications with high viscosity and/or by patients (e.g., elderly patients) with reduced finger strength and dexterity. The device includes a grip member, a push member (which causes the medication to be injected), and a force-transfer mechanism that couples the grip member to the push member. Suitably, the device is configured to be held transverse to the palm of the medication-administering hand, with a discharge port located by the outer, blade edge of the administering hand, when the device is being gripped to administer medication.
Type:
Grant
Filed:
November 20, 2017
Date of Patent:
November 16, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Peter A. Basile, Henry J. Mack, Jr., Oliver Sha, Stephen G. Miggels
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:
Grant
Filed:
October 8, 2018
Date of Patent:
November 16, 2021
Assignee:
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
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:
July 26, 2021
Publication date:
November 11, 2021
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, 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:
Application
Filed:
July 26, 2021
Publication date:
November 11, 2021
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