Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
Type:
Grant
Filed:
June 20, 2019
Date of Patent:
November 10, 2020
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Thomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley
Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
Type:
Application
Filed:
July 22, 2020
Publication date:
November 5, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Gregory L. Adams, Jason M. Cox, John S. Debenham, Scott Edmondson, Eric J. Gilbert, Yan Guo, Yu Jiang, Hubert Josien, Hyunjin M. Kim, Ping Lan, Shouwu Miao, Christopher W. Plummer, Murali Rajagopalan, Unmesh Shah, Zhongxiang Sun, Quang T. Truong, Feroze Ujjainwalla, Francisco Velazquez, Srikanth Venkatraman, Takao Suzuki, Nengxue Wang
Abstract: The invention pertains to a kit for assembling a disposable applicator for inserting an implant, in particular a rod-like implant containing an active substance, under the skin of a human or animal, the kit comprising a first component, in turn comprising a main housing part providing a handle for grasping and maneuvering the applicator, a cannula, and a cannula holder mounted in the main housing part, the main housing part having an opening which allows introduction of an implant into the proximal end of the cannula or the cannula holder, and, a second component for closing said opening, in turn comprising a second housing part and a rod attached to or forming an integral whole with the second housing part and mountable inside the cannula or the cannula holder.
Type:
Grant
Filed:
September 6, 2018
Date of Patent:
November 3, 2020
Assignee:
MERCK SHARP & DOHME B.V.
Inventors:
Dennis Cornelis Franciscus Beelen, Martin Van Hermelen, Robertus Theodoor Maria Moormann, Maurice Petrus Wilhelmus Tak
Abstract: The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
Type:
Grant
Filed:
July 5, 2016
Date of Patent:
November 3, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Amjad Ali, Xianhai Huang, Yeon-Hee Lim, Rongze Kuang, Heping Wu, Rajan Anand, Younong Yu, Edward Metzger, Michael Man-Chu Lo, Pauline C. Ting, Andrew W. Stamford, Paul Tempest
Abstract: The instant invention provides for novel lipid nanoparticle (LNP) formulations, containing cationic lipids, for use as vaccine adjuvants and/or as antigen delivery systems. It is an object of the instant invention to provide LNP formulations that demonstrate enhancements in humoral and cellular immunogenicity of vaccine antigens, particularly subunit vaccine antigens, when utilized alone or in combination with immunostimulatory agents (e.g. small molecule or oligonucleotide TLR agonists). The instant invention further identifies physical and chemical properties of the LNP formulations that can be manipulated to enhance antigen efficiency and adjuvant tolerability in vivo.
Type:
Grant
Filed:
February 23, 2015
Date of Patent:
November 3, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Marian Gindy, Danilo R. Casimiro, Andrew Bett, Jan H. Ter Meulen
Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
Type:
Grant
Filed:
September 19, 2019
Date of Patent:
October 27, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Cheol K. Chung, Mark E. Scott, Paul G. Bulger, Kevin M. Belyk, John Limanto, Guy R. Humphrey
Abstract: Therapies comprising administering at least one benzo[b]thiophene 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:
July 30, 2018
Publication date:
October 22, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Saso CEMERSKI, Jared N. CUMMING, Johnny E. KOPINJA, Samanthi A. PERERA, Benjamin Wesley TROTTER, Archie Ngai-Chiu TSE
Abstract: The present invention provides capsular polysaccharides from Streptococcus pneumoniae serotypes identified using NMR. The present invention further provides polysaccharide-protein conjugates in which capsular polysaccharides from one or more of these serotypes are conjugated to a carrier protein such as CRM197. Polysaccharide-protein conjugates from one or more of these serotypes may be included in multivalent pneumococcal conjugate vaccines having polysaccharides from multiple additional Streptococcus pneumoniae serotypes.
Type:
Application
Filed:
September 4, 2018
Publication date:
October 22, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Richard J. Porambo, Chitrananda Abeygunawardana, Luwy Kavuka Musey, Michael J. Kosinski, Yadong Adam Cui, Julie Marie Skinner
Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 23, 2019
Date of Patent:
October 20, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Iyassu K. Sebhat, Ashok Arasappan, Scott B. Hoyt, Robert R. Wilkening, Duane DeMong
Abstract: An indexing system uses a cascade of hash structures to process data entries upon ingest for indexing. The indexing system may be used for enhancing database privacy, anonymization, or data compression. A hash structure, for example, a bloom filter or hash table, passes a representation of the data entries to a subsequent hash structure in the cascade responsive to determining that the hash structure previously filtered an instance of the same representation. The indexing system can generate the representations of the data entries using one or more hash functions. A terminal hash structure of the cascade may index the data entries responsive to determining that the data entries satisfy a criteria for anonymization. For instance, the indexing system determines that there exists a threshold number of data entries describing a population of subjects having the same combination of data elements.
Abstract: Vaccine formulations are described comprising physically separated, lyophilized antigens and adjuvant components, which may be in lyoparticle form, as well as methods of using and making such formulations. Reconstituted formulations are also described.
Type:
Application
Filed:
October 22, 2018
Publication date:
October 15, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Akhilesh Bhambhani, Muneeswara Babu Medi, Maya Salnikova, William James Smith, David S. Thiriot
Abstract: Described are antibody peptide conjugates (APCs) comprising an antibody conjugated to a peptide analog of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have agonist activity at the glucagon (GCG) receptor and the glucagon-like peptide 1 (GLP-1) receptor and the use of such APCs for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.
Type:
Grant
Filed:
October 4, 2016
Date of Patent:
October 13, 2020
Assignees:
Merck Sharp & Dohme Corp., Ambryx, Inc.
Inventors:
Paul Carrington, Grigori Ermakov, Robert M. Garbaccio, Wolfgang Seghezzi, Elisabetta Bianchi, Federica Orvieto, Dennis Gately, Nick Knudsen, Anthony Manibusan
Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
Type:
Grant
Filed:
November 26, 2018
Date of Patent:
October 13, 2020
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Songnian Lin, Lin Yan, Pei Huo, Dmitri Pissarnitski, Danqing Feng, Ravi Nargund, Yuping Zhu, Ahmet Kekec, Christina B. Madsen-Duggan, Zhi-Cai Shi, Zhicai Wu, Yingjun Mu
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.
Abstract: Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.
Type:
Grant
Filed:
April 1, 2019
Date of Patent:
October 6, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael D. Altman, Brandon D. Cash, Matthew Lloyd Childers, Jared N. Cumming, Duane E. DeMong, Andrew Marc Haidle, Timothy J. Henderson, James P. Jewell, Matthew A. Larsen, Jongwon Lim, Min Lu, Ryan D. Otte, Benjamin Wesley Trotter
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.
Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
Type:
Grant
Filed:
January 23, 2018
Date of Patent:
September 29, 2020
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Tao Yu, John A. McCauley, Alan Whitehead, James M. Apgar, Izzat T. Raheem, Guizhen Dong, Sherman T. Waddell, Hong Li
Abstract: The present invention relates to monobactam compounds of Formula (I) and pharmaceutically acceptable salts thereof. The present invention also relates to compositions which comprise a monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.
Type:
Application
Filed:
September 27, 2018
Publication date:
September 24, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Tesfaye Biftu, Xianhai Huang, Weiguo Liu, Weidong Pan, Min Park, Alexander Pasternak, Wanying Sun, Haifeng Tang, Yi Zang