Abstract: The invention provides certain bicyclic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
Inventors:
Thomas D. Aicher, Chad A. VanHuis, William D. Thomas, John K. MacLean, Brian M. Andresen, Kenneth J. Barr, Corey E. Bienstock, Neville J. Anthony, Matthew Daniels, Kun Liu, Yuan Liu, Catherine M. White, Blair T. Lapointe, Nunzio Sciammetta, Vladimir Simov
Abstract: The invention relates to boron-containing compounds with bicyclic structural units and to electronic devices, in particular organic electroluminescent devices, containing said compounds.
Abstract: The present application relates to spirobifluorene derivatives of a formula (I), to the use thereof in electronic devices, especially in organic electroluminescent devices (OLEDs), where they may be used in hole-transporting function, and to processes for preparing said derivatives. The compounds have one or more properties selected from very good hole-conducting properties, very good electron-blocking properties, high glass transition temperature, high oxidation stability, good solubility and high thermal stability.
Type:
Grant
Filed:
December 8, 2015
Date of Patent:
March 5, 2019
Assignee:
Merck Patent GmbH
Inventors:
Jochen Pfister, Frank Stieber, Elvira Montenegro, Teresa Mujica-Fernaud
Abstract: Metal complexes containing one or more amidoimine ligands, methods of making such metal complexes, and methods of using such metal complexes to prepare metal-containing films are provided.
Type:
Grant
Filed:
October 24, 2014
Date of Patent:
March 5, 2019
Assignee:
MERCK PATENT GMBH
Inventors:
Ravi Kanjolia, Shaun Garratt, David Thompson, Jeffrey Anthis
Abstract: A method of producing mixtures of interference pigments having special effects comprises mixing at least one large particle size interference pigment with at least one normal size interference pigment of predetermined colors and in proportions desired to obtain a unique effect.
Abstract: This application is directed to the use of biomarkers for predicting the sensitivity to treatment with an FGF-18 compound of a patient having a cartilage disorder, such as osteoarthritis, cartilage injury, fractures affecting joint cartilage or surgical procedures with impact on joint cartilage (e.g., microfracture), in order to reduce the risk of adverse events and increase the overall benefit after therapy.
Type:
Grant
Filed:
August 5, 2013
Date of Patent:
March 5, 2019
Assignee:
MERCK PATENT GMBH
Inventors:
Christoph Hubertus Ladel, Alix Anne Simone Berton, Armand Valsesia, Pierre Jacques Farmer
Abstract: The present invention relates to compounds according to Formula (I-1) and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
Type:
Grant
Filed:
February 11, 2016
Date of Patent:
March 5, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Blair T. Lapointe, Peter H. Fuller, Hakan Gunaydin, Kun Liu, Nunzio Sciammetta, Benjamin Wesley Trotter, Hongjun Zhang, Kenneth J. Barr, John K. F. Maclean, Danielle F. Molinari, Vladimir Simov
Abstract: Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting 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 pain disorders, cough, and itch using the same.
Type:
Grant
Filed:
December 14, 2016
Date of Patent:
March 5, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Thomas J. Greshock, James Mulhearn, Junying Zheng, Ronald M. Kim, Ting Zhang, Anthony J. Roecker, Walter Won, Philippe Nantermet, Rajan Anand, Gang Zhou, Deping Wang, Liangqin Guo
Abstract: The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R4 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
Type:
Grant
Filed:
December 4, 2015
Date of Patent:
March 5, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Mark W. Embrey, Thomas H. Graham, Izzat T. Raheem, John D. Schreier, Sherman T. Waddell, John S. Wai, Lihong Hu, Xuanjia Peng
Abstract: The present invention relates to metallo-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-beta-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta-lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
Type:
Grant
Filed:
June 24, 2016
Date of Patent:
March 5, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Frank Bennett, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Xin Gu, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Yuhua Huang, Dexi Yang, Katherine Young, Li Xiao, Zhibo Zhang, Jianmin Fu
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:
June 24, 2016
Date of Patent:
March 5, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Meredeth Ann McGowan, Hua Zhou, Jason D. Katz, Lihu Yang, Joey L. Methot, Kathryn Ann Lipford, Shimin Xu, Ning Fu, Guoquan Xu, Deqian Bian, Jianmin Fu, Yabin Li, Kin Chiu Fong
Abstract: The invention relates to an in silico screening method to identify candidate excipients for reducing aggregation of a protein in a formulation. The method combines computational molecular modeling and molecular dynamics simulations to identify sites on a protein where non-specific self-interaction and interaction of different test excipients may occur, determine the relative binding energies of such interactions, and select one or more test excipients that meet specified interaction criteria for use as candidate excipients in empirical screening studies.
Abstract: The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one 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:
October 31, 2018
Publication date:
February 28, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
JIANMING BAO, XIAOLEI GAO, SANDRA L. KNOWLES, CHUNSING LI, I, MICHAEL MAN-CHU LO, ROBERT D. MAZZOLA, JR., DEBRA L. ONDEYKA, ANDREW W. STAMFORD, FENGQI ZHANG
Abstract: The present invention relates to formulations for the preparation of organic electronic devices which comprise at least one specific A/JV-dialkylaniline and at least one organic functional material selected from organic conductors, organic semiconductors, organic fluorescent compounds, organic phosphorescent compounds, organic light-absorbent compounds, organic light-sensitive compounds, organic photosensitisation agents and other organic photoactive compounds, selected from organometallic complexes of transition metals, rare earths, lanthanides and actinides.
Abstract: The invention relates to a liquid-crystalline medium which comprises at least one compound of the formula I, in which R1, R1*, Z1, Z2 and L1-3 have the meanings defined herein, and to the use thereof for an active-matrix display, in particular based on the VA, PSA, PS-VA, PALC, FFS, PS-FFS, PS-IPS or IPS effect.
Type:
Grant
Filed:
October 2, 2017
Date of Patent:
February 26, 2019
Assignee:
MERCK PATENT GMBH
Inventors:
Harald Hirschmann, Monika Bauer, Martina Windhorst, Marcus Reuter, Constanze Brocke, Rocco Fortte, Matthias Bremer, Sabine Schoen
Abstract: The invention relates to a liquid-crystalline medium which comprises at least one compound of the formula I, in which R1, R1*, Z1, Z2 and L1-3 have the meanings defined herein, and to the use thereof for an active-matrix display, in particular based on the VA, PSA, PS-VA, PALC, FFS, PS-FFS, PS-IPS or IPS effect.
Type:
Grant
Filed:
June 16, 2015
Date of Patent:
February 26, 2019
Assignee:
MERCK PATENT GMBH
Inventors:
Harald Hirschmann, Monika Bauer, Martina Windhorst, Marcus Reuter, Constanze Brocke, Rocco Fortte, Matthias Bremer, Sabine Schoen
Abstract: The present invention provides a liquid-crystal display device capable of maintaining a high voltage holding ratio even without an alignment film. The liquid-crystal display device of the present invention includes a pair of substrates, a liquid crystal layer which is sandwiched between the substrates and which contains a liquid crystal material, and a polymer layer which is disposed on a surface of each of the substrates and which controls the alignment of liquid crystal molecules. The outermost surfaces of both the substrates comprise substantially no alignment film. The polymer layer is formed by polymerizing one or more radical polymerizable monomer species added to the liquid crystal layer. At least one species of the one or more radical polymerizable monomer species is a biphenyl compound having a specific structure.
Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
Type:
Grant
Filed:
February 8, 2017
Date of Patent:
February 26, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
John Y. L. Chung, Amude Kassim, John Limanto, Michael Shevlin, Peter E. Maligres, Daniel A. DiRocco, James F. Dropinski, Rose Mathew, Yi Ning Ji Chen, Edward C. Sherer, Mikhail Reibarkh, Artis Klapars, Alan Hyde, Susan L. Zultanski, Aaron Moment, Bryon Simmons, Tyler A. Davis, Timothy James Wright, Ralph Calabria, Louis charles Campeau