Abstract: The present invention relates to processes for the preparation of N-protected (2S,5R)-6-hydroxy-7-oxo-N-piperidin-4-yl-1,6-diazabicyclo[3.2.1]octane-2-carboxamide intermediates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.
Type:
Application
Filed:
September 14, 2017
Publication date:
August 1, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Jianguo Yin, Zhijian Liu, Nobuyoshi Yasuda, Mark Weisel
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:
Application
Filed:
January 11, 2019
Publication date:
August 1, 2019
Applicant:
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 invention relates to novel conjugated polymers containing one or more units based on dithieno[3,2-c;2?,3?-e]azepine-4,6-dione that is fused to further aromatic rings, to methods for their preparation and educts or intermediates used therein, to polymer blends, mixtures and formulations containing them, to the use of the polymers, polymer blends, mixtures and formulations as organic semiconductors in, or for the preparation of, organic electronic (OE) devices, especially organic photovoltaic (OPV) devices and organic photodetectors (OPD), and to OE, OPV and OPD devices comprising, or being prepared from, these polymers, polymer blends, mixtures or formulations.
Abstract: The present application relates to novel compounds and to devices which contain these compounds. The application also relates to a device for regulating the passage of energy from an outside space into an inside space, to a window containing the said device, and to uses of the said devices and compounds.
Type:
Grant
Filed:
November 11, 2015
Date of Patent:
July 30, 2019
Assignee:
Merck Patent GmbH
Inventors:
Peer Kirsch, Susann Gunst, Michael Junge, Andreas Beyer, Ursula Patwal
Abstract: The invention relates to novel organic semiconducting compounds, which are small molecules or conjugated polymers, containing one or more isoindigo or thienoisoindigo based polycyclic units, to methods for their preparation and educts or intermediates used therein, to compositions, polymer blends and formulations containing them, to the use of the compounds, compositions and polymer blends as organic semiconductors in, or for the preparation of, organic electronic (OE) devices, especially organic photovoltaic (OPV) devices, organic photodetectors (OPD), Perovskite based solar cells, organic field effect transistors (OFET) and organic light emitting diodes (OLED), and to OE, OPV, OPD, OFET and OLED devices comprising these compounds, compositions or polymer blends.
Type:
Grant
Filed:
February 12, 2015
Date of Patent:
July 30, 2019
Assignee:
MERCK PATENT GMBH
Inventors:
Lana Nanson, Nicolas Blouin, William Mitchell
Abstract: A liquid-crystalline medium having a nematic phase, a dielectric anisotropy of 0.5 or more and a ratio of the dielectric constant perpendicular to the director (??) to the dielectric anisotropy (??), i.e. (??/??), of 2.0 or less and comprises one or more compounds of formula I: wherein the parameters have the meaning given in the text. An electro-optical display containing such a medium, particularly in an active-matrix display based on the IPS or FFS effect. Methods for using of the compounds of formula I for improvement of the transmission and/or response times of a liquid-crystalline medium which comprises one or more additional mesogenic compounds.
Abstract: The present invention relates to new proteins that bind to MMP9 and comprise at least one fragment of a heavy chain variable region and/or at least one fragment of a light chain variable region of an antibody. In particular, the MMP9 binding proteins according to the invention are able to neutralize MMP9 activity and are useful in the prevention and/or treatment of inflammatory and/or autoimmune diseases or cancers. In particular, the MMP9 binding proteins according to the invention are useful in diagnosis of MMP9-related disorders.
Type:
Grant
Filed:
August 13, 2015
Date of Patent:
July 30, 2019
Assignees:
CALYPSO BIOTECH SA, MERCK PATENT GMBH
Inventors:
Yolande Chvatchko Missotten, Laurence Goffin, Olivier Leger, Steven M. Dunn, Christine Power, Kinsey Maundrell
Abstract: A pigment mixture comprising at least two or three interference pigments of different interference colours selected from the colours red, green and blue, suitable for use in paints, coatings, printing inks, security printing inks, plastics, ceramic materials, glasses and in the preparation of pigment preparations, dry preparations and in particular cosmetic formulations.
Type:
Application
Filed:
January 23, 2019
Publication date:
July 25, 2019
Applicant:
MERCK PATENT GMBH
Inventors:
Christoph SCHMIDT, Carsten PLUEG, Uwe LENZ, Sabine SCHOEN
Abstract: Described herein are crystalline forms of a compound of formula (III?), including toluene solvates of TATD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane.
Type:
Application
Filed:
March 4, 2019
Publication date:
July 25, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Kristos Adrian Moshos, Valdas Jurkauskas, Giovanni Fogliato, Manuel Scanu, You Seok Hwang
Abstract: The present invention is directed to substituted triazolo bicyclic compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
Type:
Grant
Filed:
June 27, 2016
Date of Patent:
July 23, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Gregori J. Morriello, Lehua Chang, Ashley Forster, Yili Chen, Michael P. Dwyer, Zack Zhiqiang Guo, Ming Wang, Shimin Xu, Yingjian Bo, Jianmin Fu
Abstract: The present invention relates to liquid crystalline (LC) medium, to a method of its production and to the use of such LC media in polymer network liquid crystalline (PNLC) light modulation elements operated in the reverse mode. Furthermore, the present invention relates to such light modulation elements, as such, to the use of such light modulation elements as light shutters for transparent OLED displays, and to a method of production of such light modulation elements according to the present invention.
Abstract: A polymerizable LC material comprising at least one di- or multireactive mesogenic compound selected from the group of compounds of formula I, at least one monoreactive mesogenic compound selected from the group of compounds of formula II, wherein the parameter A11 to A21, L21, p, P11 to P22, R21, Sp11 to Sp21, X11 to X21, and Z11 to Z21 have one of the meanings as given in claim 1, and at least one carbazole oxime ester photoinitiator. Furthermore, a method for preparation of the polymerizable LC material, a polymer film with improved thermal durability obtainable from the corresponding polymerizable LC material, a method of preparation of such polymer film, and the use of such polymer film and said polymerizable LC material for optical, electro-optical, decorative or security devices.
Type:
Grant
Filed:
May 16, 2017
Date of Patent:
July 23, 2019
Assignee:
Merck Patent GmbH
Inventors:
Stephen Mulcahy, Iain Gardiner, Jack Bradford, Eduardo Beltran Gracia, Graham Smith
Abstract: The invention relates to improved fullerene derivatives, to methods for their synthesis and any educts or intermediates used in such methods, to compositions and formulations containing fullerene derivatives, to the use of the fullerene derivatives, compositions and formulations in, or for the preparation of, organic electronic (OE) devices like for example organic photovoltaic (OPV) devices or organic photodetectors (OPD), and to OE, OPV and OPD devices comprising, or being prepared from, these fullerene derivatives, compositions or formulations.
Type:
Grant
Filed:
October 3, 2016
Date of Patent:
July 23, 2019
Assignees:
Nano-C, Inc., Merck Patent GmbH
Inventors:
Edward A. Jackson, Henning Richter, Nicolas Blouin, Stéphane Berny
Abstract: A reloadable auto injector wherein a syringe assembly is movably positioned between a first position in which the needle is accommodated inside a housing and a second position in which the needle protrudes outside the housing. The assembly comprises a syringe, a plunger rod and a plunger rod driver configured to apply a force to the plunger rod to advance the plunger rod in the syringe for delivering at least one dose of medicament. A syringe driver is configured to apply a force to the assembly thereby moving the assembly from the first position to the second position. A reload handle may be connected to the assembly so that user operation of the reload handle retracts the assembly to the first position and simultaneously reload the syringe driver to thereby ready the auto injector for delivering a further dose of medicament. The plunger rod driver is not re-activated.
Type:
Grant
Filed:
September 10, 2012
Date of Patent:
July 23, 2019
Assignee:
MERCK PATENT GMBH
Inventors:
Soeren Bechmann, Flemming Madsen, Esben W. Johansen
Abstract: The present invention relates to monoclonal antibodies which have high anti-RSV neutralizing titers. The invention further provides for isolated nucleic acids encoding the antibodies of the invention and host cells transformed therewith. The invention yet further provides for diagnostic, prophylactic and therapeutic methods employing the antibodies and nucleic acids of the invention, particularly as a passive immunotherapy agent in infants and the elderly.
Type:
Grant
Filed:
March 22, 2018
Date of Patent:
July 23, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Kalpit A. Vora, Kara S. Cox, Aimin Tang, Zhifeng Chen, Daniel DiStefano, Lan Zhang, Hua-Poo Su
Abstract: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
Type:
Grant
Filed:
March 11, 2016
Date of Patent:
July 23, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Dong-Ming Shen, Christopher J. Sinz, Alejandro Crespo, Johnathan E. Wilson, Troy McCracken, Shimin Xu, Haitang Li
Abstract: The present disclosure describes an IHC assay for detecting and quantifying spatially proximal pairs of PD-1-expressing cells (PD-1+ cells) and PD-Ligand-expressing cells (PD-L+ cells) in tumor tissue, and the use of the assay to generate proximity biomarkers that are predictive of which cancer patients are most likely to benefit from treatment with a PD-1 antagonist. The disclosure also provides methods for testing tumor samples for the proximity biomarkers, as well as methods for treating subjects with a PD-1 antagonist based on the test results.
Type:
Application
Filed:
January 17, 2019
Publication date:
July 18, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Robert H. Pierce, Jennifer H. Yearley, Scott P. Turner, Belma Dogdas, Ansuman Bagchi
Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.
Type:
Application
Filed:
August 10, 2017
Publication date:
July 18, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
John P. Caldwell, Mary Ann Caplen, Jared N. Cumming, Kevin D. Dykstra, Alan Hruza, Claire Lankin, Derun Li, Hong Liu, Amy McCracken, Brian McKittrick, Ashwin Rao, Jayaram Tagat, Haiqun Tang, Brandon M. Taoka, Andreas Verras, Shawn P. Walsh, Wen-Lian Wu, Tianyuan Zhang
Abstract: The invention relates to a liquid-crystalline medium and to the use thereof for an active-matrix display, in particular based on the VA, PSA, PS-VA, PM-VA, SS-VA, PALC, IPS, PS-IPS, FFS or PS-FFS effect.
Abstract: The invention relates to a polymerisable LC material comprising at least one di- or multireactive mesogenic compound and at least one compound of formula CO-1, wherein R1, R2, L1, L2, L3, and n have one of the meanings as given in claim 1. Furthermore, the present invention relates also to a method for its preparation, a polymer film with improved thermal durability obtainable from the corresponding polymerisable LC material, to a method of preparation of such polymer film, and to the use of such polymer film and said polymerisable LC material for optical, electro-optical, decorative or security devices.