Abstract: The present invention is directed to 5,5-bicyclic oxazole compounds which are antagonists of orexin receptors. 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 orexin 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 orexin receptors are involved.
Type:
Grant
Filed:
December 14, 2015
Date of Patent:
June 5, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Nigel Liverton, Thomas S. Reger, Jason W. Skudlarek
Abstract: The present invention relates to cell culture media comprising polymer embedded components. Some components show poor stability in dry powder cell culture media. Others are hygroscopic. Such components can be embedded into polymers to increase stability and reduce clumping.
Type:
Grant
Filed:
June 16, 2014
Date of Patent:
June 5, 2018
Assignee:
MERCK PATENT GMBH
Inventors:
Michael Howard Rayner-Brandes, Joerg Von Hagen
Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
Type:
Grant
Filed:
March 10, 2017
Date of Patent:
June 5, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).
Inventors:
Phieng Siliphaivanh, David L. Sloman, David Witter, Umar Faruk Mansoor, Joseph Kozlowski, Ziping Liu, Jianmin Fu, Zhilong Wan, Wei Liu, Yimin Qian, Xianhai Huang
Abstract: The invention relates to lateral fluorinated reactive mesogens (RMs) comprising a tolane group, to mixtures and formulations comprising them, to polymers obtained form such RMs and RM mixtures, and the use of the RMs, RM mixtures and polymers in optical or electrooptical components or devices, like optical films for liquid crystal displays (LCDs).
Type:
Application
Filed:
May 2, 2016
Publication date:
May 31, 2018
Applicant:
Merck Patent GmbH
Inventors:
Graham SMITH, Mark GOEBEL, Kevin ADLEM, Sarah WHITEHOUSE, Tara PERRETT
Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or pharmaceutically acceptable salt thereofs, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or pharmaceutically acceptable salts thereof.
Type:
Application
Filed:
May 23, 2016
Publication date:
May 31, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Joie GARFUNKLE, Olga ORNOSKI, Dann L. PARKER, JR., Subharekha RAGHAVAN, Libo XU
Abstract: The present disclosure describes baseline and on treatment blood-based gene signature biomarkers that are predictive of tumor sensitivity to therapy with a PD-1 antagonist. The on-treatment biomarkers comprise a PD-L1 gene signature or an interferon gamma gene signature and the baseline gene signature biomarker comprises genes associated with the oxidative phosphorylation pathway. The disclosure also provides methods and kits for testing tumor samples for these biomarkers, as well as methods for treating subjects with a PD-1 antagonist based on the test results.
Type:
Application
Filed:
April 12, 2016
Publication date:
May 31, 2018
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Mark Ayers, Jared Lunceford, Andrey Loboda, Michael Nebozhyn, Terrill K. McClanahan, Heather Hirsch
Abstract: The present invention is directed to dihydropyrazolopyrimidinone 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:
Application
Filed:
May 31, 2016
Publication date:
May 31, 2018
Applicants:
Merck Sharp & Dohme Corp., MSD R & D (China) Co. LTD.
Inventors:
Dong-Ming Shen, Michael P. Dwyer, Christopher J. Sinz, Deping Wang, Shawn J. Stachel, Daniel V. Paone, Ashley Forster, Richard Berger, Yili Chen, Yimin Qian, Shimin Xu, Chunmei Hu
Abstract: The present invention relates to compounds of the formula (1) and (2) which are suitable for use in electronic devices, in particular organic electroluminescent devices.
Type:
Grant
Filed:
September 16, 2011
Date of Patent:
May 29, 2018
Assignee:
Merck Patent GmbH
Inventors:
Philipp Stoessel, Dominik Joosten, Arne Buesing
Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is —C(?O) or —S(O)2—, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
Type:
Grant
Filed:
July 28, 2014
Date of Patent:
May 29, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jian Liu, Pengcheng Patrick Shao, Arto K. Krikorian, Petr Vachal
Abstract: The present application relates to a compound of a formula (I) which contains an indenocarbazole group, a carbazole group and an electron-deficient group bonded to the indenocarbazole group. The compound is suitable for use in electronic devices, in particular in organic electroluminescent devices.
Type:
Grant
Filed:
November 15, 2013
Date of Patent:
May 29, 2018
Assignee:
Merck Patent GmbH
Inventors:
Amir Hossain Parham, Thomas Eberle, Anja Jatsch, Christof Pflumm, Jonas Valentin Kroeber, Rémi Manouk Anèmian
Abstract: The present invention relates to an LDS-active additive for LDS plastics, to a polymer composition comprising an additive of this type, and to an article having metallized conductor tracks in which a polymeric basic body of the article or a polymeric coating on a basic body comprises an LDS additive of the said type.
Abstract: The invention relates to combinations of 4-[(S)-2-Azetidin-1-yl-1-(4-chloro-3-trifluoromethyl-phenyl)-ethylamino]-quinazoline-8-carboxylic acid amide and/or its physiologically acceptable salts and solvates, and an inhibitor of Her2, and the use of such combinations for the treatment of cancer.
Type:
Grant
Filed:
March 9, 2015
Date of Patent:
May 29, 2018
Assignee:
Merck Patent GmbH
Inventors:
Bayard R. Huck, Erik Wilker, Andreas Machl, Remigiusz Kaleta
Abstract: The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.
Type:
Grant
Filed:
June 2, 2014
Date of Patent:
May 29, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Craig A. Coburn, Milana Maletic, Yunfu Luo, Zhiqi Qi, Chunsing Li, Tingting Yu, Richard Soll
Abstract: Novel azaquinazoline carboxamide derivatives of formula (I) wherein W1, W2, W3, W4, R1, R2, R3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.
Type:
Grant
Filed:
August 3, 2016
Date of Patent:
May 29, 2018
Assignee:
Merck Patent GmbH
Inventors:
Bayard R. Huck, Ruoxi Lan, Justin Potnick, Lizbeth Celeste Deselm, Mark W. Cronin, Jr., Constantin Neagu, Xiaoling Chen, Roch Boivin, Theresa L. Johnson, Andreas Goutopoulos
Abstract: A liquid crystal display device includes: a polymer layer that controls the alignment of liquid crystal molecules on at least one of the first substrate and the second substrate. The polymer layer is formed by polymerizing one or more radical-polymerizable monomers added to the liquid crystal layer. At least one of the radical-polymerizable monomers is a compound represented by P-Sp1-Z2-A1-(Z1-A2)n1-Z3-Sp2-P. In an example encompassed by the formula, P represents a radical-polymerizable group. Sp1 and Sp2 each represent a direct bond or an alkylene group. A1 represents a divalent aromatic hydrocarbon group. A2 represents a phenylene group. Z1, Z2, and Z3 may be the same or different. At least one of Z1, Z2, and Z3 represents a direct bond, or an —NRCO— group or —CONR— group. R represents a hydrogen atom or a C1-C6 linear alkyl group or alkenyl group. n1 is 0 or 1.
Abstract: The invention relates to novel conjugated polymers containing one or more [1,2,5]Thiadiazolo[3,4-e]isoindole-5,7-dione (TID) repeating units, 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.
Type:
Grant
Filed:
June 3, 2014
Date of Patent:
May 29, 2018
Assignee:
MERCK PATENT GMBH
Inventors:
Nicolas Blouin, Agnieszka Pron, Graham Morse, Lana Nanson, Michal Krompiec, Stephane Berny
Abstract: The invention provides humanized mouse anti-human IL-31 antibodies and antibody fragments that are capable of binding IL-31 and thereby neutralizing, inhibiting, limiting, or reducing the proinflammatory or pro-pruritic effects of IL-31.
Inventors:
Angela M. Amend Kwasnik, Benjamin R. Bartfield, Peter Basile, Jeffrey C. Givand, Philip G. Green, Sharad Gupta, Christin L. O'Neill, Steven Carl Persak, Robert Stianchi, Ari Tao Adler, Florian Altmann, Thomas Junk, Florian Kössler, Martin Meier, Scott R. Mackie, Pernilla Danielsson