Abstract: The invention provides compounds of Formula (I) for inhibiting gh cosidases, prodrugs of the compounds, and pharmaceutical compositions comprising the compounds or prodrugs of the compounds. The invention also provides method of treating diseases and disorders related to deficiency or over-expression of O-gh coprotein 2-acetamido-2-deoxy-?-D-glucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-?-D-glucopyranoside (O-GlcNAc).
Abstract: This invention relates to indazole compounds of the structural formula: (structure represented) or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment or amelioration of conditions that could be treated by inhibiting aldosterone synthase.
Type:
Grant
Filed:
December 17, 2013
Date of Patent:
December 20, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott B. Hoyt, Jerry Andrew Taylor, Clare London, Yusheng Xiong, Andrew John Cooke
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:
Application
Filed:
February 23, 2015
Publication date:
December 15, 2016
Applicant:
Merck Sharp & dohme Corp
Inventors:
Marian Gindy, Danilo R. Casimiro, Andrew Bett, Jan H. Ter Meulen
Abstract: This invention provides a buffered solution comprising acadesine, as well as compositions, formulations and kits containing said solution. The solution, compositions, formulation, and kits can be used to prevent morbidity/mortality in a patient or to treat an ischaemic condition, a condition regulated by adenosine, or a condition associated with reduced blood flow to a tissue in a patient.
Type:
Application
Filed:
August 23, 2016
Publication date:
December 15, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Valentyn Antochshuk, Mohammed Shameem, Amardeep Singh Bhupender BHALLA
Abstract: This invention relates to imidazopyridyl compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
Type:
Grant
Filed:
October 16, 2015
Date of Patent:
December 13, 2016
Assignee:
Merck Sharp & Dohme
Inventors:
Amjad Ali, D. Jonathan Bennett, Jaiqiang Cai, Emma Carswell, Andrew Cooke, Scott B. Hoyt, Michael Lo, Clare London, John MacLean, Min K. Park, Paul Ratcliffe, Jerry Andrew Taylor, Brent Whitehead, Yusheng Xiong
Abstract: Methods are disclosed for increasing the yield and N-glycosylation site occupancy of paucimannose or complex N-glycans of recombinant glycoproteins produced in a recombinant host cell lacking dolichyl-P-Man:Man5GlcNAc2-PP-dolichyl alpha-1,3 mannosyltransferase (Alg3p) activity. In particular, the present invention provides recombinant host cells for producing recombinant glycoproteins that comprise a disruption of the expression of an OS-9 family gene in the host cell and which overexpress one or more Trypanosoma brucei STT3 proteins.
Abstract: The present invention relates to anti-TIGIT antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.
Type:
Application
Filed:
August 17, 2015
Publication date:
December 8, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Sybil M. G. Williams, Drake LaFace, Laurence Fayadat-Dilman, Gopalan Raghunathan, Linda Liang, Wolfgang Seghezzi
Abstract: 3,3?-Disubstituted indoline compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
Type:
Application
Filed:
October 6, 2014
Publication date:
December 8, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
JONATHAN E. WILSON, Petr Vachal, Ravi Kurukulasuriya
Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Application
Filed:
February 6, 2015
Publication date:
December 8, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Shawn Stachel, Daniel V. Paone, Jing Li, Anthony Ginnetti, Jianmin Fu, Shimin Xu
Abstract: The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.
Type:
Grant
Filed:
July 15, 2013
Date of Patent:
December 6, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Timothy A. Cernak, Kevin D. Dykstra, Dong-Ming Shen, Kun Liu, Andrew Stamford, John Qiang Tan
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.
Type:
Application
Filed:
February 6, 2015
Publication date:
December 1, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Santhosh F. Neelamkavil, Scott D. Edmondson, Zhuyan Guo, Alan W. Hruza, Zahid Hussain, Charles A. Lesburg, Remond Moningka, Anthony K. Ogawa, Rudrajit Mal
Abstract: The present invention is directed to compositions comprising an extrudate or solid solution of a compound, or a salt thereof, of Formula I (API): Formula I, wherein “Ra” is independently H or —F, in a water-soluble polymer matrix which further comprises a disintegration system allowing a tablet made therefrom to rapidly disintegrate in the environment in which the API is to be released.
Type:
Application
Filed:
January 30, 2015
Publication date:
December 1, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Mary Ann Johnson, Leonardo Resende Allain, W. Mark Eickhoff, Craig B. Ikeda, Chad D. Brown, Francis J. Flanagan, JR., Rebecca Nofsinger, Melanie Marota, Lisa Lupton, Paresh B. Patel, Hanmi Xi, Wei Xu
Abstract: The present disclosure is directed to disintegration systems for solid pharmaceutical dosage forms, which allow rapid disintegration of solid dosage forms that comprise solid dispersion formulations that include pharmaceutically active agents, polymers and optionally surfactants. The present disclosure is also directed to solid pharmaceutical dosage forms, such as tablets, comprising solid dispersion formulations and the disintegration systems, to methods for preparing the disintegration systems, and to methods for preparing the solid pharmaceutical dosage forms.
Type:
Application
Filed:
February 4, 2015
Publication date:
December 1, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Melanie J. Marota, Chad David Brown, Craig B. Ikeda, Mary Ann Johnson, Hanmi Xi, Wei Xu, Lixia Cai
Abstract: The present disclosure is directed to compositions comprising blended materials comprising a first solid dispersion formulation, which comprises an HCV NS3/NS4a protease inhibitor or a pharmaceutically acceptable salt thereof, one or more pharmaceutically acceptable polymers or a mixture thereof, and optionally one or more pharmaceutically acceptable surfactants or a mixture thereof; a second solid dispersion formulation, which comprises an HCV NS5a inhibitor or a pharmaceutically acceptable salt thereof, one or more pharmaceutically acceptable polymers or a mixture thereof; and optionally one or more pharmaceutically acceptable surfactants or a mixture thereof; and optionally one or more excipients. The present disclosure is also directed to oral dosage forms, such as tablets or capsules comprising the disclosed blended compositions comprising the disclosed solid dispersion formulations, and the methods for making these solid dispersion formulations and pharmaceutical compositions.
Type:
Application
Filed:
February 3, 2015
Publication date:
December 1, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Pavithra Sundararajan, Agam Sheth, Jesse Kuiper, Patrick Jules Marsac, Elise Miller, Justin David Moser, Adam Socia, Angela M. Wagner
Abstract: The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts thereof, that are potentially useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula I, to their possible use in the treatment of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.
Type:
Grant
Filed:
October 8, 2012
Date of Patent:
November 29, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Hong Shen, Jason M. Cox, Christine Yang, Zhicai Wu
Inventors:
Angela M. Amend Kwasnik, Benjamin R. Bartfeld, 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
Inventors:
Angela M. Amend Kwasnik, Benjamin R. Bartfeld, 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