Abstract: Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
Type:
Application
Filed:
August 8, 2016
Publication date:
February 16, 2017
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Petr Vachal, Izzat Raheem, Zhiqiang Guo, Timothy John Hartingh
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:
April 21, 2015
Publication date:
February 16, 2017
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Yeon-Hee Lim, Zhuyan Guo, Amjad Ali, Scott D. Edmondson, Weiguo Liu, Giocanda V. Gallo-Etienne, Heping Wu, Ying-Duo Gao, Andrew W. Stamford, Younong Yu, Nancy J. Kevin, Rajan Anand, Deyou Sha, Santhosh F. Neelamkavil, Zahid Hussain, Puneet Kumar, Remond Moningka, Joseph L. Duffy, Jiayi Xu, Yu Jiang, Anjan Chakrabarti, Hiroki Sone
Abstract: This invention relates to triazolopyridyl 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 19, 2015
Date of Patent:
February 14, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
D. Jonathan Bennett, Jaiqiang Cai, Emma Carswell, Andrew Cooke, Scott B. Hoyt, Clare London, John MacLean, Paul Ratcliffe, Jerry Andrew Taylor, Yusheng Xiong, Swapan Kumar Samanta, Bheemashankar A. Kulkarni
Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.
Type:
Application
Filed:
September 16, 2016
Publication date:
February 9, 2017
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
Abstract: In its many embodiments, the present invention provides certain iminothiadiazepane dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
Type:
Application
Filed:
December 16, 2014
Publication date:
February 9, 2017
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
Xing Dai, Jared N. Cumming, Jack D. Scott, Hong Liu, Anandan Palani
Abstract: In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists ofCGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
Type:
Application
Filed:
October 14, 2016
Publication date:
February 2, 2017
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
Abstract: The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A?, R2 R3, R4 and R are as defined herein. The present invention also relates to compositions comprising at least one Heterocycle-Substituted Tetracyclic Compound, and methods of using the Heterocycle-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient.
Type:
Grant
Filed:
December 31, 2013
Date of Patent:
January 31, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Wensheng Yu, Ling Tong, Joseph A. Kozlowski, Oleg Selyutin, Lei Chen, Jae-Hun Kim, Deyou Sha, Razia Rizvi, Bandarpalle Shankar
Abstract: The present invention is directed to piperidinyloxy lactone compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyloxy lactone 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 pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Abstract: The invention relates generally to methods for purifying a Fc-fusion protein produced in a eukaryotic expression system. More specifically, the invention provides a robust and scalable downstream purification process suitable for use in manufacturing TNFR:Fc for human administration which comprises an optimized Protein A affinity chromatography step and two ion exchange chromatography steps both of which are operated in the bind-and-elute mode.
Type:
Grant
Filed:
July 3, 2012
Date of Patent:
January 31, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Joseph Nti-Gyabaah, Ijeoma Ikechukwu, Matthew Pettroff, Christine Cho Lee
Abstract: The present invention is directed to 2-pyridyloxy-4-ester compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ester 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 pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Abstract: The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
Type:
Grant
Filed:
June 25, 2013
Date of Patent:
January 31, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Craig A. Coburn, Milana Maletic, Richard Soll, Chunsing Li, Yunfu Luo, Zhiqi Qi
Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
Type:
Grant
Filed:
August 14, 2013
Date of Patent:
January 31, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Kenneth J. Barr, Corey E. Bienstock, John K. Maclean, Hongjun Zhang, Richard T. Beresis, Neville J. Anthony, Blair T. Lapointe, Nunzio Sciammetta
Abstract: A mixing apparatus (1) for mixing slaughter offal with a preservative agent, the apparatus comprising an offal collection tank (3) with a bottom (4) provided with a discharge opening (5) connectable to a closable discharge, an agitator (8) extending into the offal collection tank, and a pump unit (9) operatively connectable to the discharge, wherein the apparatus further comprises a preservative reservoir (7) mounted on top of the collection tank (3). A collection and preservation system is provided, wherein the addition of preservation agent can be strictly controlled, can easily and quickly be installed and connected when it is to be used. After use, the system is easily removed and cleaned.
Type:
Application
Filed:
February 25, 2016
Publication date:
January 26, 2017
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Adolph Bartholomeus Gijtenbeek, Harry van Tuijn, Marinus Johannes Gerardus Maria Ploegmakers
Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
Type:
Grant
Filed:
June 19, 2014
Date of Patent:
January 24, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Shuwen He, Zhong Lai, Xing Dai, Dong Xiao, Clare London, Nicolas Zorn, Ravi Nargund, Anandan Palani, Casey C. McComas, Peng Li, Xuanjia Peng, Richard Soll
Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
Type:
Grant
Filed:
August 16, 2012
Date of Patent:
January 24, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Casey C. McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
Abstract: The present invention is directed to 4-fluoropiperidine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Type:
Grant
Filed:
January 13, 2014
Date of Patent:
January 24, 2017
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Andrew Cooke, Scott D. Kuduk, Craig Stump, Peter Williams
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