Abstract: The instant invention relates to liquid pharmaceutical compositions containing CGRP receptor antagonists. The CGRP receptor antagonist liquid pharmaceutical compositions of the instant invention are alcohol-free, low volume liquid pharmaceutical compositions that can be taken without water for the treatment of migraine headache.
Type:
Application
Filed:
September 10, 2018
Publication date:
March 7, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Majid Mahjour, Leonardo R. Allain, Sutthilug Sotthivirat, Russell G. Maus, Rebecca Nofsinger, Lisa Lupton, Wei Xu, Francis Flanagan
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 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 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 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: 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: 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: Described herein are crystalline forms of a compound of formula (II?), including toluene solvates off A TD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane. Provided herein is a crystalline form of a compound of formula (II?): wherein X is CI, Br, or I; and R1 and R2 are each independently an oxygen protecting group; processes for making the crystalline form, and use of said form in the synthesis of antibacterial cephalosporins such as ceftolozane.
Type:
Grant
Filed:
August 14, 2015
Date of Patent:
March 5, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Kristos Adrian Moshos, Valdas Jurkauskas, Giovanni Fogliato, Manuel Scanu, You Seok Hwang
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: 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 a pharmaceutically acceptable salt thereof, 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 a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
May 23, 2016
Date of Patent:
February 26, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Joie Garfunkle, Olga Ornoski, Dann L. Parker, Jr., Subharekha Raghavan, Libo Xu, Zhiqiang Yang
Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.
Type:
Grant
Filed:
December 17, 2015
Date of Patent:
February 26, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jian Liu, Joseph A. Kozlowski, Sobhana Babu Boga, Xiaolei Gao, Deodial Guy Guiadeen, Jiaqiang Cai, Shilan Liu, Dahai Wang, Hao Wu, Chundao Yang
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:
Grant
Filed:
October 24, 2016
Date of Patent:
February 26, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jiayi Xu, Amjad Ali, Wei Zhou, Ying-Duo Gao, Scott D. Edmondson, Eric Mertz, Santhosh F. Neelamkavil, Weiguo Liu, Wanying Sun, Dong-Ming Shen, Bart Harper, Cheng Zhu, Thomas Bara, Yeon-Hee Lim, Meng Yang
Abstract: An inertion funnel includes a hollow ring with an attachment point on an outside edge and a plurality of output apertures on the inside edge allows for an even flow of gas around the circumference of the ring and through the output apertures into a filter funnel below. The attachment point allows the attachment of a hose or other fitting through which gas flows into the hollow ring, which rests above and around the opening of the filter funnel. On the inside of the ring, an angled downward opening allows gas to flow out of the ring and into the filter funnel. Uniformly distributed around the opening are vanes that direct the flow of gas from the ring into the filter funnel below.
Type:
Grant
Filed:
August 20, 2018
Date of Patent:
February 26, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Matthew Franklin Hagan, Mark Dennis Weisel
Abstract: The present invention is directed to hydroxymethyl piperidine 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:
November 30, 2015
Date of Patent:
February 26, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Nigel Liverton, Yunfu Luo
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
Abstract: The present invention relates to processes for the preparation of N-protected 4-((2S,5R)-5-((benzyloxy)amino)piperidine-2-carboxamido)piperidine-1-carboxylates. 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.
Abstract: Methods for display of recombinant whole immunoglobulins or immunoglobulin libraries on the surface of eukaryote host cells, including yeast and filamentous fungi, are described. The methods are useful for screening libraries of recombinant immunoglobulins in eukaryote host cells to identify immunoglobulins that are specific for an antigen of interest.
Type:
Application
Filed:
October 3, 2018
Publication date:
February 21, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Bianka Prinz, Natarajan Sethuraman, Dongxing Zha, Stefan Wildt, Piotr Bobrowicz
Abstract: Disclosed are formulations and tablets made therefrom comprising the compound of Formula IA or Formula IB which have sustained-release properties, and the dispersion containing the compounds of Formula IA or IB which facilitates such sustained release: Formula IA, Formula IB.