Patents Assigned to Merck Sharp & Dohme
  • Patent number: 9511052
    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
  • Publication number: 20160347757
    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
  • Publication number: 20160346214
    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
  • Publication number: 20160346198
    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
  • Publication number: 20160346289
    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
  • Patent number: 9505730
    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
  • Patent number: 9504690
    Abstract: The present invention relates to novel Tetracyclic Xanthene Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b and R2 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Xanthene Derivative, and methods of using the Tetracyclic Xanthene Derivatives for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: November 29, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Stuart B. Rosenblum, Joseph A. Kozlowski, Richard Soll, Hao Wu, Bin Hu, Bin Zhong, Dahai Wang, Changmao Shen, Fei Sun
  • Patent number: 9505739
    Abstract: The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: November 29, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Hao Wu
  • Publication number: 20160339074
    Abstract: The present invention is directed to compositions comprising the HCV NS3/4A inhibitor, (1aR,5S,8S,10R,22aR)-5-tert-butyl-N-{(1R,2S)-1-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopro-pyl}-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxa-diazacyclononadecino[11,12-b]quinoxaline-8-carboxamide, or a pharmaceutically acceptable salt thererof, an oral absorption enhancing polymer, and, optionally, a surfactant. The present invention is also directed to solid dispersions and pharmaceutical compositions containing or made from these compositions, and the methods for making these solid dispersions and pharmaceutical compositions.
    Type: Application
    Filed: February 3, 2015
    Publication date: November 24, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Melanie J. Marota, Craig McKelvey, Nicholas Birringer, Jesse Kuiper, Paul A. Harmon, Adam J. Socia, Patrick Jules Marsac, Stephen L. Conway
  • Publication number: 20160340315
    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: November 24, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Santhosh F. Neelamkavil, Scott D. Edmondson, Zhuyan Guo, Alan W. Hruza, Zahid Hussain, Remond Moningka, Nancy Jo Kevin
  • Patent number: 9499545
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP 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: Grant
    Filed: September 12, 2014
    Date of Patent: November 22, 2016
    Assignee: 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
  • Patent number: 9499541
    Abstract: The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP 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: Grant
    Filed: October 2, 2014
    Date of Patent: November 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman, Heather E. Stevenson
  • Patent number: 9499502
    Abstract: The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be useful as BACE inhibitors and/or 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 uses, including Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: April 12, 2012
    Date of Patent: November 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wen-Lian Wu, Duane A. Burnett, Andrew W. Stamford, Jared N. Cumming, Chad E. Bennett, Eric J. Gilbert, Jack D. Scott, Younong Yu, Xuanjia Peng
  • Patent number: 9499534
    Abstract: The invention provides certain thiazole-substituted aminopyrimidine compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, and the subscripts r, s, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Grant
    Filed: April 22, 2014
    Date of Patent: November 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth L. Arrington, Byron DuBois, John S. Debenham, Ping Liu, Alan B. Northrup, Jason W. Szewczyk, Liping Wang, Ming Wang
  • Publication number: 20160333021
    Abstract: The present invention relates to compounds of formula (I) that are metallo-?-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with ?-lactam antibiotics for overcoming resistance.
    Type: Application
    Filed: January 16, 2015
    Publication date: November 17, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mihir Mandal, Haifeng Tang, Li Xiao, Jing Su, Guoqing Li, Shu-Wei Yang, Weidong Pan, Haiqun Tang, Reynalda DeJesus, Jacqueline Hicks, Matthew Lombardo, Hong Chu, William Hagmann, Alex Pasternak, Xin Gu, Jinlong Jiang, Shuzhi Dong, Fa-Xiang Ding, Clare London, Dipshikha Biswas, Katherine Young, David N. Hunter, Zhiqiang Zhao, Dexi Yang
  • Patent number: 9493400
    Abstract: This invention relates to a resolution process for the preparation of fluoroleucine alkyl esters.
    Type: Grant
    Filed: March 25, 2013
    Date of Patent: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nelo Rivera, Yadagiri R. Pendri, Sreenivas Mende, Bramhananda N. Reddy
  • Patent number: 9493461
    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: February 3, 2014
    Date of Patent: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Hong Liu, Anandan Palani, Shuwen He, Zhong Lai, Ravi Nargund, Karen Marcantonio, Dong Xiao, Linda L. Brockunier, Nicolas Zorn, Qun Dang, Xuanjia Peng, Peng Li
  • Patent number: 9493440
    Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. 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 LRRK-2 kinase is involved.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Wei Li, Andrew Stamford, Marc Poirer, Paul Tempest
  • Patent number: D773646
    Type: Grant
    Filed: August 27, 2014
    Date of Patent: December 6, 2016
    Assignee: Merck Sharp & Dohme Corp
    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
  • Patent number: D773647
    Type: Grant
    Filed: August 27, 2014
    Date of Patent: December 6, 2016
    Assignee: Merck Sharp & Dohme Corp.
    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