Patents Assigned to Merck Sharp and Dohme
  • Inhibitors of Akt activity
    Patent number: 8614221
    Abstract: The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: December 24, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Weiming Fan, Thomas F. N. Haxell, Matthew G. Jenks, Nobuhiko Kawanishi, Shuliang Lee, Hao Liu, Michael J. Malaska, Joseph A. Moore, III, Yoshio Ogino, Yu Onozaki, Bharathi Pandi, Michael R. Peel, Toshihiro Sakamoto, Tony Siu
  • Fused tricyclic silyl compounds and methods of use thereof for the treatment of viral diseases
    Patent number: 8609635
    Abstract: The present invention relates to novel Fused Tricyclic Silyl Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, D, M1, X1 and X2 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Silyl Compound, and methods of using the Fused Tricyclic Silyl Compounds for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: March 4, 2011
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anilkumar Gopinadhan Nair, Kartik M. Keertikar, Seong Heon Kim, Joseph A. Kozlowski, Stuart Rosenblum, Oleg B. Selyutin, Michael Wong, Wensheng Yu, Qingbei Zeng
  • Thiazolyl mGluR5 antagonists and methods for their use
    Patent number: 8609852
    Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
    Type: Grant
    Filed: July 26, 2012
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph E. Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao
  • Fused Tricyclic Compounds as novel mTOR inhibitors
    Patent number: 8609675
    Abstract: The present invention provides Fused Tricyclic Compounds of the Formula (I) wherein Q, R1, R2, R3, and R4 are as defined herein, and pharmaceutically acceptable salts of such Fused Tricyclic Compounds. The Fused Tricyclic Compounds are useful in the treatment of cancer and other proliferative disorders.
    Type: Grant
    Filed: June 30, 2010
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Cliff C. Cheng, Hongbo Zeng, Gerald W. Shipps, Jr., Yongqi Deng, Zhaoyang Meng, Lianyun Zhao, Yang Nan, Binyuan Sun, Duan Liu, Panduranga A. Reddy, M. Arshad Siddiqui
  • Methods and compositions for RNA interference
    Patent number: 8609830
    Abstract: The invention provides methods and compositions for gene silencing by RNA interference. In particular, the invention provides methods for gene silencing or RNA knockdown using small interfering RNAs (siRNAs) having partial sequence homology to its target gene. The invention also provides methods for identifying common and/or differential responses to a plurality of different siRNAs targeting a gene. The invention also provides methods for evaluating the relative activity of the two strands of an siRNA. The invention further provides methods of designing siRNAs for gene silencing. The invention further provides methods of using siRNAs as therapeutics for treatment of diseases.
    Type: Grant
    Filed: May 17, 2004
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Aimee L. Jackson, Steven R. Bartz, Julja Burchard, Janell M. Schelter, Peter S. Linsley
  • Trifluoromethylsulfonamide gamma secretase inhibitor
    Patent number: 8609897
    Abstract: The present invention is directed to a novel trifluoromethylsulfonamide derivative which inhibits the processing of APP by the putative ?-secretase and thus is useful in the treatment or prevention of Alzheimer's disease. This compound possesses favorable pharmacokinetic properties in higher species (rhesus) and thus can be dosed on an intermittent dosing regiment (e.g., once weekly). When dosed on such a regiment the compound exhibits significant and continuous A? lowering without the manifestation of Notch associated gastrointestinal toxicity for extended periods, e.g., 7 days. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew Daniels, Jed Hubbs, Thomas Miller
  • 4, 5, 6-trisubstituted pyrimidine derivatives as factor IXa inhibitors
    Patent number: 8609676
    Abstract: The present invention relates to novel heterocyclic compounds of Formulae (I): (Chemical formula should be inserted here as it appears on abstract in paper form) Formula (I) as disclosed herein, or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme, Corp.
    Inventors: Mariappan V. Chelliah, Samuel Chackalamannil, William J. Greenlee, Keith Eagan, Zhuyan Guo, Martin C. Clasby, Yan Xia, Charles L. Jayne, Michael Dwyer, Kartik M. Keertikar, Tin-Yau Chan, Li Wang
  • Pyrrolidine derived beta 3 adrenergic receptor agonists
    Patent number: 8604038
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gergori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
  • Substituted bicyclic piperidinyl- and piperazinyl-sulfonamides useful to inhibit 11?-hydroxysteroid dehydrogenase type-1
    Patent number: 8604195
    Abstract: In its many embodiments, the present invention relates to a novel class of substituted bicyclic piperidinyl- and piperazinylsulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Unmesh Shah, Craig D. Boyle, Samuel Chackalamannil
  • Methods for treatment of polyposis
    Patent number: 8603465
    Abstract: The present invention relates to method for treating medical disorders mediated by mutations in the APC gene by administering an IGF1R inhibitor. Such disorders include, for example, familial adenomatous polyposis (FAP).
    Type: Grant
    Filed: August 6, 2007
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme, Corp.
    Inventor: Siu-Long Yao
  • Process for large scale production of plasmid DNA by fermentation
    Patent number: 8603798
    Abstract: The present invention relates generally to a method for increasing the yield of plasmid DNA production. The method includes the steps of selecting a highly productive clonal subtype of a strain of E. coli, including but not limited to the DH5 strain, harboring a DNA plasmid and cultivating said clonal subtype with fed-batch fermentation in a chemically-defined medium. The plasmid DNA production process described herein can generate record quantities of plasmid DNA when said highly productive clonal subtypes are cultivated on an industrial scale. The disclosed method can be used for the production of pharmaceutical grade DNA for use in polynucleotide vaccination and gene therapy treatment regimens.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michel Chartrain, Laura Kizer Bentley, Barbara Ann Krulewicz, Kristin M. Listner, Wen-jun Sun, Chanyong Brian Lee
  • Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors
    Patent number: 8603998
    Abstract: In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits.
    Type: Grant
    Filed: November 5, 2008
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Timothy J. Guzi, David A. Parry, Marc A. Labroli, Michael D. Dwyer, Kamil Paruch
  • USE OF IL-23 AND IL-17 ANTAGONISTS TO TREAT AUTOIMMUNE OCULAR INFLAMMATORY DISEASE
    Publication number: 20130323251
    Abstract: Novel methods and drug products for treating autoimmune ocular inflammatory disease are disclosed, which involve administration of agents that antagonize one or both of IL-17 and IL-23 activity.
    Type: Application
    Filed: August 6, 2013
    Publication date: December 5, 2013
    Applicants: The Government of the United States of America as represented by the Secretary of the Dep. of H.H.S., Merck Sharp & Dohme Corp.
    Inventors: Daniel J. Cua, Robert A. Kastelein, Van T. Tsai, Rachel Caspi, Phyllis Silver, Dror Luger
  • MODULATION OF PILR RECEPTORS TO TREAT SEPSIS
    Publication number: 20130323239
    Abstract: The present invention provides methods of using agonists and antagonists of PILR? and PILR?, respectively, to treat immune mediated sepsis. Also provided are methods of prophylactically treating with agonists and antagonists of PILR? and PILR?, respectively, to prevent the development of sepsis.
    Type: Application
    Filed: August 8, 2013
    Publication date: December 5, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Antara Banerjee, Paul G. Heyworth
  • MAMMALIAN CELL SURFACE ANTIGENS; RELATED REAGENTS
    Publication number: 20130324483
    Abstract: Purified genes encoding a T cell surface antigen from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this antigen are provided. Methods of using said reagents and diagnostic kits are also provided.
    Type: Application
    Filed: August 9, 2013
    Publication date: December 5, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Daniel M. Gorman, Troy D. Randall, Albert Zlotnik
  • USE OF MDL-1 ANTAGONISTS TO TREAT SPONDYLARTHROPATHY
    Publication number: 20130323246
    Abstract: The invention provides methods for treating spondylarthropathy with antagonists of MDL-1 alone or in combination with IL-23 antagonists.
    Type: Application
    Filed: February 14, 2012
    Publication date: December 5, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Daniel J. Cua, Barbara Joyce-Shaikh, Drake LaFace, Jonathan P. Sherlock
  • PROCESS FOR THE PREPARATION OF AN OREXIN RECEPTOR ANTAGONIST
    Publication number: 20130324728
    Abstract: The present invention is directed to processes for preparing a pyridyl piperidine compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.
    Type: Application
    Filed: October 24, 2011
    Publication date: December 5, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Yun Shao Feng, Anthony Moses, Yong-Li Zhong
  • CATHEPSIN CYSTEINE PROTEASE INHIBITORS
    Publication number: 20130324610
    Abstract: This invention relates to deuterated compounds which are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: February 9, 2012
    Publication date: December 5, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Kelem Kassahun, Christne Fandozzi, Donald R. Gauthier, Lisa A. Shipley
  • Process for preparing a 2-alkynyl substituted 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine
    Patent number: 8598343
    Abstract: A process for preparing 7-[2-[4-(6-fluoro-3-methyl-1,2-benzisoxazol-5-yl)-1-piperazinyl]ethyl]-2-(1-propynyl)-7H-pyrazolo-[4,3-e]-[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, intermediates useful in that process, and processes for preparing said intermediates are disclosed.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: December 3, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shen-Chun Kuo, Yonggang Chen, Jeffrey M. Eckert, William W. Leong, Nanfei Zou, Gabriel C. Kuklis
  • Anti-PCSK9 and methods for treating lipid and cholesterol disorders
    Patent number: 8598320
    Abstract: The present invention provides compositions and methods for treating disorders of cholesterol and lipid metabolism by administration of an anti-PCSK9 antibody or a peptide inhibitor of PCSK9.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: December 3, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph A. Hedrick, Frederick James Monsma, Jr., Tatyana Churakova, Diane Hollenbaugh