Patents Assigned to Merck Sharp
  • Factor IXa inhibitors
    Patent number: 8980916
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: March 17, 2015
    Assignees: Merck Sharp & Dohme Corp., Mochida Pharmaceutical Co., Ltd.
    Inventors: Matthew Voss, Hiroki Sone, Samuel Chackalamannil, Munetaka Ohkouchi
  • Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
    Patent number: 8980929
    Abstract: The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jacqueline D. Hicks, Tesfaye Biftu, Ping Chen, Xiaoxia Qian, Robert R. Wilkening
  • Extraction and diagnostic fluid devices, systems and methods of use
    Patent number: 8979770
    Abstract: The present invention provides devices, systems and methods for RNA isolation from biological samples containing white blood cells, such as whole blood. The devices have a device body that includes a first chamber having a first membrane that selectively binds white blood cells, a second chamber having a second membrane that reversibly binds RNA and a plurality of ports that are removably attached to a reagent pack and waste receptacle via a valving system controlled by a control unit.
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas L. Fare, Deborah A. Kessler, Kristopher A. Kilian
  • Antiviral compounds of three linked aryl moieties to treat diseases such as hepatitis C
    Patent number: 8980920
    Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Ether benzotriazole derivatives
    Patent number: 8975286
    Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: August 16, 2010
    Date of Patent: March 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek
  • Aryloxmethyl cyclopropane derivatives as PDE10 inhibitors
    Patent number: 8975261
    Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: March 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
  • Formulations for cathepsin K inhibitors
    Patent number: 8975296
    Abstract: The instant invention relates to pharmaceutical compositions containing cathespin K inhibitors. Also disclosed are processes for making said pharmaceutical compositions.
    Type: Grant
    Filed: March 20, 2013
    Date of Patent: March 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haihong Fan, Majid Mahjour, Justin Moser, Bhagwant Rege
  • Inhibitors of catechol O-methyl transferase and their use in the treatment of psychotic disorders
    Patent number: 8969364
    Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: March 3, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, Scott T. Harrison, James C. Barrow, Zhijian Zhao, Jeffrey Melamed, Nathan R. Kett, Amy Zartman
  • Cycloalkylnitrile pyrazole carboxamides as janus kinase inhibitors
    Patent number: 8962608
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: February 24, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason Brubaker, Christopher Dinsmore, Dawn Marie Hoffman, Joon Jung, Duan Liu, Scott Peterson, Tony Siu, Luis E. Torres, Hongjun Zhang, Zhongyong Wei, Feng Shi
  • Substituted imidazopyridines as HDM2 inhibitors
    Patent number: 8962611
    Abstract: The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: February 24, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew P. Christopher, Francesc Xavier Fradera Llinas, Michelle Machacek, Michelle Martinez, Michael Hale Reutershan, Manami Shizuka, Binyuan Sun, Christopher Francis Thompson, B. Wesley Trotter, Matthew E. Voss, Michael D. Altman, Stephane L. Bogen, Ronald J. Doll
  • PREDICTIVE BIOMARKER USEFUL FOR CANCER THERAPY MEDIATED BY A CDK INHIBITOR
    Publication number: 20150051227
    Abstract: The present invention provides a predictive biomarker whose expression level is useful for identifying patients responsive to a therapeutically effective dose of a CDK inhibitor. In one embodiment of the invention, the predictive biomarker is the ratio of MCL-1 to BCL-xL (MCL-1:BCL-xL ratio) and the CDK inhibitor is SCH 927965 (Dinaciclib).
    Type: Application
    Filed: March 27, 2013
    Publication date: February 19, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Robert Nolan Booher, Heather A. Hirsch, Leigh Scott Zawel, Stephen Eric Fawell
  • Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
    Patent number: 8957062
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: February 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
  • Pyrazolopyrimidine PDE 10 inhibitors
    Patent number: 8957077
    Abstract: The present invention is directed to pyrazolopyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: September 26, 2011
    Date of Patent: February 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, Izzat T. Raheem, John D. Schreier
  • SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF
    Publication number: 20150045346
    Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Application
    Filed: June 27, 2012
    Publication date: February 12, 2015
    Applicants: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS INC.
    Inventors: Tong-Shuang Li, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • VACCINES AGAINST CLOSTRIDIUM DIFFICILE COMPRISING RECOMBINANT TOXINS
    Publication number: 20150044250
    Abstract: The present invention relates to recombinant C. difficile toxin A (TcdA) and toxin B (TcdB) and binary toxin A (CDTa) proteins comprising specifically defined mutations relative to the native toxin sequence that substantially reduce or eliminate toxicity. The invention also relates to vaccines and immunogenic compositions comprising these recombinant toxins, as well as combinations of these toxins with binary toxin B (CDTb), which are capable of providing protection against C. difficile infection and/or the effects thereof. The invention also relates to methods of inducing an immune response to C. difficile comprising administering the vaccines and immunogenic compositions described herein to a patient. The invention also encompasses methods of expressing recombinant C. difficile toxin A and toxin B and CDTa mutants and CDTb in recombinant expression systems.
    Type: Application
    Filed: January 25, 2013
    Publication date: February 12, 2015
    Applicants: Intervet Inc., Merck Sharp & Dohme Corp.
    Inventors: Jon Henry Heinrichs, Jean-Luc Bodmer, Susan Lynn Secore, Aaron Rudy Goerke, Ivette Caro-Aguilar, Marie-Pierre Gentile, Melanie S. Horton, Matthew Ryan Miezeiewski, Julie M. Skinner, Paulus Jacobus Antonius Sondermeijer, Shyamsundar Subramanian, Karin Huberdina Antonia van der Heijden-Liefkens, Su Wang, Jinfu Xie, Rachel Flora Xoconostle, Julie K. Zorman
  • Amino-heteroaryl derivatives as HCN blockers
    Patent number: 8952001
    Abstract: The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Simon James Anthony Grove, Angus John Morrison, Craig Jamieson, Ronald Palin, John Kinnaird Ferguson Maclean
  • Substituted 1,3-benzothiazol-2(3H)-ones and [1,3]thiazolo[5,4-B]pyridin-2(1H)-ones as positive allosteric modulators of mGluR2
    Patent number: 8952005
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark E. Layton, Michael J. Kelly, III
  • Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 8951965
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: June 2, 2014
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 8952166
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Fa-Xiang Ding, Shuzhi Dong, Jessica Frie, Xin Gu, Jinlong Jiang, Alexander Pasternak, Haifeng Tang, Zhicai Wu, Yang Yu, Takao Suzuki
  • Mammalian expression vector pUHAB
    Patent number: 8951790
    Abstract: The present invention relates to the construction and utilization of a new mammalian expression vector that contains a unique multiple cloning site (MCS), designated pUHAB. The pUHAB vector comprises a high copy replication origin (ColE1), a drug resistance gene (TK-Hygromycin), and a human cytomegalovirus promoter operably associated with a unique intron (hCMV/intron). Further, pUHAB comprises a selectable marker conferring resistance to kanamycin in bacterial cells, and a phage f1(+) region. pUHAB can be used to transiently or stably express cloned genes when transfected into mammalian cells. The invention also encompasses kits and host cells and cell lines comprising pUHAB, and methods of producing a recombinant protein using pUHAB.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Deba P. Saha