Patents Assigned to Merck Sharp
  • Prolylcarboxypeptidase inhibitors
    Patent number: 8921394
    Abstract: Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: December 30, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Dong-Ming Shen, Min Shu
  • Substituted-1,3,8-triazaspiro[4.5]decane-2,4-diones
    Patent number: 8921555
    Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: December 30, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
  • INHIBITORS OF HEPATITIS C VIRUS REPLICATION
    Publication number: 20140371138
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, John A. McCauley, Steven W. Ludmerer, Kun Liu, Joseph P. Vacca, Hao Wu, Bin Hu, Richard Soll, Fei Sun, Xinghai Wang, Man Yan, Chengren Zhang, Mingwei Zheng, Bin Zhong, Jian Zhu
  • Piperidinone carboxamide azaindane CGRP receptor antagonists
    Patent number: 8912210
    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: November 10, 2011
    Date of Patent: December 16, 2014
    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
  • Pyrimidine ether derivatives and methods of use thereof
    Patent number: 8912206
    Abstract: The present invention relates to Pyrimidine Ether Derivatives, compositions comprising a Pyrimidine Ether Derivative, and methods of using the Pyrimidine Ether Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: December 16, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Santhosh Francis Neelamkavil, Andrew Stamford, Samuel Chackalamannil, William J. Greenlee
  • Bicyclic heterocycle derivatives and their use as modulators of the activity of GPR119
    Patent number: 8907095
    Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
    Type: Grant
    Filed: October 20, 2008
    Date of Patent: December 9, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yan Xia, Craig D. Boyle, William J. Greenlee, Samuel Chackalamannil, Charles Lee Jayne
  • Fused bicyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors
    Patent number: 8907086
    Abstract: The present invention is directed to novel bicyclic heterocycles 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: March 1, 2012
    Date of Patent: December 9, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Chad E. Bennett, Duane A. Burnett, Hongmei Li, Yonggang Chen, Troy McCracken, Monica Vicarel
  • Fused tricyclic compounds as mTOR inhibitors
    Patent number: 8901142
    Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine and dipyrazolopyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine or dipyrazolopyrimidine compounds.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: December 2, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoyang Meng, M. Arshad Siddiqui, Panduranga Adulla P. Reddy, Mehul F. Patel, Yang Nan
  • Tricyclic indole derivatives and methods of use thereof
    Patent number: 8901139
    Abstract: The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: December 2, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Srikanth Venkatraman, Anilkumar Gopinadhan Nair, Kevin X. Chen, Francisco Velazquez, Qingbei Zeng, Duan Liu, Yueheng Jiang, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Stephen J. Gavalas, Patrick A. Pinto, Oleg B. Selyutin, Bancha Vibulbhan
  • Antibodies to human programmed death receptor PD-1
    Patent number: 8900587
    Abstract: Antibodies which block binding of hPD-1 to hPD-L1 or hPD-L2 and their variable region sequences are disclosed. A method of increasing the activity (or reducing downmodulation) of an immune cell through the PD-1 pathway is also disclosed.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: December 2, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregory John Carven, Hans Van Eenenneem, Gradus Johannes Dulos
  • Drug delivery system
    Patent number: 8900615
    Abstract: The subject invention provides a drug delivery system comprising at least one compartment consisting of (i) a drug-loaded thermoplastic polymer core, (ii) a drug-loaded thermoplastic polymer intermediate layer and (iii) a non-medicated thermoplastic polymer skin covering the intermediate layer, wherein said intermediate layer is loaded with (a) crystals of a first pharmaceutically active compound and with (b) a second pharmaceutically active compound in dissolved form and wherein said core is loaded with said second compound in dissolved form.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: December 2, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Rudolf Johannes Joseph Groenewegen, Wouter de Graaff
  • ILT3 binding molecules and uses therefor
    Patent number: 8901281
    Abstract: The present invention provides binding molecules that specifically bind to ILT3, e.g., human ILT3 (hILT3), on antigen presenting cells, such as for example, monocytes, macrophages and dendritic cells (DC), e.g., monocyte-derived dendritic cells (MDDC). Various aspects of the invention relate to binding molecules, and pharmaceutical compositions thereof. Methods of using the binding molecules of the invention to detect human ILT3 or to modulate human ILT3 activity, either in vitro or in vivo, are also encompassed by the invention.
    Type: Grant
    Filed: June 19, 2006
    Date of Patent: December 2, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul Ponath, Patricia Rao, Michael Rosenzweig, L. Mary Smith, Jose F. Ponte
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 8901087
    Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: November 8, 2011
    Date of Patent: December 2, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiang Chang, Kun Liu, Ernest J. McEachern, Changwei Mu, Harold G. Selnick, Feng Shi, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou, Yongbao Zhu
  • PYRROLOPYRIMIDINES AS JANUS KINASE INHIITORS
    Publication number: 20140349998
    Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 27, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sean P Ahearn, Matthew Christopher, Christopher Dinsmore, Joon Jung, Qinglin Pu, Alexey Rivkin, Mark E. Scott, David J. Witter, Hyun Chong Woo, Brandon Cash
  • ANTI-GITR ANTIBODIES
    Publication number: 20140348841
    Abstract: Antibodies to human GITR are provided, as well as uses thereof, e.g., in treatment of proliferative and immune disorders.
    Type: Application
    Filed: April 24, 2014
    Publication date: November 27, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Xiao Min Schebye, Grigori P. Ermakov, Douglas J. Hodges, Leonard G. Presta
  • IMIDAZOPYRIDIN-2-ONE DERIVATIVES
    Publication number: 20140350002
    Abstract: The present invention is directed to imidazopyridin-2-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: Application
    Filed: June 14, 2012
    Publication date: November 27, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Hannah D. Fiji, Michael J. Kelly, III, Jeffrey C. Kern, Mark E. Layton, Joseph E. Pero, Alexander J. Reif, Michael A. Rossi
  • SUBSTITUTED PYRIMIDINES
    Publication number: 20140349972
    Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Application
    Filed: September 19, 2012
    Publication date: November 27, 2014
    Applicant: MERCK SHARP & DOHME CORP
    Inventors: Qun Dang, Changyou Zhou, Wuxin Zou, Yuxia Hua
  • Fused heterocyclic indane carboxamide CGRP receptor antagonists
    Patent number: 8895572
    Abstract: The present invention is directed to fused heterocyclic indane carboxamide 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: December 16, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Anthony Ginnetti, Daniel V. Paone
  • Soluble guanylate cyclase activators
    Patent number: 8895583
    Abstract: This inventions relates to compounds having the structure Formula I and pharmaceutically acceptable salts thereof which are soluble guanylate cyclase activators. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Q. Tan, Ronald M. Kim, John W. Mirc
  • Crystalline forms of a dipeptidyl peptidase-IV inhibitor
    Patent number: 8895603
    Abstract: Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
    Type: Grant
    Filed: June 25, 2012
    Date of Patent: November 25, 2014
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.
    Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang