Patents Assigned to Merck Sharp and Dohme
  • PYRIDONE DERIVATIVES
    Publication number: 20120316200
    Abstract: The present invention is directed to novel phenylpyridone derivative compounds. The compounds act as a melanin concentrating hormone receptor antagonists, and can be useful in preventing, treating or acting as a remedial agent for various circular system diseases, nervous system diseases, metabolic diseases, genital diseases, respiratory diseases and digestive diseases.
    Type: Application
    Filed: April 7, 2011
    Publication date: December 13, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Linus S. Lin, Richard Soll, Jingchao Dong, Hao Wu, Takao Suzuki, Bin Hu, Dejun Liu, Jinglai Hao, Ming Xu
  • Inhibitors of janus kinases and/or 3-phosphoinositide-dependent protein kinase-1
    Patent number: 8329722
    Abstract: The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer.
    Type: Grant
    Filed: March 10, 2008
    Date of Patent: December 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tony Siu, Jonathan Young, Michael Altman, Alan Northrup, Ekaterina Kozina, Christopher Dinsmore, David J. Guerin, Kevin A. Keenan, Joon O. Jung, Solomon Kattar, Rachel N. MacCoss
  • Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
    Patent number: 8329905
    Abstract: This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: December 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kelvin H. Yong, Ilia A. Zavialov, Jianguo Yin, Xiaoyong Fu, Thiruvettipuram K. Thiruvengadam
  • Imidizo[1,2-A]pyrazines useful as AHCY hydrolase inhibitors
    Patent number: 8329697
    Abstract: The present invention is directed to AHCY inhibitors of formula (I) which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: December 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert M. Garbaccio, Antonella Converso, Mark E. Fraley, Timothy J. Hartingh
  • Cyclic benzimidazole derivatives useful as anti-diabetic agents
    Patent number: 8329914
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: December 11, 2012
    Assignees: Merck Sharp & Dohme Corp, Metabasas Therapeutics, Inc.
    Inventors: Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka, Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion
  • Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
    Patent number: 8324384
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: February 3, 2010
    Date of Patent: December 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
  • Biaryl-spiroaminooxazoline analogues as alpha 2C adrenergic receptor modulators
    Patent number: 8324213
    Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: October 6, 2009
    Date of Patent: December 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Youngong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
  • Substituted imidazoles as bombesin receptor subtype-3 modulators
    Patent number: 8318767
    Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: November 27, 2012
    Assignees: Merck Sharp & Dohme Corp, Albany Molecular Research, Inc.
    Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Jian Liu, Michael M.-C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
  • Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
    Patent number: 8318667
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type (2) diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: February 15, 2010
    Date of Patent: November 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Libo Xu, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
  • Substituted aryl and heteroaryl derivatives, compositions containing such compounds and methods of use
    Patent number: 8318760
    Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: November 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John E. Stelmach, Keith G. Rosauer, Emma R. Parmee, James R. Tata
  • Pyrimidinone derivatives and methods of use thereof
    Patent number: 8318751
    Abstract: The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disease, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: November 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig D. Boyle, Samuel Chackalamannil, Claire M. Lankin, Unmesh G. Shah, Bernard R. Neustadt, Hong Liu, Andrew W. Stamford
  • Cathepsin cysteine protease inhibitors
    Patent number: 8318748
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: November 27, 2012
    Assignees: Merck, Sharp & Dohme Corp., Axys Pharmaceuticals, Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
  • 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors
    Patent number: 8318735
    Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: November 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gerald W. Shipps, Jr., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Lianyun Zhao, Shuyi Tang, Tzu T. Wong, Praveen K. Tadikonda, Luis E. Torres, M. Arshad Siddiqui, Michael P. Dwyer, Kartik M. Keertikar, Timothy J. Guzi
  • HCV NS3 protease inhibitors
    Patent number: 8309540
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: October 22, 2007
    Date of Patent: November 13, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel J. Liverton, Joseph P. Vacca, John A. McCauley, Joseph J. Romano, Michael T. Rudd
  • Spiroindalones
    Patent number: 8309544
    Abstract: The present invention relates to spiroindalone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: May 12, 2008
    Date of Patent: November 13, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joan M. Fletcher, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
  • Engineered anti-IL-23R antibodies
    Patent number: 8309085
    Abstract: Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: November 13, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Leonard G. Presta
  • Compositions and methods for short interfering nucleic acid inhibition of Na1.8
    Patent number: 8309703
    Abstract: The invention provides short interfering nucleic acids, either single-stranded or double-stranded, that cause RNAi-induced degradation of mRNA from the Nav1.8 sodium channel gene; to pharmaceutical compositions comprising such short interfering nucleic acids; recombinant vectors comprising such short interfering nucleic acids; a method for inhibiting translation of an mRNA; a method for inhibiting expression of a polypeptide; a method for blocking the membrane potential in a cell; a method for blocking the sodium current in a cell; and a method for inhibiting chronic pain.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: November 13, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sameer Goregaoker, John C. Hunter, Tony Priestley
  • Efficient production of heterologous proteins using mannosyl transferase inhibitors
    Patent number: 8309325
    Abstract: Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidinediones inhibitors of Pmt-mediated O-linked glycosylation.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: November 13, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ranjit Desai, Lihu Yang
  • Substituted aryl sulfone derivatives as calcium channel blockers
    Patent number: 8304434
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Grant
    Filed: September 30, 2008
    Date of Patent: November 6, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Prasun K. Chakravarty, Yanbing Ding, Joseph L. Duffy, Hassan Pajouhesh, Pengcheng Patrick Shao, Sriram Tyagarajan, Feng Ye
  • Hexahydrocyclopentyl[f]indazole sulfonamides and derivatives thereof as selective glucocorticoid receptor modulators
    Patent number: 8299048
    Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: February 24, 2009
    Date of Patent: October 30, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell