Patents Assigned to Merck Sharp
  • Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 8415297
    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: February 17, 2012
    Date of Patent: April 9, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber
  • Cyclic benzimidazole derivatives useful as anti-diabetic agents
    Patent number: 8410284
    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 12, 2009
    Date of Patent: April 2, 2013
    Assignees: Merck Sharp & Dohme Corp, Metabasis Therapeutics, Inc.
    Inventors: Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka, Brett C. Bookser
  • Bicyclic heterocycle derivatives and methods of use thereof
    Patent number: 8410122
    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 a GPCR in a patient.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: April 2, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew Stamford, Hong Liu
  • Bipyridine carboxamide orexin receptor antagonists
    Patent number: 8410142
    Abstract: The present invention is directed to bipyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.
    Type: Grant
    Filed: February 29, 2008
    Date of Patent: April 2, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
  • Hexahydro-1H-4,7-methanoisoindole-1,3-dione compounds
    Patent number: 8410111
    Abstract: The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction.
    Type: Grant
    Filed: August 21, 2012
    Date of Patent: April 2, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Kausik K. Nanda, B. Wesley Trotter
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 8404856
    Abstract: Heteroaromatic compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein ring A is: (ii-a), (ii-b), (ii-c), (ii-d), or (ii-e); and wherein n, L, M, U, X, Y, Z, RE, RF, R1, R2A, R2B, R2C, R3, R8, R9 and R10 are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts and prodrugs are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts and prodrugs can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: March 26, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas J. Tucker, Robert Tynebor, John T. Sisko, Neville Anthony, Robert Gomez, Samson M. Jolly
  • Engineered anti-IL-23P19 antibodies
    Patent number: 8404813
    Abstract: Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
    Type: Grant
    Filed: February 21, 2011
    Date of Patent: March 26, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Leonard G. Presta
  • 2,3-substituted azaindole derivatives for treating viral infections
    Patent number: 8404845
    Abstract: The present invention relates to 2,3-Substituted Azaindole Derivatives, compositions comprising at least one 2,3-Substituted Azaindole Derivatives, and methods of using the 2,3-Substituted Azaindole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: March 26, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Srikanth Venkatraman, F. George Njoroge, Joseph A. Kozlowski
  • METHOD FOR PREPARING ANTIBODIES HAVING IMPROVED PROPERTIES
    Publication number: 20130071390
    Abstract: The present invention is directed to methods and compositions for the production of Fc-containing polypeptides having improved properties and comprising mutations at positions 243 and 264 of the Fc region.
    Type: Application
    Filed: May 25, 2011
    Publication date: March 21, 2013
    Applicant: MERCK, SHARP & DOHME CORP
    Inventors: Terrance A. Stadheim, Dongxing Zha, Liming Liu
  • Macrocyclic spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease
    Patent number: 8399473
    Abstract: The present invention is directed to 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 2, 2007
    Date of Patent: March 19, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Philippe G Nantermet, M. Katharine Holloway, Keith P. Moore, Shaun R. Stauffer
  • 2,5-disubstituted phenyl carboxamide orexin receptor antagonists
    Patent number: 8399494
    Abstract: The present invention is directed to 2,5-disubstituted phenyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.
    Type: Grant
    Filed: October 26, 2009
    Date of Patent: March 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeffrey M. Bergman, Paul J. Coleman, Anthony J. Roecker, John D. Schreier
  • Antidiabetic tricyclic compounds
    Patent number: 8399507
    Abstract: Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: March 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gui-Bai Liang, Xibin Liao, Weiguo Liu, Paul E. Finke, Dooseop Kim, Lihu Yang, Songnian Lin
  • Acyl bipiperidinyl compounds useful as GPR 119 agonists
    Patent number: 8399485
    Abstract: Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: December 10, 2007
    Date of Patent: March 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harold B. Wood, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang, Ralph T. Mosley
  • Methods of using MIR34 as a biomarker for TP53 functional status
    Patent number: 8399248
    Abstract: In one aspect, the invention generally relates to use of miR-34 as a biomarker to estimate TP53 function in a cell. In another aspect, the invention generally relates to multiple uses of miR-34 and siRNAs functionally and structurally related to miR-34 for the treatment of cancer.
    Type: Grant
    Filed: May 5, 2008
    Date of Patent: March 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michele A. Cleary, Aimee L. Jackson, Peter S. Linsley, Julja Burchard, Lee P. Lim, Jill F. Magnus, Lin He, Xingyue He, Scott W. Lowe, Gregory J. Hannon
  • Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists
    Patent number: 8399480
    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: April 2, 2009
    Date of Patent: March 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
  • ENGINEERED ANTI-IL-23R ANTIBODIES
    Publication number: 20130064817
    Abstract: Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
    Type: Application
    Filed: November 7, 2012
    Publication date: March 14, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Leonard G. Presta
  • Indole derivatives as CRTH2 receptor antagonists
    Patent number: 8394819
    Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: March 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey Methot
  • Thiazole carboxamide derivatives and their use to treat cancer
    Patent number: 8394960
    Abstract: The present invention relates to novel Heterocyclic Ether or Thioether Derivatives, compositions comprising the Heterocyclic Ether or Thioether Derivatives, and methods for using the Heterocyclic Ether or Thioether 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 infection, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: March 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gerald W. Shipps, Jr., Matthew Richards, Cliff C. Cheng, Xiaohua Huang
  • Cyclic benzimidazole derivatives useful as anti-diabetic agents
    Patent number: 8394969
    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: September 21, 2009
    Date of Patent: March 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brett C. Bookser, Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka
  • 2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8394837
    Abstract: The present invention is directed to 2,3,4,6-substituted pyridyl derivative compounds 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: November 18, 2005
    Date of Patent: March 12, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, James C. Barrow, Shaun R. Stauffer, Joseph P. Vacca, Keith P. Moore, Shawn J. Stachel, Mattahew G. Stanton