Abstract: Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
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
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
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
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
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
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
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
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
Abstract: Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
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
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
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
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
Abstract: The present invention is directed to certain Aza-Indole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
Type:
Application
Filed:
May 4, 2011
Publication date:
March 7, 2013
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
Abbas M Walji, Philippe G. Nantermet, Keith P. Moore, Rachel Anne Storr, Laura Vassallo, Constantine Kreatsoulas
Abstract: The present invention is directed to quinolone compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, pain or sleep disorders, and to novel M1 receptor positive allosteric modulator compounds of formulae (II) to (VIII). 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 in which the M1 receptor is involved.
Type:
Grant
Filed:
December 4, 2006
Date of Patent:
March 5, 2013
Assignee:
Merck, Sharp & Dohme, Corp.
Inventors:
William D. Shipe, Craig Lindsley, David Hallett
Abstract: Methods, biomarkers, and expression signatures are disclosed for assessing the regulation status of growth factor pathway signaling in a cell sample or subject. More specifically, several aspects of the invention provide a set of genes which can be used as biomarkers and gene signatures for evaluating growth factor pathway deregulation status in a sample; classifying a cell sample as having a deregulated or regulated growth factor signaling pathway; determining whether an agent modulates the growth factor signaling pathway in sample; predicting response of a subject to an agent that modulates the growth factor signaling pathway; assigning treatment to a subject; and predicting evaluating the pharmacodynamic effects of cancer therapies designed to regulate growth factor pathway signaling.
Type:
Grant
Filed:
March 19, 2009
Date of Patent:
March 5, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
James Watters, Andrey Loboda, Michael Nebozhyn
Abstract: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is 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 the neuropeptide S receptor is involved.
Type:
Grant
Filed:
November 3, 2009
Date of Patent:
March 5, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
James C. Barrow, Mark T. Bilodeau, Christopher D. Cox, John C. Hartnett, Nathan R. Kett, Yiwei Li, Peter J. Manley, Jeffrey Melamed, William D. Shipe, B. Wesley Trotter, Amy Zartman
Abstract: The compound having the structural formula I or a pharmaceutically acceptable salt thereof, is disclosed, as well as its use in the treatment of central nervous system diseases, in particular Parkinson's disease, Extra Pyramidal Syndrome, restless legs syndrome and attention deficit hyperactivity disorder, pharmaceutical compositions comprising it, and combinations with other agents.
Type:
Grant
Filed:
July 6, 2009
Date of Patent:
March 5, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Jean E. Lachowicz
Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
Type:
Grant
Filed:
June 24, 2008
Date of Patent:
March 5, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Paul Harrington, Solomon Kattar, Thomas A. Miller, Matthew G. Stanton, Paul Tempest, David J. Witter