Abstract: The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
Type:
Grant
Filed:
June 21, 2010
Date of Patent:
February 12, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina Madsen-Duggan
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.
Abstract: Nucleic acids encoding various monocyte cell proteins from a primate, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.
Type:
Application
Filed:
October 12, 2012
Publication date:
February 7, 2013
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Gosse Jan Adema, Linde Meyaard, Daniel M. Gorman, Terrill K. McClanahan, Sandra M. Zurawski, Gerard Zurawski, Lewis L. Lanier, Joseph H. Phillips
Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
Type:
Grant
Filed:
August 23, 2010
Date of Patent:
February 5, 2013
Assignee:
Merck, Sharp & Dohme, Corp.
Inventors:
Ying Huang, Guoqing Li, Andrew W. Stamford
Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
Type:
Grant
Filed:
June 16, 2008
Date of Patent:
February 5, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael Altman, Matthew Christopher, Jonathan B. Grimm, Andrew Haidle, Kaleen Konrad, Jongwon Lim, Rachel N. MacCoss, Michelle Machacek, Ekundayo Osimboni, Ryan D. Otte, Tony Siu, Kerrie Spencer, Brandon Taoka, Paul Tempest, Kevin Wilson, Hyun Chong Woo, Jonathan Young, Anna Zabierek
Abstract: A compound having the structure wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2) (C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is; Y1 is selected from the group consisting of C(O)—O— and P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
Type:
Grant
Filed:
May 30, 2012
Date of Patent:
February 5, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Iyassu K. Sebhat, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
Abstract: This invention provides compounds of Formula (I) which are PAFR antagonists: Formula (I) and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.
Type:
Grant
Filed:
December 8, 2009
Date of Patent:
February 5, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Anthony Ogawa, Hyun O. Ok, Debra Ondeyka, Feroze Ujjainwalla, Ellen Vande Bunte
Abstract: The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment 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 treatment of such diseases in which orexin receptors are involved.
Type:
Grant
Filed:
October 27, 2008
Date of Patent:
January 29, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jeffrey M. Bergman, Paul J. Coleman, Christopher D. Cox, Anthony J. Roecker
Abstract: The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
Type:
Grant
Filed:
September 30, 2009
Date of Patent:
January 29, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Andrew Stamford, Michael W. Miller, Duane Eugene DeMong, William J. Greenlee, Joseph A. Kozlowski, Brian J. Lavey, Michael K. C. Wong, Wensheng Yu, Xing Dai, De-Yi Yang, Guowei Zhou
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: A compound having the structure useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
Type:
Grant
Filed:
March 5, 2012
Date of Patent:
January 29, 2013
Assignee:
Merck Sharp & Dohme Corp
Inventors:
Amjad Ali, Michael Man-Chu Lo, Zhiqiang Guo, Brent Whitehead, Timothy J. Henderson, Lin Yan, Shrenik K. Shah
Abstract: The present invention is directed to 2,3-disubstituted piperidine amide 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 15, 2009
Date of Patent:
January 22, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher D. Cox, Broc Flores, John D. Schreier
Abstract: The present invention is directed to 2,4-disubstituted pyrrolidine amide 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 15, 2009
Date of Patent:
January 22, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Paul J. Coleman, Christopher D. Cox, John D. Schreier
Abstract: Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.
Type:
Grant
Filed:
June 4, 2010
Date of Patent:
January 22, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Kevin M. Belyk, Henry G. Morrison, Philip Jones, Vincenzo Summa, V. Brett Cooper, Amar J. Mahajan, Daniel J. Kumke, Hsien-Hsin Tung, Lawrence Wai, Vanessa Pruzinsky, Philip Pye, Remy Angelaud, Danny Mancheno
Abstract: The present invention is directed to certain Oxazole 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:
April 4, 2011
Publication date:
January 17, 2013
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
Abstract: The present invention features methods for enhancing the ability of a genotype 2b NS5B sequence to function in a replicon, for producing replicons containing a functional genotype 2b NS5B, and for using replicons to measure the ability of a compound to affect HCV replication that is sustained with the genotype 2b polymerase. Also featured is a genotype 1b NS4B adaptive mutation. The ability to produce replicons containing a functional genotype 2b NS5B is illustrated by the production of chimeric replicons based on HCV genotype 1b where substantially all the NS5B sequence is replaced with a genotype 2b NS5B.
Type:
Grant
Filed:
November 3, 2004
Date of Patent:
January 15, 2013
Assignees:
Merck Sharp & Dohme Corp., Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A.
Inventors:
Steven W. Ludmerer, Donald J. Graham, Robert L. LaFemina, Osvaldo A. Flores, Maura Pizzuti, Cinzia Traboni
Abstract: The compounds of Formula I are pro-drugs of CETP inhibitors having a central oxazolidinone ring. The compounds cyclize by the elimination of HX to form an oxazolidinone ring after administration to a patient.
Type:
Grant
Filed:
September 21, 2009
Date of Patent:
January 15, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Sander G. Mills, Amjad Ali, Cameron Smith
Abstract: A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
Type:
Grant
Filed:
October 22, 2010
Date of Patent:
January 15, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Amjad Ali, Christopher Franklin, Ravi Nargund, Michael Man-Chu Lo, Lin Yan, Pei Huo
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:
August 17, 2010
Date of Patent:
January 15, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Edmondson, Richard Berger, Lehua Chang, Vincent J. Colandrea, Jeffrey J. Hale, Bart Harper, Nam Fung Kar, Bing Li, Greg J. Morriello, Christopher R. Moyes, Deyou Sha, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu