Abstract: The present invention is directed to thioether-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the thioether-piperidinyl compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Abstract: The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R11 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
Type:
Application
Filed:
December 17, 2014
Publication date:
November 3, 2016
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
Thomas H. Graham, Wensheng Liu, Tao Yu, Yonglian Zhang, Sherman T. Waddell, John S. Wai, Paul J. Coleman, John M. Sanders, Mark W. Embrey, Abbas M. Walji, Ronald Dale Ferguson, II, Christine Ng Di Marco, Thomas G. Steele, Lihong Hu, Xuanjia Peng
Abstract: The present invention is directed to 2-amino-3-ester pyridyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-amino-3-ester pyridyl compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Abstract: The present invention is directed to piperidinyloxy lactone compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyloxy lactone compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.
Type:
Grant
Filed:
September 10, 2010
Date of Patent:
November 1, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher J Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
Type:
Grant
Filed:
January 22, 2014
Date of Patent:
November 1, 2016
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Ronald M. Kim, Jian Liu, Xiaolei Gao, Sobhana Babu Boga, Deodialsingh Guiadeen, Joseph A. Kozlowski, Wensheng Yu, Rajan Anand, Younong Yu, Oleg B. Selyutin, Ying-Duo Gao, Hao Wu, Shilan Liu, Chundao Yang, Hongjian Wang
Abstract: The present disclosure describes gene signature biomarkers that are useful for identifying cancer patients who are most likely to benefit from treatment with a PD-1 antagonist. The disclosure also provides methods and kits for testing tumor samples for the biomarkers, as well as methods for treating subjects with a PD-1 antagonist based on the test results.
Type:
Application
Filed:
December 15, 2014
Publication date:
October 27, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Mark Ayers, Andrey Loboda, Jared Lunceford, Terrill K. McClanahan, Erin Murphy, Michael Nebozhyn, Robert H. Pierce
Abstract: The present disclosure describes PD-L1 gene signature biomarkers that are useful for identifying cancer patients who are most likely to benefit from treatment with a PD-1 antagonist. The disclosure also provides methods and kits for testing tumor samples for the biomarkers, as well as methods for treating subjects with a PD-1 antagonist based on the test results.
Type:
Application
Filed:
December 15, 2014
Publication date:
October 27, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Mark Ayers, Andrey Loboda, Jared Lunceford, Terrill K. McClanahan, Erin Murphy, Michael Nebozhyn, Robert H. Pierce
Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof. Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
Type:
Application
Filed:
December 16, 2014
Publication date:
October 27, 2016
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
JIAN LIU, RONALD M. KIM, JOSEPH KOZLOWSKI, ARTO D. KRIKORIAN, RAJAN ANAND
Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R3, R5, R6, A, Cy and the subscripts r, s, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
Type:
Application
Filed:
December 15, 2014
Publication date:
October 27, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Michelle R. Machacek, Eric T. Romeo, Alan B.. Nortrup, Michael D. Altman
Abstract: Disclosed are the ERK inhibitors of formula (1.0) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). This invention provides compounds that are ERK inhibitors (i.e., ERK2 inhibitors). This invention also provides a pharmaceutical composition comprising an effective amount of at least one (e.g., 1) compound of formula (1.0) and a pharmaceutically acceptable carrier.
Type:
Application
Filed:
December 12, 2014
Publication date:
October 27, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Kathryn Lipford, Danielle Falcone, David L. Sloman, David J. Witter
Abstract: Novel tricyclic compounds of Formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing osteoporosis and similar conditions. The compounds are effective as calcium sensing receptor antagonists. Pharmaceutical compositions and methods of treatment are also included.
Type:
Application
Filed:
December 17, 2014
Publication date:
October 27, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Gui-Bai Liang, Changyou Shou, Xianghong Huo, Haisheng Wang
Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Type:
Application
Filed:
December 17, 2014
Publication date:
October 27, 2016
Applicants:
MERCK SHARP & DOHME CORP., MERCK CANADA INC.
Inventors:
John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Satyanarayana Tummanapalli, Vouy Linh Truong, Peter D. Williams
Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (“A?”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's disease, are also disclosed.
Type:
Grant
Filed:
February 27, 2015
Date of Patent:
October 25, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Jeffrey A. Misiaszek, Guoqing Li
Abstract: The present disclosure describes an IHC assay for detecting and quantifying spatially proximal pairs of PD-1-expressing cells (PD-1+ cells) and PD-Ligand-expressing cells (PD-L+ cells) in tumor tissue, and the use of the assay to generate proximity biomarkers that are predictive of which cancer patients are most likely to benefit from treatment with a PD-1 antagonist. The disclosure also provides methods for testing tumor samples for the proximity biomarkers, as well as methods for treating subjects with a PD-1 antagonist based on the test results.
Type:
Application
Filed:
December 8, 2014
Publication date:
October 20, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Robert H. Pierce, Jennifer H. Yearley, Scott P. Turner, Belma Dogdas, Ansuman Bagchi
Abstract: Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein the saccharide for at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
Type:
Application
Filed:
June 24, 2016
Publication date:
October 20, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Songnian Lin, Lin Yan, Ahmet Kekec, Yuping Zhu, David N. Hunter, Pei Huo, Danqing Feng, Ravi P. Nargund, Christopher R. Moyes, Zhiqiang Zhao, Brenda Pipik, Dmitri Pissarnitski, Joseph L. Duffy, Erin N. Guidry
Abstract: The present invention is directed to 2-pyridyloxy-3-ester-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Abstract: The present disclosure describes IFN-? gene signature biomarkers that are useful for identifying cancer patients who are most likely to benefit from treatment with a PD-1 antagonist. The disclosure also provides methods and kits for testing tumor samples for the biomarkers, as well as methods for treating subjects with a PD-1 antagonist based on the test results.
Type:
Application
Filed:
December 15, 2014
Publication date:
October 20, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Mark Ayers, Andrey Loboda, Jared Lunceford, Terrill K. McClanahan, Erin Murphy, Michael Nebozhyn, Robert H. Pierce
Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
December 5, 2014
Publication date:
October 20, 2016
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Xiaoqing Han, Alan Whitehead, Subharekha Raghavan, Jonathan Groeper, Jian Guo, Yong Zhang