Patents Assigned to Merck Sharp
  • Substituted biaryl derivatives and methods of use thereof
    Patent number: 9301929
    Abstract: The present invention relates to Substituted Biaryl Derivatives, compositions comprising a Substituted Biaryl Derivative, and methods of using the Substituted Biaryl Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: April 5, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig D. Boyle, Claire M. Lankin, William J. Greenlee, Joel M. Harris
  • Spirolactam CGRP receptor antagonists
    Patent number: 9296750
    Abstract: The present invention is directed to spirolactam analogs which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: March 29, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
  • PROCESS OF MAKING AND USING PHARMACEUTICAL FORMULATIONS OF ANTINEOPLASTIC AGENTS
    Publication number: 20160082005
    Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.
    Type: Application
    Filed: December 3, 2015
    Publication date: March 24, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sydney O. Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
  • 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as Btk inhibitors
    Patent number: 9290504
    Abstract: The present invention relates to 6-5 membered fused pyridine ring 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 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: March 22, 2016
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Tjeerd A. Barf, Christiaan Gerardus Johannes Maria Jans, Petrus Antonius De Adrianus Man, Arthur A. Oubrie, Hans C. A. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan-Gerard Sterrenburg, Jacobus C. H. M. Wijkmans
  • Azabenzimidazole hexahydrofuro[3,2-b]furan derivatives
    Patent number: 9290517
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: August 19, 2013
    Date of Patent: March 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James M. Apgar, Ashok Arasappan, Tesfaye Biftu, Ping Chen, Danqing Feng, Erin Guidry, Jacqueline D. Hicks, Ahmet Kekec, Kenneth J. Leavitt, Bing Li, Troy McCracken, Iyassu Sebhat, Xiaoxia Qian, Lan Wei, Robert R. Wilkening, Zhicai Wu
  • Quinolines and aza-quinolines as CRTHreceptor modulators
    Patent number: 9290453
    Abstract: The invention provides certain quinolines and aza-quinolines of the Formula (I), and their pharmaceutically acceptable salts, wherein E, J1, Ja, Jb, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: March 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher W. Boyce, Salem Fevrier, Kevin D. McCormick, Anandan Palani, Robert G. Aslanian, Phieng Siliphaivanh, Joey L. Methot, William Colby Brown, Henry Vaccaro
  • Device for calibrating and verifying the integrity of resistivity-based sensing probes
    Patent number: 9291656
    Abstract: A calibration device for sensing probes includes a housing; a test resistor within the housing; and probe holder by means of which the sensing probe's electrodes can be brought into electrical contact with the test resistor. The test resistor provides a known or a knowable test resistance between the sensing probe's electrodes. In an embodiment having a variable-resistance test resistor, the device includes an access point at which resistance across the test resistor can be measured using an ohm meter. Furthermore, the device includes one or more access points at which resistance, as measured by the sensing probe, can be measured using an ohm meter; using a monitoring device to which the sensing probe ordinarily is connected when in use; or, in some cases, using either.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: March 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Ralph Green
  • Substituted isoquinolines as CRTH2 receptor modulators
    Patent number: 9290454
    Abstract: The invention provides certain substituted isoquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: March 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xianhai Huang, Anandan Palani, Ashwin U. Rao, Hongjun Zhang, Wei Zhou
  • Aminopyrimidines as Syk inhibitors
    Patent number: 9290490
    Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis and cancer.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: March 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Kaleen Konrad Childers, Maria Emilia Di Francesco, John Michael Ellis, Christian Fischer, Jonathan Grimm, Andrew M. Haidle, Solomon D. Kattar, Alan B. Northrup, Ryan D. Otte, Alessia Petrocchi, Adam J. Schell, Hua Zhou
  • CRYSTALLINE POLYMORPHIC FORMS OF AN ANTIDIABETIC COMPOUND
    Publication number: 20160075650
    Abstract: The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.
    Type: Application
    Filed: March 26, 2015
    Publication date: March 17, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: JOHN Y. L. CHUNG
  • AMIDATION PROCESS
    Publication number: 20160075645
    Abstract: This invention describes an amidation process whereby perfluorinated amino acids can be activated and treated with an amine in the presence of a coupling agent and a pyridine derivative to yield amides, without loss of optical purity.
    Type: Application
    Filed: November 23, 2015
    Publication date: March 17, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Guy Humphrey, Kelvin Yong
  • QUINOLINE AMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20160075656
    Abstract: The present invention is directed to quinoline amide compounds of 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, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositious comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: November 18, 2015
    Publication date: March 17, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Kelly- Ann S. Schlegel, Zhi-Qiang Yang
  • ALPHA 7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEREOF-III
    Publication number: 20160075684
    Abstract: The present invention relates to chemical compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7 nAChR).
    Type: Application
    Filed: April 24, 2014
    Publication date: March 17, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Andrew Harvey, Belinda Huff, Rajinder Singh, Nathan Kuchel
  • Soluble guanylate cyclase activators
    Patent number: 9284301
    Abstract: The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds 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 compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
    Type: Grant
    Filed: March 22, 2011
    Date of Patent: March 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Darby Schmidt, Subharekha Raghavan, John Stelmach, Jian Guo, Jonathan Groeper, Linda Brockunier, Keith Rosauer, Hong Shen, Rui Liang, Fa-Xiang Ding
  • N-methyl tetrahydroquinoline M1 receptor positive allosteric modulators
    Patent number: 9284312
    Abstract: The present invention is directed to N-methyl tetrahydroquinoline compounds of 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, schizophrenia, pain or sleep disorders. 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 mediated by the M1 receptor.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: March 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Christina Ng DiMarco, Thomas J. Greshock
  • MDL-1 ligand
    Patent number: 9284377
    Abstract: The invention provides methods for modulation interactions between MDL-1 and its binding partner, Gal9. Also provided are methods to screen for modulators of MDL-1/Gal9 interaction.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: March 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Barbara Joyce-Shaikh, Douglas C. Wilson, Daniel J. Cua, Drake M. LaFace, Joseph H. Phillips
  • Cyclobutyl benzimidazoles as PDE 10 inhibitors
    Patent number: 9284302
    Abstract: The present invention is directed to substituted cyclobutyl benzimidazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: March 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger
  • HALO AND TRIFLUOROMETHYL SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20160068514
    Abstract: The present invention is directed to halo and trifluoromethyl substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 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.
    Type: Application
    Filed: April 21, 2014
    Publication date: March 10, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: Scott D. KUDUK
  • NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    Publication number: 20160068532
    Abstract: Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I).
    Type: Application
    Filed: April 25, 2014
    Publication date: March 10, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Xianhai Huang, Ronald D. Ferguson, Wei Zhou, Christopher W. Boyce, Phieng Siliphaivanh, David J. Witter, Milana M. Maletic, Joseph A. Kozlowski, Kevin J. Wilson
  • Medical injector pen
    Patent number: D752210
    Type: Grant
    Filed: August 27, 2014
    Date of Patent: March 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Angela M. Amend Kwasnik, Benjamin R. Bartfeld, Peter Basile, Jeffrey C. Givand, Philip G. Green, Sharad Gupta, Christin L. O'Neill, Steven Carl Persak, Robert Stianchi, Ari Tao Adler, Florian Altmann, Thomas Junk, Florian Kössler, Martin Meier, Scott R. Mackie, Pernilla Danielsson