Patents Assigned to Merck Sharp
  • Bipyridylaminopyridines as Syk inhibitors
    Patent number: 9145391
    Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: September 29, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Denis Deschenes, Michael D. Altman, John Michael Ellis, Christian Fischer, Andrew M. Haidle, Solomon D. Kattar, Alan B. Northrup, Adam J. Schell, Graham F. Smith, Brandon M. Taoka, Corey Bienstock, Maria Emilia Di Francesco, Anthony Donofrio, Scott Peterson, Kerrie B. Spencer, James Patrick Jewell, Amjad Ali, David Jonathan Bennett, Qun Dang, John Wai
  • Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
    Patent number: 9145426
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of W, Z, R1H, R2, R3, R4, ring A, ring B, m, n, p, and -L1- is as defined herein. The novel 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 thereto. 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, including Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: April 2, 2012
    Date of Patent: September 29, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
  • NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    Publication number: 20150266895
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Application
    Filed: September 26, 2013
    Publication date: September 24, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kevin J. Wilson, David J. Witter, Phieng Siliphaivanh, Kathryn Lipford, David Sloman, Danielle Falcone, Brendan O'Boyle, Umar Faruk Mansoor, Jongwon Lim, Joey L. Methot, Christopher Boyce, Lei Chen, Matthew H. Daniels, Salem Fevrier, Xianhai Huang, Ravi Kurukulasuriya, Ling Tong, Wei Zhou, Joseph Kozlowski, Milana M. Maletic, Bidhan A. Shinkre, Jayanth Thiruvellore Thatai, Raman Kumar Bakshi, Ganesh Babu Karunakaran
  • POSACONAZOLE INTRAVENOUS SOLUTION FORMULATIONS STABILIZED BY SUBSTITUTED BETA-CYCLODEXTRIN
    Publication number: 20150265715
    Abstract: The present invention relates to aqueous solutions useful as pharmaceutical compositions of posaconazole for intravenous administration. These compositions include a solubilizing agent, such as a modified ?-cyclodextrin in an acidified solution, which can also include a chelating agent such as disodium edetate (EDTA). In clinical trials, a 200 mg posaconazole dose of the selected composition was found to achieve acceptable pharmacokinetic properties.
    Type: Application
    Filed: March 25, 2015
    Publication date: September 24, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Susan K. Heimbecher, David Monteith, James D. Pipkin
  • HCV NS3 Protease Inhibitors
    Publication number: 20150266897
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Application
    Filed: April 3, 2015
    Publication date: September 24, 2015
    Applicants: MSD ITALIA S.R.L., MERCK SHARP & DOHME CORP.
    Inventors: Nigel J. Liverton, Vincenzo Summa, Maria Emilia Di Francesco, Marco Ferrara, Kevin F. Gilbert, Steven Harper, John A. McCauley, Charles J. McIntyre, Alessia Petrocchi, Marco Pompei, Joseph J. Romano, Michael T. Rudd, John W. Butcher, M. Katharine Holloway
  • Inhibitors of the Renal Outer Medullary Potassium channel
    Patent number: 9139585
    Abstract: This invention relates to compounds of Formula I-VI having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: September 22, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn P. Walsh, Alexander Pasternak, Reynalda K. DeJesus, Haifeng Tang, Barbara Pio, Aurash Shahripour, Kevin M. Belyk, Harry R. Chobanian, Yan Guo, Jessica L. Frie, Zhi-Cai Shi, Helen Chen, Timothy A. Blizzard, Brian Cato
  • Fused tricyclic aryl compounds useful for the treatment of viral diseases
    Patent number: 9139569
    Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: May 12, 2010
    Date of Patent: September 22, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge, Craig A. Coburn
  • Aminomethyl biaryl benzotriazole derivatives
    Patent number: 9139576
    Abstract: The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: September 22, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Robert M. Garbaccio, Scott D. Kuduk, Adam W. Johnson, Jason W. Skudlarek
  • Method for producing proteins in that lack detectable cross binding activity to antibodies against host cell antigens
    Patent number: 9139632
    Abstract: Methods for producing proteins and glycoproteins in Pichia pastoris that lack detectable cross binding activity to antibodies made against host cell antigens are described. In particular, methods are described wherein recombinant Pichia pastoris strains that do not display a ?-mannosyltransferase 2 activity with respect to an N-glycan or O-glycan and do not display at least one activity selected from a ?-mannosyltransferase 1, 3, and 4 activity to produce recombinant proteins and glycoproteins. These recombinant Pichia pastoris strains can produce proteins and glycoproteins that lack detectable ?-mannosidase resistant ?-mannose residues thereon and thus, lack cross binding activity to antibodies against host cell antigens. Further described are methods for producing bi-sialylated human erythropoietin in Pichia pastoris that lack detectable cross binding activity to antibodies against host cell antigens.
    Type: Grant
    Filed: October 11, 2010
    Date of Patent: September 22, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Piotr Bobrowicz, Sujatha Gomathinayagam, Stephen Hamilton, Huijuan Li, Natarajan Sethuraman, Terrance A. Stadheim, Stefan Wildt
  • Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes
    Patent number: 9138426
    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: January 7, 2015
    Date of Patent: September 22, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber
  • NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    Publication number: 20150258074
    Abstract: Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).
    Type: Application
    Filed: September 26, 2013
    Publication date: September 17, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Kevin J. Wilson, David J. Witter, Matthew H. Daniels, Angie R. Angeles, Phieng Siliphaivanh, David Sloman, Brendan O'Boyle, Danielle Falcone, Catherine White, Ron Ferguson, Wei Zhou, Kathryn Lipford, Umar Faruk Mansoor, Salem Fevrier, Xianhai Huang, Ravi Kurukulasuriya, Judson E. Richard, Shuyi Tang, Christopher Boyce, Joseph Kozlowski, Raman Kumar Bakshi, Ganesh Babu Karunakaran
  • Thrombin inhibitors
    Patent number: 9133147
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2), wherein R4 is H, C1-6 alkyl, aryl, or C3-8 cycloalkyl; R1 is a heterocycle or —(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; R2 is OH, NH2 or NHSO2CH3; R3 is C1-6 alkyl.
    Type: Grant
    Filed: March 22, 2013
    Date of Patent: September 15, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Timothy Allen Blizzard, Tesfaye Biftu
  • QUANTIFICATION OF TAU IN BIOLOGICAL SAMPLES BY IMMUNOAFFINITY ENRICHMENT AND MASS SPECTROMETRY
    Publication number: 20150253341
    Abstract: The present invention provides a quantitative immunoaffinity LC-MS/MS assay for detection and quantification of Tau protein in a biological sample.
    Type: Application
    Filed: February 6, 2015
    Publication date: September 10, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Thomas McAvoy, Michael E. Lassman, Omar F. Laterza
  • COMPOSITION FOR INHIBITION OF CATHEPSIN K
    Publication number: 20150250759
    Abstract: The present invention relates to the a method of inhibiting bone resorption in a mammal in need thereof with an oral pharmaceutical composition comprising a cathepsin K inhibitor, or a pharmaceutically acceptable salt thereof, or a mixture thereof, according to a continuous schedule having a dosage interval of once weekly, biweekly, twice monthly or once monthly.
    Type: Application
    Filed: May 21, 2015
    Publication date: September 10, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Anastasia Daifotis, Selwyn Aubrey Stoch, Basil Avery Ince, Cameron Black
  • 2-PYRIDYLOXY-3-ESTER-4-NITRILE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20150252033
    Abstract: The present invention is directed to 2-pyridyloxy-3-ester-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-ester-4-nitrile compounds described herein in the 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: October 14, 2013
    Publication date: September 10, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Substituted benzopiperazines as CETP inhibitors
    Patent number: 9126976
    Abstract: Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: August 13, 2012
    Date of Patent: September 8, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rajan Anand, Vincent J. Colandrea, Maud Reiter, Petr Vachal, Aaron Zwicker, Jonathan E. Wilson, Fengqi Zhang, Kake Zhao
  • FSH receptor antagonists
    Patent number: 9127007
    Abstract: The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: September 8, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
  • Kisspeptide-pentasaccharide conjugates
    Patent number: 9127038
    Abstract: The invention relates to kisspeptide-pentasaccharide conjugates having the general formula (I) wherein Z1 is Tyr or D-Tyr; Z3 is Trp, Hyp, Phe or Lys(R2); Z5 is Thr, Aib or Ala; Z7 is Gly or azaGly; Z8 is Leu; or Z7 and Z8 together represent; Z10 is Phe or Trp; n is 0 or 1; or R2, when present, represents a pentasaccharide derivative having the formula (II) wherein R is methyl or SO3X; X is a positively charged counterion; with the proviso that when R2 is present, R1 is H or (C1-6) alkylcarbonyl; R3 is H or (C1-3)alkyl; and L represents a pharmacologically inactive linker moiety having 10-50 atoms; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same as well as to the use of said kisspeptide-pentasaccharide conjugates in the treatment of female infertility.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: September 8, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Marion Blomenrohr, Martin De Kort, Miranda Maria Cornelia Van Der Lee, Jeffry Abraham Jacobus Wisse
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9126957
    Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: September 8, 2015
    Assignees: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS, INC.
    Inventors: Harold G. Selnick, Kun Liu, Ernest J. McEachern, Yuanxi Zhou, Yongbao Zhu
  • Extracts from kibdelos porangium as antibacterial agents
    Patent number: 9126983
    Abstract: The present invention relates to novel compounds of formulae (I) and (II) and pharmaceutically acceptable salts thereof that are useful in the treatment and/or prevention of human and animal bacterial infections and associated diseases and conditions; compositions containing such compounds; derivation of such compounds by fermentation and isolation, partial synthesis and total synthesis; methods of inhibiting bacterial growth; methods of treating, preventing or controlling bacterial infection; biologically pure cultures of bacterial strains from which such compounds may be produced; and processes for preparing compositions containing such compounds.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: September 8, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme de Espana SA
    Inventors: Sheo Singh, Jon D. Polishook, Deborah L. Zink, Olga Genilloud, Michael Goetz, Francisca Vicente, David Brian Olsen, Scott Knoble Smith