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  • LIQUID CRYSTAL SYSTEM AND LIQUID CRYSTAL DISPLAY
    Publication number: 20130193376
    Abstract: The instant invention relates to mesogenic systems comprising a) a polymeric component, component A, obtained or obtainable from polymerisation of a precursor comprising one or more mesogenic mono-reactive compounds, one or more di-reactive compounds, which optionally are also mesogenic compounds and optionally a photo-initiator and a low molecular weight component, component B, comprising one or more mono-reactive, mesogenic compounds, one or more mesogenic compounds and one or more chiral dopants, exhibiting a Blue Phase, as well as to the use of these systems in deices and to these devices.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicant: MERCK PATENT GMBH
    Inventor: MERCK PATENT GMBH
  • Oral pharmaceutical formulation of omarigliptin
    Patent number: 9937153
    Abstract: The present invention is directed to stable, oral pharmaceutical formulations of dipeptidyl peptidase-4 inhibitors, such as omarigliptin. Such pharmaceutical formulations comprise omarigliptin; and neutral excipients, wherein the neutral excipient is present in the amount of at least 75% by weight of the pharmaceutical formulation and comprises at least one non-reducible sugar diluent or a mixture of non-reducible sugar diluents.
    Type: Grant
    Filed: August 25, 2014
    Date of Patent: April 10, 2018
    Assignees: Merck Sharp & Dohme LTD., Merck Sharp & Dohme Corp.
    Inventors: Vincent Brett Cooper, Kathryn Alanna Bradley, Samuel Robert Pygall, Rajan Gupta, Madison Paige Stanford, Lin Xie
  • RORgammaT INHIBITORS
    Publication number: 20140038942
    Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.
    Type: Application
    Filed: February 10, 2012
    Publication date: February 6, 2014
    Applicants: Merck Sharp & Dohme B.V., Merck Sharp & Dohme Corp.
    Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
  • 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
    Patent number: 4537902
    Abstract: Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.
    Type: Grant
    Filed: June 11, 1979
    Date of Patent: August 27, 1985
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Microbial transformation product having immunosuppressive activity
    Patent number: 5352783
    Abstract: Microbial transformation of a macrolide immunosuppressant by the microorganism Streptomyces sp., (Merck Culture Collection MA 6960) ATCC No. 55387 yields a compound of the structural formula (I): ##STR1## This compound is an immunosuppressant useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: October 4, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Ali Shafiee, Byron H. Arison, Shieh-Shung T. Chen, Randall R. Miller, Ralph A. Stearns
  • Methods and intermediates for preparing macrolactams
    Patent number: 9073825
    Abstract: A first aspect of the present invention describes a compound selected from group consisting of: wherein R is either H, C(O)RA, or C(O)NHCH(X)COOH; provided that X is a C2-C6 alkyl, or a C3-C8 cycloalkyl and RA is a C1-6 alkyl or aryl; These compounds are used to make Compound A
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: July 7, 2015
    Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.
    Inventors: Nobuyoshi Yasuda, Jeffrey T. Kuethe, Guy Humphrey, Gregory L. Beutner, Yong-Li Zhong, Edward Cleator, Carl Baxter
  • Tricyclic compounds useful as inhibitors of kinases
    Patent number: 8518964
    Abstract: The present invention provides inhibitors of kinases, specifically I?B kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-?B-mediated diseases.
    Type: Grant
    Filed: November 17, 2006
    Date of Patent: August 27, 2013
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Jean-Francois Truchon, Nicolas Lachance, Cheuk Lau, Yves Leblanc, Christophe Mellon, Patrick Roy, Elise Isabel, Ryan D Otte, Jonathan R Young
  • METHOD FOR TREATING A DISEASE ASSOCIATED WITH SOLUBLE, OLIGOMERIC SPECIES OF AMYLOID BETA 1-42
    Publication number: 20130089537
    Abstract: This invention is a method and kit for treating a disease associated with, or resulting from, the accumulation of soluble oligomer amyloid beta 1-42 using an antibody, or antibody fragment thereof, that has a higher affinity for amyloid beta 1-42 oligomers than for amyloid beta 1-42 monomer, amyloid beta 1-40 monomer, plaques and amyloid beta fibrils and, optionally, a tau therapeutic or an inhibitor of amyloid beta production or aggregation.
    Type: Application
    Filed: December 4, 2012
    Publication date: April 11, 2013
    Applicants: MERCK SHARP & DOHME CORP., ACUMEN PHARMACEUTICALS, INC.
    Inventors: Acumen Pharmaceuticals, Inc., Merck Sharp & Dohme Corp.
  • Aryl thiopyrano[4,3,2-cd]indoles as inhibitors of leukotriene biosynthesis
    Patent number: 5314898
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, psoriasis, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: June 29, 1992
    Date of Patent: May 24, 1994
    Assignees: Merck & Co., Inc., Merck Frosst Canada Inc.
    Inventors: John Y. L. Chung, Robert A. Reamer, Yves Girard, Pierre Hamel
  • Quinoxalinone derivatives as insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
    Publication number: 20130123257
    Abstract: The present invention relates to quinoxalinone derivatives of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these quinoxalinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Application
    Filed: January 4, 2013
    Publication date: May 16, 2013
    Applicant: Merck Patent GmbH
    Inventor: Merck Patent GmbH
  • Process for preparing chiral dipeptidyl peptidase-IV inhibitors
    Patent number: 9527855
    Abstract: A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: December 27, 2016
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.
    Inventors: Michael J. Zacuto, Robert F. Dunn, Aaron J. Moment, Jacob M. Janey, David Lieberman, Faye Sheen, Nadine Bremeyer, Jeremy Scott, Jeffrey T. Kuethe, Lushi Tan, Qinghao Chen
  • Inhibitors of janus kinases
    Patent number: 7763634
    Abstract: The instant invention provides for tetracyclic 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 5, 2007
    Date of Patent: July 27, 2010
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.
    Inventors: Jonathan R. Young, Andrew Haidle, Paul Tempest, Michelle Machacek
  • BTK INHIBITORS
    Publication number: 20180079752
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts 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 of Formula I in the treatment of Btk mediated disorders.
    Type: Application
    Filed: May 31, 2016
    Publication date: March 22, 2018
    Applicants: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME B.V.
    Inventors: ADRIANUS PETRUS ANTONIUS DE MAN, RONALD KIM, JIAN LIU, JOSEPH A. KOZLOWSKI, SOBHANA BABU BOGA, THIERRY FISCHMANN, DEODIAL Guy GUIADEEN, ILSE HENDRICA MARIA POLS-DE ROOIJ, SHILAN LIU, HAO WU
  • Process for producing FK-506
    Patent number: 5194378
    Abstract: Described is a new process for producing the macrolide immunosuppressant, FK-506 under fermentation conditions utilizing the microorganism, Streptomyces sp., (Merck Culture Collection No. MA 6858) ATCC No. 55098. The immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: October 7, 1991
    Date of Patent: March 16, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Gino M. Salituro, Francis Dumont, George M. Garrity, Leeyuan Huang, E. Tracy T. Jones, Mary N. Omstead, Isabel M. Fernandez, Teresa D. Matas
  • Process for preparing chiral dipeptidyl peptidase-IV inhibitors
    Patent number: 9187488
    Abstract: A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.
    Type: Grant
    Filed: June 25, 2012
    Date of Patent: November 17, 2015
    Assignees: Merck Sharp & Dohme Corp, Merck Sharp & Dohme Ltd.
    Inventors: Michael J. Zacuto, Robert F. Dunn, Aaron J. Moment, Jacob M. Janey, David Lieberman, Faye Sheen, Nadine Bremeyer, Jeremy Scott, Jeffrey T. Kuethe, Lushi Tan, Qinghao Chen
  • BIARYL-SPIROAMINOOXZAOLINE ANALOGUES AS ALPHA 2C ADRENERGIC RECEPTOR MODULATORS
    Publication number: 20130225582
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: April 4, 2013
    Publication date: August 29, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • ANTIBODIES FOR THE DETECTION OF INTEGRIN COMPLEXES IN FFPE MATERIAL
    Publication number: 20130203079
    Abstract: The invention relates to antibodies that are capable to bind the extracellular domain of integrin. Another object of the invention concerns the use of said antibodies for detecting integrins in archival formalin fixed paraffin embedded (FFPE) tissue. The invention also relates to methods for preparing monoclonal rabbit antibodies, wherein the immunogen is an insect expression culture-derived recombinant extracellular integrin domain, and another method for screening anti-integrin antibodies that discriminate between closest integrin homologues and that are especially suited for immunohistochemistry in FFPE material.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 8, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventor: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
  • Microbial transformation product of L-683,590
    Patent number: 4975372
    Abstract: Described is a new immunosuppressant, L-685,487, a monodemethylated rearranged derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, unidentified Actinomycete (Merck Cultrue Collection MA 6474) ATCC No. 53828. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: January 13, 1989
    Date of Patent: December 4, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Byron H. Arison, Edward S. Inamine, Shieh-Shung T. Chen, Linda S. Wicker
  • Inhibitors of HIV protease
    Patent number: 5250563
    Abstract: Novel cytochalasins are the biotransformed products after incubation with a substrate in a culture of the microorganism Kibdelosporangium sp. (Merck Culture Collection MA 6559), ATCC No. 53771. The compounds of the present invention inhibit HIV protease and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: October 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, George A. Doss, Russell B. Lingham
  • FK-520 microbial transformation product
    Patent number: 4987139
    Abstract: Described is a new immunosuppressant, L-687,795, a C-13, C-15, C-31 trisdemethylated, ring rearranged derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, Actinoplanacete sp. (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: May 5, 1989
    Date of Patent: January 22, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Linda S. Wicker, Byron H. Arison
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