Patents Assigned to Merck Sharp and Dohme
  • C20-C21 substituted glucocorticoid receptor agonists
    Patent number: 8524697
    Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: September 3, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John C. Anthes, Kevin D. McCormick, John A. Hey, Robert G. Aslanian, Purakkattle J. Biju, Michael Y. Berlin, Hongwu Yang, Yeon-Hee Lim, Yoon Joo Lee, Rema Danielle Bitar, Phillippa H. Solomon
  • MCP1-Ig fusion variants
    Patent number: 8524217
    Abstract: The present invention provides, in part, MCP1-Ig fusion polypeptides exhibiting surprisingly beneficial properties as well as methods for treating various diseases (e.g., inflammatory diseases) by administering any of such fusions.
    Type: Grant
    Filed: May 11, 2011
    Date of Patent: September 3, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonard G. Presta, Chuan-Chu Chou
  • NOVEL LOW MOLECULAR WEIGHT CYCLIC AMINE CONTAINING CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY
    Publication number: 20130225836
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
    Type: Application
    Filed: October 31, 2011
    Publication date: August 29, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Matthew G. Stanton, Gregory L. Beutner
  • 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.
  • Gamma secretase modulators
    Patent number: 8518975
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: August 27, 2013
    Assignee: Merck Sharp + Dohme Corp.
    Inventors: Robert G. Aslanian, Xianhai Huang, Anandan Palani, Jun Qin, Wei Zhou, Xiaohong Zhu, Robert D. Mazzola, Jr., Pawan Dhondi, William J. Greenlee
  • Pyrazolo[1,5-a]pyridines as MARK inhibitors
    Patent number: 8518911
    Abstract: The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: August 27, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason D. Katz, Sandra L. Knowles, James P. Jewell, David L. Sloman, Matthew G. Stanton, Njamkou Noucti
  • 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
  • Process and intermediates for the synthesis of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds
    Patent number: 8519168
    Abstract: This application discloses a novel process for the preparation of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds, which have utility, for example, in the treatment of CXC chemokine-mediated diseases, and intermediates useful in the synthesis thereof.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: August 27, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xiaoyong Fu, Frank Bruno Guenter, Agnes S. Kim-Meade, Kenneth Stanley Matthews, Mathew Thomas Maust, Gerald Werne, Jason L. Winters, Jianguo Yin, Shuyi Zhang, David J. Moloznik
  • RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
    Patent number: 8518907
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of CTNNB1 gene expression and/or activity, and/or modulate a beta-catenin gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against CTNNB1 gene expression.
    Type: Grant
    Filed: August 2, 2011
    Date of Patent: August 27, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Duncan Brown, James J. Cunningham, Marian Gindy, Victoria Pickering, Matthew G. Stanton, Steven M. Stirdivant, Walter R. Strapps
  • BETA-AMINO HETEROCYCLIC DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
    Publication number: 20130217695
    Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) 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: Application
    Filed: March 20, 2013
    Publication date: August 22, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • RECOMBINANT SUBUNIT DENGUE VIRUS VACCINE
    Publication number: 20130216575
    Abstract: The present invention provides dengue virus vaccines and immunogenic compositions for administration to human subjects. The vaccine compositions of the present invention comprise recombinantly produced monomeric and/or dimeric forms of truncated dengue virus envelope glycoprotein that, when formulated together with an adjuvant and a pharmaceutically acceptable carrier, induce balanced tetravalent immune responses. In preferred embodiments of the compositions described herein, the DEN4 protein component is a dimeric form of DEN4. The compositions are designed to be acceptable for use in the general population, including immunosuppressed, immunocompromised, and immunosenescent individuals. Also provided herein are methods of inducing a protective immune response in a human patient population by administering the compositions described herein to the patients.
    Type: Application
    Filed: October 27, 2011
    Publication date: August 22, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Beth-Ann Griswold Coller, Vidya B. Pai, D. Elliot Parks, Michele Yelmene, Andrew J. Bett, Timothy Martyak
  • RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
    Publication number: 20130217756
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity, and/or modulate a gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against target gene expression.
    Type: Application
    Filed: October 25, 2011
    Publication date: August 22, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Mark Cancilla, James John Cunningham, Michael W. Flanagan, Henry J. Haringsma, Denise M. Kenski, Matthew G. Stanton, Steven M. Stirdivant, Aarron T. Willingham
  • FORMULATIONS FOR CATHEPSIN K INHIBITORS
    Publication number: 20130217766
    Abstract: The instant invention relates to pharmaceutical compositions containing cathespin K inhibitors. Also disclosed are processes for making said pharmaceutical compositions.
    Type: Application
    Filed: March 20, 2013
    Publication date: August 22, 2013
    Applicant: Merck, Sharp & Dohme, Corp.
    Inventor: Merck, Sharp & Dohme, Corp.
  • HIV integrase inhibitors
    Patent number: 8513234
    Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.
    Type: Grant
    Filed: October 2, 2009
    Date of Patent: August 20, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard C. A. Isaacs, Wayne J. Thompson, Peter D. Williams, Dai-Shi Su, Shankar Venkatraman, Mark W. Embrey, Thorsten E. Fisher, John S. Wai, David C. Dubost, Richard G. Ball, Eric J. Choi, Tao Pei, Sarah L. Trice, Neil Campbell, Matthew Maddess, Peter E. Maligres, Michael Shevlin, Zhiguo Jake Song, Dietrich P. Steinhuebel, Neil A. Strotman, Jingjun Yin
  • P38 kinase inhibiting agents
    Patent number: 8513289
    Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: August 20, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hiroo Koyama, Soumya P. Sahoo, Ginger Xu-Qiang Yang, Daniel J. Miller
  • Engineered anti-TSLP antibody
    Patent number: 8512705
    Abstract: The invention relates to binding compounds that specifically bind to human TSLP, as well as uses thereof, e.g., in the treatment of inflammatory disorders.
    Type: Grant
    Filed: June 25, 2012
    Date of Patent: August 20, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonard G. Presta, Rene de Waal Malefyt
  • Engineered anti-IL-23p19 antibodies
    Patent number: 8513389
    Abstract: Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: August 20, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonard G. Presta, Brian M. Beyer, Richard N. Ingram, Peter Orth, Yan-Hui Liu
  • 3-imidazo[4,5-b]pyridin-5-ol derivatives useful in the treatment of GPR81 receptor disorders
    Patent number: 8507473
    Abstract: The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.
    Type: Grant
    Filed: September 10, 2009
    Date of Patent: August 13, 2013
    Assignees: Arena Pharmaceuticals, Inc., Merck Sharp & Dohme Corp.
    Inventors: P. Douglas Boatman, Benjamin R. Johnson, Jae-Kyu Jung, Michelle Kasem, Thomas O. Schrader, Philip J. Skinner, Steven Colletti
  • 3- and 6-quinolines with N-attached heterocyclic CGRP receptor antagonists
    Patent number: 8507477
    Abstract: Compounds of Formula (I): (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. 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 receptors are involved.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: August 13, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Michael R. Wood, Ian M. Bell, June J. Kim, Harold G. Selnick, Craig A. Stump
  • Soluble guanylate cyclase activators
    Patent number: 8507512
    Abstract: This inventions relates to compounds having the structure Formula I and pharmaceutically acceptable salts thereof which are soluble guanylate cyclase activators. 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: February 24, 2010
    Date of Patent: August 13, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Emma R. Parmee, Christopher Joseph Sinz, Olga A. Ziouzina