Patents Assigned to Merck & Co., Inc.
  • Publication number: 20100298342
    Abstract: The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: September 4, 2007
    Publication date: November 25, 2010
    Applicants: MERCK & CO., INC., SUNESIS PHARMACEUTICALS, INC.
    Inventors: Melissa S. Egbertson, Shaun R. Stauffer, Craig A. Coburn, James C. Barrow, Lou Anne Neilson, Jenny M. Wai, Wenjin Yang, Wanli Lu, Bruce Fahr
  • Publication number: 20100275625
    Abstract: Intelligent refrigerator system for storing pharmaceutical product containers, such as vials, ampules, syringes, bottles, medication tubes, blister packs and cartons, at the point of dispensing. Embodiments of the invention use product identification technology, such as radio-frequency identification (RFID) tags and readers, to uniquely identify containers as they are added to or removed from the cold storage compartment of the refrigerator, and automatically retrieve from a local or remote database a variety of details associated with the containers and their contents, such as manufacturing data, expiration dates, time out of refrigeration, inventory levels, safety information, usage statistics, known contraindications and warnings, etc. If the details indicate that there is a problem with a particular pharmaceutical (e.g.
    Type: Application
    Filed: July 8, 2010
    Publication date: November 4, 2010
    Applicant: MERCK & CO, INC.
    Inventor: Alan J. Lowenstein
  • Patent number: 7820680
    Abstract: Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula I: wherein a, b, Y, R1, R2, R3 and R4 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se 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.
    Type: Grant
    Filed: March 4, 2005
    Date of Patent: October 26, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Peter D. Williams, John S. Wai, Mark W. Embrey, Donnette D. Staas, Linghang Zhuang
  • Patent number: 7811563
    Abstract: The present invention relates to antibodies that differentially recognize multi-dimensional conformations of A?-derived diffusible ligands, also known as ADDLs. The antibodies of the invention can distinguish between Alzheimer's Disease and control human brain extracts and are useful in methods of detecting ADDLs and diagnosing Alzheimer's Disease. The present antibodies also block binding of ADDLs to neurons, assembly of ADDLs, and tauphosphorylation and are there useful in methods for the preventing and treating diseases associated with soluble oligomers of amyloid ? 1-42.
    Type: Grant
    Filed: October 21, 2005
    Date of Patent: October 12, 2010
    Assignees: Northwestern University, Merck & Co., Inc.
    Inventors: Paul Acton, Zhiqiang An, Andrew J. Bett, Robert Breese, Elizabeth Chen Dodson, Gene Kinney, William L Klein, Mary P. Lambert, Xiaoping Liang, Paul Shughrue, William R. Strohl, Kirsten Viola, Lei Chang
  • Publication number: 20100256698
    Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Application
    Filed: April 2, 2010
    Publication date: October 7, 2010
    Applicant: MERCK & CO., INC.
    Inventors: B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
  • Publication number: 20100256106
    Abstract: Novel compounds of the structural formula (I) are antagonists of the 5-HT6 receptor and are useful in the treatment, prevention and suppression of diseases mediated by the 5-HT6 receptor. The compounds of the present invention are useful in the treatment of obesity, diabetes, metabolic disorder, cognitive disorders, age related cognitive disorder, depression, mania, bipolar disorders, schizophrenia, anxiety, generalized anxiety disorder, panic disorder, and obsessive compulsive disorder, epilepsy, convulsions, migraine, substance withdrawal from substances including but not limited to opiates, nicotine, tobacco products, alcohol, benzodiazepines, sedatives, and the like, sleep disorders, attention deficit/hyperactivity disorder, and Alzheimer's disease.
    Type: Application
    Filed: November 25, 2008
    Publication date: October 7, 2010
    Applicant: MERCK & CO., INC.
    Inventors: Alexander Pasternak, Michael J. Szymonifka
  • Patent number: 7807829
    Abstract: The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(tri-fluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.
    Type: Grant
    Filed: November 3, 2005
    Date of Patent: October 5, 2010
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.
    Inventors: James Michael McNamara, Louis Matty, Jonathan D. Rosen
  • Publication number: 20100227903
    Abstract: A pharmaceutical composition comprises (a) a CETP inhibiting compound, or a pharmaceutically acceptable salt thereof; (b) a concentration-enhancing polymer, and (c) optionally one or more surfactants; wherein the compound has the structure shown as Formula I below. The composition raises HDL-cholesterol and lowers LDL-cholesterol.
    Type: Application
    Filed: February 9, 2007
    Publication date: September 9, 2010
    Applicant: MERCK & CO., INC.
    Inventors: Sarah Geers, Michael Lowinger, Craig A. McKelvey, Robert F. Meyer, Dina Zhang
  • Patent number: 7790739
    Abstract: The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: October 18, 2006
    Date of Patent: September 7, 2010
    Assignee: Merck & Co., Inc. and Merck Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Ana Esther Gabarda Ortega
  • Publication number: 20100222322
    Abstract: Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment 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: June 23, 2006
    Publication date: September 2, 2010
    Applicant: MERCK & CO., INC.
    Inventors: Scott E. Wolkenberg, Zhijian Zhao, Craig W. Lindsley
  • Patent number: 7786287
    Abstract: The present invention features assays employing a beta-lactamase reporter system, an HCV replicon enhanced cell, and/or a chimeric HCV replicon containing a 3? UTR based on the HCV-1a 3? UTR. These features can be employed alone or together, and are preferably combined together to measure HCV replicon activity and the affect of compounds on such activity.
    Type: Grant
    Filed: April 11, 2003
    Date of Patent: August 31, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Osvaldo A. Flores, Jay Grobler, Edward M. Murray, Paul D. Zuck
  • Patent number: 7780963
    Abstract: The present invention relates to antibodies that differentially recognize multi-dimensional conformations of A?-derived diffusible ligands, also known as ADDLs. The antibodies of the invention can distinguish between Alzheimer's Disease and control human brain extracts and are useful in methods of detecting ADDLs and diagnosing Alzheimer's Disease. The present antibodies also block binding of ADDLs to neurons, assembly of ADDLS, and tau phosphorylation and are there useful in methods for the preventing and treating diseases associated with soluble oligomers of amyloid ?1-42.
    Type: Grant
    Filed: October 21, 2005
    Date of Patent: August 24, 2010
    Assignees: Merck & Co., Inc., Northwestern University
    Inventors: Paul Acton, Zhiqiang An, Andrew J. Bett, Robert Breese, Lei Chang, Elizabeth Chen Dodson, Gene Kinney, William Klein, Mary P. Lambert, Xiaoping Liang, Paul Shughrue, William R. Strohl, Kirsten Viola
  • Publication number: 20100204486
    Abstract: The present invention is concerned with novel processes for the preparation of (+)-1-aryl-3-azabicyclo[3,10]hexanes or a pharmaceutically acceptable salt thereof, and (?)-1-aryl-3-azabicyclo[3,10]hexanes or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., pain, depression, anxiety disorders, eating disorders and urinary incontinence.
    Type: Application
    Filed: April 27, 2007
    Publication date: August 12, 2010
    Applicant: MERCK & CO., INC.
    Inventors: Edward G. Corley, Jerry A. Murry, Bryon Simmons, Feng Xu
  • Publication number: 20100197763
    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 cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression and/or activity, including PDE4B1, PDE4B2, and PDE4B3 gene expression and/or activity. The present invention is also directed to compounds, compositions, and methods relating to traits, diseases and conditions that respond to the modulation of expression and/or activity of genes involved in cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression pathways or other cellular processes that mediate the maintenance or development of such traits, diseases and conditions, including but not limited to IL-6, IL-7, IL-8, IL-15, TNF-alpha and matrix metalloproteinases (MMPs), such as MMP-I, MMP-2, MMP-3, MMP-9 and MMP-12.
    Type: Application
    Filed: May 2, 2008
    Publication date: August 5, 2010
    Applicant: MERCK & CO., INC.
    Inventors: Vasant Jadhav, Ivan Richards, Walter Strapps, Chandra Vargeese
  • Patent number: 7767399
    Abstract: Methods of isolating clinical-grade plasmid DNA from manufacturing processes, including large-scale fermentation regimes, are disclosed which encompass alternatives to two core unit operations common to plasmid DNA purification processes. The novel upstream and downstream purification processes disclosed herein provide for reduced production costs and increase process robustness. Either or both of the purification processes disclosed herein may be used in combination with additional purification steps known in the art that are associated with DNA plasmid purification technology.
    Type: Grant
    Filed: January 27, 2006
    Date of Patent: August 3, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Jason C. Murphy, David B. Boyd, Adam Joel Kristopeit, Russel Jackson Lander, Michael Albert Winters
  • 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
  • Patent number: 7756644
    Abstract: Methodology for the automated selection and/or optimization of T-cell epitopes is disclosed. The invention provides a data processing system which utilizes sequence-based statistical pattern recognition to compute an epitope selection matrix based on the informational content of epitopes known to bind to a particular major histocompatibility class I allele. The resulting Bayes-corrected scoring matrix is used to predict the relative binding affinities of candidate T-cell epitopes derived from immunologically relevant antigens of self or foreign origin. One aspect of the invention describes an analytical method for identification of modifications in known or predicted T-cell epitopes that confer upon the epitopes the ability to elicit stronger cellular immune response due to more efficient processing and/or presentation to T-cells.
    Type: Grant
    Filed: May 8, 2006
    Date of Patent: July 13, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Arthur Fridman, Ansuman Bagchi, Wendy Bailey
  • Patent number: 7754213
    Abstract: High affinity antibody antagonists of human interleukin-13 receptor alpha 1 are disclosed. The antibody molecules are effective in the inhibition of IL-13R?1-mediated activities and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with hIL-13R?1 activity. The present invention also discloses nucleic acid encoding said antibody molecules, vectors, host cells, and compositions comprising the antibody molecules. Methods of using the antibody molecules for inhibiting or antagonizing IL-13R?1-mediated activities are also disclosed.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: July 13, 2010
    Assignees: Merck & Co., Inc., CSL Limited
    Inventors: Andrew Donald Nash, Manuel Baca, Louis Jerry Fabri, Dennis Zaller, William R. Strohl, Zhiqiang An
  • Patent number: 7745639
    Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: March 4, 2003
    Date of Patent: June 29, 2010
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, J. Christopher Culberson, George D. Hartman, Brenda J. Mariano, Maricel Torrent
  • Patent number: 7744887
    Abstract: Human scFvs are disclosed which interact with a conformational epitope along the pre-hairpin, N-helix coiled coil structure within the heptad repeat 1 (HR1) region of gp41 of HIV. These antibodies, as well as IgG conversions, are shown to neutralize diverse HIV isolates. Isolated nucleic acid molecules are also disclosed which encode relevant portions of these antibodies, as well as the purified forms of the expressed antibodies or relevant antibody fragments, such as VH and VL chains. The antibody compositions disclosed within this specification may provide for a therapeutic treatment against HIV infection by reducing viral load levels within an infected individual, thus prolonging the asymptomatic phase of HIV infection. These antibodies will also be useful in assays to identify HIV antiviral compounds as well as allowing for the identification of candidate HIV vaccines, such as HIV peptide vaccines.
    Type: Grant
    Filed: May 31, 2005
    Date of Patent: June 29, 2010
    Assignees: Merck & Co., Inc., Whitehead Insitute of Biomedical Research, MedImmune Limited, Istitute di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: John W. Shiver, Michael D. Miller, Romas Geleziunas, Daria J. Hazuda, Peter S. Kim, Debra M. Eckert, Michael J. Root, Simon N. Lennard, Elisabetta Bianchi