Patents Assigned to Merck & Co.
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Publication number: 20100298288Abstract: Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moietyType: ApplicationFiled: June 16, 2008Publication date: November 25, 2010Applicant: MERCK & CO., INCInventors: Julianne A. HUNT, Ramzi F. Sweis, Dooseop Kim, Florida Kallashi, Peter J. Sinclair
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Publication number: 20100298342Abstract: 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: ApplicationFiled: September 4, 2007Publication date: November 25, 2010Applicants: 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
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Publication number: 20100275625Abstract: 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: ApplicationFiled: July 8, 2010Publication date: November 4, 2010Applicant: MERCK & CO, INC.Inventor: Alan J. Lowenstein
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Patent number: 7820680Abstract: 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: GrantFiled: March 4, 2005Date of Patent: October 26, 2010Assignee: Merck & Co., Inc.Inventors: Peter D. Williams, John S. Wai, Mark W. Embrey, Donnette D. Staas, Linghang Zhuang
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Patent number: 7811563Abstract: 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: GrantFiled: October 21, 2005Date of Patent: October 12, 2010Assignees: 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
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Publication number: 20100256106Abstract: 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: ApplicationFiled: November 25, 2008Publication date: October 7, 2010Applicant: MERCK & CO., INC.Inventors: Alexander Pasternak, Michael J. Szymonifka
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Publication number: 20100256698Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: ApplicationFiled: April 2, 2010Publication date: October 7, 2010Applicant: MERCK & CO., INC.Inventors: B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
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Patent number: 7807829Abstract: 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: GrantFiled: November 3, 2005Date of Patent: October 5, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: James Michael McNamara, Louis Matty, Jonathan D. Rosen
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Publication number: 20100227903Abstract: 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: ApplicationFiled: February 9, 2007Publication date: September 9, 2010Applicant: MERCK & CO., INC.Inventors: Sarah Geers, Michael Lowinger, Craig A. McKelvey, Robert F. Meyer, Dina Zhang
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Patent number: 7790739Abstract: 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: GrantFiled: October 18, 2006Date of Patent: September 7, 2010Assignee: Merck & Co., Inc. and Merck Sharp & Dohme Corp.Inventors: Jongwon Lim, Ana Esther Gabarda Ortega
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Publication number: 20100222322Abstract: 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: ApplicationFiled: June 23, 2006Publication date: September 2, 2010Applicant: MERCK & CO., INC.Inventors: Scott E. Wolkenberg, Zhijian Zhao, Craig W. Lindsley
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Patent number: 7786287Abstract: 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: GrantFiled: April 11, 2003Date of Patent: August 31, 2010Assignee: Merck & Co., Inc.Inventors: Osvaldo A. Flores, Jay Grobler, Edward M. Murray, Paul D. Zuck
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Patent number: 7780963Abstract: 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: GrantFiled: October 21, 2005Date of Patent: August 24, 2010Assignees: Merck & Co., Inc., Northwestern UniversityInventors: 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
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Publication number: 20100204486Abstract: 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: ApplicationFiled: April 27, 2007Publication date: August 12, 2010Applicant: MERCK & CO., INC.Inventors: Edward G. Corley, Jerry A. Murry, Bryon Simmons, Feng Xu
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Publication number: 20100197763Abstract: 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: ApplicationFiled: May 2, 2008Publication date: August 5, 2010Applicant: MERCK & CO., INC.Inventors: Vasant Jadhav, Ivan Richards, Walter Strapps, Chandra Vargeese
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Patent number: 7767399Abstract: 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: GrantFiled: January 27, 2006Date of Patent: August 3, 2010Assignee: Merck & Co., Inc.Inventors: Jason C. Murphy, David B. Boyd, Adam Joel Kristopeit, Russel Jackson Lander, Michael Albert Winters
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Patent number: 7763634Abstract: 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: GrantFiled: June 5, 2007Date of Patent: July 27, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: Jonathan R. Young, Andrew Haidle, Paul Tempest, Michelle Machacek
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Patent number: 7754213Abstract: 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: GrantFiled: October 19, 2007Date of Patent: July 13, 2010Assignees: Merck & Co., Inc., CSL LimitedInventors: Andrew Donald Nash, Manuel Baca, Louis Jerry Fabri, Dennis Zaller, William R. Strohl, Zhiqiang An
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Patent number: 7756644Abstract: 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: GrantFiled: May 8, 2006Date of Patent: July 13, 2010Assignee: Merck & Co., Inc.Inventors: Arthur Fridman, Ansuman Bagchi, Wendy Bailey
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Patent number: 7744887Abstract: 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: GrantFiled: May 31, 2005Date of Patent: June 29, 2010Assignees: 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