Patents Assigned to Merck & Co., Inc.
  • Patent number: 7521207
    Abstract: The Macaca mulatta (rhesus monkey) Nur77 (rhNur77) nuclear receptor and the nucleic acid encoding the rhNur77 nuclear receptor are described. Further described are methods for identifying analytes that modulate expression or activity of the rhNur77 nuclear receptor. Analytes that affect Nur77 expression or activity may be used to treat or inhibit inflammatory diseases, for example, osteoarthritis and various bone, neurological, and prostrate disorders. The rhNur77 may also be used to treat various cancers, for example, prostate, ovarian, colon, lung, and gastric cancer.
    Type: Grant
    Filed: March 16, 2006
    Date of Patent: April 21, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Carlo J. Gambone, Azriel Schmidt
  • Patent number: 7517532
    Abstract: 8,9-Dihydroxydihydropyridopyrazine-1,6-diones and 8,9-dihydroxypyridopyrazine-1,6-diones are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the pyridopyrazinediones are of Formula (I): (I), wherein R1, R2, R3, R4 and R5 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.
    Type: Grant
    Filed: September 10, 2003
    Date of Patent: April 14, 2009
    Assignee: Merck & Co., Inc.
    Inventors: John S. Wai, Boyoung Kim, Thorsten E. Fisher, Peter D. Williams, H. Marie Langford
  • Patent number: 7514409
    Abstract: Compounds of Formula I are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn's disease, multiple sclerosis, asthma, and rheumatoid arthritis.
    Type: Grant
    Filed: March 7, 2005
    Date of Patent: April 7, 2009
    Assignee: Merck & Co., Inc.
    Inventors: William K. Hagmann, Linus S. Lin, Ping Liu, Richard A. Mumford, Thomas S. Reger, Nicholas D. Smith, Nicholas S. Stock, Jasmine Zunic
  • Patent number: 7514431
    Abstract: The present invention is directed to compounds of the formula I: I (wherein R1, R2, R3, R4, R5, R6, X, Z and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: April 7, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Changyou Zhou, Alexander Pasternak, Lihu Yang
  • Publication number: 20090087492
    Abstract: The present invention relates to a process, for the production of crystalline particles of an active organic compound The process includes the steps of generating a micro-seed by a wet-milling process and subjecting the micro-seed to a crystallization process. The resulting crystalline particles have a mean particle size of less than about 100 ?m. The present invention also provides for a pharmaceutical composition which includes the crystalline particles produced by the method described herein and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: March 12, 2007
    Publication date: April 2, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Brian K. Johnson, Hsien Hsin Tung, Ivan Lee, Aaron S. Cote, Cindy Starbuck, Michael Midler
  • Patent number: 7511152
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: December 5, 2005
    Date of Patent: March 31, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Dongfang Meng, Donald M. Sperbeck, Kenneth J. Wildonger
  • Patent number: 7507858
    Abstract: This invention relates to iminodiacetic acid and diamine hydroxamic acid derivatives, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: March 24, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Sandro Belvedere, Thomas A. Miller, David J. Witter
  • Patent number: 7507836
    Abstract: The present invention is directed to compounds which are allosteric modulators of metabotropic glutamate receptors, including the mGluR5 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: March 22, 2004
    Date of Patent: March 24, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Mark E. Duggan, Craig W. Lindsley, David D. Wisnoski
  • Patent number: 7504402
    Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
    Type: Grant
    Filed: December 14, 2004
    Date of Patent: March 17, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Sherman T. Waddell, Gina M. Santorelli, Milana M. Maletic, Aaron H. Leeman, Xin Gu, Donald W. Graham, James M. Balkovec, Susan D. Aster
  • Patent number: 7504429
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a substituted pyrrole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Grant
    Filed: July 20, 2004
    Date of Patent: March 17, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Annette S. Kim, Xufang Zhang
  • Patent number: 7504425
    Abstract: This invention relates to compounds of formula (I), and a method for treating anthrax or inhibiting lethal factor by administrating a composition containing a compound of formula (I) and a pharmaceutically acceptable carrier. This invention further relates to the use of the compounds of formula (I) to treat other conditions related to an anthrax infection.
    Type: Grant
    Filed: May 23, 2003
    Date of Patent: March 17, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Yusheng Xiong, Kevin Chapman, Suresh Singh, Jian Guo, Arthur A. Patchett
  • Patent number: 7501435
    Abstract: The instant invention provides for compounds which comprise substituted triazoloquinazolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: April 24, 2007
    Date of Patent: March 10, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Arrington, Edward J. Brnardic, Vadim Y. Dudkin, Mark E. Fraley, Shaei Y. Huang, Cheng Wang
  • Patent number: 7498036
    Abstract: Synthetic DNA molecules encoding the HPV58 L1 protein are provided. Specifically, the present invention provides polynucleotides encoding HPV58 L1 protein, wherein said polynucleotides are codon-optimized for high level expression in a yeast cell. The synthetic molecules may be used to produce HPV58 virus-like particles (VLPs), and to produce vaccines and pharmaceutical compositions comprising the HPV58 VLPs. The vaccines of the present invention provide effective imnunoprophylaxis against papillomavirus infection through neutralizing antibody and cell-mediated immunity and are also useful for treatment of existing HPV infections.
    Type: Grant
    Filed: November 10, 2004
    Date of Patent: March 3, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Janine T. Bryan, Michelle K. Brownlow, Loren D. Schultz, Xin-Min Wang, Kathrin U. Jansen
  • Patent number: 7495123
    Abstract: The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.
    Type: Grant
    Filed: April 5, 2005
    Date of Patent: February 24, 2009
    Assignees: Solvias AG, Merck & Co., Inc.
    Inventors: Yi Xiao, Yongkui Sun, Thorsten Rosner, Nelo R. Rivera, Shane W. Krska, Andrew M. Clausen, Joseph D. Armstrong, III, Felix Spindler, Christophe Malan
  • Patent number: 7495029
    Abstract: Disclosed are prodrugs of (2R)-2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: February 24, 2009
    Assignee: Merck & Co., Inc
    Inventors: Benito Munoz, Joseph E. Payne, Petpiboon Prasit, Thomas S. Reger, Nicholas D. Smith
  • Patent number: 7494983
    Abstract: This invention relates to potent potassium channel blocker compounds of structural Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
    Type: Grant
    Filed: August 31, 2004
    Date of Patent: February 24, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Meng Hsin Chen, James B. Doherty, Luping Liu, Swaminathan Natarajan, Robert M. Tynebor
  • Patent number: 7495020
    Abstract: A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.
    Type: Grant
    Filed: January 18, 2006
    Date of Patent: February 24, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, A. Brian Jones, Joel P. Berger, James F. Dropinski, Alexander Elbrecht, Kun Liu, Karen Lamb MacNaul, Guo-Qiang Shi, Derek J. Von Langen, Gaochao Zhou
  • Publication number: 20090047702
    Abstract: Methods for identifying modulators of KEAH6 are described. The methods are particularly useful for identifying analytes that antagonize KEAH6's effect on processing of amyloid precursor protein to A? peptide and thus useful for identifying analytes that can be used for treating Alzheimer disease.
    Type: Application
    Filed: June 14, 2006
    Publication date: February 19, 2009
    Applicant: MERCK & CO., INC.
    Inventors: John M. Majercak, William J. Ray, David J. Stone
  • Patent number: 7491737
    Abstract: The present invention is directed to compounds of the formula (I): (wherein R1, R2, R3, R4, R5, R6, R10 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: February 17, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Stephen D. Goble, Alexander Pasternak, Lihu Yang
  • Patent number: 7491713
    Abstract: Compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, D, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, pharmaceutical compositions comprising these compounds, use of these compounds and compositions to prevent or treat diseases involving CGRP.
    Type: Grant
    Filed: January 25, 2005
    Date of Patent: February 17, 2009
    Assignee: Merck + Co., Inc.
    Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W Shaw, Craig A. Stump, Theresa M. Williams