Patents Assigned to Merck Sharp & Dohme
  • Patent number: 7732472
    Abstract: The present invention relates to dihydroisoxazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: August 15, 2005
    Date of Patent: June 8, 2010
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.
    Inventors: Mark E. Fraley, Robert M. Garbaccio, George D. Hartman
  • Patent number: 7732438
    Abstract: Compounds of Formula (I) and Formula (II) (where variables R1, R2, R4, A, B, W, X, Y and Z 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, such as headache, 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 is involved.
    Type: Grant
    Filed: October 12, 2005
    Date of Patent: June 8, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Daniel V. Paone, Anthony W. Shaw, Craig M. Potteiger
  • Patent number: 7729864
    Abstract: Methods, computer program products and systems for identifying cellular constituents in a secondary tissue that serve as surrogate markers for a target gene expressed in a primary tissue of a species are provided. A classifier is constructed using cellular constituent abundances of cellular constituents in a first plurality of cellular constituents measured in the secondary tissue in a population. This population comprises a first and second subgroup. The classifier is based on a second plurality of cellular constituents that comprises all or a portion of the first plurality of cellular constituents. Abundance levels of each cellular constituent in the second plurality of cellular constituents varies between the first and second subgroup. All or portion of the population is classified into a plurality of subtypes using the classifier. Then, one or more cellular constituents that can discriminate members of the population between a first subtype and a second subtype in the plurality of subtypes are identified.
    Type: Grant
    Filed: May 28, 2004
    Date of Patent: June 1, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Eric E. Schadt
  • Patent number: 7728141
    Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
    Type: Grant
    Filed: October 29, 2004
    Date of Patent: June 1, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John S. Debenham, George A. Doss, Christina B. Madsen-Duggan, Thomas F. Walsh
  • Patent number: 7728022
    Abstract: Compounds of formula I: are disclosed. The compounds are useful in treating or preventing diseases associated with deposition of A? in the brain.
    Type: Grant
    Filed: May 6, 2005
    Date of Patent: June 1, 2010
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Michela Bettati, Ian Churcher, Victoria Alexandra Doughty, Timothy Harrison, Emmanuela Nizi, Adam Smith
  • Patent number: 7727740
    Abstract: The present invention provides methods for screening for one or more chemical agents that modulate the enzymatic activity of an L-2-hydroxy acid oxidase. The methods comprise the steps of (a) contacting an L-2-hydroxy acid oxidase, in a solution in vitro, with one or more chemical agents in the presence of a substrate that is capable of being oxidized by the L-2-hydroxy acid oxidase; (b) measuring the enzymatic activity of the L-2-hydroxy acid oxidase in the presence of the chemical agent to identify one or more candidate chemical agents that modulate L-2-hydroxy acid oxidase activity in vitro; and (c) administering the one or more identified candidate chemical agents to a test animal and measuring one or more physiological parameters.
    Type: Grant
    Filed: July 21, 2006
    Date of Patent: June 1, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pek Yee Lum, Rebecca Kaplan, Tian-Quan Cai
  • Patent number: 7723352
    Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: September 17, 2004
    Date of Patent: May 25, 2010
    Assignee: Merck Sharp & Dohme
    Inventors: B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
  • Patent number: 7723365
    Abstract: The present invention relates to oxadiazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: August 15, 2005
    Date of Patent: May 25, 2010
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio
  • Patent number: 7718796
    Abstract: An efficient syntheses for the preparation of (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one.
    Type: Grant
    Filed: April 6, 2007
    Date of Patent: May 18, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Palucki, Ian Davies, Dietrich Steinhuebel, Jonathan Rosen
  • Patent number: 7718687
    Abstract: The present invention relates to prodrugs of 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: June 27, 2005
    Date of Patent: May 18, 2010
    Assignee: Merck Sharp & Dohme Corp.,
    Inventors: Paul J. Coleman, Christopher D. Cox, George D. Hartman
  • Patent number: 7718182
    Abstract: The present invention features polypeptides comprising an amino acid sequence structurally related to SEQ ID NO: 1 or a fragment thereof, S. aureus AhpC-AhpF compositions, and uses of such polypeptides and compositions. SEQ ID NO: 1 has a full length S. aureus AhpC sequence. A derivative of SEQ ID NO: 1 containing an amino His-tag and three additional carboxyl amino acids was found to produce a protective immune response against S. aureus.
    Type: Grant
    Filed: January 17, 2006
    Date of Patent: May 18, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rosemarie Kelly, Loren D. Schultz, Mark A. Miller, Mark D. Yeager, Tessie McNeely
  • Patent number: 7718667
    Abstract: The present invention is directed to novel substituted fused aminopiperidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-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: Grant
    Filed: November 22, 2005
    Date of Patent: May 18, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Edmondson, Anthony Mastracchio, Jason M. Cox
  • Patent number: 7709476
    Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: September 17, 2004
    Date of Patent: May 4, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Charles J. McIntyre, David A. Claremon
  • Patent number: 7709010
    Abstract: The present invention relates to pharmaceutical compositions comprising virus-like particles (VLPs) of HPV, said VLPs adsorbed to an aluminum adjuvant, and an ISCOM-type adjuvant comprising a saponin, cholesterol, and a phospholipid. In preferred embodiments, the aluminum adjuvant comprises amorphous aluminum hydroxyphosphate sulfate. Another aspect of the invention provides multi-dose HPV vaccine formulations comprising HPV VLPs and an antimicrobial preservative selected from the group consisting of: m-cresol, phenol and benzyl alcohol. Also provided are methods of using the disclosed pharmaceutical compositions and formulations to induce an immune response against HPV in a human patient and to prevent HPV infection.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: May 4, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Janine T. Bryan, Michelle K. Brownlow, Li Shi, Danilo Casimiro, William L. McClements, Brian K. Meyer, Binghua Hu
  • Patent number: 7709508
    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: February 12, 2009
    Date of Patent: May 4, 2010
    Assignee: Merck Sharp & Dohme
    Inventors: Mark L. Greenlee, Dongfang Meng, Donald M. Sperbeck, Kenneth J. Wildonger
  • Patent number: 7709658
    Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
    Type: Grant
    Filed: July 21, 2006
    Date of Patent: May 4, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lushi Tan, James Christopher McWilliams, Frederick W. Hartner, Naoki Yoshikawa, Wenji Li
  • Patent number: 7705014
    Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: April 10, 2006
    Date of Patent: April 27, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Chixu Chen, Brian W. Eastman, Essa H. Hu
  • Patent number: 7700611
    Abstract: The present invention relates to a process for producing crystalline trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1?-cyclohexane]-4?-carboxamide and novel salts, hydrates and polymorphs thereof.
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: April 20, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Russell R. Ferlita, Yuji Haga, Makoto Ishikawa, Keisuke Kamei, Shinji Kato, Hisaki Kojima, Aaron Moment, Nobuaki Nonoyama, Nobuya Satake, Kazuki Shigemori, Toshihiro Wada, Yaling Wang, Steven A. Weissman, Robert M. Wenslow
  • Patent number: 7700778
    Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: September 30, 2005
    Date of Patent: April 20, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Goulet, Ravi P. Nargund, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner
  • Patent number: 7700772
    Abstract: Compounds of Formula I and Formula II: (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R33, R34, R35, R36, R37, R38, A, j, k, m, n, X, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. 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 chemokine receptors are involved.
    Type: Grant
    Filed: February 8, 2005
    Date of Patent: April 20, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lihu Yang, Alexander Pasternak, Sander G. Mills