Patents Assigned to Merck Sharp & Dohme
  • Anti-hypercholesterolemic compounds
    Patent number: 7696177
    Abstract: This invention provides cholesterol absorption inhibitors of Formula (I), and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: April 13, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert J. DeVita, Greg J. Morriello, Anthony K. Ogawa, Feroze Ujjainwalla
  • Tricyclic anilide spirolactam CGRP receptor antagonists
    Patent number: 7696192
    Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are 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: September 6, 2005
    Date of Patent: April 13, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
  • 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
    Patent number: 7696217
    Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: April 13, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William P. Dankulich, Mildred L. Kaufman, Robert S. Meissner, Helen J. Mitchell
  • Quinoline potassium channel inhibitors
    Patent number: 7692017
    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: April 6, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman
  • Triazole derivatives which are SMO antagonists
    Patent number: 7691887
    Abstract: The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a composition comprising a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof; wherein: 2 of X, Y and Z represent nitrogen atoms, and the other represents an oxygen atom; R1 and R2 are taken together with the atom to which they are attached and represent a cyclobutyl ring, optionally substituted with 1-2 fluorine atoms, and R3 represents hydrogen or a fluorine atom; or R1 represents methyl, R2 represents methyl or a fluorine atom and R3 represents a fluorine atom.
    Type: Grant
    Filed: April 15, 2008
    Date of Patent: April 6, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James M. Balkovec, Rolf Thieringer, Sherman T. Waddell
  • Isoquinoline potassium channel inhibitors
    Patent number: 7691879
    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: April 6, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: B. Wesley Trotter, Kausik K. Nanda, Nathan R. Kett, Christopher J. Dinsmore, Gerald S. Ponticello, David A. Claremon
  • 1,2,4-Oxadiazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 7687492
    Abstract: The present invention is directed to novel 1,2,4-oxadiazole derivatives 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: Grant
    Filed: April 29, 2005
    Date of Patent: March 30, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jinyou Xu, Lan Wei, Anthony Mastracchio, Scott D. Edmondson
  • Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
    Patent number: 7687534
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: March 30, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John E. Stelmach, Emma R. Parmee, James R. Tata, Keith G. Rosauer, Ronald M. Kim, Amy R. Bittner, Jiang Chang, Christopher Joseph Sinz
  • Crystalline forms of antidiabetic compounds
    Patent number: 7683092
    Abstract: Novel crystalline forms of two indole compounds connected to phenoxyalkylcarboxylic acid groups are selective PPAR gamma partial agonists that are useful in the treatment of type 2 diabetes, hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. The novel crystal forms include a crystalline free acid dihydrate and crystalline free acid anhydrate of one compound and several crystalline forms of the free acid and the sodium salt of the second compound. The invention also relates to pharmaceutical compositions comprising these novel crystal forms, processes to prepare the crystal forms and their pharmaceutical compositions, and uses of the crystal forms in the treatment of type 2 diabetes and other PPAR gamma modulated diseases.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: March 23, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dalian Zhao, Jean-Francois Marcoux, David Boardman, Aquiles E. Leyes
  • Hydroisoindoline tachykinin receptor antagonists
    Patent number: 7683068
    Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
    Type: Grant
    Filed: June 23, 2006
    Date of Patent: March 23, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jinlong Jiang, Robert J. DeVita, Sanjeev Kumar, Sander G. Mills, Richard A. Tschirret-Guth
  • Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 7678783
    Abstract: The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I) 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: Grant
    Filed: November 14, 2005
    Date of Patent: March 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Stacey Lindsley, Keith P. Moore, Shawn J. Stachel
  • Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 7678905
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: March 27, 2007
    Date of Patent: March 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber
  • Cyclohexylalanine derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 7671073
    Abstract: The present invention is directed to novel cyclohexylalanine derivatives 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: Grant
    Filed: May 13, 2005
    Date of Patent: March 2, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, David E. Kaelin, Jr., Ann E. Weber, Brian A Kirk
  • Polynucleotides encoding coccidian parasite casein kinase I, a chemotherapeutic target for antiprotozoal agents
    Patent number: 7671181
    Abstract: Isolated nucleic acid molecules encoding coccidian casein kinase I, CKI, enzymes from the species Eimeria tenella and Toxoplasma gondii are disclosed. The isolation of these coccidian CKI cDNA sequences results in the disclosure of purified forms of E. tenella and T. gondii CKI proteins, recombinant vectors and recombinant hosts which express coccidian CKI.
    Type: Grant
    Filed: January 12, 2005
    Date of Patent: March 2, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert G. K. Donald, Paul Liberator, Xiaotian Zhong
  • Selective spirocyclic glucocorticoid receptor modulators
    Patent number: 7662846
    Abstract: The present invention encompasses compounds of Formula (I) and Formula (II) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: April 19, 2004
    Date of Patent: February 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, James M. Balkovec, Richard Beresis, Steven L. Colletti, Donald W. Graham, Gool F. Patel, Cameron J. Smith
  • CGRP receptor antagonists
    Patent number: 7659264
    Abstract: The present invention is directed to compounds of Formula I: Formula I: I and Formula II: (where variables R1, R2, R3, R4, A, B, J, Q, T, V, 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, 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 5, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, James Z. Deng, Craig Potteiger, Theresa M. Williams
  • Monocyclic anilide spirolactam CGRP receptor antagonists
    Patent number: 7659300
    Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c 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: September 6, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump
  • Piperidine and azetidine derivatives as GlyT1 inhibitors
    Patent number: 7655644
    Abstract: The present invention provides compounds of formula (I), wherein both p's are one or two, R1 is generally heteroaryl or cycloalkyl, R2 is C3-6cycloalkyl or phenyl and R3 is heteroaryl, and pharmaceutically acceptable salts thereof, as GlyT1 inhibitors for treating schizophrenia, pharmaceutical compositions comprising the same and methods for their preparation.
    Type: Grant
    Filed: December 21, 2005
    Date of Patent: February 2, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Wesley Peter Blackaby, Stephen Robert Fletcher, Andrew Jennings, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street, Joanne Thomson
  • Inhibitors of Akt activity
    Patent number: 7655649
    Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: April 5, 2005
    Date of Patent: February 2, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
  • Gamma-secretase inhibitors
    Patent number: 7655675
    Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase and hence find use in treatment of Alzheimer's disease.
    Type: Grant
    Filed: October 1, 2004
    Date of Patent: February 2, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Alan John Nadin, Andrew Pate Owens, Martin Richard Teall