Patents Assigned to Merck Sharp
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • Pyrazole carboxamides as inhibitors of 11-?-hydroxysteroid dehydrogenase-1
    Patent number: 7659408
    Abstract: Pyrazole carboxamides 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: August 3, 2004
    Date of Patent: February 9, 2010
    Assignee: Merck Sharp & Dhome Corp.
    Inventors: Ying-Duo Gao, Xin Gu, Nancy J. Kevin, Sherman T. Waddell
  • 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
  • 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
  • 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
  • Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
    Patent number: 7652024
    Abstract: Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands 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 modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: January 26, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Raman K. Bakshi, James P. Dellureficio, Peter H. Dobbelaar, Liangqin Guo, Shuwen He, Qingmei Hong, Ravi P. Nargund, Zhixiong Ye
  • Octahydropyrano[3,4-C]pyrrole tachykinin receptor antagonists
    Patent number: 7652058
    Abstract: The present invention is directed to certain hydropyranopyrrolidine 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 formations 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: December 12, 2005
    Date of Patent: January 26, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert J. DeVita, Jinlong Jiang, Sander G. Mills, Jonathan R. Young
  • Hydroisoindoline tachykinin receptor antagonists
    Patent number: 7645790
    Abstract: The present invention is directed to certain hydroisoindoline compounds of formula I 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: January 26, 2005
    Date of Patent: January 12, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jaime Lynn Bunda, Robert J. DeVita, Jinlong Jiang, Sander G. Mills
  • Piperidines and related compounds for treatment of alzheimer's disease
    Patent number: 7638629
    Abstract: Compounds of formula I: selectively inhibit production of A?(1-42) and hence are useful in treatment or prevention of disease associated with deposition of ?-amyloid in the brain.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: December 29, 2009
    Assignee: Merck Sharp & Dohme Ltd,
    Inventors: Joanne Clare Hannam, Janusz Jozef Kulagowski, Andrew Madin, Mark Peter Ridgill, Eileen Mary Seward