Patents Assigned to Merck & Co., Inc.
  • Potassium channel inhibitors
    Patent number: 7569589
    Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: July 25, 2005
    Date of Patent: August 4, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Christopher J. Dinsmore, Jeffrey M. Bergman, B. Wesley Trotter, Lou Anne Neilson, Zhicai Wu, Peter Manley, John Hartnett
  • Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5
    Patent number: 7569592
    Abstract: Pyrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, circadian rhythm disorders, and other diseases.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: August 4, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Nicholas D. P. Cosford, Chixu Chen, Brian W. Eastman, Dehua Huang, Benito Munoz, Petpiboon Prasit, Nicholas D. Smith
  • Canis sphingosine 1-phosphate receptor isoform 5
    Publication number: 20090191578
    Abstract: A Canis sphingosine-1-phosphate (S1P) receptor isoform 5 (cS1P5), the nucleic acid encoding the cS1P5 receptor, and methods for using the cS1P receptor and the nucleic acid encoding the cS1P5 receptor in assays for identifying analytes which modulate activity of the cS1P5 receptor. The assay is useful for identifying analytes for treating or preventing diseases associated with S1P5 activity.
    Type: Application
    Filed: July 22, 2005
    Publication date: July 30, 2009
    Applicant: MERCK & CO., INC
    Inventors: Suzanne M. Mandala, James A. Milligan
  • Human Niemann Pick C1-Like 1 Gene (NPC1L1) Polymorphisms and Methods of Use Thereof
    Publication number: 20090192135
    Abstract: The present invention relates to the identification and use of single nucleotide polymorphisms and haplotypes in the Niemann Pick C1-Like 1 (NPC1L1) gene. In particular, methods are provided for correlating NPC1L1 polymorphisms and haplo-types with the responsiveness of a pharmaceutically active compound administered to a human subject. The invention further relates to a method for estimating the responsiveness of a pharmaceutically active compound administered to a human subject which method comprises determining at least one polymorphism in the NPC1L1 gene. The methods are based on determining polymorphisms in the NPC1L1 gene and correlating the responsiveness of a pharmaceutically active compound in the human by reference to one or more polymorphism in NPC1L1.
    Type: Application
    Filed: March 28, 2006
    Publication date: July 30, 2009
    Applicants: SCHERING CORPORATION, MERCK & CO., INC., ROSETTA INPHARMATICS LLC
    Inventors: Jason Samuel Simon, Maha Chabhar Karnoub, Michael E. Severino, David James Devlin, Andrew Stewart Plump, Eric E. Schadt
  • 3,3-disubstituted tetrahydropyranyl cyclopentyl amide modulators of chemokine receptor activity
    Patent number: 7566726
    Abstract: (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, Y and Z are 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: April 22, 2005
    Date of Patent: July 28, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Lihu Yang, Sander G. Mills, Kothandaraman Shankaran
  • Benzamidazoles, compositions containing such compounds and methods of use
    Patent number: 7563815
    Abstract: The present invention relates to substituted benzimidazoles, 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: May 5, 2004
    Date of Patent: July 21, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Emma R. Parmee, Ronald M. Kim, Rui Liang, Jiang Chang, Elizabeth Ashley Rouse, Kevin T. Chapman
  • Ophthalmic compositions for treating ocular hypertension
    Patent number: 7563816
    Abstract: This invention relates to potent potassium channel blocker compounds of 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: July 15, 2005
    Date of Patent: July 21, 2009
    Assignee: Merck & Co. Inc.
    Inventors: James B. Doherty, Dong-Ming Shen
  • Removal of aldehyde impurity by reactive polystyrene resini
    Patent number: 7563807
    Abstract: A purification method in the preparation of a substituted 8-arylquinoline, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, utilizes a polystyrene-based sulfonylhydrazine reactive resin to remove an aldehyde impurity.
    Type: Grant
    Filed: September 12, 2003
    Date of Patent: July 21, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Mirlinda Biba, Paul Compton Collins, Christopher Joseph Welch, David A. Conlon, Antoinette Drahus
  • TRIAZOLE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE-1
    Publication number: 20090181994
    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: Application
    Filed: February 3, 2009
    Publication date: July 16, 2009
    Applicant: 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
  • Polymorphic form of montelukast sodium
    Patent number: 7560559
    Abstract: The invention provides novel polymorphic form of montelukast sodium, as well as methods of using and pharmaceutical compositions containing saud novel form. Also provided are montelukast sodium: acetonitrile solvates, which are intermediates in the formation of crystalline montelukast sodium.
    Type: Grant
    Filed: April 12, 2004
    Date of Patent: July 14, 2009
    Assignees: Merck & Co., Inc., Merck Frosst Canada & Co.
    Inventors: Jun-Hong Chou, Michael B. Gentzler, James N. Michaels, Cynthia Bazin, Sophie-Dorothee Clas, Chad Dalton, Michael Guojie Wu
  • Tyrosine kinase inhibitors
    Patent number: 7560546
    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 sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Grant
    Filed: August 5, 2003
    Date of Patent: July 14, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Douglas C. Beshore, Jeffrey M. Bergman, Craig W. Lindsley
  • 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
    Patent number: 7560455
    Abstract: The pre-sent invention is directed to 3-amino-4-phenylbutanoic acid 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 10, 2004
    Date of Patent: July 14, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Danqing Dennis Feng, Gui Bai Liang, Xiaoxia Qian
  • Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity
    Patent number: 7557124
    Abstract: Compounds of Formula I: (wherein n, R1, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, 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: April 22, 2005
    Date of Patent: July 7, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Lihu Yang, Sander G. Mills, Richard Jiao
  • Aminocyclopentyl fused heterotricylicamide modulators of chemokine receptor activity
    Patent number: 7557120
    Abstract: The present invention is directed to compounds of formulae (I and II)(wherein A, D, E, X, l, m, n and R1 through R18 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: February 23, 2004
    Date of Patent: July 7, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Stephen D. Goble, Alexander Pasternak, Cheng Tang, Changyou Zhou, Lihu Yang
  • Acylated Spiropiperidine Derivatives as Melanocortin-4 Receptor Modulators
    Publication number: 20090170863
    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: Application
    Filed: September 25, 2006
    Publication date: July 2, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Tianying Jian, Jian Liu, Ravi P. Nargund
  • Amino cyclobutylamide modulators of chemokine receptor activity
    Patent number: 7553841
    Abstract: The present invention is directed to compounds of the formulas I and II: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R25, R26, Y, Z, l, m, n and the broken lines are as 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: March 15, 2004
    Date of Patent: June 30, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Richard Jiao, Lihu Yang
  • Mitotic kinesin inhibitors
    Patent number: 7553838
    Abstract: The present invention relates to 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: June 30, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Mark E. Fraley, George D. Hartman
  • Tyrosine kinase inhibitors
    Patent number: 7550478
    Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine compounds, 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: Grant
    Filed: June 22, 2006
    Date of Patent: June 23, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Christopher J. Dinsmore, Ana Esther Gabarda Ortega, David J. Guerin, James P. Jewell, Jason D. Katz, Jongwon Lim, Michelle R. Machacek, Ryan D. Otte, Jonathan R. Young
  • Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease
    Patent number: 7550481
    Abstract: The present invention is directed to phenylamide and pyridylamide derivative compounds of 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: December 15, 2004
    Date of Patent: June 23, 2009
    Assignee: Merck & Co., Inc.
    Inventors: James C. Barrow, Craig A. Coburn, Philippe G. Nantermet, Harold G. Selnick, Shawn J. Stachel, Matthew G. Stanton, Shaun R. Stauffer, Linghang Zhuang, Jennifer R. Davis
  • Inhibitors of checkpoint kinases
    Patent number: 7550477
    Abstract: The instant invention provides for compounds which comprise fused pyrazoles 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: December 29, 2006
    Date of Patent: June 23, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Brnardic, Mark E. Fraley