Patents Assigned to Merck Sharp
  • SUBSTITUTED ARYL SULFONE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
    Publication number: 20130040932
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Application
    Filed: September 24, 2012
    Publication date: February 14, 2013
    Applicants: Neuromed Pharmaceuticals Ltd., Merck Sharp & Dohme Corp.
    Inventors: Merck Sharp & Dohme Corp., Neuromed Pharmaceuticals Ltd.
  • NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS
    Publication number: 20130040929
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Application
    Filed: May 6, 2011
    Publication date: February 14, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jeffrey J. Hale, Jinlong Jiang, Dong-Ming Shen, Zhi-Cai Shi, Min Shu, Zhicai Wu, Cangming Yang
  • Mammalian receptor proteins DCRS5; methods of treatment
    Patent number: 8372402
    Abstract: Nucleic acids encoding mammalian, e.g., primate, receptors, purified receptor proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.
    Type: Grant
    Filed: January 13, 2012
    Date of Patent: February 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Madaline Chirica, Robert A. Kastelein, Kevin Moore, Christi L. Parham
  • CGRP receptor antagonists with tertiary amide, sulfonamide, carbamate and urea end groups
    Patent number: 8372859
    Abstract: Compounds of formula I: (wherein variables A, m, n, J, Re, Rf, R4, Ea, Eb, Ec, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine; and 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: April 7, 2008
    Date of Patent: February 12, 2013
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Michael R. Wood, June Kim, Melody McWherter, Harold G. Selnick, Kathy Schirripa
  • Substituted 4-hydroxypyrimidine-5-carboxamides
    Patent number: 8372857
    Abstract: The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: February 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina Madsen-Duggan
  • Tetrahydro-1H-pyrrolo fused pyridones
    Patent number: 8372863
    Abstract: The present invention relates to tetrahydro-1H-pyrrolo fused pyridone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: February 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew J. Clements, Vincent J. Colandrea, John S. Debenham, Jeffrey J. Hale, Christina B. Madsen-Duggan, Thomas F. Walsh
  • Fused ring thrombin receptor antagonists
    Patent number: 8372980
    Abstract: Fused-ring, heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein ?represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: February 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mariappan V. Chelliah, Samuel Chackalamannil
  • CATHEPSIN CYSTEINE PROTEASE INHIBIORS
    Publication number: 20130035312
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: October 11, 2012
    Publication date: February 7, 2013
    Applicants: Axys Pharmaceuticals, Inc., Merck, Sharp & Dohme, Corp.
    Inventors: Merck, Sharp & Dohme, Corp., Axys Pharmaceuticals, Inc.
  • ISOLATED MAMMALIAN MONOCYTE CELL GENES; RELATED REAGENTS
    Publication number: 20130034561
    Abstract: Nucleic acids encoding various monocyte cell proteins from a primate, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.
    Type: Application
    Filed: October 12, 2012
    Publication date: February 7, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Gosse Jan Adema, Linde Meyaard, Daniel M. Gorman, Terrill K. McClanahan, Sandra M. Zurawski, Gerard Zurawski, Lewis L. Lanier, Joseph H. Phillips
  • Substituted amide beta secretase inhibitors
    Patent number: 8367712
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: February 5, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Ying Huang, Guoqing Li, Andrew W. Stamford
  • Inhibitors of janus kinases
    Patent number: 8367706
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: June 16, 2008
    Date of Patent: February 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Altman, Matthew Christopher, Jonathan B. Grimm, Andrew Haidle, Kaleen Konrad, Jongwon Lim, Rachel N. MacCoss, Michelle Machacek, Ekundayo Osimboni, Ryan D. Otte, Tony Siu, Kerrie Spencer, Brandon Taoka, Paul Tempest, Kevin Wilson, Hyun Chong Woo, Jonathan Young, Anna Zabierek
  • Angiotensin II receptor antagonists
    Patent number: 8367711
    Abstract: A compound having the structure wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2) (C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is; Y1 is selected from the group consisting of C(O)—O— and P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: February 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Iyassu K. Sebhat, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
  • Biaryl carboxamides
    Patent number: 8367679
    Abstract: This invention provides compounds of Formula (I) which are PAFR antagonists: Formula (I) and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: February 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Hyun O. Ok, Debra Ondeyka, Feroze Ujjainwalla, Ellen Vande Bunte
  • Substituted diazepan orexin receptor antagonists
    Patent number: 8362009
    Abstract: The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: January 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeffrey M. Bergman, Paul J. Coleman, Christopher D. Cox, Anthony J. Roecker
  • Engineered anti-IL-23 antibodies
    Patent number: 8362212
    Abstract: Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
    Type: Grant
    Filed: February 13, 2009
    Date of Patent: January 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Leonard G. Presta
  • Spiro-imidazolone derivatives as glucagon receptor antagonists
    Patent number: 8361959
    Abstract: The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: January 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew Stamford, Michael W. Miller, Duane Eugene DeMong, William J. Greenlee, Joseph A. Kozlowski, Brian J. Lavey, Michael K. C. Wong, Wensheng Yu, Xing Dai, De-Yi Yang, Guowei Zhou
  • Primary amine diazeniumdiolate heterocyclic derivatives
    Patent number: 8361994
    Abstract: A compound having the structure useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: January 29, 2013
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Amjad Ali, Michael Man-Chu Lo, Zhiqiang Guo, Brent Whitehead, Timothy J. Henderson, Lin Yan, Shrenik K. Shah
  • Cyclohexyl sulphones for treatment of cancer
    Patent number: 8362075
    Abstract: Sulphones of formula (I) are disclosed for use in treatment of cancer.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: January 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
  • 2,4-disubstituted pyrrolidine orexin receptor antagonists
    Patent number: 8357709
    Abstract: The present invention is directed to 2,4-disubstituted pyrrolidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: January 22, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Christopher D. Cox, John D. Schreier
  • Process for preparing N-alkylated hydroxypyrimidinone compounds
    Patent number: 8357798
    Abstract: Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: January 22, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin M. Belyk, Henry G. Morrison, Philip Jones, Vincenzo Summa, V. Brett Cooper, Amar J. Mahajan, Daniel J. Kumke, Hsien-Hsin Tung, Lawrence Wai, Vanessa Pruzinsky, Philip Pye, Remy Angelaud, Danny Mancheno