Patents Assigned to Merck Sharp
  • Cyclic amine BACE-1 inhibitors having a benzamide substituent
    Patent number: 8278334
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables 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 pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Substituted pyridines that are JNK inhibitors
    Patent number: 8278337
    Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme
    Inventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, Jr., Umar Faruk Mansoor
  • Substituted 4-hydroxypyrimidine-5-carboxamides
    Patent number: 8278304
    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: March 12, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina B. Madsen-Duggan, Thomas F. Walsh
  • Inhibitors of Janus kinases
    Patent number: 8278335
    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: April 9, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michelle R. Machacek, Andrew Haidle, Anna A. Zabierek, Kaleen M. Konrad, Michael D. Altman
  • Potassium channel inhibitors
    Patent number: 8278317
    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: July 18, 2006
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: B. Wesley Trotter, Kausik K. Nanda, Scott E. Wolkenberg, M. Brad Nolt, David Wisnoski
  • Quinolizidinone M1 receptor positive allosteric modulators
    Patent number: 8278453
    Abstract: The present invention is directed to quinolizidinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Christina Ng Di Marco
  • Quinolizidinone M1 receptor positive allosteric modulators
    Patent number: 8273737
    Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: September 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang
  • N-substituted oxindoline derivatives as calcium channel blockers
    Patent number: 8273749
    Abstract: A series of N-substituted oxindole 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: Grant
    Filed: September 30, 2008
    Date of Patent: September 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Scott B. Hoyt, Clare London
  • RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (SINA)
    Patent number: 8273866
    Abstract: The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism.
    Type: Grant
    Filed: November 24, 2003
    Date of Patent: September 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James McSwiggen, Leonid Beigelman
  • ANGIOTENSIN II RECEPTOR ANTAGONISTS
    Publication number: 20120238608
    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: Application
    Filed: May 30, 2012
    Publication date: September 20, 2012
    Applicant: Merck Sharp & Dohme
    Inventors: Amjad Ali, Michael Man-chu Lo, Iyassu K. Sebhat, Chris Franklin, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
  • RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (siNA)
    Patent number: 8268986
    Abstract: The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism.
    Type: Grant
    Filed: May 11, 2011
    Date of Patent: September 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonid Beigelman, James McSwiggen
  • Pharmaceutical composition comprising oxyntomodulin derivatives and a method for reducing body weight using the composition
    Patent number: 8268779
    Abstract: Modified oxyntomodulin derivatives. Such derivatives can be used for the treatment of metabolic diseases such as diabetes and obesity.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: September 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ranabir Sinha Roy, Elisabetta Bianchi, Antonello Pessi, Paolo Ingallinella, Donald J. Marsh, George J. Eiermann, Yingjun Mu, Yun-Ping Zhou
  • 5, 6-ring annulated indole derivatives and use thereof
    Patent number: 8268803
    Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: September 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Frank Bennett, Srikanth Venkatraman, F. George Njoroge, Kevin X. Chen, Neng-Yang Shih, Stuart B. Rosenblum, Joseph A. Kozlowski
  • METHOD FOR PRODUCING PROTEINS IN PICHIA PASTORIS THAT LACK DETECTABLE CROSS BINDING ACTIVITY TO ANTIBODIES AGAINST HOST CELL ANTIGENS
    Publication number: 20120232007
    Abstract: Methods for producing proteins and glycoproteins in Pichia pastoris that lack detectable cross binding activity to antibodies made against host cell antigens are described. In particular, methods are described wherein recombinant Pichia pastoris strains that do not display a ?-mannosyltransferase 2 activity with respect to an N-glycan or O-glycan and do not display at least one activity selected from a ?-mannosyltransferase 1, 3, and 4 activity to produce recombinant proteins and glycoproteins. These recombinant Pichia pastoris strains can produce proteins and glycoproteins that lack detectable ?-mannosidase resistant ?-mannose residues thereon and thus, lack cross binding activity to antibodies against host cell antigens. Further described are methods for producing bi-sialylated human erythropoietin in Pichia pastoris that lack detectable cross binding activity to antibodies against host cell antigens.
    Type: Application
    Filed: October 11, 2010
    Publication date: September 13, 2012
    Applicant: MERCK SHARP & DOHME CORP
    Inventors: Piotr Bobrowicz, Sujatha Gomathinayagam, Stephen Hamilton, Huijuan Li, Natarajan Sethuraman, Terrance A. Stadheim, Stefan Wildt
  • FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY
    Publication number: 20120232086
    Abstract: The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 13, 2012
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew W. Stampford
  • Antifungal composition with enhanced bioavailability
    Patent number: 8263600
    Abstract: A liquid suspension comprising an antifungally effective amount of the micronized compound represented by the chemical structural formula I: at least one thickening agent, a non-ionic surfactant, and a pharmaceutically acceptable liquid carrier is disclosed.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Stefan Sharpe, Joel Sequeira, David Harris, Shashank Mahashabde
  • Method for detecting autoprocessed, secreted PCSK9
    Patent number: 8263353
    Abstract: The present invention provides a method for detecting autoprocessed, secreted PCSK9, a protein involved in cholesterol homeostasis, and for effectively identifying compounds that inhibit autocleavage and secretion from cells. The disclosed method involves the insertion of an epitope tag into a PCSK9 expression construct immediately C-terminal to the pro domain ending at an amino acid residue corresponding to Q152 of human PCSK9. Upon autoprocessing, the epitope tag is exposed and capable of recognition by anti-epitope antibodies or other suitable identification system, allowing for the selective and exclusive identification and/or quantification of processed PCSK9. The present disclosure thus advances the goal of providing enabling technology to the art for the effective identification of therapeutics effective in combating coronary heart disease.
    Type: Grant
    Filed: March 21, 2008
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ayesha Sitlani, Timothy S. Fisher, Joseph C. Santoro
  • Pyridyl amide T-type calcium channel antagonists
    Patent number: 8263627
    Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels 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 T-type calcium channels are involved.
    Type: Grant
    Filed: January 18, 2011
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Thomas S. Reger, Zhi-Qiang Yang
  • OXO bridged diazepan orexin receptor antagonists
    Patent number: 8263586
    Abstract: The present invention is directed to oxo bridged diazepan 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: May 14, 2008
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, David B. Whitman
  • NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS
    Publication number: 20120225886
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: August 24, 2010
    Publication date: September 6, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gregori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman