Patents Assigned to Merck Sharp
  • Publication number: 20140206563
    Abstract: A group of polypeptides that are modulated in a psoriatic sample as compared to a normal sample is provided. These polypeptides can be used as biomarkers for diagnosis and monitoring treatment of psoriasis.
    Type: Application
    Filed: January 21, 2014
    Publication date: July 24, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: Maribel Beaumont
  • Publication number: 20140206627
    Abstract: The invention relates to kisspeptide-pentasaccharide conjugates having the general formula (I) wherein Z1 is Tyr or D-Tyr; Z3 is Trp, Hyp, Phe or Lys(R2); Z5 is Thr, Aib or Ala; Z7 is Gly or azaGly; Z8 is Leu; or Z7 and Z8 together represent; Z10 is Phe or Trp; n is 0 or 1; or R2, when present, represents a pentasaccharide derivative having the formula (II) wherein R is methyl or SO3X; X is a positively charged counterion; with the proviso that when R2 is present, R1 is H or (C1-6) alkylcarbonyl; R3 is H or (C1-3)alkyl; and L represents a pharmacologically inactive linker moiety having 10-50 atoms; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same as well as to the use of said kisspeptide-pentasaccharide conjugates in the treatment of female infertility.
    Type: Application
    Filed: August 1, 2012
    Publication date: July 24, 2014
    Applicant: Merck Sharp & Dohme B.V.
    Inventors: Marion Blomenrohr, Martin De Kort, Miranda Maria Cornelia Van Der Lee, Jeffry Abraham Jacobus Wisse
  • Publication number: 20140206675
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (A?) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination nation with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers disease, are also disclosed.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Jeffrey A. Misiaszek, Guoqing Li
  • Publication number: 20140206665
    Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.
    Type: Application
    Filed: August 10, 2012
    Publication date: July 24, 2014
    Applicants: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Harold G. Selnick, Kun Liu, Ernest J. McEachern, Yuanxi Zhou, Yongbao Zhu
  • Patent number: 8785467
    Abstract: The present invention is directed to 2-alkoxy pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: September 26, 2011
    Date of Patent: July 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, Izzat T. Raheem, William D. Shipe, Cory R. Theberge
  • Patent number: 8785482
    Abstract: The present invention is directed to cyclohexene benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: July 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Scott D. Kuduk
  • Patent number: 8785481
    Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: July 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Vadim Dudkin, Robert M. Garbaccio, Adam W. Johnson, Scott D. Kuduk, Jason W. Skudlarek, Cheng Wang, Mark E. Fraley
  • Patent number: 8785634
    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 enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: July 22, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Fa-Xiang Ding, JinLong Jiang, Dong-Ming Shen, Hong Shen, Zhi-Cai Shi
  • Publication number: 20140200180
    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: January 15, 2014
    Publication date: July 17, 2014
    Applicant: Merck Sharp & Dohme Corp
    Inventors: Piotri Bobrowicz, Sujatha Gomathinayagam, Stephen Hamilton, Huijuan Li, Natarajan Setheraman, Terrance A. Stadheim, Stephan Wildt
  • Publication number: 20140200213
    Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of the variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: August 21, 2012
    Publication date: July 17, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Wen-Lian Wu, Duane A. Burnett, Andrew W. Stamford, Jared N. Cumming, Theodros Asberom, Chad Bennett, Thavalakulamgara K. Sasiskumar, Jack D. Scott
  • Patent number: 8778980
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: July 15, 2014
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Drug Discovery, Inc.
    Inventors: Zhaoning Zhu, Brian A McKittrick, Zhong-Yue Sun, Yuanzan C Ye, Johannes H Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
  • Patent number: 8778957
    Abstract: Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.
    Type: Grant
    Filed: March 8, 2010
    Date of Patent: July 15, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Amy G. Quigley
  • Patent number: 8772328
    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: October 22, 2013
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber
  • Patent number: 8772276
    Abstract: The present invention is directed to alkyne benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 8771733
    Abstract: Pharmaceutical compositions suitable for oral administration in solid dosage forms are described. The compositions comprise an effective amount of a drug compound in the form of a salt, wherein the drug salt is characterized by conversion to a less soluble form of the drug compound under certain pH conditions, and an anti-nucleating agent.
    Type: Grant
    Filed: December 2, 2005
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Maria T. Cruanes, Wei Xu, Laura M. Artino, Honggang Zhu
  • Patent number: 8772286
    Abstract: The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Tjeerd Andries Barf, Arthur Oubrie, Carsten Schultz-Fademrecht, Eduard Willem Zwart, Niels Hoogenboom, Sander Martijn De Wilde, Allard Kaptein
  • Patent number: 8772505
    Abstract: The present invention relates to novel Tricyclic Compounds, compositions comprising at least one Tricyclic Compound, and methods of using Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient. The present invention provides Tricyclic Compounds of Formula (I): Non-limiting examples of the Compounds of Formula (I) include compound 44 The Compounds of Formula (II) can be useful for inhibiting HCV viral replication or replicon activity, and for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin X. Chen, Anilkumar Gopinadhan Nair, Qingbei Zeng, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Patent number: 8765784
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is 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 metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: June 6, 2011
    Date of Patent: July 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth L. Arrington, Vadim Dudkin, Mark E. Layton, Joseph E. Pero, Alexander J. Reif
  • Patent number: 8765914
    Abstract: Purified genes encoding a cytokine referred to as interleukin-B30 (IL-B30) from a mammal, and reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this molecule are provided. Methods of using the reagents and diagnostic kits are also provided.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: July 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: J. Fernando Bazan
  • Patent number: 8765757
    Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: November 13, 2008
    Date of Patent: July 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro