Patents Assigned to Merck Sharp
  • Spirolactam bicyclic CGRP receptor antagonists
    Patent number: 8071772
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2, J and K 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. 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: November 14, 2006
    Date of Patent: December 6, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump, Cory R. Theberge, C. Blair Zartman
  • MECHANISM OF NEUROMEDIN U ACTION AND USES THEREOF
    Publication number: 20110294735
    Abstract: The use of neuromedin U receptor agonists to elevate the levels of GLP-1 and/or PYY in an individual in need of an increase in its levels of GLP-1 and/or PYY is described. Further described is the use of neuromedin U receptor agonists to lower the levels of glucagon in an individual in need of lowered glucagon levels. Thus, methods for elevating GLP-1 and/or PYY and lowering glucagon levels in an individual by administering to the individual compositions comprising a neuromedin U receptor agonist and optionally one or more dipeptidyl peptidase IV (DPP-IV) inhibitors are described.
    Type: Application
    Filed: October 30, 2009
    Publication date: December 1, 2011
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Donald J. Marsh, Andrea M. Peier, Alessandro Pocai
  • METHODS FOR CHARACTERIZING AGONISTS AND PARTIAL AGONISTS OF TARGET MOLECULES
    Publication number: 20110294696
    Abstract: In one aspect, the present invention provides methods of determining whether an agent is more like a partial agonist of a target molecule than a full agonist of the same target molecule. In another aspect, the present invention provides methods to select a candidate compound that may reduce blood plasma glucose concentration in a mammal. Populations of genes are provided that are useful in the practice of the present invention.
    Type: Application
    Filed: August 12, 2011
    Publication date: December 1, 2011
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Yejun Tan, Hongyue Dai, Pek Yee Lum, John Ryan Thompson, Joel Peter Berger, Eric Stanley Muise, Richard F. Raubertas, Kenny Kin Chung Wong
  • Surface display of whole antibodies in eukaryotes
    Patent number: 8067339
    Abstract: Methods for display of recombinant whole immunoglobulins or immunoglobulin libraries on the surface of eukaryote host cells, including yeast and filamentous fungi, are described. The methods are useful for screening libraries of recombinant immunoglobulins in eukaryote host cells to identify immunoglobulins that are specific for an antigen of interest.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: November 29, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bianka Prinz, Natarajan Sethuraman, Dongxing Zha, Stefan Wildt, Piotr Bobrowicz
  • RNA interference mediated inhibition of cyclin D1 gene expression using short interfering nucleic acid (siNA)
    Patent number: 8067575
    Abstract: This invention relates to compounds, compositions, and methods useful for modulating cyclin (e.g., cyclin D1) and/or cyclin dependent kinase (CDK) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of cyclin (e.g., cyclin D1) and/or cyclin dependent kinase (CDK) gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features 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 and methods used to modulate the expression of cyclin (e.g., cyclin D1) and/or cyclin dependent kinase (CDK) genes.
    Type: Grant
    Filed: August 28, 2008
    Date of Patent: November 29, 2011
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: James McSwiggen, Leonid Beigelman
  • Potassium channel inhibitors
    Patent number: 8067607
    Abstract: The present invention relates to pyridin-3-yl pyridin-3-amine compounds and derivatives thereof having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: November 29, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Jacob M. Hoffman, M. Brad Nolt
  • Mineralocorticoid receptor modulators
    Patent number: 8063090
    Abstract: The present invention relates to diphenylmethyl imidazole mineralocorticoid receptor modulators compounds having the structure and their use in treating cardiovascular events.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: November 22, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Philip E. Brandish, James C. Hershey, Mark E. Fraley, Justin T. Steen
  • Angiotensin II receptor antagonists
    Patent number: 8053455
    Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5;??2) Z is —O— or —(CR14R15)—; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N?N(O)—R3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: November 8, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Brent Whitehead
  • CGRP receptor antagonists
    Patent number: 8039460
    Abstract: Compounds of Formula (I): and Formula (II): (where variables R2, R4, A, B, D, W, X, Y and Z 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 12, 2005
    Date of Patent: October 18, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W. Shaw, Diem N. Nguyen, Zhengwu J. Deng, Theresa M. Williams, Joseph P. Vacca, Craig M. Potteiger, Harold G. Selnick
  • Antidiabetic bicyclic compounds
    Patent number: 8039484
    Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: October 18, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
  • 2,5-Disubstituted Piperidine Orexin Receptor Antagonists
    Publication number: 20110251237
    Abstract: The present invention is directed to 2,5-disubstituted piperidine 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: Application
    Filed: October 15, 2009
    Publication date: October 13, 2011
    Applicant: MERCK SHARP & DOHME CROP.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, John D. Schreier, David B. Whitman
  • BIARYL-SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA 2C ADRENERGIC RECEPTOR MODULATORS
    Publication number: 20110251207
    Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: October 6, 2009
    Publication date: October 13, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Adandan Palani, Michael Y. Berlin, Robert G. Aslanian
  • METHOD OF DESIGNING siRNAS FOR GENE SILENCING
    Publication number: 20110250591
    Abstract: The present invention provides a method for identifying siRNA target motifs in a transcript using a position-specific score matrix approach. The invention also provides a method for identifying off-target genes of an siRNA using a position-specific score matrix approach. The invention further provides a method for designing siRNAs with higher silencing efficacy and specificity. The invention also provides a library of siRNAs comprising siRNAs with high silencing efficacy and specificity.
    Type: Application
    Filed: May 4, 2011
    Publication date: October 13, 2011
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Aimee L. Jackson, Steven R. Bartz, Julja Burchard, Peter S. Linsley, Wei Ge, Guy L. Cavet
  • Inhibitor of vascular endothelial cell growth factor
    Patent number: 8034772
    Abstract: The vascular endothelial cell growth factor (VEGF) inhibitors of the present invention are naturally occurring or recombinantly engineered soluble forms with or without a C-terminal transmembrane region of the receptor for VEGF, a very selective growth factor for endothelial cells. The soluble forms of the receptors will bind the growth factor with high affinity but do not result in signal transduction. These soluble forms of the receptor bind VEGF and inhibit its function.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: October 11, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard L. Kendall, Kenneth A. Thomas, Jr.
  • PACKAGING FOR OXYGEN-SENSITIVE PHARMACEUTICAL PRODUCTS
    Publication number: 20110240511
    Abstract: The present invention relates to packaging and containers for oxygen-sensitive pharmaceutical products, or oxygen- and moisture-sensitive pharmaceutical products. More particularly, the invention relates to pharmaceutical packages comprising a blister pack with airflow channels and outlets, an oxygen scavenger, and, optionally, a desiccant, all of which are sealed inside an outer container having oxygen and moisture barrier properties.
    Type: Application
    Filed: December 2, 2009
    Publication date: October 6, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Matthew P. Bolton, Rey T. Chern, Arthur L. Jaeger, Matthew Moyer, Anthony P. Panarello
  • Potassium channel inhibitors
    Patent number: 8030332
    Abstract: The present invention relates to dipyridin-3-ylmethoxy compounds and derivatives thereof having the structure I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: October 4, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: B. Wesley Trotter, Richard C. A. Isaacs, Zhicai Wu, Jacob M. Hoffman, Mark T. Bilodeau, Ahren Iver Green
  • Polymer formulations of CETP inhibitors
    Patent number: 8030359
    Abstract: A pharmaceutical composition comprises (a) a CETP inhibiting compound, or a pharmaceutically acceptable salt thereof; (b) a concentration-enhancing polymer, and (c) optionally one or more surfactants; wherein the compound has the structure shown as Formula I below. The composition raises HDL-cholesterol and lowers LDL-cholesterol.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: October 4, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sarah Geers, Michael Lowinger, Craig A. McKelvey, Robert F. Meyer, Dina Zhang
  • NOVEL CRYSTALLINE FORMS OF AN INHIBITOR OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1
    Publication number: 20110237634
    Abstract: Novel crystalline salts of 3-[4-(3-ethanesulfonyl-propyl)-bicyclo[2.2.2]oct-1-yl]-4-methyl-5-(2-trifluoromethyl-phenyl)-4H-1,2,4-triazole are potent inhibitors of 11?-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.
    Type: Application
    Filed: December 7, 2009
    Publication date: September 29, 2011
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Joseph E. Lynch, Yuri Y. Bereznitski, Frederick T. Mattrey, John L. Leazer, JR., Russell R. Ferlita, Jinchu Liu, Jungjun Yin, Robert M. Wenslow, JR.
  • Histone deacetylase inhibitors with aryl-pyrazolyl-motifs
    Patent number: 8026260
    Abstract: The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.
    Type: Grant
    Filed: October 30, 2006
    Date of Patent: September 27, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joshua Close, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, David Sloman, Matthew G Stanton, Paul Tempest, David J. Witter
  • Synthetic gene control region
    Patent number: 8026082
    Abstract: The present invention provides a synthetic gene control region which comprises a gene regulatory sequence comprising a binding site for a gene regulatory protein of a yeast strain, and a promoter from filamentous fungal strain located downstream of the gene regulatory sequence; wherein the promoter can be recognized by the general transcription factors and RNA polymerase of the yeast strain; wherein the gene regulatory sequence is capable of regulating transcription initiated by the filamentous fungal promoter in the yeast strain.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: September 27, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Janine Bryan, Michelle K. Brownlow, Loren D. Schultz, Maria C. Losada, Kathrin Ute Jansen, Myra Kurtz, Stuart Kurtz, legal representative