Patents Assigned to Merck Sharp
  • Cicletanine derivatives
    Patent number: 8119806
    Abstract: A compound having the structure wherein X is selected from the group consisting of: a bond, —NHCH2(CH2)nCH2OC(O)—, —CH2NHC(O)CH2NHC(O)—, —CH2OC(O)—, —OCH(CH3)OC(O)—, —OCH2OC(O)—, —O—, —NR1—, —CR1R3—, —(CH2)p—, —(CH2)qNR1C(O)—, —CHR5NR2C(O)—, —(CH2)qC(O)—, —(CH2)qC(O)NR1—, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: February 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Iyassu K. Sebhat, Christopher L. Franklin, Kathleen M. Rupprecht, Robert K. Baker, Ravi P. Nargund, Lin Yan, Pei Huo, Dong-Ming Shen, Nicoletta Almirante, Stefano Biondi, Massimiliano Ferrario, Alessia Nicotra
  • Disubstituted aniline compounds
    Patent number: 8119685
    Abstract: The present invention relates to a novel class of disubstituted aniline compounds. These compounds can inhibit histone deacetylase and 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 compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: February 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Heidebrecht, Joey Methot, Dawn Mampreian, Thomas Miller, Phieng Siliphaivanh
  • 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta [ƒ]indazole-5-YL]ethyl phenyl derivatives as glucocorticoid receptor ligands
    Patent number: 8119681
    Abstract: The present invention is directed to 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: October 23, 2007
    Date of Patent: February 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
  • Aryl-fused spirocyclic compounds
    Patent number: 8119652
    Abstract: The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can inhibit histone deacetylase and 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 compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: May 14, 2007
    Date of Patent: February 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher Hamblett, Solomon Kattar, Dawn Mampreian, Joey Methot, Thomas Miller, Paul Tempest
  • Heterocyclic Fused Cinnoline M1 Receptor Positive Allosteric Modulators
    Publication number: 20120040978
    Abstract: The present invention is directed to heterocyclic fused cinnoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in 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: Application
    Filed: April 13, 2010
    Publication date: February 16, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore
  • Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8114887
    Abstract: The present invention is directed to spiropiperidine compounds of formula (I) 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: October 12, 2005
    Date of Patent: February 14, 2012
    Assignees: Merck, Sharp & Dohme Corp., Sunesis Pharmaceuticals, Inc.
    Inventors: James C. Barrow, Craig A. Coburn, Melissa S. Egbertson, Georgia B. McGaughey, Melody A. McWherter, Lou Anne Neilson, Kenneth E. Rittle, Harold G. Selnick, Shaun R. Stauffer, Zhi-Qiang Yang, Wenjin Yang, Wanli Lu, Bruce Fahr
  • MICRORNA AS A BIOMARKER OF PANCREATIC ISLET BETA-CELL ENGAGEMENT
    Publication number: 20120034608
    Abstract: MicroRNAs (miRNAs) are short non-coding RNAs that regulate gene expression and which play important roles in many cell types, including as described herein, the pancreatic ?-cell. Glucagon like peptide-1 (GLP-1), a hormone released from intestinal L-cells following meal intake, exerts pleiotropic effects on ?-cell function including raising intracellular cAMP levels and now represents an important therapy for type 2 diabetes. Expression of miR-132 and miR212 is upregulated by CREB protein in response increased cAMP levels in the cell; therefore, methods for detecting and evaluating ?-cell engagement by GLP-1 receptor agonists by monitoring miR-132 and miR-212 expression in a subject is described. The methods herein are particularly useful in the context of longitudinal clinical trials, such as those designed for testing the durability of any single or combination therapy in type 2 diabetes populations.
    Type: Application
    Filed: April 5, 2010
    Publication date: February 9, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Yun-Ping Zhou, Andrew D. Howard, Jin Shang
  • RENIN INHIBITORS
    Publication number: 20120035214
    Abstract: The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: April 1, 2010
    Publication date: February 9, 2012
    Applicants: Merck Canada Inc., Merck Sharp & Dohme Corp.
    Inventors: Daniel J. McKay, Melissa Arbour, Renee Aspiotis, Austin Chen, Pierre-Andre Fournier, Michel Gallant, Yongxin Han, Helene Juteau, Patrick Lacombe, Sebastien Laliberte, Sophie Lauzon, Carmela Molinaro, Paul O'Shea, Yeeman Ramtohul, Daniel Simard, Dwight MacDonald, Bruce Mackay, Christophe Mellon, Krista Morley, Chit Tsui, Sarah Jennifer Dolman, Greg Hughes, Jacob Janey
  • RNA Interference Mediated Inhibition of Signal Transducer and Activator of Transcription 6 (STAT6) Gene Expression Using Short Interfering Nucleic Acid (siNA)
    Publication number: 20120035247
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of STAT6 gene expression and/or activity, and/or modulate a STAT6 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsR-NA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against STAT6 gene expression.
    Type: Application
    Filed: March 17, 2010
    Publication date: February 9, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Victoria Pickering, Jyoti K. Shah, Walter Strapps
  • FUNCTIONALLY SELECTIVE AZANITRILE ALPHA-2C ADRENORECEPTOR AGONISTS
    Publication number: 20120028940
    Abstract: In its many embodiments, the present invention provides a novel class of azanitrile compounds as inhibitors 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: September 15, 2009
    Publication date: February 2, 2012
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Christopher W. Boyce, Jianhua Chao, Kevin D. McCormick
  • RNA Interference Mediated Inhibition of GATA Binding Protein 3 (GATA3) Gene Expression Using Short Intefering Nucleic Acid (siNA)
    Publication number: 20120029054
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of GATA3 gene expression and/or activity, and/or modulate a GATA3 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsR-NA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against GATA3 gene expression.
    Type: Application
    Filed: March 17, 2010
    Publication date: February 2, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Victoria Pickering, Jyoti K. Shah, Walter Strapps
  • Anti-ADDL monoclonal antibody and use thereof
    Patent number: 8105593
    Abstract: The present invention relates to antibodies that differentially recognize multi-dimensional conformations of A?-derived diffusible ligands, also known as ADDLs. The antibodies of the invention can distinguish between Alzheimer's Disease and control human brain extracts and are useful in methods of detecting ADDLs and diagnosing Alzheimer's Disease. The present antibodies also block binding of ADDLs to neurons, assembly of ADDLs, and tau phosphorylation and are there useful in methods for the preventing and treating diseases associated with soluble oligomers of amyloid ? 1-42.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: January 31, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gene Kinney, William R. Strohl, Zhiqiang An
  • Substituted imidazoles as bombesin receptor subtype-3 modulators
    Patent number: 8106070
    Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: January 31, 2012
    Assignees: Merck Sharp & Dohme Corp., Albany Molecular Research, Inc.
    Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Jian Liu, Michael M. -C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
  • Angiotensin II receptor antagonists
    Patent number: 8106034
    Abstract: A compound having the structure wherein R is an angiotensin receptor blocking group Y is —(CR1R20)1-7R5, or —C(O)(CR1R20)1-7R5; R1 and R20 are independently selected from the group consisting of hydrogen or C1-4 alkyl; R5 is —O—N?N(O)—NR3R4; and R3 and R4 are independently selected from the group consisting of —CH2CH2OH, —CH2CH2OCH3, —C1-4 alkyl, unsubstituted or substituted C1-6 alkenyl, unsubstituted or substituted morpholino, amino, unsubstituted or substituted benzyl, unsubstituted or substituted phenyl, unsubstituted or substituted arylC1-4 alkyl, or R3 and R4 together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, which is useful for treating hypertension.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: January 31, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo
  • Methods for diagnosis and/or prognosis of colon cancer
    Patent number: 8105777
    Abstract: The present invention relates to genetic markers whose expression is correlated with colon cancer. In one aspect, the invention provides sets of markers whose expression can be used for classifying colon cancer patients into different prognostic categories. In another aspect, the invention provides kits containing marker sets for determining prognosis of colon cancer. In another aspect, the invention provides methods of classifying cancer patients with regard to prognosis.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: January 31, 2012
    Assignees: Nederlands Kanker Instituut, Merck Sharp & Dohme Corp.
    Inventors: Hongyue Dai, Laura J. Van't Veer, Yudong He
  • RNA Interference Mediated Inhibition of Signal Transducer and Activator of Transcription 1 (STAT1) Gene Expression Using Short Interfering Nucleic Acid (siNA)
    Publication number: 20120022142
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of STAT1 gene expression and/or activity, and/or modulate a STAT1 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including 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 that are capable of mediating or that mediate RNA interference (RNAi) against STAT1 gene expression.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 26, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vasant Jadhav, Victoria Pickering, Walter Strapps
  • SURFACE DISPLAY OF WHOLE ANTIBODIES IN EUKARYOTES
    Publication number: 20120021948
    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: Application
    Filed: October 3, 2011
    Publication date: January 26, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Bianka Prinz, Natarajan Sethuraman, Dongxing Zha, Stefan Wildt, Piotr Bobrowicz
  • P2X3, RECEPTOR ANTAGONISTS FOR TREATMENT OF PAIN
    Publication number: 20120021074
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Application
    Filed: March 15, 2010
    Publication date: January 26, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Craig M. Potteiger
  • RNA Interference Mediated Inhibition of the Thymic Stromal Lymphopoietin (TSLP) Gene Expression Using Short Interfering Nucliec Acid (siNA)
    Publication number: 20120022143
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of TSLP gene expression and/or activity, and/or modulate a TSLP gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including 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 that are capable of mediating or that mediate RNA interference (RNAi) against TSLP gene expression.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 26, 2012
    Applicant: Merck Sharp & Dohme Corp
    Inventors: Vasant Jadhav, Victoria Pickering, Walter Strapps
  • Tyrosine kinase inhibitors
    Patent number: 8101603
    Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, 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: July 9, 2007
    Date of Patent: January 24, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Dinsmore, Matthew H. Katcher, Alan B. Northrup