Patents Assigned to Merck Sharp & Dohme
  • Non steroidal glucocorticoid receptor modulators
    Patent number: 8133885
    Abstract: The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocorticoid receptor activity.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: March 13, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ralf Plate, Guido Jenny Rudolf Zaman, Pedro Harold Han Hermkens, Christiaan Gerardus Johannes Maria Jans, Rogier Christian Buijsman, Adrianus Petrus Antonius De Man, Paolo Giovanni Martino Conti, Scott James Lusher, Willem Hendrik Abraham Dokter
  • Anti-ADDL antibodies and uses thereof
    Patent number: 8128930
    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: July 1, 2010
    Date of Patent: March 6, 2012
    Assignees: Northwestern University, Merck Sharp & Dohme Corp.
    Inventors: Paul Acton, Zhiqiang An, Andrew J. Bett, Robert Breese, Lei Chang, Elizabeth Chen Dodson, Gene Kinney, William L. Klein, Mary P. Lambert, Xiaoping Liang, Paul Shughrue, William R. Strohl, Kristen Viola
  • Crystalline forms of MC4R agonist and process for synthesis
    Patent number: 8129413
    Abstract: The present invention relates to a process for producing N-{(1S)-1-[2-(1-{[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}piperidin-4-yl)-5-chlorophenyl]ethyl}acetamide, and novel crystalline salts, hydrates, solvates, and polymorphic forms thereof.
    Type: Grant
    Filed: June 23, 2006
    Date of Patent: March 6, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ralph Calabria, Yu Cheng, Russell R. Ferlita, Ashkan Kamali, Jerry A. Murry, David Mathre, Andrey V. Peresypkin, Karen Thompson, Jian Wang, Robert M. Wenslow
  • PYRROLIDINE-DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS
    Publication number: 20120053181
    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: April 28, 2010
    Publication date: March 1, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Peter Lin, Lehua Chang, Scott D. Edmondson
  • Polypeptides for inducing a protective immune response against
    Patent number: 8124108
    Abstract: The present invention features polypeptides comprising an amino acid sequence structurally related to SEQ ID NO: 1 and uses of such polypeptides. SEQ ID NO: 1 is a truncated derivative of a full-length S. epidermidis polypeptide. The full-length naturally occurring polypeptide is referred to herein as full-length ORF1319e. A His-tagged derivative of SEQ ID NO: 1 was found to produce a protective immune response against S. epidermidis.
    Type: Grant
    Filed: January 18, 2008
    Date of Patent: February 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Annaliesa S. Anderson, Tessie McNeely, James C. Cook, III, William L. McClements, Donna L. Montgomery
  • Hydroxymethyl ether hydroisoindoline tachykinin receptor antagonists
    Patent number: 8124633
    Abstract: The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.
    Type: Grant
    Filed: April 7, 2008
    Date of Patent: February 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert J. DeVita, Sander G. Mills, Jinlong Jiang, Andrew J. Kassick, Jianming Bao
  • Diaryl substituted alkanes
    Patent number: 8124628
    Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Grant
    Filed: April 6, 2007
    Date of Patent: February 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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