Patents Assigned to Merck Sharp
  • Quinolinone-pyrazolone M1 receptor positive allosteric modulators
    Patent number: 8895580
    Abstract: The present invention is directed to quinolinone-pyrazolone 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: October 1, 2010
    Date of Patent: November 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. DiPardo
  • Cyclic benzimidazole derivatives useful as anti-diabetic agents
    Patent number: 8895596
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: February 21, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Jinlong Jiang, Andrew J. Kassick, Ahmet Kekec, Iyassu K. Sebhat
  • Anti-ADDL antibodies and uses thereof
    Patent number: 8889138
    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: October 11, 2010
    Date of Patent: November 18, 2014
    Assignees: Merck Sharp & Dohme Corp., Northwestern University
    Inventors: Paul Acton, Zhiqiang An, Andrew J. Bett, Robert Breese, Elizabeth Chen Dodson, Gene Kinney, William L Klein, Mary P. Lambert, Xiaoping Liang, Paul Shughrue, William R. Strohl, Kirsten Viola, Lei Chang
  • Substituted quinoxalines as inhibitors of fatty acid binding protein
    Patent number: 8889683
    Abstract: The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: November 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Clifford Cheng, Gerald W. Shipps, Jr., Xiaohua Huang, Ying Huang, Ning Shao, Ashwin Rao, Anandan Palani, Peter Orth, Johannes H. Voigt, Robert J. Herr, Lana Michele Rossiter, Qi Zeng, Xianfeng Sun
  • Applicator for inserting an implant
    Patent number: 8888745
    Abstract: The invention pertains to an applicator (1) for inserting an implant, in particular a rod-like implant (2) containing an active substance, under the skin of a human or animal, comprising a housing (3), a cannula (6) extending from the housing (3), and a handle (15) for grasping and maneuvering the applicator (1) and the cannula (6) during insertion of an implant (2). In accordance with the invention, the handle (15) extends above at least part of the length of the cannula (6). Such a handle facilitates insertion of the cannula and/or accurate positioning of the implant.
    Type: Grant
    Filed: January 20, 2006
    Date of Patent: November 18, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Iris Epkjen Hobo Van Der Graaf, Maurice Petrus Wilhelmus Tak, Juergen Schmidt, Hendricus Johannes Vertegaal
  • PHOSPHORIC ACID SALTS OF SITAGLIPTIN
    Publication number: 20140336196
    Abstract: The present invention relates to novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, and polymorphs, hydrates and solvates thereof, which are potent inhibitors of dipeptidyl peptidase-IV useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The present invention also relates to the process for preparing the novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, as well as pharmaceutical compositions containing the novel phosphoric acid salts, and methods of use thereof for the treatment of diabetes, obesity, and high blood pressure.
    Type: Application
    Filed: May 22, 2012
    Publication date: November 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Jerry L. Atwood
  • Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
    Patent number: 8883801
    Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: November 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lianyun Zhao, Duan Liu, Shuyi Tang, Amit K. Mandal, Umar Faruk Mansoor, Lalanthi Dilrukshi Vitharana, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
  • Aryl methyl benzoquinazolinone M1 receptor positive allosteric modulators
    Patent number: 8883810
    Abstract: The present invention is directed to benzoquinazolinone 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: August 29, 2013
    Date of Patent: November 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng Di Marco, Thomas J. Greshock
  • Naphthalene carboxamide M1 receptor positive allosteric modulators
    Patent number: 8883850
    Abstract: The present invention is directed to naphthalene carboxamide 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 Alzheimers 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: May 23, 2011
    Date of Patent: November 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Christina Ng DiMarco, Scott D. Kukuk
  • Piperidinone carboxamide indane CGRP receptor antagonists
    Patent number: 8883807
    Abstract: The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and 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 10, 2011
    Date of Patent: November 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, Blair C. Zartman, Heather E. Stevenson
  • METHODS FOR INCREASING N-GLYCAN OCCUPANCY AND REDUCING PRODUCTION OF HYBRID N-GLYCANS IN PICHIA PASTORIS STRAINS LACKING ALG3 EXPRESSION
    Publication number: 20140329276
    Abstract: Methods for increasing the yield and N-glycosylation site occupancy of paucimannose or complex N-glycans of recombinant glycoproteins produced in a recombinant host cell lacking dolichyl-P-Man:Man5GlcNAc2-PP-dolichyl alpha-1,3 mannosyltransferase (Alg3p) activity are disclosed. In particular, recombinant host cells are provided that comprise a disruption of the expression of an OS-9 family gene in the host cell. These recombinant host cells may then be used for producing recombinant glycoproteins. In further embodiments, the recombinant host cells further overexpress at least one heterologous single-subunit oligosaccharyltransferase, which in particular embodiments is capable of functionally suppressing the lethal phenotype of a mutation of at least one essential protein of the yeast oligosaccharyltransferase (OTase) complex.
    Type: Application
    Filed: October 23, 2012
    Publication date: November 6, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Byung-Kwon Choi, Stephen R. Hamilton, Natarajan Sethuraman
  • AX132 PCSK9 antagonists
    Patent number: 8877900
    Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: November 4, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Peter Peizhi Luo, Kevin Caili Wangr, Pingyu Zhong, Mark Hsieh, Yan Li, Xinwei Wang, Feng Dong, Andrei Golosov, Yan Ni, Weirong Wang, Laurence B. Peterson, Rose Cubbon, Sujata Sharma, Jon Condra, Jun Lu, Gopalakrishnan Parthasarathy, Stephen Soisson, Noel Byrne
  • HETEROCYCLIC COMPOUNDS AS B-RAF INHIBITORS FOR TREATMENT OF CANCER
    Publication number: 20140323519
    Abstract: This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I).
    Type: Application
    Filed: April 20, 2012
    Publication date: October 30, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: M. Arshad Siddiqui, Lianyun Zhao, Amit K. Mandal
  • Inhibitors of hepatitis C virus replication
    Patent number: 8871759
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Steven W. Ludmerer, Kun Liu, Hao Wu, Richard Soll, Bin Zhong, Jian Zhu
  • Diaryl ether derivatives as notch sparing gamma secretase inhibitors
    Patent number: 8871796
    Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: October 5, 2010
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William Colby Brown, Jason Brubaker, Christian Fischer, Richard W. Heidebrecht, John T. Hendrix, Elizabeth H. Kelley, Rachel N. MacCoss, Joey L. Methot, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Thomas Reger, Peter D. Williams, Catherine M. Wiscount
  • Fused-imidazoyl compounds useful as antimicrobial agents
    Patent number: 8871929
    Abstract: The invention relates to fused-imidazoyl compounds of Formula (I): wherein ring A, R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined herein. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and methods of using the compound of Formula (I) to treat microbial infections.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tin-Yau Chan, Henry M. Vaccaro
  • Fused bicyclic oxazolidinone CETP inhibitor
    Patent number: 8871738
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer'S disease
    Patent number: 8865701
    Abstract: The present invention is directed to spiropyrrolidine 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: February 20, 2010
    Date of Patent: October 21, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kun Liu, Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Richard Soll, Hao Wu, Xuanjin Peng, Yaxian Cai, Xiaoxiang Du, Jian Li
  • Method of treating solid cancers with pegylated IL-10
    Patent number: 8865652
    Abstract: Provided are methods of treatment for tumors. In particular, methods are provided for use of a chemically modified IL-10 to treat tumors.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: October 21, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Martin Oft, Catherine Sheppard, John Mumm, Lingling Wu
  • Cholesteryl ester transfer protein inhibitors
    Patent number: 8865707
    Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: October 21, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Peter J. Sinclair, Gayle E. Taylor