Patents Assigned to Merck Sharp
  • PROCESS FOR THE PREPARATION OF CHIRAL TERT-BUTYL 4-((1R,2S,5R)-6-(BENZYLOXY)-7-OXO-1,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXAMIDO)PIPERIDINE-1-CARBOXYLATE DERIVATIVES AND (2S,5R)-7-OXO-N-PIPERIDIN-4-YL-6-(SULFOXY)-1,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXAMIDE
    Publication number: 20160122350
    Abstract: A process for the preparation of N-protected 6-(piperidin-4-ylcarbamoyl)piperidin-3-yl sulfonates of Formula (III): which comprises contacting a lactone of Formula (II): with an azacycloalkylamine of formula (II-Am): followed by contact with a sulfonyl halide of formula (II-Su): R4—SO2W (II-Su) in the presence of tertiary amine base, wherein PG1 and PG2 are amine protective groups; k, p and q are 0, 1, or 2, and W, R2, R3, R4, R5, R6, R7, R8, and R9 are defined herein. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as ?-lactamase inhibitors.
    Type: Application
    Filed: June 5, 2014
    Publication date: May 5, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Steven P. Miller, John Limanto, Yong-Li Zhong, Nobuyoshi Yasuda, Zhijian Liu
  • CYCLIC PHOSPHONATE SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20160122380
    Abstract: The present invention relates to Cyclic Phosphonate Substituted Nucleoside Derivatives of Formula (I): (structure) and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein, as well as to compositions and methods of using the Cyclic Phosphonate Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: June 16, 2014
    Publication date: May 5, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Stephane Bogen, Vinay Girijavallabhan, Quang Truong, Ping Chen, Frank Bennett, Angela Kerekes, Qun Dang, David B. Olsen, Ian Davies
  • HCV NS3 protease inhibitors
    Patent number: 9328138
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: May 3, 2016
    Assignees: MSD Italia S.R.L., Merck Sharp & Dohme Corp.
    Inventors: Michael T. Rudd, John McCauley, Nigel Liverton, Christiane Grisé-Bard, Marie-Christine Brochu, Sylvie Charron, Virender Aulakh, Benoit Bachand, Patrick Beaulieu, Helmi Zaghdane, Yongxin Han, Marco Ferrara, Steven Harper, Vincenzo Summa, Samuel Chackalamannil, Srikanth Venkatraman, Unmesh Shah, Francisco Velazquez
  • Method for preparing Fc containing polypeptides having improved properties
    Patent number: 9328170
    Abstract: The present invention is directed to methods and compositions for the production of Fc-containing polypeptides comprising mutations at positions 243, 264, 267 and 328 of the Fc region.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: May 3, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Dongxing Zha
  • Methods for preparing oxazolidinones and compositions containing them
    Patent number: 9328087
    Abstract: Methods of preparing a class of oxazolidinones useful to impede bacterial growth are disclosed.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: May 3, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Carrie A. Costello, Jacqueline A. Ware, Robert J. Duguid
  • Cyanomethylpyrazole carboxamides as janus kinase inhibitors
    Patent number: 9328099
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: May 3, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason Brubaker, Matthew Lloyd Childers, Matthew Christopher, Joshua T. Close, Jason David Katz, Joon Jung, Scott Peterson, Phieng Siliphaivanh, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Hongjun Zhang
  • Engineered lower eukaryotic host strains for recombinant protein expression
    Patent number: 9328367
    Abstract: The present invention relates to novel engineered lower eukaryotic host cells for expressing heterologous proteins and to methods of generating such strains.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: May 3, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bo Jiang, Rebecca D. Argyros, Stephanie Nelson, Robert C. Davidson, Ronghua Chen, Jun Zhuang
  • Method for treating a disease associated with soluble, oligomeric species of amyloid beta 1-42
    Patent number: 9320793
    Abstract: This invention is a method and kit for treating a disease associated with, or resulting from, the accumulation of soluble oligomer amyloid beta 1-42 using an antibody, or antibody fragment thereof, that has a higher affinity for amyloid beta 1-42 oligomers than for amyloid beta 1-42 monomer, amyloid beta 1-40 monomer, plaques and amyloid beta fibrils and, optionally, a tau therapeutic or an inhibitor of amyloid beta production or aggregation.
    Type: Grant
    Filed: December 4, 2012
    Date of Patent: April 26, 2016
    Assignees: Acumen Pharmaceuticals, Inc., Merck Sharp & Dohme Corp.
    Inventors: William F. Goure, Franz F. Hefti, Renee C. Gaspar, Paul J. Shughrue, Fubao Wang, Weirong Wang, Ningyan Zhang, Wei-Qin Zhao, Alexander McCampbell, Min Xu
  • Ceftolozane-tazobactam pharmaceutical compositions
    Patent number: 9320740
    Abstract: Pharmaceutical compositions are provided in unit dosage forms comprising ceftolozane and tazobactam in separate unit dosage form containers, ceftolozane prepared in the absence of tazobactam, tazobactam prepared in the absence of ceftolozane, and/or compositions where ceftolozane and tazobactam are first combined within a unit dosage form container.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: April 26, 2016
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Joseph Terracciano, Nicole Miller Damour, Chun Jiang, Giovanni Fogliato, Giuseppe Alessandro Donadelli, Dario Resemini
  • FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INTEGRASE INHIBITORS
    Publication number: 20160108059
    Abstract: The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1-R8, A, X and n are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: April 18, 2014
    Publication date: April 21, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Timothy J. Hartingh, Izzat T. Raheem, John Schreier, John Sisko, John Wai, Thomas H. Graham, Lihong Hu, Xuanjia Peng
  • IMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
    Publication number: 20160108048
    Abstract: The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.
    Type: Application
    Filed: June 2, 2014
    Publication date: April 21, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Craig A. Coburn, Milana Maletic, Yunfu Luo, Zhiqi Qi, Chunsing Li, Tingting Yu, Richard Soll
  • COMBINATION THERAPIES FOR CANCER
    Publication number: 20160106835
    Abstract: A novel combination comprising a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and a PD-1 antagonist; pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf and/or immune modulation through PD-1 is beneficial, e.g., cancer.
    Type: Application
    Filed: May 28, 2014
    Publication date: April 21, 2016
    Applicants: MERCK SHARP & DOHME CORP., GLAXOSMITHKLINE LLC
    Inventors: Axel Hoos, Keith W. Orford, Patrick Chun, Venkataraman Sriram, Elaine M. Pinheiro, Scot W. Ebbinghaus
  • Treating diabetes with dipeptidyl peptidase-IV inhibitors
    Patent number: 9315508
    Abstract: The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N 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: July 18, 2013
    Date of Patent: April 19, 2016
    Assignee: Merck sharp & Dohme Corp.
    Inventor: Tesfaye Biftu
  • Imidazopyridin-2-one derivatives
    Patent number: 9315518
    Abstract: The present invention is directed to imidazopyridin-2-one 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: June 14, 2012
    Date of Patent: April 19, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hannah D. Fiji, Michael J. Kelly, III, Jeffrey C. Kern, Mark E. Layton, Joseph E. Pero, Alexander J. Reif, Michael A. Rossi
  • HIV protease inhibitors
    Patent number: 9315475
    Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: April 19, 2016
    Assignees: MERCK SHARP & DOHME CORP., MERCK CANADA INC.
    Inventors: Christian Beaulieu, David J. Bennett, Christopher J. Bungard, Ronald K. Chang, Sheldon Crane, Thomas J. Greshock, Li Hao, Kate Holloway, Jesse J. Manikowski, John A. McCauley, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Philippe G. Nantermet, Christian Nadeau, Satyanarayana Tummanapalli, William Shipe, Sanjay Kumar Singh, Vouy Linh Truong, Sivalenka Vijayasaradhi, Peter D. Williams, Catherine M. Wiscount
  • Crystalline polymorphic forms of an antidiabetic compound
    Patent number: 9315457
    Abstract: The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: April 19, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: John Y. L. Chung
  • 2-HYDROXYMETHYL-SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20160102073
    Abstract: The present invention is directed to 2-hydroxymethyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: April 21, 2014
    Publication date: April 14, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: SCOTT D. KUDUK, JASON W. SKUDLAREK
  • Antibodies, kit and method for detecting amyloid beta oligomers
    Patent number: 9310383
    Abstract: This invention is a selective A? oligomer kit and immunoassay method capable of reliably and sensitively detecting A? oligomers in a biological sample of a patient. In one embodiment the inventive assay uses a pair of anti-A? oligomer antibodies, as capture and detection antibodies, to detect and quantify A? oligomers. The method can be used to differentiate Alzheimer's disease (AD) patients from non-AD patients and/or to stratify AD patients according to the severity of their disease.
    Type: Grant
    Filed: June 3, 2015
    Date of Patent: April 12, 2016
    Assignees: Acumen Pharmaceuticals, Inc., Merck Sharp & Dohme Corp.
    Inventors: William F. Goure, Renee C. Gaspar, Alexander McCampbell, Mary J. Savage, Paul J. Shughrue, Fubao Wang, Weirong Wang, Abigail L. Wolfe, Ningyan Zhang, Wei-Qin Zhao, Min Xu
  • Anti-ADDL monoclonal antibody and uses thereof
    Patent number: 9309309
    Abstract: The present invention relates to antibodies that bind amyloid ?-derived diffusible ligands, also known as ADDLs. The antibodies of the invention are selective for ADDLs, can penetrate the brain, 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 ADDLs.
    Type: Grant
    Filed: July 9, 2014
    Date of Patent: April 12, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Renee C. Gaspar, Paul J. Shughrue, Fubao Wang, Weirong Wang, Ningyan Zhang, Wei-Qin Zhao, Min Xu, Alexander McCampbell
  • Inhibitors of catechol O-methyl transferase and their use in the treatment of psychotic disorders
    Patent number: 9309199
    Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: April 12, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, James C. Barrow, Scott T. Harrison, B. Wesley Trotter, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao