Patents Assigned to Merck Sharp and Dohme
  • Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
    Patent number: 8481712
    Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: July 9, 2013
    Assignees: Merck Sharp & Dohme Corp., ISIS Pharmaceuticals, Inc.
    Inventors: Balkrishen Bhat, Anne B. Eldrup, Thazha P. Prakash, Phillip Dan Cook, Robert L. LaFemina, Amy L. Simcoe, Carrie A. Rutkowski, Mario A. Valenciano
  • Combination cancer therapy with an AKT inhibitor and other anticancer agents
    Patent number: 8481503
    Abstract: The invention relates to combination anticancer therapy with certain Akt inhibitor and other anticancer agents such as anticancer antimetabolites, anticancer antibiotics, plant-derived anticancer agents, anticancer platinum-coordinated complex compounds, anticancer camptothecin derivatives and anticancer tyrosine kinase inhibitors.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: July 9, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Mark E. Layton, Hiroshi Hirai, Hidehito Kotani
  • Thiazole Derivatives as protein kinase inhibitors
    Patent number: 8476278
    Abstract: The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: July 2, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Panduranga Adulla P. Reddy, Tzu T. Wong, Lianyun Zhao, Shuyi Tang, Marc A. Labroli, Timothy J. Guzi, M. Arshad Siddiqui
  • Biaryl spiroaminooxazoline analogues as Alpha2C adrenergic receptor modulators
    Patent number: 8476274
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl 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: Grant
    Filed: October 18, 2012
    Date of Patent: July 2, 2013
    Assignee: 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, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
  • Engineered anti-TSLPR antibodies
    Patent number: 8475793
    Abstract: The invention relates to binding compounds that specifically bind to human TSLPR, as well as uses thereof, e.g., in the treatment of inflammatory disorders.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: July 2, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rene De Waal Malefyt, Leonard G. Presta
  • AZO-substituted pyridine and pyrimidine derivatives and their use in treating viral infections
    Patent number: 8470834
    Abstract: The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19, and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: June 25, 2013
    Assignees: Merck Sharp & Dohme Corp., Southern Research Institute
    Inventors: Cecil D. Kwong, F. George Njoroge, Subramaniam Ananthan, Feng Geng, Hollis S. Kezar, III, Joseph A. Maddry, John J. Piwinski, Robert C. Reynolds, John A. Secrist, III, Neng-Yang Shih
  • Benzimidazole and aza-benzimidazole carboxamides
    Patent number: 8470819
    Abstract: This invention provides compounds of Formula I which are PAFR antagonists: I and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.
    Type: Grant
    Filed: October 26, 2009
    Date of Patent: June 25, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lin Chu, Anthony Ogawa, Hyun O. Ok, Feroze Ujjainwalla
  • Tetrahydrofuropyridones
    Patent number: 8471024
    Abstract: The present invention relates to Tetrahydrofuropyridones compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: June 25, 2013
    Assignee: Merck Sharp & Dohme, Corp.
    Inventors: Vincent J. Colandrea, Jeffrey J. Hale, Joshua G. McCoy
  • Thiophenes as glucagon receptor antagonists, compositions, and methods for their use
    Patent number: 8470773
    Abstract: The present invention relates to compounds of the general formula: wherein R1, R2, R3, R5, s, and Z are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: June 25, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric J. Gilbert, Michael W. Miller, Andrew W. Stamford, William J. Greenlee
  • Plasmid system for multigene expression
    Patent number: 8470593
    Abstract: The present invention provides a plasmid system which facilitates the construction of a single amplifiable plasmid that, having the potential to accommodate many independent expression cassettes, has the ability to express multi-subunit complex proteins such as antibodies and receptors.
    Type: Grant
    Filed: October 18, 2011
    Date of Patent: June 25, 2013
    Assignee: Merck Sharp Dohme & Corp.
    Inventor: Deba P. Saha
  • Derivatives and analogs of chroman as functionally selective ALPHA2C adrenoreceptor agonists
    Patent number: 8470863
    Abstract: In its many embodiments, the present invention provides a novel class of chroman compounds of formula I as ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of prepaxing 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. wherein J is: Z is —[C(Rc)(Rc)]x—, where x is 1, 2, or 3.
    Type: Grant
    Filed: February 11, 2008
    Date of Patent: June 25, 2013
    Assignee: Merck Sharp & Dohme, Corp.
    Inventors: Junying Zheng, Kevin D. McCormick, Jianhua Chao, Christopher W. Boyce, Robert G. Aslanian, Younong Yu
  • FDG-pet evaluation of Ewing's sarcoma sensitivity
    Patent number: 8470297
    Abstract: This invention relates to methods for evaluating the efficacy of an IGF1R inhibitor, such as an anti-IGF1R antibody, for the treatment of an Ewing's sarcoma tumor by determining the level of tumoral glucose metabolism. Tumoral glucose metabolism is determining at an early point in the treatment regimen by any of several methods known in the art including FDG-PET/CT scan.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: June 25, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brian DerHua Lu, Siu-Long Yao, Cynthia Seidel-Dugan, Yan Wang
  • Mammalian Receptor Proteins; Related Reagents and Methods
    Publication number: 20130156729
    Abstract: Nucleic acids encoding mammalian, e.g., primate, receptors, purified receptor proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.
    Type: Application
    Filed: February 7, 2013
    Publication date: June 20, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • FDF03 ANTIBODIES AND USES THEREOF
    Publication number: 20130156771
    Abstract: The present invention relates to methods for identifying and using modulators of FDF03 biological activity in vitro and in vivo that are useful in the treatment of cancer.
    Type: Application
    Filed: February 14, 2013
    Publication date: June 20, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael E. Bigler, Drake M. LaFace, Kalyan Pande, Joseph H. Phillips
  • AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
    Publication number: 20130157940
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV 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: Application
    Filed: February 7, 2013
    Publication date: June 20, 2013
    Applicant: Merck Sharp & Dohme Corp
    Inventor: Merck Sharp & Dohme Corp
  • 6-substituted sulfonyl azabicyclo[3.2.1]octanes useful to inhibit 11?-hydroxysteroid dehydrogenase type-I
    Patent number: 8466149
    Abstract: In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: June 18, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
  • 2,5-disubstituted morpholine orexin receptor antagonists
    Patent number: 8466281
    Abstract: The present invention is directed to 2,5-disubstituted morpholine 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: Grant
    Filed: October 15, 2009
    Date of Patent: June 18, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Christopher D. Cox, Broc Flores, John D. Schreier
  • NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
    Publication number: 20130150362
    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: Application
    Filed: August 22, 2011
    Publication date: June 13, 2013
    Applicant: 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
  • HCV NS3 protease inhibitors
    Patent number: 8461107
    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: April 16, 2009
    Date of Patent: June 11, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel J. Liverton, John A. McCauley, John W. Butcher, Kevin F. Gilbert, Charles J. McIntyre, Michael T. Rudd
  • Pyrazolo[1,5-a]pyrimidine derivatives
    Patent number: 8461162
    Abstract: Compounds of the following formula (I) are inhibitors of microtubule affinity regulating kinase, and hence find use in the treatment of neurodegenerative diseases associated with hyperphosphorylation of tau.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: June 11, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew G. Stanton, Njamkou Noucti, David L. Sloman, Jongwon Lim, Benito Munoz