Patents Assigned to Merck Sharp
  • INHIBITORS OF HEPATITIS C VIRUS REPLICATION
    Publication number: 20150246917
    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: Application
    Filed: May 13, 2015
    Publication date: September 3, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Craig A. Coburn, Steven W. Ludmerer, Kun Liu, Hao Wu, Richard Soll, Bin Zhong, Jian Zhu
  • SUBSTITUED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20150246902
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 16, 2012
    Publication date: September 3, 2015
    Applicants: Merck Sharp & Dohme Corp., MSD Italia S.R.L.
    Inventors: Casey C. McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Qun Dang
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9120781
    Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: May 10, 2011
    Date of Patent: September 1, 2015
    Assignees: Simon Fraser University, Merck Sharp & Dohme Corp., Alectos Therapeutics Inc.
    Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Kun Liu, Harold G. Selnick
  • Pyridyl aminopyridines as Syk inhibitors
    Patent number: 9120785
    Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: September 1, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Maria Emilia Di Francesco, Andrew M. Haidle, Ryan D. Otte, John Michael Ellis, Kaleen Konrad Childers, Alan B. Northrup, Liping Wang
  • Process and intermediates for preparing macrolactams
    Patent number: 9120818
    Abstract: The present invention relates to macrolactam compounds, intermediates useful in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing and modifying macrolactams. One use of the compounds and methods described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. An example of an HCV inhibitory compound that can be synthesized using the procedures described herein is Compound A and derivative thereof.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: September 1, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Cheng Chen, Jongrock Kong, Guy Humphrey, Sarah Dolman, Hongmei Li, Matthew T. Tudge, Kelvin Yong, Bangping Xiang, Michael Zacuto
  • TRIAZOLYL DERIVATIVES AS SYK INHIBITORS
    Publication number: 20150239866
    Abstract: Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
    Type: Application
    Filed: September 24, 2013
    Publication date: August 27, 2015
    Applicants: MERCK CANADA INC., MERCK SHARP & DOHME CORP.
    Inventors: Michelle R. MACHACEK, Eric T. ROMEO, Solomon D. KATTAR, Matthew CHRISTOPHER, Michael D. ALTMAN, Alan B. NORTHRUP, John Michael ELLIS, Brendan O BOYLE, Anthony DONOFRIO, Jonathan GRIMM, Michael H. REUTERSHAN, Kaleen Konrad CHILDERS, Ryan D. OTTE, Brandon CASH, Yves DUCHARME, Andrew M. HAIDLE, Kerrie SPENCER, Dilrukshi VITHARANA, Lingyun WU, Li ZHANG, Peng ZHANG, Christian BEAULIEU, Daniel GUAY
  • 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derivatives
    Patent number: 9115126
    Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: August 25, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
  • SYN3 compositions and methods
    Patent number: 9115374
    Abstract: Disclosed are aqueous and lyophilized formulations containing SYN3 and methods of their use for treating bladder cancer.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: August 25, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Peter M. Ihnat, Leonore C. Witchey-Lakshmanan, Varda Sandweiss, Sydney O. Ugwu
  • SUBSTITUTED PHENYL-SPLEEN TYROSINE KINASE (SYK) INHIBITORS
    Publication number: 20150232428
    Abstract: The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Application
    Filed: August 15, 2013
    Publication date: August 20, 2015
    Applicants: Merck Canada Inc., Merck Sharp & Dohme Corp.
    Inventors: Andrew M. Haidle, Jason Burch, Daniel Guay, Jacques Yves Gauthier, Joel Robichaud, Jean Francois Fournier, John Michael Ellis, Matthew Christopher, Solomon D. Kattar, Graham F. Smith, Alan B. Northrup
  • ANTIBODIES TO HUMAN PROGRAMMED DEATH RECEPTOR PD-1
    Publication number: 20150232555
    Abstract: Antibodies which block binding of hPD-1 to hPD-L1 or hPD-L2 and their variable region sequences are disclosed. A method of increasing the activity (or reducing downmodulation) of an immune cell through the PD-1 pathway is also disclosed.
    Type: Application
    Filed: December 19, 2014
    Publication date: August 20, 2015
    Applicant: MERCK SHARP & DOHME B.V.
    Inventors: Gregory John Carven, Hans Van Eenenneem, Gradus Johannes Dulos
  • CRYSTALLINE FORM OF A REVERSE TRANSCRIPTASE INHIBITOR
    Publication number: 20150232447
    Abstract: The retrovirus designated human immunodeficiency virus (HIV), particularly the strains known as HIV type-1 (HIV-1) and type-2 (HIV-2), have been etiologically linked to the immunosuppressive disease known as acquired immunodeficiency syndrome (AIDS). HIV seropositive individuals are initially asymptomatic but typically develop AIDS related complex (ARC) followed by AIDS. Affected individuals exhibit severe immunosuppression which makes them highly susceptible to debilitating and ultimately fatal opportunistic infections. The invention is directed to a novel crystalline form of the RT inhibitor 3-chloro-5-({1-[(4-methyl-5 -oxo-4,5-dihydro-1 H-1,2, 4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethy 1)-1,2-dihydropyridin-3-yl) oxy)benzonitrile used in the treatment HIV infection and AIDS.
    Type: Application
    Filed: September 20, 2013
    Publication date: August 20, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: Courtney K. Maguire
  • Inhibitors of the Renal Outer Medullary Potassium channel
    Patent number: 9108947
    Abstract: This invention relates to compounds of Formula I having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: August 18, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato
  • Diazeniumdiolate heterocyclic derivatives
    Patent number: 9108920
    Abstract: A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: August 18, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Robert K. Baker, Zhiqiang Guo, Brent Whitehead, Timothy J. Henderson, Edward Metzger, Lin Yan, Shrenik K. Shah, James Dellureficio, Jun Wang
  • Process for the preparation of an orexin receptor antagonist
    Patent number: 9108959
    Abstract: The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: August 18, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Carl A. Baxter, Edward Cleator, Faye Sheen, Shane W. Krska, Gavin Stewart, Neil Strotman, Debra J. Wallace, Timothy Wright
  • Positive allosteric modulators of mGluR2
    Patent number: 9108937
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide 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: February 28, 2011
    Date of Patent: August 18, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
  • (1, 1, 1,3,3,3-hexafluoro-2 hydroxypropan-2-yl) phenyl derivative, pharmaceutical compositions thereof and their use for the treatment of atherosclerosis
    Patent number: 9108939
    Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: August 18, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett
  • Methods for the identification and treatment of patients sensitive to anti IGF-1R inhibition therapy
    Patent number: 9110082
    Abstract: The present invention relates to methods for treating a dalotuzumab responsive cancer, in a patient, comprising determining the expression level of liver kinase B1 (LKB1), in a cancer cell from the patient, and when said expression is determined to be lower than that of a control cell; administering, to said patient, a therapeutically effective amount of dalotuzumab. The invention also relates to methods for assessing neoplastic cells, selecting patients, selecting therapies as well as diagnostic methods.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: August 18, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Sriram Sathyanarayanan, Christopher Winter, Youyuan Xu
  • INDOLINE COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS
    Publication number: 20150225365
    Abstract: This invention relates to indo line compounds of the structural formula I, or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
    Type: Application
    Filed: October 2, 2013
    Publication date: August 13, 2015
    Applicants: ElexoPharm GmbH, Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Lina Yin, Rolf Hartmann, Qingzhong Hu, Ralf Heim, Christina Zimmer
  • MK2 inhibitors
    Patent number: 9102676
    Abstract: The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.
    Type: Grant
    Filed: June 5, 2014
    Date of Patent: August 11, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Tjeerd Andries Barf, Arthur Oubrie, Carsten Schultz-Fadermrecht, Eduard Willem Zwart, Niels Hoogenboom, Sander Martijn De Wilde, Allard Kaptein
  • Substituted pyrrolo[3,2-c]pyridines as TrkA kinase inhibitors
    Patent number: 9102673
    Abstract: The present invention is directed to compounds of formula I and Ia: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: August 11, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Barbara Hanney, Peter Manley, Michael T. Rudd, John M. Sanders, Shawn J. Stachel, Darrell Henze