Patents Assigned to Merck Sharp & Dohme
  • SUBSTITUTED PYRIDONE DERIVATIVES AS PDE10 INHIBITORS
    Publication number: 20150291561
    Abstract: The present invention is directed to substituted pyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: November 15, 2013
    Publication date: October 15, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger
  • 2-pyridyloxy-4-nitrile orexin receptor antagonists
    Patent number: 9156819
    Abstract: The present invention is directed to 2-pyridyloxy-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyl-oxy-4-nitrile compounds described herein in the 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: Grant
    Filed: October 17, 2012
    Date of Patent: October 13, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Chromatography media
    Patent number: 9156879
    Abstract: The present invention provides, in part, a chromatographic restricted access media comprising aminopropyl groups derivatized with polysuccinamide that is derivatized with 1-ethylpropylamine and denatured human serum albumin. Methods of purifying polypeptides and complexes thereof are also provided.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: October 13, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lev Z. Vilenchik, Krishna Kalghatgi
  • 2?-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
    Patent number: 9156872
    Abstract: The present invention relates to 2?-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Azido Substituted Nucleoside Derivative, and methods of using the 2?-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: October 13, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Frank Bennett, Vishal Verma, Ashok Arasappan, Kevin Chen, Ying Huang, Angela Kerekes, Latha Nair, Dmitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • Treating diabetes with dipeptidyl peptidase-IV inhibitors
    Patent number: 9156848
    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: October 13, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Tanweer A. Khan
  • N-SUBSTITUTED INDAZOLE SULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS
    Publication number: 20150284389
    Abstract: Disclosed are compounds of Formula AA and Formula AB: wherein “Heteroaryl-1”, RA1, RA2, RB1, and RC are defined herein, which novel compounds have properties for blocking Na 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formulae AA and AB or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Application
    Filed: October 23, 2013
    Publication date: October 8, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph E. Pero, Hannah D.G.F. Lehman, Mark E. Layton, Michael A. Rossi, Michael J. Kelly, III
  • TRICYCLIC SUBSTITUTED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS AND THEIR USE
    Publication number: 20150284379
    Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: October 14, 2013
    Publication date: October 8, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Eric J. Gilbert, Jared N. Cumming, Andrew W. Stamford, Younong Yu, Jack D. Scott, Ulrich Iserloh, Lingyan Wang, John P. Caldwell
  • MINERALOCORTICOID RECEPTOR ANTAGONISTS
    Publication number: 20150284376
    Abstract: The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts thereof, that are useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.
    Type: Application
    Filed: December 2, 2014
    Publication date: October 8, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Alejandro Crespo, Ping Lan, Rudrajit Mal, Anthony Ogawa, Hong Shen, Peter J. Sinclair, Zhongxiang Sun, Ellen K. Vande Bunte, Zhicai Wu, Kun Liu, Robert J. DeVita, Dong-Ming Shen, Min Shu, John Qiang Tan, Changhe Qi, Yuguang Wang, Richard Beresis
  • SECONDARY ALCOHOL SUBSTITUTED TRIAZOLES AS PDE10 INHIBITORS
    Publication number: 20150284368
    Abstract: The present invention is directed to secondary alcohol substituted triazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: November 11, 2013
    Publication date: October 8, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Christopher D. Cox, Vadim Y. Dudkin, Carol A. McVean, Thomas S. Reger, Justin T. Steen
  • Crystalline form of a reverse transcriptase inhibitor
    Patent number: 9150539
    Abstract: The retrovirus designated human immunodeficiency virus (HIV), particularly the strains known as HIV type-1 (HIV-I) 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-1H-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)-1,2-dihydropyridin-3-yl)oxy)benzonitrile used in the treatment HIV infection and AIDS.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: October 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Courtney K. Maguire
  • 2?-cyano substituted nucleoside derivatives and methods of use thereof useful for the treatment of viral diseases
    Patent number: 9150603
    Abstract: The present invention relates to 2?-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Cyano Substituted Nucleoside Derivative, and methods of using the 2?-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: October 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Angela Kerekes, Frank Bennett, Ying Huang, Latha Nair, Dmitri Pissarnitski, Vishal Verma, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • TRICYCLIC SUBSTITUTED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS AND THEIR USE
    Publication number: 20150274716
    Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 5-membered ring, and each of the remaining variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: October 14, 2013
    Publication date: October 1, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Eric J. Gilbert, Jared N. Cumming, Andrew W. Stamford, Younong Yu, Jack D. Scott, Ulrich Iserloh
  • INHIBITORS OF IRAK4 ACTIVITY
    Publication number: 20150274708
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Application
    Filed: October 3, 2013
    Publication date: October 1, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: W. Michael Seganish, Jennifer Hanisak, Guoqing Li, Rui Zhang, Haiqun Tang
  • SUBSTITUTED SPIROPIPERIDINYL COMPOUNDS USEFUL AS GPR120 AGONISTS
    Publication number: 20150274672
    Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: October 11, 2013
    Publication date: October 1, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mariappan Chelliah, Hong Dong Chu, Jason M. Cox, John S. Debenham, Keith Eagen, Ping Lan, Clare London, Michael A. Plotkin, Unmesh Shah, Christopher Joseph Sinz, Zhongxiang Sun, Henry M. Vaccaro, Srikanth Venkatraman
  • 2'-CYANO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20150274739
    Abstract: Compounds of Formula (I) are disclosed, wherein R1, R2, R3, R4, R5, and R18 are defined herein. The compounds encompassed by Formula (I) include compounds which are HCV NS5B inhibitors and other compounds which can be metabolized in vivo to HCV NS5B inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 11, 2013
    Publication date: October 1, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Vinay Girijavallabhan, Stephane Bogen, Weidong Pan, Qun Dang, Ian Davies
  • 4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
    Publication number: 20150274767
    Abstract: The present invention is directed to 4?-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.
    Type: Application
    Filed: March 26, 2015
    Publication date: October 1, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vinay M. Girijavallabhan, David B. Olsen, Zhibo Zhang, Jianmin Fu, Bing-Yu Tang
  • Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
    Patent number: 9145426
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of W, Z, R1H, R2, R3, R4, ring A, ring B, m, n, p, and -L1- is as defined herein. The novel compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: April 2, 2012
    Date of Patent: September 29, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
  • Bipyridylaminopyridines as Syk inhibitors
    Patent number: 9145391
    Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: September 29, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Denis Deschenes, Michael D. Altman, John Michael Ellis, Christian Fischer, Andrew M. Haidle, Solomon D. Kattar, Alan B. Northrup, Adam J. Schell, Graham F. Smith, Brandon M. Taoka, Corey Bienstock, Maria Emilia Di Francesco, Anthony Donofrio, Scott Peterson, Kerrie B. Spencer, James Patrick Jewell, Amjad Ali, David Jonathan Bennett, Qun Dang, John Wai
  • HCV NS3 Protease Inhibitors
    Publication number: 20150266897
    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: Application
    Filed: April 3, 2015
    Publication date: September 24, 2015
    Applicants: MSD ITALIA S.R.L., MERCK SHARP & DOHME CORP.
    Inventors: Nigel J. Liverton, Vincenzo Summa, Maria Emilia Di Francesco, Marco Ferrara, Kevin F. Gilbert, Steven Harper, John A. McCauley, Charles J. McIntyre, Alessia Petrocchi, Marco Pompei, Joseph J. Romano, Michael T. Rudd, John W. Butcher, M. Katharine Holloway
  • NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    Publication number: 20150266895
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Application
    Filed: September 26, 2013
    Publication date: September 24, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kevin J. Wilson, David J. Witter, Phieng Siliphaivanh, Kathryn Lipford, David Sloman, Danielle Falcone, Brendan O'Boyle, Umar Faruk Mansoor, Jongwon Lim, Joey L. Methot, Christopher Boyce, Lei Chen, Matthew H. Daniels, Salem Fevrier, Xianhai Huang, Ravi Kurukulasuriya, Ling Tong, Wei Zhou, Joseph Kozlowski, Milana M. Maletic, Bidhan A. Shinkre, Jayanth Thiruvellore Thatai, Raman Kumar Bakshi, Ganesh Babu Karunakaran