Patents Assigned to Merck Sharp and Dohme
  • CYCLIC AMIDE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT
    Publication number: 20140128361
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 8, 2014
    Applicants: Pharmacopeia Drug Discovery, Inc., Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey H. Lowrie, Kurt W. Salonz, Suresh D. Babu
  • CYCLOALKYL-FUSED TETRAHYDROQUINOLINES AS CRTH2 RECEPTOR MODULATORS
    Publication number: 20140128367
    Abstract: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8a, E, Y, Z, n, u, 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 associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Application
    Filed: June 14, 2012
    Publication date: May 8, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Xianhai Huang, Jason Brubaker, Scott L. Peterson, John W. Butcher, Joshua T. Close, Michelle Martinez, Rachel Nicola MacCoss, Joon O. Jung, Phieng Siliphaivanh, Hongjun Zhang, Robert G. Aslanian, Purakkattle Johny Biju, Li Dong, Ying Huang, Kevin D. McCormick, Anandan Palani, Ning Shao, Wei Zhou
  • SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT
    Publication number: 20140128368
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: June 11, 2012
    Publication date: May 8, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
  • Compounds that are ERK inhibitors
    Patent number: 8716483
    Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydropyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: May 6, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alan B. Cooper, Yang Nan, Yongqi Deng, Gerald W. Shipps, Jr., Neng-Yang Shih, Hugh Y. Zhu, Jagdish A. Desai, James J-S Wang, Sunil Paliwal, Hon-Chung Tsui, Sobhana Babu Boga, Abdul-Basit Alhassan, Xiaolei Gao, Liang Zhu, Ahmed Samatar
  • Inhibitors of diacylglycerol acyltransferase
    Patent number: 8716312
    Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the 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: November 17, 2009
    Date of Patent: May 6, 2014
    Assignee: Merck Sharp & Dohme Corporation
    Inventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
  • Method for increasing N-glycosylation site occupancy on therapeutic glycoproteins produced in
    Patent number: 8715963
    Abstract: Described is a method for increasing the N-glycosylation site occupancy of a therapeutic glycoprotein produced in recombinant host cells modified as described herein and genetically engineered to express the glycoprotein compared to the N-glycosylation site occupancy of the therapeutic glycoprotein produced in a recombinant host cell not modified as described herein. In particular, the method provides recombinant host cells that overexpress a 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, for example, the Leishmania major STT3D protein, in the presence of expression of the host cell genes encoding the endogenous OTase complex.
    Type: Grant
    Filed: February 23, 2011
    Date of Patent: May 6, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Natarajan Sethuraman, Byung-Kwon Choi, Bianka Prinz, Michael Meehl, Terrance Stadheim
  • Substituted aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes
    Patent number: 8716482
    Abstract: The present invention is directed to novel substituted aminopiperidines 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-ÏV 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: September 15, 2010
    Date of Patent: May 6, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason M. Cox, Tesfaye Biftu, Hong Dong Chu, Danqing Feng, Ann E. Weber
  • Ethenyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections
    Patent number: 8715638
    Abstract: The present invention provides compounds of Formula (A): (Chemical formula should be inserted here as it appears on abstract in paper form) (A) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19, R22, R23, 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: May 6, 2014
    Assignees: Merck Sharp & Dohme Corp., Southern Research Institute
    Inventors: Cecil D. Kwong, F. George Njoroge, Subramaniam Ananthan, Jeremy Clark, Feng Geng, Hollis S. Kezar, III, Joseph A. Maddry, John J. Piwinski, Robert C. Reynolds, Abhijit Roychowdhury, John A. Secrist, III, Neng-Yang Shih
  • METHOD FOR DETECTION OF AMYLOIDS BETA OLIGOMERS IN A FLUID SAMPLE AND USES THEREOF
    Publication number: 20140120037
    Abstract: The invention herein is directed to a selective A? oligomer immunoassay 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, 19.3 and 82E1, to detect and quantify A? oligomers in a cerebrospinal fluid (CSF) sample. The inventive assay 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. The inventive assay can also be used as a target engagement assay that can measure bound A? oligomers as a surrogate end-point for the assessment of therapeutic efficacy and/or target engagement.
    Type: Application
    Filed: December 20, 2013
    Publication date: May 1, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mary J. Savage, Paul J. Shughrue, Alexander McCampbell, Abigail L. Wolfe
  • 2,5-disubstituted piperidine orexin receptor antagonists
    Patent number: 8710076
    Abstract: The present invention is directed to 2,5-disubstituted piperidine 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: April 29, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, Anthony J. Roecker, John D. Schreier
  • Anti-GITR antibodies
    Patent number: 8709424
    Abstract: Antibodies to human GITR are provided, as well as uses thereof, e.g., in treatment of proliferative and immune disorders.
    Type: Grant
    Filed: August 31, 2010
    Date of Patent: April 29, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xiao Min Schebye, Grigori P. Ermakov, Douglas J. Hodges, Leonard G. Presta
  • Factor IXa crystals, related complexes and methods
    Patent number: 8710188
    Abstract: The present invention relates to factor IXa complexes and crystals thereof as well as methods for identifying inhibitors of factor IXa.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: April 29, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brian M. Beyer, Alan W. Hruza, Richard N. Ingram, Vincent S. Madison, Andrew J. Prongay, Paul Reichert
  • INTERLEUKIN-10 ANTIBODIES
    Publication number: 20140112919
    Abstract: The methods and compositions provided herein relate generally to IL-10 specific antibodies and uses thereof. More specifically, compositions of humanized IL-10 specific antibodies and methods to use such antibodies in modulating the biological activity of IL-10, particularly in autoimmune disorders and pathogen-mediated immunopathology.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: LEONARD G. PRESTA
  • TRICYCLIC HETEROCYCLES USEFUL AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS
    Publication number: 20140113920
    Abstract: The present invention is directed to novel tricyclic heterocycles 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: July 2, 2012
    Publication date: April 24, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: Wen-Lian Wu
  • Pyridazine carboxamide orexin receptor antagonists
    Patent number: 8703770
    Abstract: The present invention is directed to pyridazine carboxamide 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 26, 2009
    Date of Patent: April 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Christopher D. Cox, Swati P. Mercer, Anthony J. Roecker, John D. Schreier
  • Substituted pyrazolo[1,5-a]pyrido[3.2-e]pyrimidin-6-one inhibitors of mammalian target of rapamycin
    Patent number: 8703784
    Abstract: This invention relates to novel fused tricyclic compounds under Formula I that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyun Zhao, Andrew McRiner
  • Preparation of crystalline forms of dihydropyrazolopyrimidinone
    Patent number: 8703779
    Abstract: The instant invention relates to crystalline forms of MK-1775, an inhibitor of Weel kinase. Specifically, the instant invention relates to hemihydrates of MK-1775.
    Type: Grant
    Filed: September 2, 2010
    Date of Patent: April 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rositza Petrova, Eric Sirota, Robert Wenslow
  • METHODS FOR MODULATING IL-33 ACTIVITY
    Publication number: 20140105887
    Abstract: Provided herein are methods of modulating IL-33 activity, e.g., for the purpose of treating immune diseases and conditions, as well as methods of screening for compounds capable antagonizing IL-33 signaling.
    Type: Application
    Filed: August 9, 2013
    Publication date: April 17, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Alissa A. Chackerian, Robert A. Kastelein
  • PROCESS FOR PREPARING CHIRAL DIPEPTIDYL PEPTIDASE-IV INHIBITORS
    Publication number: 20140107346
    Abstract: A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.
    Type: Application
    Filed: June 25, 2012
    Publication date: April 17, 2014
    Applicants: Merck Sharp & Dohme Ltd., Merck Sharp & Dohme Corp.
    Inventors: Michael J. Zacuto, Robert F. Dunn, Aaron J. Moment, Jacob M. Janey, David Lieberman, Faye Sheen, Nadine Bremeyer, Jeremy Scott, Jeffrey T. Kuethe
  • SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF
    Publication number: 20140107044
    Abstract: The invention provides compounds 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: Application
    Filed: March 16, 2012
    Publication date: April 17, 2014
    Applicants: Merck Sharp & Dohme Corp., Alectos Therapeutics Inc.
    Inventors: Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Craig A. Coburn, Kun Liu, Harold G. Selnick