Patents Assigned to Merck Sharp
  • PROCESS FOR MAKING BETA 3 AGONISTS AND INTERMEDIATES
    Publication number: 20180065973
    Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
    Type: Application
    Filed: November 9, 2017
    Publication date: March 8, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John Y.L. CHUNG, Kevin CAMPOS, Edward CLEATOR, Robert F. DUNN, Andrew GIBSON, R. Scott HOERRNER, Stephen KEEN, Dave LIEBERMAN, Zhuqing LIU, Joseph LYNCH, Kevin M. MALONEY, Feng XU, Nobuyoshi YASUDA, Naoki YOSHIKAWA, Yong-Li ZHONG
  • ANTI-TIGIT ANTIBODIES
    Publication number: 20180066055
    Abstract: The present invention relates to anti-TIGIT antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.
    Type: Application
    Filed: November 20, 2017
    Publication date: March 8, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sybil M. G. Williams, Drake LaFace, Laurence Fayadat-Dilman, Gopalan Raghunathan, Linda Liang, Wolfgang Seghezzi
  • PROCESS FOR MAKING TETRACYCLIC HETEROCYCLE COMPOUNDS
    Publication number: 20180065985
    Abstract: The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.
    Type: Application
    Filed: November 9, 2017
    Publication date: March 8, 2018
    Applicants: Merck Sharpe & Dohme Corp., MSD R&D (China) Co., Ltd., Merck Sharp & Dohme Limited
    Inventors: Hongming Li, Jingjun Yin, Kevin M. Belyk, Kevin R. Campos, Qinghao Chen, Alan M. Hyde, Tetsuji Itoh, Artis Klapars, Matthew Thomas Tudge, Edward Cleator, Aaron M. Dumas, Louis-Charles Campeau, Yonggang Chen, Ji Qi, Wensong Xiao
  • Combination of a PD-1 antagonist and a listeria-based vaccine for treating prostate cancer
    Patent number: 9907849
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a Listeria based strain that expresses prostate-tissue specific antigen (PSA), and the use of the combination therapies for the treatment of prostate cancer.
    Type: Grant
    Filed: July 17, 2015
    Date of Patent: March 6, 2018
    Assignees: Advaxis, Inc., Merck Sharp & Dohme Corp.
    Inventors: Robert Petit, David J. Mauro, Rodolfo F. Perini
  • Diagnosis and prognosis of breast cancer patients
    Patent number: 9909185
    Abstract: The present invention relates to genetic markers whose expression is correlated with breast cancer. Specifically, the invention provides sets of markers whose expression patterns can be used to differentiate clinical conditions associated with breast cancer, such as the presence or absence of the estrogen receptor ESR1, and BRCA1 and sporadic tumors, and to provide information on the likelihood of tumor distant metastases within five years of initial diagnosis. The invention relates to methods of using these markers to distinguish these conditions. The invention also relates to kits containing ready-to-use microarrays and computer software for data analysis using the statistical methods disclosed herein.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: March 6, 2018
    Assignees: THE NETHERLANDS CANCER INSTITUTE, MERCK SHARP & DOHME CORP.
    Inventors: HongYue Dai, Yudong He, Peter S. Linsley, Mao Mao, Christopher J. Roberts, Laura Johanna Van't Veer, Marc J. Van de Vijver, Rene Bernards, A.A. M. Hart
  • PYRAZOLYL PYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS
    Publication number: 20180057480
    Abstract: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: March 21, 2016
    Publication date: March 1, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Jonathan E. Wilson, Meng Yang, Dann Parker, Zack Zhiqiang Guo, Alejandro Crespo, Deping Wang, Troy McCracken
  • METHODS FOR THE TREATMENT AND PROPHYLAXIS OF HIV AND AIDS
    Publication number: 20180055867
    Abstract: The present invention is directed to methods for inhibition of HIV reverse transcriptase, treatment of infection by HIV, prophylaxis of infection by HIV, and the treatment, prophylaxis and/or delay in the onset or progression of AIDS or ARC by administering a compound of structural Formula I or a pharmaceutically acceptable salt or co-crystal thereof, wherein X is —F or —Cl, less frequently than once daily.
    Type: Application
    Filed: February 10, 2017
    Publication date: March 1, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
  • PYRROLOTRIAZINE INHIBITORS OF IRAK4 ACTIVITY
    Publication number: 20180051030
    Abstract: The present invention relates to pyrrolotriazine 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: March 7, 2016
    Publication date: February 22, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JONGWON LIM, MICHAEL D. ALTMAN, JASON D. BRUBAKER, CRAIG R. GIBEAU
  • PYRROLOPYRIDAZINE INHIBITORS OF IRAK4 ACTIVITY
    Publication number: 20180051029
    Abstract: The present invention relates to pyrrolopyridazine 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: March 7, 2016
    Publication date: February 22, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JONGWON LIM, MICHAEL D. ALTMAN, JASON D. BRUBAKER, CRAIG R. GIBEAU
  • CARBOXAMIDE INHIBITORS OF IRAK4 ACTIVITY
    Publication number: 20180051027
    Abstract: The present invention relates to carboxamide 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: March 7, 2016
    Publication date: February 22, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JONGWON LIM, MICHAEL D. ALTMAN, MATTHEW L. CHILDERS, CRAIG R. GIBEAU, GINNY DAI HO, HONCHUNG TSUI
  • THIENOPYRAZINE INHIBITORS OF IRAK4 ACTIVITY
    Publication number: 20180051035
    Abstract: The present invention relates to thienopyrazine 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: March 7, 2016
    Publication date: February 22, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JONGWON LIM, MICHAEL D. ALTMAN, CRAIG R. GIBEAU
  • PHOSPHATE SUBSTITUTED QUINOLIZINE DERIVATIVES USEFUL AS HIV INTEGRASE INHIBITORS
    Publication number: 20180051043
    Abstract: The present invention relates to Phosphate Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Phosphate Substituted Quinolizine Derivative, and methods of using the Phosphate Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: March 25, 2016
    Publication date: February 22, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Tao Yu, Sherman T. Waddell, John A. McCauley, Thomas H. Graham, Hong Li, Izzat Raheem, Jay A. Grobler
  • FACTOR XIa INHIBITORS
    Publication number: 20180050022
    Abstract: The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Application
    Filed: August 21, 2017
    Publication date: February 22, 2018
    Applicant: MERCK SHARP & DOHME CORP
    Inventors: Dong-Ming Shen, Rongze Kuang, Puneet Kumar, Joseph L. Duffy, Cheng Zhu, Amjad Ali, Meng Yang, John S. Debenham
  • PYRAZOLOPYRIMIDINE INHIBITORS OF IRAK4 ACTIVITY
    Publication number: 20180051028
    Abstract: The present invention relates to pyrazolopyrimidine 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: March 7, 2016
    Publication date: February 22, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JONGWON LIM, MICHAEL D. ALTMAN, JASON D. BRUBAKER, CRAIG R. GIBEAU
  • TrkA kinase inhibitors, compositions and methods thereof
    Patent number: 9896447
    Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be 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 Trk-A, Trk-B and/or Trk-C.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: February 20, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Chun Sing Li, Qinghua Mao
  • COMBINATION OF A PD-1 ANTAGONIST AND VORINOSTAT FOR TREATING CANCER
    Publication number: 20180044418
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and suberoylanilide hydroxamic acid (SAHA), and the use of the combination therapies for the treatment of caner.
    Type: Application
    Filed: March 15, 2016
    Publication date: February 15, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Elaine M. Pinheiro, Ronan O'Hagan, Venkataraman Sriram, Joe Phillips
  • PROCESS FOR PREPARING RECOMBINANT INSULIN USING MICROFILTRATION
    Publication number: 20180044395
    Abstract: The use of two tandem microfiltration (MF) steps in a process for making recombinant insulin is described. The two MF steps in a single downstream purification unit operation reduce both soluble and insoluble impurities and exchange the insulin product into a suitable buffer for downstream purification.
    Type: Application
    Filed: March 3, 2016
    Publication date: February 15, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sean S. Gant, Michael J. Iammarino, Kristi Kerchner, Michael A. Rauscher, David J. Roush, Christopher H. Smith, Martin Chandler, Matthew Petroff
  • Surface anchored light chain bait antibody display system
    Patent number: 9890378
    Abstract: The present invention provides, in part, an antibody display system that simultaneously uses a secretion and a display mode. Embodiments of the invention provide a system in which a bait complexed with a monovalent antibody fragment can be captured prior to secretion in a host cell by virtue of surface displaying an antibody light chain and utilizing the covalent interaction of this light chain with the heavy chain of an antibody molecule that is co-expressed in the same host. Polypeptides, polynucleotides and host cells useful for making the antibody display system are also provided along with methods of using the system for identifying antibodies that bind specifically to an antigen of interest.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: February 13, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hussam Hisham Shaheen, Dongxing Zha
  • Process for making substituted quinazoline compounds
    Patent number: 9890128
    Abstract: The present invention is directed to a process for making Substituted Quinazoline Compounds of formula (I): which are useful for the treatment and prophylaxis of HCMV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: February 13, 2018
    Assignees: MERCK SHARP & DOHME CORP., AICURIS ANTI-INFECTIVE CURES GMBH
    Inventors: Michael Luzung, Guy Humphrey, Bangping Xiang, Kevin M. Belyk, Stephen Mark Dalby, Wilfried Schwab, Burkhard Klenke, Tom Moody, Gareth Brown
  • Glucose-responsive insulin conjugates
    Patent number: 9889205
    Abstract: Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein the saccharide for at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: February 13, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Lin Yan, Pei Huo