Patents Assigned to Merck Sharp & Dohme
  • IMIDAZO-PYRAZINYL DERIVATIVES USEFUL AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
    Publication number: 20180147208
    Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or pharmaceutically acceptable salt thereofs, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: May 23, 2016
    Publication date: May 31, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joie GARFUNKLE, Olga ORNOSKI, Dann L. PARKER, JR., Subharekha RAGHAVAN, Libo XU
  • Bicyclic ureas and thiadiazolidine-1, 1-dioxides as CETP inhibitors
    Patent number: 9981970
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is —C(?O) or —S(O)2—, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: July 28, 2014
    Date of Patent: May 29, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jian Liu, Pengcheng Patrick Shao, Arto K. Krikorian, Petr Vachal
  • Imidazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug
    Patent number: 9981969
    Abstract: The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.
    Type: Grant
    Filed: June 2, 2014
    Date of Patent: May 29, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Milana Maletic, Yunfu Luo, Zhiqi Qi, Chunsing Li, Tingting Yu, Richard Soll
  • BICYCLIC HETEROCYCLIC COMPOUNDS AS PDE2 INHIBITORS
    Publication number: 20180141952
    Abstract: The present invention is directed to dihydropyrazolopyrimidinone compounds of formulas (I) and (II) 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: June 27, 2016
    Publication date: May 24, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Michael P. Dwyer, Christopher J. Sinz, Jonathan E. Wilson, Daniel V. Paone, Yili Chen, Shimin Xu
  • SURFACE ANCHORED LIGHT CHAIN BAIT ANTIBODY DISPLAY SYSTEM
    Publication number: 20180142233
    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: Application
    Filed: January 10, 2018
    Publication date: May 24, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Hussam Hisham Shaheen, Dongxing Zha
  • Aryl linked imidazole and triazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug
    Patent number: 9975888
    Abstract: The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: May 22, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Milana M. Maletic, Yunfu Luo, Zhiqi Qi, Chun Sing Li, Tingting Yu
  • Factor XIa inhibitors
    Patent number: 9975874
    Abstract: The present invention provides a compound of Formula (I) (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: Grant
    Filed: July 23, 2015
    Date of Patent: May 22, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric Mertz, Scott D. Edmondson, Alan Hruza, Jiafang He, Sung-Sau So, Amjad Ali, Ying-Duo Gao
  • 2-pyridyloxy-3-ester-4-ether orexin receptor antagonists
    Patent number: 9975876
    Abstract: The present invention is directed to 2-pyridyloxy-3-ester-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential 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: December 4, 2014
    Date of Patent: May 22, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • 6-ALKYL DIHYDROPYRAZOLOPYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS
    Publication number: 20180134712
    Abstract: The present invention is directed to 6-alkyl dihydropyrazolopyrimidinone 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 hypo-function or basal ganglia dysfunction.
    Type: Application
    Filed: May 24, 2016
    Publication date: May 17, 2018
    Applicants: Merck Sharp & Dohme Corp., MSD R & D (China) Co. LTD.
    Inventors: Dong-Ming Shen, Michael P. Dwyer, Christopher J. Sinz, Deping Wang, Shawn J. Stachel, Daniel V. Paone, Ashley Forster, Richard Berger, Yilli Chen, Yimin Qian, Shimin Xu, Chunmel Hu, William D. Shipe, Jianmin Fu, Zhigang Guo, HAITANG LI, Yingjian Bo
  • Factor IXa inhibitors
    Patent number: 9969724
    Abstract: In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Grant
    Filed: April 10, 2015
    Date of Patent: May 15, 2018
    Assignees: Merck Sharp & Dohme Corp., Mochida Pharmaceutical Co., Ltd.
    Inventors: Isao Sakurada, Tomokazu Hirabayashi, Yoshitaka Maeda, Hiroshi Nagasue, Takashi Mizuno, Jiayi Xu, Ting Zhang, Cameron Smith, Dann Parker
  • Inhibitors of HIF prolyl hydroxylase
    Patent number: 9969752
    Abstract: The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
    Type: Grant
    Filed: September 23, 2015
    Date of Patent: May 15, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiaqiang Cai, Alejandro Crespo, Xiaoxing Du, Byron Gabriel Dubois, Deodialsingh Guiadeen, Shankaran Kothandaraman, Ping Liu, Rongqiang Liu, Weiguo Quan, Christopher Sinz, Liping Wang
  • Pharmaceutical salts of an orexin receptor antagonist
    Patent number: 9969725
    Abstract: The invention is directed to pharmaceutically acceptable salts of suvorexant, which is an antagonist of orexin receptors. The pharmaceutically acceptable salts of suvorexant are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is further directed to pharmaceutical compositions comprising pharmaceutically acceptable salts of suvorexant.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: May 15, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael McNevin, Sachin Lohani
  • Inhibitors of IRAK4 activity
    Patent number: 9969749
    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: Grant
    Filed: September 25, 2015
    Date of Patent: May 15, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brian M. Andresen, Jason D. Brubaker, Matthew L. Childers, Anthony Donofrio, Thierry Fischmann, Craig R. Gibeau, Solomon D. Kattar, Charles A. Lesburg, Jongwon Lim, John K. F. MacLean, Umar F. Mansoor, Alan B. Northrup, John M. Sanders, Luis Torres
  • Methods of modulating cytokine activity; related reagents
    Patent number: 9970944
    Abstract: Provided are methods of modulating cytokine activity, e.g., for the purpose of treating immune and inflammatory disorders, including tumors and cancer. Also provided are methods of administering agonists or antagonists of IL-33 and IL-33 receptor.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: May 15, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jochen Schmitz, Martin Oft, Robert A. Kastelein, J. Fernando Bazan
  • INDAZOLE AND AZAINDAZOLE BTK INHIBITORS
    Publication number: 20180127411
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R7, R8 and R9 are as herein described. The present invention also provides pharmaceutical compositions comprising these compounds and methods for their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.
    Type: Application
    Filed: April 4, 2016
    Publication date: May 10, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Tony SIU, Michael D. ALTMAN, Brian M. ANDRESEN, Jian LIU, Joseph KOZLOWSKI, Sobhana Babu BOGA, Younong YU, Rajan ANAND, Jiaqiang CAI, Dahai WANG, Shilan LIU
  • INTERMEDIATES FOR PREPARING CGRP RECEPTOR ANTAGONISTS
    Publication number: 20180127417
    Abstract: The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine.
    Type: Application
    Filed: December 19, 2017
    Publication date: May 10, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Frank Chen, Carmela Molinaro, W. Peter Wuelfing, Nobuyoshi Yasuda, Jianguo Yin, Yong-Li Zhong, Joseph Lynch
  • METHODS OF MODULATING CYTOKINE ACTIVITY; RELATED REAGENTS
    Publication number: 20180128837
    Abstract: Provided are methods of modulating cytokine activity, e.g., for the purpose of treating immune and inflammatory disorders, including tumors and cancer. Also provided are methods of administering agonists or antagonists of IL-33 and IL-33 receptor.
    Type: Application
    Filed: December 20, 2017
    Publication date: May 10, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jochen Schmitz, Martin Oft, Robert A. Kastelein, J. Fernando Bazan
  • Antibody neutralizing human respiratory syncytial virus
    Patent number: 9963500
    Abstract: The present invention relates to monoclonal antibodies which have high anti-RSV neutralizing titers. The invention further provides for isolated nucleic acids encoding the antibodies of the invention and host cells transformed therewith. The invention yet further provides for diagnostic, prophylactic and therapeutic methods employing the antibodies and nucleic acids of the invention, particularly as a passive immunotherapy agent in infants and the elderly.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: May 8, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kalpit A. Vora, Kara S. Cox, Aimin Tang, Zhifeng Chen, Daniel DiStefano, Lan Zhang, Hua-Poo Su
  • Geminally substituted cyanoethylpyrazolo pyridones as Janus kinase inhibitors
    Patent number: 9957264
    Abstract: The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: May 1, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew Lloyd Childers, Peter Fuller, David Guerin, Jason David Katz, Qinglin Pu, Mark E. Scott, Christopher F. Thompson, Michelle Martinez, Danielle Falcone, Luis Torres, Yongqi Deng, Ravi Kurukulasuriya, Hongbo Zeng, Yunfeng Bai, Norman Kong, Yumei Liu, Zhixiang Zheng
  • Medical injector pen
    Patent number: D819199
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: May 29, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Angela M. Amend Kwasnik, Benjamin R. Bartfield, Peter Basile, Jeffrey C. Givand, Philip G. Green, Sharad Gupta, Christin L. O'Neill, Steven Carl Persak, Robert Stianchi, Ari Tao Adler, Florian Altmann, Thomas Junk, Florian Kössler, Martin Meier, Scott R. Mackie, Pernilla Danielsson