Patents Assigned to Merck Sharp & Dohme
  • IN VITRO PHARMACOKINETIC-PHARMACODYNAMIC DEVICE
    Publication number: 20180291325
    Abstract: The present invention provides an in vitro cell culturing bioreactor device capable of supporting the growth of adherent or non-adherent mammalian cells. The invention also provides methods for monitoring and/or measuring the effects of therapeutic agents on cells, for determining the pharmacokinetic-pharmacodynamic relationship between a drug and a target cell, and for determining an effective dosing regimen for a drug or therapeutic agent.
    Type: Application
    Filed: May 9, 2016
    Publication date: October 11, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Donna M. Carr, Michael K. Wismer, Charles G. Garlisi
  • Factor XIa inhibitors
    Patent number: 10093683
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more compounds of Formula (I), and methods for using the compounds of Formula (I) 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: April 21, 2015
    Date of Patent: October 9, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yeon-Hee Lim, Zhuyan Guo, Amjad Ali, Scott D. Edmondson, Weiguo Liu, Gioconda V. Gallo-Etienne, Heping Wu, Ying-Duo Gao, Andrew W. Stamford, Younong Yu, Nancy J. Kevin, Rajan Anand, Deyou Sha, Santhosh F. Neelamkavil, Zahid Hussain, Puneet Kumar, Remond Moningka, Joseph L. Duffy, Jiayi Xu, Yu Jiang, Anjan Chakrabarti, Hiroki Sone
  • Kit for and method of assembling an applicator for inserting an implant
    Patent number: 10092739
    Abstract: The invention pertains to a kit for assembling a disposable applicator for inserting an implant, in particular a rod-like implant containing an active substance, under the skin of a human or animal, the kit comprising a first component, in turn comprising a main housing part providing a handle for grasping and maneuvering the applicator, a cannula, and a cannula holder mounted in the main housing part, the main housing part having an opening which allows introduction of an implant into the proximal end of the cannula or the cannula holder, and, a second component for closing said opening, in turn comprising a second housing part and a rod attached to or forming an integral whole with the second housing part and mountable inside the cannula or the cannula holder.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: October 9, 2018
    Assignee: MERCK SHARP & DOHME B.V.
    Inventors: Dennis Cornelis Franciscus Beelen, Martin Van Harmelen, Robertus Theodoor Maria Moormann, Maurice Petrus Wilhelmus Tak
  • Heteroaryl-Pyrimidinone Compounds as PDE2 Inhibitors
    Publication number: 20180280390
    Abstract: The present invention is directed to substituted pyrimidinone 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: May 2, 2016
    Publication date: October 4, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Jonathan E. Wilson, Troy McCracken
  • Benzamide imidazopyrazine Btk inhibitors
    Patent number: 10087188
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to 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: Grant
    Filed: December 17, 2015
    Date of Patent: October 2, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jian Liu, Joseph A. Kozlowski, Abdul-Basit Alhassan, Sobhana Babu Boga, Xiaolei Gao, Deodial Guy Guiadeen, Jyhshing Wang, Wensheng Yu, Jiaqiang Cai, Shilan Liu, Dahai Wang, Hao Wu, Chundao Yang
  • Formulation inhibiting effects of low acid environment
    Patent number: 10085991
    Abstract: The present invention is directed to formulations comprising PVP polymer, a dispersion of a compound of Formula I (API), and citric acid, which formulations mitigate the effects of coadministering the compound of Formula I with a proton pump inhibitor compound.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: October 2, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lei Zhu, Yvonne Cegielnik, Qun Lu
  • Process for making beta 3 agonists and intermediates
    Patent number: 10087189
    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: Grant
    Filed: November 9, 2017
    Date of Patent: October 2, 2018
    Assignee: 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
  • Tricyclic compounds as inhibitors of mutant IDH enzymes
    Patent number: 10086000
    Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N?; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: October 2, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Stephane L. Bogen, Matthew L. Childers, Francesc Xavier Fradera Llinas, Alexander J. Kim, John W. Lampe, Michelle R. Machacek, Daniel R. McMasters, Dann L. Parker, Jr., Nunzio Sciammetta, Pengcheng P. Shao, David L. Sloman, Wanying Sun, Feroze Ujjainwalla, Chunhui Huang
  • CRYSTAL FORMS OF A M1 RECEPTOR POSITIVE ALLOSTERIC MODULATOR
    Publication number: 20180273507
    Abstract: The invention is directed to novel anhydrous crystalline butenedioate salt form 1 of Compound I, which is a modulator of muscarinic M1 receptors. The novel crystalline forms of compound I are useful in the treatment or prevention of Alzheimer's disease and other disorders and diseases in which muscarinic M1 receptors are involved. The invention is further directed to pharmaceutical compositions comprising the novel crystalline forms of Compound I.
    Type: Application
    Filed: September 26, 2016
    Publication date: September 27, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: C. Scott Shultz, Courtney Maguire, Yanke Xu
  • Phosphate substituted quinolizine derivatives useful as HIV integrase inhibitors
    Patent number: 10081647
    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: Grant
    Filed: March 25, 2016
    Date of Patent: September 25, 2018
    Assignee: 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
    Patent number: 10081617
    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: Grant
    Filed: April 11, 2016
    Date of Patent: September 25, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric Mertz, Scott D. Edmondson, Sung-Sau So, Wanying Sun, Weiguo Liu, Santhosh F. Neelamkavil, Ying-Duo Gao, Alan Hruza, Yi Zang, Amjad Ali, Rudrajit Mal, Jiafang He, Rongze Kuang, Heping Wu, Anthony K. Ogawa, Andrew F. Nolting
  • ANTAGONISTS OF PCSK9
    Publication number: 20180265592
    Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.
    Type: Application
    Filed: January 31, 2018
    Publication date: September 20, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ayesha Sitlani, Carl P. Sparrow, Shilpa Pandit, Jon H. Condra, Holly A. Hammond
  • PROCESS FOR MAKING M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20180265493
    Abstract: This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.
    Type: Application
    Filed: September 26, 2016
    Publication date: September 20, 2018
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited.
    Inventors: Qinghao Chen, Shane W. Krska, Lushi Tan, Peter E. Maligres, Jeremy Scott, Carl Baxter, Gavin William Stewart, Andrew Gibb
  • Pharmaceutical Compound
    Publication number: 20180258075
    Abstract: Provided is a compound having formula (I): wherein R2 is selected from —C1, —Br and —CN; R1 and R4 are independently selected from H and —F; R631, R632, R641 and R642 are independently selected from —H, —F and substituted or unsubstituted C1-C3 alkyl groups; and R651 and R652 are independently selected from H and substituted or unsubstituted C1-C3 alkyl groups and substituted or unsubstituted phenyl groups; and wherein at least one of R631, R632, R641, R642 and R652 is not —H, or wherein when all of R631, R632, R641, R642 and R652 are —H, R651 is not Me or Et.
    Type: Application
    Filed: September 12, 2016
    Publication date: September 13, 2018
    Applicants: Merck Sharp & Dohme Corp., IOmet Pharma Ltd.
    Inventors: Phillip M. Cowley, Yongxin Han
  • PYRIMIDINONE AMIDE COMPOUNDS AS PDE2 INHIBITORS
    Publication number: 20180256575
    Abstract: The present invention is directed to pyrimidinone amide compounds which may be useful as therapeutic agents for the treatment of central nervous system and/or peripheral 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, Alzheimer's, cognitive impairment, anxiety, depression, migraines, or Huntington's disease, Parkinson's disease, Parkinson's disease dementia (PDD), and other diseases associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: May 10, 2016
    Publication date: September 13, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Deping Wang, XiaoXia Qian, Bart Harper, Meng Yang, Yingjian Bo
  • 7-AMINOCEPHEM DERIVATIVE COMPOUNDS
    Publication number: 20180258101
    Abstract: This disclosure provides methods of making certain 7-aminocephem derivatives useful in the manufacture of cephalosporin antibiotic compounds.
    Type: Application
    Filed: March 14, 2018
    Publication date: September 13, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian MOSHOS, Valdas JURKAUSKAS
  • OXY-CYANOQUINOLINONE PDE9 INHIBITORS
    Publication number: 20180258046
    Abstract: The present invention is directed to oxycyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). 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: July 27, 2016
    Publication date: September 13, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: ANTONELLA CONVERSO, MILDRED L. KAUFMAN, KEVIN RODZINAK
  • ANTIBODY THAT BINDS TO HUMAN PROGRAMMED DEATH LIGAND 2 (PD-L2) AND USES THEREOF
    Publication number: 20180258171
    Abstract: The present disclosure provides antibodies and antigen binding fragments thereof including, but not limited to, monoclonal antibodies that specifically bind to human programmed death ligand 2 (PD-L2). The invention further provides nucleic acids encoding the antibodies and antigen binding fragments of the invention and host cells transformed therewith. The antibodies and antigen binding proteins of the invention are useful in methods for the immunohistochemical detection of human PD-L2 expression in tissue samples.
    Type: Application
    Filed: September 20, 2016
    Publication date: September 13, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jennifer H. Yearley, Linda Liang, Michael Eric Bigler, Christopher John Gibson
  • Antibody neutralizing human respiratory syncytial virus
    Patent number: 10072072
    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: March 22, 2018
    Date of Patent: September 11, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kalpit A. Vora, Kara S. Cox, Aimin Tang, Zhifeng Chen, Daniel DiStefano, Lan Zhang, Hua-Poo Su
  • Ethyl N-boc piperidinyl pyrazolo pyridones as Janus kinase inhibitors
    Patent number: 10072025
    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. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the treatment and prevention of JAK-mediated diseases and disorders using the novel compounds, as well as pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: October 21, 2015
    Date of Patent: September 11, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark E. Scott, David Guerin, Danielle Molinari, Sam Kattar, Peter Fuller, Christopher Dinsmore, Norman Kong, Yunfeng Bai, Jianmin Fu, Yumei Liu, Zhixiang Zheng