Patents Assigned to Merck Sharp and Dohme Corp.
  • Patent number: 11207312
    Abstract: The present invention relates to metallo-?-lactamase inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
    Type: Grant
    Filed: July 12, 2018
    Date of Patent: December 28, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Shuzhi Dong, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Dexi Yang, Xin Gu, Jinlong Jiang, Li Xiao
  • Patent number: 11207406
    Abstract: The present invention includes antibodies and antigen-binding fragments thereof that specifically bind to human or cynomolgous monkey LAG3 as well as immunoglobulin chains thereof and polynucleotides encoding the same along with injection devices comprising such antibodies or fragments. Vaccines including such antibodies and fragments as well as compositions comprising the antibodies and fragments (e.g., including anti-PD1 antibodies) are included in the invention. Methods for treating or preventing cancer or infection using such compositions are also provided. In addition, methods for recombinant expression of the antibodies and fragments are part of the present invention.
    Type: Grant
    Filed: December 7, 2018
    Date of Patent: December 28, 2021
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Linda Liang, Laurence Fayadat-Dilman, Rene De Waal Malefyt, Gopalan Raghunathan
  • Patent number: 11208407
    Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I) Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Grant
    Filed: July 30, 2018
    Date of Patent: December 28, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hua Zhou, Abdelghani Achab, Xavier Fradera, Yongxin Han, Derun Li, Meredeth A. McGowan, Nunzio Sciammetta, David L. Sloman, Wensheng Yu
  • Publication number: 20210395224
    Abstract: The present invention is directed to cinnolinyl and quinolinyl pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors 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 diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Application
    Filed: October 24, 2019
    Publication date: December 23, 2021
    Applicants: Merck Sharp & Dohme Corp., MSD R&D (China) Co. LTD.
    Inventors: John J. Acton, III, Melissa Egbertson, Xiaolei Gao, Scott T. Harrison, Timothy J. Henderson, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Zhaoyang Meng, James Mulhearn, Vanessa L. Rada, Jeffrey W. Schubert, Oleg B. Selyutin, David M. Tellers, Ling Tong, Fengqi Zhang, Jianming Bao, Chunsing Li
  • Publication number: 20210395255
    Abstract: In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): or and pharmaceutically acceptable salts thereof, wherein, R1, R2, and R3 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
    Type: Application
    Filed: November 15, 2019
    Publication date: December 23, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Zachary G. Brill, Amjad Ali, Jared Cumming, Duane DeMong, Qiaolin Deng, Thomas H. Graham, Rongze Kuang, Yeon-Hee Lim, Christopher W. Plummer, Jenny Lorena Rico Duque, Huijun Wang, Yonglian Zhang, Kake Zhao
  • Publication number: 20210393600
    Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Application
    Filed: April 15, 2019
    Publication date: December 23, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Liangqin Guo, Hongjun Zhang, Ping Chen, Dane Clausen, Xavier Fradera, Yongxin Han, Shuwen He, Xianhai Huang, Alexander Pasternak, Qinglin Pu, Li Xiao, Feng Ye
  • Publication number: 20210395240
    Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Application
    Filed: October 28, 2019
    Publication date: December 23, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dane Clausen, Xavier Fradera, Liangqin Guo, Yongxin Han, Shuwen He, Joseph Kozlowski, Guoqing Li, Theodore A. Martinot, Alexander Pasternak, David Sloman, Li Xiao, Wensheng Yu, Rui Zhang
  • Publication number: 20210395236
    Abstract: The present invention is directed to substituted certain N-heteroaryl indazole derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. 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 diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.
    Type: Application
    Filed: October 25, 2019
    Publication date: December 23, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vladimir SIMOV, William P. KAPLAN, John J. ACTON, III, Michael J. ARDOLINO, Joanna L. CHEN, Peter H. FULLER, Hakan GUNAYDIN, Derun LI, Ping LIU, Kaitlyn Marie LOGAN, Joey METHOT, Gregori J. MORRIELLO, Santhosh F. NEELAMKAVIL, Luis TORRES, Xin YAN, Hua ZHOU
  • Publication number: 20210387966
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
    Type: Application
    Filed: October 31, 2019
    Publication date: December 16, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ashok Arasappan, Ian M. Bell, Michael J. Breslin, Christopher James Bungard, Christopher S. Burgey, Harry R. Chobanian, Jason M. Cox, Anthony T. Ginnetti, Deodial Guy Guiadeen, Kristen L. G. Jones, Mark E. Layton, Hong Liu, Jian Liu, James J. Perkins, Shawn J. Stachel, Linda M. Suen-Lai, Zhe Wu
  • Publication number: 20210388023
    Abstract: Described herein are methods of separating lipid nanoparticles (LNPs) according to their isoelectic points, the methods comprising applying a separating voltage to a separation matrix comprising carrier ampholytes and the LNPs for a sufficient time to separate the LNPs according to their isoelectic points.
    Type: Application
    Filed: November 1, 2019
    Publication date: December 16, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sha Ha, John W. Loughney, Kevin A. Minsker, Richard R. Rustandi
  • Patent number: 11198687
    Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation (I).
    Type: Grant
    Filed: September 14, 2018
    Date of Patent: December 14, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Brendan M. Crowley, Peter J. Manley, William D. Shipe
  • Patent number: 11198718
    Abstract: A process is described for purifying insulin and insulin analogs that comprises high-pressure liquid chromatography with an acidic cation exchange medium performed in the presence of a water miscible organic modifier and at an elevated temperature followed by reverse phase chromatography performed in the presence of a water miscible organic modifier and at an elevated temperature.
    Type: Grant
    Filed: August 27, 2019
    Date of Patent: December 14, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Allison D. Ortigosa, Michael P. Coleman, Shibu T. George, Michael A. Rauscher, Mark C. Sleevi, Kartoa Chow
  • Patent number: 11197921
    Abstract: The present invention provides methods for making polysaccharide-protein conjugates in which polysaccharides, typically from bacteria, are conjugated to a carrier protein by reductive amination under conditions which improve conjugation reaction consistency, increase consumption of protein during conjugation reaction, generate conjugates of higher molecular weight, and/or reduce the levels of free cyanide in the conjugate reaction product. The polysaccharide-protein conjugates obtained using these methods are useful for inclusion in multivalent vaccines.
    Type: Grant
    Filed: January 30, 2018
    Date of Patent: December 14, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jitin Bajaj, Michael Albert Winters, Emily Wen, Jian He
  • Publication number: 20210379596
    Abstract: A vial holder for holding and stabilizing vials, the vial holder comprising a base, and both a vertical mount and a horizontal mount extending from one side of the base. The vertical mount comprises a cylindrical cavity configured to receive and rotatably attach the vial to the base such that the vial is held to the base in a generally vertical orientation, while the horizontal mount comprises a body support and a neck support configured to receive and rotatably attach the body and the neck of the vial to the base such that the vial is held to the base in a generally horizontal orientation. In both orientations, the vial holder of the present invention provides easy access to most of the exterior surfaces of the vials and reduces safety hazards associated with creating sample defects on vials for purposes of qualification testing for vial inspectors.
    Type: Application
    Filed: June 2, 2021
    Publication date: December 9, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shane Owen Peechatka, Kristen Mancini
  • Publication number: 20210380677
    Abstract: The invention provides methods for using and compositions of humanized antibodies that bind tau protein that is phosphorylated at the serine at position 413.
    Type: Application
    Filed: December 15, 2020
    Publication date: December 9, 2021
    Applicants: TEIJIN PHARMA LIMITED, MERCK SHARP & DOHME CORP.
    Inventors: Hiroshi Eguchi, Takashi Murakami, Naoko Namiki, Akira Tanokura, Jeanne E. Baker, Sophie Parmentier Batteur, Angela Marie Jablonski, Daniel Stephen Malashock, Carl Mieczkowski, Gopalan (Raghu) Raghunathan
  • Publication number: 20210380694
    Abstract: The invention relates to stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof. In some embodiments the formulations of the invention comprise between 5-250 mg/mL anti-PD-1 antibody, or antigen binding fragment thereof, a buffer, a stabilizer, a surfactant, and an antioxidant in the amounts specified herein. In particular embodiments, the anti-PD-1 antibody is pembrolizumab. The invention further provides methods for treating various cancers with stable formulations of the invention. In some embodiments of the methods of the invention, the formulations are administered to a subject by intravenous or subcutaneous administration.
    Type: Application
    Filed: November 6, 2019
    Publication date: December 9, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: William P. Forrest, Jr., Chakravarthy Nachu Narasimhan, Yogita Krishnamachari
  • Publication number: 20210379020
    Abstract: The present invention provides methods of treating malaria by administration of a compound of Formula (I): or a pharmaceutically acceptable salt of said compound, to a subject in need thereof, wherein the variables X, R1, R3, R4, R5, A, B, L, m and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.
    Type: Application
    Filed: August 11, 2021
    Publication date: December 9, 2021
    Applicants: Merck Sharp & Dohme Corp., The Walter and Eliza Hall Institute of Medical Research
    Inventors: Tanweer A. Khan, Jared N. Cumming, David B. Olsen, Justin A. Boddey, Alan F. Cowman, Brad E. Sleebs
  • Publication number: 20210379278
    Abstract: A syringe holder for holding and stabilizing syringes, the syringe holder comprising a base, and both a vertical mount and a horizontal mount extending from one side of the base. The vertical mount comprises a cylindrical cavity configured to receive and rotatably attach the syringe to the base such that the syringe is held to the base in a generally vertical orientation, while the horizontal mount comprises a lower barrel support and an upper barrel support configured to receive and rotatably attach the bottom end of the barrel and the top end of the barrel of the syringe to the base such that the syringe is held to the base in a generally horizontal orientation. In both orientations, the syringe holder of the present invention provides easy access to most of the exterior surfaces of the syringes and reduces safety hazards associated with creating sample defects on syringes for purposes of qualification testing for syringe inspectors.
    Type: Application
    Filed: June 2, 2021
    Publication date: December 9, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shane Owen Peechatka, Kristen Mancini
  • Publication number: 20210380572
    Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Application
    Filed: October 11, 2019
    Publication date: December 9, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dane Clausen, Ping Chen, Xavier Fradera, Liangqin Guo, Yongxin Han, Shuwen He, Jongwon Lim, Theodore A. Martinot, Alexander Pasternak, Li Xiao, Wensheng Yu
  • Publication number: 20210380580
    Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors 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 diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Application
    Filed: June 22, 2018
    Publication date: December 9, 2021
    Applicants: Merck Sharp & Dohme Corp., MSD R&D (CHINA) CO., LTD.
    Inventors: John J. ACTON, III, Jianming BAO, Qiaolin DENG, Melissa EGBERTSON, Ronald FERGUSON, II, Xiaolei GAO, Scott Timothy HARRISON, Timothy J. HENDERSON, Sandra L. KNOWLES, Chunsing LI, Michael Man-Chu LO, Robert D. MAZZOLA, Jr., Meng NA, Michael T. RUDD, Oleg B. Selyutin, David M. TELLERS, Ling TONG, Fengqi ZHANG, Takao SUZUKI