Patents by Inventor Artis Klapars

Artis Klapars has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20230174567
    Abstract: The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3?-fluoro-thio-guanosine monophosphate or 3?-F-thio-GMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
    Type: Application
    Filed: May 20, 2021
    Publication date: June 8, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Travis Armiger, Kevin M. Belyk, Tamas Benkovics, Cheol K. Chung, Yining Ji Chen, Heather Claire Johnson, Artis Klapars, Zhijian Liu, Zhuqing Liu, Jeffrey C. Moore, Andrew J. Neel, Feng Peng, Stephan M. Rummelt, Nastaran Salehi Marzuarani, Benjamin D. Sherry, Zhiguo Jake Song, Ben William Hulme Turnbull, Lu Wang, Feng Xu
  • Patent number: 10618926
    Abstract: The present invention is directed to process for making Compounds of Formula (II): (II), and salts thereof, wherein B, X, R2, R3, R4 R7, R8 and R9 are defined herein.
    Type: Grant
    Filed: March 28, 2016
    Date of Patent: April 14, 2020
    Assignee: Merck Sharp & Dohme
    Inventors: Steven M. Silverman, Bryon Ladd Simmons, Zhuqing Liu, Jing Liao, Artis Klapars, Kevin R. Campos, Ana Inés Bellomo Peraza
  • Patent number: 10597422
    Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV 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: January 15, 2019
    Date of Patent: March 24, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Daniel DiRocco, Artis Klapars, Edward C. Sherer
  • Patent number: 10526363
    Abstract: The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.
    Type: Grant
    Filed: August 14, 2015
    Date of Patent: January 7, 2020
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.
    Inventors: John Simon Edwards, Peter Richard Mullens, Edward Cleator, Bryon L. Simmons, Courtney K. Maguire, Jeremy Peter Scott, Nobuyoshi Yasuda, Yong-Li Zhong, Lisa F. Frey, Peter G. Dormer, Andrew Brunskill, Artis Klapars, Pu Qian, Yi Zhang, Baoqiang Wan, Eric Ashley
  • Publication number: 20190144485
    Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Application
    Filed: January 15, 2019
    Publication date: May 16, 2019
    Inventors: Daniel DiRocco, Artis Klapars, Edward C. Sherer
  • Patent number: 10251903
    Abstract: The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV 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: October 20, 2015
    Date of Patent: April 9, 2019
    Assignees: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLC
    Inventors: Bryon L. Simmons, Kevin R. Campos, Artis Klapars, Alistair J. Stewart, Benjamin A. Mayes, Peter E. Maligres, Alan Hyde, Steven Mark Silverman, Yong-Li Zhong, Adel M. Moussa, Kenneth Baker, Kara Van Valkenburg
  • Patent number: 10214554
    Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV 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: February 8, 2017
    Date of Patent: February 26, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Y. L. Chung, Amude Kassim, John Limanto, Michael Shevlin, Peter E. Maligres, Daniel A. DiRocco, James F. Dropinski, Rose Mathew, Yi Ning Ji Chen, Edward C. Sherer, Mikhail Reibarkh, Artis Klapars, Alan Hyde, Susan L. Zultanski, Aaron Moment, Bryon Simmons, Tyler A. Davis, Timothy James Wright, Ralph Calabria, Louis charles Campeau
  • Patent number: 10202401
    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: Grant
    Filed: November 9, 2017
    Date of Patent: February 12, 2019
    Assignees: MSD R&D CN CO., LTD, MERCK SHARP & DOHME CORP., 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
  • Patent number: 10053460
    Abstract: The present invention relates to processes for preparing compounds of Formula I. Such compounds include interme-diates in the manufacture of 7-oxo-1,6-diazabicyclo[3.2.1 ]octane-2-carboxamide beta-lactamase inhibitors such as (2S,5R)-7-oxo-N-5 piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also relates to novel intermediates formed i these processes. The present invention relates to a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: August 21, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhijian Liu, Nobuyoshi Yasuda, Lu Yang, Artis Klapars, Kevin R. Campos, Mikhail Reibarkh
  • Publication number: 20180111954
    Abstract: The present invention is directed to process for making Compounds of Formula (II): (II), and salts thereof, wherein B, X, R2, R3, R4 R7, R8 and R9 are defined herein.
    Type: Application
    Filed: March 28, 2016
    Publication date: April 26, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Steven M. Silverman, Bryon Ladd Simmons, Zhuqing Liu, Jing Liao, Artis Klapars, Kevin R. Campos, Ana Inés Bellomo Peraza
  • 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
  • Publication number: 20170362233
    Abstract: The present invention relates to processes for preparing compounds of Formula I. Such compounds include intermediates in the manufacture of 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamide beta-lactamase inhibitors such as (2S,5R)-7-oxo-N-5 piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also relates to novel intermediates formed i these processes. The present invention relates to a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 30, 2015
    Publication date: December 21, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Zhijian Liu, Nobuyoshi Yasuda, Lu Yang, Artis Klapars, Kevin R. Campos, Mikhail Reibarkh
  • Publication number: 20170275327
    Abstract: The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.
    Type: Application
    Filed: August 14, 2015
    Publication date: September 28, 2017
    Inventors: John Edwards, Peter Richard Mullens, Ed Cleator, Bryon L. Simmons, Courtney K. Maguire, Jeremy Peter Scott, Nobuyoshi Yasuda, Yong-Li Zhong, Lisa F. Frey, Peter G. Dormer, Andrew Brunskill, Artis Klapars, Puneet Qian, Yi Zhang, Baoqiang Wan
  • Publication number: 20170246198
    Abstract: The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Application
    Filed: October 20, 2015
    Publication date: August 31, 2017
    Applicants: IDENIX Pharmaceuticals LLC, Merck Sharp & Dohme Corp.
    Inventors: Bryon L. SIMMONS, Kevin R. CAMPOS, Artis KLAPARS, Alistair J. STEWART, Benjamin A. MAYES, Peter E. MALIGRES, Alan HYDE, Steven Mark SILVERMAN, Yong-Li ZHONG, Adel M. MOUSSA, Kenneth BAKER, Kara van VALKENBURG
  • Publication number: 20170226146
    Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Application
    Filed: February 8, 2017
    Publication date: August 10, 2017
    Inventors: John Y.L. Chung, Amude Kassim, John Limanto, Michael Shevlin, Peter E. Maligres, Daniel A. DiRocco, James F. Dropinski, Rose Mathew, Yi Ning Ji Chen, Edward C. Sherer, Mikhail Reibarkh, Artis Klapars, Alan Hyde, Susan L. Zultanski, Aaron Moment, Bryon Simmons, Tyler A. Davis, Timothy James Wright, Ralph Calabria, Louis Charles Campeau
  • Patent number: 9725464
    Abstract: The present invention is directed to a process for preparing Tetracyclic Heterocycle Compounds of formula (I): which are useful as HCV NS5A inhibitors. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: August 8, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian Mangion, Cheng-yi Chen, Ingyu Jeon, Yonggang Chen, Hongmei Li, Hoa N. Nguyen, Peter E. Maligres, Artis Klapars, Ilia Zavialov, Nobuyoshi Yasuda
  • Publication number: 20170166586
    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 are useful as synthetic intermediates in the process of the invention.
    Type: Application
    Filed: July 10, 2015
    Publication date: June 15, 2017
    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
  • Publication number: 20160257698
    Abstract: The present invention is directed to a process for preparing Tetracyclic Heterocycle Compounds of formula (I): which are useful as HCV NS5A inhibitors. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Application
    Filed: October 24, 2014
    Publication date: September 8, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Ian Mangion, Cheng-yi Chen, Ingyu Jeon, Yonggang Chen, Hongmei Li, Hoa N. Nguyen, Peter E. Maligres, Artis Klapars, Ilia Zavialov, Nobuyoshi Yasuda
  • Publication number: 20150259284
    Abstract: The present invention relates to a process for preparing aminocyclohexyl ether compounds of Formula I: or the pharmaceutically acceptable salts and esters thereof. In particular, the instant invention is directed towards a process for preparing (1R,2R)-2-[(3R)-Hydroxypyrrolidinyl]-1-(3,4-dimethoxyphenethoxy)-cyclohexane as well as various intermediates.
    Type: Application
    Filed: March 19, 2015
    Publication date: September 17, 2015
    Inventors: John Limanto, Gregory L. Beutner, Jingjun Yin, Artis Klapars, Eric R. Ashley, Hallena R. Strotman, Matthew D. Truppo, Cheol K. Chung, Gregory Hughes, Zhijian Liu, Brendan Grau, Jacob Janey
  • Patent number: 9067955
    Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods, such as the reaction of Z-X with C(L)(R)(R?)2 in the present of a catalyst and a base, thereby forming C(Z)(R)(R?)2; wherein X represents I, Cl, alkylsulfonate, or arylsulfonate; Z represents optionally substituted aryl, heteroaryl or alkenyl; L represents H or a negative charge; catalyst comprises a copper atom or ion, and a ligand, wherein the ligand is an optionally substituted aryl alcohol, alkyl amine, 1,2-diamine, 1,2-aminoalcohol, 1,2-diol, imidazolium carbene, pyridine, or 1,10-phenanthroline; the ligand is a chelating ligand; and the base represents a Bronsted base; R represents H, optionally substituted alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl; R? represents independently for each occurrence H, alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl, formyl, acyl, —CO2R?, —C(O)N(R)2, sulfonyl, —P(O)(OR?)2, —CN, or —NO2; R? represents independently for each occurrence optionally substituted alky
    Type: Grant
    Filed: May 9, 2006
    Date of Patent: June 30, 2015
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Uhlenbrock, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy