Patents by Inventor Michael E. Kopach

Michael E. Kopach 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: 20230158468
    Abstract: A Solid Phase Peptide Synthesis (SPPS) device and method of using the same for manufacturing peptides is taught herein. The system comprises at least two reactors, each reactor including a quantity of SPPS resin. The reactors are positioned in series. A de-protecting agent is added to the first reactor and then transferred to the second and third reactors, in series, thereby operating to de-protect the protected N-group. Wash solvent is added to the first reactor and then transferred to the second and this operation repeated several times. Likewise, an amino acid activated ester solution is added, in series, to the first, second and third reactors, thereby operating to couple the amino acid to the de-protected N-group. Wash solvent is added to the first reactor and then transferred to the second and this operation repeated several times prior to the next cycle. The use of the reactors in series reduces the overall solvent required.
    Type: Application
    Filed: January 29, 2021
    Publication date: May 25, 2023
    Inventors: Martin D. Johnson, Michael E. Kopach, Mark R. Berglund, Stephen Robert GROSKREUTZ, Jingyao WANG, Luke P. Webster
  • Patent number: 10287287
    Abstract: The disclosure provides process developments and novel routes for the preparation of the NK-1 receptor antagonist, Compound (I) and intermediates in those routes.
    Type: Grant
    Filed: August 17, 2016
    Date of Patent: May 14, 2019
    Assignee: ELI LILLY AND COMPANY
    Inventors: Michael E. Kopach, Thomas Michael Wilson, Michael Edward Kobierski
  • Publication number: 20190062337
    Abstract: The present invention provides processes and intermediates for the preparation of {1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile: (I)
    Type: Application
    Filed: October 25, 2018
    Publication date: February 28, 2019
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Joseph R. Martinelli, David Lee Varie, Thomas Michael Wilson
  • Publication number: 20180237433
    Abstract: The disclosure provides process developments and novel routes for the preparation of the NK-1 receptor antagonist, Compound (I) and intermediates in those routes.
    Type: Application
    Filed: August 17, 2016
    Publication date: August 23, 2018
    Inventors: Michael E. Kopach, Thomas Michael Wilson, Michael Edward Kobierski
  • Patent number: 10035787
    Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.
    Type: Grant
    Filed: June 15, 2017
    Date of Patent: July 31, 2018
    Assignee: ELI LILLY AND COMPANY
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen
  • Publication number: 20180134713
    Abstract: The present invention provides processes and intermediates for the preparation of {1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile: (I)
    Type: Application
    Filed: June 16, 2016
    Publication date: May 17, 2018
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Joseph R. Martinelli, David Lee Varie, Thomas Michael Wilson
  • Publication number: 20170283394
    Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.
    Type: Application
    Filed: June 15, 2017
    Publication date: October 5, 2017
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen
  • Patent number: 9708291
    Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: July 18, 2017
    Assignee: Vanda Pharmaceuticals Inc.
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen
  • Publication number: 20160060250
    Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.
    Type: Application
    Filed: November 10, 2015
    Publication date: March 3, 2016
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen
  • Publication number: 20140206877
    Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 24, 2014
    Applicant: Eli Lilly and Company
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen
  • Publication number: 20100056795
    Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: (I) The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV
    Type: Application
    Filed: December 4, 2007
    Publication date: March 4, 2010
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen