Patents by Inventor Radomir Skoumal

Radomir Skoumal 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: 20220194921
    Abstract: 1) A process for preparing Axitinib (N-methyl-2-({3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl}sulfanyl)benzamide; compound of formula (I)) 2) A process for purifying the intermediate 2-((3-iodo-1H-indazol-6-yl)thio)-N-methylbenzamide (compound of formula (IIa)) 3) A process for purifying Axitinib using the Axitinib HCI salt (compound of formula (VIII)) as an intermediate 4) A solid form of the Axitinib HCI salt (form J) characterized by an XRPD pattern
    Type: Application
    Filed: April 9, 2020
    Publication date: June 23, 2022
    Inventors: Jakub CASTULIK, Radomir SKOUMAL
  • Publication number: 20190144452
    Abstract: The present invention relates to an improved process of preparation of idelalisib using a solid form of intermediate of formula (2); characterized by XRPD pattern having 2? values 5.5°, 10.9°, 14.3°, 16.9° (±0.2) the process comprising steps a. Reacting of compound of formula (1); ?with a chlorinating agent to obtain a product; b. Reacting of the product with (S)-2-((tert-butoxycarbonyl)amino)butanoic acid and a base, wherein pH of the reaction mixture is set between 7.5 and 10 to obtain compound of formula (2); c. Isolating a solid form of compound of formula (2); d. Transforming the compound of formula (2) into idelalisib.
    Type: Application
    Filed: November 13, 2018
    Publication date: May 16, 2019
    Inventors: Libor VYKLICKY, Zuzana BEDNAROVA, Radomir SKOUMAL
  • Patent number: 10259805
    Abstract: The present invention relates to a process for preparation of crystalline Form 1 of gefitinib of formula (1) characterized by a XRPD powder diffraction pattern comprising, inter alia, peaks at about 7.14, 11.26, 14.25, 15.86, 24.33 and 26.40 degrees 2 theta (±0.2 degrees 2 theta), the process comprising the steps: 1. Dissolving gefitinib in a solvent mixture comprising water and an alcohol selected form ethanol and butanol, wherein the ratio between water and alcohol is between 1:16 and 1:25 (vol:vol) 2. Isolating gefitinib Form 1.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: April 16, 2019
    Assignee: Synthon B.V.
    Inventors: Petr Melsa, Radomir Skoumal
  • Publication number: 20190010147
    Abstract: The present invention relates to a process for preparation of crystalline Form 1 of gefitinib of formula (1) characterized by a XRPD powder diffraction pattern comprising, inter alia, peaks at about 7.14, 11.26, 14.25, 15.86, 24.33 and 26.40 degrees 2 theta (±0.2 degrees 2 theta), the process comprising the steps: 1. Dissolving gefitinib in a solvent mixture comprising water and an alcohol selected form ethanol and butanol, wherein the ratio between water and alcohol is between 1:16 and 1:25 (vol:vol) 2. Isolating gefitinib Form 1.
    Type: Application
    Filed: December 22, 2016
    Publication date: January 10, 2019
    Inventors: Petr MELSA, Radomir SKOUMAL
  • Patent number: 7786138
    Abstract: A compound of the following formula wherein R? is a straight or branched C1-C4 alkyl group is useful in processes associated with the synthesis of montelukast and its salts.
    Type: Grant
    Filed: November 20, 2006
    Date of Patent: August 31, 2010
    Assignee: Synthon BV
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
  • Publication number: 20100099879
    Abstract: The reaction of methylmagnesium halide is improved by the presence of a cerium (III) salt such as cerium trichloride. The reactions are typically associated with the production of montelukast, a pharmaceutically useful compound of the following formula and salts thereof. Further enhancements can be derived from certain intermediates, salts thereof and/or purification thereof before and/or after the reaction involving methylmagnesium halide.
    Type: Application
    Filed: October 9, 2009
    Publication date: April 22, 2010
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
  • Patent number: 7601741
    Abstract: The reaction of methylmagnesium halide is improved by the presence of a cerium (III) salt such as cerium trichloride. The reactions are typically associated with the production of montelukast, a pharmaceutically useful compound of the following formula and salts thereof. Further enhancements can be derived from certain intermediates, salts thereof and/or purification thereof before and/or after the reaction involving methylmagnesium halide.
    Type: Grant
    Filed: November 20, 2006
    Date of Patent: October 13, 2009
    Assignee: Synthon BV
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
  • Publication number: 20090093636
    Abstract: A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (11) is provided.
    Type: Application
    Filed: December 12, 2008
    Publication date: April 9, 2009
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
  • Patent number: 7476748
    Abstract: A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (11) is provided.
    Type: Grant
    Filed: November 20, 2006
    Date of Patent: January 13, 2009
    Assignee: Synthon BV
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
  • Publication number: 20070135642
    Abstract: A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (11) is provided.
    Type: Application
    Filed: November 20, 2006
    Publication date: June 14, 2007
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
  • Publication number: 20070135643
    Abstract: The reaction of methylmagnesium halide is improved by the presence of a cerium (III) salt such as cerium trichloride. The reactions are typically associated with the production of montelukast, a pharmaceutically useful compound of the following formula and salts thereof. Further enhancements can be derived from certain intermediates, salts thereof and/or purification thereof before and/or after the reaction involving methylmagnesium halide.
    Type: Application
    Filed: November 20, 2006
    Publication date: June 14, 2007
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
  • Publication number: 20070135480
    Abstract: A compound of the following formula wherein R? is a straight or branched C1-C4 alkyl group is useful in processes associated with the synthesis of montelukast and its salts.
    Type: Application
    Filed: November 20, 2006
    Publication date: June 14, 2007
    Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal