Patents by Inventor Jakub Castulik

Jakub Castulik 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).

  • PROCESS FOR PREPARATION OF AXITINIB
    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
  • PROCESS FOR MAKING IXAZOMIB OR INTERMEDIATES THEREFOR
    Publication number: 20200199159
    Abstract: This invention relates to a process for preparing Ixazomib 1, its trimer 1.trimer, its citrate ester 2 or an intermediate for their synthesis. The process comprising at least one amide coupling reaction in the presence of a cyclic alkyl triphosphonic anhydride 9, wherein the R1 groups in the cyclic alkyl triphosphonic anhydride 9 are C1-C6 alkyl groups, preferably n-propyl groups.
    Type: Application
    Filed: August 23, 2018
    Publication date: June 25, 2020
    Inventor: Jakub CASTULIK
  • Process for making bortezomib and intermediates for the process
    Patent number: 8884009
    Abstract: The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: November 11, 2014
    Assignee: Synthon BV
    Inventors: Jakub Castulik, Miroslav Zabadal
  • PROCESS FOR MAKING BORTEZOMIB AND INTERMEDIATES FOR THE PROCESS
    Publication number: 20130203988
    Abstract: The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group.
    Type: Application
    Filed: October 14, 2010
    Publication date: August 8, 2013
    Applicant: Synthon BV
    Inventors: Jakub Castulik, Miroslav Zabadal
  • Process for making montelukast and intermediates therefor
    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
  • PROCESS FOR MAKING MONTELUKAST AND INTERMEDIATES THEREFOR
    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
  • PROCESS OF MAKING IMATINIB
    Publication number: 20090318692
    Abstract: The present invention provides a process of coupling the compound (2) and compound (3) in the presence of a coupling agent, yielding imatinib of formula (1).
    Type: Application
    Filed: December 19, 2008
    Publication date: December 24, 2009
    Inventors: Jakub Castulik, Petr Benovsky
  • Process for making montelukast and intermediates therefor
    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
  • PROCESS FOR MAKING MONTELUKAST AND INTERMEDIATES THEREFOR
    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
  • Process for making montelukast and intermediates therefor
    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
  • PROCESS FOR MAKING MONTELUKAST AND INTERMEDIATES THEREFOR
    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
  • PROCESS FOR MAKING MONTELUKAST AND INTERMEDIATES THEREFOR
    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
  • PROCESS FOR MAKING MONTELUKAST AND INTERMEDIATES THEREFOR
    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