Patents by Inventor Petr Benovsky

Petr Benovsky 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).

  • Synthesis of paliperidone
    Patent number: 7977480
    Abstract: A 9-hydroxy or 9-acyloxy group can be added to a pyridopyrimidinone ring structure by a process comprising acylating a compound of formula (5) under Vilsmeier-Haack or Friedel-Crafts conditions to form a compound (6); and transforming with a peroxo-compound to obtain the compound (1). R represents hydrogen or a C1-C20 acyl group. The process is useful in the synthesis of paliperidone and derivatives.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: July 12, 2011
    Assignee: Synthon BV
    Inventors: Jiri Bartl, Jozef Krajcovic, Petr Benovsky
  • Paliperidone ketone
    Patent number: 7932385
    Abstract: A compound of formula (7.2) or an acid addition salt thereof. The compound can be used as a reference standard for monitoring the presence thereof in a paliperidone sample, including monitoring the completion of a paliperidone reaction. Reduction in the amount of the compound in paliperidone can be achieved by crystallization in the presence of a hydride reductant.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: April 26, 2011
    Assignee: Synthon BV
    Inventors: Jozef Krajcovic, Jiri Bartl, Petr Benovsky
  • 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
  • PALIPERIDONE KETONE
    Publication number: 20100069633
    Abstract: A compound of formula (7.2) or an acid addition salt thereof. The compound can be used as a reference standard for monitoring the presence thereof in a paliperidone sample, including monitoring the completion of a paliperidone reaction. Reduction in the amount of the compound in paliperidone can be achieved by crystallization in the presence of a hydride reductant.
    Type: Application
    Filed: July 10, 2009
    Publication date: March 18, 2010
    Inventors: Jozef Krajcovic, Jiri Bartl, Petr Benovsky
  • SYNTHESIS OF PALIPERIDONE
    Publication number: 20100010218
    Abstract: A compound of formula (6) or an acid addition salt thereof in which G is (i) a leaving group A selected from a halo group and a sulfonyloxy group, or (ii) a group of the formula (20) is useful in processes of making paliperidone and related compounds.
    Type: Application
    Filed: July 10, 2009
    Publication date: January 14, 2010
    Inventors: Jiri Bartl, Petr Benovsky
  • 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
  • SYNTHESIS OF PALIPERIDONE
    Publication number: 20090156810
    Abstract: A 9-hydroxy or 9-acyloxy group can be added to a pyridopyrimidinone ring structure by a process comprising acylating a compound of formula (5) under Vilsmeier-Haack or Friedel-Crafts conditions to form a compound (6); and transforming with a peroxo-compound to obtain the compound (1). R represents hydrogen or a C1-C20 acyl group. The process is useful in the synthesis of paliperidone and derivatives.
    Type: Application
    Filed: December 10, 2008
    Publication date: June 18, 2009
    Inventors: Jiri Bartl, Jozef Krajcovic, Petr Benovsky
  • 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: 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
  • 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