Patents by Inventor Jozef Krajcovic

Jozef Krajcovic 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
  • 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: 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