Patents by Inventor Antonin Holy

Antonin Holy 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: 20130324566
    Abstract: The invention provides pyrimidine compounds of general formula (I), which reduce simultaneously the production of nitric oxide (NO) and prostaglandin E2 (PGE2). They have no negative effect on the viability of cells in concentrations decreasing the production of these factors by up to 50%; they are not cytotoxic. Furthermore, a method of preparation of the pyrimidine compounds of general formula (I), carrying 2-formamido group, a pharmaceutical composition comprising the substituted pyrimidine compounds according to the invention, and the use of these compounds for the treatment of inflammatory and cancer diseases are provided.
    Type: Application
    Filed: February 27, 2012
    Publication date: December 5, 2013
    Applicants: USTAV EXPERIMENTALNI MEDICINY AKADEMIE VED CR, V.V.I., USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CR, V.V.I.
    Inventors: Petr Jansa, Antonin Holy, Zdenek Zidek, Eva Kmonickova, Zlatko Janeba
  • Patent number: 8153787
    Abstract: The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: April 10, 2012
    Assignees: K.U. Leuven Research & Development, Institute of Organic Chemistry and Biochemistry Academy of Sciences of the Czech Republic
    Inventors: Antonin Holy, Marcela Krecmerova, Alois Piskala, Graciela Andrei, Robert Snoeck, Erik De Clercq, Johan Neyts, Lieve Naesens
  • Publication number: 20090005346
    Abstract: The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.
    Type: Application
    Filed: December 8, 2006
    Publication date: January 1, 2009
    Applicants: K.U.Leuven Research & Development, Institute of Organic Chemistry and Biochemistry Academy of Sciences of the Czech Republic
    Inventors: Antonin Holy, Marcela Krecmerova, Alois Piskala, Graciela Andrei, Erik De Clercq, Robert Snoeck, Johan Neyts, Lieve Naesens
  • Publication number: 20060241081
    Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
    Type: Application
    Filed: June 23, 2006
    Publication date: October 26, 2006
    Inventors: Jan Balzarini, Erik De Clercq, Antonin Holy, Dana Hockova
  • Patent number: 7115592
    Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
    Type: Grant
    Filed: June 16, 2004
    Date of Patent: October 3, 2006
    Assignees: Institute of Organic Chemistry, Biochemistry of the Academy of Sciences of the Czech Republic
    Inventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy, Dana Hockova
  • Publication number: 20050075318
    Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
    Type: Application
    Filed: June 16, 2004
    Publication date: April 7, 2005
    Inventors: Jan Balzarini, Erik De Clercq, Antonin Holy, Dana Hockova
  • Publication number: 20050038058
    Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
    Type: Application
    Filed: September 21, 2004
    Publication date: February 17, 2005
    Inventors: Jan Balzarini, Erik De Clercq, Antonin Holy
  • Patent number: 6818633
    Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
    Type: Grant
    Filed: June 28, 2002
    Date of Patent: November 16, 2004
    Assignees: Institute of Organic Chemistry and Biochemistry Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
    Inventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy
  • Patent number: 6653296
    Abstract: Resolved enantiomers of the formula (IA) and (IB) wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections.
    Type: Grant
    Filed: February 2, 1995
    Date of Patent: November 25, 2003
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
    Inventors: Antonin Holy, Hana Dvorakova, Erik Desire Alice De Clercq, Jan Marie Rene Balzarini
  • Publication number: 20030109499
    Abstract: Novel compounds are provided having formula (I) 1
    Type: Application
    Filed: June 28, 2002
    Publication date: June 12, 2003
    Applicant: INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ACADEMY OF SCIENCES
    Inventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy
  • Patent number: 6479673
    Abstract: Resolved enantiomers of the formula wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections.
    Type: Grant
    Filed: February 8, 2000
    Date of Patent: November 12, 2002
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting, V.Z.W.
    Inventors: Antonin Holý, Hana Dvo{haeck over (r)}áková, Erik Desire Alice DeClercq, Jan Marie Rene Balzarini
  • Patent number: 6057305
    Abstract: Resolved enantiomers of the formula ##STR1## wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections.
    Type: Grant
    Filed: August 5, 1992
    Date of Patent: May 2, 2000
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting, v.z.w.
    Inventors: Antonin Holy, Hana Dvorakova, Erik Desire Alice DeClercq, Jan Marie Rene Balzarini
  • Patent number: 5977061
    Abstract: Novel PMP, PME and HPMP and related compounds containing N-6 substituted 2,6-diaminopurine and adenine bases are provided. These compounds are useful in a variety of utilities, including as intermediates in the preparation of flame retardants, diagnostic reagents and therapeutics, including antivirals. Of particular note are compounds otherwise not known to possess anti-DNA viral activity that become potent inhibitors of DNA viruses upon substitution of the N-6 site, thereby providing a novel and unexpected and surprising use for such compounds.
    Type: Grant
    Filed: April 21, 1995
    Date of Patent: November 2, 1999
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting, v.z.w.
    Inventors: Antonin Holy, Erik Desire Alice De Clercq
  • Patent number: 5869467
    Abstract: This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyolic bases and their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.
    Type: Grant
    Filed: March 28, 1995
    Date of Patent: February 9, 1999
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
    Inventors: Antonin Holy, Ivan Rosenberg, Erik D. A. De Clercq
  • Patent number: 5733896
    Abstract: N-(3-Fluoro-2-phosphonylmethoxypropyl) derivatives of purine and pyrimidine heterocyclic bases, method of producing them and their use as active principles of drugs.The invention relates to suppression of multiplication of viruses, particularly retroviruses, by application of the new compounds, N-(3-fluoro-2-phosphonylmethoxypropyl) derivatives of purine and pyrimidine heterocyclic bases. These compounds are obtained by the reaction of the N-(3-fluoro-2-hydroxypropyl) derivatives of purine and pyrimidine heterocyclic bases with diesters of p-toluenesulfonyloxymethylphosphonic acid in the presence of sodium hydride.
    Type: Grant
    Filed: March 18, 1994
    Date of Patent: March 31, 1998
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
    Inventors: Antonin Holy, Jindrich Jindrich, Erik De Clercq, Jan Balzarini
  • Patent number: 5641763
    Abstract: This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyclic bases and their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.
    Type: Grant
    Filed: October 11, 1994
    Date of Patent: June 24, 1997
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
    Inventors: Antonin Holy, Ivan Rosenberg, Erik D. A. De Clercq
  • Patent number: 5352786
    Abstract: The invention relates to new compounds, di(2-propyl) esters of (R)-, (S)- and (RS)-1-fluoro-2-phosphonomethoxy-3-p-toluenesulfonyloxypropane and the method of producing them. The compounds can be used with advantage in the preparation of N-(3-fluoro-2-phosphonomethoxypropyl) derivatives of heterocyclic purine and pyrimidine bases that have antiviral activity.
    Type: Grant
    Filed: January 13, 1993
    Date of Patent: October 4, 1994
    Assignee: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic
    Inventors: Jindrich Jindrich, Antonin Holy
  • Patent number: 5142051
    Abstract: This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyclic bases andd their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.
    Type: Grant
    Filed: July 17, 1987
    Date of Patent: August 25, 1992
    Assignees: Ceskoslovenska Akademie Ved, Rega Institut
    Inventors: Antonin Holy, Ivan Rosenberg, Erik D. A. De Clercq
  • Patent number: 5130427
    Abstract: The invention relates to the new compound (2R)-2-[di(2-propyl)phosphonylmethoxy]-3-p-toluenesulfonyloxy-1-trimethyla cetoxypropane and the method of producing it. The compound may be used for producing (S)-N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of the heterocyclic purine and pyrimidine bases of antiviral activity.
    Type: Grant
    Filed: July 12, 1991
    Date of Patent: July 14, 1992
    Assignee: Ceskoslovenska akademie ved
    Inventors: Petr Alexander, Antonin Holy, Hana Dvorakova
  • Patent number: RE35558
    Abstract: The invention relates to the new compound (2R)-2-[di(2-propyl)phosphonylmethoxy]-3-p-toluenesulfonyloxy-1-trimethyla cetoxypropane and the method of producing it. The compound may be used for producing (S)-N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of the heterocyclic purine and pyrimidine bases of antiviral activity.
    Type: Grant
    Filed: July 14, 1994
    Date of Patent: July 8, 1997
    Assignee: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic
    Inventors: Petr Alexander, Antonin Holy, Hana Dvorakova