Patents by Inventor Jan Balzarini

Jan Balzarini 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: 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
  • Publication number: 20040209823
    Abstract: We describe the use of bicyclic carbohydrates for the treatment of hepatitis C virus infections. Different bicyclic carbohydrates were tested in vitro against DNA-viruses, retro-viruses and Flaviviridae sp., an important family of human and animal RNA pathogens. Significant activity was observed against the bovine viral diarrhea virus (BVDV). As pestiviruses, such as BVDV, share many similarities with hepatitis C virus (HCV), the bicyclic carbohydrates in general and the preferred bicyclic carbohydrates more specifically are expected to be a treatment for hepatitis C viral infections.
    Type: Application
    Filed: December 22, 2003
    Publication date: October 21, 2004
    Inventors: Benedikt Sas, Johan Van Hemel, Jan Vandenkerckhove, Eric Peys, Johan Van der Eycken, Bart Ruttens, Jan Balzarini, Eric De Clercq, Johan Neyts
  • Patent number: 6638919
    Abstract: Compounds of the formula wherein Ar is aryl, R1 and R2 are hydrogen alkyl, alkyl substituted with phenyl, and aryl, O, NH, NR4 and S, R5 is hydrogen, alkyl or aryl or alkylene when taken with R1, and R3 is hydrogen, alkyl, alkyl substituted with phenyl, aryl, a heterocyclic group or a polycyclic group, are antiviral agents. A typical embodiment is (1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol O-[phenyl-(methoxy-L-alaninyl)]phosphate.
    Type: Grant
    Filed: March 27, 2001
    Date of Patent: October 28, 2003
    Assignees: University College Cardiff Consultants Limited, Rega Foundation
    Inventors: Christopher McGuigan, Jan Balzarini
  • Publication number: 20030148967
    Abstract: A compound having the formula (I) wherein Ar is an, optionally substituted, aromatic ring system, the aromatic ring system comprising one six-membered aromatic ring or two fused six-membered aromatic rings; R8 and R9 are each independently selected form the group comprising hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, aryl; Q is selected from the group comprising O, S and CY2, where Y may be the same or different and is selected from H, alkyl and halogens; X is selected from the group comprising O, NH, S, N-alkyl, (CH2)m where m is 1 to 10, and CY2 where Y may be the same or different and is selected from hydrogen, alkyl and halogens; Z is selected from the group comprising O, S, NH, and N-alkyl; U″ is H and U′ is selected from H and CH2T, or U′ and U″ are joined so as to form a ring moiety including Q wherein U′—U″ together is respectively selected from the group comprising &mdash
    Type: Application
    Filed: October 17, 2002
    Publication date: August 7, 2003
    Inventors: Christopher McGuigan, Jan Balzarini
  • Publication number: 20030130226
    Abstract: Disclosed is a pharmaceutical composition comprising a ribonucleoside analogue in accordance with general formula I or II as herein defined, in admixture with a physiologically acceptable excipient diluent or carrier.
    Type: Application
    Filed: July 30, 2002
    Publication date: July 10, 2003
    Applicant: Medical Research Council
    Inventors: David Loakes, Daniel M. Brown, Kazuo Negishi, Kei Moriyama, Jan Balzarini
  • Publication number: 20030120071
    Abstract: Aryl substituted phosphoryl derivatives of the formula 1
    Type: Application
    Filed: August 12, 2002
    Publication date: June 26, 2003
    Inventors: Christopher McGuigan, Jan Balzarini
  • Patent number: 6573247
    Abstract: A compound having formula (I), wherein R is selected from the group comprising C5 to C20 alkyl, C5 to C20 cycloalkyl, halogens, aryl and alkylaryl; R′ is selected from the group comprising hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, alkyl; R″ is selected from the group comprising hydrogen, alkyl, cycloalkyl, halogens, alkyloxy, aryloxy and aryl; Q is selected from the group comprising O, S and CY2, where Y may be the same or different and is selected from H, alkyl and halogens; X is selected from the group comprising O, NH, S, N-alkyl, (CH2)n where n is 1 to 10, and CY2 where Y may be the same or different and is selected from hydrogen, alkyl and halogens; Z is selected from the group comprising O, S, NH, and N alkyl; U″ is H and U′ is selected from H and CH2T, or U′ and U″ are joined so as to form a ring moiety including Q wherein U′-U″ together is respectively selected fro
    Type: Grant
    Filed: January 6, 2000
    Date of Patent: June 3, 2003
    Assignees: University College Cardiff Consultants Limited, Rega Foundation
    Inventors: Christopher McGuigan, Christopher Yarnold, Garry Jones, Jan Balzarini, Erik De Clercq
  • Patent number: 6455513
    Abstract: Aryl substituted phosphoryl derivatives of the formula In which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X1 is O, NR3, S, CR3R4, CR3W1 or CW1W2, X2 and X6 are a bond or X6 is CH2 and X2 is O, NR3, S, CR3R4, CR3W1 or CW1W2, R3 and R4 are H, alkyl or phenyl, groups, W1 and W2 are heteroatoms, X3 is alkylene, X4 is oxygen or CH2, X5 is a bond or CH2, Z is O, NR5, S, alkyl or phenyl, R5 is H, alkyl or phenyl, J is H, alkyl, phenyl, or a heterocyclic or polycyclic group, Q is O, NR6, S, CR6R7, CR6W3 or CW3W4, R6 and R7 are H, alkyl, or phenyl, and W3 and W4 are hetero atoms, T1 and T2 are H or CH2R8, R8 is H, OH or F, or T1 and T2 together are —CH═CH— or —C(R9)(R10)C(R11)(R12)—, R9 is H, halogeno, CN, NH2, CO-alkyl, or alkyl, R10, R11, and R12 are H, N3, halogen, CN, NH2, CO-alkyl, or alkyl, and B is a purine or pyrimidine base, have antiviral activity, as for example against HIV.
    Type: Grant
    Filed: August 24, 1999
    Date of Patent: September 24, 2002
    Assignees: University College Cardiff Consultants Ltd., Rega Foundation
    Inventors: Christopher McGuigan, Jan Balzarini
  • Publication number: 20010031745
    Abstract: Chemical compounds comprising nucleoside phosphoramides, their preparation and their therapeutic use in treating viral infections, particularly HIV and HBV are disclosed. The compounds contain a substituted adenine analogue moiety comprising 2-amino-6-(cyclopropylamino)-9H-purin-9-yl. The compounds show both anti-viral activity and acid stability. Salts and esters of the phosphoramidates are included. A representative compound is (1S, 4R), -4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol1 O-[phenyl-(methoxy-L-alaninyl)]-phosphate.
    Type: Application
    Filed: March 27, 2001
    Publication date: October 18, 2001
    Inventors: Christopher McGuigan, Jan Balzarini
  • 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: 5596018
    Abstract: An antiviral agent against viruses causative of AIDS, containing fuchsinic acid as an active ingredient.The antiviral agents provided by the present invention inhibit cellular infection by AIDS-causing virus and progress of the infection into ARC and are effective in the treatment of AIDS.
    Type: Grant
    Filed: August 20, 1993
    Date of Patent: January 21, 1997
    Assignee: Toray Industries, Inc.
    Inventors: Masanori Baba, Dominique Schols, Rudi Pauwels, Jan Balzarini, Erik De Clercq