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).

  • Patent number: 10993957
    Abstract: Phosphoramidate derivates of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
    Type: Grant
    Filed: June 28, 2018
    Date of Patent: May 4, 2021
    Assignee: NuCana plc
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Patent number: 10610538
    Abstract: The present invention relates to a class of novel pradimicins and analogues and derivatives thereof, including the compounds of formula A, I and 111, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof and their use to treat or prevent kinetoplastid infections and their use to manufacture a medicine to treat or prevent kinetoplastid infections, particularly infections with trypanosoma and leishmania, such as Trypanosoma brucei, Trypanosoma cruzi and Leischmania donovani. wherein Ra, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the claim 1 or as described in detail in the description of the invention. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent kinetoplastid infections.
    Type: Grant
    Filed: October 10, 2013
    Date of Patent: April 7, 2020
    Assignees: Katholieke Universiteit Leuven, Consejo Superior de Investigaciones Científicas - CSIC
    Inventors: Jan Balzarini, Dolores González Pacanowska, Luis Miguel Ruiz Pérez, Victor Castillo Acosta, Yasuhiro Igarashi
  • Publication number: 20190201432
    Abstract: Phosphoramidate derivates of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
    Type: Application
    Filed: June 28, 2018
    Publication date: July 4, 2019
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Patent number: 10167302
    Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, and their use in medicine particular as anti-viral agents; wherein: X is selected from O and NR11; Y is selected from O, S and NR12; A is selected from —(CR1R2)n-, —(CR9R10)—, —(CR9R10)—(CR1R2)n-, —(CR1R3)—(CR2R4)—(CR1R2)n-, —CR3?CR4—(CR1R2)n- and —C?C—(CR1R2)n-; R1 and R2 are independently selected from H, alkyl, hydroxyl, hydroxymethyl and halogen; R3 and R4 are independently selected from H and alkyl, or R3 and R4 together with the carbon atoms to which they are attached form a mono or bicyclic ring system selected from cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl and heteroaryl; R5 is selected from H, P(?O)(OH)2 and P(?O)(OH)—O—P(?O)(OH)2; R6 is selected from H and alkyl; R7 and R8 are independently selected from H, alkyl, halogen and hydroxymethyl R9 and R19 together with the carbon atoms to which they are attached form a mono or bicyclic ring system selected
    Type: Grant
    Filed: May 20, 2015
    Date of Patent: January 1, 2019
    Assignees: UNIVERSITY COLLEGE CORK, KATHOLIEKE UNIVERSITEIT LEUVEN
    Inventors: Anita Maguire, Alan Ford, Jan Balzarini, Wim Dehaen
  • Patent number: 10022390
    Abstract: Phosphoramidate derivates of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: July 17, 2018
    Assignee: NuCana plc
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Patent number: 9822137
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, wherein the groups are as defined in the claims. Further aspects of the invention relate to pharmaceutical compositions comprising compounds of formula (I), and the use of compounds of formula (I) in the preparation of a medicament for treating a viral disorder.
    Type: Grant
    Filed: November 20, 2013
    Date of Patent: November 21, 2017
    Assignees: UNIVERSITY COLLEGE CORK, KATHOLIEKE UNIVERSITEIT LEUVEN
    Inventors: Wim Dehaen, Jan Balzarini, Anita Maguire, Sarah Jane Keane, Alan Ford, Nuala Maguire, Nicholas D. Mullins
  • Publication number: 20170312302
    Abstract: Phosphoramidate derivates of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
    Type: Application
    Filed: April 18, 2017
    Publication date: November 2, 2017
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Publication number: 20170218001
    Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, and their use in medicine particular as anti-viral agents; wherein: X is selected from O and NR11; Y is selected from O, S and NR12; A is selected from —(CR1R2)n-, —(CR9R10)—, —(CR9R10)—(CR1R2)n-, —(CR1R3)—(CR2R4)—(CR1R2)n-, —CR3?CR4—(CR1R2)n- and —C?C—(CR1R2)n-; R1 and R2 are independently selected from H, alkyl, hydroxyl, hydroxymethyl and halogen; R3 and R4 are independently selected from H and alkyl, or R3 and R4 together with the carbon atoms to which they are attached form a mono or bicyclic ring system selected from cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl and heteroaryl; R5 is selected from H, P(?O)(OH)2 and P(?O)(OH)—O—P(?O)(OH)2; R6 is selected from H and alkyl; R7 and R8 are independently selected from H, alkyl, halogen and hydroxymethyl R9 and R19 together with the carbon atoms to which they are attached form a mono or bicyclic ring system selected
    Type: Application
    Filed: May 22, 2015
    Publication date: August 3, 2017
    Inventors: Anita MAGUIRE, Alan Ford, Jan BALZARINI, Wim DEHAEN
  • Patent number: 9655915
    Abstract: Phosphoramidate derivatives of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
    Type: Grant
    Filed: November 17, 2015
    Date of Patent: May 23, 2017
    Assignee: NuCana BioMed Limited
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Patent number: 9427447
    Abstract: A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH2, Y is O, S or NH, Z is O, S or CH2, R1 is C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl, and one of R2 and R3 is OH, and the other of R3 and R2 is a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety R2 or R3 may be (IV): in which R4, R5, R6 and R7 are each independently H or C1-2 alkyl. In preferred embodiments, one of R2 or R3 is valine, leucine, isoleucine or alanine, particularly valine.
    Type: Grant
    Filed: September 10, 2014
    Date of Patent: August 30, 2016
    Assignees: University College Cardiff Consultants Limited, K.U. Leuven Research and Development
    Inventors: Christopher McGuigan, Jan Balzarini, Marco Migliore
  • Publication number: 20160243140
    Abstract: The present invention relates to a class of novel pradimicins and analogues and derivatives thereof, including the compounds of formula A, I and 111, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof and their use to treat or prevent kinetoplastid infections and their use to manufacture a medicine to treat or prevent kinetoplastid infections, particularly infections with trypanosoma and leishmania, such as Trypanosoma brucei, Trypanosoma cruzi and Leischmania donovani. wherein Ra, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the claim 1 or as described in detail in the description of the invention. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent kinetoplastid infections.
    Type: Application
    Filed: October 10, 2013
    Publication date: August 25, 2016
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN, CONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICAS - CSIC
    Inventors: Jan Balzarini, Dolores González Pacanowska, Luis Miguel Rui Pérez, Victor Castillo Acosta, Yasuhiro Igarashi
  • Publication number: 20160244476
    Abstract: A compound of formula (I) wherein Ar can be one six-membered or two fused six-membered aromatic rings; R8 and R9 can be hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, or aryl; Q can be O, S or CY2, where Y may be H, alkyl or halogens; X can be O, NH, S, N-alkyl, (CHR2)m where m is 1 to 10, and CY2; Z can be O, S, NH, or N-alkyl; U? is H and U? can be H or CH2; wherein: T can be OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2 or N3; T? and T? can be H or halogen; and W can be H or a phosphate group. Compounds show anti-viral activity, for example with respect to varicella zoster virus.
    Type: Application
    Filed: April 29, 2016
    Publication date: August 25, 2016
    Inventors: Christopher McGuigan, Jan Balzarini
  • Publication number: 20160166596
    Abstract: Phosphoramidate derivatives of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
    Type: Application
    Filed: November 17, 2015
    Publication date: June 16, 2016
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Patent number: 9351970
    Abstract: A compound of formula (I) wherein Ar can be one six-membered or two fused six-membered aromatic rings; R8 and R9 can be hydrogen, alkyl, cycloalkyl, halogen, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, or aryl; Q can be O, S or CY2, where Y may be H, alkyl or halogen; X can be O, NH, S, N-alkyl, (CHR2)m where m is 1 to 10, and CY2; Z can be O, S, NH, or N-alkyl; U? is H and U? can be H or CH2; wherein: T can be OH, H, halogen, O-alkyl, O-acyl, O-aryl, CN, NH2 or N3; T? and T? can be H or halogen; and W can be H or a phosphate group. Compounds show anti-viral activity, for example with respect to varicella zoster virus.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: May 31, 2016
    Assignees: Rega Foundation, University College Cardiff Consultants Limited
    Inventors: Christopher McGuigan, Jan Balzarini
  • Patent number: 9278958
    Abstract: The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R0, R1, R2, A, and X have defined meanings as described in claim 1.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: March 8, 2016
    Assignees: Katholieke Universiteit Leuven K.U. Leuven R&D, Universita Degli Studi Di Ferrara
    Inventors: Jan Balzarini, Wim Dehaen, Joice Thomas, Sandra Liekens, Romeo Romagnoli, Pier Giovanni Baraldi
  • Patent number: 9221866
    Abstract: Phosphoramidate derivatives of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: December 29, 2015
    Assignee: NuCana Biomed Limited
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Publication number: 20150291640
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, wherein the groups are as defined in the claims. Further aspects of the invention relate to pharmaceutical compositions comprising compounds of formula (I), and the use of compounds of formula (I) in the preparation of a medicament for treating a viral disorder.
    Type: Application
    Filed: November 20, 2013
    Publication date: October 15, 2015
    Inventors: Wim Dehaen, Jan Balzarini, Anita Maguire, Sarah Jane Keane, Alan Ford, Nuala Maguire, Nicholas D. Mullins
  • Publication number: 20150183817
    Abstract: Phosphoramidate derivatives of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
    Type: Application
    Filed: December 4, 2014
    Publication date: July 2, 2015
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Publication number: 20150126559
    Abstract: The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R0, R1, R2, A, and X have defined meanings as described in claim 1.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 7, 2015
    Applicant: UNIVERSITA DEGLI STUDI DI FERRARA
    Inventors: Jan Balzarini, Wim Dehaen, Joice Thomas, Sandra Liekens, Romeo Romagnoli, Pier Giovanni Baraldi
  • Publication number: 20150080318
    Abstract: A compound of the general formula (III): wherein X is O, S, NH or CH2; Y is O, S or NH; Z is O, S or CH2; R1 is C1-8 alkyl, especially C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl; at least one of R2 and R3 is H—[R4-R5]n—R6—, in which: H—[R4-R5]n— comprises an oligopeptide, R4 being an amino acid and R5 being an amino acid selected from proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine, R6 is a neutral, non-polar amino acid moiety that is bonded to R5 by a peptide bond, and n is 1, 2, 3, 4 or 5; and the other of R3 and R2 is H—[R4-R5]n—R6— or H; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 19, 2014
    Publication date: March 19, 2015
    Inventors: Jan Balzarini, Maria Jose Camarasa, Sonsoles Velazquez