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: 20110015147
    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: September 24, 2010
    Publication date: January 20, 2011
    Inventors: Christopher MCGUIGAN, Jan BALZARINI
  • Patent number: 7820631
    Abstract: A nucleoside analogue compound is provided which has a six-membered aromatic ring system, the aromatic ring system being substituted in the para position with an unbranched unsubstituted alkyl or alkoxy moiety, wherein the alkyl or alkoxy moiety, in total, has from 3 to 8 carbon atoms. This compound shows anti-vira1 activity, for example with respect to varicella zoster virus and can thus be used in therapeutic methods for the prophylaxis and treatment of viral infections such as varicella zoster virus.
    Type: Grant
    Filed: April 12, 2001
    Date of Patent: October 26, 2010
    Assignees: Rega Foundation, University College Cardiff Consultants Limited
    Inventors: Christopher McGuigan, Jan Balzarini
  • Publication number: 20100256087
    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: August 27, 2008
    Publication date: October 7, 2010
    Inventors: Jan Balzarini, Maria Jose Camarasa, Sonsoles Velazquez
  • Publication number: 20100222295
    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: Application
    Filed: May 9, 2007
    Publication date: September 2, 2010
    Inventors: Christopher McGuigan, Jan Balzarini, Marco Migliore
  • Publication number: 20100099869
    Abstract: This invention relates to a purine or pyrimidine phosphonate compound of formula (I) or pharmaceutically acceptable salt thereof; wherein B, X, and R1-R3 are as defined in classes and subclasses herein. These compounds may be used as antiviral precursors. The invention also relates to therapeutic compositions of these compounds and their use for the preparation of a medication for testing and/or preventing a viral infection in a patient. The invention also provides methods for making these compounds. In particular, the invention provides an H-phosphinate precursor intermediate of formula (II) wherein B is a purine or pyrimidine base as defined herein and R1 is selected from the group comprising a hydrogen atom, and a methyl, ethyl, hydroxymethyl, hydroxyethyl and C1-6haloalkyl group.
    Type: Application
    Filed: November 8, 2007
    Publication date: April 22, 2010
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE-CNRS, UNIVERSITE DE LA MEDITERRANEE, K.U. LEUVEN RESEARCH & DEVELOPMENT
    Inventors: Bruno Canard, Karine Alvarez, Karine Barral, Jean-Louis Romette, Johan Neyts, Jan Balzarini
  • Publication number: 20100075917
    Abstract: The invention relates to a pharmaceutical composition containing as an active ingredient at least one compound selected from the compounds of the formula (II), in which the S atom is bonded to the nucleoside carbon at T or to the nucleoside carbon at 3?, and from the compounds of the following formula (III): formulae in which B is a nucleotide natural or modified base, x is 0, 1 or 2, and R1 and R represent a carbonated group or a molecular hydrocarbon remnant that can be substituted and/or interrupted by one or more atoms and/or by one or more groups containing one or more atoms, said atoms being selected from N, O, P, S, Si, X where X is halogen. The invention also relates to pharmaceutically acceptable carrier.
    Type: Application
    Filed: October 29, 2007
    Publication date: March 25, 2010
    Applicant: UNIVERSITE JOSEPH FOURIER (GRENOBLE 1)
    Inventors: Jean-Luc Decout, Beatrice Gerland, Jerome Desire, Michel Lepoivre, Jan Balzarini
  • Publication number: 20090042793
    Abstract: The field of the invention relates to the use of carbohydrate binding compounds as a medicine, their use to treat or prevent viral infections, their use to manufacture a medicine to treat or prevent viral infections and their use in a vaccination strategy. The present invention relates to the use of said compounds to manufacture a medicine to treat or prevent viral infections of subjects, more in particular infections with viruses having glycosilated envelop proteins such as Retroviridae (i.e. Lentivirinae), like HIV (human immunodeficiency virus), Flaviviridae, like HCV (hepatitis C virus), Hepadnaviridae, like HBV (hepatitis B virus), Coronaviridae, like SARS corona virus, and Orthomyxoviridae, like influenza A, B or C.
    Type: Application
    Filed: September 21, 2006
    Publication date: February 12, 2009
    Inventor: Jan Balzarini
  • Publication number: 20080214648
    Abstract: The present invention provides new prodrugs which are conjugates of a therapeutic compound and a peptide wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV).
    Type: Application
    Filed: May 10, 2004
    Publication date: September 4, 2008
    Inventors: Herman Augustinus De Kock, Piet Tom Bert Paul Wigerinck, Jan Balzarini
  • Publication number: 20080076824
    Abstract: The present invention relates to the discovery of a novel class of compounds that inhibit the replication of human immunodeficiency virus (HIV) and approaches to identify these compounds. More specifically, it has been found that enzymatically prepared alpha-hydroxyglycinamide and synthetically prepared alpha-hydroxyglycinamide inhibit the replication of HIV in human serum. Embodiments include methods to identify modified glycinamide compounds that inhibit HUV, methods to isolate and synthesize modified glycinamide compounds, and therapeutic compositions comprising these compounds.
    Type: Application
    Filed: August 16, 2005
    Publication date: March 27, 2008
    Inventors: Jan Balzarini, Anders Vahlne, Marita Hogberg, Weimin Tong
  • Publication number: 20070275900
    Abstract: The present invention provides a new prodrug technology and new prodrugs in order to increase the solubility, to modulate plasma protein binding or to enhance the biovailability of a drug. In the present invention the prodrugs are conjugates of a therapeutic compound and a peptide (eg tetrapeptide or hexapeptide) wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV). The present invention furthermore provides a method of producing said prodrugs, to enhance brain and lymphatic delivery of drugs and/or to extend drug half-lives in plasma.
    Type: Application
    Filed: May 10, 2004
    Publication date: November 29, 2007
    Inventor: Jan Balzarini
  • Publication number: 20070191373
    Abstract: 6-substituted-3-substituted-3H-furo[2,3-d]pyrimidin-2-one and 6-substituted-2-substituted-furo[2,3-d]pyrimidine novel compounds are useful in the treatment of viral infection, in particular cytomegalovirus viral infection. The substituents are independently selected from alkyl, aryl, alkenyl and alkynyl. The preferred substituent at the 6 position is alkyl.
    Type: Application
    Filed: April 21, 2004
    Publication date: August 16, 2007
    Inventors: Christopher McGuigan, Jan Balzarini, Erik De Clerq
  • 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: 7125853
    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: Grant
    Filed: December 22, 2003
    Date of Patent: October 24, 2006
    Assignee: Kemin Pharma B.V.B.A.
    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: 7049303
    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: Grant
    Filed: July 30, 2002
    Date of Patent: May 23, 2006
    Assignee: Medical Research Council
    Inventors: David Loakes, Daniel M. Brown, Kazuo Negishi, Kei Moriyama, Jan Balzarini
  • Patent number: 7019135
    Abstract: Compounds of the general formula (I) are described wherein R, R?, R?, Q, T, T?, T?, T??, W, X, and Z are as defined in the specification. Compounds according to the invention preferably display potent anti-viral activity against, for example, cytomegalo virus.
    Type: Grant
    Filed: May 8, 2001
    Date of Patent: March 28, 2006
    Assignees: University College Cardiff Consultants Limited, Rega Foundation
    Inventors: Christopher McGuigan, Jan Balzarini, Erik De Clercq
  • Patent number: 7018989
    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. Particularly preferred are thymine and adenine derivatives of amino acid phenoxyphosphoroamidates.
    Type: Grant
    Filed: August 12, 2002
    Date of Patent: March 28, 2006
    Assignee: University College Cardiff Consultants, LTD
    Inventors: Christopher McGuigan, Jan Balzarini
  • Publication number: 20050250677
    Abstract: Novel glycopeptide antibiotic derivatives, processes for their preparation, their use as a medicine, their use to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections are provided. The present invention relates to the use of glycopeptide antibiotics and their semisynthetic derivatives to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections of subjects, more in particular infections with viruses belonging to Retroviridae, Herpes viridae, Flaviviridae and the Coronaviridae, like HIV (human immunodeficiency virus), HCV (hepatitis C virus), BVDV (bovine viral diarrhoea virus), SARS (severe acute respiratory syndrome) causing virus, FCV (feline coronavirus), HSV (herpes simplex virus), VZV (varicella zoster virus) and CMV (cytomegalovirus).
    Type: Application
    Filed: September 1, 2003
    Publication date: November 10, 2005
    Inventors: Jan Balzarini, Maria Preobrazhenskaya, Erik De Clercq
  • Publication number: 20050096319
    Abstract: The present invention relates to the discovery of a novel class of compounds that inhibit the replication of human immunodeficiency virus (HIV) and approaches to identify these compounds. More specifically, it has been found that enzymatically prepared alpha-hydroxyglycinamide and synthetically prepared alpha-hydroxyglycinamide inhibit the replication of HIV in human serum. Embodiments include methods to identify modified glycinamide compounds that inhibit HIV, methods to isolate and synthesize modified glycinamide compounds, and therapeutic compositions comprising these compounds.
    Type: Application
    Filed: August 18, 2004
    Publication date: May 5, 2005
    Inventors: Jan Balzarini, Anders Vahlne, Marita Hogberg, Weimin Tong
  • 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: 20050043268
    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: May 7, 2004
    Publication date: February 24, 2005
    Inventors: David Loakes, Daniel Brown, Kazuo Negishi, Kei Moriyama, Jan Balzarini, Craig Cameron, Jamie Arnold, Christian Castro, Victoria Korneeva, Jason Graci