Patents by Inventor Erik De Clercq

Erik De Clercq 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: 20070185062
    Abstract: The present invention relates to novel phosponate nucleosides, more specifically to novel phosponalkoxy substituted nucleosides. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections.
    Type: Application
    Filed: March 4, 2005
    Publication date: August 9, 2007
    Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De clercq
  • Publication number: 20060275748
    Abstract: In a study of HIV-1 integrase (IN) complexes derived from nuclei of human cells stably expressing the viral protein from a synthetic gene it was demonstrated that in the nuclear extracts IN exists as part of a large distinct complex with apparent Stokes radius of 61 ?, which dissociates upon dilution yielding a core molecule of 41 ?. The IN complexes were isolated from cells expressing FLAG-tagged IN. By present invention it was demonstrated that the 41 ? core is tetramer of IN, whereas 61 ? molecules are composed of IN tetramers associated with a cellular protein with an apparent molecular weight of 76 kDa. This integrase interacting protein (Inip76) was found to be identical to LEDGF/DFS70/p75 a protein implicated in regulation of gene expression and cellular stress-response. HIV-1 IN and Inip76 co-localized in the nuclei of human cells stably expressing IN. Furthermore, it has been demonstrated by present invention that recombinant Inip76 strongly promoted strand-transfer activity of HIV-1 IN in vitro.
    Type: Application
    Filed: September 26, 2003
    Publication date: December 7, 2006
    Applicant: KULEUVEN RESEARCH AND DEVELOPMENT
    Inventors: Zeger Debyser, Petr Cherepanov, Erik De Clercq
  • 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: 7049332
    Abstract: An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R1 is selected from hydrogen, methyl or ethyl, R2 is selected from hydrogen, SH or —SR0 wherein R0 is methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: May 23, 2006
    Assignee: K. U. Leuven Research & Development
    Inventors: Erik De Clercq, Arthur Van Aerschot, Piet Herdewijn, Irene Lagoja, Christophe Pannecoucque
  • 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
  • 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: 20050239821
    Abstract: The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine derivative having the general formula (Z): (formula). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.
    Type: Application
    Filed: July 3, 2003
    Publication date: October 27, 2005
    Inventors: Johan Neyts, Gerhard Purstinger, Erik De Clercq
  • 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
  • Publication number: 20040122024
    Abstract: An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R1 is selected from hydrogen, methyl or ethyl, R2 is selected from hydrogen, SH or —SR0 wherein R0 is methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isoprop
    Type: Application
    Filed: February 11, 2004
    Publication date: June 24, 2004
    Inventors: Erik De Clercq, Arthur Van Aerschot, Piet Herdewijn, Irene Lagoja, Christophe Pannecoucque
  • Publication number: 20030187003
    Abstract: The invention provides the use of a pyrano[2,3-d:6,5-d′] dipyrimidine derivative for the manufacture of a medicine for the treatment of a retroviral infection in a mammal. It also provides a product containing: (a) one or more derivatives of a pyrano[2,3-d:6,5-d′] dipyrimidine; and (b) one or more anti-retroviral drugs, including drugs effective against one or more retroviral or cellular proteins involved in the entry and/or replication of a retrovirus, in respective proportions such as to provide a synergistic effect against a retroviral infection in a mammal, as a combined preparation for simultaneous, separate or sequential use in retroviral infection therapy.
    Type: Application
    Filed: February 24, 2003
    Publication date: October 2, 2003
    Inventors: Erik De Clercq, Zeger Debyser, Willem Plymers, Christophe Pannecouque, Myriam Witvrouw
  • Publication number: 20030176370
    Abstract: A compound, which can show potent anti-viral activity against, for example, cytomegalo virus, has the formula (I), wherein R is selected from the group comprising, optionally substituted, C5 to C20 alkyl and, optionally substituted, C5 to C20 cycloalkyl; 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, NH, S, N-alkyl 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, Se, 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; T is selected from the group comprising H, halogens, alkyl (C1 to C10),
    Type: Application
    Filed: November 8, 2002
    Publication date: September 18, 2003
    Inventors: Christopher McGuigan, Jan Maria Rene Balzarini, Erik De Clercq
  • 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: 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
  • Patent number: 4988678
    Abstract: The antitumor activity of 5-fluorouracil and its precursors against adenocarcinomas can be potentiated without a corresponding increase in toxicity by combining these compounds with (E)-5-(2-bromovinyl)-uracil or a precursor thereof. The combinations may have the form of a single composition or two separate compositions.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: January 29, 1991
    Assignee: Stichting Rega VZW
    Inventors: Erik De Clercq, Masaaki Iigo
  • Patent number: 4894365
    Abstract: The antitumor activity of 5-fluorouracil and its precursors against adenocarcinomas can be potentiated without a corresponding increase in toxicity by combining these compounds with (E)-5-(2-bromovinyl)-uracil or a precursor thereof. The combinations may have the form of a single composition or two separate compositions.
    Type: Grant
    Filed: February 11, 1988
    Date of Patent: January 16, 1990
    Assignee: Stichting Rega VZW
    Inventors: Erik De Clercq, Masaaki Iigo
  • Patent number: 4724233
    Abstract: The (S) and (RS) forms of certain phosphonylmethoxyalkyl adenines and their salts have an antiviral effect against several DNA viruses and can be used for the treatment of virus diseases in human and veterinary medicine.
    Type: Grant
    Filed: April 21, 1986
    Date of Patent: February 9, 1988
    Assignees: Stichting Rega VZW, Ceskoslovenska Akademie VED
    Inventors: Erik De Clercq, Antonin Holy, Ivan Rosenberg
  • Patent number: 4605658
    Abstract: Certain esters of 3-(adenin-9-yl)-2-hydroxypropanoic acid are disclosed which exhibit an improved broad spectrum antiviral activity while having a low toxicity for living cells. They can be used for treatment of virus diseases in human and veterinary practice.
    Type: Grant
    Filed: October 5, 1984
    Date of Patent: August 12, 1986
    Assignees: Ceskoslovenska Akademie Ved., Stichting Rega VZW
    Inventors: Antonin Holy, Erik de Clercq
  • Patent number: 4382925
    Abstract: The invention relates to E-5-(2-halogenovinyl)-2'-deoxycytidines, e.g. E-5-(bromovinyl)-2'-deoxycytidine and E-5-(2-iodovinyl)-2'-deoxycytidine. These substances are endowed with specific antiviral activities towards herpes simplex virus and with an extremely low toxicity which makes them useful in antiviral medicines and for treatment of virus diseases in man and animal. They may be synthesized by introduction of an E-5-(2-halogenovinyl) sidechain into 2'-deoxycytidine, or by condensation of a trialkylsilyl derivative of E-5-(2-halogenovinyl)-cytosine with a hydroxyl-protected reactive derivative of 2'-deoxy-D-erythro-pentofuranose.
    Type: Grant
    Filed: October 2, 1980
    Date of Patent: May 10, 1983
    Assignees: The University of Birmingham, Stichting Rega V.Z.W.
    Inventors: Erik de Clercq, Gabriel A. Verhelst, Albert S. Jones, Richard T. Walker