Patents by Inventor Erik D. A. De Clercq

Erik D. A. 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).

  • 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
  • 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
  • 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: 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: 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: 5607922
    Abstract: 1,5-Anhydrohexitol nucleoside analogues represented by the general formula I: ##STR1## wherein the hexitol has the D-configuration and the carbon atom on which the base moiety and the X substituent stand both have the (S)-configuration and further wherein:B is a heterocyclic ring selected from the group consisting of pyrimidine and purine bases; andX is hydrogen, azido, F, Cl, Br, I, amino, --NHR.sup.2, --N(R.sup.2).sub.2, --OR.sup.2, --SR.sup.2, or CN; wherein R.sup.1 and R.sup.2 are the same or different and are selected from the group consisting of hydrogen, substituted or unsubstituted C.sub.1 -C.sub.20 alkyl, substituted or unsubstituted C.sub.1 -C.sub.20 alkenyl, aroyl, C.sub.1 -C.sub.20 alkanoyl, and phosphoryl.These nucleoside analogues are useful as antiviral agents against herpes simplex virus, vaccina virus, or varicella zoster virus. The definition of the X group should include --N(R.sup.2).sub.2 instead of --N(N.sup.2).sub.2.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: March 4, 1997
    Assignee: Stichting Rega VZW
    Inventors: Erik D. A. De Clercq, Piet A. M. Herdewijn, Arthur A. E. Van Aerschot
  • Patent number: 5461060
    Abstract: The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I'] and having antiviral activity, particularly antiretroviral activity such as anti-HIV activity: ##STR1## and pharmaceutical compositions having antiviral activity and comprising the above-described derivative(s) as an active ingredient.
    Type: Grant
    Filed: September 3, 1993
    Date of Patent: October 24, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik D. A. De Clercq, Masanori Baba, Richard T. Walker, Masaru Ubasawa
  • Patent number: 5318972
    Abstract: A pyrimidine nucleoside derivative and pharmaceutically acceptable salt thereof specified by the presence of ethyl group or isopropyl group at 5-position of the pyrimidine ring and the presence of a (substituted) phenylthio or a (substituted) benzyl group at 6-position of the pyrimidine ring is provided. The pyrimidine nucleoside derivative and pharmaceutically acceptable salt thereof show a markedly higher anti-retroviral activity than conventional analogous compounds and have a relatively low toxicity against the host cells, and therefore, are useful as an active ingredient of antiviral agent.
    Type: Grant
    Filed: March 28, 1991
    Date of Patent: June 7, 1994
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik D. A. De Clercq, Masanori Baba, Richard T. Walker, Masaru Ubasawa
  • Patent number: 5292505
    Abstract: Sulphated vinyl polymers such as sulphated polyvinylalcohol, sulphated copolymers of (meth)acrylic acid and vinylalcohol, and pharmaceutically acceptable salts thereof, have an antiviral effect against human immunodeficiency virus and may therefore be used as a therapeutic agent for treating retrovirus infections like AIDS and AIDS-related diseases. Their antiviral activity is apparently based on inhibition of virus adsorption; their inhibitory effect on giant cell formation is stronger than that of dextran sulphate.
    Type: Grant
    Filed: January 15, 1992
    Date of Patent: March 8, 1994
    Assignees: Stichting Rega VZW, Richter Gedeon Vegyeszeti Gyar RT
    Inventors: Masanori Baba, Erik D. A. De Clercq, Sandor Gorog, Miklos Low, Miklos Nagy, Sandorne Gyorgyi
  • Patent number: 5152978
    Abstract: Sulphated vinyl polymers such as sulphated polyvinylalcohol, sulphated copolymers of (meth)acrylic acid and vinylalcohol, and pharmaceutically acceptable salts thereof, have an antiviral effect against human immunodeficiency virus and may therefore be used as a therapeutic agent for treating retrovirus infections like AIDS and AIDS-related diseases. Their antiviral activity is apparently based on inhibition of virus adsorption; their inhibitory effect on giant cell formation is stronger than that of dextran sulphate.
    Type: Grant
    Filed: February 23, 1989
    Date of Patent: October 6, 1992
    Assignees: Stichting Rega VZW, Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Masanori Baba, Erik D. A. De Clercq, Sandor Gorog, Miklos Low, Miklos Nagy, Sandorne Gyorgyi
  • 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: 5137724
    Abstract: The antiviral activity of 5-fluoro-uracil, 5-fluoro-2'-deoxyuridine and similar thymilydate synthetase inhibitors towards herpes viruses can be potentiated dramatically by combining these compounds with compounds having viral thymidine kinase inhibiting activity.
    Type: Grant
    Filed: July 22, 1991
    Date of Patent: August 11, 1992
    Assignee: Stichting Rega VZW
    Inventors: Jan M. R. Balzarini, Erik D. A. De Clercq
  • Patent number: 5116822
    Abstract: The compound 2',3'-dideoxycytidinene has an antiviral effect against human immunodeficiency virus (HIV) and may therefore be used as a therapeutic agent for treating AIDS and related diseases.
    Type: Grant
    Filed: July 2, 1990
    Date of Patent: May 26, 1992
    Assignees: Stichting Rega VZW, The United States of America as represented by the Department of Health and Human Serices
    Inventors: Erik D. A. De Clercq, Piet A. M. M. Herdewijn, Samuel Broder, Jan M. R. Balzarini
  • Patent number: 5112835
    Abstract: 6-substitutted acyclopyrimidine nucleoside derivatives represented by the following general formula I: ##STR1## wherein R.sup.1 represents a hydrogen or halogen atom or a group of alkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl; R.sup.2 represents a group of arylthio, alkylthio, cycloalkylthio, aryl sulfoxide, alkyl sulfoxide, cycloalkyl sulfoxide, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy; R.sup.3 represents a hydroxyalkyl group of which alkyl portion may contain an oxygen atom; X represents an oxygen or sulfur atom or amino group; Y represents an oxygen or sulfur atom; and A represents .dbd.N-- or --NH-- or pharmaceutically acceptable salts thereof, processes for their preparation and antiviral agents containing them as active ingredients.
    Type: Grant
    Filed: November 21, 1989
    Date of Patent: May 12, 1992
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik D. A. De Clercq, Masanori Baba, Richard T. Walker, Masaru Ubasawa
  • Patent number: 4963533
    Abstract: The present invention relates to a composition containing the compound 2', 3'-dideoxycytidinene which has an antiviral effect against human immunodeficiency virus (HIV) and may therefore be used as a therapeutic agent for the treatment of AIDS and AIDS related diseases.
    Type: Grant
    Filed: October 24, 1986
    Date of Patent: October 16, 1990
    Assignees: Stichting Rega VZW (REGA), The Government of the United States of America
    Inventors: Erik D. A. de Clercq, Piet A. M. M. Herdewijn, Samuel Broder, Jan M. R. Balzarini
  • Patent number: 4548819
    Abstract: Compounds of the general formula ##STR1## (wherein X represents an oxygen or sulphur atom, R.sup.1 represents a hydroxy or amino group, R.sup.2 represents a hydrogen atom or a group of formula --CH.sub.2 OR.sup.3.sub.a and R.sup.3 and R.sup.3.sub.a which may be the same or different, each represents an amino acid acyl radical) and physiologically acceptable salts thereof are useful for the treatment of viral infections and have been found to have a surprisingly high water-solubility which renders them of value in the formulation of aqueous pharmaceutical preparations. Processes for preparing the compounds are described.
    Type: Grant
    Filed: June 23, 1983
    Date of Patent: October 22, 1985
    Inventors: Erik D. A. De Clercq, Hubert J. H. E. Vander Haeghe, Roger H. C. Busson
  • Patent number: 4424211
    Abstract: The novel substance E-5-(2-bromovinyl)-2'-deoxyuridine and its corresponding iodovinyl derivative are gifted with specific antiviral activities towards herpes simplex virus. They may be synthesized by a condensation reaction followed by separation of anomers.
    Type: Grant
    Filed: December 21, 1981
    Date of Patent: January 3, 1984
    Assignees: Rega Instituut VZW, University of Birmingham
    Inventors: Albert S. Jones, Richard T. Walker, Erik D. A. de Clercq, Philip J. Barr