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).
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Patent number: 7115592Abstract: 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: GrantFiled: June 16, 2004Date of Patent: October 3, 2006Assignees: Institute of Organic Chemistry, Biochemistry of the Academy of Sciences of the Czech RepublicInventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy, Dana Hockova
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Patent number: 6818633Abstract: 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: GrantFiled: June 28, 2002Date of Patent: November 16, 2004Assignees: 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
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Publication number: 20030109499Abstract: Novel compounds are provided having formula (I) 1Type: ApplicationFiled: June 28, 2002Publication date: June 12, 2003Applicant: INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ACADEMY OF SCIENCESInventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy
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Patent number: 5869467Abstract: 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: GrantFiled: March 28, 1995Date of Patent: February 9, 1999Assignees: 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
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Patent number: 5641763Abstract: 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: GrantFiled: October 11, 1994Date of Patent: June 24, 1997Assignees: 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
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Patent number: 5607922Abstract: 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: GrantFiled: December 17, 1993Date of Patent: March 4, 1997Assignee: Stichting Rega VZWInventors: Erik D. A. De Clercq, Piet A. M. Herdewijn, Arthur A. E. Van Aerschot
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Patent number: 5461060Abstract: 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: GrantFiled: September 3, 1993Date of Patent: October 24, 1995Assignee: Mitsubishi Kasei CorporationInventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik D. A. De Clercq, Masanori Baba, Richard T. Walker, Masaru Ubasawa
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Patent number: 5318972Abstract: 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: GrantFiled: March 28, 1991Date of Patent: June 7, 1994Assignee: Mitsubishi Kasei CorporationInventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik D. A. De Clercq, Masanori Baba, Richard T. Walker, Masaru Ubasawa
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Patent number: 5292505Abstract: 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: GrantFiled: January 15, 1992Date of Patent: March 8, 1994Assignees: Stichting Rega VZW, Richter Gedeon Vegyeszeti Gyar RTInventors: Masanori Baba, Erik D. A. De Clercq, Sandor Gorog, Miklos Low, Miklos Nagy, Sandorne Gyorgyi
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Patent number: 5152978Abstract: 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: GrantFiled: February 23, 1989Date of Patent: October 6, 1992Assignees: 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
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Patent number: 5142051Abstract: 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: GrantFiled: July 17, 1987Date of Patent: August 25, 1992Assignees: Ceskoslovenska Akademie Ved, Rega InstitutInventors: Antonin Holy, Ivan Rosenberg, Erik D. A. De Clercq
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Patent number: 5137724Abstract: 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: GrantFiled: July 22, 1991Date of Patent: August 11, 1992Assignee: Stichting Rega VZWInventors: Jan M. R. Balzarini, Erik D. A. De Clercq
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Patent number: 5116822Abstract: 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: GrantFiled: July 2, 1990Date of Patent: May 26, 1992Assignees: Stichting Rega VZW, The United States of America as represented by the Department of Health and Human SericesInventors: Erik D. A. De Clercq, Piet A. M. M. Herdewijn, Samuel Broder, Jan M. R. Balzarini
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Patent number: 5112835Abstract: 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: GrantFiled: November 21, 1989Date of Patent: May 12, 1992Assignee: Mitsubishi Kasei CorporationInventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik D. A. De Clercq, Masanori Baba, Richard T. Walker, Masaru Ubasawa
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Patent number: 4963533Abstract: 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: GrantFiled: October 24, 1986Date of Patent: October 16, 1990Assignees: Stichting Rega VZW (REGA), The Government of the United States of AmericaInventors: Erik D. A. de Clercq, Piet A. M. M. Herdewijn, Samuel Broder, Jan M. R. Balzarini
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Patent number: 4548819Abstract: 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: GrantFiled: June 23, 1983Date of Patent: October 22, 1985Inventors: Erik D. A. De Clercq, Hubert J. H. E. Vander Haeghe, Roger H. C. Busson
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Patent number: 4424211Abstract: 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: GrantFiled: December 21, 1981Date of Patent: January 3, 1984Assignees: Rega Instituut VZW, University of BirminghamInventors: Albert S. Jones, Richard T. Walker, Erik D. A. de Clercq, Philip J. Barr