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: 20070185062Abstract: 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: ApplicationFiled: March 4, 2005Publication date: August 9, 2007Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De clercq
-
Publication number: 20060275748Abstract: 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: ApplicationFiled: September 26, 2003Publication date: December 7, 2006Applicant: KULEUVEN RESEARCH AND DEVELOPMENTInventors: Zeger Debyser, Petr Cherepanov, Erik De Clercq
-
Publication number: 20060241081Abstract: 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: ApplicationFiled: June 23, 2006Publication date: October 26, 2006Inventors: Jan Balzarini, Erik De Clercq, Antonin Holy, Dana Hockova
-
Patent number: 7049332Abstract: 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: GrantFiled: February 23, 2001Date of Patent: May 23, 2006Assignee: K. U. Leuven Research & DevelopmentInventors: Erik De Clercq, Arthur Van Aerschot, Piet Herdewijn, Irene Lagoja, Christophe Pannecoucque
-
Patent number: 7019135Abstract: 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: GrantFiled: May 8, 2001Date of Patent: March 28, 2006Assignees: University College Cardiff Consultants Limited, Rega FoundationInventors: Christopher McGuigan, Jan Balzarini, Erik De Clercq
-
Publication number: 20050250677Abstract: 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: ApplicationFiled: September 1, 2003Publication date: November 10, 2005Inventors: Jan Balzarini, Maria Preobrazhenskaya, Erik De Clercq
-
Publication number: 20050239821Abstract: 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: ApplicationFiled: July 3, 2003Publication date: October 27, 2005Inventors: Johan Neyts, Gerhard Purstinger, Erik De Clercq
-
Publication number: 20050075318Abstract: 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: ApplicationFiled: June 16, 2004Publication date: April 7, 2005Inventors: Jan Balzarini, Erik De Clercq, Antonin Holy, Dana Hockova
-
Publication number: 20050038058Abstract: 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: ApplicationFiled: September 21, 2004Publication date: February 17, 2005Inventors: Jan Balzarini, Erik De Clercq, Antonin Holy
-
Publication number: 20040122024Abstract: 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 isopropType: ApplicationFiled: February 11, 2004Publication date: June 24, 2004Inventors: Erik De Clercq, Arthur Van Aerschot, Piet Herdewijn, Irene Lagoja, Christophe Pannecoucque
-
Publication number: 20030187003Abstract: 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: ApplicationFiled: February 24, 2003Publication date: October 2, 2003Inventors: Erik De Clercq, Zeger Debyser, Willem Plymers, Christophe Pannecouque, Myriam Witvrouw
-
Publication number: 20030176370Abstract: 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: ApplicationFiled: November 8, 2002Publication date: September 18, 2003Inventors: Christopher McGuigan, Jan Maria Rene Balzarini, Erik De Clercq
-
Patent number: 6573247Abstract: 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 froType: GrantFiled: January 6, 2000Date of Patent: June 3, 2003Assignees: University College Cardiff Consultants Limited, Rega FoundationInventors: Christopher McGuigan, Christopher Yarnold, Garry Jones, Jan Balzarini, Erik De Clercq
-
Patent number: 5733896Abstract: 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: GrantFiled: March 18, 1994Date of Patent: March 31, 1998Assignees: 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: 5596018Abstract: 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: GrantFiled: August 20, 1993Date of Patent: January 21, 1997Assignee: Toray Industries, Inc.Inventors: Masanori Baba, Dominique Schols, Rudi Pauwels, Jan Balzarini, Erik De Clercq
-
Patent number: 4988678Abstract: 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: GrantFiled: June 29, 1989Date of Patent: January 29, 1991Assignee: Stichting Rega VZWInventors: Erik De Clercq, Masaaki Iigo
-
Patent number: 4894365Abstract: 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: GrantFiled: February 11, 1988Date of Patent: January 16, 1990Assignee: Stichting Rega VZWInventors: Erik De Clercq, Masaaki Iigo
-
Patent number: 4724233Abstract: 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: GrantFiled: April 21, 1986Date of Patent: February 9, 1988Assignees: Stichting Rega VZW, Ceskoslovenska Akademie VEDInventors: Erik De Clercq, Antonin Holy, Ivan Rosenberg
-
Patent number: 4605658Abstract: 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: GrantFiled: October 5, 1984Date of Patent: August 12, 1986Assignees: Ceskoslovenska Akademie Ved., Stichting Rega VZWInventors: Antonin Holy, Erik de Clercq
-
Patent number: 4382925Abstract: 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: GrantFiled: October 2, 1980Date of Patent: May 10, 1983Assignees: The University of Birmingham, Stichting Rega V.Z.W.Inventors: Erik de Clercq, Gabriel A. Verhelst, Albert S. Jones, Richard T. Walker