Patents Assigned to Tibotec BVBA
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Patent number: 8227407Abstract: Macrocylic compounds having inhibitory activity on the replication of the hepatitis C virus (HCV) of the general formula (I) X is N, CH and where X bears a double bond it is C; R1a and R1b are hydrogen, C3-7cycloalkyl, aryl, Het, C1-6alkoxy, C1-6alkyl optionally substituted with halo, C1-6alkoxy, cyano, polyhaloC1-6alkoxy, C3-7cycloalkyl, aryl, or with Het; or R1a and R1b together with the nitrogen to which they are attached form a 4 to 6 membered heterocyclic ring which may be optionally substituted; Het being a heterocyclic ring; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—CO—, —O—C(?O)—NR5a— or —O—C(?O)—NR5a—C1-4alkanediyl-; n is 3, 4, 5, or 6; p is 1, or 2; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl, amino, mono- or diC1-6alkylamino; R4 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring systemType: GrantFiled: January 16, 2008Date of Patent: July 24, 2012Assignees: Medivir AB, Tibotec BVBAInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist, Lourdes Salvador Odén
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Patent number: 8137921Abstract: The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the RSV F1 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN57 (SEQ ID NO: 1); a second helical polypeptide consisting essentially of the sequence of C45 (SEQ ID NO: 2) wherein said IQN57 is labeled with a light emitting fluorophore and said C45 is labeled with an ultra-violet excitable fluorophore.Type: GrantFiled: December 12, 2007Date of Patent: March 20, 2012Assignee: Tibotec BVBAInventors: Dirk André E Roymans, Koenraad Lodewijk August van Acker, Inge Vereycken, Géry Karel Julia Dams
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Patent number: 7863428Abstract: This invention relates to hydrolase fluorogenic substrates with improved cell permeability, methods for the preparation thereof, and methods of measuring activities of hydrolases, particularly in cell-based assays. The substrates easily diffuse into the cells, where they are enzymatically processed to yield photostable fluorescent products, and are particularly fitted for visualising enzyme-derived activities in cell-based assays.Type: GrantFiled: December 26, 2003Date of Patent: January 4, 2011Assignee: Tibotec BVBAInventors: Inge Dierynck, Jan Ludwig Goeman, Koenraad Lodewijk August Van Acker, Johan Theo André Van Der Eycken
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Patent number: 7622582Abstract: 4-substituted 1,5-dihydro-pyrido[3,2-b]indol-2-ones of formula (I): the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein n is 1, 2 or 3; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; X is NR2, O, S, SO, SO2; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, which are optionally substituted; R2 is aryl substituted with —COOR4; or R2 is: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b (b-5); -a1=a2-a3=a4- is —CH?CH—CH?CH—; —N?CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N—; wherein hydrogen atoms in (c-1)-(c-5) may be replaced by certain radicals; R3 is optionally substituted phenyl or a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted; R21 is halo, hydroxy, amino, carboxyl, C1-6alkyl, C3-7cycloalkyl, arylC1-6alkyl, formyl, C1-6alkylcarbonyl, C1Type: GrantFiled: May 17, 2005Date of Patent: November 24, 2009Assignee: Tibotec BVBAInventors: Bart Rudolf Romanie Kesteleyn, Wim Van De Vreken, Dominique Louis Nestor Ghislain Surleraux, Sandrine Marie Helene Vendeville, Pierre Jean-Marie Bernard Raboisson, Piet Tom Bert Paul Wigerinck, Annick Ann Peeters
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Patent number: 7585870Abstract: This invention concerns HIV replication inhibitors of formula (I), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.Type: GrantFiled: February 20, 2004Date of Patent: September 8, 2009Assignee: Tibotec BVBAInventors: Jerôme Emile Georges Guillemont, Elisabeth Thérese Jeanne Pasquier, Jan Heeres, Kurt Hertogs, Eva Bettens, Paulus Joannes Lewi, Marc René De Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Frank Xavier Jozef Herwig Arts
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Publication number: 20070238727Abstract: Compounds of formula (I) the N-oxides, salts, stereoisomeric forms, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, a carbonyl derivative, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)-methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R2 is (i) aryl substituted with a radical —COOR4; (ii) C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, substituted with aryl which is substituted with a radical —COOR4; (iii) C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, substituted with —NR5a—C(?NR5b)—NR5cR5d, —O—NR5a—C(?NR5b)—NR5cR5d, -sulfonyl-R6, —NR7R8, —NR9R10, a radical (a-1), (a-2), (a-3), (a-4), (a-5); or (iv) a radical of formula: (a-6), (b-2), —CpH2p—CH(OR14)—CqH2q—R15; —CH2—CH2—(O—CH2—CH2)m—OR14; —CH2—CH2—(O—CH2—CH2)m—NR17aR17b; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, a carbonyl derivative, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1.Type: ApplicationFiled: May 17, 2005Publication date: October 11, 2007Applicant: Tibotec BVBAInventors: Bart Kesteleyn, Maxime Francis Canard, Wim Van De Vreken, Pierre Jean-Marie Raboisson, Dominique Louis Surleraux, Piet Tom Wigerinck
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Patent number: 7235215Abstract: A capillary filling system automatically plucks capillaries from a capillary roll, and transports them to a filling station where the capillaries are filled with compounds. The filled capillaries are then fixed on a template where they are then ready to be used for experimentation. A method of filling the capillaries is also disclosed.Type: GrantFiled: September 7, 2001Date of Patent: June 26, 2007Assignee: Tibotec BVBAInventors: Franck Velghe, Werner René Irène De Beukeleer, Ignace Maria S. M. Van De Maele
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Patent number: 7189505Abstract: The present invention relates to methods and products for the evaluation of HIV treatment. The methods are based on evaluating molecular events at the HIV integrase resulting in altered therapeutic efficacy of the investigated compounds. The methods rely on providing an integrase gene and evaluating either through genotyping or phenotyping the integrase gene. The present invention relates to the fields of diagnostics, drug screening, pharmacogenetics and drug development.Type: GrantFiled: August 15, 2005Date of Patent: March 13, 2007Assignee: Tibotec BVBAInventors: Johan Hendrika Jozef Vingerhoets, Lieve Emma Jan Michiels, Inge Dierynck
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Patent number: 7129036Abstract: The invention relates to reporter molecules comprising at least one detection domain capable of emitting a signal and at least one membrane anchoring domain, which promotes the association of the reporter molecule with a membrane. The degree and rate of membrane association of the reporter molecule is approximated by the signal emitted by the detection domain. This signal provides a marker for the membrane association status of the membrane anchoring portion, or of the reporter molecule as a whole. Treatments or agents may be tested for their ability to alter membrane association or localization by observing or measuring the signal emitted by the detection domain. Thus, the invention provides means and methods for determining the capability of an agent to interfere at least in part with the distribution of a reporter molecule in a cell. These methods are useful for drug discovery; the phenotypic evaluation of cells, preferably patient cells; and for tailoring a therapeutic program for treating a patient.Type: GrantFiled: May 26, 2000Date of Patent: October 31, 2006Assignee: Tibotec BVBAInventors: Koenraad Lodewijk August Van Acker, Inge Dierynck, Rudi Wilfried Jan Pauwels
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Patent number: 7016110Abstract: The apparatus for automatically focusing an image in a microscope includes onto an object plane includes an optical system configured to form an optical image of a sample plane to be observed, an autofocusing detection system, and a focus correction system. The autofocusing system includes an autofocusing light beam source for generating autofocusing light beams. The autofocusing system further includes a detection system lens for directing autofocusing light beams to an autofocusing detection device, and an autofocusing detection device for determining the amount of displacement of the image of the object plane from a desired focused reference plane. The focusing correction system includes a feedback controller and focus adjusting device for automatically adjusting the distance between an objective lens and the sample plane in order to properly focus the image in the optical system. A related method of automatically focusing an image of an object plane in a microscope.Type: GrantFiled: March 8, 2001Date of Patent: March 21, 2006Assignee: Tibotec BVBAInventor: Marc Jan René Leblans
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Patent number: 6974938Abstract: The apparatus for automatically focusing an image in a microscope includes onto an object plane includes an optical system configured to form an optical image of a sample plane to be observed, an autofocusing detection system, and a focus correction system. The autofocusing system includes an autofocusing light beam source for generating autofocusing light beams. The autofocusing system further includes a detection system lens for directing autofocusing light beams to an autofocusing detection device, and an autofocusing detection device for determining the amount of displacement of the image of the object plane from a desired focused reference plane. The focusing correction system includes a feedback controller and focus adjusting device for automatically adjusting the distance between an objective lens and the sample plane in order to properly focus the image in the optical system. A related method of automatically focusing an image of an object plane in a microscope is also provided.Type: GrantFiled: March 8, 2000Date of Patent: December 13, 2005Assignee: Tibotec BVBAInventors: Marc Jean Rene Leblans, Philip Arthur Van Donink
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Patent number: 6868875Abstract: A method for dispensing a volume of fluids from a reservoir, through a fluid outlet in fluid communication with said reservoir, into each well of at least a series of wells, whereby the fluid is dispensed into said series of wells at a continuous uninterrupted flow. A micro titer plate constructed from a hydrophobic and more in particular from a plastic material containing a plurality of series of wells and to an apparatus able to perform the above method.Type: GrantFiled: March 8, 2001Date of Patent: March 22, 2005Assignee: Tibotec BVBAInventors: Werner René Irène De Beukeleer, Christiaan Hubert Simon Roelant
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Patent number: 6800437Abstract: The present invention is directed to reporter molecules and tags that may be used to monitor a target substance in a biological system. More particularly, the present invention relates to the use of an apo metal binding protein as a reporter molecule or tag. An apo metal binding protein may be bound to a protein or tissue or introduced into a cell. The invention also relates to methods of utilizing the apo metal binding protein for detecting a cell expressing a protein of interest, localizing a protein in a cell, and designing a therapeutic agent for treating a disease or infection.Type: GrantFiled: August 4, 2000Date of Patent: October 5, 2004Assignee: Tibotec BvbaInventors: Inge Dierynck, Christiaan Hubert Simon Roelant, Rudi Wilfried Jan Pauwels, Koenraad Lodewijk August Van Acker, Jan Octaaf Antoon De Kerpel
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Patent number: 6544480Abstract: A device and related method for dispensing liquid. The device includes a housing configured to contain a plurality of liquid dispensing members containing a liquid and configured to contain a receiving member in a receiving position to receive the liquid from the plurality of liquid dispensing members. The housing defines a first pressure chamber and a second pressure chamber. The first pressure chamber is capable of being sealed relative to the second pressure chamber. The device also includes a differential pressure generator operably connected to one of the first and second pressure chambers. The generator is capable of generating a pressure differential between the first and second pressure chambers to cause the plurality of liquid dispensing members to dispense liquid onto the receiving member.Type: GrantFiled: October 26, 1999Date of Patent: April 8, 2003Assignee: Tibotec BVBAInventors: Franck Velghe, Werner De Beukeleer, Chris Roelant, Rudi Pauwels