Patents Assigned to Tibotec Pharmaceuticals Ltd.
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Patent number: 8084494Abstract: The present invention concerns substituted aminophenylsulfonamide compounds, their use as protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present substituted aminophenylsulfonamide compounds with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.Type: GrantFiled: November 28, 2006Date of Patent: December 27, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Herman Augustinus De Kock, Tim Hugo Maria Jonckers, Stefaan Julien Last, Paul Jozef Gabriel Maria Boonants, Dominique Louis Nestor Ghislain Surleraux, Piet Tom Bert Paul Wigerinck
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Patent number: 8076062Abstract: The present invention is directed to the field of nucleic acid diagnostics and the identification of base variation in target nucleic acid sequences. More particularly, the present invention relates to the use of such genotypic characterization of a target population of HIV and the subsequent association, i.e., correlation, of this information to phenotypic interpretation in order to correlate virus mutational profiles with drug resistance. The invention also relates to methods of utilizing the mutational profiles of the invention in drug development, i.e., drug discovery, drug design, drug modification, and therapy, treatment design, clinical management and diagnostic analysis.Type: GrantFiled: October 30, 2008Date of Patent: December 13, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Hilde Azijn, Marie-Pierre T. M. M. G De Bethune, Johan Hendrika Jozef Vingerhoets
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Patent number: 8076513Abstract: A process for the preparation of N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives in which a (1-benzyl-2-hydroxy-3-isobutylamino-propyl)-carbamic acid derivative is reacted with a p-nitrophenylsulfonyl halide to provide the desired product in a high yield and degree of purity.Type: GrantFiled: April 25, 2008Date of Patent: December 13, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Hartmut Burghard Zinser, Peter Hermann Hölzle
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Patent number: 8067463Abstract: The present invention provides a compound having the structure (I) and processes for the production thereof and the intermediates used in such process.Type: GrantFiled: February 24, 2006Date of Patent: November 29, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventor: Bruno Linclau
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Patent number: 8034835Abstract: Inhibitors of RSV replication of formula (I) which can be represented by formula (I) the salts and stereochemically isomeric forms thereof, wherein R is a radical of formula Q is hydrogen or C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both a radical —OR4 and a heterocycle; Alk is C1-6alkanediyl; X is O or S; -a1=a2-a3=a4- is —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH— or —CH?CH—CH?N—; R1 is Ar or a heterocycle; R2 is hydrogen, C1-6alkyl, substituted C1-6alkyl, C3-7cycloalkyl; R3 is hydrogen, C1-6alkyl, cyano, aminocarbonyl, polyhaloC1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 is hydrogen or C1-6alkyl; Ar is phenyl or substituted phenyl; Het is a heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).Type: GrantFiled: June 20, 2006Date of Patent: October 11, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Jean-François Bonfanti, Philippe Muller, Jérôme Michel Claude Fortin, Frédéric Marc Maurice Doublet
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Patent number: 8030318Abstract: Substituted fused bicyclic pyrimidine compounds having an amide-substituted pyridylamine group at C-4 of the pyrimidine ring are useful in the treatment of conditions associated with HCV.Type: GrantFiled: March 27, 2006Date of Patent: October 4, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Kenneth Alan Simmen, Dominique Louis Nestor Ghislain Surleraux, Tse-I Lin, Oliver Lenz, Pierre Jean-Marie Bernard Raboisson, Sarvajit Chakravarty, Barry Patrick Hart
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Patent number: 8022077Abstract: The present invention relates to the use of pyrido[2,3-d]pyrimidines of formula (I) wherein L, R1, R2 and R3 have specific meaning. The present invention also relates to the use of the compounds of formula (I) as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds of formula (I) per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.Type: GrantFiled: May 12, 2006Date of Patent: September 20, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Kenneth Alan Simmen, Dominique Louis Nestor Ghislain Surleraux, Tse-I Lin, Oliver Lenz, Pierre Jean-Marie Bernard Raboisson
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Patent number: 8012939Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein each variable has specific definitions. Pharmaceutical compositions containing compounds (I) and process for preparing compounds (I) are also provided. Bioavailable combinations of the inhibitors of HCV of Formula (I) with ritonavir are also provided.Type: GrantFiled: July 28, 2006Date of Patent: September 6, 2011Assignees: Tibotec Pharmaceuticals Ltd. Co, Medivir ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Wim Van De Vreken, Ismet Dorange, Yvan Simonnet, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Hans Kristian Wallberg
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Patent number: 8008251Abstract: Inhibitors of HCV of formula (I). and the N-oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.Type: GrantFiled: July 28, 2006Date of Patent: August 30, 2011Assignees: Tibotec Pharmaceuticals Ltd., Medivir ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Mats Stefan Lindström, Pia Cecilia Kahnberg, Dmitry Antonov, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist
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Patent number: 7994187Abstract: HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(?O)—R5, —C(?O)—OR4, —C(?O)—NR6R7, —OR4, —O—C(?O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(?O)—C1-6alkyl, —O—C1-6alkyl-C(?O)—OR4, —O—C1-6alkyl-C(?O)—NR6R7, —NR6R7, —NR8—C(?O)—R5, —NR8—C(?O)—OR4, —NR8—C(?O)—NR6R7, —NR8—C(?O)—C1-6alkyl-C(?O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N?CH—NR6R7, —NH—C(?NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-6alkyl, polyhaloC1-6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, pyrimidType: GrantFiled: April 3, 2007Date of Patent: August 9, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Bart Rudolf Romanie Kesteleyn, Wim Bert Griet Schepens
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Patent number: 7989471Abstract: Inhibitors of HCV of formula (I) and the N-oxides, salts, and stereochemically isomeric forms thereof, wherein the terms R1, L, R2, R3, R4, and n have specific definitions; pharmaceutical compositions containing compounds of formula (I), and processes for preparing compounds of formula (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.Type: GrantFiled: July 28, 2006Date of Patent: August 2, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Wim Van De Vreken, David Craig McGowan, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux
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Publication number: 20110165093Abstract: The present invention concerns the microbicidal activity of certain pyrimidine or triazine containing non-nucleoside reverse transcriptase inhibitors. The compounds of the present invention inhibit the systemic infection of a human being with HIV, in particular, the present compounds prevent sexual HIV transmission in humans.Type: ApplicationFiled: March 8, 2011Publication date: July 7, 2011Applicant: TIBOTEC PHARMACEUTICALS LTD.Inventors: Jens (Marcel) Van Roey, Marie-Pierre T.M.M.G. De Bethune, Paul Stoffels
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Patent number: 7956196Abstract: Novel 1,3-dihydro-benzimidazol-2-ylidene amine derivatives of formula the addition salts and stereochemically isomeric forms wherein each Alk is C1-6alkanediyl; Q is hydrogen; C1-6alkyl substituted with one or two Ar2 radicals; C1-6alkyl substituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; —CO—Ar2; or Q is a radical of formula wherein t is 1, 2 or 3; R4 is amino, mono-or di(C1-6alkyl)amino; R1 is Ar2, —CO—Ar2 or a monocyclic or bicyclic heterocycle which may optionally be substituted; R2 is as R1 and additionally can be hydrogen; where Q is other than hydrogen, R3 is hydrogen; and where Q is other than hydrogen, R3 is a radical: wherein R6 is hydrogen, C1-6alkyl, substituted C1-6alkyl; R7, R8, R9 are halo, cyano, C1-6alkyl, substituted C1-6alkyl, C2-6alkenyl, cyanoC2-6alkenyl, C2-6alkynyl, cyanoC2 6alkynyl, Ar1, R10a—0—, R10a—S—, —N(R5aR5b), R10a—O—C(?O)—, N(R5aR5b)—C(?O)—, R10a—C(?O)—NR5b—, R10b—C(?O)—O—; and R8 and/or R9 may also beType: GrantFiled: March 17, 2006Date of Patent: June 7, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Jean-François Bonfanti, Jérôme Michel Claude Fortin, Ismet Dorange
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Patent number: 7935711Abstract: HIV replication inhibitors of formula (I) a pharmaceutically acceptable addition salt; or a stereochemically isomeric form thereof, wherein R1 is halo; R2 and R3 each independently are C1-6alkyl. Pharmaceutical compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: February 20, 2006Date of Patent: May 3, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Herman Augustinus De Kock, Piet Tom Bert Paul Wigerinck
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Patent number: 7935710Abstract: The present invention concerns the microbicidal activity of certain pyrimidine or triazine containing non-nucleoside reverse transcriptase inhibitors. The compounds of the present invention inhibit the systemic infection of a human being with HIV, in particular, the present compounds prevent sexual HIV transmission in humans.Type: GrantFiled: May 13, 2003Date of Patent: May 3, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Jens Marcel Van Roey, Marie-Pierre T.M. M. G. De Bethune, Paul Stoffels
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Patent number: 7863306Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them.Type: GrantFiled: October 7, 2009Date of Patent: January 4, 2011Assignee: Tibotec Pharmaceuticals LtdInventors: Dominique Louis Nestor Ghislain Surleraux, Sandrine Marie Helene Vendeville, Wim Gaston Verschueren, Marie-Pierre T. M. M. G. De Bethune, Herman Augustinus De Kock, Abdellah Tahri
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Patent number: 7803836Abstract: The present invention concerns substituted aminophenylsulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present substituted aminophenylsulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.Type: GrantFiled: November 28, 2006Date of Patent: September 28, 2010Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Herman Augustinus De Kock, Tim Hugo Maria Jonckers, Stefaan Julien Last, Paul Jozef Gabriel Maria Boonants, Dominique Louis Nestor Ghislain Surleraux, Piet Tom Bert Paul Wigerinck
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Publication number: 20100234375Abstract: This invention concerns 5-(hydroxymethylene and aminomethylene)pyrimidine derivatives having HIV (Human Immunodeficiency Virus) replication inhibiting properties, to the preparation thereof and to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: March 30, 2007Publication date: September 16, 2010Applicant: TIBOTEC PHARMACEUTICALS LTD.Inventors: Jerôme Emile Georges Guillemont, Céline Isabelle Mordant, Benoit Antoine Schmitt
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Patent number: 7772411Abstract: The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate as well as intermediates for use in said process. More in particular the invention relates to processes for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate which make use of 4-amino-N-((2R,3S)-3-amino-2-hydroxy-4-phenylbutyl)-N-(isobutyl)benzene sulfonamide intermediate, and to processes amenable to industrial scaling up. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as HIV protease inhibitors.Type: GrantFiled: December 23, 2004Date of Patent: August 10, 2010Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Nicolaas Martha Felix Goyvaerts, Piet Tom Bert Paul Wigerinck, Hartmut Burghard Zinser, Birgit M. Ebert
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Patent number: 7763641Abstract: The present invention concerns the compounds having the formula (I), N-oxides, salt, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by C1-6alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC1-6alkyl, carboxyl, C3-7cycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, —(R7a)n—M—R7b, Het1 and Het2; whereby the optional substituents on any amino function are independently selected from R5 and —A—R6; and on (ii) a nitrogen atom if present by hydroxy or —A—R6. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them.Type: GrantFiled: December 20, 2002Date of Patent: July 27, 2010Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Sandrine Marie Helene Vendeville, Wim Gaston Verschueren, Abdellah Tahri, Samuel Leo Christiaan Moors, Montserrat Erra Sola