Patents by Inventor Pierre Jean-Marie Raboisson
Pierre Jean-Marie Raboisson 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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Publication number: 20230278964Abstract: This application relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and medical uses thereof.Type: ApplicationFiled: January 24, 2023Publication date: September 7, 2023Inventors: David Craig MC GOWAN, Werner Constant Johan EMBRECHTS, Jérôme Émile Georges GUILLEMONT, Ludwig Paul COOYMANS, Tim Hugo Maria JONCKERS, Pierre Jean-Marie RABOISSON
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Patent number: 11597704Abstract: This application relates to quinazoline derivatives of formula (I), pharmaceutical compositions comprising the compounds of formula (I), and the use of the compounds of formula (I) in the treatment or prevention of a viral infection, of a virus-induced disease, of cancer or of an allergy.Type: GrantFiled: February 28, 2019Date of Patent: March 7, 2023Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COMPANYInventors: David Craig Mc Gowan, Werner Constant Johan Embrechts, Jérôme Émile Georges Guillemont, Ludwig Paul Cooymans, Tim Hugo Maria Jonckers, Pierre Jean-Marie Raboisson
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Patent number: 11040963Abstract: The present invention provides piperazine derivatives exhibiting high affinity to the stem region (viral membrane proximal part) of influenza hemagglutinin as determined through competition binding and high virus neutralization activity while having low cytotoxity. Furthermore, the present invention relates to pharmaceutical compositions comprising said piperazine derivatives, methods of preparing said piperazine derivatives, as well as said piperazine derivatives for use in medical prevention or treatment, especially for preventing or treating influenza.Type: GrantFiled: February 1, 2018Date of Patent: June 22, 2021Assignee: JANSSEN VACCINES & PREVENTION B.V.Inventors: Maria Van Dongen, Jaroslaw Juraszek, Griet Wim Bert Schepens, Charles Edward Lawson, Brian Shook, Maria Tim Hugo Jonckers, Abdellah Tahri, Bernard Pierre Jean-Marie Raboisson, Nestor CHristophe Francis Robert Buyck
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Publication number: 20210040046Abstract: This application relates to quinazoline derivatives of formula (I), pharmaceutical compositions comprising the compounds of formula (I), and the use of the compounds of formula (I) in the treatment or prevention of a viral infection, of a virus-induced disease, of cancer or of an allergy.Type: ApplicationFiled: February 28, 2019Publication date: February 11, 2021Applicant: Janssen Sciences Ireland UnlimiInventors: David Craig MC GOWAN, Werner Constant Johan EMBRECHTS, Jérôme Émile Georges GUILLEMONT, Ludwig Paul COOYMANS, Tim Hugo Maria JONCKERS, Pierre Jean-Marie RABOISSON
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Publication number: 20200010459Abstract: The present invention provides piperazine derivatives exhibiting high affinity to the stem region (viral membrane proximal part) of influenza hemagglutinin as determined through competition binding and high virus neutralization activity while having low cytotoxity. Furthermore, the present invention relates to pharmaceutical compositions comprising said piperazine derivatives, methods of preparing said piperazine derivatives, as well as said piperazine derivatives for use in medical prevention or treatment, especially for preventing or treating influenza.Type: ApplicationFiled: February 1, 2018Publication date: January 9, 2020Inventors: Maria VAN DONGEN, Jaroslaw JURASZEK, Griet Wim Bert SCHEPENS, Charles Edward LAWSON, Brian SHOOK, Maria Tim, Hugo JONCKERS, Abdellah TAHRI, Bernard Pierre, Jean-Marie RABOISSON, Nestor CHristophe, Francis, Robert BUYCK
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Patent number: 9365582Abstract: Inhibitors of HCV replication of formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; 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; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-memberType: GrantFiled: December 20, 2013Date of Patent: June 14, 2016Assignee: Janssen Sciences Ireland UCInventors: Pierre Jean-Marie Raboisson, Herman Augustinus De Kock, David Craig McGowan, Lili Hu, Abdellah Tahri, Sandrine Marie Helene Vendeville, Wim Van De Vreken
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Patent number: 9233933Abstract: Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1-R5, B and Z have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.Type: GrantFiled: January 4, 2013Date of Patent: January 12, 2016Assignee: Janssen Sciences Ireland UCInventors: Koen Vandyck, Geerwin Yvonne Paul Haché, Geert Rombouts, Wim Gaston Verschueren, Pierre Jean-Marie Raboisson
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Publication number: 20150005295Abstract: Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1-R5, B and Z have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.Type: ApplicationFiled: January 4, 2013Publication date: January 1, 2015Inventors: Koen Vandyck, Geerwin Yvonne Paul Haché, Geert Rombouts, Wim Gaston Verschueren, Pierre Jean-Marie Raboisson
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Publication number: 20140113929Abstract: Inhibitors of HCV replication of formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; 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; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-memberType: ApplicationFiled: December 20, 2013Publication date: April 24, 2014Applicant: Janssen R&D Ireland (formerly Tibotec Pharmaceuticals)Inventors: Pierre Jean-Marie Raboisson, Herman Augustinus De Kock, David Craig Mc Gowan, Lili Hu, Abdellah Tahri, Sandrine Marie Helene Vendeville, Wim Van De Vreken
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Patent number: 8481510Abstract: Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8? form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.Type: GrantFiled: May 11, 2010Date of Patent: July 9, 2013Assignees: Janssen Products, LP, Medivir ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Raboisson, Koen Vandyck, Steven Maurice Van Hoof, Lili Hu, Abdellah Tahri
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Publication number: 20120065156Abstract: Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8? form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.Type: ApplicationFiled: May 11, 2010Publication date: March 15, 2012Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Raboisson, Koen Vandyck, Steven Maurice Van Hoof, Lili Hu, Abdellah Tahri
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Publication number: 20100022578Abstract: Inhibitors of HCV replication of formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; 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; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-membered saturateType: ApplicationFiled: November 16, 2007Publication date: January 28, 2010Inventors: Pierre Jean-Marie Raboisson, Herman Augustinus De Kock, David Craig Mc Gowan, Wim Van De Vreken, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Patent number: 7514427Abstract: HIV inhibitory compounds of formula: salts and stereoisomers thereof, wherein R1 and R2 are hydrogen or optionally substituted C1-10alkyl; R3 is n is 1, 2 or 3; R3a is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, aminocarbonyl, C 1-4alkyloxycarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C1-4alkylcarbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het; or R3 is a monocyclic or bicyclic aromatic heterocyclic ring system, wherein one, two, three or four ring members are nitrogen, oxygen and sulfur, and wherein the remaining ring members are carbon atoms; and wherein each of said heterocyclic ring systems may optionally be substituted; X is —NR7—, —O— or —S—; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.Type: GrantFiled: January 10, 2006Date of Patent: April 7, 2009Assignee: Tibotec Pharmaceuticals, Ltd.Inventors: Bart Rudolf Romanie Kesteleyn, Pierre Jean-Marie Raboisson, Wim Van De Vreken, Maxime Francis Jean-Marie Ghislain Canard
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Publication number: 20090062311Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein each dashed line represents an optional double bond; 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; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—CO—, —O—C(?O)—NR5a— or —O—C(?O)—NR5a—C1-4alkanediyl-; 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 system contains one nitrogen, and optiType: ApplicationFiled: January 16, 2008Publication date: March 5, 2009Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Raboisson, Lili Hu, Dominique Louis Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Lourdes Salvador Oden
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Publication number: 20080167296Abstract: HIV inhibitory compounds of formula: salts and stereoisomers thereof, wherein R1 and R2 are hydrogen or optionally substituted C1-10alkyl; R3 is n is 1, 2 or 3; R3a is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, aminocarbonyl, CI 4alkyloxycarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C1-4alkylcarbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het; or R3 is a monocyclic or bicyclic aromatic heterocyclic ring system, wherein one, two, three or four ring members are nitrogen, oxygen and sulfur, and wherein the remaining ring members are carbon atoms; and wherein each of said heterocyclic ring systems may optionally be substituted; X is —NR7—, —0— or —S—; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.Type: ApplicationFiled: January 10, 2006Publication date: July 10, 2008Inventors: Bart Rudolf Romanie Kesteleyn, Pierre Jean-Marie Raboisson, Wim Van De Vreken, Maxime Francis Jean-Marie Ghislain Canard
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Publication number: 20070265295Abstract: 1-heterocyclyl-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 a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted.Type: ApplicationFiled: May 17, 2005Publication date: November 15, 2007Inventors: Bart Kesteleyn, Pierre Jean-Marie Raboisson, Dominique Surleraux, Geerwin Hache, Sandrine Vendeville, Piet Tom Wigerinck, Annick Peeters
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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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Publication number: 20070213320Abstract: 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, CType: ApplicationFiled: May 17, 2005Publication date: September 13, 2007Inventors: Bart Kesteleyn, Wim Van De Vreken, Dominique Louis Surleraux, Sandrine Vendeville, Pierre Jean-Marie Raboisson, Piet Tom Wigerinck, Annick Peeters
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Publication number: 20070155716Abstract: The present invention relates to the use of bi-cyclic pyrimidines 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 processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present bi-cyclic pyrimidines with other anti-HCV agents.Type: ApplicationFiled: March 9, 2007Publication date: July 5, 2007Inventors: Kenneth SIMMEN, Tse-I Lin, Oliver Lenz, Dominique Louis Surleraux, Pierre Jean-Marie Raboisson