Patents Assigned to Janssen R&D Ireland
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Patent number: 8846672Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: September 30, 2014Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Steven Maurice Paula Van Hoof, Sandrine Marie Helene Vendeville
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Patent number: 8841310Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.Type: GrantFiled: October 7, 2009Date of Patent: September 23, 2014Assignee: Janssen R & D IrelandInventor: Paul Stoffels
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Publication number: 20140255347Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line 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; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogeType: ApplicationFiled: May 23, 2014Publication date: September 11, 2014Applicants: Janssen R&D Ireland, Medivir ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
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Patent number: 8815849Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? 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 HCV inhibitors, in HCV therapy.Type: GrantFiled: July 26, 2011Date of Patent: August 26, 2014Assignee: Janssen R&D IrelandInventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
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Patent number: 8784858Abstract: A degradable, removable, pharmaceutical implant for the sustained release of one or more drugs in a subject, wherein the pharmaceutical implant is composed of a tube comprising an outer wall made of a degradable polymer completely surrounding a cavity, wherein the outer wall has a plurality of openings and wherein the cavity contains one or more sets of micro-particles, which micro-particles contain an active agent or a combination of two or more active agents, and wherein the size of the microparticles is selected such that the majority of the microparticles cannot pass through the openings.Type: GrantFiled: December 20, 2010Date of Patent: July 22, 2014Assignee: Janssen R&D IrelandInventors: Deborah M. Schachter, Lieven Elvire Colette Baert, Guenter Kraus, Qiang Zhang, Iksoo Chun
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Publication number: 20140171499Abstract: New pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate and processes for producing them are disclosed.Type: ApplicationFiled: February 19, 2014Publication date: June 19, 2014Applicant: Janssen R&D IrelandInventors: Hans Wim Pieter VERMEERSCH, Daniel Joseph Christiaan THONE, Luc Donne Marie-Louise JANSSENS, Piet Tom Bert Paul WIGERINCK
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Publication number: 20140171451Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: ApplicationFiled: August 10, 2012Publication date: June 19, 2014Applicant: Janssen R&D IrelandInventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
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Patent number: 8754116Abstract: Inhibitors of HCV replication of formula (I) wherein W is a heterocycle of formula and the remaining variables are as defined in the specification.Type: GrantFiled: April 20, 2012Date of Patent: June 17, 2014Assignee: Janssen R&D IrelandInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Dominique Louis Nestor Ghislain Surleraux, Wim Van De Vreken
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Patent number: 8754105Abstract: Inhibitors of HCV replication of formula (I) the N-oxides, salts, and stereochemically isomeric forms 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 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 optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—C(?O)—, —O—C(?O)—NR4a— or —O—C(?O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(?O)OR5, —C(?O)R6, —C(?O)NR4aR4b, —C(?O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and wheType: GrantFiled: May 17, 2011Date of Patent: June 17, 2014Assignees: Medivir AB, Janssen R&D IrelandInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Rabiosson, Abdellah Tahri, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Dmitry Antonov
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Patent number: 8754093Abstract: Etravirine (TMC125) nicotinamide co-crystal, its preparation, and use in the treatment of HIV infection.Type: GrantFiled: March 26, 2010Date of Patent: June 17, 2014Assignee: Janssen R&D IrelandInventors: Matthew F. Sansone, Mark Tawa, Julius F. Remenar, Lieven Elvire Colette Baert
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Patent number: 8754106Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line 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; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogType: GrantFiled: March 15, 2013Date of Patent: June 17, 2014Assignees: Janssen R&D Ireland, Medivir ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
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Patent number: 8741926Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line 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; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogeType: GrantFiled: November 28, 2012Date of Patent: June 3, 2014Assignees: Janssen R&D Ireland, Medivir ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linnea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
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Publication number: 20140142070Abstract: This invention relates to solid oral dosage forms of the HIV inhibitor Darunavir and/or a pharmaceutically acceptable salt or solvate thereof, and combination formulations thereof.Type: ApplicationFiled: July 6, 2012Publication date: May 22, 2014Applicant: Janssen R&D IrelandInventors: Urbain Alfons C Delaet, Philip Erna H. Heyns, Eugeen Maria Jozef Jans, Roel Jos M. Mertens, Geert Van Der Avoort
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Patent number: 8722696Abstract: A process for preparing a particle comprising a co-precipitate surrounding a neutral hydrophilic carrier, said process comprising spraying an organic solution on a neutral hydrophilic carrier, said solution comprising at least one triazine or pyrimidine active ingredient having HIV inhibiting properties, one surface active agent, and one hydrophilic polymer, wherein the spraying of whole of the solution occurs in at least two separate steps, each of these steps followed by a grinding step of the product obtained at the end of the preceding step.Type: GrantFiled: September 3, 2009Date of Patent: May 13, 2014Assignee: Janssen R&D IrelandInventors: Gaël Lamoureux, Gérard Cousin, Daniel Joseph Christiaan Thoné
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Patent number: 8722892Abstract: The present invention relates to synthesis procedures and intermediates of a compound of formula: and the salts thereof.Type: GrantFiled: May 31, 2012Date of Patent: May 13, 2014Assignee: Janssen R&D IrelandInventors: Andras Horvath, Dominique Paul Michel Depre, Dominic John Ormerod
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Publication number: 20140127797Abstract: The invention concerns novel mutations or mutational profiles of HIV-1 protease cleavage sites (CS) in the Gag region correlated with a phenotype causing alterations in sensitivity to anti-HIV drugs. The present invention also relates to the use of 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 further relates to methods of utilizing the mutational profiles of the invention in databases, drug development, i.e., drug design, and drug modification, therapy and treatment design and clinical management.Type: ApplicationFiled: August 21, 2013Publication date: May 8, 2014Applicant: JANSSEN R&D IRELANDInventors: INGE DIERYNCK, SANDRA DE MEYER
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Patent number: 8716293Abstract: Compound having formula I and pharmaceutically acceptable salts or solvates thereof, their pharmaceutical formulations and use as HIV inhibitors.Type: GrantFiled: April 1, 2011Date of Patent: May 6, 2014Assignee: Janssen R&D IrelandInventors: Johannes Wilhelmus J. Thuring, Jean-Francois Bonfanti
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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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Publication number: 20140107101Abstract: Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1, R2, R4, R5, R6 and R7 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.Type: ApplicationFiled: March 15, 2013Publication date: April 17, 2014Applicant: JANSSEN R&D IRELANDInventor: Janssen R&D Ireland
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Publication number: 20140107172Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, solvates thereof, wherein R and R? are, each independently, —CR1R2R3, aryl, heteroaryl or heteroC4-6cycloalkyl, whereby aryl and heteroaryl may optionally be substituted with 1 or 2 substituents selected from halo and methyl. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.Type: ApplicationFiled: March 15, 2013Publication date: April 17, 2014Applicant: JANSSEN R&D IRELANDInventor: JANSSEN R&D IRELAND