Patents Assigned to Janssen R&D Ireland
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Patent number: 8673551Abstract: The present invention relates to methods and means for the evaluation of HIV replicative capacity in a given environment. In particular, the invention provides a growth competition assay that can determine relative viral fitness using a recombinant tagged HIV-1 virus system. The methods rely on plasmid vectors, amplicons, primers and probes, and the generation of replication-competent viruses therefrom. Said methods and materials may find use in multiple fields including diagnostics, drug screening, pharmacogenetics and drug development.Type: GrantFiled: December 7, 2006Date of Patent: March 18, 2014Assignees: Speedx Pty Ltd., Janssen R&D IrelandInventors: Laurence Tatiana Rimsky, Inky Paul Madeleine De Baere, Bart Anna Julien Maes, Marie-Pierre T. M. M. G. De Bethune, Guenter Kraus, Elisa Mokany, Alison Velyian Todd
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Publication number: 20140073642Abstract: This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.Type: ApplicationFiled: May 18, 2012Publication date: March 13, 2014Applicant: Janssen R&D IrelandInventors: David McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Stefaan Julien Last, Werner Embrechts, Serge Maria Aloysius Pieters
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Patent number: 8664391Abstract: The present invention relates to compounds of formula (I) that have CYP450 inhibiting properties and are useful as boosting agents when used with HIV treatments. These compounds are represented by formula including the salts and stereoisomeric forms thereof, wherein R1 is 5-thiazolyl or 3-pyridinyl; R2 is iso-butyl, 2,2-dimethylpropyl; 2-hydroxy-2-methyl-propyl or cyclohexylmethyl; R3 is phenyl optionally substituted with one or more halogens, trifluoromethyl, C1-6-alkyl or C1-6-alkoxy wherein optionally two of said alkoxy groups are be linked to each other to form a 5 or 6-membered ring; heteroaryl; C3-7cycloalkyl optionally substituted with one or more halogens; C1-6alkyl optionally substituted with heteroaryl; —O—CH2— (heteroaryl). As boosting agents they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered, or improve the bioavailability of certain drugs.Type: GrantFiled: October 7, 2009Date of Patent: March 4, 2014Assignee: Janssen R&D Ireland LtdInventors: Tim Hugo Maria Jonckers, Wim Bert Griet Schepens, Geerwin Yvonne Paul Haché, Beate Sabine Hallenberger, Jennifer Chiyomi Sasaki, Judith Eva Baumeister, Gerben Albert Van 'T Klooster
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Patent number: 8637663Abstract: 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 saturatType: GrantFiled: November 16, 2007Date of Patent: January 28, 2014Assignee: Janssen R&D IrelandInventors: Pierre Jean-Marie Bernard Raboisson, Herman Augustinus De Kock, David Craig McGowan, Wim Van De Vreken, Lili Hu, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Publication number: 20130324527Abstract: 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: ApplicationFiled: December 16, 2011Publication date: December 5, 2013Applicant: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdella Tahri, Steven Maurice Paula Van Hoof, Sandrine Marie Helene Vendeville
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Patent number: 8592161Abstract: 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: December 20, 2006Date of Patent: November 26, 2013Assignee: Janssen R&D IrelandInventors: Sandra De Meyer, Hilde Azijn, Marie-Pierre T. M. M. G. De Bethune
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Patent number: 8592429Abstract: HIV inhibitors of formula (I) wherein R1 is halo, C1-4 alkoxy, trifluoromethoxy; R2 is a group of formula (A); R3 is a group of formula (B); R4 is a group of formula (C); n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4 allyl, halo; R7 and R8 are C1-4 allyl or C1-4 alkoxy-C1-4 alkyl; R9 is C1-4 allyl, cyclopropyl, trifluoromethyl, C1-4 alkoxy, or dimethylamino; R10 is hydrogen, C1-4 alkyl, cyclopropyl, trifluoromethyl, C1-4 alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.Type: GrantFiled: December 10, 2010Date of Patent: November 26, 2013Assignee: Janssen R&D IrelandInventors: Genadiy Kalayanov, Bart Rudolf Romanie Kesteleyn, Kevin Parkes, Bengt Bertil Samuelsson, Wim Bert Griet Schepens, Johannes Wilhelmus J. Thuring, Hans Kristian Wallberg, Jörg Kurt Wegner
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Patent number: 8580981Abstract: 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 novel intermediates for use in said process. (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 an HIV protease inhibitor.Type: GrantFiled: September 1, 2009Date of Patent: November 12, 2013Assignee: Janssen R&D IrelandInventors: Piet Tom Bert Paul Wigerinck, Dominique Louis Nestor Ghislain Surleraux, Wim Gaston Verschueren, Herman Augustinus De Kock, Wim Albert Alex Aelterman
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Patent number: 8557854Abstract: A method for improving the pharmacokinetics of drugs, which are metabolized by cytochrome P450 monooxygenase is disclosed. More specifically it relates to a method for improving the pharmacokinetics of retroviral protease inhibitors and in particular for improving the pharmacokinetics of human immunodeficiency virus (HIV) protease inhibitors. A pharmaceutical composition and its use in the manufacture of a medicament for the inhibition or treatment of an HIV infection or AIDS in a human being are also part of the invention.Type: GrantFiled: April 14, 2006Date of Patent: October 15, 2013Assignee: Janssen R&D IrelandInventors: Gerben Albert Van 'T Klooster, Piet Tom Bert Paul Wigerinck, Sandra De Meyer, Lieven Elvire Colette Baert, Herman Augustinus De Kock
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Publication number: 20130267508Abstract: Benzimidazoles having inhibitory activity on RSV replication and having the formula the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof, compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: ApplicationFiled: December 16, 2011Publication date: October 10, 2013Applicant: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Lili Wu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Publication number: 20130267556Abstract: Azaindoles having inhibitory activity on RSV replication and having the formula I compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: ApplicationFiled: December 16, 2011Publication date: October 10, 2013Applicant: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Publication number: 20130267555Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: ApplicationFiled: December 16, 2011Publication date: October 10, 2013Applicant: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Publication number: 20130261151Abstract: 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 compositionsType: ApplicationFiled: December 16, 2011Publication date: October 3, 2013Applicant: JANSSEN R & D IRELANDInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Publication number: 20130243857Abstract: The invention provides multilayer tablets that contain rilpivirine hydrochloride, emtricitabine, and tenofivir disoproxil fumarate. The tablets are useful for the treatment of HIV.Type: ApplicationFiled: November 18, 2011Publication date: September 19, 2013Applicant: JANSSEN R & D IRELANDInventors: Reza Oliyai, Lauren Wiser, Mark Menning
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Patent number: 8524716Abstract: The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein R1; R3; and R4 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: GrantFiled: December 23, 2008Date of Patent: September 3, 2013Assignee: Janssen R&D IrelandInventors: Pierre Jean-Marie Bernard Raboisson, Lili Hu, Sandrine Marie Helene Vendeville, Origène Nyanguile, Abdellah Tahri
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Patent number: 8518987Abstract: 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: GrantFiled: August 6, 2009Date of Patent: August 27, 2013Assignee: 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: 20130123244Abstract: 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: ApplicationFiled: July 26, 2011Publication date: May 16, 2013Applicant: JANSSEN R&D IRELANDInventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
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Patent number: 8436036Abstract: Compounds of the formula I: including any possible stereoisomers thereof, or a pharmaceutically acceptable salt and/or solvate thereof, as well as pharmaceutical formulations and the use of compounds of formula I as HCV inhibitors.Type: GrantFiled: April 23, 2010Date of Patent: May 7, 2013Assignee: Janssen R&D IrelandInventors: Samuel Dominique Demin, David McGowan, Stefaan Julien Last, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20130102777Abstract: The present invention relates to an improved method for the preparation of 13-cyclohexyl-3-methoxy-6-[methyl-(2-{2-[methyl-(sulphamoyl)-amino]-ethoxy}-ethyl)-carbamoyl]-7H-indolo-[2,1-a]-[2]-benzazepine-10-carboxylic acid. The present invention also relates to a new compound, namely tert-butyl (methyl-{2-[2-(methylamino)-ethoxy]-ethyl}-sulphamoyl)-carbamate, used in this improved method.Type: ApplicationFiled: June 24, 2011Publication date: April 25, 2013Applicant: JANSSEN R&D IRELANDInventors: Tom Cornelis Hortense Govaerts, Jean-Pierre-Andre Marc Bongartz, Patrick Hubert J. Nieste
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Patent number: 8383584Abstract: Compounds of the formula I: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.Type: GrantFiled: February 8, 2008Date of Patent: February 26, 2013Assignees: Medivir AB, Janssen R&D IrelandInventors: Dmitry Antonov, Susana Ayesa Alvarez, Anna Karin Gertrud Linnea Belfrage, Carl Erik Daniel Jönsson, David Craig McGowan, Karl Magnus Nilsson, Pierre Jean-Marie Bernard Raboisson, Åsa Annica Kristina Rosenquist, Bengt Bertil Samuelsson