Patents by Inventor Ruben Gerardus George Leenders

Ruben Gerardus George Leenders 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).

  • Patent number: 11926614
    Abstract: The present invention relates to compounds of formula (I), tautomers, stereoisomers, pharmaceutically acceptable salts and pro-drugs thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy wherein a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); a C3-5 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or an aryl group optionally substituted by one or more (e.g.
    Type: Grant
    Filed: June 19, 2019
    Date of Patent: March 12, 2024
    Assignees: OSLO UNIVERSITETSSYKEHUS HF, FORSCHUNGSVERBUND BERLIN E.V., UNIVERSITY OF OULU
    Inventors: Stefan Krauss, Marc Nazare, Lari Lehtio, Jo Waaler, Anita Wegert, Ruben Gerardus George Leenders
  • Publication number: 20230322721
    Abstract: The present invention relates to compounds of general formula (I), tautomers, stereoisomers, N-oxides, pharmaceutically acceptable salts and pro-drug thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy: wherein: a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); a C3-5 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or an aryl group optionally substituted by one or more (e.g.
    Type: Application
    Filed: July 6, 2021
    Publication date: October 12, 2023
    Inventors: Stefan KRAUSS, Jo WAALER, Anita WEGERT, Ruben Gerardus George LEENDERS, Lari LEHTIO
  • Publication number: 20210269419
    Abstract: The present invention relates to compounds of formula (I), tautomers, stereoisomers, pharmaceutically acceptable salts and pro-drugs thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy wherein a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); a C3-5 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or an aryl group optionally substituted by one or more (e.g.
    Type: Application
    Filed: June 19, 2019
    Publication date: September 2, 2021
    Inventors: Stefan KRAUSS, Marc NAZARE, Lari LEHTIO, Jo WAALER, Anita WEGERT, Ruben Gerardus George LEENDERS
  • Patent number: 9388156
    Abstract: The invention relates to novel compounds that are useful for modulating mitochondrial morphology and/or expression of OXPHOS enzymes and/or cellular ROS. The compounds are derivatives of TroloxrM wherein the carboxylic acid moiety is replaced by an amide moiety and wherein the nitrogen atom of the amide moiety is connected via a linker to a cationic nitrogen atom. The compounds of the invention are formulated into pharmaceutical or cosmetic compositions. The invention further relates to methods wherein the compounds of the invention are used for treating or preventing mitochondrial disorders, conditions associated with mitochondrial dysfunction, including adverse drug effects, and/or neoplastic diseases. The invention also relates to cosmetic methods for treating or delaying further aging of the skin and veterinary applications.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: July 12, 2016
    Assignee: Khondiron IP B.V.
    Inventors: Richard Hendrik Blaauw, Ruben Gerardus George Leenders, Geert Jan Sterk, Pedro Harold Han Hermkens
  • Publication number: 20150166501
    Abstract: The invention relates to novel compounds that are useful for modulating mitochondrial morphology and/or expression of OXPHOS enzymes and/or cellular ROS. The compounds are derivatives of TroloxrM wherein the carboxylic acid moiety is replaced by an amide moiety and wherein the nitrogen atom of the amide moiety is connected via a linker to a cationic nitrogen atom. The compounds of the invention are formulated into pharmaceutical or cosmetic compositions. The invention further relates to methods wherein the compounds of the invention are used for treating or preventing mitochondrial disorders, conditions associated with mitochondrial dysfunction, including adverse drug effects, and/or neoplastic diseases. The invention also relates to cosmetic methods for treating or delaying further aging of the skin and veterinary applications.
    Type: Application
    Filed: July 12, 2013
    Publication date: June 18, 2015
    Applicant: Khondrion IP B.V.
    Inventors: Richard Hendrik Blaauw, Ruben Gerardus George Leenders, Geert Jan Sterk, Pedro Harold Han Hermkens
  • Patent number: 8026245
    Abstract: The present invention relates to the use of a compound of formula (I) for the manufacture of a medicament for the prevention or the treatment of HIV infection wherein the compound of formula (I) is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A and B each represents a radical of formula and wherein —C-D- represents a bivalent radical of formula —N?CH—NR17—??(c-1); or —NR17—CH?N—??(c-2); provided that when A represents a radical of formula (a) then B represents a radical of formula (b) and when A represents a radical of formula (b) then B represents a radical of formula (a).
    Type: Grant
    Filed: September 21, 2004
    Date of Patent: September 27, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative, Paulus Joannes Lewi, Marc René de Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Jan Heeres, Hendrik Maarten Vinkers, Ruben Gerardus George Leenders, Dirk Alfons Leo Vandenput
  • Patent number: 7705148
    Abstract: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
    Type: Grant
    Filed: February 14, 2008
    Date of Patent: April 27, 2010
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Didier Philippe Robert Schils, Joannes Josephus Maria Willems, Bart Petrus Anna Maria Jozef Medaer, Elisabeth Therese Jeanne Pasquier, Paul Adriaan Jan Janssen, Jan Heeres, Ruben Gerardus George Leenders, Jérôme Emile Georges Guillemont
  • Patent number: 7585861
    Abstract: The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 5, 2004
    Date of Patent: September 8, 2009
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Jozef Herwig Arts, legal representative, Marc René de Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Ruben Gerardus George Leenders, Georges Joseph Cornelius Hoomaert, Amuri Kilonda, Donald William Ludovici
  • Patent number: 7563922
    Abstract: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) ?in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) ?with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: July 21, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Didier Philippe Robert Schils, Joannes Josephus Maria Willems, Bart Petrus Anna Maria Jozef Medaer, Elisabeth Therese Jeanne Pasquier, Paul Adriaan Jan Janssen, Jan Heeres, Ruben Gerardus George Leenders, Jérôme Emile Georges Guillemont
  • Patent number: 7399856
    Abstract: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) ?in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) ?with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
    Type: Grant
    Filed: August 7, 2003
    Date of Patent: July 15, 2008
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Didier Philippe Robert Schils, Joannes Josephus Maria Willems, Bart Petrus Anna Maria Jozef Medaer, Elisabeth Therese Jeanne Pasquier, Paul Adriaan Jan Janssen, Jan Heeres, Ruben Gerardus George Leenders, Jérôme Emile Georges Guillemont
  • Publication number: 20080167464
    Abstract: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
    Type: Application
    Filed: February 14, 2008
    Publication date: July 10, 2008
    Inventors: Didier Philippe Robert Schils, Joannes Josephus Maria Willems, Bart Petrus Anna Maria Jozef Medaer, Elisabeth Therese Jeanne Pasquier, Paul Adriaan Jan Janssen, Jan Heeres, Ruben Gerardus George Leenders, Jerome Emile Georges Guillemont
  • Patent number: 7276510
    Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, provided that when Q is halo then Z is N; or when Q is polyhaloC1-6alkyl then Y is hydrogen or C1-6alkyl; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 3, 2001
    Date of Patent: October 2, 2007
    Assignee: Janssen Pharmaceutica, Inc.
    Inventors: Michael Joseph Kukla, Donald William Ludovici, Robert William Kavash, Bart Lieven Daniel De Corte, Jan Heeres, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Marc René de Jonge, Koen Jeanne Alfons Van Aken, Alain Krief, Ruben Gerardus George Leenders
  • Publication number: 20030171374
    Abstract: This invention concerns HIV replication inhibitors of formula 1
    Type: Application
    Filed: November 8, 2002
    Publication date: September 11, 2003
    Inventors: Michael Joseph Kukla, Donald William Ludovici, Robert William Kavash, Bart Lieven Daniel De Corte, Jan Heeres, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Marc Rene de Jonge, Koen Jeanne Alfons Van Aken, Alain Krief, Ruben Gerardus George Leenders