Patents by Inventor Jan Heeres

Jan Heeres 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).

  • Publication number: 20160296519
    Abstract: This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.
    Type: Application
    Filed: June 13, 2016
    Publication date: October 13, 2016
    Inventors: Lieven Elvire Colette BAERT, Paulus Joannes LEWI, Jan HEERES
  • Patent number: 9365776
    Abstract: The present invention relates to a process for the hydrotreatment of a vegetal biomass. Specifically, the present invention relates to a process for the hydrotreatment of a vegetal biomass comprising: a) subjecting said vegetal biomass to a hydrotreatment in a first reactor, said hydrotreatment comprises contacting said vegetal biomass in an aqueous medium and a metal oxide, a mixed metal oxide, or a metal-metalloid oxide catalyst comprising at least 35% by weight of metal oxide, mixed metal oxide, or metal-metalloid oxide relative to the total weight of the catalyst, with hydrogen at a pressure in the range of 10 to 400 bar and at a temperature in the range of 50° C. to 300° C. until a predetermined level of the hydrotreatment of said biomass is obtained and wherein the metal oxide, a mixed metal oxide, or a metal-metalloid oxide catalyst comprises nickel. Further, the present invention relates to a metal oxide, mixed metal oxide or metal-metalloid oxide catalyst.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: June 14, 2016
    Assignee: BTG BIOMASS TECHNOLOGY GROUP B.V.
    Inventors: Robertus Hendrikus Venderbosch, Agnes Retno Ardiyanti, Hero Jan Heeres, Vadim Yakovlev, Dmitry Ermakov, Sofia Khromova, Valentin Parmon
  • Publication number: 20160151276
    Abstract: This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.
    Type: Application
    Filed: February 5, 2016
    Publication date: June 2, 2016
    Inventors: Lieven Elvire Colette BAERT, Paulus Joannes LEWI, Jan HEERES
  • Patent number: 9199961
    Abstract: The present invention relates to a method for preparing caprolactone, comprising converting 5-hydroxymethyl-2-furfuraldehyde by hydrogenation into at least one intermediate compound selected from the group of 2,5-tetrahydrofuran-dimethanol, 1,6-hexanediol and 1,2,6-hexanetriol, and preparing caprolactone from said intermediate compound. Further, the invention relates to a method for preparing 1,2,6-hexanetriol comprising preparing 5-hydroxymethyl-2-furfaldehyde from a renewable source, converting 5-hydroxymethyl-2-furfaldehyde into 2,5-tetrahydrofuran-dimethanol and converting 2,5-tetrahydrofuran-dimethanol into 1,2,6-hexanetriol. Further, the invention relates to a method for preparing 1,6-hexanediol from 1,2,6-hexanetriol, wherein 1,2,6-hexanetriol is subjected to a ring closure reaction, thereby forming (tetrahydro-2H-pyran-2-yl)methanol, and the (tetrahydro-2H-pyran-2-yl)methanol is hydrogenated, thereby forming 1,6-hexane diol.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: December 1, 2015
    Assignee: NEDERLANDSE ORGANISATIE VOOR WETENSCHAPPELIJK ONDERZOEK (NWO)
    Inventors: Johannes Gerardus De Vries, Teddy, Pim Huat Phua, Ignacio Vladimiro Melián Cabrera, Hero Jan Heeres
  • Publication number: 20150126510
    Abstract: The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.
    Type: Application
    Filed: March 18, 2013
    Publication date: May 7, 2015
    Applicants: Universiteit Antwerpen, Shakturana CV
    Inventors: Jan Heeres, Koen Augustyns, Pieter Van Der Veken, Jurgen Joossens, Venkatraj Muthusamy, Kevin Karel Florentina Arien, Guido Louis Emile Vanham, Paulus Lewi (deceased)
  • Patent number: 8946248
    Abstract: HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is —CH2—CH2—, —CH?CH—, —C?C—; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, R2 hydroxy, halo, C1-6alkyl, carboxyl, cyano, —C(?O)R6, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl; X1 is —NR1—, —O—, —S—, —S(?O)p—; R3 is H, C1-6alkyl, halo; R4 is H, C1-6alkyl, halo; R5 is nitro, amino, mono- and diC1-4alkylamino, aryl, halo, —CHO, —CO—R6, —COOR7, —NH—C(?O)H, —NH—C(?O)R6, —CH?N—O—R8; R6 is C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or polyhaloC1-4alkyl; R7 is hydrogen, C1-6alkyl, arylC1-6alkyl; R8 is hydrogen, C1-6alkyl, aryl; p is 1 or 2; aryl is optionally substituted phenyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.
    Type: Grant
    Filed: September 29, 2005
    Date of Patent: February 3, 2015
    Assignee: Janssen R&D Ireland
    Inventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
  • Publication number: 20140343006
    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, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Inventors: Jerome Emile Georges Guillemont, Patrice Palandijian, Marc Rene DeJonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desire Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
  • Publication number: 20140323488
    Abstract: The present invention relates to novel compounds (I) containing two disubstituted triazine rings covalently linked by an organic linker, thereby creating dimers. These compounds show activity against the causative infective agents of infectious diseases such as African trypanosomiasis, Chagas disease, Leishmaniasis, Malaria and HIV. The invention further relates to the prevention and/or treatment of these diseases.
    Type: Application
    Filed: November 9, 2012
    Publication date: October 30, 2014
    Inventors: Venkatraj Muthusamy, Louis Maes, Jan Heeres, Koen Augustyns, Pieter Van Der Veken, Jurgen Joossens, Paulas Joannes Lewi
  • Publication number: 20140305358
    Abstract: In a carpet manufacturing method, for a plurality of yarns each having a length, a plurality of marks are provided on each yarn at selected locations along the yarn. In the carpet manufacturing method and in a carpet manufacturing assembly, each yarn is stored on or in an associated storage, and fed from its associated storage to a carpet manufacturing apparatus. For each yarn, the marks on the yarn are detected upstream of the carpet manufacturing apparatus. On the basis of the detection of the marks, the uptake of the yarn by the carpet manufacturing apparatus is controlled, whereafter, in the carpet manufacturing apparatus, the yarns are processed to form at least part of a carpet.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 16, 2014
    Inventor: Robert Jan Heeres
  • Patent number: 8828982
    Abstract: This invention concerns the use of a compound for the manufacture of a medicament for the prevention of HIV infection via sexual intercourse and related intimate contact between partners, wherein the compound is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: September 9, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Paulus Joannes Lewi, Marc René de Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Jéròme Emile Georges Guillemont, Elisabeth Therese Jeanne Pasquier, Frank Xavier Jozef Herwig Arts
  • Patent number: 8575342
    Abstract: Compounds of formula (I), N-oxides, pharmaceutical acceptable salts, quaternary amines or stereoisomeric forms thereof, and their use as HIV replication inhibitors, In the formula, -a1=a2-a3=a4- and -b1=b2-b3=b4- may be —C?C—C?C—; X1 may be O, NR1, etc.; R1, R2, R2a, R3, R4 and R5 are assorted substituents as defined in the specification.
    Type: Grant
    Filed: September 29, 2005
    Date of Patent: November 5, 2013
    Assignee: Tibotech Pharmaceuticals Ltd.
    Inventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
  • Patent number: 8530655
    Abstract: This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substitut
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: September 10, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Chih Yung Ho, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, Koenraad Jozef Lodewijk Marcel Andries, Frank Xavier Jozef Herwig Arts
  • Publication number: 20130219774
    Abstract: The present invention relates to a process for the hydrotreatment of a vegetal biomass. Specifically, the present invention relates to a process for the hydrotreatment of a vegetal biomass comprising: a) subjecting said vegetal biomass to a hydrotreatment in a first reactor, said hydrotreatment comprises contacting said vegetal biomass in an aqueous medium and a metal oxide, a mixed metal oxide, or a metal-metalloid oxide catalyst comprising at least 35% by weight of metal oxide, mixed metal oxide, or metal-metalloid oxide relative to the total weight of the catalyst, with hydrogen at a pressure in the range of 10 to 400 bar and at a temperature in the range of 50° C. to 300° C. until a predetermined level of the hydrotreatment of said biomass is obtained and wherein the metal oxide, a mixed metal oxide, or a metal-metalloid oxide catalyst comprises nickel. Further, the present invention relates to a metal oxide, mixed metal oxide or metal-metalloid oxide catalyst.
    Type: Application
    Filed: August 30, 2011
    Publication date: August 29, 2013
    Applicant: BTG BIOMASS TECHNOLOGY GROUP B.V.
    Inventors: Robertus Hendrikus Venderbosch, Agnes Retno Ardiyanti, Hero Jan Heeres, Vadim Yakovlev, Dmitry Ermakov, Sofia Khromova, Valentin Parmon
  • Publication number: 20130137863
    Abstract: The present invention relates to a method for preparing caprolactone, comprising converting 5-hydroxymethyl-2-furfuraldehyde by hydrogenation into at least one intermediate compound selected from the group of 2,5-tetrahydrofuran-dimethanol, 1,6-hexanediol and 1,2,6-hexanetriol,and preparing caprolactone from said intermediate compound. Further, the invention relates to a method for preparing 1,2,6-hexanetriol comprising preparing 5-hydroxymethyl-2-furfaldehyde from a renewable source, converting 5-hydroxymethyl-2-furfaldehyde into 2,5-tetrahydrofuran-dimethanol and converting 2,5-tetrahydrofuran-dimethanol into 1,2,6-hexanetriol. Further, the invention relates to a method for preparing 1,6-hexanediol from 1,2,6-hexanetriol, wherein 1,2,6-hexanetriol is subjected to a ring closure reaction, thereby forming (tetrahydro-2H-pyran-2-yl)methanol, and the (tetrahydro-2H-pyran-2-yl)methanol is hydrogenated, thereby forming 1,6-hexane diol.
    Type: Application
    Filed: March 23, 2011
    Publication date: May 30, 2013
    Applicant: NEDERLANDSE ORGANISATIE VOOR WETENSCHAPPELIJK ONDERZOEK (NWO)
    Inventors: Johannes Gerardus De Vries, Teddy, Pim Huat Phua, Ignacio Vladimiro Melián Cabrera, Hero Jan Heeres
  • Publication number: 20120190697
    Abstract: HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH?N—NH—C(?O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted
    Type: Application
    Filed: March 2, 2012
    Publication date: July 26, 2012
    Inventors: Jerôme Emile Georges GUILLEMONT, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
  • Patent number: 8153640
    Abstract: HIV replication inhibitors of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0, 1, 2, 3 and in certain cases also 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6
    Type: Grant
    Filed: October 27, 2005
    Date of Patent: April 10, 2012
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
  • Publication number: 20120076835
    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; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 30, 2011
    Publication date: March 29, 2012
    Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts
  • Patent number: 8080551
    Abstract: HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: December 20, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
  • Publication number: 20110263625
    Abstract: This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C3-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substitut
    Type: Application
    Filed: July 6, 2011
    Publication date: October 27, 2011
    Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, Koenraad Jozef Lodewijk Marcel Andries, Frank Xavier Jozef Herwig Arts
  • Patent number: 8026248
    Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxy-carbonyl; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 ar
    Type: Grant
    Filed: April 21, 2005
    Date of Patent: September 27, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken