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).
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Patent number: 8026245Abstract: 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: GrantFiled: September 21, 2004Date of Patent: September 27, 2011Assignee: 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
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Patent number: 8003789Abstract: This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 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(C1-6alkyl)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, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halType: GrantFiled: October 31, 2007Date of Patent: August 23, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7923554Abstract: The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(?O)pR6; —NH—S(?O)pR6; —C(?O)R6; —NHC(?O)H; —C(?O)NHNH2; NHC(?O)R6; C(?NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14; —C(?O)—NHR13; —C(?O)—NR13R1Type: GrantFiled: August 10, 2005Date of Patent: April 12, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Georges Joseph Cornelius Hoornaert, Amuri Kilonda, Jan Heeres, Paulus Joannes Lewi, Marc René de Jonge, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Lucien Maria Henricus Koymans, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
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Publication number: 20110077261Abstract: 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: ApplicationFiled: December 6, 2010Publication date: March 31, 2011Inventors: Lieven Elvire Colette Baert, Paulus Joannes Lewi, Jan Heeres
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Patent number: 7763631Abstract: The present invention concerns compounds of formula (A1)(A2)N—R1 (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(?O)—R8; —S(?O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formulaType: GrantFiled: September 13, 2005Date of Patent: July 27, 2010Assignee: Janssen Pharmaceutica NVInventors: 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
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Patent number: 7705148Abstract: 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: GrantFiled: February 14, 2008Date of Patent: April 27, 2010Assignee: 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
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Publication number: 20100034810Abstract: 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)pR6Type: ApplicationFiled: September 25, 2009Publication date: February 11, 2010Inventors: Jan HEERES, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, Marc Rene de Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desire Daeyaert, Hendrik Maarten Vinkers, Jerome Emile Georges Gullemont, Elisabeth Theresa Jeanne Pasquier
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Publication number: 20090298141Abstract: The invention relates to the use of a centrifugal contact-separator for carrying out a non-radioactive reaction in a liquid-liquid emulsion formed from two immiscible liquids. The invention also relates to a process for carrying out a reaction in a centrifugal contact-separator, and to a process for carrying out a catalytic reaction in a centrifugal contact-separator. An example of a process for carrying out a reaction, comprising the following steps: i) continuously introducing a liquid phase A and a liquid phase B into at least one first centrifugal contact separator, where in liquid phases A and B are immiscible and wherein phase A and/or phase B comprise at least one reactant ii) mixing phase A and phase B thereby allowing an emulsion to be formed iii) applying a centrifugal force that allows phase separation of the emulsion, such that phases A? and B? are obtained; iv) optionally, recovering a reaction product from at least one or the phases A? and B?.Type: ApplicationFiled: September 15, 2006Publication date: December 3, 2009Applicant: DSM IP Assets B.V.Inventors: Johannes Gerardus De Vries, Gerald Jan Kwant, Hero Jan Heeres
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Patent number: 7585861Abstract: 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: GrantFiled: February 5, 2004Date of Patent: September 8, 2009Assignee: 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
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Patent number: 7585870Abstract: This invention concerns HIV replication inhibitors of formula (I), 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: GrantFiled: February 20, 2004Date of Patent: September 8, 2009Assignee: Tibotec BVBAInventors: Jerôme Emile Georges Guillemont, Elisabeth Thérese Jeanne Pasquier, Jan Heeres, Kurt Hertogs, Eva Bettens, Paulus Joannes Lewi, Marc René De Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Frank Xavier Jozef Herwig Arts
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Patent number: 7563922Abstract: 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: GrantFiled: April 23, 2007Date of Patent: July 21, 2009Assignee: 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
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Publication number: 20090181993Abstract: HIV replication inhibitors of formula (I), 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—; 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)—R10; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C1-6alkenyl or C2-6 alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X3—R3; X1 is —NR1—, —O—, —C(?O)—, —CH2—, —CHOH—, —S—, —S(?O)p—R3 is CN; amino; C1-6alkyl; halo; optionally substitutedType: ApplicationFiled: September 29, 2005Publication date: July 16, 2009Inventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
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Publication number: 20090124644Abstract: HIV replication inhibitors of formula pharmaceutically acceptable addition salts or stereochemically isomeric forms thereof, wherein X is NR4, S, SO or SO2; the preparation of these compounds as well as pharmaceutical compositions comprising these compounds; the use of these compounds for the prevention or the treatment of HIV infection.Type: ApplicationFiled: January 27, 2006Publication date: May 14, 2009Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Jan Heeres, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, Rudolf Leemans, Luc Jozef Raphael Moens
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Patent number: 7531548Abstract: HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a 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—; 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)rR6; C(?NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C2-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 is —NR1—, —O—, —C(?O)—, CH2, —CHOH—, —S—, —S(?O)r—; R3 is CN; amino; C1-6alkyl; halo; optionally subsType: GrantFiled: September 29, 2005Date of Patent: May 12, 2009Assignee: Tibotec Pharmaceuticals LtdInventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
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Patent number: 7514445Abstract: This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(?O)—; R21—S(?O)p—; R7—S(?O)p—; R7—S(?O)p—NH—; R21—S(?O)p—NH—; R7—C(?O)—; —NHC(?O)H; —CType: GrantFiled: October 29, 2002Date of Patent: April 7, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy Jean Edgard Freyne, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Werner Constant Johan Embrechts, Christopher John Love, Paul Adriaan Jan Janssen, Paulus Joannes Lewi, Jan Heeres, Marc René de Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Koen Jeanne Alfons Van Aken, Gaston Stanislas Marcella Diels
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Publication number: 20090012092Abstract: The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(?O)pR6; —NH—S(?O)pR6; —C(?O)R6; —NHC(?O)H; —C(?O)NHNH2; NHC(?O)R6; C(?NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14 —C(?O)—NHR13; —C(?O)—NR13 R1Type: ApplicationFiled: August 10, 2005Publication date: January 8, 2009Inventors: Georges Joseph Cornelius Hoornaert, Amuri Kilonda, Jan Heeres, Paulus Joannes Lewi, Marc Rene de Jonge, Frederik Frans Desire Daeyaert, Hendrik Maarten Vinkers, Lucien Maria Henricus Koymans, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts
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Publication number: 20080287511Abstract: The present invention relates to the novel anthelmintic compound tetrahydro-furan-2-carboxylic acid-[3-(2,3,5,6-tetrahydro-imidazo[2,1-b]thiazol-6-yl)-phenyl]-amide and the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, as well as pharmaceutical compositions comprising said novel compound, processes for preparing said compound and compositions, and the use thereof as a medicine, in particular in treatment, control and prevention of endo- and ectoparasite infections in warm-blooded animals.Type: ApplicationFiled: January 26, 2006Publication date: November 20, 2008Inventors: Jan Heeres, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Kathleen Marie Jeanne Alice Vlaminck, Pierre Josef Hektor Valere Ottevaere, Oscar Franz Joseph Vanparijs, Frank Xavier Jozef Herwig Arts
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Patent number: 7449575Abstract: This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H)-furanone; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1 is optionally substituted phenyl; for the manufacture of a medicine for the treatment ofType: GrantFiled: August 12, 2005Date of Patent: November 11, 2008Assignee: Janssen Pharmaceutica, Inc.Inventors: Paul A. J. Janssen, Jan Heeres, Henri E. L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
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Patent number: 7442705Abstract: This invention concerns HIV replication inhibitors of formula (I), 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: GrantFiled: February 20, 2004Date of Patent: October 28, 2008Assignee: Tibotec Pharmaceuticals LtdInventors: Jerôme Emile Georges Guillemont, Elisabeth Thérese Jeanne Pasquier, Jan Heeres, Kurt Hertogs, Eva Bettens, Paulus Joannes Lewi, Marc René De Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Frank Xavier Jozef Herwig, legal representative, Paul Adriaan Jan Janssen
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Publication number: 20080262007Abstract: 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: ApplicationFiled: September 29, 2005Publication date: October 23, 2008Inventors: Jerome Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi