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).

  • Patent number: 7034019
    Abstract: 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 formula
    Type: Grant
    Filed: May 3, 2001
    Date of Patent: April 25, 2006
    Assignee: Janssen Pharmaceutica N.V.
    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
  • Publication number: 20060063789
    Abstract: 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 represents 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 O or S; 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; —C(?O)NHNH2; R7—C(?O)—NH—;
    Type: Application
    Filed: October 29, 2002
    Publication date: March 23, 2006
    Inventors: Eddy Jean Freyne, Peter Antonius, Marc Willems, Werner Johan, Paul Janssen, Paulus Joannes, Jan Heeres, Marc de Jonge, Lucien Koymans, Frederik Daeyaert, Michael Kukla, Hugo Gabriel, Bony Nuydens, Marc Mercken, Donald Ludovici, Herwig Janssen, Paul Maria, Graziella Janssen, Jasmine Werner, Maroussia Janssen, Theodora Arts
  • Patent number: 7015221
    Abstract: This invention concerns the use of the 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 or substituted C1-6alkyl; 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(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR4, —NH—S(?O)pR4, —C(?O)R4, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R4, —C(?NH)R4 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 substituted phenyl, pyridinyl, pyrimidinyl, pyra
    Type: Grant
    Filed: August 27, 2003
    Date of Patent: March 21, 2006
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
  • Publication number: 20060009474
    Abstract: 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 formula
    Type: Application
    Filed: September 13, 2005
    Publication date: January 12, 2006
    Inventors: Michael Kukla, Donald Ludovici, Robert Kavash, Bart De Corte, Jan Heeres, Paul Janssen, Lucien Koymans, Marc de Jonge, Koen Van Aken, Alain Krief
  • Publication number: 20050288278
    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, C1-6alkyloxy-carbonyl, 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(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —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 subst
    Type: Application
    Filed: August 16, 2005
    Publication date: December 29, 2005
    Inventors: Bart De Corte, Marc De Jonge, Jan Heeres, Chih Ho, Paul Janssen, Robert Kavash, Lucien Koymans, Michael Kukla, Donald Ludovici, Koen Van Aken
  • Publication number: 20050277641
    Abstract: This invention concerns the use of the 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 or substituted C1-6alkyl; 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(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR4, —NH—S(?O)pR4, —C(?O)R4, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R4, —C(?NH)R4 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 substituted phenyl, pyridinyl, pyrimidinyl, pyra
    Type: Application
    Filed: August 27, 2003
    Publication date: December 15, 2005
    Inventors: Bart De Corte, Marc de Jonge, Jan Heeres, Paul Janssen, Robert Kavash, Lucien Koymans, Michael Kukla, Donald Ludovici, Koen Van Aken
  • Patent number: 6962916
    Abstract: 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, C1-6alkyloxycarbonyl, 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 of s
    Type: Grant
    Filed: March 26, 2003
    Date of Patent: November 8, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Paul A. J. Janssen, Jan Heeres, Henri E. L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
  • Publication number: 20050197354
    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.
    Type: Application
    Filed: April 21, 2005
    Publication date: September 8, 2005
    Inventors: Koenraad Jozef Andries, Bart De Corte, Marc De Jonge, Jan Heeres, Chih Ho, Marcel Janssen, Paul Janssen, Lucien Koymans, Michael Kukla, Donald Ludovici, Koen Van Aken
  • Publication number: 20050192305
    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
    Type: Application
    Filed: April 21, 2005
    Publication date: September 1, 2005
    Inventors: Koenraad Jozef Andries, Bart De Corte, Marc De Jonge, Jan Heeres, Chih Ho, Marcel Janssen, Paul Janssen, Lucien Koymans, Michael Kukla, Donald Ludovici, Koen Van Aken
  • Publication number: 20050176713
    Abstract: 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 represents 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 O or S; 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; —C(?O)NHNH2; R7—C(?O)—NH—;
    Type: Application
    Filed: October 29, 2002
    Publication date: August 11, 2005
    Inventors: Eddy Jean Freyne, Peter Jacobus Johannes Buijnsters, Marc Willems, Werner Constant Embrechts, Jean Fernand Lacrampe, Paul Adriaan Janssen, Herwig Josephus Janssen, Paul Janssen, Graziella Janssen, Jasmine Janssen, Maroussia Godelieve Janssen, Theodora Joanna Arts, Paulus Lewi, Jan Heeres, Marc de Jonge, Lucien Maria Koymans, Frederik Frans Daeyaert, Rony Nuydens, Marc Mercken
  • Patent number: 6903213
    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, C16alkyloxy-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
    Type: Grant
    Filed: June 28, 2002
    Date of Patent: June 7, 2005
    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
  • Patent number: 6878717
    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, C1-6alkyloxy-carbonyl, 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(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —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 subs
    Type: Grant
    Filed: November 1, 1999
    Date of Patent: April 12, 2005
    Inventors: Bart De Corte, Marc Rene 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
  • Patent number: 6858609
    Abstract: 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(3H7)-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 o
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: February 22, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Paul A. J. Janssen, Jan Heeres, Henri E. L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
  • Publication number: 20050004125
    Abstract: 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; —
    Type: Application
    Filed: October 29, 2002
    Publication date: January 6, 2005
    Inventors: Eddy Jean Edgard Freyne, Peter Jacobus Buijnsters, Marc Willems, Werner Embrechts, Christopher Love, Paul Janssen, Paulus Lewi, Jan Heeres, Marc de Jonge, Lucien Koymans, Hendrik Vinkers, Koen Van Aken, Gaston Diels
  • Publication number: 20040198739
    Abstract: 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, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents pheynl, 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; 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)NHNH?2?, —NHC(═O)R6, —C(═NH)R6 or a 5-membered hetrocycl; X1 is —NR5—,
    Type: Application
    Filed: February 3, 2004
    Publication date: October 7, 2004
    Inventors: Jerome Emile Georges Guillemont, Patrice Palandjian, Marc Rene de Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desire Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen
  • Patent number: 6774235
    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, 1, 2, 3 or 4; R1 and R2 are each independently 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 of the aforementioned C1-12alkyl groups may optionally and each individually 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; and each R4 independently is hydroxy, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is —X—R5 or —X—Alk—R6; wherein R5 and R6 each independently are indanyl, indolyl or phen
    Type: Grant
    Filed: February 5, 2002
    Date of Patent: August 10, 2004
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frederik Frans Desiré Daeyaert, 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
  • Publication number: 20040102456
    Abstract: This invention concerns a compound of formula 1
    Type: Application
    Filed: August 20, 2003
    Publication date: May 27, 2004
    Inventors: Paul Adriaan Jan Janssen, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Lucien Maria Henricus Koymans, Marc Rene de Jonge, Jan Heeres, Frederik Frans Desire Daeyaert, Georges Joseph Cornelius Hoornaert, Frans Joseph Cornelius Compernolle, Amuri Kilonda
  • Patent number: 6703506
    Abstract: The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts thereof and stereochemically isomeric forms thereof, wherein —A—B— forms a bivalent radical of formula —N═CH— (a), —CH═N— (b), —CH═CH— (c), L represents the acyl moiety of an amino acid; D is an azole containing 1,3- or 1,4-dioxolane derivative as broad-spectrum antifungals; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: November 15, 2002
    Date of Patent: March 9, 2004
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Lieven Meerpoel, Jan Heeres, Robert Jozef Maria Hendrickx
  • Publication number: 20040039005
    Abstract: This invention concerns the use of compounds of formula 1
    Type: Application
    Filed: August 5, 2003
    Publication date: February 26, 2004
    Inventors: Bart De Corte, Marc Rene 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
  • Patent number: 6638932
    Abstract: This invention concerns the use of the 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 or substituted C1-6alkyl; 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(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR4, —NH—S(═O)pR4, —C(═O)R4, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R4, —C(═NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alk
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: October 28, 2003
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken