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: 20030199473
    Abstract: This invention concerns the compounds of formula 1
    Type: Application
    Filed: March 26, 2003
    Publication date: October 23, 2003
    Applicant: Janssen Pharmaceutica N.V.
    Inventors: Paul A.J. Janssen, Jan Heeres, Henri E.L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
  • Publication number: 20030186990
    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 1
    Type: Application
    Filed: November 7, 2002
    Publication date: October 2, 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
  • 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
  • Publication number: 20030158210
    Abstract: The present invention concerns novel compounds of formula 1
    Type: Application
    Filed: November 15, 2002
    Publication date: August 21, 2003
    Inventors: Lieven Meerpoel, Jan Heeres, Robert Jozef Maria Hendrickx
  • Publication number: 20030114472
    Abstract: This invention concerns the use of compounds of formula 1
    Type: Application
    Filed: November 1, 1999
    Publication date: June 19, 2003
    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
  • Publication number: 20030083317
    Abstract: This invention concerns the use of the compounds of formula 1
    Type: Application
    Filed: June 28, 2002
    Publication date: May 1, 2003
    Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc Rene 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: 6512116
    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: May 4, 2001
    Date of Patent: January 28, 2003
    Assignee: Janssen Pharmaceutica NV
    Inventors: Lieven Meerpoel, Jan Heeres, Robert Jozef Maria Hendrickx
  • Publication number: 20020147181
    Abstract: This invention concerns the compounds of formula 1
    Type: Application
    Filed: November 15, 2001
    Publication date: October 10, 2002
    Inventors: Paul A.J. Janssen, Jan Heeres, Henri E.L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
  • Patent number: 6440440
    Abstract: This invention concerns compounds of formula. stereochemically isomeric forms thereof, acid or base addition salts thereof, N-oxides thereof, or quaternary ammonium derivatives thereof, wherein the dotted line is an optional bond; X is a direct bond when the dotted line represents a bond, or X is hydrogen or hydroxy, when the dotted line does not represent a bond; R1, R2, R5 and R6 are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, —SO3H, and the like; R3 and R4 are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, nitro, amino, cyano, trifluoromethyl, or trifluoromethoxy; L is a radical of formula wherein A1 is a direct bond or C1-6alkanediyl; A2 is C2-6alkanediyl; and R7 to R11 are hydrogen, C1-6alkyl, aminoC1-6alkyl and the like; having biocidal properties; their preparation, compositions containing them and their use as a biocide.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: August 27, 2002
    Inventors: Lieven Meerpoel, Mark Arthur Josepha Van der Flaas, Louis Jozef Elisabeth Van Der Veken, Jan Heeres
  • Patent number: 6440986
    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, C1-6alkyloxycarbonyl,; 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
    Type: Grant
    Filed: December 27, 2000
    Date of Patent: August 27, 2002
    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
  • Publication number: 20020115668
    Abstract: This invention concerns the use of the compounds of formula 1
    Type: Application
    Filed: February 5, 2002
    Publication date: August 22, 2002
    Inventors: Frederik Frans Desire Daeyaert, 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
  • Patent number: 6387906
    Abstract: The present invention concerns novel compounds of formula a N-oxide form, a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein n is zero, 1, 2 or 3; X is N or CH; each R1 independently is halo, nitro, cyano, amino, hydroxy, C1-4alkyl, C1-4alkyloxy or trifluoromethyl; R2 is hydrogen; C3-7alkenyl; C3-7alkynyl, aryl; C3-7cycloalkyl; optionally substituted C1-6alkyl R3 and R4 each independently are hydrogen, C1-6alkyl, C3-7cycloalkyl or aryl; or R3 and R4 taken together form a bivalent radical —R3—R4— of formula: wherein R5a, R5b, R5c, R5d each independently are hydrogen, C1-6alkyl or aryl; and aryl is optionally substituted phenyl; as antifungals; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: January 7, 2000
    Date of Patent: May 14, 2002
    Inventors: Lieven Meerpoel, Jan Heeres, Frank Christopher Odds, Hugo Florent Adolf Vanden Bossche, Louis Jozef Elisabeth Van der Veken
  • Patent number: 6384030
    Abstract: The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein L represent a radical of formula wherein each Alk independently represents an optionally substituted C1-6alkanediyl; is 1, 2 or 3; Y is O, S or NR2; R1 represents hydrogen, aryl, Het1, or an optionally substituted C1-6alkyl; each R2 independently represents hydrogen or C1-6alkyl; or in case R1 and R2 are attached to the same nitrogen atom, they may be taken together to form a heterocyclic radical; or they may be taken together to form an azido radical; each R3 independently represents hydrogen, hydroxy or C1-4alkyloxy; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; Het1 represents an optionally substituted monocyclic or bicyclic heterocyclic radical; Het2 is the same as Het1 and may also be piperazinyl
    Type: Grant
    Filed: November 9, 2000
    Date of Patent: May 7, 2002
    Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Jan Heeres, Frank Christopher Odds
  • Patent number: 6380194
    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 R1and 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; Ar1is optionally substituted phenyl; for the manufacture of a medicine for the t
    Type: Grant
    Filed: September 26, 1997
    Date of Patent: April 30, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Paul A. J. Janssen, Jan Heeres, Henri E. L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
  • Patent number: 6372729
    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 phenyl; each of
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: April 16, 2002
    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
  • Patent number: 6346518
    Abstract: The present invention is concerned with the stereoisomeric forms of itraconazole (X=Cl) and saperconazole (X=F), which may be represented by the formula and the pharmaceutically acceptable acid addition salt forms thereof, processes for preparing said stereoisomeric forms, the complexes thereof with cyclodextrin derivatives, pharmaceutical compositions comprising said complexes and methods of preparing said complexes and pharmaceutical compositions.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: February 12, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Jean Louis Mesens, Jozef Peeters
  • Publication number: 20010039281
    Abstract: The present invention concerns novel compounds of formula 1
    Type: Application
    Filed: May 4, 2001
    Publication date: November 8, 2001
    Inventors: Lieven Meerpoel, Jan Heeres, Robert Jozef Maria Hendrickx
  • Publication number: 20010011094
    Abstract: This invention concerns the use of the compounds of formula 1
    Type: Application
    Filed: December 27, 2000
    Publication date: August 2, 2001
    Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc Rene 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: 6262052
    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: July 26, 1999
    Date of Patent: July 17, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Lieven Meerpoel, Jan Heeres, Robert Jozef Maria Hendrickx
  • Patent number: 6197972
    Abstract: The present invention concerns novel compounds of formula (I). wherein R1 is C1-10alkyl, C3-7cycloalkyl or C1-6alkyl substituted with C3-7cycloalkyl; R2 is hydrogen or C1-6alkyl; Alk represents C1-3alkanediyl; —A— represents a bivalent radical of formula —CH═CH—N═CH— (a), —N═CH—N═CH— (b), —CH═N—N═CH— (c), —CH═CH—CH═N— (d); in said bivalent radicals a hydrogen atom may be replaced by C1-6alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C1-6alkyl or C1—6alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C1-6alkyl or C1-6alkyloxy; the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: February 17, 1999
    Date of Patent: March 6, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Leo Jacobus Jozef Backx, Paul August Clement Luyts