Patents by Inventor Bart Kesteleyn

Bart Kesteleyn 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: 20070265295
    Abstract: 1-heterocyclyl-1,5-dihydro-pyrido[3,2-b]indol-2-ones of formula (I): the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein n is 1, 2 or 3; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; X is NR2, O, S, SO, SO2; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, which are optionally substituted; R2 is aryl substituted with —COOR4; or R2 is: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b (b-5); -a1=a2-a3=a4- is —CH?CH—CH?CH—; —N?CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N—; wherein hydrogen atoms in (c-1)-(c-5) may be replaced by certain radicals; R3 is a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted.
    Type: Application
    Filed: May 17, 2005
    Publication date: November 15, 2007
    Inventors: Bart Kesteleyn, Pierre Jean-Marie Raboisson, Dominique Surleraux, Geerwin Hache, Sandrine Vendeville, Piet Tom Wigerinck, Annick Peeters
  • Publication number: 20070249655
    Abstract: The present invention concerns combinations comprising a compound of formula (I) the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters or metabolites thereof, wherein n is 1, 2 or 3; R1 is H, CN, halo, aminoC(?O), C(?O)OH, C1-4alkyloxyC(?O), C1-4alkylC(?O), mono- or di(C1-4alkyl)aminoC(?O), arylaminoC(?O), N-(aryl)-N-(C1-4alkyl)aminoC(?O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; R2 is H, C1-4alkyl, C2-10alkenyl, C3-7cycloalkyl, wherein said C1-10alkyl, C2-10alkenyl and C3-7cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxyC(?O), aminoC(?O), C1-4alkyloxyC(?O), mono- or di(C1-4alkyl)aminoC(?O), C1-4alkylC(?O), methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1; and another HIV inhibitor.
    Type: Application
    Filed: May 17, 2005
    Publication date: October 25, 2007
    Inventors: Bart Kesteleyn, Wim Van De Vreken, Natalie Kindermans, Maxime Francis Canard, Kurt Hertogs, Eva Bettens, Veronique De Vroey, Dirk Jochmans, Piet Wigerinck, Abdellah Tahri, Jing Wang, Dominique Louis Surleraux
  • Publication number: 20070238727
    Abstract: Compounds of formula (I) the N-oxides, salts, stereoisomeric forms, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, a carbonyl derivative, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)-methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R2 is (i) aryl substituted with a radical —COOR4; (ii) C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, substituted with aryl which is substituted with a radical —COOR4; (iii) C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, substituted with —NR5a—C(?NR5b)—NR5cR5d, —O—NR5a—C(?NR5b)—NR5cR5d, -sulfonyl-R6, —NR7R8, —NR9R10, a radical (a-1), (a-2), (a-3), (a-4), (a-5); or (iv) a radical of formula: (a-6), (b-2), —CpH2p—CH(OR14)—CqH2q—R15; —CH2—CH2—(O—CH2—CH2)m—OR14; —CH2—CH2—(O—CH2—CH2)m—NR17aR17b; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, a carbonyl derivative, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1.
    Type: Application
    Filed: May 17, 2005
    Publication date: October 11, 2007
    Applicant: Tibotec BVBA
    Inventors: Bart Kesteleyn, Maxime Francis Canard, Wim Van De Vreken, Pierre Jean-Marie Raboisson, Dominique Louis Surleraux, Piet Tom Wigerinck
  • Publication number: 20070213320
    Abstract: 4-substituted 1,5-dihydro-pyrido[3,2-b]indol-2-ones of formula (I): the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein n is 1, 2 or 3; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; X is NR2, O, S, SO, SO2; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, which are optionally substituted; R2 is aryl substituted with —COOR4; or R2 is: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b (b-5); -a1=a2-a3=a4- is —CH?CH—CH?CH—; —N?CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N—; wherein hydrogen atoms in (c-1)-(c-5) may be replaced by certain radicals; R3 is optionally substituted phenyl or a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted; R21 is halo, hydroxy, amino, carboxyl, C1-6alkyl, C3-7cycloalkyl, arylC1-6alkyl, formyl, C1-6alkylcarbonyl, C
    Type: Application
    Filed: May 17, 2005
    Publication date: September 13, 2007
    Inventors: Bart Kesteleyn, Wim Van De Vreken, Dominique Louis Surleraux, Sandrine Vendeville, Pierre Jean-Marie Raboisson, Piet Tom Wigerinck, Annick Peeters
  • Publication number: 20070167434
    Abstract: This invention concerns the compounds the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R2 is hydrogen, aryl substituted with a radical —COOR4; or R2 is substituted C1-10alkyl, C2-20alkenyl or C3-7cycloalkyl; or R is a radical of formula: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b (b-5); -a1=a2-a3=a4- is —CH?CH—CH?CH—; —N?CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N— (c-5); wherein one of the hydrogen atoms in (c-1)-(c-5) is replaced by particular radicals; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, substituted carbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1.
    Type: Application
    Filed: May 17, 2005
    Publication date: July 19, 2007
    Inventor: Bart Kesteleyn
  • Publication number: 20060173000
    Abstract: The present invention concerns the compounds of formula (I) their N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites, wherein n is 1, 2 or 3; R1 is H, CN, halo, aminoC(?O), C(?O)OH, C1-4alkyloxyC(?O), C1-4alkylC(?O), mono- or di(C1-4alkyl)aminoC(?O), arylaminoC(?O), N-(aryl)-N—(C1-4alkyl)aminoC(?O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het, or Het2; R2 is H, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, wherein said C1-10alkyl, C2-10alkenyl and C3-7cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxyC(?O), aminoC(?O), C1-4alkyloxyC(?O), mono- or di(C1-4alkyl)aminoC(?O), C1-4alkylC(?O), methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1; for use as a medicine. The invention further relates to a novel subgroup of the compounds of formula (I), and to compositions comprising compounds of formula (I).
    Type: Application
    Filed: November 14, 2003
    Publication date: August 3, 2006
    Inventors: Bart Kesteleyn, Wim Van De Vreken, Natalie Kindermans, Maxime Francis Canard, Kurt Hertogs, Eva Bettens, Veronique Corine De Vroey, Dirk Jochmans