Patents by Inventor Marcel Jozef Maria Van der Aa

Marcel Jozef Maria Van der Aa 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: 8188103
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions including compounds of formula (I) wherein R1, R3, L, X, Y and Z have defined meanings.
    Type: Grant
    Filed: December 3, 2010
    Date of Patent: May 29, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Marcel Jozef Maria Van der Aa, Albertus Henricus Maria Theresia Van Heertum, Jacobus Alphonsus Josephus van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
  • Publication number: 20110077245
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R3, L, X, Y and Z have defined meanings.
    Type: Application
    Filed: December 3, 2010
    Publication date: March 31, 2011
    Inventors: Marcel Jozef Maria Van der Aa, Albertus Henricus Maria Theresia Van Heertum, Jacobus Alphonsus Josephus van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
  • Patent number: 7875621
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions containing compounds of formula (I) wherein R1, R3, L, X, Y and Z have defined meanings.
    Type: Grant
    Filed: June 28, 2005
    Date of Patent: January 25, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Marcel Jozef Maria Van Der Aa, Albertus Henricus Maria Theresia Van Heertum, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijin Leopold Wouters
  • Patent number: 7803823
    Abstract: This invention concerns the use of a compound of formula (I?) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(?O)2—; mono- or di(C1-6alkyl)aminoS(?O)2; —C(?N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula L is optionally substituted phenyl or
    Type: Grant
    Filed: May 1, 2007
    Date of Patent: September 28, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Christopher John Love, Guy Rosalia Eugeen Van Lommen, Julien Georges Pierre-Olivier Doyon, Jean-Pierre André Marc Bongartz, Marcel Jozef Maria Van der Aa, Robert Jozef Maria Hendrickx, Peter Jacobus Johannes Antonius Buijnsters, Ludwig Paul Cooymans, Nele Vandermaesen, Erwin Coesemans, Gustaaf Maria Boeckx
  • Patent number: 7232838
    Abstract: This invention concerns the use of a compound of formula (I?), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxy -carbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(?O)2—; mono- or di(C1-6alkyl)aminoS(?O)2; —C(?N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula (b-1), (b-2), or (b-3), L is optionally subs
    Type: Grant
    Filed: August 9, 2002
    Date of Patent: June 19, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Christopher John Love, Guy Rosalia Eugeen Van Lommen, Julien Georges Pierre-Olivier Doyon, Jean-Pierre André Marc Bongartz, Marcel Jozef Maria Van der AA, Robert Jozef Maria Hendrickx, Peter Jacobus Johannes Antonius Buijnsters, Ludwig Paul Cooymans, Nele Vandermaesen, Erwin Coesemans, Gustaaf Maria Boeckx
  • Patent number: 7208503
    Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NH—, C3-6cycloalkyl, hydroxymethyl or benzoyloxymethyl; R2 is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; is Ar2, Ar2CH2— or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: March 13, 2003
    Date of Patent: April 24, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond Antoine Stokbroekx, Marc André Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
  • Patent number: 6833369
    Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; is Ar2, Ar2CH2— or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: October 19, 2001
    Date of Patent: December 21, 2004
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Raymond Antoine Stokbroekx, Marc André Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
  • Publication number: 20040254191
    Abstract: This invention concerns the use of a compound of formula (I′), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxy-carbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono -or di(C1-6alkyl)amino, aminocarbonyl, mono -or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono -or di(C1-6alkyl)aminocarbonyl; C1-6kyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(═O)2—; mono -or di(C1-6alkyl)aminoS(═O)2; —C(═N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula (b-1), (
    Type: Application
    Filed: February 11, 2004
    Publication date: December 16, 2004
    Inventors: Christopher John Love, Guy Rosalia Eugeen Van Lommen, Julien Georges Pierre-Olivier Doyon, Jean-Pierre Andre Marc Bongartz, Marcel Jozef Maria Van der AA, Robert Jozef Maria Hendrickx, Peter Jacobus Johannes Buijnsters, Ludwig Paul Cooymans, Nele Vandermaesen, Erwin Coesemans, Gustaaf Maria Boeckx
  • Publication number: 20040009987
    Abstract: This invention concerns compounds of formula 1
    Type: Application
    Filed: October 19, 2001
    Publication date: January 15, 2004
    Inventors: Raymond Antoine Stokbroekx, Marc Andre Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
  • Publication number: 20030181460
    Abstract: This invention concerns compounds of formula 1
    Type: Application
    Filed: March 13, 2003
    Publication date: September 25, 2003
    Inventors: Raymond Antoine Stokbroekx, Marc Andre Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
  • Patent number: 6602873
    Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1—NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula —CH═CH—CH═CH—; R4, R5 and R6 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; or when R4 and R5 are adjacent to each other they may be taken together to form a radical of formula —CH═CH—CH═CH—; A is a bivalent radical of formula NR7, NR7-Alk1-X-, NR7-Alk1-X-Alk2-, O-Alk1-X-, O-Alk1-X-Alk2- or S-Alk1-X-; wherein X is a direct bond, —O—, —S—, C═O, —NR8&md
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: August 5, 2003
    Assignee: Janssen Pharamaceutica, N.V.
    Inventors: Raymond Antoine Stokbroekx, Marc André Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
  • Publication number: 20020061890
    Abstract: This invention concerns compounds of formula 1
    Type: Application
    Filed: November 19, 2001
    Publication date: May 23, 2002
    Inventors: Raymond Antoine Stokbroekx, Marc Andre Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
  • Publication number: 20010046999
    Abstract: This invention concerns compounds of formula 1
    Type: Application
    Filed: May 24, 2001
    Publication date: November 29, 2001
    Inventors: Raymond Antoine Stokbroekx, Marc Andre Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
  • Patent number: 6265407
    Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1—NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula —CH═CH—CH═CH—; R4, R5 and R6 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; or when R4 and R5 are adjacent to each other they may be taken together to form a radical of formula —CH═CH—CH═CH—; A is a bivalent radical of formula NR7, NR7—Alk1—X—, NR7—Alk1—X—Alk2—, O—Alk1—X—, O—Alk1—X—Alk2— or S—Alk1
    Type: Grant
    Filed: August 14, 2000
    Date of Patent: July 24, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond Antoine Stokbroekx, Marc André Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
  • Patent number: 5985878
    Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH.sub.2 groups of the ##STR1## moiety which may also contain one double bond, may be substituted with C.sub.1-6 alkyl, amino, aminocarbonyl, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyloxycarbony, C.sub.1-6 alkylcarbonylamino, hydroxy or C.sub.1-6 alkyloxy; and/or 2 C-atoms of said CH.sub.2 groups may be bridged with C.sub.2-4 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, mono- or di(C.sub.1-6 alkyl)amino, Ar, ArNH--, C.sub.3-6 cycloalkyl, hydroxymethyl or benzyloxymethyl; R.sup.2 and R.sup.3 are hydrogen, or taken together may form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH--; in case X represents CH then L is a radical L.sup.1, L.sup.2 or L.sup.3 ; or in case X represents N then L is a radical L.
    Type: Grant
    Filed: July 9, 1998
    Date of Patent: November 16, 1999
    Assignee: Janssen Pharmaceuticals, N.V.
    Inventors: Raymond Antoine Stokbroekx, Marcel Jozef Maria Van der Aa, Marc Willems, Lieven Meerpoel, Marcel Gerebernus Maria Luyckx, Robert Tuman
  • Patent number: 5811426
    Abstract: The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X is O or S; Y is CH or N; R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R.sup.6 is C.sub.1-4 alkyl; C.sub.1-4 alkyl substituted with arylcyclohexyl; aryl or arylcarbonyl; wherein aryl is phenyl optionally substituted with one or two substituents selected from halo and C.sub.1-4 alkyl;Z is C=O or CHOH; and ##STR2## Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a medicine.
    Type: Grant
    Filed: January 8, 1997
    Date of Patent: September 22, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Raymond Antoine Stokbroekx, Marc Willems, Marcel Jozef Maria Van der Aa
  • Patent number: 5650411
    Abstract: The use for the manufacture of a medicament for treating Helicobacter-related diseases of a compound of formula ##STR1## a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, whereinX and Y each independently are CH or N;R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl;R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy;Z is C.dbd.O or CHOH; andAr is phenyl optionally substituted with up to three substituents selected from hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, halo, trifluoromethyl, triC.sub.1-4 alkylsilyloxy, nitro, amino and cyano or pyridinyl substituted with hydroxy or C.sub.
    Type: Grant
    Filed: July 18, 1995
    Date of Patent: July 22, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Joseph Hector Mostmans, Luc Alfons Leo Van Der Eycken, Frank Christopher Odds, Raymond Antoine Stokbroekx, Marcel Jozef Maria Van der Aa
  • Patent number: 5639754
    Abstract: The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X is O or S; Y is CH or N; R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R.sup.6 is C.sub.1-4 alkyl; C.sub.1-4 alkyl substituted with arylcyclohexyl; aryl or arylcarbonyl; wherein aryl is phenyl optionally substituted with one or two substituents selected from halo and C.sub.1-4 alkyl;Z is C.dbd.O or CHOH; and ##STR2## is a radical of formula ##STR3## Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a medicine.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: June 17, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Raymond Antoine Stokbroekx, Marc Willems, Marcel Jozef Maria Van der Aa