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).
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Patent number: 8188103Abstract: 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: GrantFiled: December 3, 2010Date of Patent: May 29, 2012Assignee: Janssen Pharmaceutica NVInventors: 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
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Publication number: 20110077245Abstract: 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: ApplicationFiled: December 3, 2010Publication date: March 31, 2011Inventors: 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
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Patent number: 7875621Abstract: 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: GrantFiled: June 28, 2005Date of Patent: January 25, 2011Assignee: Janssen Pharmaceutica NVInventors: 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
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Patent number: 7803823Abstract: 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 orType: GrantFiled: May 1, 2007Date of Patent: September 28, 2010Assignee: Janssen Pharmaceutica NVInventors: 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
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Patent number: 7232838Abstract: 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 subsType: GrantFiled: August 9, 2002Date of Patent: June 19, 2007Assignee: 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
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Patent number: 7208503Abstract: 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: GrantFiled: March 13, 2003Date of Patent: April 24, 2007Assignee: 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
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Patent number: 6833369Abstract: 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: GrantFiled: October 19, 2001Date of Patent: December 21, 2004Assignee: Janssen Pharmaceutica, NVInventors: Raymond Antoine Stokbroekx, Marc André Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
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Publication number: 20040254191Abstract: 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: ApplicationFiled: February 11, 2004Publication date: December 16, 2004Inventors: 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
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Publication number: 20040009987Abstract: This invention concerns compounds of formula 1Type: ApplicationFiled: October 19, 2001Publication date: January 15, 2004Inventors: Raymond Antoine Stokbroekx, Marc Andre Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
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Publication number: 20030181460Abstract: This invention concerns compounds of formula 1Type: ApplicationFiled: March 13, 2003Publication date: September 25, 2003Inventors: Raymond Antoine Stokbroekx, Marc Andre Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
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Patent number: 6602873Abstract: 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&mdType: GrantFiled: May 24, 2001Date of Patent: August 5, 2003Assignee: 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
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Publication number: 20020061890Abstract: This invention concerns compounds of formula 1Type: ApplicationFiled: November 19, 2001Publication date: May 23, 2002Inventors: Raymond Antoine Stokbroekx, Marc Andre Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
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Publication number: 20010046999Abstract: This invention concerns compounds of formula 1Type: ApplicationFiled: May 24, 2001Publication date: November 29, 2001Inventors: Raymond Antoine Stokbroekx, Marc Andre Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
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Patent number: 6265407Abstract: 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—Alk1Type: GrantFiled: August 14, 2000Date of Patent: July 24, 2001Assignee: 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
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Patent number: 5985878Abstract: 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: GrantFiled: July 9, 1998Date of Patent: November 16, 1999Assignee: Janssen Pharmaceuticals, N.V.Inventors: Raymond Antoine Stokbroekx, Marcel Jozef Maria Van der Aa, Marc Willems, Lieven Meerpoel, Marcel Gerebernus Maria Luyckx, Robert Tuman
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Patent number: 5811426Abstract: 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: GrantFiled: January 8, 1997Date of Patent: September 22, 1998Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Raymond Antoine Stokbroekx, Marc Willems, Marcel Jozef Maria Van der Aa
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Patent number: 5650411Abstract: 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: GrantFiled: July 18, 1995Date of Patent: July 22, 1997Assignee: 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
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Patent number: 5639754Abstract: 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: GrantFiled: May 23, 1995Date of Patent: June 17, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Raymond Antoine Stokbroekx, Marc Willems, Marcel Jozef Maria Van der Aa