Patents by Inventor Joseph Elisabeth Leenaerts
Joseph Elisabeth Leenaerts 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: 7476662Abstract: The invention concerns novel substituted tetracyclic imidazole derivatives useful for the treatment of elevated intracranial pressure (ICP) and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine. The novel compounds comprise compounds according to the general Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-l-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-?]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof.Type: GrantFiled: June 11, 2002Date of Patent: January 13, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Koenraad Arthur Van Rossem, Manuel Jesús Alcázar-Vaca, Pedro Martínez-Jiménez, José Manuel Bartolomé-Nebreda, Antonio Gómez-Sánchez, Francisco Javier Fernández-Gadea, Jos Van Reempts
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Patent number: 7435736Abstract: The invention concerns substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK1 and NK1/NK3-antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety, depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.Type: GrantFiled: December 17, 2003Date of Patent: October 14, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Patent number: 7410970Abstract: The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS.Type: GrantFiled: October 7, 2003Date of Patent: August 12, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck, Gaston Stanislas Marcella Diels
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Patent number: 7390822Abstract: The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the compounds according to Formula (I) in which A=B is C?O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A=B and R1 together form a benzoxazolyl radical; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen.Type: GrantFiled: October 10, 2002Date of Patent: June 24, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Francisco Javier Fernández-Gadea, Paul Joannes Ludovicus Herijgers, Theo Frans Meert, Antonio Gómez-Sánchez, Willem Flameng, Marcel J. M. Borgers
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Publication number: 20080070924Abstract: This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in acute and chronic pain treatments, more in particular in inflammatory, post-operative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NK1-receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression and tolerance in opioid-based treatments of pain.Type: ApplicationFiled: June 7, 2004Publication date: March 20, 2008Inventors: Frans Eduard Janssens, Francois Maria Sommen, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck, Theo Frans Meert
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Patent number: 7282508Abstract: The present invention relates to novel 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. In particular are claimed compounds according to Formula (I) in which A?B is C?O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A?B and R1 together form a benzoxazolyl radical; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen. The invention also relates to processes for the preparation of the compounds according to the invention and their use in medicine, in particular as selective non-peptide ?-opioid agonists for use in the treatment of various pain conditions.Type: GrantFiled: October 10, 2002Date of Patent: October 16, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Francisco Javier Fernández-Gadea, Antonio Gómez-Sánchez, Theo Frans Meert
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Patent number: 7148214Abstract: This invention concerns the compounds of formula or a prodrug, a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof wherein R1, R2, —A—B—, L, and n have the meaning given in the description. The invention relates to preparations and compositions of the present compounds and their use as medicines.Type: GrantFiled: December 15, 1999Date of Patent: December 12, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts
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Patent number: 7087595Abstract: This invention concerns the compounds of formula or a prodrug, a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof wherein R1, R2, -A-B—, L, and n have the meaning given in the description. The invention relates to preparations and compositions of the present compounds and their use as medicines.Type: GrantFiled: July 26, 2004Date of Patent: August 8, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts
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Publication number: 20060128721Abstract: This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in opioid-based acute and chronic pain treatments, more in particular in inflammatory, post-operative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NK1-receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression in opioid-based treatments of pain.Type: ApplicationFiled: June 7, 2004Publication date: June 15, 2006Inventors: Frans Janssens, Francois Sommen, Benoit Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts, Yves Emiel, Maria Van Roosbroeck, Theo Frans Meert
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Publication number: 20040260096Abstract: The present invention relates to novel 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives according to Formula (I) 1Type: ApplicationFiled: March 31, 2004Publication date: December 23, 2004Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Francisco Javier Fernandez-Gadea, Theo Frans Meert
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Publication number: 20040167138Abstract: The invention concerns novel substituted tetracyclic imidazole derivatives useful for the treatment of elevated intracranial pressure (ICP) and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine. The novel compounds comprise compounds according to the general Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenylmethyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-a]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof.Type: ApplicationFiled: December 5, 2003Publication date: August 26, 2004Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Koengaard Arthur Van Rossem, Manuel Jesus Alcazar-Vaca, Pedro Martinez-Jimenez, Jose Manuel Bartolome-Nebreda, Antonio Gomez-Sanchez, FranciscoJavier Fernandez-Javier, Jos Van Reempts
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Publication number: 20030087895Abstract: This invention concerns the compounds of formula 1Type: ApplicationFiled: July 2, 2002Publication date: May 8, 2003Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Francois Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux
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Patent number: 6521621Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent; R2 is Ar2, Ar2C1-6alkyl, Het1 or Het1C1-6alkyl; R3 is hydrogen or C1-6alkyl; L is hydrogen; Ar3; C1-6alkyl; C1-6alkyl substituted with 1 or 2 substituents selected from hydroxy, C1-6alkyloxy, Ar3, Ar3C1-6alkyloxy and Het2; C3-6alkenyl; Ar3C3-6alkenyl; di(Ar3)C3-6alkenyl or a radical of formula (a-1), (a-2), (a-3), (a-4) or (a-5); Ar1, Ar2 and Ar3 are each phenyl or substituted phenyl; Het1 and Het2 are each monocyclic or a bicyclic heterocycles; as substancType: GrantFiled: December 22, 2000Date of Patent: February 18, 2003Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck
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Patent number: 6476018Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula —X—COOR5, —X—CONR6R7 or —X—COR10 wherein —X— is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is —CH2—, —CH2—CH2—, —CH═CH—, —CHOH—CH2&mdasType: GrantFiled: February 2, 2001Date of Patent: November 5, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Francois Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux
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Patent number: 6251894Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; ═Q is ═O or ═NR3; X is a covalent bond or —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted; R2 is Ar2, Ar2C1-6alkyl, Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; L is a piperidine derivative of formula (a-1) or a spiro piperidine derivative of formula (a-2); Ar1 is phenyl or substituted phenyl; Ar2 is naphtalenyl; phenyl or substituted phenyl; and Het is a monocyclic or bicyclic heterocycle; each monocyclic and bicyclic heterocycle may optionally be substituted on a carbon atom; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: June 22, 1998Date of Patent: June 26, 2001Assignee: Janssen Pharmaceuticals N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck
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Patent number: 6218381Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula —X—COOR5, —X—CONR6R7 or —X—COR10 wherein —X— is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is —CH2—, —CH2—CH2—, —CH═CH—, —CHOH—CH2&mdasType: GrantFiled: September 17, 1998Date of Patent: April 17, 2001Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, François Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux
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Patent number: 6197772Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: April 3, 1998Date of Patent: March 6, 2001Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck
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Patent number: 6110939Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; X is a covalent bond or a bivalent radical of formula --O--, --S--, --NR.sup.3 --; .dbd.Q is .dbd.O or .dbd.NR.sup.3 ; R.sup.1 is Ar.sup.1, Ar.sup.1 C.sub.1-6 alkyl or di(Ar.sup.1)C.sub.1-6 alkyl wherein the C.sub.1-6 alkyl group is optionally substituted; R.sup.2 is Ar.sup.2, Ar.sup.2 C.sub.1-6 alkyl, Het or HetC.sub.1-6 alkyl; L is a benzimidazole or imidazopyridine derivative of formula (A) or (B) Ar.sup.1 is optionally substituted phenyl Ar.sup.2 is naphtalenyl or optionally substituted phenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: June 19, 1998Date of Patent: August 29, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Fran.cedilla.ois Maria Sommen, Dominique Louis Nester Ghislaine Surleraux, Joseph Elisabeth Leenaerts
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Patent number: 5674866Abstract: The present invention is concerned with novel imidazoazepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; --A--B-- is a radical of formula --X--CH.dbd.CH-- (a-1); --CH.dbd.CH--X-- (a-2); or --CH.dbd.CH-- CH.dbd.CH-- (a-3); X represents O, S or NR.sup.1 ; R.sup.1 represents hydrogen or C.sub.1-6 alkyl; -----Y is a radical of formula .dbd.O (b-1); --OH (b-2); or .dbd.N--OH (b-3); and L represents hydrogen, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkyloxycarbonyl, phenylcarbonyl, C.sub.1-6 alkyl or C.sub.1-6 alkyl substituted with C.sub.1-4 alkyloxycarbonyl, hydroxycarbonyl, aryl, aryloxy or a radical of formula ##STR2## --D--Z-- is --S--CH.dbd.CH--, --S--CH.sub.2 --CH.sub.2 --, --S--CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --; and aryl is phenyl or phenyl substituted with halo, hydroxy or C.sub.1-4 alkyloxy.Type: GrantFiled: December 13, 1995Date of Patent: October 7, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts