Patents by Inventor Frans Eduard Janssens
Frans Eduard Janssens 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: 7355051Abstract: The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is C1?6alkyl optionally substituted with trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1?4alkoxy, C1?4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1?4alkyl-carbonyl, Ar2carbonyl, C1?4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1?4alkylcarbonyloxy, Ar2carbonyloxy, Ar2(CH2)ncarbonyloxy, C1?4alkoxy-carbonyl(CH2)noxy, mono- or di(C1?4alkyl)aminocarbonyl, mono- or di(C1?4alkyl)-aminocarbonyloxy, aminosulfonyl, mono- or di(C1?4alkyl)aminosulfonyl or a heterocycles selected from the group consisting of pyrrolidinyl, pyrrolyl, dihydropyrrolyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxType: GrantFiled: December 20, 2004Date of Patent: April 8, 2008Assignee: Tibotec PharmaceuticalsInventors: Jean-François Bonfanti, Koenraad Jozef Lodewijk Andries, Frans Eduard Janssens, François Maria Sommen, Jerôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe
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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: 7304052Abstract: The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- represents a saturated or an unsaturated homopiperidinyl having one double bond, and wherein said bivalent radical -{circle around (A)}- is substituted with R2 being hydrogen, hydroxy, C1-4alkyl, or C1-4alkyloxy; -a1=a2-a3=a4- represents an optionally substituted bivalent radical; R1 is hydrogen, C1-6alkyl, aryl1, C1-6alkyl substituted with aryl1, C1-4alkyloxycarbonyl, aryl1carbonyl, aryl1C1-6alkylarbonyl C1-4alkylcarbonyl, trifluoromethyl, trifluoromethylcarbonyl, C1-6alkylsulfonyl, aryl1sulfonyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl; X represents O, S or NR3, wherein R3 is hydrogen, C1-6alkyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl, C1-4alkyl substituted with aryl2 and optionally with hydroxy, C1-4alkylcarbonylC1-4alkyl suType: GrantFiled: December 14, 2000Date of Patent: December 4, 2007Assignee: Janssen Pharmaceuitca N.V.Inventors: Frans Eduard Janssens, Jérôme Emile Georges Guillemont, François Maria Sommen
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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: 7179811Abstract: This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and methods of their use in treating respiratory syncytial viral infections.Type: GrantFiled: April 2, 2004Date of Patent: February 20, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7173034Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of for CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.Type: GrantFiled: June 3, 2005Date of Patent: February 6, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7173054Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections.Type: GrantFiled: June 3, 2005Date of Patent: February 6, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
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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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Patent number: 7071192Abstract: The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4-represents a radical of formula —CH?CH—CH?CH—; —N—CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4)—; X1 is NR4, S, S(?O), S(?O)2, O, CH2, C(?O), CH(?CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(?O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3: provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the a position relative to a nitrogen atom; G is a diType: GrantFiled: June 20, 2000Date of Patent: July 4, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Jean Fernand Armand Lacrampe, Jérôme Emile Georges Guillemont, Marc Gaston Venet, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 6924287Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be replaced; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.Type: GrantFiled: June 20, 2000Date of Patent: August 2, 2005Assignee: Janssen Pharmacatica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
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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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Patent number: 6747028Abstract: This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and methods of their use in treating respiratory syncytial viral infections.Type: GrantFiled: December 27, 2001Date of Patent: June 8, 2004Assignee: Hanssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Koenraad Jozef Lodewijk Marcel Andries
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Publication number: 20030139393Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: June 19, 2002Publication date: July 24, 2003Inventors: Frans Eduard Janssens, Jerome Emile Georges Guillemont, Francois Maria Sommen
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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: 6346540Abstract: The present invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and 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; p is 0, 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 of formula —O—CH2—CH2—O— or —O—CH2—CH2—CH2—O—; R2 is Ar2; Ar2C1-6alkyl; Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; R4 is hydrogen; C1-4alkyl; C1-4alkyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4alkyloxycarbonyl or Ar3; R5 is hydrogen; hydroxy; Ar3; Ar3C1-6alkyloxy; di(Ar3)C1-6alkyloxy; Ar3C1-6alkylthio; di(Ar3)C1-6alkylthio; Ar3C1-6alkylsulfoxy; di(Ar3)C1-6alkylsulfoxy;Type: GrantFiled: July 13, 2000Date of Patent: February 12, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux, Yves Emiel Maria Van Roosbroeck
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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