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: 8604200Abstract: This invention concerns substituted diaza-spiro-[4.4]-nonane 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 and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. 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: March 3, 2006Date of Patent: December 10, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Sophie Coupa, Alain Philippe Poncelet, Yvan Rene Ferdinand Simonnet, Bruno Schoentjes
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Patent number: 7994173Abstract: The present invention is concerned with novel compounds of formula (I) having fundic relaxating activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.Type: GrantFiled: January 24, 2008Date of Patent: August 9, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Jerome Emile Georges Guillemont, Francois Maria Sommen, Jean-Francois Bonfanti
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Patent number: 7795261Abstract: This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, anxiety, depression, emesis and IBS. 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: September 14, 2010Assignee: Janssen Pharmaceutica NVInventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Patent number: 7732437Abstract: The invention concerns a novel histamine receptor antagonist and the use of an histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemida, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. 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-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: November 22, 2002Date of Patent: June 8, 2010Assignee: Janssen Pharmaceutica, NV.Inventors: Frank Tegtmeier, 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, Jozef Leo Henri Van Reempts
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Publication number: 20100004260Abstract: The present invention is concerned with novel compounds of formula (I) having fundic relaxating activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.Type: ApplicationFiled: January 24, 2008Publication date: January 7, 2010Applicant: JANSSEN PHARMACEUTICA NVInventor: Frans Eduard Janssens
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Patent number: 7612056Abstract: This invention concerns substituted diaza-spiro-[4.5]-decane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence.Type: GrantFiled: April 4, 2005Date of Patent: November 3, 2009Assignee: Jenssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Bruno Schoentjes, Sophie Coupa, Alain Philippe Poncelet, Yvan René Ferdinand Simonnet
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Publication number: 20090221641Abstract: This invention concerns substituted diaza-spiro-[4.4]-nonane derivatives having neurokinin antagonistic activity, in particular NK1 antagonist ic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nocicept ion, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. 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: ApplicationFiled: March 3, 2006Publication date: September 3, 2009Applicant: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Sophie Coupa, Alain Phillippe Poncelet, Yvan Rene Ferdinand Simonnet, Bruno Schoentjes
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Patent number: 7572786Abstract: This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety and depression, irritable bowel syndrom (IBS), circadian rhythm disturbances, visceral 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: August 11, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Francois Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Patent number: 7544694Abstract: This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, COPD and micturition disorders such as urinary incontinence.Type: GrantFiled: April 4, 2005Date of Patent: June 9, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Bruno Schoentjes, Sophie Coupa, Alain Philippe Poncelet, Yvan René Ferdinand Simonnet
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Patent number: 7528149Abstract: 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: January 22, 2007Date of Patent: May 5, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Koenraads Jozef Lodewijk Marcell Andries
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Patent number: 7514424Abstract: The invention concerns substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives having neurokinin antagonistic activity, in particular NK˜antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of pain, emesis, anxiety, depression and IBS.Type: GrantFiled: December 17, 2003Date of Patent: April 7, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Publication number: 20090036466Abstract: The present invention concerns 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 Ar1 or C1-6alkyl substituted with one or more substituents selected from trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4alkylcarbonyl, Ar2-carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2-carbonyloxy, Ar2(CH2)ncarbonyloxy, hydroxy-C2-4-alkyloxy, C1-4alkoxycarbonyl(CH2)noxy, mono- or di(C1-4alkyl)-aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, dioxolanyl optionally substituted with one or two C1-6alkyl radicals, and a heterocycle selected from pyrrolidinyl, pyrrolyl, dihydropyrrolyl, thiazolidinyl, imidazolyl, triazoType: ApplicationFiled: December 20, 2004Publication date: February 5, 2009Inventors: Jean-Francois Bonfanti, Koenraad Jozef Lodewijk Andries, Frans Eduard Janssens, Francois Maria Sommen, Jerome Emile Georges Guillemont, Jean Fernand Armand Lacrampe
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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: 7407969Abstract: 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 ? position relative to a nitrogen atom; G is a dirType: GrantFiled: October 11, 2005Date of Patent: August 5, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Jean Fernand Armand Lacrampe, Jerome Emile Geroges Guilemont, Marc G Venet, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7390811Abstract: 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. Certain compounds of formula (I) are new.Type: GrantFiled: September 11, 2006Date of Patent: June 24, 2008Assignee: 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: 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: 20080146613Abstract: 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, Ar2-carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2-carbonyloxy, 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-diType: ApplicationFiled: February 13, 2008Publication date: June 19, 2008Inventors: Jean-Francois BONFANTI, Koenraad Jozef Lodewikjk Andries, Frans Eduard Janssens, Francois Maria Sommen, Jerome Emile Georges Guillemont, Jean Fernand Armand Lacrampe
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Patent number: 7361657Abstract: 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: January 12, 2006Date of Patent: April 22, 2008Assignee: 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