Patents by Inventor Marcel Frans Leopold De Bruyn
Marcel Frans Leopold De Bruyn 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: 9751860Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds of the invention can be administered to a patient in need thereof to treat or prevent psychosis including, but not limited to, schizophrenia, schizophreniform disorder and schizoaffective disorder. Compounds of the present invention include those encompassed by Formula I.Type: GrantFiled: September 13, 2016Date of Patent: September 5, 2017Assignee: Janssen Pharmaceutica NVInventors: Marcel Frans Leopold De Bruyn, Gregor James MacDonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck
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Publication number: 20170022181Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: ApplicationFiled: September 13, 2016Publication date: January 26, 2017Inventors: Marcel Frans Leopold De Bruyn, Gregor James Macdonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van den Keytus, Yves Emiel Maria Van Roosbroeck
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Patent number: 9468640Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: GrantFiled: January 26, 2015Date of Patent: October 18, 2016Assignee: JANSSEN PHARMACEUTICA NVInventors: Marcel Frans Leopold De Bruyn, Gregor James Macdonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van den Keybus, Yves Emiel Maria Van Roosbroeck
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Publication number: 20150141432Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: ApplicationFiled: January 26, 2015Publication date: May 21, 2015Inventors: Marcel Frans, Leopold De Bruyn, Gregor James Macdonald, Ludo Edmond, Josephine Kennis, Xavier Jean, Michel Langlois, Frans Alfons, Maria Van den Keybus, Yves Emiel, Maria Van Roosbroeck
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Patent number: 8940743Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: GrantFiled: October 24, 2006Date of Patent: January 27, 2015Assignee: Janssen Pharmaceutica NVInventors: Marcel Frans Leopold De Bruyn, Gregor James MacDonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck
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Patent number: 8440701Abstract: The present invention relates to substituted 1-(alkyl)-3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.Type: GrantFiled: October 15, 2008Date of Patent: May 14, 2013Assignee: Janssen Pharmaceutica NVInventors: Johannes Wilhelmus John F. Thuring, Theodorus Dinklo, Anne Simone Josephine Lesage, Marcel Frans Leopold De Bruyn, Wei Zhuang
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Patent number: 8143419Abstract: The present invention relates to 3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.Type: GrantFiled: April 19, 2007Date of Patent: March 27, 2012Assignee: Janssen Pharmaceutica N. V.Inventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Anne Simone Josephine Lesage, Wei Zhuang, Marcel Frans Leopold De Bruyn, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck, Theodorus Dinklo, James Edward Stewart Duffy
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Publication number: 20100216846Abstract: The present invention relates to substituted 1-(alkyl)-3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.Type: ApplicationFiled: October 15, 2008Publication date: August 26, 2010Inventors: Johannes Wilhelmus John F. Thuring, Theodorus Dinklo, Anne Simone Josephine Lesage, Marcel Frans Leopold De Bruyn, Wei Zhuang
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Publication number: 20090253691Abstract: The present invention relates to 3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.Type: ApplicationFiled: April 19, 2007Publication date: October 8, 2009Applicants: JANSSEN PHARMACEUTICA N.V., BIOFOCUS DPI LIMITEDInventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Anne Simone Josephine Lesage, Wei Zhuang, Marcel Frans Leopold De Bruyn, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck, Theodorus Dinklo
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Publication number: 20080227791Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: ApplicationFiled: October 24, 2006Publication date: September 18, 2008Applicant: Janssen Pharmaceutica N.V.Inventors: Marcel Frans Leopold De Bruyn, Gregor James Macdonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck
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Patent number: 7423048Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a1?a2-a3?a4- is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH?; -Z1-Z2- is a bivalent radical; -A- is a bivalent radical of formula —N(R6)-Alk2- or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alType: GrantFiled: February 16, 2006Date of Patent: September 9, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Kristol Van Emelen, Marcel Frans Leopold De Bruyn, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Maria Encamacion Matesanz-Ballesteros, José Manuel Bartolomé-Nebreda
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Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7273862Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical.Type: GrantFiled: November 29, 2004Date of Patent: September 25, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marcel Frans Leopold De Bruyn
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Patent number: 7081453Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein —a1?a2—a3?a4— is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH?; —Z1—Z2— is a bivalent radical; —A— is a bivalent radical of formula —N(R6)—Alk2— or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula (d-1), (d-2), (d-3), (d-4), (d-5) wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonylType: GrantFiled: June 13, 2001Date of Patent: July 25, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marcel Frans Leopold De Bruyn, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Maria Encarnacion Matesanz-Ballesteros, José Manuel Bartolomé-Nebreda
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Patent number: 6900222Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is aType: GrantFiled: May 23, 2000Date of Patent: May 31, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 6864273Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical.Type: GrantFiled: May 23, 2000Date of Patent: March 8, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marcel Frans Leopold De Bruyn
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Patent number: 6852714Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6-Alk2-(b-1), or -Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hType: GrantFiled: September 5, 2002Date of Patent: February 8, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
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Patent number: 6747045Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or -Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6aType: GrantFiled: April 3, 2002Date of Patent: June 8, 2004Assignee: Janssen Pharmaceutica N.V.Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
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Publication number: 20040019051Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein —a1═a2—a3═a4— is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH═; —Z1—Z2— is a bivalent radical; —A— is a bivalent radical of formula —N(R6)—Alk2— or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula (d-1), (d-2), (d-3), (d-4), (d-5) wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl orType: ApplicationFiled: June 12, 2003Publication date: January 29, 2004Inventors: Kristof Van Emelen, Marcel Frans Leopold De Bruyn, Manuel Jesus Alcazar-Vaca, Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea, Maria Encarnacion Matesanz-Ballesteros, Jose Manuel Bartolome-Nebreda
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Publication number: 20030149093Abstract: The present invention of compounds of formula (I) 1Type: ApplicationFiled: September 5, 2002Publication date: August 7, 2003Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn