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).

  • Patent number: 9751860
    Abstract: 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: Grant
    Filed: September 13, 2016
    Date of Patent: September 5, 2017
    Assignee: Janssen Pharmaceutica NV
    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
  • Publication number: 20170022181
    Abstract: 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: Application
    Filed: September 13, 2016
    Publication date: January 26, 2017
    Inventors: 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
  • Patent number: 9468640
    Abstract: 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: Grant
    Filed: January 26, 2015
    Date of Patent: October 18, 2016
    Assignee: JANSSEN PHARMACEUTICA NV
    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
  • Publication number: 20150141432
    Abstract: 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: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    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
  • Patent number: 8940743
    Abstract: 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: Grant
    Filed: October 24, 2006
    Date of Patent: January 27, 2015
    Assignee: Janssen Pharmaceutica NV
    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
  • Patent number: 8440701
    Abstract: 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: Grant
    Filed: October 15, 2008
    Date of Patent: May 14, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Johannes Wilhelmus John F. Thuring, Theodorus Dinklo, Anne Simone Josephine Lesage, Marcel Frans Leopold De Bruyn, Wei Zhuang
  • Patent number: 8143419
    Abstract: 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: Grant
    Filed: April 19, 2007
    Date of Patent: March 27, 2012
    Assignee: 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
  • Publication number: 20100216846
    Abstract: 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: Application
    Filed: October 15, 2008
    Publication date: August 26, 2010
    Inventors: Johannes Wilhelmus John F. Thuring, Theodorus Dinklo, Anne Simone Josephine Lesage, Marcel Frans Leopold De Bruyn, Wei Zhuang
  • Publication number: 20090253691
    Abstract: 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: Application
    Filed: April 19, 2007
    Publication date: October 8, 2009
    Applicants: JANSSEN PHARMACEUTICA N.V., BIOFOCUS DPI LIMITED
    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
  • Publication number: 20080227791
    Abstract: 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: Application
    Filed: October 24, 2006
    Publication date: September 18, 2008
    Applicant: 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
  • Patent number: 7423048
    Abstract: 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 C1-6al
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: September 9, 2008
    Assignee: 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
  • Patent number: 7358239
    Abstract: 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 is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 7273862
    Abstract: 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: Grant
    Filed: November 29, 2004
    Date of Patent: September 25, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristof Van Emelen, Marcel Frans Leopold De Bruyn
  • Patent number: 7081453
    Abstract: 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 aminocarbonyl
    Type: Grant
    Filed: June 13, 2001
    Date of Patent: July 25, 2006
    Assignee: 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
  • Patent number: 6900222
    Abstract: 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 a
    Type: Grant
    Filed: May 23, 2000
    Date of Patent: May 31, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 6864273
    Abstract: 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: Grant
    Filed: May 23, 2000
    Date of Patent: March 8, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristof Van Emelen, Marcel Frans Leopold De Bruyn
  • Patent number: 6852714
    Abstract: 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 h
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: February 8, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
  • Patent number: 6747045
    Abstract: 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, C1-6a
    Type: Grant
    Filed: April 3, 2002
    Date of Patent: June 8, 2004
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
  • Publication number: 20040019051
    Abstract: 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
    Type: Application
    Filed: June 12, 2003
    Publication date: January 29, 2004
    Inventors: 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
  • Publication number: 20030149093
    Abstract: The present invention of compounds of formula (I) 1
    Type: Application
    Filed: September 5, 2002
    Publication date: August 7, 2003
    Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn