Patents by Inventor José Manuel Bartolomé-Nebreda

José Manuel Bartolomé-Nebreda 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).

  • Bicyclic thiazoles as allosteric modulators of mGluR5 receptors
    Patent number: 9040707
    Abstract: The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James MacDonald, Andrés Avelino Trabanco-Suárez, Susana Conde-Ceide, Gary John Tresadern, José Manuel Bartolomé-Nebreda, Joaquin Pastor-Fernández
  • Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mGluR5 receptors
    Patent number: 9029366
    Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: May 12, 2015
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
  • Substituted 6-methylnicotinamides as mGluR5 positive allosteric modulators
    Patent number: 8969389
    Abstract: In one aspect, the invention relates to substituted 6-methylnicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: March 3, 2015
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Ya Zhou, Jason Manka, Gregor McDonald, José Manuel Bartolome-Nebreda
  • Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists
    Patent number: 8933101
    Abstract: The present invention relates to [1-(benzyl)-piperidin-4-yl]-([1,3,4]thiadiazol-2-yl)-amine and [1-(benzyl)-piperidin-4-yl]-(thiazol-2-yl)-amine derivatives of formula (I) 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: April 18, 2008
    Date of Patent: January 13, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James MacDonald, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
  • 4-alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists
    Patent number: 8906921
    Abstract: The present invention relates to (1-benzyl-piperidin-4-yl)-(4-alkoxy-pyridazin-3-y1)-amines 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: April 18, 2008
    Date of Patent: December 9, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James MacDonald, José Manuel Bartolomé-Nebreda
  • Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mGluR5 receptors
    Patent number: 8901125
    Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: December 2, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
  • Piperazin-1-yl-trifluoromethyl-substituted-pyridines as fast dissociating dopamine 2 receptor antagonists
    Patent number: 8895562
    Abstract: The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines 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: July 29, 2009
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Michiel Luc Maria Van Gool
  • FAST-DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS
    Publication number: 20140336381
    Abstract: The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines 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: July 28, 2014
    Publication date: November 13, 2014
    Inventors: Gregor James Macdonald, Xavier Jean Michel Langlois, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
  • SUBSTITUTED IMIDAZOPYRIMIDIN-5(6H)-ONES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
    Publication number: 20140329838
    Abstract: In one aspect, the invention relates to imidazopyrimidin-5(6H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 13, 2014
    Publication date: November 6, 2014
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Jose Manuel Bartolome-Nebreda, Gregor Macdonald, Susana Conde-Ceide, Carrie K. Jones, Maria Luz Martin-Martin, Han Min Tong
  • Substituted imidazopyrimidin-5(6H)-ones as allosteric modulators of MGLUR5 receptors
    Patent number: 8865725
    Abstract: In one aspect, the invention relates to imidazopyrimidin-5(6H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: October 21, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Jose Manuel Bartolome-Nebreda, Gregor James MacDonald, Susana Conde-Ceide, Carrie K. Jones, Maria Luz Martin-Martin, Han Min Tong
  • Imidazo[1,2-a]pyrazine derivatives and their use for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases
    Patent number: 8859543
    Abstract: The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
    Type: Grant
    Filed: March 8, 2011
    Date of Patent: October 14, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James MacDonald, Joaquin Pastor-Fernández, Michiel Luc Maria Van Gool, María Luz Martín-Martín, Greta Constantia Peter Vanhoof
  • Naphthyridinone analogs as mGluR5 positive allosteric modulators
    Patent number: 8853237
    Abstract: In one aspect, the invention relates to naphthyridinone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: October 7, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Jason Manka, Jon Jacobs, Ya Zhou, José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Susana Conde-Ceide, Carrie K. Jones
  • BICYCLIC PYRAZOLE COMPOUNDS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
    Publication number: 20140213593
    Abstract: In one aspect, the invention relates to bicyclic pyrazole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 31, 2014
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor Macdonald, Han Min Tong, Carrie K. Jones
  • Fast-dissociating dopamine 2 receptor antagonists
    Patent number: 8791120
    Abstract: The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines of formula (I) 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: February 11, 2008
    Date of Patent: July 29, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James MacDonald, Xavier Jean Michel Langlois, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
  • Imidazo[1,2-b]pyridazine derivatives and their use as PDE10 inhibitors
    Patent number: 8716282
    Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: May 6, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Joaquin Pastor-Fernández, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, Óscar Delgado-González, Greta Constantia Peter Vanhoof, Michiel Luc Maria Van Gool, María Luz Martín-Martín, Sergio-Alvar Alonso-de Diego, Kelly Ann Swinney, Carina Leys, Johan Erwin Edmond Weerts, Stijn Wuyts
  • Dihydronaphthyridinyl(organo)methanone analogs as positive allosteric mGluR5 modulators
    Patent number: 8710074
    Abstract: In one aspect, the invention relates to dihydronaphthyridinyl(organo)methanone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2012
    Date of Patent: April 29, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Jason Manka, Jon Jacobs, Ya Zhou, José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Susana Conde-Ceide, Eric S. Dawson
  • Substituted pyrazolo[1,5-A]pyrazine compounds as allosteric modulators of mGluR5 receptors
    Patent number: 8703946
    Abstract: In one aspect, the invention relates to substituted pyrazolo[1,5-a]pyrazine compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: April 22, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Carrie K. Jones, Shaun R. Stauffer, José Manuel Bartolome-Nebreda, Gregor James McDonald, Susana Conde-Ceide, Han Min Tong
  • BICYCLIC TRIAZOLE AND PYRAZOLE LACTAMS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
    Publication number: 20140057870
    Abstract: In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 27, 2014
    Applicant: VANDERBILT UNIVERSITY
    Inventors: P. Jeffrey Conn, CRAIG W. LINDSLEY, SHAUN R. STAUFFER, José Manuel Bartolomé-Nebreda, SUSANNA CONDE-CEIDE, GREGOR JAMES MACDONALD, HAN MIN TONG, CARRIE K. JONES, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, CHRYSA MALOSH
  • SUBSTITUTED BICYCLIC ALKOXY PYRAZOLE ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
    Publication number: 20130345203
    Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 19, 2013
    Publication date: December 26, 2013
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
  • SUBSTITUTED BICYCLIC CYCLOALKYL PYRAZOLE LACTAM ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
    Publication number: 20130345204
    Abstract: In one aspect, the invention relates to substituted bicyclic cycloalkyl pyrazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 19, 2013
    Publication date: December 26, 2013
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong