Patents by Inventor José Ignacio Andrés-Gil
José Ignacio Andrés-Gil 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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Publication number: 20140057870Abstract: 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: ApplicationFiled: October 22, 2013Publication date: February 27, 2014Applicant: VANDERBILT UNIVERSITYInventors: 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
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Publication number: 20130345203Abstract: 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: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Inventors: 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
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Publication number: 20130345206Abstract: 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: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Inventors: 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
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Publication number: 20130345205Abstract: In one aspect, the invention relates to substituted bicyclic aralkyl 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: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
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Patent number: 8592422Abstract: 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: GrantFiled: December 16, 2011Date of Patent: November 26, 2013Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James MacDonald, Han Min Tong, Carrie K. Jones, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Chrysa Malosh
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Publication number: 20130230459Abstract: The present invention relates to novel, selective, radiolabelled mGluR2 ligands which are useful for imaging and quantifying the metabotropic glutamate receptor mGluR2 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.Type: ApplicationFiled: November 8, 2011Publication date: September 5, 2013Applicant: Janssen Pharmaceuticals, Inc.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, José Maria Cid-Núñez, Andrés Avelino Trabanco-Suárez, Guy Maurits R. Bormans, Sofie Jeanne Leopoldine Celen, Michel Koole
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Patent number: 8466153Abstract: The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles of the general formula (I); or a pharmaceutically acceptable salt thereof, or a stereoisomeric form, that are fast dissociating dopamine 2 receptor antagonists, as well as 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: December 5, 2007Date of Patent: June 18, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Gregor James MacDonald, José Ignacio Andrés-Gil, Frans Alfons Maria Van Den Keybus, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
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Patent number: 8329704Abstract: The present invention concerns aryl and heteroaryl substituted pyrazinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.Type: GrantFiled: December 18, 2006Date of Patent: December 11, 2012Assignee: Janssen Pharmaceutica, N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Rosa María Álvarez-Escobar, Julen Oyarzabal Santamarina, Frank Matthias Dautzenberg, Jacqueline Macritchie, Donald Simpson, Sonia Martinez Gonzalez
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Publication number: 20120225844Abstract: 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: ApplicationFiled: December 16, 2011Publication date: September 6, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Carrie K. Jones, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Chrysa Malosh
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Publication number: 20120213703Abstract: The present invention relates to novel, selective, radiolabelled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.Type: ApplicationFiled: October 27, 2010Publication date: August 23, 2012Inventors: José Ignacio Andrés-Gil, Meri De Angelis, Guy Maurits R. Bormans, Sofie Jeanne Leopoldine Celen
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Patent number: 8158643Abstract: The present invention concerns aryl and heteroaryl substituted diaza-spiro-pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.Type: GrantFiled: December 4, 2007Date of Patent: April 17, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Frank Matthias Dautzenberg, Joannes Theodorus Maria Linders
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Publication number: 20110305637Abstract: The present invention relates to novel, selective, radiolabeled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme in tissues using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.Type: ApplicationFiled: February 22, 2010Publication date: December 15, 2011Inventors: José Ignacio Andrés-Gil, Guy Maurits R. Bormans, Sofie Jeanne Leopoldine Celen, Meri De Angelis
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Publication number: 20100166655Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.Type: ApplicationFiled: March 15, 2007Publication date: July 1, 2010Applicants: JANSSEN PHARMACEUTICA N.V., ADDEX PHARMACEUTICALS S.A.Inventors: Hassan Julien Imogai, Vincent Mutel, Jose Maria Cid-Nunez, Jose Ignacio Andres-Gil, Andres Avelino Trabanco-Suarez, Julen Oyarzabal Santamarina, Frank Matthias Dautzenberg, Gregor James MaCdonald, Shirley Elizabeth Pullan, Robert Johannes Lutjens, Guillaume Albert Jacques Duvey, Vanthea Nhem, Terry Palrick Finn, Gagik Melikyan
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Publication number: 20100105694Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in claim 1, having selective 2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.Type: ApplicationFiled: October 10, 2007Publication date: April 29, 2010Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Lourdes Linares De La Morena, Sonia Martinez Gonzalez, Julen Oyarzabal Santamarina, Joaquin Pastor-Fernández, Juan Antonio Vega-Ramiro, Francisca Delgado-Jiménez, Wilhelmus Helena Ignatius Maria Drinkenburg
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Publication number: 20100076187Abstract: The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles 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: December 5, 2007Publication date: March 25, 2010Inventors: Gregor James MacDonald, José Ignacio Andrés-Gil, Frans Alfons Maria Van Den Keybus, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
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Publication number: 20100035909Abstract: The present invention concerns aryl and heteroaryl substituted diaza-spiro-pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.Type: ApplicationFiled: December 4, 2007Publication date: February 11, 2010Inventors: Jose Ignacio Andres-Gil, Manuel Jesus Alcazar-Vaca, Frank Matthias Dautzenberg, Joannes Theodorus Maria Linders
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Publication number: 20100029620Abstract: The present invention concerns substituted triazolone, tetrazolone and imidazolone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective ?2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.Type: ApplicationFiled: December 20, 2005Publication date: February 4, 2010Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Joaquin Pastor-Fernández, Xavier Jean,Michel Langlois, Julen Oyarzabal-Santamarina, Juan Antonio Vega-Ramiro
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Patent number: 7635696Abstract: The present invention relates to novel isoxazoline-indole derivatives according to Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, with a binding affinity towards dopamine receptors, in particular towards dopamine D2 and/or D3 receptors, with selective serotonin reuptake inhibition (SSRI) properties and showing an affinity for the 5-HT1A receptor, pharmaceutical compositions comprising the compounds according to the invention, the use thereof for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic disorders, most in particular schizophrenia and processes for their production, wherein the variables are further defined in the application.Type: GrantFiled: November 25, 2005Date of Patent: December 22, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, José Manuel Bartolomé-Nebreda, Manuel Jesus Alcázar-Vaca, Maria de las Mercedes Garcia-Martin, Antonius Adrianus Hendrikus Petrus Megens
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Publication number: 20090281099Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective ?2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.Type: ApplicationFiled: May 21, 2007Publication date: November 12, 2009Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Lourdes Linares De La Morena, Sonia Martinez Gonzalez, Julen Oyarzabal Santamarina, Joaquin Pastor-Fernàndez, Juan Antonio Vega Ramiro, Francisca Delgado-Jiménez, Wilhelmus Helena Drinkenburg
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Publication number: 20090111801Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective ?2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.Type: ApplicationFiled: April 19, 2007Publication date: April 30, 2009Applicant: Janssen Pharmaceutica N.V.Inventors: Jose Ignacio Andres-Gil, Manuel Jesus Alcazar-Vaca, Maria Lourdes Linares De La Morena, Sonia Martinez Gonzalez, Julen Oyarzabal Santamarina, Joaquin Pastor-Fernandez, Juan Antonio Vega Ramiro, Francisca Delgado-Jimenez, Wilhelmus Helena Ignatius Maria Drinkenburg