Patents by Inventor Joaquin Pastor-Fernandez
Joaquin Pastor-Fernandez 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: 20130065883Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3, and/or Flt3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: ApplicationFiled: February 18, 2011Publication date: March 14, 2013Applicant: Centro Nacional de Investigaceiones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Julen Oyarzabal Santamarina, Carl-Gustaf Pierre Saluste, Carmen Blanco Aparicio, Rosa Maria Alvarez Escobar, Virginia Rivero Buceta
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Publication number: 20130053371Abstract: There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: ApplicationFiled: January 24, 2011Publication date: February 28, 2013Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLÓGICAS (CNIO)Inventors: Joaquin Pastor Fernández, Sonia Martinez Gonzalez, Rosa Maria Alvarez Escobar, Antonlo Rodriguez Hergueta, José Ignacio Martin Hernando, Francisco Ramos Lima
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Publication number: 20130029967Abstract: There is provided compounds of formula (I), wherein A1, A2, A3, A4, n, the dotted lines, B1, B1a, B2, B2a, B3, B3a, B4, B4a, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: ApplicationFiled: September 24, 2010Publication date: January 31, 2013Applicant: Centro Nacional de Investigaciones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Sonia Martinez Gonzalez, Rosa Maria Alvarez Escobar, Sonsoles Rodriguez Aristegui, Esther Gonzales Cantalapiedra, Ana Isabel Hernandez Higueras, Carmen Varela Busto
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Publication number: 20120329792Abstract: 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: ApplicationFiled: March 8, 2011Publication date: December 27, 2012Inventors: 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
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Publication number: 20120258955Abstract: 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: ApplicationFiled: December 16, 2010Publication date: October 11, 2012Applicant: JANSSEN PHARMACEUTICA NVInventors: Gregor James MacDonald, Andrés Avelino Trabanco-Suárez, Susana Conde-Ceide, Gary John Tresadern, José Manuel Bartolomé-Nebreda, Joaquin Pastor-Fernández
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Publication number: 20120252800Abstract: 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: ApplicationFiled: December 16, 2010Publication date: October 4, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Gregor James MacDonald, Gary John Tresadern, Andrés Avelino Trabanco-Suárez, Joaquin Pastor-Fernández
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Publication number: 20120220581Abstract: 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: ApplicationFiled: October 27, 2010Publication date: August 30, 2012Applicant: Janssen-Cilag, S.A.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
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Publication number: 20120094996Abstract: There is provided compounds of formula (I): wherein R1, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.Type: ApplicationFiled: April 1, 2010Publication date: April 19, 2012Applicant: Centro Nacional de Investigaciones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Guido Kurz, Sonia Martinez Gonzalez
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Publication number: 20120083492Abstract: There is provided compounds of formula (I), wherein R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: ApplicationFiled: April 16, 2010Publication date: April 5, 2012Applicant: Centro Nacional De Investigaciones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Sonia Martínez Gonzalez, Julen Oyarzabal Santamarina
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Publication number: 20110269752Abstract: 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: ApplicationFiled: April 28, 2011Publication date: November 3, 2011Inventors: 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 Martin-Martín, Sergio-Alvar Alonso-de Diego, Kelly Ann Swinney, Carina Leys, Johan Erwin Edmond Weerts, Stijn Wuyts
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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: 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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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
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Publication number: 20080269251Abstract: 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: December 18, 2006Publication date: October 30, 2008Inventors: Jose Ignacio Andre-Gil, Manuel Jesus Alcazar-Vaca, Maria Lourdes De La Morena, Sonio Martinez Gonzalez, Julen Oyarzabal Santanarina, Joaquin Pastor-Fernandez, Juan Antonio Vega Ramiro, Wilhelmus Helena Ignatius Maria Drinkenburg
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Patent number: 7169786Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonine (5-HT) reuptake inhibitor activity in combination with additional ?2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative.Type: GrantFiled: February 13, 2002Date of Patent: January 30, 2007Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Manuel Jesús Alcázar-Vaca, José Maria Cid-Nuñez, Joaquin Pastor-Fernandez, Antonius Adrianus Hendrikus Petrus Megens, Godelieve Irma Christine Maria Heylen, Xavier Jean Michel Langlois, Margaretha Henrica Maria Bakker, Thomas Horst Wolfgang Steckler
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Publication number: 20040122037Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S ; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight.Type: ApplicationFiled: August 21, 2003Publication date: June 24, 2004Inventors: Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea, Manuel Jesus Alcazar-Vaca, Jose Maria Cid-Nunez, Joaquin Pastor-Fernandez, Antonius Adrianus Henrikus Petrus Megens, Godelieve Maria Heylen, Xavier Jean Michel Langlois, Margaretha Henrica Maria Bakker, Thomas Horst Wolfgang Steckler