Janssen Pharmaceutica Nv

Vanderbilt University

Beerse Pharmaceutica Nv

José Manuel Bartolomé-Nebreda

Gregor James MacDonald

Susana Conde-Ceide

Michiel Luc Maria Van Gool

Craig William Lindsley

P Jeffrey Conn

José Ignacio Andrés-Gil

Shaun R Stauffer

Manuel Jesús Alcázar-Vaca

Carrie K Jones

Han Min Tong

Francisco Javier Fernández-Gadea

Joaquin Pastor-Fernández

Frans E Janssens

Joseph Elisabeth Leenaerts

Marcel Frans Leopold De Bruyn

Antonius Adrianus Hendrikus Petrus Megens

María Luz Martín-Martín

Xavier Jean Michel Langlois

Greta Constantia Peter Vanhoof

Antonio Gómez-Sánchez

Jason Manka

Ya Zhou

Pedro Martínez-Jiménez

Miguel Angel Pena-Piñón

Koenraad Arthur Van Rossem

Jon Jacobs

Andrés Avelino Trabanco-Suárez

Kristof Van Emelen

Gary John Tresadern

Frans Alfons Maria Van Den Keybus

Manuel Jesus Alcazar Vaca

Frank Tegtmeier

Johan Erwin Edmond Weerts

Carina Leys

Óscar Delgado-González

Sergio-Alvar Alonso-de Diego

Maria Encarnacion Matesanz-Ballesteros

Francisca Delgado-Jiménez

Stijn Wuyts

Margaretha Henrica Maria Bakker

Kelly Ann Swinney

Chrysa Malosh

Gregor Macdonald

Laurent Christian L Leclercq

Maria Encamacion Matesanz-Ballesteros

Gregor James Macdonald

Kristol Van Emelen

Rosa Maria Alvarez-Escobar

Jos Van Reempts

Maria De Las Mercedes Garcia-Martin

Manuel Jesus Alcázar-Vaca

Jozef Leo Henri Van Reempts

Eric S Dawson

José Ignacio ANDRÉS-Gil

ÓScar Delgado-GONZÁLEZ

The present invention relates to novel imidazo[1,2-b]pyridazine and imidazo[1,2-a]-pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which may be 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.

Inhibitors of phosphodiesterase 10 enzyme

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.

Fast-dissociating dopamine 2 receptor antagonists

In one aspect, the invention relates to substituted pyrazolo[1,5-a]pyrazines 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.

Substituted pyrazolo[1,5-a]pyrazines as mGluR5 receptor modulators

In one aspect, the invention relates to novel bicyclic oxazole and thiazole compounds which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 ('mGluR5'); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions; and methods for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. 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.

Bicyclic oxazole and thiazole compounds and their use as allosteric modulators of mGluR5 receptors

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.

Bicyclic thiazoles as allosteric modulators of mGluR5 receptors

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.

Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mGluR5 receptors

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.

Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists

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.

4-alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists

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. 

Piperazin-1-yl-trifluoromethyl-substituted-pyridines as fast dissociating dopamine 2 receptor antagonists

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.

Substituted imidazopyrimidin-5(6H)-ones as allosteric modulators of MGLUR5 receptors

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.

Imidazo[1,2-a]pyrazine derivatives and their use for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases

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.

Naphthyridinone analogs as mGluR5 positive allosteric modulators

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. 

The present invention relates to novel imidazo[1,2-]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.

Imidazo[1,2-b]pyridazine derivatives and their use as PDE10 inhibitors

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Toledo, Spain

José Manuel Bartolomé-Nebreda