Janssen Pharmaceutica Nv

Xavier Jean Michel Langlois

Gregor James MacDonald

Andrés Avelino Trabanco-Suárez

Ludo Edmond Josephine Kennis

Yves Emiel Maria Van Roosbroeck

Marcel Frans Leopold De Bruyn

Frans Alfons Maria Van Den Keybus

Michiel Luc Maria Van Gool

José Manuel Bartolomé-Nebreda

José Ignacio Andrés-Gil

Frederik Jan Rita Rombouts

Antonius Adrianus Hendrikus Petrus Megens

Meri De Angelis

Greta Constantia Peter Vanhoof

Peter Jacobus Johannes Antonius Buijnsters

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. 

Piperidin-4YL-pyridazin-3-ylamine derivatives as fast dissociating dopamine 2 receptor antagonists

The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE10). In particular, the invention relates to combinations of 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives which have been found to inhibit phosphodiesterase 2 (PDE2), with inhibitors of phosphodiesterase 10 (PDE10). Particular PDE10 inhibitors are selected from the group of MP-10, PQ-10, TP-10, papaverine, and the compounds disclosed in WO 2011/051324 and in WO 2011/110545. The invention is also directed to pharmaceutical compositions comprising such combinations, to processes for preparing such compositions, to the use of PDE2 inhibitors, in particular of 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives for the potentiation of said PDE10 inhibitors, and to the use of said PDE10 inhibitors for the potentiation of the effect of said PDE2 inhibitors, in particular, 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives, and to the use of such combinations and compositions for the prevention and treatment of disorders in which PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases.

Combinations comprising PDE 2 inhibitors such as 1-aryl-4-methyl-[1,2,4]triazolo-[4,3-A]]quinoxaline compounds and PDE 10 inhibitors for use in the treatment of neurological of metabolic disorders

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.

Piperidin-4-yl-pyridazin-3-ylamine derivatives as fast dissociating dopamine 2 receptor antagonists

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

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. 

Growing community of inventors

Beerse, Belgium

Xavier Jean Michel Langlois