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US 8,895,562 B2Granted
Piperazin-1-yl-trifluoromethyl-substituted-pyridines as fast dissociating dopamine 2 receptor antagonists
AssigneeJanssen Pharmaceutica NV
InventorsJosé Manuel Bartolomé-Nebreda, Gregor James MacDonald, Michiel Luc Maria Van Gool
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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.
Claims5
A compound of formula (I)
- or a stereoisomeric form thereof, wherein
- -A1=A2- is —N═CR1— or —CR1═N—;
- R1 is hydrogen, hydroxy, halo, cyano, C1-3alkyloxy or C1-3alkyl;
- R2 is phenyl;
- phenyl substituted with one, two or three substituents selected from the group consisting of halo, cyano, C1-3alkyl, hydroxyC1-3alkyl, mono- and polyhalo -C1-3alkyl, C1-3alkyloxy, C1-3alkyloxyC1-3alkyl aminocarbonyl, mono-and di(C1-3alkyl)aminocarbonyl, amino, mono- and di(C1-3alkyl)amino;
- pyridinyl;
- pyridinyl substituted with one or two substituents selected from the group consisting of halo, C1-3 alkyloxy, arylC1-3alkyloxy, mono- and di(C1-3alkyl)amino, and arylC1-3alkylamino;
- thienyl substituted with one or two substituents selected from the group consisting of halo and C1-3alkyl;
- or a salt thereof.
6 more elements
Dependencies are inferred from the claim text.