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US 2010/0137368 A1Published application
Pyridine derivatives as fast dissociating dopamine 2 receptor antagonists
AssigneeJanssen Pharmaceutica NV
InventorsGregor James MacDonald, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool, Francisca Delgado-Jiménez
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Abstract
The present invention relates to (1-benzyl-piperidin-4-yl)-(pyridin-2-yl)-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.
Claims11
A compound of formula (I)
- or a pharmaceutically acceptable salt or a solvate thereof, or a stereoisomeric form thereof, wherein
- R is hydrogen or C1-6alkyl;
- R1 is phenyl;
- phenyl substituted with 1, 2 or 3 substituents each independently selected from the group consisting of halo, cyano, C1-4alkyl, C1-4alkyloxy, perfluoroC1-4alkyl, and perfluoroC1-4alkyloxy;
- thienyl;
- thienyl substituted with 1 or 2 substituents selected from the group consisting of halo and C1-4alkyl;
- C1-4alkyl;
- C1-4alkyl substituted with hydroxyl, C3-8cycloalkyl or C5-7cycloalkenyl;
- R2 is hydrogen or C1-6alkyl;
- R3, R4, R5 and R6 each independently are hydrogen, halo, C1-4alkyl, trifluoromethyl, cyano or OR7;
- R7 is hydrogen, C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-4alkyl or perfluoroC1-4alkyl;
- provided that R6 is other than cyano when R1 represents phenyl and R3, R4 and R5 are hydrogen.
9 more elements
(canceled)
Dependencies are inferred from the claim text.