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US 2010/0076187 A1Published application
Fast dissociating dopamine 2 receptor antagonists
AssigneeJanssen Pharmaceutica NV
InventorsGregor James MacDonald, José Ignacio Andrés-Gil, Frans Alfons Maria Van Den Keybus, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
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Abstract
The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles 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.
Claims10
A compound of formula (I)
- or a pharmaceutically acceptable salt or 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 hydrogen, halo, cyano, C1-4alkyl,
- C1-4alkyloxy, perfluoroC1-4alkyl, and trifluoromethoxy;
- 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;
- C3-8cycloalkyl;
- or C5-7cycloalkenyl;
- R2 is hydrogen or C1-6alkyl;
- R3 and R4 each independently are hydrogen, C1-4alkyl or halo, or R3 and R4 together form a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring comprising at least one oxygen, nitrogen or sulfur atom.
12 more elements
Dependencies are inferred from the claim text.