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US 2012/0059006 A1Published application
Sigma receptor inhibitors
AssigneeLaboratorios Del Dr. Esteve, S.A.
InventorsRosa CUBERES-ALTISENT, Joerg HOLENZ
Life of this patent
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Abstract
The invention relates to compounds of formula I having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
Claims14
1-17. (canceled)
A method of treating or preventing a sigma receptor mediated disease or condition, said method comprising administering to a patient in need of such a treatment a therapeutically effective amount of a compound of the formula I:
- wherein
- R1 is selected from the group formed by hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyclylalkyl, —COR8, —C(O)OR8, —C(O)NR8R9 —C═NR8, —CN, —OR8, —OC(O)R8, —S(O)t—R8 , —NR8R9, —NR8C(O)R9, —NO2, —N═CR8R9, or halogen;
- R2 is selected from the group formed by hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyclylalkyl, —COR8, —C(O)OR8, —C(O)NR8R9—C═NR8, —CN, —OR8, —OC(O)R8, —S(O)t—R8, —NR8R9, —NR8C(O)R9, —NO2, —N═CR8R9, or halogen;
- Y is selected from substituted or unsubstituted, branched or linear C1-6-alkyl;
- substituted or unsubstituted C3-8-cycloalkyl;
- R5 and R6 are independently selected from the group formed by hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyclylalkyl, —COR8, —C(O)OR8, —C(O)NR8R9 —C═NR8, —CN, —OR8, —OC(O)R8, —S(O)t—R8 , —NR8R9, —NR8C(O)R9, —NO2, —N═CR8R9, or halogen;
- together form, with the nitrogen atom to which they are attached, a substituted or unsubstituted heterocyclyl group;
- n is selected from 1, 2, 3, 4, 5, 6, 7 or 8;
- t is 1,2 or 3;
- R8 and R9 are each independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, or halogen;
- optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
8 more elements
Dependencies are inferred from the claim text.