Sigma-1 receptor ligands and therapeutic uses thereof
AssigneesUniversite De Strasbourg, Centre National De La Recherche Scientifique, Institut National de la Sante et de la Recherche Medicale, Universite De Montpellier, Ecole Pratique Des Hautes Etudes
InventorsJean-Jacques Bourguignon, Martine Schmitt, Jacques Bricard, Tangui Maurice
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Abstract
The present invention relates to the field of medicine. More specifically, the present invention relates to compounds that are sigma-1 receptor agonists and their use for the treatment of central nervous system disorders, including cognitive or neurodegenerative disorders, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, Amyotrophic lateral sclerosis, and multiple sclerosis.
Claims14
A compound having the following formula (I):
- wherein:
- R1 represents:
- an aryl(C1-C6)alkyl group;
- an aryl(C2-C6)alkenyl group;
- an aryl group;
- a heteroaryl group;
- a heterocycle group;
- a cycloalkyl group;
- or
- a -QR group, with Q being O or S, and R being alkyl, aryl or aralkyl;
- said group being optionally substituted by at least one-OH, halogen, (C1-C6)alkyl optionally substituted by one or more fluorine atoms, or (C1-C6)alkyloxy;
- Z represents CR2;
- R2 represents H, a (C1-C4)alkyl or a phenyl group;
- X and Y are N and CR6 respectively;
- R6 is H or a (C1-C4)alkyl group;
- n is 3, 4, 5, or 6;
- R3 and R4:
- represent independently a radical selected from a hydrogen atom, a (C1-C6)alkyl, (C2-C6)alkenyl, cycloalkyl, heterocycle, aryl, heteroaryl, and aryl(C1-C6)alkyl,
- said radical being optionally substituted by at least one substituent selected from the group consisting of a hydroxy, a (C1-C6)alkyl, a (C1-C6)alkoxy, a cycloalkyl, a heterocycle, an aryl, and a heteroaryl;
- or
- form, together with the nitrogen to which they are bound, a nitrogen-based heterocycle,
- said nitrogen-based heterocycle being optionally substituted by at least one substituent selected from the group consisting of a hydroxy, oxo, (C1-C6)alkyl, (C2-C6)alkenyl, cycloalkyl, aryl, heteroaryl, heterocycle, aryl(C1-C6)alkyl, hydroxy(C1-C6)alkyl, and said nitrogen-based heterocycle being optionally fused with at least one 5-14 membered ring selected from aryl and heteroaryl;
- each of R5 represents independently H, OH, or a (C1-C4)alkyl group;
- and
- wherein the heteroaryl group and heteroaryl comprise independently between 5 and 14 atoms and comprise one or two heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur and the heterocycle group and heterocycle are independently a saturated or unsaturated mono-, bi- or tri-cyclic alkyl group having between 3 and 20 atoms of carbons atoms and comprising one or two heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur;
- a stereoisomer, a solvate or any pharmaceutical salt thereof.
Dependencies are inferred from the claim text.