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US 2015/0031692 A1Published application
Substituted pyrano and furanoquinolines, their preparation and use as medicaments
AssigneeLaboratorios Del Dr. Esteve, S.A.
InventorsJosé-Luis Diaz-Fernández, Ute Christmann
Life of this patent
Estimating the term…
Abstract
The present invention relates to new substituted pyrano and furanoquinolines having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
Claims18
1-17. (canceled)
A compound of general formula (I):
- wherein
- R1 is a saturated or unsaturated C3-9 cycloalkyl optionally at least monosubstituted, optionally at least containing one heteroatom as a ring member selected from N, O or S, which may be condensed with an optionally at least monosubstituted mono or polycyclic ring system;
- R2 is selected from the group consisting of hydrogen;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C1-10 or —CH2R5;
- R3 and R4 are independently selected from the group consisting of hydrogen;
- —NO2;
- —CF3;
- —OH;
- —SH;
- —NR5R6;
- —CN;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C1-10;
- a saturated or unsaturated C3-9 cycloalkyl optionally at least monosubstituted, optionally at least containing one heteroatom as a ring member selected from N, O or S which may be condensed with an optionally at least monosubstituted mono or polycyclic ring system;
- a substituted or unsubstituted aryl;
- —NHC(O)NHR7;
- —NHC(S)NHR7;
- —C(O)OR8;
- —OR9;
- —NR10C(O)R11;
- —SR12;
- —C(O)NR13R14;
- —SO2NR15R16, or halogen;
- R5 to R12 are independently selected from hydrogen;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C1-10;
- substituted or unsubstituted aryl;
- substituted or unsubstituted C3-9 cycloalkyl optionally at least containing one heteroatom as a ring member selected from N, O or S which may be condensed with an optionally at least monosubstituted mono or polycyclic ring system;
- or substituted or unsubstituted heteroaryl which may be condensed with an optionally at least monosubstituted mono or polycyclic ring system;
- R13 to R16 are independently selected from hydrogen;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C1-10;
- substituted or unsubstituted aryl;
- substituted or unsubstituted C3-9 cycloalkyl optionally at least containing one heteroatom as a ring member selected from N, O or S which may be condensed with an optionally at least monosubstituted mono or polycyclic ring system;
- substituted or unsubstituted heteroaryl which may be condensed with an optionally at least monosubstituted mono or polycyclic ring system;
- or R13 to R16 together with a bridging nitrogen form a C3-9 cycloalkyl optionally containing at least one additional heteroatom as a ring member selected from N, O or S;
- n is 0 or 1;
- with the proviso that at least one of R3 or R4 is always different from hydrogen and with the proviso that when R1 is cyclohexyl, unsubstituted tetrahydrofurane or substituted pyrrolidine, if R3 or R4 are in position 8 when n=0 or in position 9 when n=1, they are not tert-butyl,
- or a pharmaceutically acceptable salt, isomer, prodrug or solvate thereof.
33 more elements
A compound according to claim 8, wherein R3 and R4 are independently selected from the group consisting of hydrogen;
- halogen;
- —NO2;
- —CF3;
- —OH;
- —SH;
- —NR5R6;
- —CN;
- a substituted or unsubstituted, branched or unbranched C1-6alkyl;
- —NHC(O)NHR7;
- —C(O)OR8;
- —OR9;
- —SR12;
- —SO2NR15R16 or a group selected from:
- wherein R independently represents a hydrogen;
- substituted or unsubstituted, branched or unbranched C1-6alkyl, an OH or a halogen and wherein m=0 or 1 and p=3 or 4.
12 more elements
Dependencies are inferred from the claim text.