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US 2024/0182489 A1Published application
New 5,6,7,8-Tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one Derivatives as Sigma Ligands
AssigneeAcondicionamiento Tarrasense
InventorsUte CHRISTMANN, Jose Luís DÍAZ-FERNÁNDEZ
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Abstract
The present invention relates to new 5,6,7,8-tetrahydropyrido[4′,3′:4,5]thieno[2,3d] pyrimidin-4(3H)-one derivatives as sigma ligands having a great affinity for sigma receptors, especially sigma-1 (σ1), as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
Claims21
1-15. (canceled)
A compound of the formula:
- or a corresponding salt, co-crystal or prodrug thereof, or a corresponding solvate thereof, wherein
- R1 is an aryl optionally substituted with one or more R1a substituents;
- each of R1a is independently a halogen atom;
- a branched or unbranched C1-6 alkyl;
- —CN;
- an —OR′ where R′ is hydrogen or an unsubstituted C1-6 alkyl;
- or an optionally substituted heterocyclyl group containing one or more heteroatoms selected from N, O or S;
- R2 is a branched or unbranched C1-6 alkyl;
- or a C1-6 haloalkyl;
- R3 is a hydrogen;
- or a branched or unbranched C1-6 alkyl;
- with the proviso that when R1 is an unsubstituted phenyl, then R3 is not methyl;
- and
- with the proviso that when R3 is a hydrogen, then R1 is not a phenyl group substituted with a pyrazole.
11 more elements
Dependencies are inferred from the claim text.