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US 2017/0362215 A1Published application
1-methylpyrazole-piperazine compounds having multimodal activity against pain
AssigneeLaboratorios Del Dr. Esteve, S.A.
InventorsCarmen ALMANSA-ROSALES, Monica GARCIA-LOPEZ, Lourdes GARRIGA-SANAHUJA
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Abstract
The present invention relates to 1-methylpyrazole-piperazine compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
Claims19
1-15. (canceled)
A compound of general formula (l):
- wherein
- n is 1, 2, 3, 4, 5 or 6;
- Y—W is CRy—N or N—CRw;
- X is a bond or —CR6R6′—;
- R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclyl;
- R2 is substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclyl;
- R3 is hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, or substituted or unsubstituted alkylheterocyclyl;
- R4, R4′, R4″ and R4′″ are independently selected from hydrogen or unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, and unsubstituted C2-6 alkynyl;
- R5′ and R5′ are independently selected from hydrogen or unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, and unsubstituted C2-6 alkynyl;
- R6 is selected from hydrogen, halogen, —OR7, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, —C(O)OR7, —C(O)NR7R7′, —NR7C(O)R7′, and —NR7R7′″—;
- R6′ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- wherein R7, R7′ and R7″ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, and unsubstituted acetyl;
- and R7′″ is selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl and -Boc;
- Ry is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- Rw is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- optionally as a stereoisomer, a racemate or a mixture of at least two of stereoisomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
13 more elements
Dependencies are inferred from the claim text.