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US 8,138,186 B2Granted
Pyrazole derivatives as sigma receptors antagonists
AssigneeLaboratorios Del Dr. Esteve, S.A.
InventorsRosa Cuberes-Altisent, Joerg Holenz
Life of this patent
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Abstract
The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.
Claims22
Compounds of formula (I),
- wherein
- R1 represents a hydrogen atom;
- F;
- Cl;
- Br;
- I;
- CF3;
- OH;
- SH;
- NH2;
- CN;
- an unbranched or branched, saturated or unsaturated, substituted or unsubstituted C1-6 aliphatic group;
- an unbranched or branched, saturated or unsaturated, substituted or unsubstituted alkoxy radical;
- a saturated or unsaturated, substituted or unsubstituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with a substituted or unsubstituted mono- or polycyclic ring system;
- a branched or unbranched, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group is substituted or unsubstituted;
- a substituted or unsubstituted aryl group which may be condensed with a substituted or unsubstituted mono- or polycyclic ring system;
- a substituted or unsubstituted heteroaryl group which may be condensed with a substituted or unsubstituted mono- or polycyclic ring system;
- a branched or unbranched alkyl-aryl group in which the aryl group is substituted or unsubstituted and/or condensed with a mono- or polycyclic ring system;
- a branched or unbranched alkyl-heteroaryl group in which the heteroaryl group is substituted or unsubstituted and/or condensed with a mono- or polycyclic ring system;
- a (C═O)—R7 group;
- a (C═O)—O—R8 group;
- a (S═O2)—R9 group;
- or a (C═O)—NR10R11 group;
- R2 represents a hydrogen atom;
- F;
- Cl;
- Br;
- I;
- CF3;
- OH;
- SH;
- NH2;
- CN;
- an unbranched or branched, saturated or unsaturated, substituted or unsubstituted aliphatic group;
- an unbranched or branched, saturated or unsaturated, substituted or unsubstituted alkoxy radical;
- a saturated or unsaturated, substituted or unsubstituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with a substituted or unsubstituted mono- or polycyclic ring system;
- a branched or unbranched, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group is substituted or unsubstituted;
- a substituted or unsubstituted aryl group which may be condensed with a substituted or unsubstituted mono- or polycyclic ring system;
- a substituted or unsubstituted heteroaryl group which may be condensed with a substituted or unsubstituted mono- or polycyclic ring system;
- a branched or unbranched alkyl-aryl group in which the aryl group is substituted or unsubstituted and/or condensed with a mono- or polycyclic ring system;
- a branched or unbranched alkyl-heteroaryl group in which the heteroaryl group is substituted or unsubstituted and/or condensed with a mono- or polycyclic ring system;
- a (C═O)—R7 group;
- a (C═O)—O—R8 group;
- a (S═O)—R9 group;
- or a (C═O)—NR10R11 group;
- R3 is hydrogen;
- R4 and R5 form together with the bridging nitrogen atom a substituted or unsubstituted heterocyclyl group which is optionally condensed with a substituted or unsubstituted mono- or polycyclic ring system;
- X represents an oxygen atom;
- a CH—R12 group with R12 being a —CH3, SH, OH, NH2, CF3 group;
- Cl, F, Br, I, or CN;
- Y represents a (S═O2) group;
- m is selected from 1, 2, 3 or 4;
- n is selected from 0 or 1;
- p is selected from 0 or 1;
- s is selected from 1, 2, 3 or 4;
- and n plus p is 1;
- R7, R8, R9, R10 and R11, identical or different, represent a hydrogen atom;
- an unbranched or branched, saturated or unsaturated, substituted or unsubstituted C1-6 aliphatic group;
- a branched or unbranched, substituted or unsubstituted C1-6 alkoxy radical;
- a saturated or unsaturated, substituted or unsubstituted, optionally at least one heteroatom as ring member containing cycloalkyl group;
- a branched or unbranched, substituted or unsubstituted, optionally at least one heteroatom as ring member containing C1-6 alkyl-cycloalkyl group;
- a substituted or unsubstituted aryl group;
- a substituted or unsubstituted heteroaryl group;
- a branched or unbranched, substituted or unsubstituted C1-6 alkyl-aryl;
- a branched or unbranched, substituted or unsubstituted C1-6 alkyl-heteroaryl group;
- optionally in form of one of the stereoisomers, a racemate or in form of a mixture of at least two of the stereoisomers, in any mixing ratio, or a corresponding salt thereof.
63 more elements
Dependencies are inferred from the claim text.