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US 8,299,113 B2Granted
Bicyclic tetrahydropyrrole compounds
AssigneeLaboratorios Del Dr. Esteve, S.A.
InventorsMiguel Angel Pericas-Brondo, Antonio Torrens-Jover, Susana Yenes-Minguez, Félix Cuevas Cordobes, Carmen Garcia Granda
Life of this patent
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Abstract
The present invention relates to substituted bicyclic tetrahydropyrrole compounds of general 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.
Claims36
A substituted bicyclic tetrahydropyrrole compound of general formula (I)
- wherein
- R1 represents a hydrogen atom;
- an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cyclyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another, optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another, at least mono-substituted mono- or polycyclic ring system or;
- an optionally, at least mono-substituted benzhydryl group;
- wherein the bond between Y and Z may be unsaturated (Y═Z) or saturated (Y—Z);
- in case of Y and Z being (Y═Z), Y represents CH and Z represents C—R6;
- C—CHR7R7a;
- a C—(C═O)—R8 group;
- a C—CH2(SO2)—R9 group;
- a C—CH2(SO2)—NR10R10a group;
- or a C—(C═O)—NR10R10a group;
- in case of Y and Z being (Y—Z), Y represents CH2;
- C—R11R12;
- a CH—(C═O)—R16 group;
- a CH—(SO2)—R17 group;
- CH—(SO2)—NR18R18a group;
- or a CH—(C═O)—NR18R18a group and Z represents CH—R6;
- CH—CHR7R7a;
- a CH—(C═O)—R8 group;
- a CH—CH2(SO2)—R9 group;
- a CH—CH2(SO2)—NR10R10a group;
- or a CH—(C═O)—NR10R10a group;
- R2, R3, R4, and R6 represent a hydrogen atom;
- a linear or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic group;
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cyclyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another, optionally at least mono-substituted mono- or polycyclic ring system or;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another, at least mono-substituted mono- or polycyclic ring system;
- R5, R5a, identical or different, represent a hydrogen atom;
- a linear or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic group;
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cyclyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another, optionally at least mono-substituted mono- or polycyclic ring system or;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another, at least mono-substituted mono- or polycyclic ring system;
- R7, R7a, identical or different, represent a hydrogen atom;
- a linear or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic group;
- an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted alkoxy radical;
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cyclyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another, optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another, at least mono-substituted mono- or polycyclic ring system;
- R8, R9, R13, R14, R15, R16 and R17 represent a hydrogen atom;
- a linear or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic group;
- an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted alkoxy radical;
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cyclyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system or;
- a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another, optionally at least mono-substituted mono- or polycyclic ring system or;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another, at least mono-substituted mono- or polycyclic ring system;
- R10, R10a, identical or different, represent a hydrogen atom;
- a linear or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic group;
- an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted alkoxy radical;
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cyclyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another, optionally at least mono-substituted mono- or polycyclic ring system or;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another, at least mono-substituted mono- or polycyclic ring system;
- R11 and R12, identical or different, represent a hydrogen atom;
- a linear or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic group;
- an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted alkoxy radical;
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cyclyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another, optionally at least mono-substituted mono- or polycyclic ring system or;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another, at least mono-substituted mono- or polycyclic ring system;
- a —{SO2)—R13-group;
- or a —NR14R15-group;
- R18 and R18a, identical or different, represent a hydrogen atom;
- a linear or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic group;
- an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted alkoxy radical;
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cyclyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another, optionally at least mono-substituted mono- or polycyclic ring system or;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another, at least mono-substituted mono- or polycyclic ring system;
- R19 represent a hydrogen atom;
- a linear or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic group;
- an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted alkoxy radical;
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cyclyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another, optionally at least mono-substituted mono- or polycyclic ring system;
- a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another, at least mono-substituted mono- or polycyclic ring system;
- optionally in form of one of the stereoisomers, or a corresponding salt thereof.
80 more elements
Dependencies are inferred from the claim text.