AR021751A1 - MONOCICLIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE AS AN ANTAGONIST OF NK2 TAQUIQUININE RECEIVER IN THE TREATMENT OF DEPATOLOGIES WHERE THERE IS RELEASE OF TACHIQUININS - Google Patents

Abstract

Compuestos monocíclicos de la formula general (1) donde: X1, X2, X3, X4, ya sean iguales o diferentes, forman un grupo seleccionado entre: -CONR-, -NRCO-,-CH2-NR-, -NR-CH2- donde R es H, alquilo C1-3, bencilo; f y m, ya sean iguales o diferentes, sonun numero seleccionado entre 0, 1 y 2; R1 y R2, ya seaniguales o diferentes, forman un grupo -(CH2)r-Ar, donde r es igual a 0, 1, 2 y Ar es un grupo aromático seleccionado entre: benceno, naftalina, tiofeno,benzotiofeno, piridina, quinolina, indol,furano, benzofuran, tiazol, benzotiazol, imidazol, benzoimidazol, con posibilidad de sustitucion por medio de hasta 2sustitutos seleccionados entre alquilo C1-3, haloalquilo, alquiloxi C1-3, amino C2-4-alquiloxi, halogenos, OH, NH2, CN, NR6R7, dondeR6 y R7, ya sean iguales odiferentes, son H o alquilo C1-3; R3 es un grupo seleccionado entre los siguientes grupos: -(CH2)r-Ar1 donde r es igual a 0, 1, 2 y Ar1 es un grupo aromáticoseleccionado entre: benceno, naftalina, tiofeno, benzotiofeno, piridina, quinolina, indol, furano, benzofurano, tiazol, benzotiazol, imidazol, benzoimidazol,con posibilidad de sustitucion por medio de hasta 2 sustitutos seleccionados entre alquilo C1-3 y haloalquilo, alquiloxi C1-3 y amino alquiloxi, halogenos, OH,NH2, CN, NR6R7, donde R6 y R7, ya sean iguales o diferentes, son H o alquilo C1-3; R5 es H; R4 es un grupo seleccionado entre: -NR8R9, donde R8 es H o alquiloC1-3 y R9 es un metanosulfonilo, tosilo, tetrahidropiranilo, tetrahidrotiopiranilo, posiblemente mono o bisustituido por oxígeno en el átomo S, piperidiloposiblemente sustituido en el átomo N por un alquilo C1-3, acilo C1-3, amino sulfonilo, metanosulfonilo; o un grupo (CH2)g-R10 donde g es 1, 2, 3 y R10 seselecciona entre morfolino, furano,CN; o R8 y R9 junto con el átomo N al que están vinculados forman piperacina posiblemente sustituida en uno de susnitrogenos por alquilo C1-3, acilo C1-3 o metanosulfonilo; N(R11)CO(CH2)h-R12 donde R11 es H o alquilo C1-3; h es 0, 1, 2, 3; y R12 seselecciona entre:morfolino, pirrolidino posiblemente sustituido por hidroxi o hidroximetil, piperidina posiblemente sustituido por un grupo hidroxicarboxilamido oMonocyclic compounds of the general formula (1) where: X1, X2, X3, X4, whether the same or different, form a group selected from: -CONR-, -NRCO -, - CH2-NR-, -NR-CH2- where R is H, C1-3 alkyl, benzyl; f and m, whether the same or different, are a number selected from 0, 1 and 2; R1 and R2, whether equal or different, form a group - (CH2) r-Ar, where r is equal to 0, 1, 2 and Ar is an aromatic group selected from: benzene, naphthalene, thiophene, benzothiophene, pyridine, quinoline , indole, furan, benzofuran, thiazole, benzothiazole, imidazole, benzoimidazole, with the possibility of substitution by means of up to 2 substitutes selected from C1-3 alkyl, haloalkyl, C1-3 alkyloxy, C2-4-alkyloxy, halogens, OH, NH2 , CN, NR6R7, where R6 and R7, whether equal or different, are H or C1-3 alkyl; R3 is a group selected from the following groups: - (CH2) r-Ar1 where r is equal to 0, 1, 2 and Ar1 is an aromatic group selected from: benzene, naphthalene, thiophene, benzothiophene, pyridine, quinoline, indole, furan , benzofuran, thiazole, benzothiazole, imidazole, benzoimidazole, with the possibility of substitution by means of up to 2 substitutes selected from C1-3 alkyl and haloalkyl, C1-3 alkyloxy and amino alkyloxy, halogens, OH, NH2, CN, NR6R7, where R6 and R7, whether the same or different, are H or C1-3 alkyl; R5 is H; R4 is a group selected from: -NR8R9, where R8 is H or C1-3alkyl and R9 is a methanesulfonyl, tosyl, tetrahydropyranyl, tetrahydrothiopyranyl, possibly mono or bis-substituted by oxygen in the S atom, piperidylpossibly substituted on the N atom by an alkyl C1-3, C1-3 acyl, amino sulfonyl, methanesulfonyl; or a group (CH2) g-R10 where g is 1, 2, 3 and R10 is selected from morpholino, furan, CN; or R8 and R9 together with the N atom to which they are linked form piperazine possibly substituted in one of susnitrogens by C1-3 alkyl, C1-3 acyl or methanesulfonyl; N (R11) CO (CH2) h-R12 where R11 is H or C1-3 alkyl; h is 0, 1, 2, 3; and R12 is selected from: morpholino, pyrrolidino possibly substituted by hydroxy or hydroxymethyl, piperidine possibly substituted by a hydroxycarboxylamide group or