AR058180A1 - Indeno derivados, su preparacion y su uso como medicamentos - Google Patents

Indeno derivados, su preparacion y su uso como medicamentos

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Publication number
AR058180A1
AR058180A1 ARP060104876A ARP060104876A AR058180A1 AR 058180 A1 AR058180 A1 AR 058180A1 AR P060104876 A ARP060104876 A AR P060104876A AR P060104876 A ARP060104876 A AR P060104876A AR 058180 A1 AR058180 A1 AR 058180A1
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AR
Argentina
Prior art keywords
alkyl
independently selected
substituted
phenyl
radical
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ARP060104876A
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English (en)
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Esteve Labor Dr
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Priority claimed from ES200502720A external-priority patent/ES2274725B1/es
Application filed by Esteve Labor Dr filed Critical Esteve Labor Dr
Publication of AR058180A1 publication Critical patent/AR058180A1/es

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Abstract

La presente hace referencia a su procedimiento de preparacion, a su aplicacion como medicamento y a composiciones farmacéuticas que los comprenden. Los compuestos muestran afinidad por los receptores 5-HT6 por lo que se utilizan para el tratamiento de las enfermedades mediadas por estos receptores. Reivindicacion 1: Un indeno derivado de formula general (1) donde: n es 0, 1, 2, 3 o 4; R1 representa un radical cicloalifático saturado o insaturado, opcionalmente al menos monosustituido, opcionalmente al menos con un heteroátomo seleccionado entre N, O y S como miembro del anillo que puede estar condensado con un sistema anular mono o policíclico opcionalmente al menos monosustituido; un radical -NR8R9-; un radical -CONR8R9; -COOH; o -OH donde R8 y R9 representan, independientemente entre sí, un átomo de H; o un radical alifático C1-5 lineal o ramificado, saturado o insaturado, que puede estar sustituido con 1, 2, 3 sustituyentes seleccionados independientemente entre F, Cl, Br, -OH, -NH2, -SH, -O-CH3, -O-C2H5, -NO2, -CN, -NH-CH3 y -S-CH3; R8 y R9 conjuntamente con el N forman un anillo heterocíclico de 3 a 9 miembros saturado, insaturado o aromático, que puede estar sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre C1-5 alquil, -O-C1-5 alquil, -S-C1-5-alquil, oxo (=O), tioxo (=S), -C(=O)-OH, -C(=O)-O-C1-5-alquil, -O-C(=O)-C1-5 alquil, F, Cl. Br, I, -CN, -CF3, -OCF3, -SCF3, -OH, -SH, -NH2, -NH(C1-5 alquil), -N(C1-5 alquil)2, -NO2, -CHO, -CF2H, -CFH2, -C(=O)-NH2, -C(=O)-NH(C1-5 alquil), -C(=O)-N(C1-5 alquil)2, -S(=O)2-C1-5 alquil, -S(=O)2-fenil y que pueden contener 1, 2 o 3 heteroátomos adicionales independientemente seleccionados entre N, O y S como miembros del anillo; R2, R3, R4 y R5 representan, independientemente entre sí, un átomo de H, -NO2, -NH2, -SH, -OH, -CN, -C(=O)-H, -C(=O)-R10, -OR11, -SR12, -SOR13, -S(=O)2-E13, S(=O)2-N(R14)R15, -N(R16)-S(=O)2-R17, -NH-R18, -NR19R20, -N(R21)-CO-R22; F, Cl, BR, I, un radical alifático C1-6 lineal o ramificado, saturado o insaturado, que puede estar sustituido por 1, 2 o 3 sustituyentes independientemente seleccionados entre F, Cl, Br, -OH, -NH2, -SH, -O-CH3, -O-C2H5, -NO2, -CN, -NH-CH3 y -S-CH3; o un radical arilo o heteroarilo de 5 a 14 miembros, que puede estar sustituido con 1, 2 o 3 sustituyentes independientemente seleccionados entre -CF3, C1-5- alquil, -O-C1-5- alquil, -S-C1-5-alquil, -C(=O)-OH, -C(=O)-O-C1-5 alquil, -O-C(=O)-C1-5-alquil, F, Cl Br, I, - CN, -OCF3, -SCF3, -OH, -SH, -NH2, -NH(C1-5 alquil), -N(C1-5 alquil)2, -NH-C(=O)-C1-5 alquil, -N(C1-5-alquil)-C(=O)-C1-5-alquil, -NO2, -CHO, -CF2H, -CFH2, -C(=O)-NH2, -C(=O)-NH(C1-5 alquil), -C(=O)-N(C1-5 alquil)2, -S(=O)2-C1-5 alquil, -S(=O)2-fenil, ciclopropil, ciclobutil, ciclopentil, ciclohexil, fenil, fenoxi, benciloxi y bencil y que pueden estar unidos a través de un grupo C1-6 alquileno lineal o ramificado y donde el radical heteroarilo contiene 1, 2 o 3 heteroátomos independientemente seleccionados entre N, O y S como miembros del anillo; con la condicion de que al menos uno de los sustituyentes R2, R3, R4 y R5 represente un radical -NO2, -SOR13, -S(=O)2-R13, -S(=O)2-N(R14)R15, -N(R16)-S(=O)2-R17, -N(R21)-CO-R22; A representa C=C(R6)R'6 o (R6)C-R'6 lo que significa, respectivamente, compuestos tipos (2) y (3); R6 y R'6, idénticos o diferentes, representan un átomo de H, -NO2, -NH2, -SH, -OH, -CN, -C(=O)-R10, -OR11, -SR12, F, Cl, BR, I, un radical alifático C1-10 lineal o ramificado, saturado o insaturado, que puede estar sustituido por 1, 2 o 3 sustituyentes independientemente seleccionados entre F, Cl, Br, -OH, -SH, -O-CH3, -O-C2H5, -NO2, -CN, y -S-CH3; o un radical arilo o heteroarilo de 5 a 14 miembros, que puede ser sustituido por 1, 2 o 3 sustituyentes independientemente seleccionado entre -CF3, C1-5- alquil, -O-C1-5- alquil, -S-C1-5-alquil, -C(=O)-OH, -C(=O)-O-C1-5 alquil, -O-C(=O)-C1-5-alquil, F, Cl Br, I, -CN, -OCF3, -SCF3, -OH, -SH, -NH2, -NH(C1-5 alquil), -N(C1-5 alquil)2, -NH-C(=O)-C1-5 alquil, -N(C1-5-alquil)-C(=O)-C1-5-alquil, -NO2, -CHO, -CF2H, -CFH2, -C(=O)-NH2, -C(=O)-NH(C1-5 alquil), -C(=O)-N(C1-5 alquil)2, -S(=O)2-C1-5 alquil, -S(=O)2-fenil, ciclopropil, ciclobutil, ciclopentil, ciclohexil, fenil, fenoxi, benciloxi y bencil y que pueden estar unidos a través de un grupo C1-6 alquileno, C2-6 alquenileno o C1-6 ilideno lineales o ramificados y donde el radical heteroaril contiene 1, 2 o 3 heteroátomos independientemente seleccionados entre N, O y S como miembros del anillo; R7 representa un átomo de H, un radical alifático C1-6 lineal o ramificado que pude estar sustituido por 1, 2 o 3 sustituyentes independientemente seleccionados entre F, Cl, Br, -OH, -SH, -O- CH3, -O-C2H5, -NO2, -CN y -S-CH3; R10 a R22 representan, independientemente entre sí, un átomo de H, un radical alifático C1-5 lineal o ramificado, saturado o insaturado, que puede estar sustituido con 1, 2 o 3 sustituyentes independientemente seleccionados entre F, Cl, Br, -OH, NH2, -SH, -O-CH3, -O-C2H5, -NO2, -CN, -NH-CH3 y -S-CH3; un radical cicloalifático de 3 a 8 miembros saturado o insaturado, que puede estar sustituido con 1, 2 o 3 sustituyentes seleccionados entre C1-5-alquil, -O- C1-5-alquil, -S-C1-5-alquil, oxo (=O), tioxo (=S), -C(=O)-OH, -C(=O)-O-C1-5 alquil, -O-C(=O)-C1-5 alquil, F, Cl, Br, I, -CN, -CF3, -OCF3, -SCF3, -OH, -SH, -NH2, -NH(C1-5 alquil), -N(C1-5 alquil)2, -NO2, -CHO, -CF2H, -CFH2, -C(=O)-NH2, -C(=O)NH(C1-5 alquil), -C(=O)-NC1-5 alquil)2, -S(=O)2-C1-5 alquil, -S(=O)2-fenil, ciclopropil, ciclobutil, ciclopentil, ciclohexil, fenil, fenoxi, benciloxi y bencil y que opcionalmente puede contener 1, 2 o 3 heteroátomos independientemente seleccionados entre N, O y S como miembros del anillo y que pueden estar unidos a través de un grupo C1-6 alquileno lineal o ramificado; o un radical arilo o heteroarilo de 5 a 14 miembros que puede estar sustituidos con 1, 2 o 3 sustituyentes independientemente seleccionados entre -CF3, C1-5- alquil, -O-C1-5- alquil, -S-C1-5-alquil, -C(=O)-OH, -C(=O)-O-C1-5 alquil, -O-C(=O)-C1-5-alquil, F, Cl Br, I, -CN, -OCF3, -SCF3, -OH, -SH, -NH2, -NH(C1-5 alquil), -N(C1-5 alquil)2, -NH-C(=O)-C1-5 alquil, -N(C1-5- alquil)-C(=O)-C1-5-alquil, -NO2, -CHO, -CF2H, -CFH2, -C(=O)-NH2, -C(=O)-NH(C1-5 alquil), -C(=O)-N(C1-5 alquil)2, -S(=O)2-C1-5 alquil, -S(=O)2-fenil, ciclopropil, ciclobutil, ciclopentil, ciclohexil, fenil, fenoxi, benciloxi y bencil y que pueden estar unidos a través de un grupo C1-6 alquileno, C2-6 alquenileno o C2-6 alquinileno lineales o ramificados y donde el radical heteroarilo contiene 1, 2 o 3 heteroátomos independientemente seleccionados entre N, O y S como miembros del anillo; con la condicion de que cuando R1 sea -COOH; R2, R3, R4 o R5 no sean -SOR13, -S(=O)2-R13 o -S(=O)2-N(R14)R15 y A no represente C=C(R6)R6' dándose la situacion conjunta en que R6 o R6' sean uno H y el otro un fenilo sustituido por -S(=O)2-C1-5 alquil, - NH2, -O-C1-5 alquil, F, Cl, Br, CN, -C(=O)-OH o -C(=O)-O-C1-5 alquil, o la situacion en que tanto R6 como R6' representen -OR11, y con la condicion de que cuando R1 sea -OH; R2, R3, R4 o R5 no sean -S(=O)2-R13 o -S(=O)2-N(R14)R15, y con la condicion de que cuando R1 sea -CONR8R9; R2, R3, R4 o R5 no sean -SOR13, -S(=O)2-R13 o -S(=O)2-N(R14)R15 y A no represente C=C(R6)R'6 dándose la situacion conjunta en que R6 o R'6 sean uno H y el otro un fenilo sustituido por -S(=O)2-C1-5 alquil, -NH2, -O-C1- 5 alquil, F, Cl, Br, CN, -C(=O)-OH o -C(=O)-O-C1-5 alquil, o una sal farmacéuticamente aceptable, un isomero, un profármaco o un solvato del mismo, opcionalmente en forma de uno de sus esteroisomeros, preferiblemente enantiomeros o diasteromeros, un racemato o en forma de una mezcla de al menos dos esteroisomeros, preferiblemente enantiomeros y/o diasteromeros, en cualquier proporcion de mezcla o una sal fisiologicamente aceptable de los mismos o el correspondiente solvato de los mismos.
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