AR054189A1 - Derivados de indol para el tratamiento de enfermedades inflamatorias - Google Patents

Derivados de indol para el tratamiento de enfermedades inflamatorias

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Publication number
AR054189A1
AR054189A1 ARP060101712A ARP060101712A AR054189A1 AR 054189 A1 AR054189 A1 AR 054189A1 AR P060101712 A ARP060101712 A AR P060101712A AR P060101712 A ARP060101712 A AR P060101712A AR 054189 A1 AR054189 A1 AR 054189A1
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Argentina
Prior art keywords
alkyl
group
haloalkyl
aryl
heteroaryl
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ARP060101712A
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English (en)
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Juergen Mack
Peter Mickolaus
Rainer Walter
Ralf Anderskewitz
Horst Dollinger
Rolf Goeggel
Birgit Jung
Joerg Kley
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Boehringer Ingelheim Int
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Priority claimed from DE102005019718A external-priority patent/DE102005019718A1/de
Priority claimed from DE102005023207A external-priority patent/DE102005023207A1/de
Priority claimed from DE102005035575A external-priority patent/DE102005035575A1/de
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR054189A1 publication Critical patent/AR054189A1/es

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Abstract

Son apropiados para el tratamiento de trastornos o enfermedades gastrointestinales o de las vías respiratorias, enfermedades inflamatorias de las articulaciones, la piel o los ojos, enfermedades del sistema nervioso periférico o central o enfermedades cancerígenos, así como composiciones farmacéuticas que contienen estos compuestos. Reivindicacion 1: Compuesto de la formula (1), en donde significan: A es CO, C=NH, alquileno C1-6 o cicloalquileno C3-8; B1 es fenilo o un anillo aromático o no aromático, que eventualmente puede contener uno, dos o tres heteroátomos seleccionados del grupo oxígeno, azufre y nitrogeno y que puede estar eventualmente mono- o polisustituido con uno o varios radicales seleccionados del grupo OH, O-alquiloC1-6, O-haloalquiloC1-6, halogeno, alquilo C1-6 y haloalquilo C1-6; B2 es fenilo o un heteroarilo, que puede contener uno, dos o tres heteroátomos seleccionados del grupo oxígeno, azufre y nitrogeno; X es O, S, NR5 o CR6R7; n es 0, 1, 2 o 3; R1 es H, alquilo C1-6, haloalquilo C1-6, COR1.1, COOR1.1, CH2COOR1.1; R1.1 es H o alquilo C1-6; R2 es H, alquilo o haloalquilo C1-6; o R1 y R2 forman junto con el nitrogeno un heterociclo no aromático, que puede contener uno, dos o tres heteroátomos seleccionados del grupo oxígeno y nitrogeno; o R2, N, A y B1 forman juntos un grupo bicíclico de la formula (2), en donde significan: A es CO, C=NH o alquilo C1-3; m es 1, 2 o 3; y R3 es H o un radical seleccionado del grupo compuesto por OH, haloalquilo C1-6, un arilo C6-10, un heteroarilo C5-10 y un heterociclo C3-10, en donde el heterociclo C3-10 y el heteroarilo C5-10 pueden contener uno, dos o tres heteroátomos seleccionados del grupo oxígeno, azufre y nitrogeno, que puede estar eventualmente sustituido con uno o varios radicales seleccionados del grupo compuesto por alquilo C1-6, arilo C6-10, eventualmente cicloalquilo C3-8 en puente y haloalquilo C1-6, que puede estar eventualmente sustituido con un radical del grupo compuesto por alquilo C1-6, haloalquilo C1-6, OH, halogeno y arilo C6-10; R3 es alquilo C1-6, que pueden estar eventualmente sustituido con uno o varios radicales seleccionados del grupo compuesto por hidrogeno, OH, CN, CNH2, CNH-alquiloC1-6, CON(alquiloC1-6)2, COOH, COO-alquiloC1-6, COH, CO-alquiloC1-6, CO-ariloC6-10, OH, O-alquiloC1-6, O-haloalquiloC1-6, halogeno, SH, S-alquiloC1-6, S-haloalquiloC1-6, SO2-alcanolC1-6; SO2-alquiloC1-6, SO2-haloalquiloC1-6, SO2-NH2, SO2-NH-alquiloC1-6, SO2-N(alquiloC1-6)2, NO2, NH2, NH-alquiloC1-6 y N(alquiloC1-6)2; o R3 es un radical seleccionado del grupo compuesto por cicloalquilo C3-8, cicloalquenilo C5-8, alquilo C1-6 y alcanol, que puede estar eventualmente sustituido con uno o varios radicales seleccionados del grupo compuesto por arilo C6-10, cicloalquilo C3-8, un heteroarilo C5-10 y un heterociclo C3-10, puede estar eventualmente sustituido con uno o varios radicales del grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1.-6, CN, CONH2, CONH-alquiloC1-6, CON(alquiloC1-6)2, COOH, COO-alquiloC1-6, COH, CO-alquiloC1-6, COarilo, OH, O-alquiloC1-6, O-haloalquiloC1-6, halogeno, SH, S-alquiloC1-6, S-haloalquiloC1-6, SO2-alcanolC1-6, SO2- alquiloC1-6, SO2-haloalquiloC1-6, SO2-NH2, SO2-NH-alquiloC1-6, SO2-N(alquiloC1-6)2, NO2, NH2, NH2-alquiloC1-6, N(alquiloC1-6)2, un heteroarilo C5-10 y un heterociclo C3-10, en donde el heteroarilo C5-10 y el heterociclo C3-10 pueden estar eventualmente sustituidos con un radical seleccionado de oxo, hidroxilo, halogeno, alquilo C1-6 y haloalquilo C1-6; o R3 es un radical seleccionado de un grupo compuesto por arilo C6-10, un heteroarilo C6-10 y un heterociclo C3-10, que puede estar sustituido con uno o varios radicales seleccionados del grupo compuesto por arilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, CO-NH2, CONH-alquiloC1-6, CON(alquiloC1-6)2, COOH, COO-alquiloC1-6, COH, CO-alquiloC1-6, CO-alquiloC6- 10, OH, O-alquiloC1-6, O-haloalquiloC1-6, halogeno, SH, S-alquiloC1-6, S-haloalquiloC1-6, SO2-alquiloC1-6, SO2-alcanolC1-6, SO2-haloalquiloC1-6, SO2-NH2, SO2-NH-alquiloC1-6, SO2-N(alquiloC1-6)2, NO2, NH2, NH-alquiloC1-6, N(alquiloC1-6)2 y N-(SO2- alquiloC1-6)(R3.4; o R3 es un radical seleccionado del grupo compuesto por alquilo C1-6, arilC6-10-alquilenoC1-6, heteroarilC5-10-alquilenoC1-6, cicloalquilo C3-7, arilo C6-10, un heteroarilo C5-10 y un heterociclo C3-10, que eventualmente puede estar sustituido con uno o varios radicales del grupo compuesto por B, halogeno, OH, alquilo C1-6 y oxo; en donde B es un compuesto de la formula (3), en donde Z1 significa H, OH, halogeno, alquilo C1-6, alcanol C1-6, O(alquiloC1-6), arilo C6-10, O- ariloC6-10, NH2, NHalquiloC1-6, N(alquiloC1-6)2 o cicloalquilo C3-7; y Z2 significa OH, NH2, NHalquiloC1-6, N(alquiloC1-6)2, OalquiloC1-6, cicloalquiloC3-7mono- o bicíclico, heterocicloC3-10mono- o bicíclico, heteroarilo C5-10 mono- o bicíclico o arilo C6-10; o R3 es un radical seleccionado del grupo compuesto por arilo C6-10 y un heteroarilo C5-10, que puede estar eventualmente sustituido con alquilo C1-6, que eventualmente puede estar sustituido con un radical seleccionado del grupo compuesto por COOR3.3, NR3.3R3.4, NHCO3.3, NHCOOR3.3, fenilo, en donde el fenilo puede estar eventualmente sustituido con un radical seleccionado del grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, CN, haloalquilo C1-6, CONH2, CONH- alquiloC1-6, CON(alquiloC1-6)2, COOH, COO-alquiloC1-6, COH, CO-alquiloC1-6, OH, O-alquiloC1-6, O-haloalquiloC1-6, halogeno, SH, S-alquiloC1-6, S-haloalquiloC1-6, SO2-alquiloC1-6, SO2-haloalquiloC1-6, SO2-NH2, SO2-NH-alquiloC1-6, SO2-N(alquiloC1-6)2, NO2, NH2, NH-alquiloC1-6 y N(alquiloC1-6)2, un heterociclo C3-10 y un heteroarilo C510, en donde el heterociclo C3-10 y el heteroarilo C5-10 pueden estar eventualmente sustituidos con un grupo oxo o un grupo metilo; en donde: R3.3 es H o alquilo C1- 6; R3.4 es H, alquilo C1-6 o aralquilo C7-11, heteroarilC5-10-alquilenoC1-6; o R3 es un radical seleccionado de un grupo compuesto por arilo C6-10 y un heteroarilo C5-10, que puede estar eventualmente sustituido con NR3.1R3.2; en donde: R3.1 es H, alquilo C1-6, cicloalquilo C3-6, haloalquilo C1-6, COR3.1.1, COOR3.1.1, CONR3.1.1R3.1.2 o SO2-R3.1.1; y R3.1.1 es H, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-6 o arilo C6-10; y R3.1.2 es H, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-6 o arilo C6-10; y R3.2 es H o un radical seleccionado del grupo compuesto por alquilo C1-6, cicloalquilo C3-6 y haloalquilo C1-6, que puede estar eventualmente sustituido con uno o varios radicales seleccionados del grupo compuesto por NH2, NHalquiloC1- 6, N(alquiloC1-6)2, oxo y un heterociclo C3-10 no aromático, que puede estar sustituido con uno o dos heteroátomos seleccionados del grupo compuesto por nitrogeno, oxígeno y azufre, en donde el heterociclo C3-10 no aromático puede estar eventualmente sustituido con alquilo C1-4; o R3 es un radical seleccionado de un grupo compuesto por arilo C6-10 y un heteroarilo C5-10, que está sustituido con un heterociclo C3-10, que puede estar eventualmente sustituido con uno o varios radicales seleccionados del grupo compuesto por arilo C6-10, alquilo C1-6, cicloalquilo C3-6, CN, haloalquilo C1-6, CONH2, CONH-alquiloC1-6, CON(alquiloC1-6)2, COOH, COO-alquiloC1-6, COH, CO-alquiloC1-6, oxo, OH, O-alquiloC1-6, halogeno, SH, S- alquiloC1-6, NH2, NH-alquiloC1-6 y N(alquiloC1-6)2; o R3 es bencimidazolilo, que puede estar eventualmente sustituido con un radical seleccionado del grupo compuesto por alquilo C1-6, haloalquilo C1-6 y cicloalquilo C3-6; y R4 es alquilo C1-6, cicloalquilo C3-8, haloalquilo C1-6, OR4.1, NR4.1R4.2, CN, o halogeno; en donde significan: R4.1 es H, alquilo C1-6, cicloalquilo C3-8 o haloalquilo C1-6; R4.2 es H, alquilo C1-6, cicloalquilo C3-8 o haloalquilo C1-6; y R5 es alquilo C1-6, cicloalquilo C3-8, haloalquilo C1-6, COR5.1, CONHR5.1, CON(R5.1)2, SO2-alquiloC1-6, SO2-haloalquiloC1-6, SO2-arilo o un radical seleccionado del grupo compuesto por R5.2, SO2-alquilC1-6-R5.2, y alquilC1-6-R5.2, que puede estar eventualmente sustituido con uno o varios radicales seleccionados del grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, CN, haloalquilo C1-6, CONH2, CONH-alquiloC1-6, CON(alquiloC1-6)2, COOH, COO-alquiloC1-6, COH, CO-alquiloC1-6, O-cicloalquiloC3- 6, O-haloalquiloC1-6, O-alquiloC1-6, halogeno, SO2-alquiloC1-6, SO2-NH2, SO2-NH-alquiloC1-6, SO2-N(alquiloC1-6)2, NO2, NH2, NH-alquiloC1-6 y N(alquiloC1-6)2; en donde significan: R5.1 es alquilo C1-6, heteroarilC5-10-alquilenoC1-6 o arilC6-10- alquilenoC1-6; y R5.2 es arilo C6-10 o un heteroarilo C5-10; y R6 es H, alquilo C1-6 o haloalquilo C1-6; R7 es H, alquilo C1-6 o haloalquilo C1-6; o R6 y R7 forman juntos un carbociclo de 3-6 miembros; eventualmente en forma de sus racematos, enantiomeros, diastereoisomeros y eventualmente en forma de sus sales por adicion de ácidos, solvatos o hidratos farmacologicamente tolerables, así como sus formas deuteradas.
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