AR047160A1 - Compuestos moduladores de cb1 - Google Patents

Compuestos moduladores de cb1

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Publication number
AR047160A1
AR047160A1 ARP040104819A ARP040104819A AR047160A1 AR 047160 A1 AR047160 A1 AR 047160A1 AR P040104819 A ARP040104819 A AR P040104819A AR P040104819 A ARP040104819 A AR P040104819A AR 047160 A1 AR047160 A1 AR 047160A1
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AR
Argentina
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alkyl
hydrogen
group
compounds
formulas
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ARP040104819A
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Lilly Co Eli
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Abstract

Se describen compuestos como moduladores del receptor de cannabinoides-1 (CB1), estos compuestos son utiles en el tratamiento, prevencion y supresion de enfermedades mediadas por el receptor CB1. Como tales, los compuestos del presente son utiles para el tratamiento, prevencion y supresion de psicosis, pérdidas de memoria, trastornos cognitivos, migrana, neuropatía, trastornos neuroinflamatorios (por ejemplo, esclerosis multiple, síndrome de Guillain-Barre y las secuelas inflamatorias de la encefalitis viral), accidentes cerebrovasculares, y traumatismo craneal, trastornos de ansiedad, estrés, epilepsias, enfermedad de Parkinson, y esquizofrenia. Los compuestos también son utiles para el tratamiento de trastornos de abuso de sustancias, particularmente de opiáceos, alcohol, y nicotina. Los compuestos también son utiles para el tratamiento de la obesidad o trastornos alimenticios asociados con una ingesta excesiva de alimentos y las complicaciones asociadas que conllevan. Reivindicacion 1: Un compuesto de formula (1), en la que el resto de formula (2) es un anillo 6,5-bicíclico seleccionado de entre el grupo de formulas (3); R1 se selecciona entre el grupo compuesto por: a) hidrogeno; b) alquilcarbonilo opcionalmente sustituido con heterociclilo; c) heterociclilcarbonilo opcionalmente sustituido con alquilo o acetilo; d) alquilo o haloalquilo; e) cicloalquilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre el grupo compuesto por alquilo, halo, oxo, hidroxi, alcoxi, amino, alquilamino y dialquilamino; f) heterociclilo seleccionado entre los compuestos del grupo de formulas (4); g) arilo opcionalmente sustituido con halo, alquilo, alcoxi ciano, amino, alquilamino o dialquilamino; y h) heteroarilo seleccionado entre los compuestos del grupo de formulas (5); R2 es hidrogeno, alquilo, heterociclilo o, junto con R1 y el carbono a los que están unidos, forma un sustituyente de anillo saturado seleccionado entre el grupo compuesto por: a) cicloalquilo; y b) heterociclilo seleccionado entre el grupo compuesto por tetrahidrofuranilo, tetrahidropiranilo y piperidinilo opcionalmente N-sustituido con alquilo, acetilo o arilo, X es -NR13R3 o un compuesto de formula (6); R3 se selecciona entre el grupo compuesto por: a) hidrogeno; b) alquilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre el grupo compuesto por hidroxi, alcoxi, halogeno, amino, alquilamino y dialquilamino; c) cicloalquilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre el grupo compuesto por hidroxi, alcoxi, halo, amino, alquilamino y dialquilamino; d) heterociclilo seleccionado entre los compuestos del grupo de formulas (7); e) cicloalquilalquilo seleccionado entre los compuestos del grupo de formulas (8); f) heterociclilalquilo seleccionado entre los compuestos del grupo de formulas (9); g) arilalquilo seleccionado entre los compuestos del grupo de formulas (10); h) heteroarilalquilo seleccionado entre los compuestos del grupo de formulas (11); y el compuesto de formula (6) es un anillo heterocíclico seleccionado entre los compuestos del grupo de formulas (12); R4 es hidrogeno, fenilo, halofenilo, acilo o alcoxicarbonilo; R5 es hidrogeno, hidroxi o alcoxi; cada uno de R6 y R7 se selecciona independientemente entre hidrogeno, halo, ciano, alquilo, alcoxi, haloalquilo, haloalcoxi, amino, alquilamino, dialquilamino, alcoxicarbonilo, dialquilaminocarbonilo, arilo y ariloxi; R8 es hidrogeno, hidroxialquilo, acilo, oxo, arilo, piridinilo, alquil-SO2-O-, Rb-NH-CH2-, arilalquilo o Rc2N-CO-O-; R9 es hidrogeno, hidroxi, hidroxialquilo, acilo, halo, dihalo, oxo, arilo, haloaril-CH2-, piridinilo, alquil-SO2-O-, Ra-NH-, Rb-NH-CH2, arilalquilo, el compuesto de formula (13) o Rc2N-CO-O-; R10 es hidrogeno, alquilo, alcoxicarbonilo, arilo o haloarilo; R11 es hidrogeno, alquilo o arilo; R12 es hidrogeno o arilo; R13 es hidrogeno o alquilo; R14 es hidrogeno, alquilo, arilo o acilo; Ra es hidrogeno, alcoxicarbonilo o halofenilo; Rb es hidrogeno, alcoxi, fenilo, halofenilo, halofenilalquilo, halopiridinilo, pirimidinilo, alcoxicarbonilo, dialquilaminocarbonilo o dialquilaminotiocarbonilo; y Rc es hidrogeno o alquilo; y todas las sales, solvatos, isomeros opticos y geométricos y formas cristalinas de los mismos con la condicion de que el compuesto de formula (1) es diferente de [4- (2,3-dihidro-indol-1-sulfonil)-fenil]-(4-fenil-piperazin-1-il)-metanona, [4-(2,3-dihidro-indol-1-sulfonil)-fenil]-morfolin-4-il-metanona y [4-(2,3-dihidro-indol-1-sulfonil)-fenil]-piperidin-1-il-metanona.
ARP040104819A 2003-12-23 2004-12-21 Compuestos moduladores de cb1 AR047160A1 (es)

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US (2) US7276516B2 (es)
EP (1) EP1699761B1 (es)
JP (1) JP2007519631A (es)
AR (1) AR047160A1 (es)
AT (1) ATE502009T1 (es)
AU (1) AU2004312311A1 (es)
BR (1) BRPI0418079A (es)
CA (1) CA2549396A1 (es)
DE (1) DE602004031875D1 (es)
ES (1) ES2360112T3 (es)
IL (1) IL176069A0 (es)
NO (1) NO20063381L (es)
PE (1) PE20050598A1 (es)
SV (1) SV2005001984A (es)
TW (1) TW200522944A (es)
WO (1) WO2005066126A1 (es)
ZA (1) ZA200605159B (es)

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GB0516379D0 (en) * 2005-08-09 2005-09-14 Glaxo Group Ltd Compounds
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FR2893615B1 (fr) * 2005-11-18 2008-03-07 Sanofi Aventis Sa Derives de 3-acylindole, leur preparation et leur application en therapeutique
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US7595339B2 (en) 2009-09-29
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