AR060593A1 - 5-amido-2-carboxiamida-indoles - Google Patents

5-amido-2-carboxiamida-indoles

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Publication number
AR060593A1
AR060593A1 ARP070101539A ARP070101539A AR060593A1 AR 060593 A1 AR060593 A1 AR 060593A1 AR P070101539 A ARP070101539 A AR P070101539A AR P070101539 A ARP070101539 A AR P070101539A AR 060593 A1 AR060593 A1 AR 060593A1
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AR
Argentina
Prior art keywords
unsubstituted
halogen
substituted
alkyl
hydroxyalkyl
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ARP070101539A
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Hoffmann La Roche
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Publication of AR060593A1 publication Critical patent/AR060593A1/es

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    • A61K31/404—Indoles, e.g. pindolol
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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Abstract

Reivindicacion 1: Compuestos de la formula general (1) en la que R1 se selecciona entre el grupo formado por alquilo inferior, alquenilo inferior, alquinilo inferior, cicloalquilo, cicloalquilalquilo inferior, hidroxialquilo inferior, alcoxialquilo inferior, alquilsulfanilalquilo inferior, dialquilaminoalquilo inferior, dialquilcarbamoilalquilo inferior, fenilo sin sustituir o sustituido con uno a tres grupos seleccionados independientemente entre alquilo inferior, halogeno, halogenoalcoxi inferior e hidroxialquilo inferior, fenilalquilo inferior, en el que el anillo fenilo puede estar sin sustituir o sustituido con uno a tres grupos seleccionados independientemente entre alquilo inferior, halogeno, alcoxi inferior e hidroxialquilo inferior, heteroarilalquilo inferior, en el que el anillo heteroarilo puede estar sin sustituir o sustituido con uno o dos grupos seleccionados con independencia entre alquilo inferior, halogeno, alcoxi inferior e hidroxialquilo inferior, heterociclilalquilo inferior, en el que el anillo heterociclilo puede estar sin sustituir o sustituido con uno o dos grupos seleccionados entre alquilo inferior y halogeno, y 7-oxa-biciclo[2.2.1]heptilo; R2 se selecciona entre el grupo formado por hidrogeno, alquilo inferior, alquenilo inferior, alquinilo inferior, cicloalquilo, cicloalquilalquilo inferior, hidroxialquilo inferior, alcoxialquilo inferior, alquilsulfanilalquilo inferior, dialquilaminoalquilo inferior, dialquilcarbamoilalquilo inferior, fenilo sin sustituir o sustituido con uno a tres grupos seleccionados independientemente entre alquilo inferior, halogeno, halogenoalcoxi inferior e hidroxialquilo inferior, fenilalquilo inferior, en el que el anillo fenilo puede estar sin sustituir o sustituido con uno a tres grupos seleccionados independientemente entre alquilo inferior, halogeno, alcoxi inferior e hidroxialquilo inferior, heteroarilalquilo inferior, en el que el anillo heteroarilo puede ser estar sin sustituir o sustituido con uno o dos grupos seleccionados con independencia entre alquilo inferior, halogeno, alcoxi inferior e hidroxialquilo inferior y heterociclilalquilo inferior, en el que el anillo heterociclilo puede estar sin sustituir o sustituido con uno o dos grupos alquilo inferior; o R1 y R2 junto con el átomo de nitrogeno al que están unidos forman un anillo heterocíclico saturado o parcialmente insaturado, de 4, 5, 6 o 7 miembros, que contiene opcionalmente otro heteroátomo seleccionado entre oxígeno y azufre, un grupo sulfinilo o un grupo sulfonilo, dicho anillo heterocíclico está sin sustituir o sustituído con uno, dos o tres grupos seleccionados con independiencia entre alquilo inferior, halogeno, halogenoalquilo inferior, ciano, hidroxi, hidroxialquilo inferior, alcoxi inferior, oxo, fenilo, bencilo, piridilo y carbamoílo, o está condensado con un anillo fenilo, dicho anillo fenilo está sin sustituir o sustituido con uno, dos o tres grupos seleccionados con independencia entre alquilo inferior, alcoxi inferior y halogeno o R1 y R2 junto con el átomo de nitrogeno al que están unidos forman un grupos seleccionado entre 1-oxa-8-aza-espiro[4.5]decilo, 1,4-dioxa-8-aza-espiro[4.5]decilo y [1,4]oxazepan-7- ona; R3 se selecciona entre el grupo formado por hidrogeno, alquilo inferior, cicloalquilo, hidroxialquilo inferior, alcoxialquilo inferior, halogenoalquilo inferior, cicloalquilalquilo inferior, alcanoílo inferior, cianoalquilo inferior, alquilsulfonilo inferior, fenilsulfonilo, en el que el anillo fenilo puede estar sin sustituir o sustituido con uno a tres grupos seleccionados independientemente entre alquilo inferior, halogeno, alcoxi inferior, halogenoalcoxi inferior e hidroxialquilo inferior, fenilo sin sustituir o sustituido con uno a tres grupos seleccionados independientemente entre alquilo inferior, halogeno, ciano, morfolino, alcoxi inferior, alcoxicarbonilo inferior, halogenoalquilo inferior, halogenoalcoxi inferior, hidroxialquilo inferior, alquilsulfonilo inferior y alquilsulfonilamino inferior, benzodioxolilo, fenilalquilo inferior, en el que el anillo fenilo puede estar sin sustituir o sustituido con uno a tres grupos seleccionados independientemente entre alquilo inferior, halogeno, ciano, morfolinilo, alcoxi inferior, alcoxicarbonilo inferior, halogenoalquilo inferior, halogenoalcoxi inferior, hidroxialquilo inferior, alquilsulfonilo inferior y alquilsulfonilamino inferior y heteroarilo sin sustituir o sustituido con uno o dos grupos seleccionados con independencia entre alquilo inferior, alcoxi inferior, ciano, morfolinilo y halogeno; R4, R12 y R5 son hidrogeno, o uno de R4, R12 y R5 es halogeno y los demás son hidrogeno; G es un grupo seleccionado entre (2) y (3) en los que R6 se selecciona entre el grupo formado por alquilo inferior, cicloalquilo, cicloalquilalquilo inferior y un anillo heterocíclico que contiene oxígeno; R7 es hidrogeno; o R6 y R7 juntos son -(CH2)p-, en el que p es 3 o 4 y están unidos entre sí para formar un anillo junto con el átomo de carbono o de nitrogeno al que están unidos; n es el numero 1 o 2; m es el numero 1 o 2; R8 es hidrogeno o heterociclilalquilo inferior; R9 es hidrogeno o -NR10R11; R10 y R11 con independencia entre sí son alquilo inferior o junto con el átomo de nitrogeno al que están unidos forman un anillo heterocíclico saturado de 5 o 6 miembros, que contiene opcionalmente otro heteroátomo seleccionado entre nitrogeno, oxígeno y azufre; R13 es hidrogeno o -NR10R11; y sus sales farmacéuticamente aceptables. Estos compuestos son utiles para el tratamiento y/o prevencion de enfermedades asociadas con la modulacion de los receptores de la H3. Compuestos 5-amido-2-carboxamida-indoles, un método de preparacion y composicion farmacéutica en base al compuesto.
ARP070101539A 2006-04-12 2007-04-11 5-amido-2-carboxiamida-indoles AR060593A1 (es)

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US (2) US7601711B2 (es)
EP (1) EP2010487A1 (es)
JP (1) JP2009533375A (es)
KR (1) KR20090024115A (es)
CN (1) CN101421235A (es)
AR (1) AR060593A1 (es)
AU (1) AU2007236052A1 (es)
BR (1) BRPI0710588A2 (es)
CA (1) CA2647440A1 (es)
CL (1) CL2007001022A1 (es)
IL (1) IL194391A0 (es)
MX (1) MX2008013196A (es)
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WO (1) WO2007115938A1 (es)

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US7648979B2 (en) 2007-02-07 2010-01-19 Hoffmann-La Roche Inc. 5-amido-(1H-indol-2-yl)-piperazin-1-yl-methanone derivatives
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
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