AR061161A1 - Inhibidores triciclicos fusionados de sulfonamida de gama-secretasa - Google Patents

Inhibidores triciclicos fusionados de sulfonamida de gama-secretasa

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AR061161A1
AR061161A1 ARP070102379A ARP070102379A AR061161A1 AR 061161 A1 AR061161 A1 AR 061161A1 AR P070102379 A ARP070102379 A AR P070102379A AR P070102379 A ARP070102379 A AR P070102379A AR 061161 A1 AR061161 A1 AR 061161A1
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Argentina
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alkyl
aryl
groups
substituted
heteroaryl
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ARP070102379A
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Elan Pharm Inc
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Abstract

Los compuestos de la formula 1 son utiles en el tratamiento o prevencion de trastornos cognitivos, como mal de Alzheimer. La presente abarca también composiciones farmacéuticas que comprenden los compuestos o sus sales. Reivindicacion 1: Un compuesto de la formula (1) estereoisomeros, tautomeros, mezclas de estereoisomeros y/o tautomeros o sales farmacéuticamente aceptables de los mismos, donde el anillo C es cicloalquilo, arilo, heterocicloalquilo, o heteroarilo, cada uno de los cuales se sustituye opcionalmente con 1, 2, 3, o 4 grupos que son independientemente halogeno, alquilo C1-6, alcoxi C1-6, ariloxi, aril-alcoxi C1-6, haloalquilo C1-6, haloalcoxi C1-6, hidroxilo, hidroxi- alquilo C1-6, -NR'Rö, -alquil C1-6-NR'Rö, NR'C(O)OR', -COR', -C(O)OR', -C(O)NR' Rö, -OC(O)NR'Rö, NR'C(O)NR'Rö; -alquil C1-6-C(O)OR', -alquilo C1-6-C(O)NR'Rö, -NR'C(O)Rö, NO2, CN, oxo, aril-alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, -NR'SO2Rö, - SO2-NR'Rö, -S(O)zarilo o -S(O)zalquilo C1-6, donde las partes alquilo, alquenilo y alquinilo de los anteriores están sustituidas o insustituidas con 1, 2 o 3 grupos que son independientemente halogeno, hidroxilo, -NR'Rö o alcoxi C1-6, y donde las partes arilo o heteroarilo de los anteriores se sustituyen opcionalmente con 1, 2, 3, o 4 grupos que son independientemente alquilo C1-6, alcoxi C1-6, halogeno, haloalquilo C1-6, haloalcoxi C1-6, hidroxilo, hidroxi- alquilo C1-6, o -NR'Rö; o donde dos sustituyentes adyacentes forman -O-(CH2)1-3-O-; el anillo A es arilo, cicloalquilo, heteroarilo o heterocicloalquilo, donde cada anillo se sustituye opcionalmente en una posicion sustituible con halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2- 6, alcoxi C1-6, haloalquilo C1-6, haloalcoxi C1-6, hidroxilo, hidroxi-alquilo C1-6, CN, NO2, ariloxi, aril-alcoxi C1-6, -SO2-alquilo C1-6, -NR'Rö, alcanoilo C1-6, -C(O)OR', -alquil C1-6-C(O)OR', heteroarilo, arilo, aril-alquilo C1-6, -SO2-NR'Rö, - C(O)NR'Rö, -OC(O)NR'Rö, -NR'C(O)Rö, -NR'C(O)NR'Rö o -NR'C(O)OR'; el anillo B es un anillo heteroarilo o heterocicloalquilo, cada uno de los cuales se sustituye opcionalmente en una posicion sustituible con un grupo que es independientemente alquilo C1-6, alcoxi C1-6, -NR'Rö, -SO2-NR'Rö, -C(O)NR'Rö, -NR'SO2Rö, -NR'SO2NR'Rö, -NR'SO2-alquilo C1-6, -NR'SO2-fenilo, -NR'C(O)Rö, -NR'C(O)NR'Rö, -NR'C(O)OR', -alquil C1-6-NR'Rö, alquil C1-6-C(O)OR', -alquil C1-6-C(O)NR'Rö, NO2, CN, C(O)OR' , hidroxilo, hidroxi-alquilo C1-6, -S(O)zarilo, -S(O)zalquilo C1-6, halogeno, haloalquilo C1-6, haloalcoxi C1-6, fenilo, alcanoilo C1-6, aril-alcanoilo C1-6, aril-alquilo C1-6, arilcarbonilo, heteroarilcarbonilo, o heteroaril-alcanoilo C1-6, donde los grupos arilo o heteroarilo se sustituyen opcionalmente con de 1 a 5 grupos que son independientemente halogeno, hidroxilo, alquilo C1-6, alcoxi C1-6, alcanoilo C1-6, haloalquilo C1-6, haloalcoxi C1-6, CN o NO2 y donde cada z es independientemente 0, 1, o 2; R1 es hidrogeno o alquilo C1-6; R2 es hidrogeno, alquilo C1-6, haloalquilo C1-4, hidroxilo, hidroxi-alquilo C1-4, -NO2, -CN, alquenilo C2-6, alquinilo C2-6, alcanoilo C1-6, -C(O)OR', -NR'Rö, -X(CO)Y, -(C(R30)2)1-4X(CO)Y, cicloalquilo C3-6 insustituido, cicloalquilo C3-6 sustituido con de uno a cuatro grupos R50, arilo insustituido, arilo sustituido con de uno a cuatro grupos R50, heteroarilo insustituido; o heteroarilo sustituido con de uno a cuatro grupos R50, heterocicloalquilo insustituido; o heterocicloalquilo sustituido con de uno a cuatro grupos R50 donde cada R30 es independientemente hidrogeno o alquilo C1-6; cada R50 se selecciona independientemente de: halogeno, alquilo C1-6, haloalquilo C1-6, -OH, -O-alquilo C1-6, -OCF3, -CN, -NR60R70, -C(O)O-alquilo C1-6, -CONR60R70, -alquil C1-6-NR60R70, -NR60COalquilo, -NR60COarilo, -NR60COheteroarilo, NR60CONR60R70, X es: -O-, -NH-, o -N(alquilo)-; Y se selecciona de -O-alquilo C1-6 , -O-fenilo, -NR60R70, o - N(R30)(CH2)2- 6NR60R70; R60 y R70 se seleccionan independientemente de: hidrogeno, alquilo C1-6, cicloalquilo, arilalquilo; heteroarilalquilo; formulas (2), (o) R60 y R70 tomados conjuntamente con al átomo de nitrogeno al que están unidos forman un grupo heterocicloalquilo seleccionado de formulas (3), donde cada R80 es independientemente alquilo C1-6 insustituido o alquilo C1-6 sustituido con hidroxilo o halogeno; cada R90 es independientemente H; alquilo C1-6 insustituido; alquilo C1-6 sustituido con hidroxilo o halogeno; cicloalquilo insustituido; cicloalquilo sustituido con de uno a cuatro grupos R50; aril-alquilo C1-6; heteroarilalquilo; -C(O)O-alquilo C1-6, -C(O)O-arilo; -SO2-alquilo C1-6, -SO2-arilo; arilo insustituido; arilo sustituido con de uno a cuatro grupos R50; heteroarilo; o heteroarilo sustituido con de uno a cuatro grupos R50; cada R100 es independientemente hidrogeno o alquilo C1-6; cada r es de 0 a 4; cada s es de 0 a 3; o R1 y R2 combinados son oxo o =N-OR donde R es hidrogeno, alquilo C1-6, arilo o arilalquilo; o R1 y R2 junto con el carbono al que están unidos forman un grupo cicloalquilo C3-6 donde uno de los carbonos puede remplazarse con un heteroátomo seleccionado de N, O o S y donde dicho anillo de cicloalquilo C3-6 puede sustituirse opcionalmente con alquilo C1-6; y R' y Rö son independientemente hidrogeno, alquilo C1-6, o fenilo, donde el fenilo se sustituye opcionalmente con de 1 a 5 grupos que son independientemente halogeno, hidroxilo, alquilo C1-6, alcoxi C1-6, alcanoilo C1-6, haloalquilo C1-4, haloalcoxi C1-4, CN o NO2, o R' y Rö tomados conjuntamente con al átomo de nitrogeno al que están unidos forman un grupo heterocicloalquilo de 3 a 7 que puede tener un heteroátomo adicional seleccionado de N, O o S y que puede sustituirse opcionalmente con de 1 a 3 grupos R80 o R90; siempre que 5-tosil-4,5-dihidro-2H-pirazol[4, 3-c]quinolina, 2-fenil-5-tosil-4,5-dihidro-2H-pirazol[4, 3-c]quinolina, 7-metoxi-2-fenil-5-tosil- 4,5-dihidro-2H-pirazol[4,3-c]quinolina, 8-metoxi-5-tosil-4,5-dihidro-2H-pirazol[4,3-c]quinolina, 8-metoxi-2-fenil-5-tosil-4,5-dihidro-2H-pirazol[4,3-c]quinolina, 3-(metiltio)-5-tosil-4,5-dihidro-2H-pirazol[4,3-c]quinolina, 7-metoxi--5-tosil-4,5- dihidro-2H-pirazol[4,3-c]quinolina, 5-tosil-4,5-dihidro-2H-pirazol[4,3-c]quinolina, 1-(4-sulfamoilfenil)-5-tosil-4,5-dihidro-1H-pirazol[4,3-c]quinolin-3-carboxilato de etilo, 1-(4-sulfamoilfenil)-5-tosil-4,5-dihidro-1H-pirazol[4,3-c]quinolin-3- carboxamida y 1metil-5-tosil-4,5-dihidro-1H-pirazol[4,3-c]quinolin-3-carboxilato de etilo, no se encuentren abarcados por la formula 1.
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