AR029090A1 - Derivados pirazol triciclicos - Google Patents

Derivados pirazol triciclicos

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Publication number
AR029090A1
AR029090A1 ARP010102343A ARP010102343A AR029090A1 AR 029090 A1 AR029090 A1 AR 029090A1 AR P010102343 A ARP010102343 A AR P010102343A AR P010102343 A ARP010102343 A AR P010102343A AR 029090 A1 AR029090 A1 AR 029090A1
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Argentina
Prior art keywords
optionally substituted
group
formula
phenyl
cycloalkyl
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ARP010102343A
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English (en)
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Abbott Gmbh & Co Kg
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Abstract

Un compuesto derivado de pirazol tricíclico que está representado por la formula 1 las mezclas racémicas, las mezclas racémico-diastereoméricas, tautomeros e isomeros opticos de compuestos y las sales farmacéuticamente aceptables y las prodrogas de los mismos, en donde: m es un entero de 1 a 10; X representa a) un grupo opcionalmente sustituido de la formula -(CH2)n - en donde n es 1, 2, o 3, b) carbonilo, c) oxígeno, d) un grupo de la formula -C=NOR10, en donde R10 es un grupo alquilo C1-4, e) un grupo de la formula NR11 en donde R11 es -H, un grupo alquilo C1-4 opcionalmente sustituido, o un fenilo opcionalmente sustituido, o f) un grupo de formula S(O)p en donde p es de valor 0, 1 o 2; B representa un alquilo, un cicloalquilo, un arilo, un piridilo, un tienilo, un furilo o un pirrolilo; R1 es -H; un halo; hidroxilo, nitro, ciano, hidroxiamidino; aminometilo; formamidometilo; un alqueniloxilo opcionalmente sustituido; un alquenilo C2-4 opcionalmente sustituido; un alquinilo C2-4 opcionalmente sustituido; o un grupo representado por la formula -Y-W; con la condicion que cuando R1 es -H, un alquilo C1-6 sin sustituir, un alcoxilo C1-6 sin sustituir, un halogeno, o trifluorometilo, el anillo A se sustituye con por lo menos un sustituyente que no es un halo, un alquilo C1-6 opcionalmente sustituido o un alcoxilo C1-6 opcionalmente sustituido; Y no está o es un alquilo C1-6, alcoxilo C1-6, -O-, -S- o -C(O) -; W es -H, hidroxilo, fenilo opcionalmente sustituido, alcoxilo C1-6, o -NR2R3; con la condicion que cuando el B es fenilo y R1 es Y-W y W es -NR2R3, R2 y R3 son cada uno, independientemente, a) -H; b) un grupo alquilo C1-6 sustituido, con la condicion que el sustituyente no es -NR6R7; c) un cicloalquilo opcionalmente sustituido; d) un heterocicloalquilo opcionalmente sustituido; e) un cicloalquilo opcionalmente sustituido; f) un heterocicloalquilalquilo opcionalmente sustituido; g) un heteroarilo sustituido o un heteroaralquilo sustituido, con la condicion que el heteroarilo o heteroaralquilo se sustituye con -NR9(CH2)1-6OR4, -NR9(CH2)1-6 CO2R4, -NR9(CH2)1-6NR4R5, o un heterocicloalquilo opcionalmente sustituido; o cuando B es fenilo y R1 es -Y-W y W es -NR2R3, R2 y R3, junto con el átomo de nitrogeno a cual éstos están unidos, puede representar un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; cuando el B no es fenilo, R2 y R3 son cada uno, independientemente, -H, un grupo alquilo C1-6 opcionalmente sustituido, -NH(CH2)1-6NR4R5, un cicloalquilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un heterocicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, o un heteroaralquilo opcionalmente sustituido; o cuando el B no es fenilo, R2 y R3 junto con el átomo de nitrogeno al cual los mismos están unidos representa un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; R4, R5 y R9 son en cada caso, independientemente, -H o un alquilo C1-6; y el anillo A se sustituye opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste de a) un halo; b) un grupo alquilo C1-6 opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste de hidroxilo, halo, y NR6R7; c) un grupo alcoxilo C1-6 opcionalmente sustituido con uno o más sustituyentes seleccionado del grupo que consiste de hidroxilo, halo, -NR6R7, un fenilo opcionalmente sustituido, y -NR17C(O)R19, con la condicion que los sustituyentes no están unidos al carbono a que se une el oxígeno del grupo alcoxilo; d) un fenoxilo opcionalmente sustituido; e) hidroxilo; f) un grupo de la formula -C (O) R12 en donde R12 es hidroxilo, un alcoxilo C1-6 o -NR13R14; g) un grupo de la formula NR17R18; h) un grupo de la formula -NR17C(O)R19; i) nitro; j) aralquilo opcionalmente sustituido; k) ciano; y l) un grupo alquenilo C2-4 o un grupo alquinilo C2-4 cada uno de los cuales es opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste de un grupo alquilo C1-6, un grupo alcoxilo C1-6 y un halo; R6 y R7 son cada uno, independientemente, -H, un grupo alquilo C1-6 opcionalmente sustituido, un cicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituidos, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, un heteroaralquilo opcionalmente sustituido, o un heterocicloalquilalquilo opcionalmente sustituido; o R6 y R7 junto con el átomo de nitrogeno al cual éstos están unidos representan un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido, R13 y R14 son cada uno, independientemente, -H, un grupo alquilo C1-6 opcionalmente sustituido, un cicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituidos, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, un heteroaralquilo opcionalmente sustituido, o un heterocicloalquilalquilo opcionalmente sustituido; o R13 y R14 junto con el átomo de nitrogeno al cual éstos están unidos representan un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; R17 y R18 son cada uno, independientemente, seleccionado del grupo que consiste de -H, un grupo alquilo C1-2, un grupo cicloalquilo C3-12, y fenilo; y R19 es -H, un grupo alquilo C1-12 opcionalmente sustituido, un grupo cicloalquilo C3-12 opcionalmente sustituido, un fenilo opcionalmente sustituido o un aralquilo opcionalmente sustituido. Con la condicion que, cuando B es arilo, piridilo, tienilo, furilo o pirrolilo, entonces el anillo A es sustituido con por lo menos un sustituyente seleccionado del grupo que consiste del grupo alquilo C1-6 que es sustituido con -NR6'R7'; un alcoxilo C1-6 que es sustituido con un grupo de la formula -NR17C(O)R19 o fenilo opcionalmente sustituido; y un grupo de la formula C(O)NR13'R14'. R6' y R7' son cada uno, independientemente, -H, un cicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, un heteroalquilo opcionalmente sustituido, o un heterocicloalquilalquilo opcionalmente sustituido, con la condicion que por lo menos uno de R6' y R7' no sea -H; y R13' y R14' son cada uno, independientemente, -H, un cicloalquilo opcionalmente sustituido, un naftilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, un heteroaralquilo opcionalmente sustituido, o un heterocicloalquilalquilo opcionalmente sustituido, con la condicion que por lo menos uno de R13' p R14' no sea -H. Estos compuestos son de utilidad para inhibir la actividad de quinasa de quinasas tirosinas y quinasas serina/treonina.
ARP010102343A 2000-05-17 2001-05-17 Derivados pirazol triciclicos AR029090A1 (es)

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US09/573,366 US6462036B1 (en) 1998-11-06 2000-05-17 Tricyclic pyrazole derivatives

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EP1289525A2 (en) 2003-03-12
AU2001263272A1 (en) 2001-11-26
UY26713A1 (es) 2001-12-28
WO2001087846A2 (en) 2001-11-22
WO2001087846A3 (en) 2002-03-21
PE20011263A1 (es) 2001-12-11
CO5290256A1 (es) 2003-06-27
US6462036B1 (en) 2002-10-08
CA2409225A1 (en) 2001-11-22
JP2003533514A (ja) 2003-11-11

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