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AR041133A1 - Pirazolopirimidinas como inhibidores de la quinasa dependientes de la ciclina - Google Patents

Pirazolopirimidinas como inhibidores de la quinasa dependientes de la ciclina

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Publication number
AR041133A1
AR041133A1 ARP030103188A ARP030103188A AR041133A1 AR 041133 A1 AR041133 A1 AR 041133A1 AR P030103188 A ARP030103188 A AR P030103188A AR P030103188 A ARP030103188 A AR P030103188A AR 041133 A1 AR041133 A1 AR 041133A1
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AR
Argentina
Prior art keywords
aryl
alkyl
cycloalkyl
nr5r10
group
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Application number
ARP030103188A
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English (en)
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Pharmacopeia Drug Discovery
Schering Corp
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Application filed by Pharmacopeia Drug Discovery, Schering Corp filed Critical Pharmacopeia Drug Discovery
Publication of AR041133A1 publication Critical patent/AR041133A1/es

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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

En sus muchas realizaciones, la presenta provee una clase novedosa de compuestos de pirazolo[1,5-a]pirimidina como inhibidores de quinasas dependientes de ciclina, métodos de preparación de dichos compuestos, composiciones farmacéuticas que contienen uno o más de dichos compuestos, métodos de preparación de formulaciones farmacéuticas que comprenden uno o más de dichos compuestos, y métodos de tratamiento, prevención, inhibición, o alivio de una o más enfermedades asociadas con las CDKs a través del uso de dichos compuestos o composiciones farmacéuticas. Reivindicación 1: Un compuesto representado por la fórmula estructural (1), o una sal o un solvato aceptables para uso farmacéutico de dicho compuesto, en el cual: R es una arilo no sustituido o un arilo sustituido con uno o más restos cuyos restos pueden ser iguales o diferentes, cada resto se selecciona en forma independiente del grupo formado por halógeno, CN, -OR5, SR5, -CH2OR5, -C(O)R5, -SO3H, -S(O2)R6, -S(O2)NR5R6, -NR5R6, -C(O)NR5R6, -CF3, -OCF3 y heterociclilo; R2 se selecciona del grupo formado por R9, alquilo, alquinilo, alquinilalquilo, cicloalquilo, -CF3, -C(O2)R6, arilo, arilalquilo, heteroarilalquilo, heterociclilo, alquilo sustituido con 1-6 grupos R9 cuyos pueden ser iguales o diferentes con cada R9 seleccionado en forma independiente, arilo sustituido con 1-3 grupos arilo o heteroarilo que pueden ser iguales o diferentes y se seleccionan en forma independiente de grupos fenilo, piridilo, tiofenilo, furanilo y tiazolo, o es un resto del grupo de fórmula (2); R3 se seleccionan del grupo formado por H, halógeno, -NR5R6, -C(O)NR5R6, alquilo, alquinilo, cicloalquilo, arilo, arilalquilo, heterociclilo, heterocicliloalquilo, heteroarilo y heteroarilalquilo, o es un de resto del grupo de fórmula (3), donde cada uno de dicho alquilo, cicloalquilo, arilo, arilalquilo, heterociclilo, heterocicliloalquilo, heteroarilo y heteroarilalquilo para R3 y los restos heterociclilo cuyas estructuras se mostraron precedentemente para R3 pueden sustituirse o sustituirse en forma opcional independientemente con uno o más restos que pueden ser iguales o diferentes, cada resto se selecciona en forma independiente del grupo formado por halógeno, alquilo, arilo, cicloalquilo, CF3, CN, -OCF3,-(CR4R5)nOR5, -OR5, -NR5R6, -(CR4R5)nNR5R6, -C(O2)R5, -C(O)R5, -C(O)NR5R6, -SR6, -S(O2)R6, -S(O2)NR5R6, -N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR5R6; R4 es H, halo o alquilo; R5 es H o alquilo; R6 se selecciona del grupo formado por H, alquilo, arilo, arilalquilo, cicloalquilo, heterociclilo, heterocicliloalquilo, heteroarilo, y heteroarilalquilo, donde cada uno de dicho alquilo, arilo, arilalquilo, cicloalquilo, heterociclilo, heterocicliloalquilo, heteroarilo, y heteroarilalquilo puede estar no sustituido o sustituido en forma opcional con uno o más restos que pueden ser iguales o diferentes, cada resto se selecciona en forma independiente del grupo formado por halógeno, alquilo, arilo, cicloalquilo, heterocicliloalquilo, CF3, OCF3, CN, -OR5, -NR5R10, -N(R5)Boc, -(CR4R5)nOR5, -C(O2)R5, -C(O)R5, -C(O)NR5R10, -SO3H, -SR10, -S(O2)R7, -S(O2)NR5R10, -N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR5R10; R10 se selecciona del grupo formado por H, alquilo, arilo, arilalquilo, cicloalquilo, heterociclilo, heterocicliloalquilo, heteroarilo, y heteroarilalquilo, donde cada uno de dicho alquilo, arilo, arilalquilo, cicloalquilo, heterociclilo, heterocicliloalquilo, heteroarilo, y heteroarilalquilo puede estar no sustituido o sustituido en forma opcional con uno o más restos que pueden ser iguales o diferentes, cada resto se selecciona en forma independiente del grupo formado por halógeno, alquilo, arilo, cicloalquilo, heterocicliloalquilo, CF3, OCF3, CN, -OR5, -NR4R5, -N(R5)Boc, -(CR4R5)nOR5, -C(O2)R5, -C(O)NR4R5, -C(O)R5, -SO3H, -SR5, -S(O2)R7, -S(O2)NR4R5, -N(R5)S(02)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR4R5; o en forma opcional (i) R5 y R10 en la porción -NR5R10, o (ii) R5 y R6 en la porción -NR5R6, pueden unirse para formar un resto cicloalquilo o heterociclilo, con cada uno de dichos restos cicloalquilo o heterociclilo no sustituido o sustituido en forma independiente y opcional con uno o más grupos R9; R7 se selecciona del grupo formado por alquilo, cicloalquilo, arilo, heteroarilo, arilalquilo y heteroarilalquilo, donde cada uno de dicho alquilo, cicloalquilo, heteroarilalquilo, arilo, heteroarilo y arilalquilo puede ser insustituido o sustituido en forma independiente y opcional con uno o más restos que pueden ser iguales o diferentes, cada resto se selecciona en forma independiente del grupo formado por halógeno, alquilo, arilo, cicloalquilo, CF3, OCF3, CN, -OR5, -NR5R10, -CH2OR5, -C(O2)R5, -C(O)NR5R10, -C(O)R5, -SR10, -S(O2)R10, -S(O2)NR5R10, -N(R5)S(02)R10 -N(R5)C(O)R10 y -N(R5)C(O)NR5R10; R8 se selecciona del grupo formado por R6, -C(O)NR5R10, -S(O2)NR5R10, -C(O)R7 y -S(O2)R7; R9 se selecciona del grupo formado por, CN, -NR5R10, -C(O2)R6, -C(O)NR5R10, -OR6, -SR6, -S(O2)R7, -S(O2)NR5R10, -N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR5R10; m es 0 hasta 4, y n es 1 hasta 4, con las siguientes salvedades: (i) que cuando R es un fenilo no sustituido, entonces R2 no sea alquilo, -C(O2)R6, arilo o cicloalquilo, y (ii) que cuando R es un fenilo sustituido con un grupo hidroxilo, entonces R2 es halógeno solamente.
ARP030103188A 2002-09-04 2003-09-03 Pirazolopirimidinas como inhibidores de la quinasa dependientes de la ciclina AR041133A1 (es)

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