AR040925A1 - Compuestos de pirazol utiles como inhibidores de proteinquinasa - Google Patents

Compuestos de pirazol utiles como inhibidores de proteinquinasa

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Publication number
AR040925A1
AR040925A1 ARP010105963A ARP010105963A AR040925A1 AR 040925 A1 AR040925 A1 AR 040925A1 AR P010105963 A ARP010105963 A AR P010105963A AR P010105963 A ARP010105963 A AR P010105963A AR 040925 A1 AR040925 A1 AR 040925A1
Authority
AR
Argentina
Prior art keywords
ring
so2n
con
independently selected
nitrogen
Prior art date
Application number
ARP010105963A
Other languages
English (en)
Original Assignee
Vertex Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR040925A1 publication Critical patent/AR040925A1/es

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Abstract

Un compuesto de pirazol útil como inhibidor de proteinquinasa que responde a fórmula (1), o un derivado o prodroga farmacéuticamente aceptable del mismo, en donde: Rx y Ry son seleccionados independientemente de T-R3 ó L-Z-R3; R1 es T-(anillo D); el anillo D es un anillo monocíclico de 5-7 miembros o un anillo bicíclico de 8-10 miembros seleccionado entre arilo, heteroarilo, heterociclilo o carbociclilo, teniendo dicho anillo heteroarilo o heterociclilo 1-4 heteroátomos en el anillo seleccionados entre nitrógeno, oxígeno o azufre, en donde el anillo D está sustituido en cualquier átomo de carbono sustituible del anillo por oxo, T-R5, o V-Z-R5, y en cualquier átomo de nitrógeno del anillo por -R4; T es una ligadura de valencia o una cadena de alquilideno C1-4; Z es una cadena alquilideno C1-4; L es -O-, -S-, -SO-, -SO2-, -N(R6)SO2-, -SO2N(R6)-, -N(R6)-, -CO-, -CO2-, -N(R6)CO-, -N(R6)C(O)O-, -N(R6)CON(R6)-, -N(R6)SO2N(R6)-, -N(R6)N(R6)-, -C(O)N(R6)-, -OC(O)N(R6)-, -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -C(R6)2N(R6)C(O)-, -C(R6)2N(R6)C(O)O-, -CR6)=NN(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2N(R6)-, ó -C(R6)2N(R6)CON(R6)-; R2 y R2' son seleccionados independientemente entre -R, -T-W-R6, ó R2 y R2' son tomados conjuntamente con los átomos a los cuales están unidos para formar un anillo fusionado de 5-8 miembros, no saturado o parcialmente no saturado, que tiene 0-3 heteroátomos en el anillo, seleccionados entre nitrógeno, oxígeno o azufre, en donde cualquier carbono sustituible de dicho anillo fusionado formado por R2 y R2' está sustituido por halo, oxo, -CN, -NO2, -R7 ó -V-R6, y cualquier nitrógeno sustituible de dicho anillo formado por R2 y R2' está sustituido por R4; R3 es seleccionado entre -R, -halo, -OR, -C(=O)R, -CO2R, -COCOR, -COCH2COR, -NO2, -CN, -S(O)R, -S(O)2R, -SR, -N(R4)2, -CON(R7)2, -SO2N(R7)2, -OC(=O)R, -N(R7)COR, -N(R7)CO2(alifático C1-6), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R7)CON(R7)2, -N(R7)SO2N(R7)2, -N(R4)SO2R, ó -OC(=O)N(R7)2; cada R es seleccionado independientemente entre hidrógeno o un grupo opcionalmente sustituido seleccionado entre alifático C1-6, arilo C6-10, un anillo heteroarilo, que tiene 5-10 átomos de anillo, o un anillo heterociclilo que tiene 5-10 átomos de anillo; cada R4 es seleccionado independientemente entre -R7, -COR7, -CO2(alifático C1-6) opcionalmente sustituido), -CON(R7)2, ó -SO2R7; cada R5 es seleccionado independientemente entre -R, halo, -OR, -C(=O)R, -CO2R, -COCOR, -NO2, -CN, -S(O)R, -S(O)2R, -SR, -N(R4)2, -CON(R4)2, -SO2N(R4)2, -OC(=O)R, -N(R4)COR, -N(R4)CO2(alifático C1-6 opcionalmente sustituido), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R4)CON(R4)2, -N(R4)SO2N(R4)2, -N(R4)SO2R, ó -OC(=O)N(R4)2; V es -O-, -S-, -SO-, -SO2-, -N(R6)SO2-, -SO2N(R6)-, -N(R6)-, -CO-, -CO2-, -N(R6)CO-, -N(R6)C(O)O-, -N(R6)CON(R6)-, -N(R6)SO2N(R6)-, -N(R6)N(R6)-, -C(O)N(R6)-, -OC(O)N(R6)-, -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -C(R6)2N(R6)C(O)-, -C(R6)2N(R6)C(O)O-, -C(R6)=NN(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2N(R6)-, ó -C(R6)2N(R6)CON(R6)-; W es -C(R6)2-O, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -CO-, -CO2-, -C(R6)OC(O)-, -C(R6)OC(O)N(R6)-, -C(R6)2N(R6)CO-, -C(R6)2N(R6)C(O)O-, -C(R6)=NN(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2N(R6)-, -C(R6)2N(R6)CON(R6)-, ó -CON(R6)-; cada R6 es seleccionado independientemente entre hidrógeno o un grupo alifático C1-4 opcionalmente sustituido, o dos grupos R6 sobre el mismo átomo de nitrógeno son tomados conjuntamente con el átomo de nitrógeno para formar un anillo heterociclilo o heteroarilo de 5-6 miembros; y cada R7 es seleccionado independientemente entre hidrógeno o un grupo alifático C1-6 opcionalmente sustituido, o dos R7 sobre el mismo nitrógeno son tomados conjuntamente con el nitrógeno para formar un anillo heterociclilo o heteroarilo de 5-8 miembros. Los compuestos son útiles como inhibidores de proteinquinasas especialmente como inhibidores de Aurora-2 y GSK-3, para tratar enfermedades tales como cáncer, diabetes y enfermedad de Alzheimer.
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