AR032130A1 - Un compuesto inhibidor de quinasas proteicas, una composicion farmaceutica que lo incluye, y un metodo para tratar afecciones con dicho compuesto - Google Patents

Un compuesto inhibidor de quinasas proteicas, una composicion farmaceutica que lo incluye, y un metodo para tratar afecciones con dicho compuesto

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Publication number
AR032130A1
AR032130A1 ARP000104188A ARP000104188A AR032130A1 AR 032130 A1 AR032130 A1 AR 032130A1 AR P000104188 A ARP000104188 A AR P000104188A AR P000104188 A ARP000104188 A AR P000104188A AR 032130 A1 AR032130 A1 AR 032130A1
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AR
Argentina
Prior art keywords
substituted
heterocyclyl
aryl
optionally
inhibitors
Prior art date
Application number
ARP000104188A
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English (en)
Inventor
Mark Ledeboer
Jingrong Cao
Michael R Hale
Jeremy Green
Guy Bemis
Anne-Laure Grillot
Francisco G Salituro
Edmund M Harrington
Xingtao Gao
Christopher Baker
Original Assignee
Vertex Pharma
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Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR032130A1 publication Critical patent/AR032130A1/es

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Abstract

Un compuesto inhibidor de quinasas, de formula (1) en donde: X-Y-Z es seleccionado de uno de los restos de formulas (2) a (6); R1 es H, CONH2, T(n)-R, o T(n)-Ar2; R es un grupo alifático o alifático sustituido; n es 0 o 1; T es C(=O), CO2, CONH, S(O)2, S(O)2NH, COCH2 o CH2; cada R2 es seleccionado independientemente de hidrogeno, -R, -CH2OR, -CH2OH, -CH=O, -CH2SR, -CH2S(O)2R, -CH2(C=O)R, -CH2CO2R, -CH2CO2H, -CH2CN, -CH2NHR, -CH2N(R)2, -CH=N-OR, -CH=NNHR, -CH=NN(R)2, -CH=NNHCOR, -CH=NNHCO2R, -CH=NNHSO2R, -arilo, -arilo sustituido, -CH2(arilo), -CH2(arilo sustituido), -CH2NH2, -CH2NHCOR, -CH2NHCONHR, -CH2NHCON(R)2, -CH2NRCOR, -CH2NHCO2R, -CH2CONHR, -CH2CON(R)2, -CH2SO2NH2, -CH2(heterociclilo), -CH2(heterociclilo sustituido), -(heterociclilo), o -(heterociclilo sustituido); cada R3 es seleccionado independientemente de hidrogeno, R, COR, CO2R o S(O)2R; G es R o Ar1; Ar1 es arilo, arilo sustituido, aralquilo, aralquilo sustituido, heterociclilo, o heterociclilo sustituido, en donde Ar1 es fusionado opcionalmente a un anillo de 5 a 7 miembros parcialmente no saturado o completamente no saturado que contiene 0-3 heteroátomos; Q-NH se selecciona de las formulas (7) u (8), en donde el H de Q-NH es reemplazado opcionalmente por R3; A es N o CR3; U es CR3, O, S, o NR3; Ar2 es arilo, arilo sustituido, heterociclilo o heterociclilo sustituido, en donde Ar2 es fusionado opcionalmente a un anillo de 5 a 7 miembros parcialmente no saturado o completamente no saturado que contiene 0-3 heteroátomos; en donde cada átomo de carbono sustituible en Ar2, incluyendo el anillo fusionado si está presente, está opcionalmente e independientemente sustituido por halo, R, OR, SR, OH, NO2, CN, NH2, NHR, N(R)2, NHCOR, NHCONHR, NHCON(R)2, NRCOR, NHCO2R, CO2R, CO2H, COR, CONHR, CON(R)2, S(O)2R, SONH2, S(O)R, SO2NHR, o NHS(O)2R, y en donde cada carbono saturado en el anillo fusionado está además opcionalmente e independientemente sustituido por =O, =S, =NNHR, =NNR2, =N-OR, =NNHCOR, =NNHCO2R, =NNHSO2R, o =NR; y en donde cada átomo de nitrogeno sustituible en Ar2 está opcionalmente sustituido por R, COR, S(O)2R, o CO2R; siempre que cuando G es fenilo, X-Y-Z es N-O-CR2, A es N, y R2 es metilo, R1 no es hidrogeno o COCH3. Estos compuestos son inhibidores de quinasas proteicas, particularmente inhibidores de JNK, una quinasa proteica mamaria implicada en la proliferacion celular, la muerte celular y la respuesta a estímulos extracelulares. Métodos para producir estos inhibidores. Composiciones farmacéuticas que comprenden los inhibidores de la formula (1) y métodos para utilizar dichas composiciones en el tratamiento y la prevencion de varios trastornos.
ARP000104188A 1999-08-13 2000-08-11 Un compuesto inhibidor de quinasas proteicas, una composicion farmaceutica que lo incluye, y un metodo para tratar afecciones con dicho compuesto AR032130A1 (es)

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US14879599P 1999-08-13 1999-08-13
US16692299P 1999-11-22 1999-11-22
US21151700P 2000-06-14 2000-06-14

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AR032130A1 true AR032130A1 (es) 2003-10-29

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