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AR057995A1 - Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas heteroarilo sustituidas como inhibidoras de quinasas janus - Google Patents

Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas heteroarilo sustituidas como inhibidoras de quinasas janus

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Publication number
AR057995A1
AR057995A1 ARP060105499A ARP060105499A AR057995A1 AR 057995 A1 AR057995 A1 AR 057995A1 AR P060105499 A ARP060105499 A AR P060105499A AR P060105499 A ARP060105499 A AR P060105499A AR 057995 A1 AR057995 A1 AR 057995A1
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Argentina
Prior art keywords
cr11r12
alkyl
alkylene
nrcrd
haloalkyl
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ARP060105499A
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English (en)
Inventor
James D Rodgers
Stacy Shepard
Thomas P Maduskuie
Haisheng Wang
Nikoo Falahatpisheh
Maria Rafalski
Argyrios G Arvanitis
Storac
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Incyte Corp
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Application filed by Incyte Corp filed Critical Incyte Corp
Publication of AR057995A1 publication Critical patent/AR057995A1/es

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Abstract

Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas sustituidas con heteroarilo que modulan la actividad de las quinasas Janus y son utiles para el tratamiento de enfermedades relacionadas con la actividad de las quinasas Janus que incluyen por ejemplo, las enfermedades relacionadas con el sistema inmune, trastornos dermatologicos, trastornos proliferativos mieloides, cáncer y otras enfermedades. Reivindicacion 1: Un compuesto de formula (1), que incluye formas de sales o prodrogas aceptables para uso farmacéutico de los mismos, donde A1 y A2 se seleccionan en forma independiente entre C y N; T, U, y V se seleccionan en forma independiente entre O, S, N, CR5, y NR6; donde el anillo de 5 miembros formado por A1, A2, U, T, y V es aromático; X es N o CR4; Y es alquileno C1-8, alquenileno C2-8, alquinileno C2-8, (CR11R12)p-(cicloalquileno C3-10)-(CR11R12)q, (CR11R12)p-(arileno)-(CR11R12)q, (CR11R12)p-(heterocicloalquileno C1-10)-(CR11R12)q, (CR11R12)p-(heteroarileno)- (CR11R12)q, (CR11R12)p-O-(CR11R12)q, (CR11R12)p-S-(CR11R12)q, (CR11R12)p-C(O)-(CR11R12)q, (CR11R12)p-C(O)NRc-(CR11R12)q, (CR11R12)p-C(O)O-(CR11R12)q, (CR11R12)p-OC(O)-(CR11R12)q, (CR11R12)p-OC(O)NRc-(CR11R12)q, (CR11R12)p-NRc-(CR11R12)q, (CR11R12)p- NRcC(O)NRd-(CR11R12)q, (CR11R12)p-S(O)-(CR11R12)q, (CR11R12)p-S(O)NRc-(CR11R12)q, (CR11R12)p-S(O)2-(CR11R12)q, o (CR11R12)p-S(O)2NRc-(CR11R12)q, donde dicho alquileno C1-8, alquenileno C2-8, alquinileno C2-8, cicloalquileno, arileno, heterocicloalquileno, o heteroarileno, se sustituye opcionalmente con 1, 2, o 3 sustituyentes seleccionados en forma independiente entre -D1-D2-D3-D4; Z es H, halo, alquilo C1-4, alquenilo C2-8, alquinilo C2-8, haloalquilo C1-4, halosulfanilo, hidroxialquilo C1-4, cianoalquilo C1-4, =C-Ri, =N-Ri, Cy1, CN, NO2, ORa, SRa. C(O)Rb, C(O)NRcRd, c(o)oRa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)NRbRd, NRcC(o)oRa, C(=NRi)NRcRd, NRcC(=NRi)NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, NRcS(O)2Rb C(=NOH)Rb, C(=NO(alquilo C1-6)Rb, y S(O)2NRcRd, donde dicho alquilo C1-8, alquenilo C2-8, o alquinilo C2-8, se sustituye opcionalmente con 1, 2, 3, 4, 5, o 6 sustituyentes seleccionados en forma independiente entre halo, alquilo C1-4, alquenilo C2- 4, alquinilo C2-4, haloalquilo C1-4, halosulfanilo, hidroxialquilo C1-4, cianoalquilo C1-4, Cy1, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)NRcRd, NRcC(O)ORa, C(=NRi)NRcRd, NRcC(=NRi)NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, NRcS(O)2Rb, C(=NOH)Rb, C(=NO(alquilo C1-6))Rb, y S(O)2NRcRd donde cuando Z es H, n es 1; o la porcion -(Y)-Z se toma junto con i) A2 al cual, la porcion se encuentra unida, ii) R5 o R6 de tanto T como V, y iii) el átomo de C o N al cual el R5 o R6 de tanto T como V se encuentra unido para formar un anillo arilo, cicloalquilo, heteroarilo, o heterocicloalquilo de 4 a 20 miembros fusionado al anillo de 5 miembros formado por A1, A2, U, T, y V, donde dicho anillo arilo, cicloalquilo, heteroarilo, o heterocicloalquilo de 4 a 20 miembros se sustituye opcionalmente con 1, 2, 3, 4, o 5 sustituyentes seleccionados en forma independiente entre -(W)m-Q; W es alquilenilo C1-8, alquenilenilo C2-8, alquinilenilo C2-8, O, S, C(O), C(O)NRc', C(O)O, OC(O), OC(O)NRc', NRc', NRc'C(O)NRd', S(O), S(O)NRc', S(O)2, o S(O)2NRc'; Q es H, halo, CN, NO2, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, haloalquilo C1-8, halosulfanilo, arilo, cicloalquilo, heteroarilo, o heterocicloalquilo donde dicho alquilo C1-8, alquenilo C2-8, alquinilo C2-8, haloalquilo C1-8, arilo, cicloalquilo, heteroarilo, o heterocicloalquilo se sustituye opcionalmente con 1, 2, 3 o 4 sustituyentes seleccionados en forma independiente entre halo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, halosulfanilo, hidroxialquilo C1-4, cianoalquilo C1-4, Cy2, CN, NO2, ORa', SRa', C(O)Rb', C(O)NRc'Rd', C(O)ORa', OC(O)Rb', OC(O)NRc'Rd', NRc'Rd', NRc'C(O)Rb', NRc'C(O)NRc'Rd', NRc'C(O)ORa', S(O)Rb', S(O)NRc'Rd', S(O)2Rb', NRc'S(O)2Rb', y S(O)2NRc'Rd'; Cy1 y Cy2 se seleccionan en forma independiente entre arilo, heteroarilo, cicloalquilo, y heterocicloalquilo, cada uno sustituido opcionalmente con 1, 2, 3, 4 o 5 sustituyentes seleccionados en forma independiente entre halo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, halosulfanilo, hidroxialquilo C1-4, cianoalquilo C1-4, CN, NO2, ORaö, SRa", C(O)Rbö, C(O)NRc"Rd", C(o)oRaö, OC(O)Rbö, OC(O)NRc"Rdö, NRcöRdö, NRcöC(O)Rb", NRc"C(o)oRa", NRcös(o)Rbö, NRcös(o)2Rb", S(O)Rbö, S(O)NRc"Rdö, S(O)2Rbö, y S(O)2NRc"Rd"; R1, R2, R3, y R4 se seleccionan en forma independiente entre H, halo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, halosulfanilo, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, OR7, SR7, C(O)R8, C(O)NR9R10, C(O)OR7, OC(O)R8, OC(O)NR9R10, NR9R10, NR9C(O)R8, NRcC(O)OR7, S(O)R8, S(O)NR9R10, S(O)2R8, NR9S(O)2R8, y S(O)2NR9R10; R5 es H, halo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, halosulfanilo, CN, NO2, OR7, SR7, C(O)R8, C(O)NR9R10, C(O)OR7, OC(O)R8, OC(O)NR9R10, NR9R10, NR9C(O)R8, NR9C(O)OR7, S(O)R8, S(O)NR9R10, S(O)2R8, NR9S(O)2R8, o S(O)2NR9R10; R6 es H, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, OR7, C(O)R8, C(O)NR9R10, C(O)OR7, S(O)R8, S(O)NR9R10, S(O)2R8, o S(O)2NR9R10; R7 es H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo; R8 es H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo; R9 y R10 se seleccionan en forma independiente entre H, alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilcarbonilo C1-6, arilcarbonilo, alquilsulfonilo C1-6, arilsulfonilo, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo; o R9 y R10 junto con el átomo de N al cual se encuentran unidos forman un grupo heterocicloalquilo de 4, 5, 6 o 7 miembros; R11 y R12 se seleccionan en forma independiente entre H y -E1-E2-E3-E4; D1 y E1 se encuentran en forma independiente ausentes o se seleccionan en forma independiente entre alquileno C1-6, alquenileno C2-6, alquinileno C2-6, arileno, cicloalquileno, heteroarileno, y heterocicloalquileno, cada uno de los alquileno C1-6, alquenileno C2-6, alquinileno C2-6, arileno, cicloalquileno, heteroarileno, y heterocicloalquileno se sustituye opcionalmente con 1, 2 o 3 sustituyentes seleccionados en forma independiente entre halo, CN, NO2, N3, SCN, OH, alquilo C1-6, haloalquilo C1-6, alcoxialquilo C2-8, alcoxi C1-6, haloalcoxi, amino, alquilamino C1-6, y dialquilamino C2-8; D2 y E2 se encuentran en forma independiente ausentes o se seleccionan en forma independiente entre alquileno C1-6, alquenileno C2-6, alquinileno C2-6, (alquileno C1-6)r-O-(alquileno C1-6)s, (alquileno C1-6)r-S-(alquileno C1-6)s, (alquileno C1-6)r-NRe-(alquileno C1-6)s, (alquileno C1-6)r-CO-(alquileno C1-6)s, (alquileno C1-6)r-COO-(alquileno C1-6)s, (alquileno C1-6)r-CONRe-(alquileno C1-6)s, (alquileno C1-6)r-SO-(alquileno C1-6)s, (alquileno C1-6)r-SO2-(alquileno C1-6)s, (alquileno C1-6)r-SONRe-(alquileno C1-6)s, y (alquileno C1-6)r-NReCONRf-(alquileno C1-6)s, cada uno de los alquileno C1-6, alquenileno C2-6, y alquinileno C2-6 se sustituye opcionalmente con 1, 2 o 3 sustituyentes seleccionados en forma independiente entre halo, CN, NO2, N3, SCN, OH, alquilo C1-6, haloalquilo C1-6, alcoxialquilo C2-8, alcoxi C1-6, haloalcoxi C1-6, amino, alquilamino C1-6, y dialquilamino C2-8; D3 y E3 se encuentran en forma independiente ausentes o se seleccionan en forma independiente entre alquileno C1-6, alquenileno C2-6, alquinileno C2-6, arileno, cicloalquileno, heteroarileno, y heterocicloalquileno, cada uno de los alquileno C1-6, alquenileno C2-6, alquinileno C2-6, arileno, cicloalquileno, heteroarileno, y heterocicloalquileno se sustituye opcionalmente con 1, 2 o 3 sustituyentes seleccionados en forma independiente entre halo, CN, NO2, N, SCN, OH, alquilo C1-6, haloalquilo C1-6, alcoxialquilo C2-8, alcoxi C1-6, haloalcoxi C1-6, amino, alquilamino C1-6, y dialquilamino C2-8; D4 y E4 se seleccionan en forma independiente entre H, halo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, halosulfanilo, hidroxialquilo C1-4, cianoalquilo C1-4, Cy1, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)NRcRd, NRcC(O)ORa, C(=NRi)NRcRd, NRcC(=NRi)NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, NRcS(O)2Rb, C(=NOH)Rb, C(NO(alquilo C1-6)Rb, y S(O)2NRcRd, donde dicho alquilo C1-8, alquenilo C2-8, o alquinilo C2-8, se sustituye opcionalmente con 1 2, 3, 4, 5, o 6 sustituyentes seleccionados en forma independiente entre halo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, halosulfanilo, hidroxialquilo C1-4, cianoalquilo C1-4, Cy1, CN, NO2, OR, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)NRcRd, NRcC(O)ORa, C(=NRi)NRcRd, NRcC(=NRi)NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, NRcS(O)2Rb, C(=NOH)Rb, C(=NO(alquilo C1-6))Rb, y S(O)2NRcRd; Ra es H, Cy1, -(alquilo C1-6)-Cy1, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, donde dicho alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, o alquinilo C2-6 se sustituye opcionalmente con 1, 2, o 3 sustituyentes seleccionados en forma independiente entre OH, CN, amino, halo, alquilo C1-6, haloalquilo C1-6, halosulfanilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo y heterocicloalquilo; Rb es H, Cy1, -(alquilo C1-6)-Cy1, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, donde dicho alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, o alquinilo C2-6 se sustituye opcionalmente con 1, 2, o 3 sustituyentes seleccionados en forma independiente entre OH, CN, amino, halo, alquilo C1-6, haloalquil
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