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AR066429A1 - Derivados de imidazolopiridina y purina como inhibidores de tirosina quinasa - Google Patents

Derivados de imidazolopiridina y purina como inhibidores de tirosina quinasa

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Publication number
AR066429A1
AR066429A1 ARP080101879A ARP080101879A AR066429A1 AR 066429 A1 AR066429 A1 AR 066429A1 AR P080101879 A ARP080101879 A AR P080101879A AR P080101879 A ARP080101879 A AR P080101879A AR 066429 A1 AR066429 A1 AR 066429A1
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Argentina
Prior art keywords
carbocyclyl
heterocyclyl
case
independently selected
6alkenyl
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ARP080101879A
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English (en)
Inventor
Hai-Jun Zhang
Audrey Davies
Tao Wang
Mei Su
Stephanos Ioannidis
Michelle Lamb
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Astrazeneca Ab
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Publication of AR066429A1 publication Critical patent/AR066429A1/es

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    • C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
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    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
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    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
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Abstract

Compuestos de la formula 1 y composiciones farmacéuticas de los mismos y sus métodos de uso. Estos compuestos proveen un tratamiento para trastornos mieloproliferativos y cáncer. Reivindicacion 1: Un compuesto caracterizado porque es de Formula(1) o una sal aceptable para uso farmacéutico del mismo, en donde Q se selecciona entre N y C(R3); D se selecciona entre N y CH; R1 se selecciona entre H, -CN, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, carbociclilo de 3 a 5 miembros, heterociclilode 5 miembros, -OR1a, -SR1a, -N(R1a)2, -N(R1a)C(O)R1b, -N(R1a)N(R1a)2, -NO2, -C(O)H, C(O)R1b, -C(O)2R1a , -C(O)N(R1a)2, -OC(O)N(R1a)2 -N(R1a)C(O)2R1a, -N(R1a)C(O)N(R1a)2, -OC(O)R1b, -S(O)R1b, -S(O)2R1b, -S(O)2N(R1a)2, -N(R1a)S(O)2R1b, -C(R1a)=N(R1a), y -C(R1a)=N(OR1a), en donde dichos C1-6aIquiIo, C2-6alquenilo, C2-6aIquiniIo, carbociclilo de 3 a 5 miembros, y heterociclilo de 5 miembros están opcionalmente sustituidos con uno o más R10; R1a en cada caso se selecciona en formaindependiente entre H y C1-6aIquilo, carbociclilo de 3 a 5 miembros, y heterociclilo de 5 miembros, en donde dichos C1-6alquilo, carbociclilo de 3 a 5 miembros, y heterociclilo de 5 miembros en cada caso y en forma independiente están opcionalmentesustituidos con uno o más R10; R1b en cada caso se selecciona en forma independiente entre C1-6alquilo, C2-6alquenilo, C2-6alquiniIo, carbociclilo de 3 a 5 miembros, y heterociclilo de 5 miembros, en donde dichos C1-6aIquilo, C2-6alquenilo, C2-6alquinilo, carbociclilo de 3 a 5 miembros, y heterociclilo de 5 miembros en cada caso y en forma independiente están opcionalmente sustituidos con uno o más R10; R2 se selecciona entre H, halo, -CN, C1-6alquilo, C2-6aIqueniIo, C2-6alquiniIo,carbociclilo, heterociclilo, -OR2a, -SR2a, -N(R2a)2, -N(R2a)C(O)R2b, -N(R2a)N(R2a)2, -NO2, -C(O)H, -C(O)R2b, -C(O)2R2a, -C(O)N(R2a)2, -OC(O)N(R2a)2, -N(R2a)C(O)2R2a, -N(R2a)C(O)N(R2a)2, -OC(O)R2b, -S(O)R2b, -S(O)2R2b, -S(O)2N(R2a)2, -N(R2a)S(O)2R2b,-C(R2a)=N(R2a), y C(R2a)=N(OR2a), en donde dichos C1-6alquilo, C2-6alquenilo, C2-6alquinilo, carbociclilo, y heterociclilo están opcionalmente sustituidos con uno o más R20; R2a en cada caso se selecciona en forma independiente entre H, C1-6alquilo,carbociclilo, y heterociclilo, en donde dichos C1-6alquiIo, carbociclilo, y heterociclilo en cada caso y en forma independiente están opcionalmente sustituidos con uno o más R20; R2b en cada caso se selecciona en forma independiente entre C1-6alquiIo, C2-6alquenilo, C2-6alquinilo, carbociclilo, y heterociclilo, en donde dichos C1-6alquiIo, C2-6alquenilo, C2-6alquinilo, carbociclilo, y heterociclilo en cada caso y en forma independiente están opcionalmente sustituidos con uno o más R20;R3 se selecciona entre H, halo, -CN, C1-6aIquilo, C2-6alquenilo, C2-6alquinilo, carbociclilo, heterociclilo, -OR3a, -SR3a, -N(R3a)2, -N(R3a)C(O)R3b, -N(R3a)N(R3a)2, -NO2, -C(O)H, -C(O)R3b, -C(O)2R3a, -C(O)N(R3a)2, -OC(O)N(R3a)2, -N(R3a)C(O)2R3a, -N(R3a)C(O)N(R3a)2, -OC(O)R3b, -S(O)R3b, -S(O)2R3b, -S(O)2N(R3a)2, -N(R3a)S(O)2R3b, -C(R3a)=N(R3a) y -C(R3a)=N(OR3a), en donde dichos C1-6aIquiIo, C2-6alquenilo, C2-6alquinilo, carbociclilo, y heterociclilo están opcionalmente sustituidos con uno omás R30; R3a en cada caso se selecciona en forma independiente entre H, C1-6aIquiIo, carbociclilo, y heterociclilo, en donde dichos C1-6alquiIo, carbociclilo, y heterociclilo en cada caso y en forma independiente están opcionalmente sustituidos conuno o más R30; R3b en cada caso se selecciona en forma independiente entre C1-6aIquilo, C2-6alquenilo, C2-6aIquiniIo, carbociclilo, y heterociclilo, en donde dichos C1-6aIquiIo, C2-6alquenilo, C2-6alquinilo, carbociclilo, y heterociclilo en cadacaso y en forma independiente están opcionalmente sustituidos con uno o más R30; R4 se selecciona entre H, -CN, C1-6aIquiIo, C2-6aIqueniIo, C2-6alquiniIo, carbociclilo, heterociclilo, -N(R4a)C(O)R4b, -N(R4a)N(R4a)2, -NO2, -C(O)H, -C(O)R4b, -C(O)2R4a, -C(O)N(R4a)2, -OC(O)N(R4a)2, -N(R4a)C(O)2R4a, -N(R4a)C(O)N(R4a)2, -OC(O)R4b, -S(O)R4b, -S(O)2R4b, -S(O)2N(R4a)2, -N(R4a)S(O)2R4b, -C(R4a)=N(R4a), y -C(R4a)=N(OR4a), en donde dichos C1-6aIquiIo, C2-6alquenilo, C2-6aIquiniIo, carbociclilo, yheterociclilo están opcionalmente sustituidos con uno o más R 40; R4a en cada caso se selecciona en forma independiente entre H, C1-6aIquiIo, carbociclilo, y heterociclilo, en donde dichos C1-6aIquiIo, carbociclilo, y heterociclilo en cada caso y enforma independiente están opcionalmente sustituidos con uno o más R40; R4b en cada caso se selecciona en forma independiente entre C1-6alquilo, C2-6alquenilo, C2-6alquiniIo, carbociclilo, y heterociclilo, en donde dichos C1-6alquilo, C2-6alquenilo,C2-6-5alquinilo, carbociclilo, y heterociclilo en cada caso y en forma independiente están opcionalmente sustituidos con uno o más R40; R5 se selecciona en forma independiente entre halo, -CN, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, carbociclilo,heterociclilo, -OR5a, -SR5a, -N(R5a)2, -N(R5a)C(O)R5b, -N(R5a)N(R5a)2, -NO2, -C(O)H, -C(O)R5b, -C(O)2R5a, -C(O)N(R5a)2, -OC(O)N(R5a)2, -N(R5a)C(O)2R5a, -N(R6a)C(O)N(R5a)2, -OC(O)R5b, -S(O)R5b, -S(O)2R5b, -S(O)2N(R5a)2, -N(R5a)S(O)2R5b, -C(R5a)=N(R5a), y -C(R5a)=N(OR5a); R5a en cada caso se selecciona en forma independiente entre H, C1-6alquilo, carbociclilo, y heterociclilo; R5b en cada caso se selecciona en forma independiente entre C1-6aIquiIo, C2-6alquenilo, C2-6alquinilo,carbociclilo, y heterociclilo; R10 en cada caso se selecciona en forma independiente entre halo, -CN, C1-6aIquilo, C2-6aIquenilo, C2-6alquinilo, carbociclilo, heterociclilo, -OR10a, -SR10a, -N(R10a)2, -N(R10a)C(O)R10b, -N(R10a)N(R10a)2, -NO2, -C(O)H, -C(O)R10b, -C(O)2R10a, -C(O)N(R10a)2, -OC(O)N(R10a)2, -N(R10a)C(O)2R10a, -N(R10a)C(O)N(R10a)2, -OC(O)R10b, -S(O)R10b, -S(O)2R10b, -S(O)2N(R10a)2, -N(R10a)S(O)2R10b, -C(R10a)=N(R10a), y -C(R10a)=N(OR10a); R10a en cada caso se selecciona enforma independiente entre H, C1-6alquiIo, carbociclilo, y heterociclilo; R10b en cada caso se selecciona en forma independiente entre C1-6aIquilo, C2-6alquenilo, C2-6alquinilo, carbociclilo, y heterociclilo; R20 en cada caso se selecciona en formaindependiente entre halo, -CN, C1-6aIquilo, C2-6alqueniIo, C2-6alquinilo, carbociclilo, heterociclilo, -OR20a, SR20a, -N(R20a)2, -N(R20a)C(O)R20b, -N(R20a)N(R20a)2, -NO2, -C(O)H, -C(O)R20b, -C(O)2R20a, -C(O)N(R20a)2, -OC(O)N(R20a)2, -N(R20a)C(O)2R20a, -N(R20a)C(O)N(R20a)2, -OC(O)R20b, -S(O)R20b, -S(O)2R20b, -S(O)2N(R20a)2, -N(R20a)S(O)2R20b, -C(R20a)=N(R20a), y -C(R20a)=N(OR20a); R20a en cada caso se selecciona en forma independiente entre H, C1-6aIquilo, carbociclilo, yheterociclilo; R20b en cada caso se selecciona en forma independiente entre C1-6alquilo, C2-6alquenilo, C2-6aIquinilo, carbociclilo, y heterociclilo; R30 en cada caso se selecciona en forma independiente entre halo, -CN, C1-6aIquilo, C2-6alqueniIo,C2-6alquinilo, carbociclilo, heterociclilo, -OR30a, -SR30a, -N(R30a)2, -N(R30a)C(O)R30b, -N(R30a)N(R30a)2, -NO2, -C(O)H, -C(O)R30b, -C(O)2R30a, -C(O)N(R30a)2, -OC(O)N(R30a)2, -N(R30a)C(O)2R30a, -N(R30a)C(O)N(R30a2)2, -OC(O)R30b, -S(O)R30b, -S(O)2R30b, -S(O)2N(R30a)2, -N(R30a)S(O)2R30b, -C(R30a)=N(R30a), y -C(R30a)=N(OR30a); R30a en cada caso se selecciona en forma independiente entre H, C1-6aIquilo, carbociclilo, y heterociclilo; R30b en cada caso se selecciona en forma independienteentre C1-6alquilo, C2-6alquenilo, C2-6alquinilo, carbociclilo, y heterociclilo; R40 en cada caso se selecciona en forma independiente entre halo, -CN, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, carbociclilo, heterociclilo, -OR40a, -SR40a, -N(R40a)2,-N(R40a)C(O)R40b, -N(R40a)N(R40b)2, -NO2, -C(O)H, -C(O)R40b, -C(O)2R40a, -C(O)N(R40a)2, -OC(O)N(R40a)2, -N(R40a)C(O)2R40a, -N(R40a)C(O)N(R40a)2, -OC(O)R40b, -S(O)R40b, -S(O)2R40b, -S(O)2N(R40a)2, -N(R40a)S(O)2R40b, -C(R40a)=N(R40a) y -C(R40a)=N(OR40a) R40a en cada caso se selecciona en forma independiente entre H, C1-6aIquilo, carbociclilo, y heterociclilo; y R40b en cada caso se selecciona en forma independiente entre C1-6aIquiIo, C2-6alquenilo, C2-6aIquiniIo, carbociclilo, yheterociclilo.
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