AR053090A1 - Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos - Google Patents

Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos

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AR053090A1
AR053090A1 ARP050102978A ARP050102978A AR053090A1 AR 053090 A1 AR053090 A1 AR 053090A1 AR P050102978 A ARP050102978 A AR P050102978A AR P050102978 A ARP050102978 A AR P050102978A AR 053090 A1 AR053090 A1 AR 053090A1
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Argentina
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alkyl
alkynyl
alkenyl
cycloalkenyl
cycloalkyl
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Osi Pharm Inc
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Abstract

Compuesto de formula 1 y sales aceptables para uso farmacéutico de los mismos. Estos compuestos inhiben la enzima IGF-1R y son utiles para el tratamiento y/o prevencion de varias enfermedades y afecciones, que responden al tratamiento por inhibicion de tirosina quinasas, tales como el cancer Rivindicacion 1: Un compuesto representado por la formula 1 o una sal aceptable para uso farmacéutico del mismo, donde Q1 es arilo 1, heteroarilo1, ciclaolaquilo C3-10, heterocicililo, cicloalquenilo C3-10 o heterocicloalquenilo, cualquiera de los cuales se sustituye opcionalmente por uno a cinco sustituyentes independientes G10, R1 es alquilo C0-10, cicloalquilo C3-10, biciclo-alquilo C5-10, arilo, heteroarilo, aralquilo, heteroaralquilo, heterociclo o heterobiciclo-alquilo C5-10, cualquiera de los cuales se sustituye opcionalmente con uno o más sustituyentes independientes G11; G10 y G11 son cada uno independientemente halo, oxo, -CF3, -OCF3, -OR2, -NR2R3(R2a)j1, -C(O)R2, -CO2R2, -CONR2R3, -NO2, -S(O)j1R2, -SO2NR2R3, -NR2C(=O)R3, -NR2C(=O)NR3R2a, -NR2S(O)j1R3, -C(=S)OR2, -C(=O)SR2, -NR2C(=NR3)NR2aR3a, -NR2C(=NR3)OR2a, , NR2C(=NR3)SR2a, -OC(=O)OR2, -OC(=O)NR2R3, -OC(=O)OR2, -CO(=O)NR2R3, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquitio C1-10-alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10-alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10. cicloalquenil C3-8-alquenilo C2-10, cicloalquil C3-8-alquinilo C2-10, cicloalquenil C3-8-alquinilo C2-10, heterociclil-alquilo C0-10, heterociclil-alquenilo C2-10 o heterociclil-alquinilo C2-10, cualquiera de los cuales se sustituy opcionalmente con uno o mássustituyentes independientes halo, oxo, -CF3, -OCF3, -OR222, -NR222R333(R222a)j1a, -C(O)R222, -CO2R222, - CONR222R333, -NO2, -CN, S-(O)j1aR222, -SO2NR222R333, -NR222C(=O)R333, -NR222C(=O)OR333, -R222C(=O)NR333R222a, -NR222S(O)j1aR333, -C(=S)OR222, -C(=O)SR222, -NR222C(=NR333)NR222R333a, -NR222C(=NR333)OR222a, -NR222C(=NR333)SR222a, -OC(=O)OR222, - OC(=)NR222R333, -OC(=O)OR222, -OC(=O)NR222R333, -OC(=O)SR222, -SC(=O)OR222 o -SC(=O)NR222R333; o G10 es opcionalmente -(X1)n-(Y1)m-R4; O G41 es opcionalmente -(X1)n-(Y1)m-alquilo C0-10; o G10 y G41 son cada uno opcionalmente de manera independiente arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10 o hetarilalquinilo C2-10, cualquiera de los cuales se sustituye opcionalmente con uno o más sustituyentes independientes halo,-CF3, -OCF3, - OR222, -NR222R333(R222a)j1a, -C(O)R222, -CO2R222, -CONR222R333, -NO2, -CN, S-(O)j1aR222, -SO2NR222R333, -NR222C(=O)R333, -NR222C(=O)OR333, -R222C(=O)NR333R222a, -NR222S(O)j1aR333, -C(=S)OR222, -C(=O)SR222, -NR222C(=NR333)NR222R333a, - NR222C(=NR333)OR222a, -NR222C(=NR333)SR222a, -OC(=O)OR222, -OC(=)NR222R333, -OC(=O)OR222, -OC(=O)NR222R333, -OC(=O)SR222, -SC(=O)OR222 o -SC(=O)NR222R333; G11 es halo, oxo, -CF3, -OCF3, -OR21, -NR21R31(R21a)j3, -C(O)R21, -CO2R21, .CONR21R31, -NO2, - CN, -S(O)j3R21, -SO2NR21R31, -NR21C(=O)R31, -NR21C(=O)OR31, -NR21C(=O)NR31R21a, -NR21S(O)j3R31, -C(=S)OR21, -C(=S)OR21, -C(=O)SR21, -NR21C(=NR31)NR21aR31a, -NR21C(=NR31)OR21a, -NR21C(=NR31)SR21a, OC(=O)OR21, -OC(=O)NR21R31, -OC(=O)SR21, - SC(=O)OR21, -SC(=O)NR21R31, -P(O)OR21OR31, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10, alquiltio C1-10-alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10- alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C3-8-alquenilo C2-10, cicloalquenil C3-8-alquenilo C2-10, cicloalquil C3-8-alquinilo C2-10, cicloalquenil C3-8-alquinilo C2-10, heterociclil-alquilo C0-10, heterociclil-alquenilo C2-10 o heterociclil-alquinilo C2-10, cualquiera de los cuales se sustituye opcionalmente con uno o más sustituyentes independientes halo, oxo, -CF3, -OCF3, - OR2221, -NR2221R3331(R2221a)j3a, -C(O)R2221, -CO2R2221, -CONR2221R3331, NO2, -CN, -S(O)j3aR2221, SO2NR2221R3331, -NR2221C(=O)R3331, -NR2221C(=O)OR3331, -NR2221C(=O)NR3331R2221a, -NR2221S(O)j3aR3331, -C(=S)OR2221, -C(=O)SR2221, - NR2221C(=NR3331)NR2221aR3331a, -NR2221C(=NR3331)OR2221a, -NR2221C(=NR3331)SR2221a, -OC(=O)OR2221, -OC(=O)NR2221R3331, -OC(=O)SR2221, -SC(=O)OR2221, -P(O)OR2221OR3331 o -SC(=O)NR2221R3331; o G11 es arilalquilo C0-10, arilalquenilo C2-10, o G11 es arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10 o hetarilalquinilo C2-10, cualquiera de los cuales se sustituye opcionalmente con uno o más hetarilalquinilo C2-10, cualquiera de los cuales se sustituye opcionalmente con uno o más sustituyentes independientes halo, -CF3, -OCF3, -OR2221, -NR2221R3331(R2221a)j3a, -C(O)R2221, -CO2R2221, -CONR2221R3331, -NO2, -CN, -S(O)j3aR2221, -SO2NR2221R3331, -NR2221C(=O)R3331, -NR2221C(=O)OR3331, - NR2221C(=O)NR3331R2221a, -NR2221S(O)j3aR3331, -C(=S)OR2221, -C(=O)SR2221, -NR2221C(=NR3331)NR2221aR3331a, -NR2221C(=NR3331)OR2221a, -NR2221C(=NR3331)SR2221a, -OC(=O)OR2221, -OC(=O)NR2221R3331, -OC(=O)SR2221, -SC(=O)OR2221, -P(O)OR2221OR3331 o - SC(=O)NR2221R3331; o G11 es C, tomado junto con el carbono al cual se encuentra unido forma un doble enlace C=C que se sustituye con R5 y G12, R2, R2a, R3, R3a, R222, Rrrr1, R333, R333a, R21, R21a, R31, R31a, R2221, R2221a, R3331 y R3331a son cada uno independientemente alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alquilo C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquiltio C1-10-alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10- alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10, cicloalquenil C3-8-alquenilo C2-10, cicloalquil C3-8-alquinilo C2-10, cicloalquenil C3-8- alquinilo C2-10, heterociclil-alquilo C0-10, heterociclil-alquenilo C2-10, heterociclil-alquinilo C2-10, arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquenilo C2-10 o hetarialquinilo C2-10, cualquiera de los cuales se sustituye opcionalmente con uno o más sustituyentes independientes G13 o en el caso de -NR2R3(R2a)j1 o -NR21R31(R21a)j3 o -NR222R333(R222a)j1a o -NR222R333(R222a)j2a o -NR2221R3331(R2221a)j3a, R2 y R3 o R21 y R31 o R222 y R333 o R2221 y R3331, respectivamente, se toman opcionalmente junto con el átomo de nitrogeno al cual se encuentran unidos para formar un anillo saturado o no saturado de 3-10 miembros, donde dicho anillo se sustituye opcionalmente con uno o más sustituyentes independientes G14 y donde dicho anillo incluye opcionalmente uno o más heteroátomos independientes distintos de nitrogeno a los cuales R2 y R3 o R222 y R333 o R2221 y R3331 se encuentran unidos; X1 e Y1 son cada uno independientemente -O-, -NR7-, - S(O)j4-, -CR5R6-, -N(C(O)OR7), -N(C(O)R7)-, -N(SO2R7)-, -CH2O-, -CH2S-, -CH2H(R7)-, -CH(NR7)-, -CH2N(C(O)R7)-, -CH2N(C(O)OR7)-, -CH2N(SO2R7)-, -CH(NHR7)-, -CH(NHC(O)R7)-, -CH(NHSO2R7)-, -CH(NHC(O)OR7)-, -CH(OC(O)R7-, -CH(OC(O)NHR7)-, -CH=CH-, -C:::C- , -C(=NOR7)-, -C(O)-, -CH(OR7)-, -C(O)N(R7)-, -N(R7)C(O)-, -N(R7)S(O)-, -N(R7)S(O)2-OC(O)N(R7)-, -N(R7)C(O)N(R8)-, -NR7C(O)-O-, -S(O)N(R7)-, -S(O)2N(R7)-, -N(C(O)R7S(O)-, -N(C(O)R7)S(O)2-, -N(R7)S(O)N(R8)-, -N(R7)S(O)2N(R8)-, -C(O)N(R7)C(O)-, - S(O)N(R7)C(O)-, -S(O)2N(R7)C(O)-, -OS(O)N(R7)-, -OS(O)2N(R7)-, -N(R7)S(O)-O-, -N(R7)S(O)2-O-, -N(R7)S(O)C(O)-, -N(R7)S(O)2C(O)-, -SON(C(O)R7)-, -SO2N(C(O)R7)-, -N(R7)SON(R8)-, -(R7)SO2N(R8)-, -N(R7)SO2N(R8)-, -C(O)-O-, N(R7)P(OR8)-O-, -N(R7)P(OR8)- , -N(R7)P(O)(OR8)-O-, -N(R7)P(O)(OR8)-, N(C(O)R7)P(OR8)-O-, -N(C(O)R7)P(OR8)-, -N(C(O)R7)P(O)(OR8)-O-, -N(C(O)R7)P(OR8)-, -CH(R7)S(O)-, -CH(R7)S(O)2, --CH(R7)N(C(O)OR8)-, -CH(R7)N(C(O)R8)-, -CH(R7)N(SO2R8)-, -CH(R7)-O-. --CH(R7)S-, CH(R7)N(R8)-, - CH(R7)N(C(O)R8)-, -CH(R7)N(C(O)OR8)-, -CH(R7)N(SO2R8)-, -CH(R7)C(=NOR8)-, -CH(R7)C(O)-, -CH(R7)CH(OR8)-, -CH(R7)C(O)N(R8)-, -CH(R7)N(R8)C(O)-, -CH(R7)N(R8)S(O)-, -CH(R7)N(R8)S(O)2-, -CH(R7)OC(O)N(R8)-, -CH(R7)N(R8)C(O)N(R7a)-, -CH(R7)NR8C(O)-O-, - CH(R7)S(O)N(R8)-, -CH(R7)S(O)2N(R8)-, -CH(R7)N(C(O)R8)S(O)-, -CH(R7)N(C(O)R8)S(O)-, -CH(R7)N(R8)S(O)N(R7a)-, -CH(R7)N(R8)S(O)2N(R7a)-, -CH(R7)C(O)N(R8)C(O)-, -CH(R7)S(O)N(R8)C(O)-, -CH(R7)S(O)2N(R8)C(O)-, -CH(R7)OS(O)N(R8)-, -CH(R7)OS(O)2N(R8)-, - CH(R7)N(R8)S(O)-O-, -CH(R7)N(R8)S(O)2-O-, -CH)R7)N(R8)S(O)C(O)-, -CH(R7)N(R8)S(O)2C(O)-, -CH(R7)SON(C(O)R8)-, -CH(R7)SO2N(C(O)R8)-, -CH(R7)N(R8)SON(R7a)-, -CH(R7)N(R8)SO2N(R7Aa)-, -CH(R7)C(O)-O-, -CH(R7)N(R8)P(OR7a)-O-, -CH(R7)N(R8)P(OR7a)-, - CH(R7)N(R8)P(O)(OR7a)-O-, -CH(R7)N(R8)P(O)(OR7a)-, -CH(R7)N(C(O)R8)P(OR7a)-O-, -CH(R7)N(O)R8)P(OR7a)-, -CH(R7)N(C(O)R8)P(O)OR7a)-O- o -CH(R7)N(C(O)R8)P(OR7a)-; o X1 e Y1 se representan cada uno independientemente por una de las siguientes formulas estructurales: 1, 2, 3, 4, 5 0 6, R10 tomado junto con la fosfinamida o fosfonamida, forman un sistema anular arilo, heteroarilo o heterociclilo de 5, 6 o 7 miembros; R5, R6, G12, G13, G14 y G15 son cada uno independientemente alquilo C0- 10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquiltio C1-10-alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10-alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10, cicloalquenil C3-8-alquenilo C2-10, cicloalquil C3-8-alquinilo C2-10, cicloalquenil C3-8-alquinilo C2-10, hererociclil-alquilo C0-10, heterociclil-alquenilo C2-10, heterociclil-alquinilo C2-10, aralquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10 o hetarilalquenilo C2-10 o hetarilalquinilo C2-10, cualquiera de
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US20060019957A1 (en) 2006-01-26
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JP2008507546A (ja) 2008-03-13
MY139689A (en) 2009-10-30
IL180806A0 (en) 2007-06-03
NO20070917L (no) 2007-03-19
RU2007106068A (ru) 2008-08-27
EA200700220A1 (ru) 2007-08-31
CA2574594A1 (en) 2006-02-02
BRPI0513565A (pt) 2008-05-06
JP4918038B2 (ja) 2012-04-18
KR20070035087A (ko) 2007-03-29
MX2007000822A (es) 2007-04-02
CN101084218A (zh) 2007-12-05
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AP2007003924A0 (en) 2007-02-28
US7741324B2 (en) 2010-06-22

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