AR046337A1 - Imidazopirazina inhibidoras de las tirosinquinasas - Google Patents

Imidazopirazina inhibidoras de las tirosinquinasas

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Publication number
AR046337A1
AR046337A1 ARP040103731A ARP040103731A AR046337A1 AR 046337 A1 AR046337 A1 AR 046337A1 AR P040103731 A ARP040103731 A AR P040103731A AR P040103731 A ARP040103731 A AR P040103731A AR 046337 A1 AR046337 A1 AR 046337A1
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Argentina
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alkyl
alkynyl
alkenyl
cycloalkenyl
nr222r333
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ARP040103731A
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Osi Pharm Inc
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Publication of AR046337A1 publication Critical patent/AR046337A1/es

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Abstract

Inhiben la enzima IGF-1R y son útiles para el tratamiento y/o la prevención de diferentes enfermedades y afecciones que responden al tratamiento por inhibición de tirosinquinasas. Reivindicación 1: Un compuesto representado por la fórmula (1), o una sal del mismo aceptable para uso farmacéutico, en la cual Q1 es arilo1, heteroarilo1, cicloalquilo, heterociclilo, cicloalquenilo, o heterocicloalquenilo, cualquiera de los cuales está substituido opcionalmente con entre uno y cinco substituyentes G1 independientes; R1 es alquilo, cicloalquilo, bicicloalquilo, arilo, heteroarilo, aralquilo, heteroaralquilo, heterociclilo, o heterobicicloalquilo, cualquiera de los cuales está substituido opcionalmente con uno o más substituyentes G11 independientes; G1 y G41 son independientemente halo, oxo, -CF3, -OCF3, -OR2, -NR2R3(R3a)j1, -C(O)R2, -CO2R, -CONRaR3, -NO2, -CN, -S(O)j1R2, -SO2NR2R3, NR2(C=O)R3, NR2(C=O)OR3, NR2(C=O)NR2R3, NR2S(O)j1R3, -(C=S)OR2, -(C=O)SR2, - NR2(C=NR3)NR2aR3a, -NR2(C=NR3)OR2a, -NR2(C=NR3)SR3a, -O(C=O)OR2, -O(C=O)NR2R3, -O(C=O)SR2, -S(C=O)OR2, -S(C=O)NR2R3, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10alquilo C1-10, alcoxi C1-10alquenilo C2-10, alcoxi C1-10alquinilo C2- 10, alquiltio C1-10alquilo C1-10, alquiltio C1-10alquenilo C2-10, alquiltio C1-10alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8alquilo C1-10, cicloalquenil C3-8alquilo C1-10, cicloalquil C3-8alquenilo C1-10, cicloalquenil C3-8alquenilo C2-10, cicloalquil C3-8alquinilo C2-10, cicloalquenil C3-8alquinilo C2-10, heterociclil-alquilo C0-10,heterociclil-alquenilo C2-10, o heterociclil-alquinilo C2-10, cualquiera de los cuales está substituido opcionalmente con uno o más substituyentes independientes halo, oxo, -CF3, -OCF3, -OR222, -NR222R333(R333a)j1a, -C(O)R222, -CO2R222, -CONR222R333, -NO2, -CN, -S(O)j1aR222, -SO2NR222R333, NR222(C=O)R333, NR222(C=O)OR333, NR222(C=O)NR222R333, NR222S(O)j1aR333, -(C=S)OR222, - (C=O)R222, -NR222(C=NR333)NR222aR333a, -NR222(C=NR333)OR222a, -NR222(C=NR333)SR333a, -O(C=O)OR222, -O(C=O)NR222R333, -O(C=O)SR222, -S(C=O)OR222, o -S(C=O)NR222R333; o -(X1)n-(Y1)m-R4; o aril-alquilo C0-10, aril-alquenilo C2-10, o aril-alquinilo C2- 10, cualquiera de los cuales está substituido opcionalmente con uno o más substituyentes independientes, -CF3, -OCF3, -OR222, -NR222R333(R333a)j2a, -C(O)R222, -CO2R222, -CONR222R333, -NO2, -CN, -S(O)j2aR222, -SO2NR222R333, NR222(C=O)R333, NR222(C=O)OR333, NR222(C=O)NR222R333, NR222S(O)j2aR333, -(C=S)OR222, -(C=O)SR222, -NR222(C=NR333)NR222aR333a, -NR222(C=NR333)OR222a, -NR222(C=NR333)SR333a, -O(C=O)OR222, -O(C=O)NR222R333, -O(C=O)SR222, -S(C=O)OR222, o -S(C=O)NR222R333; o hetaril- alquilo C0-10, hetaril-alquenilo C2-10, o hetaril-alquinilo C2-10, cualquiera de los cuales está substituido opcionalmente con uno o más substituyentes independientes halo, -CF3, -OCF3, -OR222, -NR222R333(R333a)j3a, -C(O)R222, -CO2R222, - CONR222R333, -NO2, -CN, -S(O)j3aR222, -SO2NR222R333, NR222(C=O)R333, NR222(C=O)OR333, NR222(C=O)NR222R333, NR222S(O)j3aR333, -(C=S)OR222, -(C=O)SR222, -NR222(C=NR333)NR222aR333a, -NR222(C=NR333)OR222a, -NR222(C=NR333)SR333a, -O(C=O)OR222, - O(C=O)NR222R333, -O(C=O)SR222, -S(C=O)OR222, o -S(C=O)NR222R333; G11 es halo, oxo, -CF3, -OCF3, -OR21, -NR21R31(R3a1)j4, -C(O)R21, -CO2R21, -CONR21R31, -NO2, -CN, -S(O)j4R21, -SO2NR21R31, NR21(C=O)R31, NR21(C=O)OR31, NR21(C=O)NR21R31, NR21S(O)j4R31, -(C=S)OR21, -(C=O)SR21, -NR21(C=NR31)NR2a1R3a1, -NR21(C=NR31)OR2a1, -NR21(C=NR31)SR3a1, -O(C=O)OR21, -O(C=O)NR21R31, -O(C=O)SR21, -S(C=O)OR21, -S(C=O)NR21R31, -P(O)OR21OR31, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10alquilo C1-10, alcoxi C1-10alquenilo C2-10, alcoxi C1-10alquinilo C2-10, alquiltio C1-10alquilo C1-10, alquiltio C1-10alquenilo C2-10, alquiltio C1-10alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8alquilo C1-10, cicloalquenil C3-8alquilo C1-10, cicloalquil C3-8alquenilo C2-10, cicloalquenil C3-8alquenilo C2-10, cicloalquil C3-8alquinilo C2-10, cicloalquenil C3-8alquinilo C2-10, heterociclil-alquilo C0-10, heterociclil-alquenilo C2-10, o heterociclil-alquinilo C2-10, cualquiera de los cuales está substituido opcionalmente con uno o más substituyentes independientes halo, oxo, -CF3, -OCF3, -OR2221, -NR2221R3331(R333a1)j4a, -C(O)R2221, -CO2R2221, -CONR2221R3331, -NO2, -CN, -S(O)j4aR2221, -SO2NR2221R3331, NR2221(C=O)R3331, NR2221(C=O)OR3331, NR2221(C=O)NR2221R3331, NR2221S(O)j4aR3331, -(C=S)OR2221, -(C=O)SR2221, -NR2221(C=NR3331)NR222a1R333a1, -NR2221(C=NR3331)OR222a1, -NR2221(C=NR3331)SR333a1, -O(C=O)OR2221, -O(C=O)NR2221R3331, -O(C=O)SR2221, -S(C=O)OR2221, - P(O)OR2221OR3331, o -S(C=O)NR2221R3331; o aril-alquilo C0-10, aril-alquenilo C2-10, o aril-alquinilo C2-10, cualquiera de los cuales está substituido opcionalmente con uno o más substituyentes independientes halo, -CF3, -OCF3, -OR2221, - NR2221R3331(R333a1)j5a, -C(O)R2221, -CO2R2221, -CONR2221R3331, -NO2, -CN, -S(O)j5aR2221, -SO2NR2221R3331, NR2221(C=O)R3331, NR2221(C=O)OR3331, NR2221(C=O)NR2221R3331, NR2221S(O)j5aR3331, -(C=S)OR2221, -(C=O)SR2221, -NR2221(C=NR3331)NR222a1R333a1, - NR2221(C=NR3331)OR222a1, -NR2221(C=NR3331)SR333a1, -O(C=O)OR2221, -O(C=O)NR2221R3331, -O(C=O)SR2221, -S(C=O)OR2221, -P(O)OR2221OR3331, o -S(C=O)NR2221R3331; o hetaril-alquilo C0-10, hetaril-alquenilo C2-10, o hetaril-alquinilo C2-10, cualquiera de los cuales está substituido opcionalmente con uno o más independientes halo, -CF3, -OCF3, -OR2221, -NR2221R3331(R333a1)j6a, -C(O)R2221, -CO2R2221, -CONR2221R3331, -NO2, -CN, -S(O)j6aR2221, -SO2NR2221R3331, NR2221(C=O)R3331, NR2221(C=O)OR3331, NR2221(C=O)NR2221R3331, NR2221S(O)j6aR3331, -(C=S)OR2221, -(C=O)SR2221, -NR2221(C=NR3331)NR222a1R333a1, -NR2221(C=NR3331)OR222a1, -NR2221(C=NR3331)SR333a1, -O(C=O)OR2221, -O(C=O)NR2221R3331, -O(C=O)SR2221, -S(C=O)OR2221, -P(O)OR2221OR3331, o - S(C=O)NR2221R3331; o G11 se toma junto con el carbono al cual está unido para formar una unión doble que está substituida con R5 y G111; R2, R2a, R3, R3a, R222, R222a, R333, R333a, R21, R2a1, R31, R3a1, R2221, R222a1, R3331, y R333a1 son cada uno independientemente igual a alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10alquilo C1-10, alcoxi C1-10alquenilo C2-10, alcoxi C1-10alquinilo C2-10, alquiltio C1-10alquilo C1-10, alquiltio C1-10alquenilo C2-10, alquiltio C1-10alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8alquilo C1-10, cicloalquenil C3-8alquilo C1-10, cicloalquil C3-8alquenilo C2-10, cicloalquenil C3-8alquenilo C2-10, cicloalquil C3-8alquinilo C2-10, cicloalquenil C3-8alquinilo C2-10, heterociclil-alquilo C0-10, heterociclil-alquenilo C2-10, o heterociclil-alquinilo C2-10, cualquiera de los cuales está opcionalmente substituido con uno o más substituyentes G111; o aril-alquilo C0-10, aril-alquenilo C2-10, o aril-alquinilo C2-10, hetaril-alquilo C0-10, hetaril-alquenilo C2-10, o hetaril-alquinilo C2-10, cada uno de los cuales está substituido opcionalmente con uno o más substituyentes G111; o en el caso de -NR2R3(R3a)j1 o -NR222R333(R333a)j1a o -NR222R333(R333a)j2a o - NR2221R3331(R333a1)j3a o -NR2221R3331(R333a1)j4a o -NR2221R3331(R333a1)j5a o -NR2221R3331(R333a1)j6a, R2 y R3 o R222 y R333 o R2221 y R3331 tomados junto con el nitrógeno al cual están unidos forman un anillo de 3-10 miembros cíclico saturado, cíclico no saturado, cíclico saturado heterocíclico, o cíclico no saturado heterocíclico, en donde dicho anillo está opcionalmente substituido con uno o más substituyentes G111; X1 e Y1 son, cada uno independientemente -O-, -NR7-, -S(O)J7-, -CR5R6-, -N(C(O)OR7)-, -N(C(O)R7)-, -N(SO2R7)-, -CH2O-, -CH2S-, -CH2N(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-, -CsC-, -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(R7)-, -NR7C(O)O-, -S(O)N(R7)-, -S(O)2N(R7)-, -N(C(O)R7)S(O)-, -N(C(O)R7)S(O)2-, -N(R7)S(O)N(R7)-, -N(R7)S(O)2N(R7)-, -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)2O-, -N(R7)S(O)C(O), -N(R7)S(O)2C(O)-, -SON(C(O)R7)-, -SO2N(C(O)R7)-, -N(R7)SON(R7)-, -N(R7)SO2N(R7)-, -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)OR7)-, -CH(R7)N(C(O)R7)-, -CH(R7)N(SO2R7), -CH(R7)O-, -CH(R7)S-, -CH(R7)N(R7)-, -CH(R7)N(C(O)R7)-, -CH(R7)N(C(O)OR7)-, - CH(R7)N(SO2R7)-, -CH(R7)C(=NOR7)-, -CH(R7)C(O)-, -CH(R7)CH(OR7)-, -CH(R7)C(O)N(R7)-, -CH(R7)N(R7)C(O)-, -CH(R7)N(R7)S(O)-, -CH(R7)N(R7)S(O)2-, -CH(R7)OC(O)N(R7)-, -CH(R7)N(R7)C(O)N(R7)-, -CH(R7)NR7C(O)O-, -CH(R7)S(O)N(R7)-, -CH(R7)S(O)2N(R7)-, - CH(R7)N(C(O)R7)S(O)-, -CH(R7)N(C(O)R7)S(O)-, -CH(R7)N(R7)S(O)N(R7)-, -CH(R7)N(R7)S(O)2N(R7)-, -CH(R7)C(O)N(R7)C(O)-, -CH(R7)S(O)N(R7)C(O)-, -CH(R7)S(O)2N(R7)C(O)-, -CH(R7)OS(O)N(R7)-, -CH(R7)OS(O)2N(R7)-, -CH(R7)N(R7)S(O)O-, -CH(R7)N(R7)S(O)2O-, - CH(R7)N(R7)S(O)C(O)-, -CH(R7)N(R7)S(O)2C(O)-, -CH(R7)SON(C(O)R7)-, -CH(R7)SO2N(C(O)R7)-, -CH(R7)N(R7)SON(R7)-, -CH(R7)N(R7)SO2N(R7)-, -CH(R7)C(O)O-, -CH(R7)N(R7)P(OR8)O-, -CH(R7)N(R7)P(OR8)-, -CH(R7)N(R7)P(O)(OR8)O-, -CH(R7)N(R7)P(O)(OR8)-, - CH(R7)N(C(O)R7)P(OR8)O-, -CH(R7)N(C(O)R7)P(OR8)-, -CH(R7)N(C(O)R7)P(O)(OR8)O-, o -CH(R7)N(C(O)R7)P(OR8)-; o X1 y Y1 cada uno está representado por una de las fórmulas estructurales (2), (3), (4), (5), (6) ó (7); R10, tomado junto con la fosfinamida o fosfonamida, es un sistema anular arilo, heteroarilo o heterociclilo de 5, 6 o 7 miembros; R5, R6 y G111 son, cada uno independientemente alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10alquilo C1-10, alcoxi C1-10alquenilo C2-10, alcoxi C1-10alquinilo C2-10, alquiltio C1-10alquilo C1-10, alquiltio C1-10alquenilo C2-10, alquiltio C1-10alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalq
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