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ES2328833T3 - Inhibidores de proteina quinasa heterobiciclicos con anillo 6,6-biciclico. - Google Patents

Inhibidores de proteina quinasa heterobiciclicos con anillo 6,6-biciclico. Download PDF

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ES2328833T3
ES2328833T3 ES05742128T ES05742128T ES2328833T3 ES 2328833 T3 ES2328833 T3 ES 2328833T3 ES 05742128 T ES05742128 T ES 05742128T ES 05742128 T ES05742128 T ES 05742128T ES 2328833 T3 ES2328833 T3 ES 2328833T3
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cycloalkenyl
alkynyl
cycloalkyl
nr222c
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Lee D. Arnold
Cara Cesario
Heather Coate
Andrew Philip Crew
Hanqing Dong
Kenneth Foreman
Ayako Honda
Radoslaw Laufer
An-Hu Li
Kristen Michelle Mulvihill
Mark Joseph Mulvihill
Anthony Nigro
Bijoy Panicker
Arno G. Steinig
Yingchuan Sun
Qinghua Weng
Douglas S. Werner
Michael J. Wyle
Tao Zhang
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OSI Pharmaceuticals LLC
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Abstract

Un compuesto representado por la Fórmula I: **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo, en el que: X1 es C-E1; X2 es N o C-E1; Q1 es **(Ver fórmula)** en el que X11, X12, y X13 son cada uno C-E11; y uno cualquiera o dos de X14, X15, y X16 son N y los otros son CE11; R1 es alquilo C0-10, cicloalquilo C3-10, bicicloalquilo C5-10, arilo, heteroarilo, aralquilo, heteroaralquilo, heterociclilo, heterobicicloalquilo C5-10, espiroalquilo, o heteroespiroalquilo, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes G11 independientes; E1, E11, G1, y G41 son cada uno independientemente halo, -CF3, -OCF3, -OR2, -NR2R3(R2a)j1, -C(=O)R2, -CO2R2, -CONR2R3, -NO2, -CN, -S(O)j1R2, -SO2NR2R3, -NR2C(=O)R3, -NR2C(=O)OR3, -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)SR2, -SC(=O)OR2, -SC(=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, alquil C1-10-tioalquilo C1-10, alquil C1-10-tioalquenilo C2-10, alquil C1-10-tioalquinilo 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, heterociclilalquilo C0-10, heterociclilalquenilo C2-10, o heterociclilalquinilo C2-10, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes halo, oxo, -CF3, -OCF3, -OR222, -NR222R333(R222a)j1a, -C(=O)R222, -CO2R222, -C(=O)NR222R333, -NO2, -CN, -S(=O)j1aR222, -SO2NR222R333, -NR222C(=O) R333, NR222C(=O)OR333, -NR222C(=O)NR333R222a, -NR222S(O)j1aR333, -C(=S)OR222, -C(=O)SR222, -NR222C(=NR333) NR222aR333a, -NR222C(=NR333)OR222a, -NR222C(=NR333)SR222a, -OC(=O)OR222, -OC(=O)NR222R333, -OC(=O)SR222, -SC(=O)OR222, o -SC(=O)NR222R333 independientes; o E1, E11, o G1 opcionalmente es -(W1)n-(Y1)m-R4; o E1, E11, G1, o G41 opcionalmente de forma independiente es arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10, o hetaril-alquinilo C2-10, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes halo, -CF3, -OCF3, -OR222, -NR222R333(R222a)j2a, -C(O)R222, -CO2R222, -C(=O)NR222R333, -NO2, -CN, -S(O)j2aR222, -SO2NR222R333, -NR222C(=O)R333, -NR222C(=O)OR333, -NR222C(=O) NR333R222a, -NR222S(O)j2aR333, -C(=S)OR222, -C(=O)SR222, -NR222C(=NR333)NR222aR333a, -NR222C(=NR333)OR222a, -NR222C(=NR333)SR222a, -OC(=O)OR222, -OC(=O)NR222R333, -OC(=O)SR222, -SC(=O)OR222, o -SC(=O)NR222R333 independientes; G11 es halo, oxo, -CF3, -OCF3, -OR21, NR21R31(R2a1)j4, -C(O)R21, -CO2R21, -C(=O)NR21R31, -NO2, -CN, -S(O)j4 R21, -SO2NR21R31, NR21(C=O)R31, NR21C(=O)OR31, NR21C(=O)NR31R2a1, NR21S(O)j4R31, -C(=S)OR21, -C(=O)SR21, -NR21C(=NR31)NR2a1R3a1, -NR21C(=NR31)OR2a1, -NR21C(=NR31)SR2a1, -OC(=O)OR21, -OC(=O)NR21R31, -OC(=O) SR21, -SC(=O)OR21, -SC(=O)NR21R31, -P(O)OR21OR31; alquilideno C1-10, 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, alquil C1-10-tioalquilo C1-10, alquil C1-10-tioalquenilo C2-10, alquil C1-10-tioalquinilo 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, heterociclilalquilo C0-10, heterociclilalquenilo C2-10, o heterociclilalquinilo C2-10, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes halo, oxo, -CF3, -OCF3, -OR2221, -NR2221R3331(R222a1)j4a, -C(O)R2221, -CO2R2221, -C(=O)NR2221R3331, -NO2, -CN, -S (O)j4aR2221, -SO2NR2221R3331, NR2221C(=O)R3331, -NR2221C(=O)OR3331, -NR2221C(-O)NR3331R222a1, -NR2221S(O)j4aR3331, -C(=S)OR2221, -C(=O)SR2221, -NR2221C(=NR3331)NR222a1R333a1, -NR222C(=NR3331)OR222a1, -NR221C(=NR3331)SR222a1, -OC(=O)OR2221, -OC(=O)NR222R3331, -OC(=O)SR2221, -SC(=O)OR2221, -P(O)OR2221OR3331, o -SC(=O)NR2221R3331 independientes; 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 está opcionalmente sustituido con uno o más sustituyentes halo, -CF3, -OCF3, -OR2221, -NR2221R3331(R222a1)j5a, -C(O)R2221, -CO2R2221, -C(=O)NR2221R3331, -NO2, -CN, -S(O)j5a R2221, -SO2NR2221R3331, -NR2221C(=O)R3331, -NR2221C(=O)OR3331, -NR2221C(=O)NR3331R222a1, -NR2221S(O)j5aR3331, -C(=S)OR2221, -C(=O)SR2221, -NR2221C(=NR3331)NR222a1R333a1, -NR2221C(=NR3331)OR222a1, -NR2221C(=NR3331)SR222a1, -OC(=O)OR2221, -OC(=O)NR2221R3331, -OC(=O)SR2221, -SC(=O)OR2221, -P(O)OR2221OR3331, o -SC(=O)NR2222R3331 independientes; o G11 es C, que tomado junto con el carbono al que está unido forma un doble enlace C=C que está sustituido 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 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, alquil C1-10-tioalquilo C1-10, alquil C1-10-tioalquenilo C2-10, alquil C1-10-tioalquinilo 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, heterociclilalquilo C0-10, heterociclilalquenilo C2-10, heterociclilalquinilo C2-10, arilalquilo C0-10, arilalquenilo C2-10, o arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10, o hetarilalquinilo C2-10, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes G111 independientes; o en el caso de -NR2R3(R2a)j1 o -NR222R333(R222a)j1a o -NR222R333(R222a)j2a o -NR21R31(R2a1)j4 o -NR2221R3331 (R222a1) j4a o -NR2221R3331(R222a1)j5a, entonces R2 y R3, o R222 y R333, o R2221 y R3331, respectivamente, se toman opcionalmente junto con el átomo de nitrógeno al que están unidos para formar un anillo saturado o insaturado de 3-10 miembros, en los que dicho anillo está opcionalmente sustituido con uno o más sustituyentes G1111 independientes y en los que dicho anillo opcionalmente incluye uno o más heteroátomos diferentes al nitrógeno al que están unidos R2 y R3, o R222 y R333, o R2221 y R3331; W1 e Y1 son cada uno independientemente -O-, -NR7-, -S(O)j7-, -CR5R6-, -N(C(O)OR7)-, -N(C(O)R7)-, -N(SO2 R7)-, -(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-, -CC-, -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)R7)S(O)-, -N(C(O)R7S(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)2O-, -N(R7)S(O)C(O)-, -N(R7)S(O)2C(O)-, -SON(C(O)R7)-, -SO2N(C(O)R7)-, -N(R7)SON(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)2O-, -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(R7a)-, -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 (C(O)R8)p(OR7a)-, -CH(R7)N(C(O)R8)P(O)(OR7a)O-, o -CH(R7)N(C(O)R8)P(OR7a)-; R5, R6, G111, y G1111 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, alquil C1-10-tioalquilo C1-10, alquil C1-10-tioalquenilo C2-10, alquil C1-10-tioalquinilo 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, heterociclilalquilo C0-10, heterociclilalquenilo C2-10, heterociclilalquinilo C2-10, arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalqueni- lo C2-10, o hetarilalquinilo C2-10, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes halo, -CF3, -OCF3, -OR77, -NR77R87, -C(O)R77, -CO2R77, -CONR77R87, -NO2, -CN, -S(O)j5aR77, -SO2NR77R87, -NR77C(=O)R87, -NR77C(=O)OR87, -NR77C(=O)NR78R87, -NR77S(O)j5aR87, -C(=S)OR77, -C(=O)SR77, NR77C(=NR87) NR78R88, -N77C(=NR87)OR78, -NR77C(=NR87)SR78, -OC(=O)OR77, -OC(=O)NR77R87, -OC(=O)SR77, -SC(=O)OR77, -P(O)OR77OR87, o -SC(=O)NR77R87 independientes; o R5 con R6 se toman opcionalmente junto con el átomo de carbono al que están unidos para formar un anillo saturado o insaturado de 3-10 miembros, en los que dicho anillo está opcionalmente sustituido con uno o más sustituyentes R69 independientes y en los que dicho anillo opcionalmente incluye uno o más heter
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