Patent ES-2530519-T3 (ES)
Title: Compuestos macrocíclicos completamente sintéticos, con conformación restringida
Inventor: OBRECHT DANIEL
IPC: C07F7/08
Filed: 2009-08-05
Granted: 2015-03-03
Abstract: Compuestos de fórmula I, que incorporan los bloques componentes A, B y C.**Fórmula** en las que los restos a, b y c de los bloques componentes A, B y C son seleccionados de las tablas 1, 2 y 3, respectivamente, y son apropiadamente sustituidos independientemente, tal como se define a continuación,**Fórmula** en las que los sustituyentes R1 a R17 acoplados directamente a los bloques componentes A, B y C, se definen del modo siguiente: R1: H; F; Cl; Br; I; CF3; OCF3; OCHF2; NO2; CN; alquilo; alquenilo; alquinilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR18R19)qOR20; -(CR18R19)qSR20; -(CR18R19)qNR4R11; -(CR18R19)qOCONR4R11; -(CR18R19)qOCOOR21; -(CR18R19)qNR4COOR21; -(CR18R19)qNR4COR22 ; -(CR18R19)qNR4CONR4R11; -(CR18R19)qNR4SO2R23;-(CR18R19)qNR4SO2NR4R11; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; -(CR18R19)qPO(OR21)2; -(CR18R19)qOPO(OR21)2; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qOSO3R21; -(CR18R19)qR24; -(CR18R19)qR25; o -(CR18R19)qR26; R2:H; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR18R19)qOR20; -(CR18R19)qSR20; -(CR18R19)qNR4R11; -(CR18R19)qOCONR4R11; -(CR18R19)qOCOOR21; -(CR18R19)qNR4COOR21; -(CR18R19)qNR4COR22 ; -(CR18R19)qNR4CONR4R11; -(CR18R19)qNR4SO2R23; -(CR18R19)qNR4SO2NR4R11;-(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; -(CR18R19)qPO(OR21)2; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qR24; -(CR18R19)qR25; o -(CR18R19)qR26; R3: H; CF3; alquilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R4: H; aqluilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R5, R7 y R9 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilaquilo; -(CR18R19)sOR20; -(CR18R19)sSR20; -(CR18R19)sNR4R11; -(CR18R19)sOCONR4R11; -(CR18R19)sOCOOR21; -(CR18R19)sNR4COOR21; -(CR18R19)sNR4COR22 ; -(CR18R19)sNR4CONR4R11; -(CR18R19)sNR4SO2R23; -(CR18R19)sNR4SO2NR4R11; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; -(CR18R19)qPO(OR21)2; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qR24; -(CR18R19)qR25; o -(CR18R19)qR26; R6, R8 y R10 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; o heteroarilaquilo; R11: H; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR18R19)rOR20; -(CR18R19)rSR20; -(CR18R19)rNR4R27; -(CR18R19)rOCONR4R27; -(CR18R19)rOCOOR2; -(CR18R19)rNR4COOR21; -(CR18R19)rNR4CONR4R27; -(CR18R19)rNR4SO2R23; -(CR18R19)rNR4SO2NR4R27; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R27; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qSO2NR4R27; -(CR18R19)qR24; -(CR18R19)sR25; o -(CR18R19)qR26; R12 y R13 se definen independientemente como H; o alquilo; R14 y R16 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilaquilo; -(CR18R19)sOR20; -(CR18R19)sNR4R11; -(CR18R19)sNR4COOR21; -(CR18R19)sNR4COR22 ; -(CR18R19)sNR4CONR4R11; -(CR18R19)sNR4SO2R23; -(CR18R19)sNR4SO2NR4R11; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; o -(CR18R19)qCOR22; R15 y R17 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; o heteroarilalquilo; en el que los sustituyentes R1 a R17 se definen del modo siguiente: R18: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR29R30)sOR31; -(CR29R30)sSR31; -(CR29R30)sNR28R31; -(CR29R30)sOCONR28R31; -(CR29R30)sOCOOR21; -(CR29R30)sNR28COOR21; -(CR29R30)sNR28COR31; -(CR29R30)sNR28CONR28R31; -(CR29R30)sNR28SO2R23; -(CR29R30)sNR28SO2NR28R31; -(CR29R30)qCOOR21; -(CR29R30)qCONR28R31; -(CR29R30)qSO2NR28R31; -(CR29R30)qPO(OR21)2; -(CR29R30)qCOR31; -(CR29R30)qSO2R23; -(CR29R30)qR24; -(CR29R30)qR25; o -(CR29R30)qR26; R19: H; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R20: H; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; heteroarilalquilo; -(CR29R30)rOR31; -(CR29R30)rSR31; -(CR29R30)rNR28R31; -(CR29R30)rOCONR28R31; -(CR29R30)rNR28COOR21; -(CR29R30)rNR28COR31; -(CR29R30)rNR28CONR28R31; -(CR29R30)rNR28SO2R23;-(CR29R30)rNR28SO2NR28R31; -(CR29R30)qCOOR21; -(CR29R30)qCONR28R31; -(CR29R30)qSO2NR28R31; -(CR29R30)qCOR31; -(CR29R30)qSO2R23; -(CR29R30)qR24; -(CR29R30)qR25; o -(CR29R30)qR26; R21: alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R22: alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR29R30)sOR31; -(CR29R30)sSR31; -(CR29R30)sNR28R31; -(CR29R30)sOCONR28R31; -(CR29R30)sNR28COOR21; -(CR29R30)sNR28COR31 ; -(CR29R30)sNR28CONR28R31; -(CR29R30)sNR28SO2R23; -(CR29R30)sNR28SO2NR28R31; -(CR29R30)sCOOR21; -(CR29R30)sCONR28R31; -(CR29R30)sSO2NR28R31; -(CR29R30)tCOR31; -(CR29R30)sSO2R23; -(CR29R30)tR24; -(CR29R30)tR25; o -(CR29R30)tR26; R23: H; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; o bien -(CR32R33)tR24; R24: arilo, o un grupo opcionalmente sustituido del tipo C6H2R34R35R31; o un grupo heteroarilo, uno de los grupos de fórmulas H1-H34, tal como se muestran a continuación en la Tabla 4: