ES2649156T3 - Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim - Google Patents

Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim Download PDF

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ES2649156T3
ES2649156T3 ES14702167T ES14702167T ES2649156T3 ES 2649156 T3 ES2649156 T3 ES 2649156T3 ES 14702167 T ES14702167 T ES 14702167T ES 14702167 T ES14702167 T ES 14702167T ES 2649156 T3 ES2649156 T3 ES 2649156T3
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Yun-Long Li
David M. Burns
Hao Feng
Chu-Biao Xue
Anlai Wang
Jun Pan
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Incyte Holdings Corp
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Abstract

Un compuesto de fórmula (I):**Fórmula** o una sal farmacéuticamente aceptable del mismo, en donde: Cy es C3-7 cicloalquilo no sustituido o sustituido o heterocicloalquilo de 4-10 miembros sustituido o no sustituido, en donde los átomos del anillo del heterocicloalquilo consisten en átomos de carbono y 1, 2 o 3 heteroátomos seleccionados de O, N o S, en el que el C3-7 cicloalquilo sustituido o heterocicloalquilo sustituido de 4-10 miembros de formación de Cy está sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados cada uno independientemente de halógeno, RCy1, C1-6 haloalquilo, CN, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(>=NRe1)NRc1Rd1, NRc1C(>=NRe1)NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1 y S(O)2NRc1Rd1 , en el que cada RCy1 se selecciona independientemente de C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C6-10 arilo, heteroarilo de 5-10 miembros, C3-7 cicloalquilo y heterocicloalquilo de 4-7 miembros, cada uno de los cuales es independientemente no sustituido o sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de halógeno, RCy2, C1-6 haloalquilo, CN, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(>=NRe1)NRc1Rd1, NRc1C(>=NRe1)NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1 y S(O)2NRc1Rd1, y en el que cada RCy2 es independientemente C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C6-10 arilo, heteroarilo de 5- 10 miembros, C3-7 cicloalquilo y heterocicloalquilo de 4-7 miembros, cada uno de que es independientemente no sustituido o sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de halógeno, CN, ORa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Ra1, NRc1Ra1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1 y S(O)2NRc1Rd1; A 1 es N o CR1; R1 es H, halógeno, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, CN, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(>=NRe2)NRc2Rd2, NRc2C(>=NRe2)NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2 o S(O)2NRc2Rd2; y R2 es H, halógeno, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, CN, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(>=NRe2)NRc2Rd2, NRc2C(>=NRe2)NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2 o S(O)2NRc2Rd2; o A1 y R2 en combinación, junto con el átomo de carbono al que R2 está unido, forman un anillo carbocíclico insaturado o parcialmente saturado de 5, 6 o 7 miembros o anillo heterocíclico que contiene 3 a 7 átomos de carbono en el anillo y 0, 1 o 2 heteroátomos en el anillo, cada uno seleccionado independientemente de N, o y S, donde el anillo formado por la combinación de A1 y R2 es no sustituido o sustituido por 1, 2 o 3 sustituyentes seleccionados independientemente de halógeno, C1-6 alquilo, CN, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Ra2, NRc2Rd2, NRcC(O)Rb2, NRc2C(O)NRc2Ra2, NRc2C(O)ORa2 y oxo; R3 es H, halógeno o NH2; R4 es H o halógeno; A5 es N o CR5; A6 es N o CR6; A7 es N o CR7; A8 es N o CR8; a condición de que 0, 1 o 2 de A5, A6, A7 y A8 son N; R5 es H o halógeno; R6 es H o halógeno; R7 es H, halógeno, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, Cy7, -L7-Cy7, CN, ORa3, SRa3, C(O)Rb3 , C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C (O)NRc3Rd3, NRc3C(O)ORa3, C(>=NRe3)NRc3Rd3, NRc3C(>=NRe3)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3 o S(O)2NRc3Rd3, en el que dicho C1-6 alquilo, C2-6 alquenilo o C2-6 alquinilo R formandO7 son cada uno independientemente no sustituido o sub- stituted con 1, 2 o 3 sustituyentes seleccionados independientemente de halógeno, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, CN, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(>=NRe3)NRc3Rd3, NRc3C(>=NRe3)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3 y S(O)2NRc3Rd3 ; Cy7 está no sustituido o sustituido C6-10 arilo, no sustituido o sustituido heteroarilo de 5-10 miembros, no sustituido o sustituido C3-6 cicloalquilo o no sustituido o sustituido de 4-7 miembros, heterocicloalquilo, en el que el sustituido C6-10 arilo, heteroarilo de 5-10 miembros, C3-6 cicloalquilo o heterocicloalquilo de 4-7 formando Cy7 está sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados cada uno independientemente de halógeno, RCy7, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, CN, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(>=NRe3)NRc3Rd3, NRc3C(>=NRe3)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3 y S(O)2NRc3Rd3 , en el que cada RCy7 es C1-6 alquilo, cada uno de los cuales es independientemente no sustituido o sustituido por 1, 2 o 3 subconstituyentes seleccionados independientemente de halógeno, CN, ORa3, SRa3, C(O)Rb3, C (O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(>=NRe3)NRc3Rd3, NRc3C(>=NRe3)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3 NRc3S(O)2Rb3 y S(O)2NRc3Rd3 ; L7 está no sustituido C1-6 alquileno o C1-6 alquileno sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre F, Cl, CN, OH, O (C1-6 alquilo), NH2, NH(C1-6 alquilo) y N(C1-6 alquilo)2; R8 es H, halógeno, CN o C1-6 alquilo; Ra1, Rb1, Rc1y Rd1 se seleccionan cada uno independientemente de H, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C6-10 arilo, C3-7 cicloalquilo, heteroarilo de 5-10 miembros, heterocicloalquilo de 4-10 miembros, C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo-C1-3 alquilo y heterocicloalquilo de 4-10 miembros-C1-3 alquilo, en el que dicho C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo-C1-3 alquilo y heterocicloalquilo de 4-10 miembros-C1-3 alquilo formando Ra1, Rb1, Rc1y Rd1 están cada uno opcionalmente sustituidos con 1, 2, 3, 4 o 5 sustituyentes seleccionados independientemente de C1-6 alquilo, halo, CN, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(>=NRe4)NRc4Rd4, NRc4C(>=NRe4)NRc4Rd4, S(O)Rb4, S(O)NRc4Rd4, S(O)2Rb4, NRc4S(O)2Rb4 y S(O)2NRc4Rd4 ; o Rc1y Rd1 unidos al mismo átomo de N, junto con el átomo de N al que están ambos unidos, forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros o grupo heteroarilo de 5 miembros, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de C1-6 alquilo, halo, CN, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(>=NRe4)NRc4Rd4, NRc4C(>=NRe4)NRc4Rd4, S(O)Rb4, S(O)NRc4Rd4, S(O)2Rb4, NRc4S(O)2Rb4 y S(O)2NRc4Rd4 ; Ra2, Rb2, Rc2 y Rd2 se seleccionan cada uno independientemente de H, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C6-10 arilo, C3-7 cicloalquilo, heteroarilo de 5-10 miembros, heterocicloalquilo de 4-10 miembros-C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo-C1-3 alquilo y heterocicloalquilo de 4-10 miembros-C1-3 alquilo, en el que dicho C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo-C1-3 alquilo y heterocicloalquilo de 4-10 miembros -C1-3 alquilo formando Ra2, Rb2, Rc2 y Rd2 están cada uno opcionalmente sustituidos con 1, 2, 3, 4 o 5 sustituyentes seleccionados independientemente de C1-6 alquilo, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(>=NRe5)NR5Rd5, NRc5C(>=NRe5)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5(O)2Rb5 y S(O)2NRc5Rd5 ; o Rc2 y Rd2 unidos al mismo átomo de N, junto con el átomo de N al que están ambos unidos, forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros o grupo heteroarilo de 5 miembros, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de C1-6 alquilo, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(>=NRe5)NRc5Rd5, NRc5C(>=NRe5)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5 y S(O)2NRc5Rd5 ; Ra3, Rb3, Rc3 y Rd3 se seleccionan cada uno independientemente de H, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C6-10 arilo, C3-7 cicloalquilo, heteroarilo de 5-10 miembros, heterocicloalquilo de 4-10 miembros-C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo-C1-3 alquilo y heterocicloalquilo 4-10 miembros- C1-3 alquilo, en el que dicho C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo-C1-3 alquilo y heterocicloalquilo 4-10 miembros-C1-3 alquilo formando Ra3, Rb3, Rc3 y Rd3 están cada uno opcionalmente sustituidos con 1, 2, 3, 4 o 5 sustituyentes seleccionados independientemente de C1-6 alquilo, halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(>=NRe6)NRc6Rd6, NRc6C(>=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6 y S(O)2NRc6Rd6; o Rc3 y Rd3 unidos al mismo átomo de N, junto con el átomo de N al que están ambos unidos, forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros o grupo heteroarilo de 5 miembros, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de C1-6 alquilo, halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(>=NRe6)NRc6Rd6, NRc6C(>=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6 y S(O)2NRc6Rd6 ; Ra4, Rb4, Rc4 y Rd4 se seleccionan cada uno independientemente de H, C1-6 alquilo, C1-6 haloalquilo, C2-6 alquenilo, C2-6 alquinilo, arilo, C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo- C1-3 alquilo y heterocicloalquilo de 4-10 miembros-C1-3 alquilo, en el que dicho C1-6 alquilo, C1-6 haloalquilo, C2-6 alquenilo, C2-6 alquinilo C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo-C 1-3 alquilo y heterocicloalquilo de 4-10 miembros-C1-3 alquilo formando Ra4, Rb4, Rc4 y Rd4 están cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de OH, CN, amino, NH(C1-6 alquilo), N(C1-6 alquilo)2, halo, C1-6 alquilo, C1-6 alcoxi, C1-6 haloalquilo y C1-6 haloalcoxi; o Rc4 y Rd4 unidos al mismo átomo de N, junto con el átomo de N al que están ambos unidos, forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros o grupo heteroarilo de 5 miembros, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de OH, CN, amino, NH(C1-6 alquilo), N(C1-6 alquilo)2, halo, C1-6 alquilo, C1-6 alcoxi, C1-6 haloalquilo y C1-6 haloalcoxi; Ra5, Rb5, Rc5 y Rd5 se seleccionan 5 cada uno independientemente de H, C1-6 alquilo, C1-6 haloalquilo, C2-6 alquenilo, C2-6 alquinilo, arilo, C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo- C1-3 alquilo y heterocicloalquilo de 4-10 miembros-C1-3 alquilo, en el que dicho C1-6 alquilo, C1-6 haloalquilo, C2-6 alquenilo, C2-6 alquinilo C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo-C 1-3 alquilo y 4-10 miembros heterocicloalquilo-C1-3 alquilo formando Ra5, Rb5, Rc5 y Rd5 están cada uno opcionalmente sustituidos con 1, 2 o 3 sustituyentes seleccionados independientemente de OH, CN, amino, NH(C1-6 alquilo), N(C1-6 alquilo)2, halo, C1-6 alquilo, C1-6 alcoxi, C1-6 haloalquilo y C1-6 haloalcoxi; o Rc5 y Rd5 unidos al mismo átomo de N, junto con el átomo de N al que están ambos unidos, forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros o grupo heteroarilo de 5 miembros, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de OH, CN, amino, NH(C1-6 alquilo), N(C1-6 alquilo)2, halo, C1-6 alquilo, C1-6 alcoxi, C1-6 haloalquilo y C1-6 haloalcoxi; Ra6, Rb6, Rc6 y Rd6 se seleccionan cada uno independientemente de H, C1-6 alquilo, C1-6 haloalquilo, C2-6 alquenilo, C2-6 alquinilo, arilo, C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo- C1-3 alquilo y heterocicloalquilo de 4-10 miembros-C1-3 alquilo, en el que dicho C1-6 alquilo, C1-6 haloalquilo, C2-6 alquenilo, C2-6 alquinilo C6-10 arilo-C1-3 alquilo, heteroarilo de 5-10 miembros-C1-3 alquilo, C3-7 cicloalquilo-C 1-3 alquilo y 4-10 miembros heterocicloalquilo-C1-3 alquilo formando Ra6, Rb6, Rc6 y Rd6 están cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de OH, CN, amino, NH(C1-6 alquilo), N(C1-6 alquilo)2, halo, C1-6 alquilo, C1-6 alcoxi, C1-6 haloalquilo y C1-6 haloalcoxi; o Rc6 y Rd6 unidos al mismo átomo de N, junto con el átomo de N al que están ambos unidos, forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros o grupo heteroarilo de 5 miembros, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de OH, CN, amino, NH(C1-6 alquilo), N(C1-6 alquilo)2, halo, C1-6 alquilo, C1-6 alcoxi, C1-6 haloalquilo y C1-6 haloalcoxi; y Re1, Re2, Re3, Re4, Re5 y Re6 son cada uno, independientemente, H, CN o NO2
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JP2016505021A (ja) 2016-02-18
WO2014110574A1 (en) 2014-07-17
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EP2943485B1 (en) 2017-09-20
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