AR084366A1 - N-(1-(fenil sustituido)etil)-9h-purin-6-aminas como inhibidores de pi3k - Google Patents

N-(1-(fenil sustituido)etil)-9h-purin-6-aminas como inhibidores de pi3k

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Publication number
AR084366A1
AR084366A1 ARP110104779A ARP110104779A AR084366A1 AR 084366 A1 AR084366 A1 AR 084366A1 AR P110104779 A ARP110104779 A AR P110104779A AR P110104779 A ARP110104779 A AR P110104779A AR 084366 A1 AR084366 A1 AR 084366A1
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Argentina
Prior art keywords
alkyl
aminosulfonyl
carbamyl
independently selected
haloalkyl
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ARP110104779A
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Eddy W Yue
Richard P Sparks
Yun Li
Andrew P Long-Combs
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Incyte Corp
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Publication of AR084366A1 publication Critical patent/AR084366A1/es

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Abstract

La presente proporciona derivados de N-(1-(fenil sustituido)etil)-9H-purin-6-aminas que modulan la actividad de fosfoinositida 3-quinasas (PI3Ks) y son de utilidad en el tratamiento de enfermedades relacionadas con la actividad de las PI3K incluyendo, por ejemplo, trastornos inflamatorios, trastornos de base inmune, cáncer y otras enfermedades.Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales farmacéuticamente aceptables; en donde: Ar es un resto de fórmula (2) ó (3); X es CH o N; Y es CH o N; R1 está seleccionado de alquilo C1-6, alquenilo C2-6, alquinilo C2-6 y haloalquilo C1-6 en donde dicho alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos seleccionados, de modo independiente, de halo, OH, CN, NR1aR2b, alcoxi C1-6 y haloalcoxi C1-6; cada R1a y R2b está seleccionado, de modo independiente, de H y alquilo C1-6; o cualquier R1a y R2b junto con el átomo de N al que están unidos forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros, que está opcionalmente sustituido con 1, 2, 3 ó 4 sustituyentes seleccionados, de modo independiente, de alquilo C1-6; R2 está seleccionado de halo, CN, alquilo C1-6, haloalquilo C1-6, -L-(alquilo C1-6), -L-(haloalquilo C1-6) y -L-(alquilen C1-4)n-Cy2 y -(alquilen C1-4)n-Cy2; en donde dicho alquilo C1-6 en dicho alquilo C1-6 y -L-(alquilo C1-6) está opcionalmente sustituido con 1, 2, 3 ó 4 grupos R2a seleccionados de modo independiente; L es O, NRB, S, S(O), S(O)2, C(O), C(O)NRB, S(O)NRB, S(O)2NRB, NRBC(O), NRBS(O) y NRBS(O)2; RA y RB están seleccionados cada uno, de modo independiente, de H y alquilo C1-6; Cy2 está seleccionado de cicloalquilo C3-7, heterocicloalquilo de 4 - 7 miembros, fenilo y heteroarilo de 5 - 6 miembros; cada uno de los cuales está sustituido con p grupos R2a seleccionados de modo independiente; en donde p es 0, 1, 2, 3 ó 4; cada R2a está seleccionado, de modo independiente, de OH, NO2, CN, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, amino, alquil C1-6-amino, di(alquil C1-6)amino, tio, alquil C1-6-tio, alquil C1-6-sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di-(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6) aminocarbonilamino; R3 es halo, CN, NO2, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, -(alquilen C1-4)r-Cy3, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb o S(O)2NRcRd; en donde dicho alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos R3a seleccionados de modo independiente; Cy3 está seleccionado de cicloalquilo C3-7, heterocicloalquilo de 4 - 7 miembros, fenilo y heteroarilo de 5 - 6 miembros; cada uno de los cuales está opcionalmente sustituido con 1, 2, 3 ó 4 grupos R3a seleccionados de modo independiente; siempre que uno de los siguientes sea verdadero: (i) R3 es -(alquilen C1-4)r-Cy3; o (ii) R2 está seleccionado de -L-(alquilen C1-4)n-Cy2 y -(alquilen C1-4)n-Cy2 o (iii) R3 es -(alquilen C1-4)r-Cy3; y R2 está seleccionado de -L-(alquilen C1-4)n-Cy2 y -(alquilen C1-4)n-Cy2; cada R3a está seleccionado, de modo independiente, de halo, CN, NO2, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, cicloalquilo C3-7, heterocicloalquilo de 4 - 7 miembros, fenilo, heteroarilo de 5 - 6 miembros, (heterocicloalquilo de 4 - 7 miembros)-alquilo C1-4, fenil-alquilo C1-4, (heteroarilo de 5 - 6 miembros)-alquilo C1-4, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd y S(O)2NRcRd; en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, heterocicloalquilo de 4 - 7 miembros, fenilo, heteroarilo de 5 - 6 miembros, (heterocicloalquilo de 4 - 7 miembros)-alquilo C1-4, fenil-alquilo C1-4 y (heteroarilo de 5 - 6 miembros)-alquilo C1-4 están cada uno opcionalmente sustituidos con 1, 2, 3 ó 4 grupos seleccionados, de modo independiente, de OH, NO2, CN, halo, alquilo C1-6, cianoalquilo C1-6, HO-alquilo C1-6, alcoxi C1-4-alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, amino, alquil C1-6-amino, di(alquil C1-6)amino, tio, alquil C1-6-tio, alquil C1-6-sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6)aminocarbonilamino; R4 está seleccionado de H, OH. NO2, CN, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, ciano-alquilo C1-6, HO-alquilo C1-6, alcoxi C1-4-alquilo C1-6, cicloalquilo C3-7, alcoxi C1-6, haloalcoxi C1-6, amino, alquil C1-6-amino, di(alquil C1-6)amino, tio, alquil C1-6-tio, alquil C1-6-sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6)aminocarbonilamino; R5 está seleccionado de halo, OH, CN, alquilo C1-4, alcoxi C1-4 y haloalcoxi C1-4; cada Ra, Rc y Rd está seleccionado, de modo independiente, de H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, heterocicloalquilo de 4 - 7 miembros, fenilo, heteroarilo de 5 - 6 miembros, (heterocicloalquilo de 4 - 7 miembros)-alquilo C1-4, fenil-alquilo C1-4 y (heteroarilo de 5 - 6 miembros)-alquilo C1-4 en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, heterocicloalquilo de 4 - 7 miembros, fenilo, heteroarilo de 5 - 6 miembros, (heterocicloalquilo de 4 - 7 miembros)-alquilo C1-4, fenil-alquilo C1-4 y (heteroarilo de 5 - 6 miembros)-alquilo C1-4 están sustituidos opcionalmente cada uno con 1, 2, 3, 4 ó 5 sustituyentes seleccionados, de modo independiente, de OH, NO2, CN, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, ciano-alquilo C1-6, HO-alquilo C1-6, alcoxi C1-4-alquilo C1-6, cicloalquilo C3-7, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, amino, alquil C1-6-amino, di(alquil C1-6)amino, tio, alquil C1-6-tio, alquil C1-6-sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6-carbonilo, alcoxi C1-6-carbonilo, alquil C1-6-carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6)aminocarbonilamino; cada Rb está seleccionado, de modo independiente, de alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, heterocicloalquilo de 4 - 7 miembros, fenilo, heteroarilo de 5 - 6 miembros, (heterocicloalquilo de 4 - 7 miembros)-alquilo C1-4, fenilalquilo C1-4 y (heteroarilo de 5 - 6 miembros)-alquilo C1-4; cada uno opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes seleccionados, de modo independiente, de OH, NO2, CN, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, ciano-alquilo C1-6, HO-alquilo C1-6, alcoxi C1-4-alquilo C1-6, cicloalquilo C3-7, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, amino, alquil C1-6-amino, di(alquil C1-6)amino, tio, alquil C1-6-tio, alquil C1-6- sulfinilo, alquil C1-6-sulfonilo, carbamilo, alquil C1-6-carbamilo, di(alquil C1-6)carbamilo, carboxi, alquil C1-6 carbonilo, alcoxi C1-6-carbonilo, alquil C1-6 carbonilamino, alquil C1-6-sulfonilamino, aminosulfonilo, alquil C1-6-aminosulfonilo, di(alquil C1-6)aminosulfonilo, aminosulfonilamino, alquil C1-6-aminosulfonilamino, di(alquil C1-6)aminosulfonilamino, aminocarbonilamino, alquil C1-6-aminocarbonilamino y di(alquil C1-6)aminocarbonilamino; cada Re está seleccionado, de modo independiente, de H, alquilo C1-4, CN, OH, alcoxi C1-4, alquil C1-4-sulfonilo, carbamilo, alquil C1-4-carbamilo, di(alquil C1-4)carbamilo y alquil C1-4-carbonilo; cada Rf está seleccionado, de modo independiente, de alquil C1-4-sulfonilo, alquil C1-4-carbonilo y alcoxi C1-4-carbonilo; n es 0 ó 1; y r es 0 ó 1.
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