AR078675A1 - Derivados de pirazolo[3,4-d]pirimidina inhibidores de jak quinasas, composiciones farmaceuticas que los comprenden, metodo para prepararlos y uso de los mismos para el tratamiento o profilaxis de trastornos inmunologicos, inflamatorios y autoinmunes. - Google Patents

Derivados de pirazolo[3,4-d]pirimidina inhibidores de jak quinasas, composiciones farmaceuticas que los comprenden, metodo para prepararlos y uso de los mismos para el tratamiento o profilaxis de trastornos inmunologicos, inflamatorios y autoinmunes.

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AR078675A1
AR078675A1 ARP100103813A ARP100103813A AR078675A1 AR 078675 A1 AR078675 A1 AR 078675A1 AR P100103813 A ARP100103813 A AR P100103813A AR P100103813 A ARP100103813 A AR P100103813A AR 078675 A1 AR078675 A1 AR 078675A1
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Argentina
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alkyl
alkynyl
alkenyl
same
optionally substituted
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Cellzome Ltd
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Abstract

Reivindicacion 1: Un compuesto de formula (1) o una sal, profármaco o metabolito farmacéuticamente aceptable de éste, donde R es H o F; el anillo A es un heterociclo aromático de 5 miembros en el cual Z1, Z2 y Z3 están independientemente seleccionados del grupo integrado por C(R1), N, N(R1), O y S, con la condicion de que por lo menos uno de Z1, Z2, Z3 es N; cada R1 es independientemente H, halogeno, CN; C(O)OR2, OR2; C(O)R2; C(O)N(R2R2; S(O)2N(R2R2a); S(O)N(R2R2a); S(O)2R2; S(O)R2; N(R2)S(O)2N(R2aR2b); N(R2)S(O)N(R2aR2b); SR2; N(R2R2a); NO2; OC(O)R2; N(R2)C(O)R2a; N(R2)S(O)2R2a; N(R2)S(O)R2a; N(R2)C(O)N(R2aR2b); N(R2)C(O)OR2a; OC(O)N(R2R2a); T1; alquilo C1-6; alquenilo C2-6; o alquinilo C2-6, donde alquilo C1-6; alquenilo C2-6 y alquinilo C2-6 están sustituidos opcionalmente con uno o más R3, que son iguales o diferentes; R2, R2a, R2b están independientemente seleccionados del grupo integrado por H; T1; alquilo C1-6; alquenilo C2-6; y alquinilo C2-6, donde alquilo C1-6; alquenilo C2-6; y alquinilo C2-6 están sustituidos opcionalmente con uno o más R3, que son iguales o diferentes; R3 es halogeno; CN; C(O)OR4; OR4; C(O)R4; C(O)N(R4R4a); S(O)2N(R4R4a); S(O)N(R4R4a); S(O)2R4; S(O)R4; N(R4)S(O)2N(R4aRb); N(R4)S(O)2N(R4aR4b); SR4; N(R4aR4b); NO2; OC(O)R4; N(R4)C(O)R4a; N(R4)S(O)2R4a; N(R4)S(O)R4a; N(R4)C(O)N(R4aR4b); N(R4)C(O)OR4a; OC(O)N(R4R4a); o T1; R4, R4a, R4b están independientemente seleccionados del grupo integrado por H; T1; alquilo C1-6; alquenilo C2-6; y alquinilo C2-6, donde alquilo C1-6; alquenilo C2-6; y alquinilo C2-6 están sustituidos opcionalmente con uno o más halogeno, que son iguales o diferentes; T1 es cicloalquilo C3-7 o heterociclilo de 4 a 7 miembros saturado, donde T1 está opcionalmente sustituido con uno o más R10, que son iguales o diferentes; Y es (C(R5R5a))n; n es 0, 1, 2, 3 o 4; R5, R5a están independientemente seleccionados del grupo integrado por H; y alquilo C1-6 no sustituido; o forman en conjunto oxo (=O); opcionalmente, R5, R5a se unen para formar un cicloalquilo C3-7 no sustituido; X1 es C(R6) o N; X2 es C(R6a) o N; X3 es C(R6b) o N; X4 es C(R6c) o N; X5 es C(R6d) o N, con la condicion de que como máximo dos de X1, X2, X3, X4, X5 son N; R6, Ra, R6b, R6c, R6d están independientemente seleccionados del grupo integrado por H; halogeno; CN; C(O)OR7; OR7; C(O)R7; C(O)N(R7R7a); S(O)2N(R7R7a); S(O)N(R7R7a); S(O)2R7; S(O)R7; N(R7)S(O)2N(R7a7b); N(R7)S(O)N(R7aR7b); SR7; N(R7aR7b); NO2; OC(O)R7; N(R7)C(O)R7a; N(R7)S(O)2R7a; N(R7)S(O)R7a; N(R7)C(O)N(R7aR7b); N(R7)C(O)OR7a; OC(O)N(R7R7a); o T2; alquilo C1-6; alquenilo C2-6; y alquinilo C2-6; donde alquilo C1-6; alquenilo C2-6; y alquinilo C2-6 están sustituidos opcionalmente con uno o más R11, que son iguales o diferentes; opcionalmente uno de los pares R6/R6a, R6a/R6b se une para formar un anillo T3; R7, R7a, R7b están independientemente seleccionados del grupo integrado por H; T2; alquilo C1-6; alquenilo C2-6; y alquinilo C2-6, donde alquilo C1-6; alquenilo C2-6; y alquinilo C2-6 están sustituidos opcionalmente con uno o más R8, que son iguales o diferentes; R8 es halogeno; CN; C(O)OR9; OR9; C(O)R9; C(O)N(R9R9a); S(O)2N(R9R9a); S(O)N(R9R9a); S(O)2R9; S(O)R9; N(R9)S(O)2N(R9a9b); N(R9)S(O)2N(R9aR9b); SR9; N(R9aR9b); NO2; OC(O)R9; N(R9)C(O)R9a; N(R9)S(O)2R9a; N(R9)S(O)R9a; N(R9)C(O)N(R9aR9b); N(R9)C(O)OR9a; OC(O)N(R9R9a); o T2; R9, R9a, R9b están independientemente seleccionados del grupo integrado por H; T2 alquilo C1-6; alquenilo C2-6, y alquinilo C2-6, donde alquilo C1-6, alquenilo C2-6, y alquinilo C2-6 están sustituidos opcionalmente con uno o más R12, que son iguales o diferentes; R10 es halogeno; CN; C(O)OR13; OR13; oxo (=O), donde el anillo está saturado por lo menos parcialmente; C(O)R13; C(O)N(R13R13a); S(O)2N(R13R13a); S(O)N(R13R13a); S(O)2R13; S(O)R13; N(R13)S(O)2N(R13a13b); N(R13)S(O)N(R13aR13b); SR13; N(R13aR13b); NO2; OC(O)R13; N(R13)C(O)R13a; N(R13)S(O)2R13a; N(R13)S(O)R13a; N(R13)C(O)N(R13aR13b); N(R13)C(O)OR13a; OC(O)N(R13R13a); alquilo C1-6; alquenilo C2-6, y alquinilo C2-6, donde alquilo C1-6, alquenilo C2-6, y alquinilo C2-6 están sustituidos opcionalmente con uno o más R14, que son iguales o diferentes; R13, R13a, R3b están independientemente seleccionados del grupo integrado por H; alquilo C1-6, alquenilo C2-6; y alquinilo C2-6, donde alquilo C1-6; alquenilo C2-6; y alquinilo C2-6 están sustituidos opcionalmente con uno o más R14, que son iguales o diferentes; R11, R12 están independientemente seleccionados del grupo integrado por halogeno; CN; C(O)OR15; OR15; C(O)R15; C(O)N(R15R15a); S(O)2N(R15R15a); S(O)N(R15R15a); S(O)2R15; S(O)R15; N(R15)S(O)2N(R15a15b); N(R15)S(O)N(R15aR15b); SR15; N(R15aR15b); NO2; OC(O)R15; N(R15)C(O)R15a; N(R15)S(O)2R15a; N(R15)S(O)R15a; N(R15)C(O)N(R15aR15b); N(R15)C(O)OR15a; OC(O)N(R15R15a); o T2; R15, R15a, R15b están independientemente seleccionados del grupo integrado por H; T2; alquilo C1-6; alquenilo C2-6, y alquinilo C2-6, donde alquilo C1-6, alquenilo C2-6, y alquinilo C2-6 están sustituidos opcionalmente con uno o más halogenos que son iguales o diferentes; R14 es halogeno; CN; C(O)OR16; OR16; C(O)R16; C(O)N(R16R16a); S(O)2N(R16R16a); S(O)N(R16R16a); S(O)2R16; S(O)R16; N(R16)S(O)2N(R16a16b); N(R16)S(O)N(R16aR16b); SR16; N(R16aR16b); NO2; OC(O)R16; N(R16)C(O)R16a; N(R16)S(O)2R16a; N(R16)S(O)R16a; N(R16)C(O)N(R16aR16b); N(R16)C(O)OR16a; o OC(O)N(R16R16a); R16, R16a, R16b están independientemente seleccionados del grupo integrado por H; alquilo C1-6; alquenilo C2-6, y alquinilo C2-6, donde alquilo C1-6, alquenilo C2-6, y alquinilo C2-6 están sustituidos opcionalmente con uno o más halogenos que son iguales o diferentes; T2 es fenilo; naftilo; indenilo; indanilo; cicloalquilo C3-7; heterociclilo de 4 a 7 miembros; o heterobiciclilo de 7 a 11 miembros, donde T2 está opcionalmente sustituido con uno o más R17, que son iguales o diferentes; T3 es fenilo; cicloalquilo C3-7; o heterociclilo de 4 a 7 miembros, donde T3 está opcionalmente sustituido con uno o más R18, que son iguales o diferentes; R17, R18 están independientemente seleccionados del grupo integrado por halogeno; CN; C(O)OR19; OR19; oxo (=O), donde el anillo está saturado por lo menos parcialmente; C(O)R19; C(O)N(R19R19a); S(O)2N(R19R19a); S(O)N(R19R19a); S(O)2R19; S(O)R19; N(R19)S(O)2N(R19a19b); N(R19)S(O)N(R19aR19b); SR19; N(R19aR19b); NO2; OC(O)R19; N(R19)C(O)R19a; N(R19)S(O)2R19a; N(R19)S(O)R19a; N(R19)C(O)N(R19aR19b); N(R19)C(O)OR19a; OC(O)N(R19R19a); alquilo C1-6; alquenilo C2-6, y alquinilo C2-6, donde alquilo C1-6, alquenilo C2-6, y alquinilo C2-6 están sustituidos opcionalmente con uno o más R20, que son iguales o diferentes: R19, R19a, R19b están independientemente seleccionados del grupo integrado por H; alquilo C1-6, alquenilo C2-6, y alquinilo C2-6, donde alquilo C1-6; alquenilo C2-6; y alquinilo C2-6 están sustituidos opcionalmente con uno o más R20, que son iguales o diferentes; R20 es halogeno; CN; C(O)OR21; OR21; C(O)R21; C(O)N(R21R21a); S(O)2N(R21R21a); S(O)N(R21R21a); S(O)2R21; S(O)R21; N(R21)S(O)2N(R21a21b); N(R21)S(O)N(R21aR21b); SR21; N(R21aR21b); NO2; OC(O)R21; N(R21)C(O)R21a; N(R21)S(O)2R21a; N(R21)S(O)R21a; N(R21)C(O)N(R21aR21b); N(R21)C(O)OR21a; o OC(O)N(R21R21a); R21, R21a, R21b están independientemente seleccionados del grupo integrado por H; alquilo C1-6; alquenilo C2-6, y alquinilo C2-6, donde alquilo C1-6, alquenilo C2-6, y alquinilo C2-6 están sustituidos opcionalmente con uno o más halogenos que son iguales o diferentes.
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