ES2677919T3 - Aminoalquil-quinazolonas sustituidas con pirimidina como inhibidores de la fosfatidilinositol 3-quinasa - Google Patents

Aminoalquil-quinazolonas sustituidas con pirimidina como inhibidores de la fosfatidilinositol 3-quinasa Download PDF

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ES2677919T3
ES2677919T3 ES13821357T ES13821357T ES2677919T3 ES 2677919 T3 ES2677919 T3 ES 2677919T3 ES 13821357 T ES13821357 T ES 13821357T ES 13821357 T ES13821357 T ES 13821357T ES 2677919 T3 ES2677919 T3 ES 2677919T3
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alkyl
substituted
haloalkyl
aryl
unsubstituted
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Jerry Evarts
Leena Patel
Jennifer A. TREIBERG
Stephane Perreault
Arthur Yeung
Lafe J. Ii Purvis
Musong Kim
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Gilead Calistoga LLC
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Abstract

Un compuesto que tiene la estructura de la Fórmula (II):**Fórmula** o una sal farmacéuticamente aceptable o solvato del mismo, en donde: R1 es: arilo no sustituido; heteroarilo no sustituido; cicloalquilo no sustituido; alquilo no sustituido; arilo, heteroarilo, o cicloalquilo sustituido con 1 o 2 sustituyentes seleccionados independientemente del grupo que consiste en halo, -OR1a, -C(O)OR1a, -C(O)R1a, NH2, alquilo, haloalquilo, y C1-6 alquilo sustituido con OH o NH2, en donde R1a es H, alquilo, haloalquilo, NH2, o -O(C1-6 alquilo); o alquilo sustituido con OH; n es 0, 1, 2 o 3; cada R2 es independientemente halo, OH, CN, haloalquilo, alquilo no sustituido, alquilo sustituido con 1 a 5 sustituyentes seleccionados de hidroxilo, haloalquilo, alcoxi, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, amino, ciano, halo, y carboxilo, o R2 es SO2R2a, en donde R2a es alquilo; R3 es: arilo no sustituido o arilo sustituido con 1 a 5 sustituyentes seleccionados de halo, OR, -C(O)NR2, -SO2NR2, alquilo, haloalquilo, heterocicloalquilo, heteroarilo, alcoxi, amino, ciano, y carboxilo, donde cada R es independientemente seleccionado de hidrógeno, alquilo, y haloalquilo; heteroarilo no sustituido o heteroarilo sustituido con 1 a 5 sustituyentes seleccionados de alquilo, haloalquilo, halo, NH2, OR, -C(O)OR, heterocicloalquilo, arilo, y ciano, donde cada R es independientemente seleccionado de hidrógeno, alquilo, y haloalquilo; heterocicloalquilo no sustituido o heterocicloalquilo sustituido con 1 a 5 sustituyentes seleccionados de alquilo, haloalquilo, cicloalquilo, arilo, heteroarilo, alcoxi, amino, ciano, halo, carboxilo, e hidroxilo; o R3 es: C6-12 arilo no sustituido; C6-12 arilo sustituido con 1 o 2 sustituyentes seleccionados independientemente del grupo que consiste en halo, alquilo, haloalquilo, arilo, ciano, -OR3a, -C(O)NR3aR3b, -SO2R3a, -SO2NR3aR3b, y alquilo sustituido con NR3aR3b, en donde R3a y R3b son independientemente hidrógeno, C1-6 alquilo, o -SO2R3c, en donde R3c es alquilo; C3-12 heteroarilo no sustituido con 1 o 2 heteroátomos independientemente seleccionados del grupo que consiste en nitrógeno, oxígeno y azufre; C3-12 heterocicloalquilo no sustituido con 1 o 2 heteroátomos independientemente seleccionados del grupo que consiste en nitrógeno, oxígeno y azufre; o C3-12 heterocicloalquilo con 1 o 2 heteroátomos independientemente seleccionados del grupo que consiste en nitrógeno, oxígeno y azufre, y sustituido con 1 o 2 sustituyentes alquilo; R4 es hidrógeno, alquilo, o NH2; R5 es alquilo o alquilo sustituido con OH o OR5a, en donde R5a es alquilo; y R6 es hidrógeno, o R5 junto con el carbono al que está unido y R6 junto con el nitrógeno al cual está unido se toman juntos para formar un heterociclo de cuatro, cinco o seis miembros.
ES13821357T 2012-12-21 2013-12-20 Aminoalquil-quinazolonas sustituidas con pirimidina como inhibidores de la fosfatidilinositol 3-quinasa Active ES2677919T3 (es)

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US201261745429P 2012-12-21 2012-12-21
PCT/US2013/077311 WO2014100765A1 (en) 2012-12-21 2013-12-20 Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors

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US (2) US9018221B2 (es)
EP (1) EP2941426B1 (es)
JP (1) JP6125663B2 (es)
AR (1) AR094313A1 (es)
AU (1) AU2013364068B2 (es)
BR (1) BR112015014585A2 (es)
CA (1) CA2895782C (es)
ES (1) ES2677919T3 (es)
NZ (1) NZ708864A (es)
PT (1) PT2941426T (es)
TW (1) TW201441216A (es)
UY (1) UY35242A (es)
WO (1) WO2014100765A1 (es)

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