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ES2586527T3 - Compuestos heterocíclicos y uso de los mismos como moduladores del receptor de tirosina quinasas de tipo III - Google Patents

Compuestos heterocíclicos y uso de los mismos como moduladores del receptor de tirosina quinasas de tipo III Download PDF

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Publication number
ES2586527T3
ES2586527T3 ES12780613.1T ES12780613T ES2586527T3 ES 2586527 T3 ES2586527 T3 ES 2586527T3 ES 12780613 T ES12780613 T ES 12780613T ES 2586527 T3 ES2586527 T3 ES 2586527T3
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heterocyl
alkyl
heteroaryl
run
ruc
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ES2586527T9 (es
Inventor
Michael J. Hadd
Michael D. Hocker
Mark W. Holladay
Gang Liu
Martin W. Rowbottom
Shimin Xu
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Ambit Bioscience Corp
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Ambit Bioscience Corp
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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Abstract

Un compuesto que tiene la fórmula VIIb:**Fórmula** o una de sus sales farmacéuticamente aceptables, solvatos, hidratos, clatratos, un estereoisómero individual, una mezcla de estereoisómeros o una mezcla racémica de estereoisómeros, en donde: R1 y R2 se selecciona cada uno independientemente de hidrógeno o halógeno; R3 es hidrógeno o alquilo; cada Q1 es independientemente deuterio, halógeno, ciano, oxo, tioxo, alquilo, halogenoalquilo, aminoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, cicloalquenilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, heterociclilo, heterociclilalquilo, -RuORx, -RuORuN(Ry)(Rz), -RuN(Ry)(Rz), -RuSRx, -RuC(J)Rx, -RuC(J)ORx, -RuC(J)N(Ry)(Rz), -RuS(O)tRw, -RuN(Rx)C(J)Rx, -RuN(Rx)C(J)ORx, -RuN(Rx)S(O)tRw, >=NORd, o -C(>=NRy)N(Ry)ORx, donde los grupos alquilo, halogenoalquilo, aminoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo y heterociclilo están opcionalmente sustituidos con uno o más grupos Q3, en una realización, de 1 a 3 grupos Q3; cada Q3 se selecciona independientemente de deuterio, halógeno, hidroxilo, alquilo, halogenoalquilo e hidroxialquilo; Y es -(CR5R6)q-; R5 y R6 son cada uno independientemente hidrógeno, halógeno, alquilo, halogenoalquilo o hidroxialquilo; Z es O, S, o NH; cada W es independientemente CR8 o N; R8 es hidrógeno, halógeno, halogenoalquilo o alquilo; W1 es N o C; W2 es N o C; R9b es hidrógeno o alquilo; W4 es N o CR11b; W5 es N o CR13; R11b y R13 son cada uno independientemente hidrógeno o Q2; Q2 es halógeno, deuterio, ciano, oxo, tioxo, alquilo, halogenoalquilo, halogenoalquenilo, aminoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, cicloalquenilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, heterociclilo, heterociclilalquilo, -RuORx, -RuORuORx, -RuORuN(Ry)(Rz), -RuN(Ry)(Rz), -RuSRx, -RuC(J)Rx, -RuC(J)ORx, -RuC(J)N(Ry)(Rz), -RuC(J)RuN(Ry)(Rz), -RuC(J)N(Ry)ORx, -C(>=NORx)Rx, -RuS(O)tRw, -RuN(Rx)C(J)Rx, -RuN(Rx)C(J)ORx, -RuN(Rx)S(O)tRw o -C(>=NRy)N(Ry)ORx, donde los grupos alquilo, halogenoalquilo, aminoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo y heterociclilo están opcionalmente sustituidos con uno o más grupos Q4; en una realización, de 1 a 3 grupos Q4, cada Q4 se selecciona independientemente de halógeno, deuterio, hidroxilo, alquilo, halogenoalquilo e hidroxialquilo; Q5 y Q6 son cada uno independientemente hidrógeno, deuterio, halógeno, ciano, oxo, tioxo, alquilo, halogenoalquilo, aminoalquilo, alquenilo, halogenoalquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, cicloalquenilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, heterociclilo, heterociclilalquilo, -RuORx, -RuORuORx, -RuORuN(Ry)(Rz), -RuN(Ry)(Rz), -RuSRx, -RuC(J)Rx, -RuC(J)ORx, -RuC(J)N(Ry)(Rz), -RuC(J)RuN(Ry)(Rz), -RuC(J)N(Ry)ORx, -C(>=NORx)Rx, -RuS(O)tRw, -RuN(Rx)C(J)Rx, -RuN(Rx)C(J)ORx, -RuN(Rx)S(O)tRw o -C(>=NRy)N(Ry)ORx, donde los grupos alquilo, halogenoalquilo, aminoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo y heterociclilo están opcionalmente sustituidos con uno o más grupos Q8; cada Q8 se selecciona independientemente de halógeno, deuterio, hidroxilo, alquilo, halogenoalquilo e hidroxialquilo; cada Rd es independientemente hidrógeno o alquilo; cada Ru es independientemente alquileno, alquenileno o un enlace directo; Rw es alquilo, halogenoalquilo, hidroxialquilo, alcoxialquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, cicloalquenilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo oheteroaralquilo; cada Rx es independientemente hidrógeno, alquilo, halogenoalquilo, hidroxialquilo, alcoxialquilo, cianoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, cicloalquenilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo; Ry y Rz se selecciona cada uno independientemente del (i) o (ii) siguientes: (i) Ry y Rz son cada uno independientemente hidrógeno, alquilo, halogenoalquilo, hidroxialquilo, alcoxialquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, cicloalquenilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo; o (ii) Ry y Rz, junto con el átomo de nitrógeno al que están unidos, forman un heterociclilo o heteroarilo, opcionalmente sustituido con uno o más, en una realización, 1, 2 o 3 grupos Q7; cada Q7 se selecciona independientemente de halógeno, deuterio, oxo, tioxo, hidroxi, alcoxi, alquilo, halogenoalquilo, hidroxialquilo, aminoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, cicloalquenilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, heterociclilo y heterociclilalquilo; J es O, NRx o S; cada t es independientemente un número entero de 0-2; n es 1 o 2; y q es un número entero de 0-4.
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