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ES2684517T3 - Compuestos de heterociclilo como inhibidores de MEK - Google Patents

Compuestos de heterociclilo como inhibidores de MEK Download PDF

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ES2684517T3
ES2684517T3 ES13712929T ES13712929T ES2684517T3 ES 2684517 T3 ES2684517 T3 ES 2684517T3 ES 13712929 T ES13712929 T ES 13712929T ES 13712929 T ES13712929 T ES 13712929T ES 2684517 T3 ES2684517 T3 ES 2684517T3
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Bhavesh Dave
Rakesh Kumar Banerjee
Samiron Phukan
Abhijit Datta Khoje
Rajkumar HANGARGE
Jitendra Sambhaji Jadhav
Venkata P. Palle
Rajender Kumar Kamboj
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Abstract

Un compuesto de la fórmula general I, su forma tautomérica, su estereoisómero, su sal farmacéuticamente aceptable, sus combinaciones con un medicamento adecuado y su composición farmacéutica.**Fórmula** en el que: R1 se selecciona del grupo que consiste en hidrógeno, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido y heterociclilo sustituido o no sustituido; R2 se selecciona del grupo que consiste en -(C(Rc))(Rd))mC(>=O)-N(R6)R7, -C(>=O)N(R8)R9 y -O-(C(Rc)(Rd)m-C(>=O)- N(R6)R7; R3 se selecciona del grupo que consiste en hidrógeno, alquilo sustituido o no sustituido y cicloalquilo sustituido o no sustituido; R4 se selecciona del grupo que consiste en hidrógeno, halógeno, alquilo sustituido o no sustituido y cicloalquilo sustituido o no sustituido; R5 es arilo sustituido o no sustituido, en el que los sustituyentes se seleccionan de Ra y Rb; R6 y R7 se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido y heterociclilo sustituido o no sustituido; o R6 y R7 tomados junto con el nitrógeno al que están unidos forman un heterociclo sustituido o no sustituido; R8 y R9 se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, cicloalquilo sustituido o no sustituido y heterociclilo sustituido o no sustituido, o R8 y R9 tomados junto con el nitrógeno al que están unidos forman un heterociclo sustituido o no sustituido; con la condición de que tanto R8 como R9 no pueden ser hidrógeno al mismo tiempo; y cuando R8 y R9 no forman parte de un heterociclo formado junto con el nitrógeno al que están unidos, al menos uno de los R8 y R9 es cicloalquilo sustituido o no sustituido o heterociclilo sustituido o no sustituido; Ra y Rb se seleccionan del grupo que consiste en hidrógeno, halógeno y haloalquilo; Rc y Rd se seleccionan independientemente del grupo que consiste en hidrógeno, halógeno, hidroxilo y alquilo sustituido o no sustituido; o Rc y Rd tomados junto con el carbono al que están unidos forman un cicloalquilo sustituido o no sustituido; m es un número entero seleccionado del grupo que consiste en 1, 2, 3 y 4; adicionalmente en la que: cuando el grupo alquilo o grupo alquenilo está sustituido, el grupo alquilo o grupo alquenilo está sustituido con 1 a 4 sustituyentes seleccionados independientemente del grupo que consiste en oxo, halógeno, nitro, ciano, perhaloalquilo, cicloalquilo, arilo, heteroarilo, heterociclilo, -OR10b, -SO2R10a, -C(>=O)OR10a, -OC(>=O)R10a, - C(>=O)N(H)R10, -OR10a, -C(>=O)N(alquilo)R10, -N(H)C(>=O)R10a, -N(H)R10, -N(alquilo)R10-N(H)C(>=O)N(H)R10, - N(H)C(>=O)N(alquilo)R10, -NH-SO2-alquilo, y -NH-SO2-cicloalquilo; cuando el grupo cicloalquilo o el grupo cicloalquenilo está sustituido, el grupo cicloalquilo o cicloalquenilo está sustituido con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en oxo, halógeno, nitro, ciano, alquilo, alquenilo, perhaloalquilo, hidroxialquilo, arilo, heteroarilo, heterociclilo, -OR10b, -SO2R10a, -C(>=O)R10a, - C(>=O)OR10a, -OC(>=O)R10a, -C(>=O)N(H)R10, -C(>=O)N(alquilo)R10, -N(H)C(>=O)R10a, -N(H)R10, -N(alquilo)R10, - N(H)C(>=O)N(H)R10, y -N(H)C(>=O)N(alquilo)R10, -NH-SO2-alquilo, y -NH-SO2-cicloalquilo; cuando el grupo arilo está sustituido, el grupo arilo está sustituido con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en halógeno, nitro, ciano, hidroxi, alquilo, alquenilo, perhaloalquilo, cicloalquilo, cicloalquenilo, heterociclo, -O-alquilo, -O-perhaloalquilo, -N(alquil)alquilo, -N(H)alquilo, -NH2, -SO2- alquilo, -SO2-perhaloalquilo, -N(alquilo)C(>=O)alquilo, -N(H)C(>=O)alquilo, -C(>=O)N(alquil)alquilo, -C(>=O)N(H)alquilo, - C(>=O) NH2, -SO2N(alquil)alquilo, -SO2N(H)alquilo, -SO2NH2, -NH-SO2-alquilo, y -NH-SO2-cicloalquilo; cuando el grupo heteroarilo está sustituido, el grupo heteroarilo está sustituido con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en halógeno, nitro, ciano, hidroxi, alquilo, alquenilo, perhaloalquilo, cicloalquilo, cicloalquenilo, heterociclo, -O-alquilo, O-perhaloalquilo, -N(alquil)alquilo, -N(H)alquilo, -NH2, -SO2-alquilo, -SO2-perhaloalquilo, -N(alquil)C(>=O)alquilo, -N(H)C(>=O)alquilo, -C(>=O)N(alquil)alquilo, -C(>=O)N(H)alquilo, - C(>=O)NH2, -SO2N(alquil)alquilo, alquilo -SO2N(H), -SO2NH2, alquilo -NH-SO2, y cicloalquilo -NH-SO2; cuando el grupo heterociclilo está sustituido, el grupo heterociclilo está sustituido con 1 a 3 sustituyentes, cuando la heterocíclico grupo está sustituido en un carbono del anillo del 'heterociclo', los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, nitro, ciano, oxo, alquilo, alquenilo, perhaloalquilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo, heterociclilo, -OR10b, -C(>=O)OR10a, -OC(>=O)R10a, -C(>=O)N(H)R10, - C(>=O)N(alquilo)R10, -N(H)C(>=O)R10a, -N(H)R10, -N(alquilo)R10, -N(H)C(>=O)N(H)R10, -N(H)C(>=O)N(alquilo)R10; cuando el grupo heterocíclico está sustituido en un nitrógeno del anillo del 'heterociclo', los sustituyentes se seleccionan independientemente del grupo que consiste en alquilo, alquenilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo, - SO2R10a, -C(>= O)R10a, C(>=O)OR10a, -C(>=O)N(H)R10, -C(>=O)N(alquilo)R10, -NH-SO2-alquilo y -NH-SO2-cicloalquilo; cuando el grupo heterocíclico está sustituido en un azufre del anillo del "heterociclo", el azufre está sustituido con 1 o 2 grupos oxo; R10 se selecciona del grupo que consiste en hidrógeno, alquilo, alquenilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo y heterociclilo; R10a se selecciona del grupo que consiste en alquilo, alquenilo, perhaloalquilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo y heterociclilo; y R10b se selecciona del grupo que consiste en hidrógeno, alquilo, alquenilo, perhaloalquilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo y heterociclilo.
ES13712929T 2012-03-14 2013-03-11 Compuestos de heterociclilo como inhibidores de MEK Active ES2684517T3 (es)

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IN288KO2012 2012-03-14
PCT/IB2013/051908 WO2013136249A1 (en) 2012-03-14 2013-03-11 Heterocyclyl compounds as mek inhibitors

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MX355474B (es) * 2012-03-14 2018-04-16 Lupin Ltd Compuestos de heterociclilo como inhibidores de mek.
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US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
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RU2667892C2 (ru) * 2013-10-25 2018-09-25 Шанхай Хэнжуй Фармасьютикал Ко., Лтд. Производные пиридилкетона, способ их получения и их фармацевтическое применение
WO2016009306A1 (en) * 2014-07-15 2016-01-21 Lupin Limited Heterocyclyl compounds as mek inhibitors
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