AR089568A1 - Compuestos heterociclicos y sus metodos de usos - Google Patents

Compuestos heterociclicos y sus metodos de usos

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Publication number
AR089568A1
AR089568A1 ARP120103819A ARP120103819A AR089568A1 AR 089568 A1 AR089568 A1 AR 089568A1 AR P120103819 A ARP120103819 A AR P120103819A AR P120103819 A ARP120103819 A AR P120103819A AR 089568 A1 AR089568 A1 AR 089568A1
Authority
AR
Argentina
Prior art keywords
heteroaryl
alkyl
hydrogen
heterocyclyl
haloalkyl
Prior art date
Application number
ARP120103819A
Other languages
English (en)
Original Assignee
Ambit Biosciences Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ambit Biosciences Corp filed Critical Ambit Biosciences Corp
Publication of AR089568A1 publication Critical patent/AR089568A1/es

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    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/423—Oxazoles condensed with carbocyclic rings
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    • A61K31/425—Thiazoles
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/04—Ortho-condensed systems

Abstract

Se proporcionan en la presente compuestos heterocíclicos para el tratamiento de enfermedades mediadas por CSF1R, FLT3, KIT y/o PDGFRb quinasa. También se proporcionan composiciones farmacéuticas que comprenden los compuestos y métodos de uso de los compuestos y las composiciones. Reivindicación 1: Un compuesto que tiene la fórmula (1), R¹ y R² están seleccionados cada uno, de modo independiente, de hidrógeno, deuterio, halógeno, hidroxilo y alcoxi o R¹ y R² forman juntos =O; R³ es hidrógeno o alquilo; R⁴ es cicloalquilo, cicloalquenilo, arilo, heterociclilo o heteroarilo, donde R⁴ está opcionalmente sustituido con uno o varios, en una forma de realización, uno a tres, en otra forma de realización, uno, dos o tres grupos seleccionados de Q¹; cada Q¹ es, de modo independiente, deuterio, halo, ciano, oxo, tioxo, alquilo, haloalquilo, 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, haloalquilo, aminoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo y heterociclilo están opcionalmente sustituidos con uno o varios grupos Q³, en una forma de realización, uno a tres grupos Q³; cada Q³ está seleccionado, de modo independiente, de deuterio, halo, hidroxilo, alquilo, haloalquilo e hidroxialquilo; Y es -(CR⁵R⁶)q-; R⁵ y R⁶ son cada uno, de modo independiente, hidrógeno, deuterio, halo, alquilo, haloalquilo o hidroxialquilo; Z es O, S o NR⁷; R⁷ es hidrógeno, deuterio o alquilo; cada W es, de modo independiente, CR⁸ o N; R⁸ es hidrógeno, deuterio, halo, haloalquilo o alquilo; el anillo A es un arilo monocíclico, bicíclico o tricíclico, heteroarilo o heterociclilo opcionalmente sustituido con uno a cuatro sustituyentes seleccionados de Q²; W¹ es N o C; W² es N, NR⁹ᵃ o CR⁹ᵇ; W³ es N, NR¹⁰ᵃ o CR¹⁰ᵇ; W⁴ es N, NR¹¹ᵃ o CR¹¹ᵇ; R⁹ᵃ, R⁹ᵇ, R¹⁰ᵃ, R¹⁰ᵇ, R¹¹ᵃ y R¹¹ᵇ están seleccionados de la siguiente manera: i) R⁹ᵃ, R¹⁰ᵃ y R¹¹ᵃ son cada uno, de modo independiente, hidrógeno, deuterio o alquilo y R⁹ᵇ, R¹⁰ᵇ y R¹¹ᵇ son cada uno, de modo independiente, hidrógeno o Q²; o ii) R⁹ᵃ y R¹⁰ᵇ, R⁹ᵇ y R¹⁰ᵇ, R⁹ᵇ y R¹⁰ᵃ, R¹⁰ᵇ y R¹¹ᵃ, R¹⁰ᵃ y R¹¹ᵇ o R¹⁰ᵇ y R¹¹ᵇ junto con los átomos a los que están unidos, forman un arilo, heteroarilo o anillo heterociclilo, opcionalmente sustituido con uno o varios, en una forma de realización, uno a tres, en otra forma de realización, uno, dos o tres grupos seleccionados de Q²; y el resto de R⁹ᵃ o R¹¹ᵃ es hidrógeno, deuterio o alquilo; y el resto de R⁹ᵇ o R¹¹ᵇ es hidrógeno o Q²; o iii) R⁹ᵃ y R¹⁰ᵇ, R⁹ᵇ y R¹⁰ᵇ, R⁹ᵇ y R¹⁰ᵃ, R¹⁰ᵇ y R¹¹ᵃ, R¹⁰ᵃ y R¹¹ᵇ o R¹⁰ᵇ y R¹¹ᵇ junto con los átomos a los que están unidos, forman un arilo, heteroarilo o anillo heterociclilo opcionalmente fusionado a un anillo fenilo opcionalmente sustituido con uno o varios, en una forma de realización, uno a tres, en otra forma de realización, uno, dos o tres grupos seleccionados de Q²; y el resto de R⁹ᵃ o R¹¹ᵃ es hidrógeno o alquilo y el resto de R⁹ᵇ o R¹¹ᵇ es hidrógeno o Q²; cada Q² es, de modo independiente, halo, deuterio, ciano, oxo, tioxo, alquilo, haloalquilo, haloalquenilo, 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, haloalquilo, aminoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo y heterociclilo están opcionalmente sustituidos con uno o varios grupos Q⁴; en una forma de realización, uno a tres grupos Q⁴, cada Q⁴ está seleccionado, de modo independiente, de halo, deuterio, hidroxilo, alquilo, haloalquilo e hidroxialquilo; Rᵈ es hidrógeno o alquilo; cada Rᵘ es, de modo independiente, alquileno, alquenileno o un enlace directo; Rʷ es alquilo, haloalquilo, hidroxialquilo, alcoxialquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, cicloalquenilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo; cada Rˣ es, de modo independiente, hidrógeno, alquilo, haloalquilo, hidroxialquilo, alcoxialquilo, cianoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, cicloalquenilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo; Rʸ y Rᶻ están seleccionados cada uno, de modo independiente, de (i) ó (ii) siguiente: (i) Rʸ y Rᶻ son cada uno, de modo independiente, hidrógeno, alquilo, haloalquilo, 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 varios, en una forma de realización, uno, dos o tres grupos Q⁷; cada Q⁷ está seleccionado, de modo independiente, de halo, deuterio, oxo, tioxo, hidroxi, alcoxi, alquilo, haloalquilo, hidroxialquilo, aminoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, cicloalquenilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, heterociclilo y heterociclilalquilo; J es O, NRˣ o S; cada t es, de modo independiente, un número entero de 0 - 2; n es 1 ó 2; y; q es un número entero de 0 - 4; en donde los compuestos están seleccionados de modo tal que: i) cuando W es CH; W¹ es C; Z es S; R¹ es hidrógeno o hidroxilo y R² es hidrógeno o R¹ y R² forman juntos =O; entonces el anillo A no sea piridina; ii) cuando W es CH; W¹ es N; Z es S; R¹ y R² son hidrógeno, entonces el anillo A no sea pirrolidina; iii) cuando W es CH, Z es NH, R¹ y R² forman juntos =O, q es 0 y R⁴ es piridinilo, entonces el anillo A no sea fenilo, iv) cuando W es CH, Z es NH, R¹ y R² forman juntos =O, q es 0 y R⁴ es fenilo, entonces el anillo A no sea pirrolidina y v) cuando Z es N, uno de R¹ y R² es metilo y el otro de R¹ y R² es H, q es 0 y R³ es piridina y W¹ es N, el anillo A no pueda ser piperidina, 1,2,3,4-tetrahidroisoquinolina o isoindolina.
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